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Darboren
Darbepoetin Alfa
Darboren
Darbepoetin Alfa
Indications
Anaemia
Indication detailsView
Anemia Due To Chronic Kidney Disease: Darbepoetin Alfa is indicated for the treatment of anemia due to chronic kidney disease (CKD), including patients on dialysis and patients not on dialysis.
Anemia Due To Chemotherapy In Patients With Cancer: Darbepoetin Alfa is indicated for the treatment of anemia in patients with non-myeloid malignancies where anemia is due to the effect of concomitant myelosuppressive chemotherapy, and upon initiation, there is a minimum of two additional months of planned chemotherapy.
Anemia Due To Chemotherapy In Patients With Cancer: Darbepoetin Alfa is indicated for the treatment of anemia in patients with non-myeloid malignancies where anemia is due to the effect of concomitant myelosuppressive chemotherapy, and upon initiation, there is a minimum of two additional months of planned chemotherapy.
Therapeutic classView
Haematopoietic Agents
PharmacologyView
Darbepoetin alfa stimulates erythropoiesis by the same mechanism as endogenous erythropoietin. Erythropoietin interacts with progenