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Erectomed
Tadalafil
Erectomed
Tadalafil
Indications
Pulmonary arterial hypertension
Indication detailsView
Tadalafil is indicated in-
- Erectile Dysfunction (ED)
- Benign Prostatic Hyperplasia (BPH)
- Both Erectile Dysfunction and signs and symptoms of Benign Prostatic Hyperplasia
Therapeutic classView
Drugs for Erectile Dysfunction
PharmacologyView
Tadalafil is a selective phosphodiesterase type 5 (PDE5) inhibitor. Inhibition of PDE5 increases cGMP in smooth muscle cells. cGMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum, causing penile erection. PDE5 also is present in smooth muscles of the prostate and bladder wall. Inhibiting PDE5 increases cGMP concentrations leading to relaxation of smooth muscle in the prostate and bladder. Smooth muscle relaxation may improve blood flow to the urinary tract and widen the opening of the bladder neck, resulting in improved voiding.
DosageView
Erectile Dysfunction: For most patients the recommended starting dose is 10 mg. The dose may be increased to 20 mg or decreased to 5 mg based on requirement. The maximum dosing frequency is once daily. Tadalafil is effective for up to 36 hours.
Benign prostatic hyperplasia: The recommended dose is 5 mg taken at the same time every day.
Combined Erectile Dysfunction and Benign prostatic hyperplasia: The recommended dose is 5 mg at the same time every day.
Side effectsView
Headache, Dyspepsia, Back pain, Myalgia, Nasal pharyngitis, Nasal congestion are common side effects. Change in Color Vision, Sudden vision loss, Hearing loss, Stevens-Johnson Syndrome, Exfoliative dermatitis, Angina, Stroke, Myocardial infarction, Severe hypotension, Tachycardia may also occur rarely.
ContraindicationsView
- Use of Nitrates (for example, Nitroglycerine, Isosorbide): may increase hypotensive effects of Nitrates
- Hypersensitivity reactions to Tadalafil
PrecautionsView
Angina, renal impairment, hepatic impairment, bleeding concomitant with Nitrates, Alpha Blockers, Alcohol, CYP3A4 Inhibitors (for example, Ritonavir, Ketoconazole, Itraconazole), other PDE5 inhibitors precaution should be taken in all these conditions.
InteractionsView
May interact with Nitrates for example, Isosorbide, Nitroglycerin, Alpha adrenergic blockers, Antihypertensives, Alcohol, Antacids (magnesuim hydroxide/aluminum hydroxide), Ketoconazole, Ritonavir, Erythromycin, Itraconazole, Grapefruit juice, other HIV protease inhibitors, Rifampin, Carbamazepine, Phenytoin & Phenobarbital.
Pregnancy & lactationView
Tadalafil has been assigned to pregnancy category B by the USFDA. Tadalafil is only recommended for use during pregnancy when benefit outweighs risk. There are no data on the excretion of Tadalafil in human milk. Caution should be used when administering tadalafil to nursing women.
StorageView
Keep in a dry place, away from light and heat. Keep out of the reach of children.
Erectomed
Tadalafil
Erectomed
Tadalafil
Indications
Pulmonary arterial hypertension
Indication detailsView
Tadalafil is indicated in-
- Erectile Dysfunction (ED)
- Benign Prostatic Hyperplasia (BPH)
- Both Erectile Dysfunction and signs and symptoms of Benign Prostatic Hyperplasia
Therapeutic classView
Drugs for Erectile Dysfunction
PharmacologyView
Tadalafil is a selective phosphodiesterase type 5 (PDE5) inhibitor. Inhibition of PDE5 increases cGMP in smooth muscle cells. cGMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum, causing penile erection. PDE5 also is present in smooth muscles of the prostate and bladder wall. Inhibiting PDE5 increases cGMP concentrations leading to relaxation of smooth muscle in the prostate and bladder. Smooth muscle relaxation may improve blood flow to the urinary tract and widen the opening of the bladder neck, resulting in improved voiding.
DosageView
Erectile Dysfunction: For most patients the recommended starting dose is 10 mg. The dose may be increased to 20 mg or decreased to 5 mg based on requirement. The maximum dosing frequency is once daily. Tadalafil is effective for up to 36 hours.
Benign prostatic hyperplasia: The recommended dose is 5 mg taken at the same time every day.
Combined Erectile Dysfunction and Benign prostatic hyperplasia: The recommended dose is 5 mg at the same time every day.
Side effectsView
Headache, Dyspepsia, Back pain, Myalgia, Nasal pharyngitis, Nasal congestion are common side effects. Change in Color Vision, Sudden vision loss, Hearing loss, Stevens-Johnson Syndrome, Exfoliative dermatitis, Angina, Stroke, Myocardial infarction, Severe hypotension, Tachycardia may also occur rarely.
ContraindicationsView
- Use of Nitrates (for example, Nitroglycerine, Isosorbide): may increase hypotensive effects of Nitrates
- Hypersensitivity reactions to Tadalafil
PrecautionsView
Angina, renal impairment, hepatic impairment, bleeding concomitant with Nitrates, Alpha Blockers, Alcohol, CYP3A4 Inhibitors (for example, Ritonavir, Ketoconazole, Itraconazole), other PDE5 inhibitors precaution should be taken in all these conditions.
InteractionsView
May interact with Nitrates for example, Isosorbide, Nitroglycerin, Alpha adrenergic blockers, Antihypertensives, Alcohol, Antacids (magnesuim hydroxide/aluminum hydroxide), Ketoconazole, Ritonavir, Erythromycin, Itraconazole, Grapefruit juice, other HIV protease inhibitors, Rifampin, Carbamazepine, Phenytoin & Phenobarbital.
Pregnancy & lactationView
Tadalafil has been assigned to pregnancy category B by the USFDA. Tadalafil is only recommended for use during pregnancy when benefit outweighs risk. There are no data on the excretion of Tadalafil in human milk. Caution should be used when administering tadalafil to nursing women.
StorageView
Keep in a dry place, away from light and heat. Keep out of the reach of children.
Erectus
Tadalafil
Erectus
Tadalafil
Indications
Pulmonary arterial hypertension
Indication detailsView
Tadalafil is indicated in-
- Erectile Dysfunction (ED)
- Benign Prostatic Hyperplasia (BPH)
- Both Erectile Dysfunction and signs and symptoms of Benign Prostatic Hyperplasia
Therapeutic classView
Drugs for Erectile Dysfunction
PharmacologyView
Tadalafil is a selective phosphodiesterase type 5 (PDE5) inhibitor. Inhibition of PDE5 increases cGMP in smooth muscle cells. cGMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum, causing penile erection. PDE5 also is present in smooth muscles of the prostate and bladder wall. Inhibiting PDE5 increases cGMP concentrations leading to relaxation of smooth muscle in the prostate and bladder. Smooth muscle relaxation may improve blood flow to the urinary tract and widen the opening of the bladder neck, resulting in improved voiding.
DosageView
Erectile Dysfunction: For most patients the recommended starting dose is 10 mg. The dose may be increased to 20 mg or decreased to 5 mg based on requirement. The maximum dosing frequency is once daily. Tadalafil is effective for up to 36 hours.
Benign prostatic hyperplasia: The recommended dose is 5 mg taken at the same time every day.
Combined Erectile Dysfunction and Benign prostatic hyperplasia: The recommended dose is 5 mg at the same time every day.
Side effectsView
Headache, Dyspepsia, Back pain, Myalgia, Nasal pharyngitis, Nasal congestion are common side effects. Change in Color Vision, Sudden vision loss, Hearing loss, Stevens-Johnson Syndrome, Exfoliative dermatitis, Angina, Stroke, Myocardial infarction, Severe hypotension, Tachycardia may also occur rarely.
ContraindicationsView
- Use of Nitrates (for example, Nitroglycerine, Isosorbide): may increase hypotensive effects of Nitrates
- Hypersensitivity reactions to Tadalafil
PrecautionsView
Angina, renal impairment, hepatic impairment, bleeding concomitant with Nitrates, Alpha Blockers, Alcohol, CYP3A4 Inhibitors (for example, Ritonavir, Ketoconazole, Itraconazole), other PDE5 inhibitors precaution should be taken in all these conditions.
InteractionsView
May interact with Nitrates for example, Isosorbide, Nitroglycerin, Alpha adrenergic blockers, Antihypertensives, Alcohol, Antacids (magnesuim hydroxide/aluminum hydroxide), Ketoconazole, Ritonavir, Erythromycin, Itraconazole, Grapefruit juice, other HIV protease inhibitors, Rifampin, Carbamazepine, Phenytoin & Phenobarbital.
Pregnancy & lactationView
Tadalafil has been assigned to pregnancy category B by the USFDA. Tadalafil is only recommended for use during pregnancy when benefit outweighs risk. There are no data on the excretion of Tadalafil in human milk. Caution should be used when administering tadalafil to nursing women.
StorageView
Keep in a dry place, away from light and heat. Keep out of the reach of children.
Erectus
Tadalafil
Erectus
Tadalafil
Indications
Pulmonary arterial hypertension
Indication detailsView
Tadalafil is indicated in-
- Erectile Dysfunction (ED)
- Benign Prostatic Hyperplasia (BPH)
- Both Erectile Dysfunction and signs and symptoms of Benign Prostatic Hyperplasia
Therapeutic classView
Drugs for Erectile Dysfunction
PharmacologyView
Tadalafil is a selective phosphodiesterase type 5 (PDE5) inhibitor. Inhibition of PDE5 increases cGMP in smooth muscle cells. cGMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum, causing penile erection. PDE5 also is present in smooth muscles of the prostate and bladder wall. Inhibiting PDE5 increases cGMP concentrations leading to relaxation of smooth muscle in the prostate and bladder. Smooth muscle relaxation may improve blood flow to the urinary tract and widen the opening of the bladder neck, resulting in improved voiding.
DosageView
Erectile Dysfunction: For most patients the recommended starting dose is 10 mg. The dose may be increased to 20 mg or decreased to 5 mg based on requirement. The maximum dosing frequency is once daily. Tadalafil is effective for up to 36 hours.
Benign prostatic hyperplasia: The recommended dose is 5 mg taken at the same time every day.
Combined Erectile Dysfunction and Benign prostatic hyperplasia: The recommended dose is 5 mg at the same time every day.
Side effectsView
Headache, Dyspepsia, Back pain, Myalgia, Nasal pharyngitis, Nasal congestion are common side effects. Change in Color Vision, Sudden vision loss, Hearing loss, Stevens-Johnson Syndrome, Exfoliative dermatitis, Angina, Stroke, Myocardial infarction, Severe hypotension, Tachycardia may also occur rarely.
ContraindicationsView
- Use of Nitrates (for example, Nitroglycerine, Isosorbide): may increase hypotensive effects of Nitrates
- Hypersensitivity reactions to Tadalafil
PrecautionsView
Angina, renal impairment, hepatic impairment, bleeding concomitant with Nitrates, Alpha Blockers, Alcohol, CYP3A4 Inhibitors (for example, Ritonavir, Ketoconazole, Itraconazole), other PDE5 inhibitors precaution should be taken in all these conditions.
InteractionsView
May interact with Nitrates for example, Isosorbide, Nitroglycerin, Alpha adrenergic blockers, Antihypertensives, Alcohol, Antacids (magnesuim hydroxide/aluminum hydroxide), Ketoconazole, Ritonavir, Erythromycin, Itraconazole, Grapefruit juice, other HIV protease inhibitors, Rifampin, Carbamazepine, Phenytoin & Phenobarbital.
Pregnancy & lactationView
Tadalafil has been assigned to pregnancy category B by the USFDA. Tadalafil is only recommended for use during pregnancy when benefit outweighs risk. There are no data on the excretion of Tadalafil in human milk. Caution should be used when administering tadalafil to nursing women.
StorageView
Keep in a dry place, away from light and heat. Keep out of the reach of children.
Eredex
Yohimbine Hydrochloride
Eredex
Yohimbine Hydrochloride
Indications
Libido
Indication detailsView
Yohimbine is indicated in erectile dysfunction, loss of libido & exhaustion.
Therapeutic classView
Herbal and Nutraceuticals
PharmacologyView
Yohimbe is a potent alpha-2 adrenoceptor blocker and a weak alpha-1 adrenergic antagonist with some antidopaminergic properties. Yohimbe interacts with adrenoceptors that are selectively stimulated by clonidine, alpha-methylnorepinephrine, tramazoline, guanabenz & guanfacin. It also interacts with compounds that are nonselectively stimulated by norepinephrine and epinephrine. Yohimbe has a modest beneficial effect in the management of erectile dysfunction. Because of the alpha-2 adrenergic blockade, the drug is an effective treatment for sexual disorders such as decreased libido and decreased sexual response, caused by selective serotonin reuptake inhibitors.
DosageView
1 capsule 3 times daily or as advised by the physician
Side effectsView
Anxiety states, elevated blood pressure, exanthema, nausea, insomnia, tachycardia, tremor, mania and vomiting.
ContraindicationsView
The drug should not be used by patients with liver and kidney diseases, chronic inflammation of the sexual organs or prostate gland or with a history of gastric or duodenal ulcers
PrecautionsView
Patients taking Yohimbe should avoid alcohol ingestion
InteractionsView
Theoretically, Yohimbe may counteract the hypotensive effect of antihypertensive medications, resulting inadequate blood pressure control. It may potentiate pharmaceutical MAO-inhibitors
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Erian
Cinchocaine + Hydrocortisone + Framycetin + Esculin
Erian
Cinchocaine + Hydrocortisone + Framycetin + Esculin
Indications
Pruritus ani
Indication detailsView
This is indicated for the treatment of-
- Internal and external haemorrhoids
- Haemorrhoids post-partum
- Anal pruritus, peri-anal eczema, anal fissures and proctitis
- Post-haemorrhoidectomy application to relieve pain and discomfort
Therapeutic classView
Compound steroidal preparations, Drugs used in Ano-rectal region
PharmacologyView
The local anaesthetic Cinchocaine Hydrochloride prevents or relieves the severe pain sometimes encountered in strangulated haemorrhoids, fissures and perianal haematomata, whilst the corticosteroid (Hydrocortisone) acts as a decongestant, anti-inflammatory and anti-pruritic agent and by so doing eliminates itching, inflammation and mucous discharge. The broad spectrum antibiotic, Framycetin Sulphate, will eradicate most infections which may already be present or arise in lesions of the anorectal area and Esculin has a skin protective action.
DosageView
Ointment: Apply the ointment in a small quantity with the finger, on the painful or pruritic area, morning and evening and after each stool. For deep application, insert the cannula or applicator to full extent and squeeze tube gently from lower end whilst withdrawing.
Suppository: A suppository is inserted morning and evening, and after each stool.
Suppository: A suppository is inserted morning and evening, and after each stool.
Side effectsView
Long-term continuous treatment with topical corticosteroids should be avoided as far as possible as this may cause atrophic changes in the skin leading to thinning, loss of elasticity, dilatation of superficial blood vessels, telangiectasia and ecchymoses. These changes are particularly likely to occur when occlusive dressings are used. Systemic absorption of topically applied corticosteroids may occur, particularly under the following conditions: when large quantities are used or when application is made to wide areas of the body, or to damaged skin; when potent topical corticosteroids are used, and when the occlusive dressing technique is applied. Depression of the hypothalamic-pituitary-adrenal axis with consequent suppression of the adrenal gland may occur. These effects are most likely to be severe in children. Growth may be retarded and a Cushingoid state may be produced. Benign intracranial hypertension has been rarely reported.
ContraindicationsView
Known hypersensitivity to any of the four ingredients. Corticosteroids have been shown to be teratogenic in animals following dermal application. As these agents are absorbed percutaneously, teratogenicity following topical application cannot be excluded. Therefore this product should not be used during pregnancy. Topical corticosteroid preparations are contraindicated in the treatment of herpes simplex, vaccinia or varicella, or tuberculous infection of the anal region.
PrecautionsView
Discontinue use if sensitization occurs. Other specific measures against infections, allergy, and other causal factors must not be neglected. The possibility, however rare, that prolonged use of this preparation might produce systemic corticosteroid effects, should be borne in mind. Patients should be advised to inform subsequent physicians of the previous use of hydrocortisone.
Pregnancy & lactationView
The safe use of topical corticosteroids during pregnancy has not been fully established. Therefore, during pregnancy, they should not be used unnecessarily on extended areas, in large amounts or for prolonged periods of time.
Pediatric usageView
Not recommended for use in children.
StorageView
Store at a cool and dry place, protected from light. Store below 25° C. Do not freeze.
Erian
Cinchocaine + Hydrocortisone + Framycetin + Esculin
Erian
Cinchocaine + Hydrocortisone + Framycetin + Esculin
Indications
Pruritus ani
Indication detailsView
This is indicated for the treatment of-
- Internal and external haemorrhoids
- Haemorrhoids post-partum
- Anal pruritus, peri-anal eczema, anal fissures and proctitis
- Post-haemorrhoidectomy application to relieve pain and discomfort
Therapeutic classView
Compound steroidal preparations, Drugs used in Ano-rectal region
PharmacologyView
The local anaesthetic Cinchocaine Hydrochloride prevents or relieves the severe pain sometimes encountered in strangulated haemorrhoids, fissures and perianal haematomata, whilst the corticosteroid (Hydrocortisone) acts as a decongestant, anti-inflammatory and anti-pruritic agent and by so doing eliminates itching, inflammation and mucous discharge. The broad spectrum antibiotic, Framycetin Sulphate, will eradicate most infections which may already be present or arise in lesions of the anorectal area and Esculin has a skin protective action.
DosageView
Ointment: Apply the ointment in a small quantity with the finger, on the painful or pruritic area, morning and evening and after each stool. For deep application, insert the cannula or applicator to full extent and squeeze tube gently from lower end whilst withdrawing.
Suppository: A suppository is inserted morning and evening, and after each stool.
Suppository: A suppository is inserted morning and evening, and after each stool.
Side effectsView
Long-term continuous treatment with topical corticosteroids should be avoided as far as possible as this may cause atrophic changes in the skin leading to thinning, loss of elasticity, dilatation of superficial blood vessels, telangiectasia and ecchymoses. These changes are particularly likely to occur when occlusive dressings are used. Systemic absorption of topically applied corticosteroids may occur, particularly under the following conditions: when large quantities are used or when application is made to wide areas of the body, or to damaged skin; when potent topical corticosteroids are used, and when the occlusive dressing technique is applied. Depression of the hypothalamic-pituitary-adrenal axis with consequent suppression of the adrenal gland may occur. These effects are most likely to be severe in children. Growth may be retarded and a Cushingoid state may be produced. Benign intracranial hypertension has been rarely reported.
ContraindicationsView
Known hypersensitivity to any of the four ingredients. Corticosteroids have been shown to be teratogenic in animals following dermal application. As these agents are absorbed percutaneously, teratogenicity following topical application cannot be excluded. Therefore this product should not be used during pregnancy. Topical corticosteroid preparations are contraindicated in the treatment of herpes simplex, vaccinia or varicella, or tuberculous infection of the anal region.
PrecautionsView
Discontinue use if sensitization occurs. Other specific measures against infections, allergy, and other causal factors must not be neglected. The possibility, however rare, that prolonged use of this preparation might produce systemic corticosteroid effects, should be borne in mind. Patients should be advised to inform subsequent physicians of the previous use of hydrocortisone.
Pregnancy & lactationView
The safe use of topical corticosteroids during pregnancy has not been fully established. Therefore, during pregnancy, they should not be used unnecessarily on extended areas, in large amounts or for prolonged periods of time.
Pediatric usageView
Not recommended for use in children.
StorageView
Store at a cool and dry place, protected from light. Store below 25° C. Do not freeze.
Eridon
Domperidone Maleate
Eridon
Domperidone Maleate
Indications
Vomiting
Indication detailsView
Dyspeptic symptom complex, often associated with delayed gastric emptying, gastroesophageal reflux and esophagitis:
Parkinson's disease: In dopamine-agonist induced nausea and vomiting.
Radiological studies: Speeding barium transit in follow-through radiological studies.
- Epigastric sense of fullness, feeling of abdominal distension, upper abdominal pain
- Eructation, flatulence, early satiety
- Nausea and vomiting
- Heartburn with or without regurgitations of gastric contents in the mouth
- Non-ulcer dyspepsia
Parkinson's disease: In dopamine-agonist induced nausea and vomiting.
Radiological studies: Speeding barium transit in follow-through radiological studies.
Therapeutic classView
Motility Stimulants, Motility stimulants/Dopamine antagonist, Prokinetic drugs
PharmacologyView
Domperidone is a dopamine antagonist that principally blocks the dopamine receptors located in the ChemoreceptorTrigger Zone (CTZ) and stomach. Its gastroprokinetic action is based on its blocking effect of dopamine receptors that have an influence on the motility of the gastrointestinal tract. Due to its weak penetration across the blood-brain barrier, Domperidone has almost no effect on the dopaminergic receptors in the brain, therefore, excluding psychotropic and neurologic side effects. Domperidone restores normal motility and tone of the upper gastrointestinal tract, facilitates gastric emptying, enhances antral and duodenal peristalsis and regulates contraction of the pylorus. Domperidone also increases esophageal peristalsis and lower esophageal sphincter pressure, and thus prevents regurgitation of gastric content.
DosageView
Domperidone should be taken 15-30 minutes before meals and, if necessary, before retiring.
The usual recommended oral dose of Domperidone is as follows:
The usual recommended oral dose of Domperidone is as follows:
- Adults: 10-20 mg (1-2 tablet or 10-20 ml suspension), every 6-8 hours daily. The maximum dose of Domperidone is 80 mg daily.
- Children: 2-4 ml suspension/10 kg body weight or 0.4-0.8 ml paediatric drops/10 kg body weight, every 6-8 hours daily.
- Adults: 10-20 mg (1-2 tablet or 10-20 ml suspension), every 6-8 hours daily.
- Children: 0.2-0.4 mg/kg (2-4 ml suspension/10 kg or 0.4-0.8 ml paediatric drops/10 kg) body weight, every 6-8 hours daily.
- Adults: 20 mg (2 tablets or 20 ml suspension), every 6-8 hours daily
- Children: 0.2-0.4 mg/kg (2-4 ml suspension/10 kg or 0.4-0.8 ml paediatric drops/10 kg) body weight, every 6-8 hours daily. (In acute nausea and vomiting maximum period of treatment is 12 weeks).
- Adults (including elderly): 30-60 mg every 4-8 hours.
- Children: The maximum daily dose rectally in children's is 30 mg for those weighting 10 to 25 kg. The dose may be divided throughout day if necessary.
- The maximum period of treatment is 12 weeks.
Side effectsView
Domperidone may produce hyperprolactinemia (1.3%).This may result in galactorrhea, breast enlargement, and soreness and reduced libido. Dry mouth (1%), thirst, headache (1.2%), nervousness, drowsiness (0.4%), diarrhea (0.2%), skin rash and itching (0.1%) may occur during treatment with domperidone. Extra-pyramidal reactions are seen in 0.05% of patients in clinical studies.
ContraindicationsView
Domperidone is contraindicated to patients having known hypersensitivity to this drug and in the case of neonates. Domperidone should not be used whenever gastrointestinal stimulation might be dangerous i.e., gastrointestinal hemorrhage, mechanical obstruction or perforation. Also contraindicated in patients with prolactin releasing pituitary tumor (prolactinoma).
PrecautionsView
Domperidone should be used with absolute caution in the case of children because there may be an increased risk of extra-pyramidal reactions in young children because of an incompletely developed blood-brain barrier. Since domperidone is highly metabolized in liver, it should be used with caution in patient with hepatic impairment.
InteractionsView
Domperidone may reduce the risk of hypoprolactemic effect of bromocriptine. The action of Domperidone on Gl function may be antagonized by antimuscarinics and opoid analgesics. Care should be exercised when domperidone is administered in combination with MAO (monoamine oxidase) inhibitors.
Pregnancy & lactationView
The safety of domperidone has not been proven and it is therefore not recommended during pregnancy. Animal studies have not demonstrated the teratogenic effect in the fetus. Domperidone may precipitate galactorrhea and improve post-natal lactation. It is secreted in breast milk but in very small quantities insufficient to be considered harmful.
Overdose effectsView
There are no reported cases of overdose.
StorageView
Store below 30°C, Protected from light & moisture. Keep out of children's reach.
Eridon
Domperidone Maleate
Eridon
Domperidone Maleate
Indications
Vomiting
Indication detailsView
Dyspeptic symptom complex, often associated with delayed gastric emptying, gastroesophageal reflux and esophagitis:
Parkinson's disease: In dopamine-agonist induced nausea and vomiting.
Radiological studies: Speeding barium transit in follow-through radiological studies.
- Epigastric sense of fullness, feeling of abdominal distension, upper abdominal pain
- Eructation, flatulence, early satiety
- Nausea and vomiting
- Heartburn with or without regurgitations of gastric contents in the mouth
- Non-ulcer dyspepsia
Parkinson's disease: In dopamine-agonist induced nausea and vomiting.
Radiological studies: Speeding barium transit in follow-through radiological studies.
Therapeutic classView
Motility Stimulants, Motility stimulants/Dopamine antagonist, Prokinetic drugs
PharmacologyView
Domperidone is a dopamine antagonist that principally blocks the dopamine receptors located in the ChemoreceptorTrigger Zone (CTZ) and stomach. Its gastroprokinetic action is based on its blocking effect of dopamine receptors that have an influence on the motility of the gastrointestinal tract. Due to its weak penetration across the blood-brain barrier, Domperidone has almost no effect on the dopaminergic receptors in the brain, therefore, excluding psychotropic and neurologic side effects. Domperidone restores normal motility and tone of the upper gastrointestinal tract, facilitates gastric emptying, enhances antral and duodenal peristalsis and regulates contraction of the pylorus. Domperidone also increases esophageal peristalsis and lower esophageal sphincter pressure, and thus prevents regurgitation of gastric content.
DosageView
Domperidone should be taken 15-30 minutes before meals and, if necessary, before retiring.
The usual recommended oral dose of Domperidone is as follows:
The usual recommended oral dose of Domperidone is as follows:
- Adults: 10-20 mg (1-2 tablet or 10-20 ml suspension), every 6-8 hours daily. The maximum dose of Domperidone is 80 mg daily.
- Children: 2-4 ml suspension/10 kg body weight or 0.4-0.8 ml paediatric drops/10 kg body weight, every 6-8 hours daily.
- Adults: 10-20 mg (1-2 tablet or 10-20 ml suspension), every 6-8 hours daily.
- Children: 0.2-0.4 mg/kg (2-4 ml suspension/10 kg or 0.4-0.8 ml paediatric drops/10 kg) body weight, every 6-8 hours daily.
- Adults: 20 mg (2 tablets or 20 ml suspension), every 6-8 hours daily
- Children: 0.2-0.4 mg/kg (2-4 ml suspension/10 kg or 0.4-0.8 ml paediatric drops/10 kg) body weight, every 6-8 hours daily. (In acute nausea and vomiting maximum period of treatment is 12 weeks).
- Adults (including elderly): 30-60 mg every 4-8 hours.
- Children: The maximum daily dose rectally in children's is 30 mg for those weighting 10 to 25 kg. The dose may be divided throughout day if necessary.
- The maximum period of treatment is 12 weeks.
Side effectsView
Domperidone may produce hyperprolactinemia (1.3%).This may result in galactorrhea, breast enlargement, and soreness and reduced libido. Dry mouth (1%), thirst, headache (1.2%), nervousness, drowsiness (0.4%), diarrhea (0.2%), skin rash and itching (0.1%) may occur during treatment with domperidone. Extra-pyramidal reactions are seen in 0.05% of patients in clinical studies.
ContraindicationsView
Domperidone is contraindicated to patients having known hypersensitivity to this drug and in the case of neonates. Domperidone should not be used whenever gastrointestinal stimulation might be dangerous i.e., gastrointestinal hemorrhage, mechanical obstruction or perforation. Also contraindicated in patients with prolactin releasing pituitary tumor (prolactinoma).
PrecautionsView
Domperidone should be used with absolute caution in the case of children because there may be an increased risk of extra-pyramidal reactions in young children because of an incompletely developed blood-brain barrier. Since domperidone is highly metabolized in liver, it should be used with caution in patient with hepatic impairment.
InteractionsView
Domperidone may reduce the risk of hypoprolactemic effect of bromocriptine. The action of Domperidone on Gl function may be antagonized by antimuscarinics and opoid analgesics. Care should be exercised when domperidone is administered in combination with MAO (monoamine oxidase) inhibitors.
Pregnancy & lactationView
The safety of domperidone has not been proven and it is therefore not recommended during pregnancy. Animal studies have not demonstrated the teratogenic effect in the fetus. Domperidone may precipitate galactorrhea and improve post-natal lactation. It is secreted in breast milk but in very small quantities insufficient to be considered harmful.
Overdose effectsView
There are no reported cases of overdose.
StorageView
Store below 30°C, Protected from light & moisture. Keep out of children's reach.
Erinlar
Ceritinib
Erinlar
Ceritinib
Indication detailsView
Ceritinib is indicated for the treatment of adult patients with metastatic non-small cell lung cancer (NSCLC) whose tumors are anaplastic lymphoma kinase (ALK)-positive as detected by an FDA-approved test.
PharmacologyView
Ceritinib is a kinase inhibitor. Targets of Ceritinib inhibition identified in either biochemical or cellular assays at clinically relevant concentrations include ALK, insulin- like growth factor 1 receptor (IGF-1R), insulin receptor (InsR), and ROS1. Among these, Ceritinib is most active against ALK. Ceritinib inhibited autophosphorylation of ALK, ALK-mediated phosphorylation of the downstream signaling protein STAT3, and proliferation of ALK dependent cancer cells in in vitro and in vivo assays.
Absorption: After a single oral administration of Ceritinib in patients, peak plasma levels (Cmax) of Ceritinib were achieved at approximately 4 to 6 hours, and AUC and C max increased dose proportionally over 50 to 750 mg under fasted conditions. The absolute bioavailability of Ceritinib has not been determined.
Distribution: Ceritinib is 97% bound to human plasma proteins, independent of drug concentration. The apparent volume of distribution is 4230 L following a single 750 mg fasted Ceritinib dose in patients. Ceritinib also has a slight preferential distribution to red blood cells, relative to plasma, with a mean in vitro blood-to-plasma ratio of 1.35.
Elimination: Following a single 750 mg fasted Ceritinib dose, the geometric mean apparent plasma terminal half life (t½) of Ceritinib was 41 hours in patients. Ceritinib demonstrates nonlinear PK over time. The geometric mean apparent clearance of Ceritinib was lower at steady-state (33.2 L/h) after 750 mg daily dosing than after a single 750 mg dose (88.5 L/h).
Metabolism: In vitro studies demonstrated that CYP3A was the major enzyme involved in the metabolic clearance of Ceritinib. Following oral administration of a single 750 mg radiolabeled Ceritinib dose under fasted conditions, Ceritinib as the parent compound was the main circulating component (82%) in human plasma.
Excretion: Following oral administration of a single 750 mg radiolabeled Ceritinib dose under fasted conditions, 92.3% of the administered dose was recovered in the feces (with 68% as unchanged parent compound) while 1.3% of the administered dose was recovered in the urine.
Absorption: After a single oral administration of Ceritinib in patients, peak plasma levels (Cmax) of Ceritinib were achieved at approximately 4 to 6 hours, and AUC and C max increased dose proportionally over 50 to 750 mg under fasted conditions. The absolute bioavailability of Ceritinib has not been determined.
Distribution: Ceritinib is 97% bound to human plasma proteins, independent of drug concentration. The apparent volume of distribution is 4230 L following a single 750 mg fasted Ceritinib dose in patients. Ceritinib also has a slight preferential distribution to red blood cells, relative to plasma, with a mean in vitro blood-to-plasma ratio of 1.35.
Elimination: Following a single 750 mg fasted Ceritinib dose, the geometric mean apparent plasma terminal half life (t½) of Ceritinib was 41 hours in patients. Ceritinib demonstrates nonlinear PK over time. The geometric mean apparent clearance of Ceritinib was lower at steady-state (33.2 L/h) after 750 mg daily dosing than after a single 750 mg dose (88.5 L/h).
Metabolism: In vitro studies demonstrated that CYP3A was the major enzyme involved in the metabolic clearance of Ceritinib. Following oral administration of a single 750 mg radiolabeled Ceritinib dose under fasted conditions, Ceritinib as the parent compound was the main circulating component (82%) in human plasma.
Excretion: Following oral administration of a single 750 mg radiolabeled Ceritinib dose under fasted conditions, 92.3% of the administered dose was recovered in the feces (with 68% as unchanged parent compound) while 1.3% of the administered dose was recovered in the urine.
DosageView
Patients should be selected for treatment of metastatic NSCLC with Ceritinib based on the presence of ALK positivity in tumor specimens. The recommended dose of Ceritinib is 450 mg orally once daily with food until disease progression or unacceptable toxicity. If a dose of Ceritinib is missed, that dose should be made up unless the next dose is due within 12 hours. If vomiting occurs during the course of treatment, an additional dose should not be administered and the next scheduled dose of Ceritinib should be continued. Or, as directed by the registered physician.
Side effectsView
- Gastrointestinal Adverse Reactions
- Hepatotoxicity
- Interstitial Lung Disease/Pneumonitis
- QT Interval Prolongation
- Hyperglycemia
- Bradycardia
- Pancreatitis
ContraindicationsView
It is contraindicated in patients with known hypersensitivity to Ceritinib or any other components of this product.
PrecautionsView
Gastrointestinal Adverse Reactions: Severe gastrointestinal toxicity occurred in patients treated with Ceritinib 750 mg under fasted conditions. Diarrhea, nausea, vomiting, or abdominal pain occurred in 95% of 925 patients, including severe cases (Grade 3 or 4) in 14% of patients treated with Ceritinib across clinical studies. Diarrhea, nausea, vomiting, or abdominal pain leading to dose interruptions or reductions occurred in 36% of patients and leading to treatment discontinuation occurred in 1.6% of patients. Patients should be monitored and managed using standards of care, including antidiarrheals, antiemetics, or fluid replacement, as indicated. Based on the severity of the adverse drug reaction, Ceritinib should be withheld with resumption at a reduced dose.
Hepatotoxicity: Drug-induced hepatotoxicity occurred in patients treated with Ceritinib. Elevations in alanine aminotransferase (ALT) greater than 5 times the upper limit of normal (ULN) occurred in 28% and elevations in aspartate aminotransferase (AST) greater than 5 times ULN occurred in 16% of 925 patients across clinical studies. Concurrent elevations in ALT greater than 3 times the ULN and total bilirubin greater than 2 times the ULN, with alkaline phosphatase less than 2 times the ULN occurred in 0.3% of patients across clinical studies. Approximately 1.0% of patients required permanent discontinuation due to hepatotoxicity. It should be monitor with liver laboratory tests including ALT, AST, and total bilirubin once a month and as clinically indicated, with more frequent testing in patients who develop transaminase elevations. Based on the severity of the adverse drug reaction, Ceritinib should be withheld with resumption at a reduced dose, or permanently discontinue Ceritinib.
Interstitial Lung Disease (ILD)/Pneumonitis: Severe, life-threatening, or fatal ILD/pneumonitis occurred in patients treated with Ceritinib. Across clinical studies, ILD/pneumonitis was reported in 2.4% of 925 patients treated with Ceritinib. National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) Grade 3 or 4 ILD/pneumonitis was reported in 1.3% of patients, with fatal events reported in 0.2% of patients. Ten patients (1.1%) discontinued Ceritinib across clinical studies due to ILD/pneumonitis. Patients should be monitored for pulmonary symptoms indicative of ILD/pneumonitis.
QT Interval Prolongation: QTc interval prolongation, which may lead to an increased risk for ventricular tachyarrhythmia (e.g., torsades de pointes) or sudden death, occurred in patients treated with Ceritinib. Across clinical studies, 6% of 919 patients with at least one post-baseline ECG assessment experienced a QTc interval increase over baseline of greater than 60 msec. Approximately 1.3% of patients taking Ceritinib 750 mg fasted were found to have a QTc greater than 500 msec. When possible, use of Ceritinib should be avoided in patients with congenital long QT syndrome. Periodic monitoring should be conducted with electrocardiograms (ECGs) and electrolytes in patients with congestive heart failure, bradyarrhythmias, electrolyte abnormalities, or those who are taking medications that are known to prolong the QTc interval.
Hyperglycemia: Hyperglycemia occurred in patients receiving Ceritinib. Across clinical studies, CTCAE Grade 3 or 4 hyperglycemia, based on laboratory values, occurred in 13% of 925 patients. Fasting serum glucose should be monitored prior to the start of Ceritinib treatment and periodically thereafter as clinically indicated. Based on the severity of the adverse drug reaction, Ceritinib should be withheld until hyperglycemia is adequately controlled, then resume Ceritinib at a reduced dose.
Bradycardia: Bradycardia occurred in patients receiving Ceritinib. Across clinical studies, sinus bradycardia, defined as a heart rate of less than 50 beats per minute (bpm), was noted as a new finding in 1% of 925 patients. Bradycardia was reported as an adverse drug reaction in 1% of patients. No patient required discontinuation and 0.1% required interruption with subsequent dose reduction for bradycardia. Using Ceritinib should be avoided in combination with other agents known to cause bradycardia (e.g., beta-blockers, nondihydropyridine calcium channel blockers, clonidine, and digoxin) to the extent possible. Heart rate and blood pressure should be regularly monitored. In cases of symptomatic bradycardia that is not life threatening, Ceritinib should be withheld until recovery to asymptomatic bradycardia or to a heart rate of 60 bpm or above, evaluate the use of concomitant medications, and adjust the dose of Ceritinib.
Pancreatitis: Pancreatitis occurred in patients receiving Ceritinib. Pancreatitis, including one fatality, occurred in less than 1% of patients receiving Ceritinib in clinical studies. CTCAE Grade 3 or 4 elevations of amylase occurred in 7% of patients receiving Ceritinib across clinical studies, while CTCAE Grade 3 or 4 elevations of lipase occurred in 14% of patients. Lipase and amylase should be monitored prior to the start of Ceritinib treatment and periodically thereafter as clinically indicated. Based on the severity of the laboratory abnormalities, Ceritinib should be withheld with resumption at a reduced dose.
Embryo-Fetal Toxicity: Based on its mechanism of action and findings in animal studies, Ceritinib can cause fetal harm when administered to a pregnant woman. Pregnant women should be advised of the potential risk to a fetus. Females of reproductive potential should be advised to use effective contraception during treatment with Ceritinib and for 6 months following completion of therapy. Based on the potential for genotoxicity, males with female partners of reproductive potential should be advised to use condoms during treatment with Ceritinib and for 3 months following completion of therapy.
Hepatotoxicity: Drug-induced hepatotoxicity occurred in patients treated with Ceritinib. Elevations in alanine aminotransferase (ALT) greater than 5 times the upper limit of normal (ULN) occurred in 28% and elevations in aspartate aminotransferase (AST) greater than 5 times ULN occurred in 16% of 925 patients across clinical studies. Concurrent elevations in ALT greater than 3 times the ULN and total bilirubin greater than 2 times the ULN, with alkaline phosphatase less than 2 times the ULN occurred in 0.3% of patients across clinical studies. Approximately 1.0% of patients required permanent discontinuation due to hepatotoxicity. It should be monitor with liver laboratory tests including ALT, AST, and total bilirubin once a month and as clinically indicated, with more frequent testing in patients who develop transaminase elevations. Based on the severity of the adverse drug reaction, Ceritinib should be withheld with resumption at a reduced dose, or permanently discontinue Ceritinib.
Interstitial Lung Disease (ILD)/Pneumonitis: Severe, life-threatening, or fatal ILD/pneumonitis occurred in patients treated with Ceritinib. Across clinical studies, ILD/pneumonitis was reported in 2.4% of 925 patients treated with Ceritinib. National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE) Grade 3 or 4 ILD/pneumonitis was reported in 1.3% of patients, with fatal events reported in 0.2% of patients. Ten patients (1.1%) discontinued Ceritinib across clinical studies due to ILD/pneumonitis. Patients should be monitored for pulmonary symptoms indicative of ILD/pneumonitis.
QT Interval Prolongation: QTc interval prolongation, which may lead to an increased risk for ventricular tachyarrhythmia (e.g., torsades de pointes) or sudden death, occurred in patients treated with Ceritinib. Across clinical studies, 6% of 919 patients with at least one post-baseline ECG assessment experienced a QTc interval increase over baseline of greater than 60 msec. Approximately 1.3% of patients taking Ceritinib 750 mg fasted were found to have a QTc greater than 500 msec. When possible, use of Ceritinib should be avoided in patients with congenital long QT syndrome. Periodic monitoring should be conducted with electrocardiograms (ECGs) and electrolytes in patients with congestive heart failure, bradyarrhythmias, electrolyte abnormalities, or those who are taking medications that are known to prolong the QTc interval.
Hyperglycemia: Hyperglycemia occurred in patients receiving Ceritinib. Across clinical studies, CTCAE Grade 3 or 4 hyperglycemia, based on laboratory values, occurred in 13% of 925 patients. Fasting serum glucose should be monitored prior to the start of Ceritinib treatment and periodically thereafter as clinically indicated. Based on the severity of the adverse drug reaction, Ceritinib should be withheld until hyperglycemia is adequately controlled, then resume Ceritinib at a reduced dose.
Bradycardia: Bradycardia occurred in patients receiving Ceritinib. Across clinical studies, sinus bradycardia, defined as a heart rate of less than 50 beats per minute (bpm), was noted as a new finding in 1% of 925 patients. Bradycardia was reported as an adverse drug reaction in 1% of patients. No patient required discontinuation and 0.1% required interruption with subsequent dose reduction for bradycardia. Using Ceritinib should be avoided in combination with other agents known to cause bradycardia (e.g., beta-blockers, nondihydropyridine calcium channel blockers, clonidine, and digoxin) to the extent possible. Heart rate and blood pressure should be regularly monitored. In cases of symptomatic bradycardia that is not life threatening, Ceritinib should be withheld until recovery to asymptomatic bradycardia or to a heart rate of 60 bpm or above, evaluate the use of concomitant medications, and adjust the dose of Ceritinib.
Pancreatitis: Pancreatitis occurred in patients receiving Ceritinib. Pancreatitis, including one fatality, occurred in less than 1% of patients receiving Ceritinib in clinical studies. CTCAE Grade 3 or 4 elevations of amylase occurred in 7% of patients receiving Ceritinib across clinical studies, while CTCAE Grade 3 or 4 elevations of lipase occurred in 14% of patients. Lipase and amylase should be monitored prior to the start of Ceritinib treatment and periodically thereafter as clinically indicated. Based on the severity of the laboratory abnormalities, Ceritinib should be withheld with resumption at a reduced dose.
Embryo-Fetal Toxicity: Based on its mechanism of action and findings in animal studies, Ceritinib can cause fetal harm when administered to a pregnant woman. Pregnant women should be advised of the potential risk to a fetus. Females of reproductive potential should be advised to use effective contraception during treatment with Ceritinib and for 6 months following completion of therapy. Based on the potential for genotoxicity, males with female partners of reproductive potential should be advised to use condoms during treatment with Ceritinib and for 3 months following completion of therapy.
InteractionsView
Effect of Other Drugs on Ceritinib: Strong CYP3A Inhibitors: A strong CYP3A4/P-gp inhibitor (ketoconazole) increased the systemic exposure of Ceritinib so it should be avoided. If concomitant use of strong CYP3A inhibitors including certain antivirals (e.g., ritonavir), macrolide antibiotics (e.g., telithromycin), antifungals (e.g., ketoconazole), and nefazodone is unavoidable, the Ceritinib dose should be reduced by approximately one third, rounded to the nearest multiple of the 150 mg dosage strength. After discontinuation of a strong CYP3A inhibitor, the Ceritinib dose should be resumed that was taken prior to initiating the strong CYP3A inhibitor. Grapefruit and grapefruit juice should not be consumed as they may inhibit CYP3A.
Strong CYP3A Inducers: A strong CYP3A4/P-gp inducer (Rifampin) decreased the systemic exposure of Ceritinib. Concurrent use of strong CYP3A inducers (e.g., Carbamazepine, Phenytoin, Rifampin, and St. John's Wort) should be avoided during treatment with Ceritinib.
Effect of Ceritinib on Other Drugs: CYP3A Substrates: Ceritinib increased the systemic exposure of a sensitive CYP3A substrate (Midazolam) so it should be avoided. If concomitant use is unavoidable, dose reduction of the sensitive CYP3A substrates should be considered. If Ceritinib is coadministered with other CYP3A substrates, it should be referred to the CYP3A substrate labeling for dosage recommendation with strong CYP3A inhibitors.
CYP2C9 Substrates: Ceritinib increased the systemic exposure of a CYP2C9 substrate (Warfarin). The frequency of INR monitoring should be increased if coadministration with warfarin is unavoidable as the anti-coagulant effect of Warfarin may be enhanced. Coadministration of Ceritinib should be avoided with CYP2C9 substrates for which minimal concentration changes may lead to serious toxicities. If concomitant use of such CYP2C9 substrates is unavoidable, dose reduction should be considered for the coadministered CYP2C9 substrates.
Strong CYP3A Inducers: A strong CYP3A4/P-gp inducer (Rifampin) decreased the systemic exposure of Ceritinib. Concurrent use of strong CYP3A inducers (e.g., Carbamazepine, Phenytoin, Rifampin, and St. John's Wort) should be avoided during treatment with Ceritinib.
Effect of Ceritinib on Other Drugs: CYP3A Substrates: Ceritinib increased the systemic exposure of a sensitive CYP3A substrate (Midazolam) so it should be avoided. If concomitant use is unavoidable, dose reduction of the sensitive CYP3A substrates should be considered. If Ceritinib is coadministered with other CYP3A substrates, it should be referred to the CYP3A substrate labeling for dosage recommendation with strong CYP3A inhibitors.
CYP2C9 Substrates: Ceritinib increased the systemic exposure of a CYP2C9 substrate (Warfarin). The frequency of INR monitoring should be increased if coadministration with warfarin is unavoidable as the anti-coagulant effect of Warfarin may be enhanced. Coadministration of Ceritinib should be avoided with CYP2C9 substrates for which minimal concentration changes may lead to serious toxicities. If concomitant use of such CYP2C9 substrates is unavoidable, dose reduction should be considered for the coadministered CYP2C9 substrates.
Pregnancy & lactationView
Ceritinib can cause fetal harm when administered to a pregnant woman. If it is used during pregnancy or if the patient becomes pregnant while taking it, the patient should be apprised of the potential hazard to the fetus. There are no data regarding the presence of Ceritinib or its metabolites in human milk, the effects of Ceritinib on the breastfed infant, or its effects on milk production. Because of the potential for serious adverse reactions including gastrointestinal adverse reactions, hepatotoxicity, pneumonitis, bradycardia and pancreatitis, a woman should be advised not to breastfeed during treatment with Cerinib and for 2 weeks following completion of therapy.
Pediatric usageView
Females: Ceritinib can cause fetal harm when administered to a pregnant woman. Females of reproductive potential should be advised to use effective contraception during treatment with Ceritinib and for 6 months following completion of therapy.
Males: Based on the potential for genotoxicity, males with female partners of reproductive potential should be advised to use condoms during treatment with Ceritinib and for 3 months following completion of therapy.
Pediatric Use: The safety and effectiveness of Ceritinib in pediatric patients have not been established.
Geriatric Use: Of the 925 patients in clinical studies of Ceritinib, 18% were 65 years or older, while 5% were 75 years or older. No overall differences in safety or effectiveness were observed between these subjects and younger subjects.
Hepatic Impairment: For patients with severe hepatic impairment (Child-Pugh C), the dose of Ceritinib should be reduced by approximately one-third, rounded to the nearest multiple of the 150 mg dosage strength. No dose adjustment is recommended in patients with mild (Child-Pugh A) or moderate (Child-Pugh B) hepatic impairment.
Males: Based on the potential for genotoxicity, males with female partners of reproductive potential should be advised to use condoms during treatment with Ceritinib and for 3 months following completion of therapy.
Pediatric Use: The safety and effectiveness of Ceritinib in pediatric patients have not been established.
Geriatric Use: Of the 925 patients in clinical studies of Ceritinib, 18% were 65 years or older, while 5% were 75 years or older. No overall differences in safety or effectiveness were observed between these subjects and younger subjects.
Hepatic Impairment: For patients with severe hepatic impairment (Child-Pugh C), the dose of Ceritinib should be reduced by approximately one-third, rounded to the nearest multiple of the 150 mg dosage strength. No dose adjustment is recommended in patients with mild (Child-Pugh A) or moderate (Child-Pugh B) hepatic impairment.
StorageView
Store below 30°C in a cool and dry place, away from sunlight. Keep out of reach of children.
Erlocent
Erlotinib
Erlocent
Erlotinib
Indications
Pancreatic cancer
Indication detailsView
First-line treatment of patients with metastatic Non-Small Cell Lung cancer (NSCLC) whose tumors have Epidermal Growth Factor Receptor (EGFR) exon 19 deletions or exon 21 substitution mutations as detected.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Therapeutic classView
Targeted Cancer Therapy
DosageView
NSCLC: The recommended daily dose of Erlotinib for NSCLC is 150 mg taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Side effectsView
The most common adverse reactions (20%) with Erlotinib from a pooled analysis of studies were rash, diarrhea, anorexia, fatigue, dyspnea, cough, nausea, and vomiting. The following serious adverse reactions, which may include fatalities.
- Interstitial Lung Disease (ILD)
- Renal Failure
- Hepatotoxicity with or without Hepatic Impairment
- Gastrointestinal Perforation
- Bullous and Exfoliative Skin Disorders
- Myocardial Infarction/Ischemia
- Cerebrovascular Accident
- Microangiopathic Hemolytic Anemia with Thrombocytopenia
- Ocular Disorders
- Hemorrhage in Patients Taking Warfarin
PrecautionsView
- Interstitial Lung Disease (ILD): Occurs in 1.1% of patients. Withhold Erlotinib for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue Erlotinib if ILD is diagnosed.
- Renal Failure: Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold Erlotinib for severe renal toxicity.
- Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome: Monitor periodic liver testing. Withhold or discontinue Erlotinib for severe or worsening liver tests.
- Gastrointestinal perforations-discontinue Erlotinib.
- Bullous and exfoliative skin disorders-discontinue Erlotinib.
- Myocardial infarction (Ml)/ischemia: The risk of Ml is increased in patients with pancreatic cancer.
InteractionsView
Anticoagulants: Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
Pregnancy & lactationView
Pregnancy category D. Based on its mechanism of action, Erlotinib can cause fetal harm when administered to a pregnant woman. It is not known whether Erlotinib is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions in nursing infants from Erlotinib, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric usageView
Pediatric use: The safety and effectiveness of Erlotinib in pediatric patients have not been established.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Overdose effectsView
Single oral doses of Erlotinib up to 1,000 mg in healthy subjects and weekly doses up to 1,600 mg in cancer patients have been tolerated. Repeated twice-daily doses of 200 mg single-agent Erlotinib in healthy subjects were poorly tolerated after only a few days of dosing. Based on the data from these studies, an unacceptable incidence of severe adverse reactions, such as diarrhea, rash, and liver transaminase elevation, may occur above the recommended dose. In case of suspected overdose, Erlotinib should be withheld and symptomatic treatment instituted.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.
Erlocent
Erlotinib
Erlocent
Erlotinib
Indications
Pancreatic cancer
Indication detailsView
First-line treatment of patients with metastatic Non-Small Cell Lung cancer (NSCLC) whose tumors have Epidermal Growth Factor Receptor (EGFR) exon 19 deletions or exon 21 substitution mutations as detected.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Therapeutic classView
Targeted Cancer Therapy
DosageView
NSCLC: The recommended daily dose of Erlotinib for NSCLC is 150 mg taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Side effectsView
The most common adverse reactions (20%) with Erlotinib from a pooled analysis of studies were rash, diarrhea, anorexia, fatigue, dyspnea, cough, nausea, and vomiting. The following serious adverse reactions, which may include fatalities.
- Interstitial Lung Disease (ILD)
- Renal Failure
- Hepatotoxicity with or without Hepatic Impairment
- Gastrointestinal Perforation
- Bullous and Exfoliative Skin Disorders
- Myocardial Infarction/Ischemia
- Cerebrovascular Accident
- Microangiopathic Hemolytic Anemia with Thrombocytopenia
- Ocular Disorders
- Hemorrhage in Patients Taking Warfarin
PrecautionsView
- Interstitial Lung Disease (ILD): Occurs in 1.1% of patients. Withhold Erlotinib for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue Erlotinib if ILD is diagnosed.
- Renal Failure: Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold Erlotinib for severe renal toxicity.
- Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome: Monitor periodic liver testing. Withhold or discontinue Erlotinib for severe or worsening liver tests.
- Gastrointestinal perforations-discontinue Erlotinib.
- Bullous and exfoliative skin disorders-discontinue Erlotinib.
- Myocardial infarction (Ml)/ischemia: The risk of Ml is increased in patients with pancreatic cancer.
InteractionsView
Anticoagulants: Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
Pregnancy & lactationView
Pregnancy category D. Based on its mechanism of action, Erlotinib can cause fetal harm when administered to a pregnant woman. It is not known whether Erlotinib is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions in nursing infants from Erlotinib, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric usageView
Pediatric use: The safety and effectiveness of Erlotinib in pediatric patients have not been established.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Overdose effectsView
Single oral doses of Erlotinib up to 1,000 mg in healthy subjects and weekly doses up to 1,600 mg in cancer patients have been tolerated. Repeated twice-daily doses of 200 mg single-agent Erlotinib in healthy subjects were poorly tolerated after only a few days of dosing. Based on the data from these studies, an unacceptable incidence of severe adverse reactions, such as diarrhea, rash, and liver transaminase elevation, may occur above the recommended dose. In case of suspected overdose, Erlotinib should be withheld and symptomatic treatment instituted.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.
Erlonix
Erlotinib
Erlonix
Erlotinib
Indications
Pancreatic cancer
Indication detailsView
First-line treatment of patients with metastatic Non-Small Cell Lung cancer (NSCLC) whose tumors have Epidermal Growth Factor Receptor (EGFR) exon 19 deletions or exon 21 substitution mutations as detected.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Therapeutic classView
Targeted Cancer Therapy
DosageView
NSCLC: The recommended daily dose of Erlotinib for NSCLC is 150 mg taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Side effectsView
The most common adverse reactions (20%) with Erlotinib from a pooled analysis of studies were rash, diarrhea, anorexia, fatigue, dyspnea, cough, nausea, and vomiting. The following serious adverse reactions, which may include fatalities.
- Interstitial Lung Disease (ILD)
- Renal Failure
- Hepatotoxicity with or without Hepatic Impairment
- Gastrointestinal Perforation
- Bullous and Exfoliative Skin Disorders
- Myocardial Infarction/Ischemia
- Cerebrovascular Accident
- Microangiopathic Hemolytic Anemia with Thrombocytopenia
- Ocular Disorders
- Hemorrhage in Patients Taking Warfarin
PrecautionsView
- Interstitial Lung Disease (ILD): Occurs in 1.1% of patients. Withhold Erlotinib for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue Erlotinib if ILD is diagnosed.
- Renal Failure: Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold Erlotinib for severe renal toxicity.
- Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome: Monitor periodic liver testing. Withhold or discontinue Erlotinib for severe or worsening liver tests.
- Gastrointestinal perforations-discontinue Erlotinib.
- Bullous and exfoliative skin disorders-discontinue Erlotinib.
- Myocardial infarction (Ml)/ischemia: The risk of Ml is increased in patients with pancreatic cancer.
InteractionsView
Anticoagulants: Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
Pregnancy & lactationView
Pregnancy category D. Based on its mechanism of action, Erlotinib can cause fetal harm when administered to a pregnant woman. It is not known whether Erlotinib is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions in nursing infants from Erlotinib, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric usageView
Pediatric use: The safety and effectiveness of Erlotinib in pediatric patients have not been established.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Overdose effectsView
Single oral doses of Erlotinib up to 1,000 mg in healthy subjects and weekly doses up to 1,600 mg in cancer patients have been tolerated. Repeated twice-daily doses of 200 mg single-agent Erlotinib in healthy subjects were poorly tolerated after only a few days of dosing. Based on the data from these studies, an unacceptable incidence of severe adverse reactions, such as diarrhea, rash, and liver transaminase elevation, may occur above the recommended dose. In case of suspected overdose, Erlotinib should be withheld and symptomatic treatment instituted.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.
Erlonix
Erlotinib
Erlonix
Erlotinib
Indications
Pancreatic cancer
Indication detailsView
First-line treatment of patients with metastatic Non-Small Cell Lung cancer (NSCLC) whose tumors have Epidermal Growth Factor Receptor (EGFR) exon 19 deletions or exon 21 substitution mutations as detected.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Therapeutic classView
Targeted Cancer Therapy
DosageView
NSCLC: The recommended daily dose of Erlotinib for NSCLC is 150 mg taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Side effectsView
The most common adverse reactions (20%) with Erlotinib from a pooled analysis of studies were rash, diarrhea, anorexia, fatigue, dyspnea, cough, nausea, and vomiting. The following serious adverse reactions, which may include fatalities.
- Interstitial Lung Disease (ILD)
- Renal Failure
- Hepatotoxicity with or without Hepatic Impairment
- Gastrointestinal Perforation
- Bullous and Exfoliative Skin Disorders
- Myocardial Infarction/Ischemia
- Cerebrovascular Accident
- Microangiopathic Hemolytic Anemia with Thrombocytopenia
- Ocular Disorders
- Hemorrhage in Patients Taking Warfarin
PrecautionsView
- Interstitial Lung Disease (ILD): Occurs in 1.1% of patients. Withhold Erlotinib for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue Erlotinib if ILD is diagnosed.
- Renal Failure: Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold Erlotinib for severe renal toxicity.
- Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome: Monitor periodic liver testing. Withhold or discontinue Erlotinib for severe or worsening liver tests.
- Gastrointestinal perforations-discontinue Erlotinib.
- Bullous and exfoliative skin disorders-discontinue Erlotinib.
- Myocardial infarction (Ml)/ischemia: The risk of Ml is increased in patients with pancreatic cancer.
InteractionsView
Anticoagulants: Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
Pregnancy & lactationView
Pregnancy category D. Based on its mechanism of action, Erlotinib can cause fetal harm when administered to a pregnant woman. It is not known whether Erlotinib is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions in nursing infants from Erlotinib, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric usageView
Pediatric use: The safety and effectiveness of Erlotinib in pediatric patients have not been established.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Overdose effectsView
Single oral doses of Erlotinib up to 1,000 mg in healthy subjects and weekly doses up to 1,600 mg in cancer patients have been tolerated. Repeated twice-daily doses of 200 mg single-agent Erlotinib in healthy subjects were poorly tolerated after only a few days of dosing. Based on the data from these studies, an unacceptable incidence of severe adverse reactions, such as diarrhea, rash, and liver transaminase elevation, may occur above the recommended dose. In case of suspected overdose, Erlotinib should be withheld and symptomatic treatment instituted.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.
Erloren
Erlotinib
Erloren
Erlotinib
Indications
Pancreatic cancer
Indication detailsView
First-line treatment of patients with metastatic Non-Small Cell Lung cancer (NSCLC) whose tumors have Epidermal Growth Factor Receptor (EGFR) exon 19 deletions or exon 21 substitution mutations as detected.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Therapeutic classView
Targeted Cancer Therapy
DosageView
NSCLC: The recommended daily dose of Erlotinib for NSCLC is 150 mg taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Side effectsView
The most common adverse reactions (20%) with Erlotinib from a pooled analysis of studies were rash, diarrhea, anorexia, fatigue, dyspnea, cough, nausea, and vomiting. The following serious adverse reactions, which may include fatalities.
- Interstitial Lung Disease (ILD)
- Renal Failure
- Hepatotoxicity with or without Hepatic Impairment
- Gastrointestinal Perforation
- Bullous and Exfoliative Skin Disorders
- Myocardial Infarction/Ischemia
- Cerebrovascular Accident
- Microangiopathic Hemolytic Anemia with Thrombocytopenia
- Ocular Disorders
- Hemorrhage in Patients Taking Warfarin
PrecautionsView
- Interstitial Lung Disease (ILD): Occurs in 1.1% of patients. Withhold Erlotinib for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue Erlotinib if ILD is diagnosed.
- Renal Failure: Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold Erlotinib for severe renal toxicity.
- Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome: Monitor periodic liver testing. Withhold or discontinue Erlotinib for severe or worsening liver tests.
- Gastrointestinal perforations-discontinue Erlotinib.
- Bullous and exfoliative skin disorders-discontinue Erlotinib.
- Myocardial infarction (Ml)/ischemia: The risk of Ml is increased in patients with pancreatic cancer.
InteractionsView
Anticoagulants: Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
Pregnancy & lactationView
Pregnancy category D. Based on its mechanism of action, Erlotinib can cause fetal harm when administered to a pregnant woman. It is not known whether Erlotinib is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions in nursing infants from Erlotinib, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric usageView
Pediatric use: The safety and effectiveness of Erlotinib in pediatric patients have not been established.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Overdose effectsView
Single oral doses of Erlotinib up to 1,000 mg in healthy subjects and weekly doses up to 1,600 mg in cancer patients have been tolerated. Repeated twice-daily doses of 200 mg single-agent Erlotinib in healthy subjects were poorly tolerated after only a few days of dosing. Based on the data from these studies, an unacceptable incidence of severe adverse reactions, such as diarrhea, rash, and liver transaminase elevation, may occur above the recommended dose. In case of suspected overdose, Erlotinib should be withheld and symptomatic treatment instituted.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.
Erloren
Erlotinib
Erloren
Erlotinib
Indications
Pancreatic cancer
Indication detailsView
First-line treatment of patients with metastatic Non-Small Cell Lung cancer (NSCLC) whose tumors have Epidermal Growth Factor Receptor (EGFR) exon 19 deletions or exon 21 substitution mutations as detected.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Therapeutic classView
Targeted Cancer Therapy
DosageView
NSCLC: The recommended daily dose of Erlotinib for NSCLC is 150 mg taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Side effectsView
The most common adverse reactions (20%) with Erlotinib from a pooled analysis of studies were rash, diarrhea, anorexia, fatigue, dyspnea, cough, nausea, and vomiting. The following serious adverse reactions, which may include fatalities.
- Interstitial Lung Disease (ILD)
- Renal Failure
- Hepatotoxicity with or without Hepatic Impairment
- Gastrointestinal Perforation
- Bullous and Exfoliative Skin Disorders
- Myocardial Infarction/Ischemia
- Cerebrovascular Accident
- Microangiopathic Hemolytic Anemia with Thrombocytopenia
- Ocular Disorders
- Hemorrhage in Patients Taking Warfarin
PrecautionsView
- Interstitial Lung Disease (ILD): Occurs in 1.1% of patients. Withhold Erlotinib for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue Erlotinib if ILD is diagnosed.
- Renal Failure: Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold Erlotinib for severe renal toxicity.
- Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome: Monitor periodic liver testing. Withhold or discontinue Erlotinib for severe or worsening liver tests.
- Gastrointestinal perforations-discontinue Erlotinib.
- Bullous and exfoliative skin disorders-discontinue Erlotinib.
- Myocardial infarction (Ml)/ischemia: The risk of Ml is increased in patients with pancreatic cancer.
InteractionsView
Anticoagulants: Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
Pregnancy & lactationView
Pregnancy category D. Based on its mechanism of action, Erlotinib can cause fetal harm when administered to a pregnant woman. It is not known whether Erlotinib is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions in nursing infants from Erlotinib, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric usageView
Pediatric use: The safety and effectiveness of Erlotinib in pediatric patients have not been established.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Overdose effectsView
Single oral doses of Erlotinib up to 1,000 mg in healthy subjects and weekly doses up to 1,600 mg in cancer patients have been tolerated. Repeated twice-daily doses of 200 mg single-agent Erlotinib in healthy subjects were poorly tolerated after only a few days of dosing. Based on the data from these studies, an unacceptable incidence of severe adverse reactions, such as diarrhea, rash, and liver transaminase elevation, may occur above the recommended dose. In case of suspected overdose, Erlotinib should be withheld and symptomatic treatment instituted.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.
Erlotin
Erlotinib
Erlotin
Erlotinib
Indications
Pancreatic cancer
Indication detailsView
First-line treatment of patients with metastatic Non-Small Cell Lung cancer (NSCLC) whose tumors have Epidermal Growth Factor Receptor (EGFR) exon 19 deletions or exon 21 substitution mutations as detected.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Therapeutic classView
Targeted Cancer Therapy
DosageView
NSCLC: The recommended daily dose of Erlotinib for NSCLC is 150 mg taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Side effectsView
The most common adverse reactions (20%) with Erlotinib from a pooled analysis of studies were rash, diarrhea, anorexia, fatigue, dyspnea, cough, nausea, and vomiting. The following serious adverse reactions, which may include fatalities.
- Interstitial Lung Disease (ILD)
- Renal Failure
- Hepatotoxicity with or without Hepatic Impairment
- Gastrointestinal Perforation
- Bullous and Exfoliative Skin Disorders
- Myocardial Infarction/Ischemia
- Cerebrovascular Accident
- Microangiopathic Hemolytic Anemia with Thrombocytopenia
- Ocular Disorders
- Hemorrhage in Patients Taking Warfarin
PrecautionsView
- Interstitial Lung Disease (ILD): Occurs in 1.1% of patients. Withhold Erlotinib for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue Erlotinib if ILD is diagnosed.
- Renal Failure: Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold Erlotinib for severe renal toxicity.
- Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome: Monitor periodic liver testing. Withhold or discontinue Erlotinib for severe or worsening liver tests.
- Gastrointestinal perforations-discontinue Erlotinib.
- Bullous and exfoliative skin disorders-discontinue Erlotinib.
- Myocardial infarction (Ml)/ischemia: The risk of Ml is increased in patients with pancreatic cancer.
InteractionsView
Anticoagulants: Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
Pregnancy & lactationView
Pregnancy category D. Based on its mechanism of action, Erlotinib can cause fetal harm when administered to a pregnant woman. It is not known whether Erlotinib is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions in nursing infants from Erlotinib, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric usageView
Pediatric use: The safety and effectiveness of Erlotinib in pediatric patients have not been established.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Overdose effectsView
Single oral doses of Erlotinib up to 1,000 mg in healthy subjects and weekly doses up to 1,600 mg in cancer patients have been tolerated. Repeated twice-daily doses of 200 mg single-agent Erlotinib in healthy subjects were poorly tolerated after only a few days of dosing. Based on the data from these studies, an unacceptable incidence of severe adverse reactions, such as diarrhea, rash, and liver transaminase elevation, may occur above the recommended dose. In case of suspected overdose, Erlotinib should be withheld and symptomatic treatment instituted.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.
Erlotin
Erlotinib
Erlotin
Erlotinib
Indications
Pancreatic cancer
Indication detailsView
First-line treatment of patients with metastatic Non-Small Cell Lung cancer (NSCLC) whose tumors have Epidermal Growth Factor Receptor (EGFR) exon 19 deletions or exon 21 substitution mutations as detected.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Maintenance treatment of patients with locally advanced or metastatic NSCLC whose disease has not progressed after four cycles of platinum based first-line chemotherapy.
Treatment of locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen.
First-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer, in combination with gemcitabine.
Therapeutic classView
Targeted Cancer Therapy
DosageView
NSCLC: The recommended daily dose of Erlotinib for NSCLC is 150 mg taken on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Pancreatic Cancer: The recommended daily dose of Erlotinib for pancreatic cancer is 100 mg taken once daily in combination with gemcitabine. Take Erlotinib on an empty stomach, i.e., at least one hour before or two hours after the ingestion of food. Treatment should continue until disease progression or unacceptable toxicity occurs.
Reduce Erlotinib by 50 mg decrements: If severe reactions occur with concomitant use of strong CYP3A4 inhibitors (such as atazanavir, Clarithromycin, Indinavir, Itraconazole, Ketoconazole, Nefazodone, Nelfinavir, Ritonavir, Saquinavir, Telithromycin, Voriconazole or grapefruit or grapefruit juice] or when using concomitantly with an inhibitor of both CYP3A4 and CYP1A2 (e.g., Ciprofloxacin).
Increase Erlotinib by 50 mg increments as tolerated for: Concomitant use with CYP3A4 inducers, such as rifampin, rifabutin, rifapentine, phenytoin, carbamazepine, phenobarbital, or St. John's Wort. Increase doses by 50 mg increments at 2 week intervals to a maximum of 450 mg. Avoid concomitant use, if possible.
Concurrent cigarette smoking: Increase by 50 mg increments at 2 week intervals to a maximum of 300 mg. Immediately reduce the dose of Erlotinib to the recommended dose (150 mg or 100 mg daily) upon cessation of smoking.
Side effectsView
The most common adverse reactions (20%) with Erlotinib from a pooled analysis of studies were rash, diarrhea, anorexia, fatigue, dyspnea, cough, nausea, and vomiting. The following serious adverse reactions, which may include fatalities.
- Interstitial Lung Disease (ILD)
- Renal Failure
- Hepatotoxicity with or without Hepatic Impairment
- Gastrointestinal Perforation
- Bullous and Exfoliative Skin Disorders
- Myocardial Infarction/Ischemia
- Cerebrovascular Accident
- Microangiopathic Hemolytic Anemia with Thrombocytopenia
- Ocular Disorders
- Hemorrhage in Patients Taking Warfarin
PrecautionsView
- Interstitial Lung Disease (ILD): Occurs in 1.1% of patients. Withhold Erlotinib for acute onset of new or progressive unexplained pulmonary symptoms, such as dyspnea, cough and fever. Discontinue Erlotinib if ILD is diagnosed.
- Renal Failure: Monitor renal function and electrolytes, particularly in patients at risk of dehydration. Withhold Erlotinib for severe renal toxicity.
- Hepatotoxicity with or without hepatic impairment including hepatic failure and hepatorenal syndrome: Monitor periodic liver testing. Withhold or discontinue Erlotinib for severe or worsening liver tests.
- Gastrointestinal perforations-discontinue Erlotinib.
- Bullous and exfoliative skin disorders-discontinue Erlotinib.
- Myocardial infarction (Ml)/ischemia: The risk of Ml is increased in patients with pancreatic cancer.
InteractionsView
Anticoagulants: Interaction with coumarin-derived anticoagulants, including warfarin, leading to increased International Normalized Ratio (INR) and bleeding adverse reactions.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
CYP3A4 inhibitors: Erlotinib is metabolized predominantly by CYP3A4. Co-treatment with the potent CYP3A4 inhibitor ketoconazole increased Erlotinib AUC by 67%. When Erlotinib was co-administered with Ciprofloxacin, an inhibitor of both CYP3A4 and CYP1A2, the Erlotinib exposure [AUC] and maximum concentration [Cmax] increased by 39% and 17%, respectively.
CYP3A4 inducers: Pre-treatment with the CYP3A4 inducer Rifampicin for 7-11 days prior to Erlotinib decreased Erlotinib AUC by 58% to 80%. Dose modifications are recommended.
Drugs affecting gastric pH: Co-administration of Erlotinib with omeprazole decreased Erlotinib AUC by 46% and co-administration of Erlotinib with Ranitidine 300 mg decreased Erlotinib AUC by 33%.
Pregnancy & lactationView
Pregnancy category D. Based on its mechanism of action, Erlotinib can cause fetal harm when administered to a pregnant woman. It is not known whether Erlotinib is present in human milk. Because many drugs are present in human milk and because of the potential for serious adverse reactions in nursing infants from Erlotinib, a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.
Pediatric usageView
Pediatric use: The safety and effectiveness of Erlotinib in pediatric patients have not been established.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Geriatric use: No overall differences in safety or efficacy were observed between subjects 65 years and older and those younger than 65.
Overdose effectsView
Single oral doses of Erlotinib up to 1,000 mg in healthy subjects and weekly doses up to 1,600 mg in cancer patients have been tolerated. Repeated twice-daily doses of 200 mg single-agent Erlotinib in healthy subjects were poorly tolerated after only a few days of dosing. Based on the data from these studies, an unacceptable incidence of severe adverse reactions, such as diarrhea, rash, and liver transaminase elevation, may occur above the recommended dose. In case of suspected overdose, Erlotinib should be withheld and symptomatic treatment instituted.
StorageView
Store at a temperature not exceeding 30°C in a dry place. Protect from light and moisture.
Ermac
Erythromycin (Oral)
Ermac
Erythromycin (Oral)
Indications
Susceptible infections
Indication detailsView
Erythromycin is highly effective in the treatment of a wide variety of clinical infections.
- Upper respiratory tract infections: Tonsilitis, Peritonsillar abscess, Pharyngitis, laryngitis, Sinusitis. Secondary infections in colds and influenza.
- Lower respiratory tract infections: Tracheitis, acute and chronic bronchitis.
- Ear infections: Otitis media, otitis externa, mastoiditis.
- Eye infections: Blepharitis, established trachoma.
- Skin and Soft tissue infections: Boils and carbuncles, impetigo, abscesses, pustular acne, paromychia, cellulitis, erysipelas.
- Gastrointestinal tract infections: Cholecystitis, staphylococcal enterocolitis.
- Prophylaxis: Pre and post-operative, trauma, burns, rheumatic fever.
- Other infections: Osteomyelitis, diptheria, scarlet fever, whooping cough.
Therapeutic classView
Anti-diarrhoeal Antimicrobial drugs, Macrolides
PharmacologyView
Erythromycin inhibits microsomal protein synthesis in susceptible organisms by inhibiting the translocation process. Specific binding to the 50S subunit or 70S ribosome occurs in these organisms but there is no binding to the stable 80S mammalian ribosome. Erythromycin is active against many Grampositive bacteria, some Gram-negative bacteria and against mycoplasmas and chlamydia.
Absorption: Erythromycin base is destroyed by acid and is therefore administered in the form of stable ester. The rates of absorption of the base and esters are diminished by the presence of food. The stearate is hydrolyzed in the intestine and the free erythromycin absorbed.
Blood concentration: After an oral dose of 500 mg. of the base of stearate, peak serum concentrations of 0.9 to 1.4 or 0.4 to 1.8 mg/ml. respectively are attained in 1 to 4 hours. Half-life: The serum half-life is 1.2 to 4 hours. In subjects with oliguria, the half-life is about 5 hours.
Distribution: Erythromycin is widely distributed throughout body tissue and fluids with some retention in the liver and spleen, protein binding of erythromycin base is 73%. Erythromycin enters the cerebrospinal fluid when the meninges are inflamed. It also crosses the placenta and is excreted in the milk.
Excretion: 5 to 15 % of the dose of erythromycin is excreted in the urine and large amounts of the unchanged active substance are excreted in the bile.
Absorption: Erythromycin base is destroyed by acid and is therefore administered in the form of stable ester. The rates of absorption of the base and esters are diminished by the presence of food. The stearate is hydrolyzed in the intestine and the free erythromycin absorbed.
Blood concentration: After an oral dose of 500 mg. of the base of stearate, peak serum concentrations of 0.9 to 1.4 or 0.4 to 1.8 mg/ml. respectively are attained in 1 to 4 hours. Half-life: The serum half-life is 1.2 to 4 hours. In subjects with oliguria, the half-life is about 5 hours.
Distribution: Erythromycin is widely distributed throughout body tissue and fluids with some retention in the liver and spleen, protein binding of erythromycin base is 73%. Erythromycin enters the cerebrospinal fluid when the meninges are inflamed. It also crosses the placenta and is excreted in the milk.
Excretion: 5 to 15 % of the dose of erythromycin is excreted in the urine and large amounts of the unchanged active substance are excreted in the bile.
DosageView
Adult and Children over 8 years: 250-500 mg every six hours for mild to moderate infections. This may be increased upto 4 gm. or more daily in severe cases.
Elderly: No special dosage recommendation. Erythromycin may be administered if desired, three times daily or twice daily by giving one-third or half of the total daily requirement 8 hourly or 12 hourly respectively.
Children aged 2 to 8 years: 250 mg. every six hours or 30-50 mg/kg body weight per day divided into four equal dosage.
Infants and Children upto 2 years: 500 mg. in divided doses or 30-50 mg/kg body weight in divided doses.
Elderly: No special dosage recommendation. Erythromycin may be administered if desired, three times daily or twice daily by giving one-third or half of the total daily requirement 8 hourly or 12 hourly respectively.
Children aged 2 to 8 years: 250 mg. every six hours or 30-50 mg/kg body weight per day divided into four equal dosage.
Infants and Children upto 2 years: 500 mg. in divided doses or 30-50 mg/kg body weight in divided doses.
Side effectsView
Allergic reactions are rare and mild although anaphylaxis has occurred. Occasionally there is abdominal discomfort after oral administration, sometimes with nausea and vomiting. This discomfort usually subsides after a few days without it being necessary to reduce the dosage.
ContraindicationsView
Known hypersensitivity to Erythromycin.
PrecautionsView
Erythromycin should be given with care in patients with impaired hepatic function, as erythromycin is excreted principally in the bile.
InteractionsView
Recent data from studies of erythromycin reveals that its use in patients who are receiving high dosage of theophylline may be associated with an increase of serum theophylline levels and potential theophylline toxicity. In such cases this dose of theophylline should be reduced.
Pregnancy & lactationView
Clinical and Laboratory studies have been shown no evidence in human of teratogenicity or toxicity. However, caution should be exercised when prescribing this drug to pregnant patients and lactating mothers since erythromycin crosses the placental barrier and is excreted in breast milk.
Overdose effectsView
In case of overdosage, Erythromycin should be discontinued. Overdosage should be handled with the prompt elimination of unabsorbed drug and all other appropriate measures should be instituted. Erythromycin is not removed by peritoneal dialysis or haemodialysis.
ReconstitutionView
Direction for reconstitution of suspension: Shake the bottle to loosen powder. Add 60 ml or 100 ml of boiled and cooled water to the dry powder of the bottle. For ease of preparation, add water to the bottle in two proportions. Shake well after each addition until all the powder is in suspension.
Shake the suspension well before each use. Keep the bottle tightly closed. The reconstituted suspension should be stored in a cool and dry place, preferably in refrigerator and unused portion should be discarded after 7 days.
Shake the suspension well before each use. Keep the bottle tightly closed. The reconstituted suspension should be stored in a cool and dry place, preferably in refrigerator and unused portion should be discarded after 7 days.
StorageView
Keep below 25°C temperature, away from light & moisture. Keep out of the reach of children.
Ermite
Permethrin
Ermite
Permethrin
Indications
Scabies
Indication detailsView
Permethrin cream is indicated for the treatment of scabies and crab lice infestations (Pediculosis). Scabies can affect everyone in the family. If one is infected, all family members must be treated together.
Therapeutic classView
Parasiticidal preparations
PharmacologyView
Permethrin cream contains Permethrin, a pyrethroid, which is a topical scabicidal agent for the treatment of infestation with Sarcoptes Scabiei (scabies). It acts on the nerve cell membrane to disrupt the sodium channel current by which the polarization of the membrane is regulated. Delayed repolarization & paralysis of the pests are the consequences of this disturbance.
Pharmacokinetics: The only approved route of administration is the topical route and there are few human data available on systemic exposure or kinetics following permethrin application to the skin. Some presystemic metabolism occurs in skin. Less than 0.5% of applied permethrin is absorbed during the first 48 hours. Absorbed permethrin is rapidly metabolized by ester hydrolysis, most likely in the liver and the products are excreted primarily in the urine.
Pharmacokinetics: The only approved route of administration is the topical route and there are few human data available on systemic exposure or kinetics following permethrin application to the skin. Some presystemic metabolism occurs in skin. Less than 0.5% of applied permethrin is absorbed during the first 48 hours. Absorbed permethrin is rapidly metabolized by ester hydrolysis, most likely in the liver and the products are excreted primarily in the urine.
DosageView
Recommended duration of Treatment:
- Adults and children over 12 years: a full tube
- Children aged 6-12 years: up to 1⁄2 of a tube
- Children aged 1-5 years: up to ¼ of a tube
- Children aged 2 months to 1 year: up to ⅛ of a tube
- Children Less then 2 month: dose is not established
AdministrationView
Before application of Permethrin cream the skin should be clean, cool and dry. Do not have a hot shower or bath before applying.
For adults and children over 2 years: Apply the cream to the whole body from the neck down, rubbing lightly into the skin until the cream disappears. It is important to include all skin surfaces, such as between the fingers and toes, under the nails and on the soles of the feet.
For babies under 2 years: Apply to the face, neck, ears and scalp as well, only avoiding the area immediately around the eyes and mouth.
Leave cream on for at least 8 hours, before washing off. Reapply to any area that may be washed during the 8h treatment time (such as after washing the hands). If necessary, permethrin cream should be used again after 7 days as per the advice of the doctor.
For adults and children over 2 years: Apply the cream to the whole body from the neck down, rubbing lightly into the skin until the cream disappears. It is important to include all skin surfaces, such as between the fingers and toes, under the nails and on the soles of the feet.
For babies under 2 years: Apply to the face, neck, ears and scalp as well, only avoiding the area immediately around the eyes and mouth.
Leave cream on for at least 8 hours, before washing off. Reapply to any area that may be washed during the 8h treatment time (such as after washing the hands). If necessary, permethrin cream should be used again after 7 days as per the advice of the doctor.
Side effectsView
In Scabies patients, skin discomfort, usually described as burning, stinging or tingling occurs in a few individuals soon after the cream is applied. Others transient signs and symptoms of irritation including enythema, edema, eczema, rash and puritis.
ContraindicationsView
Permethrin is contraindicated in patients with known hypersensitivity to any component of pyrethroids or permethrin. Nursing staff who routinely apply permethrin may wear globes to avoid any possible irritation to the hands.
PrecautionsView
Scabies infestation is often accompanied by pruritus, edema & erythema. Treatment with permethrin may temporarily exacerbate these conditions. Patients should be advised to avoid contact with eyes during application & to flash with water immediately if the cream gets in the eyes.
InteractionsView
The treatment of eczemodous like reactions with corticosteroids should be withheld prior to treatment with permethrin, as there is a risk of exacerbating the scabies infestation by reducing the immune response to the mite.
Pregnancy & lactationView
In the absence of specific studies in pregnant women, its use in pregnancy should only follow medical advice. It is not known whether permethrin is excreted in human milk so it should not be used in nursing mothers.
StorageView
Store in a cool, dry place, away from light & keep out of the reach of children...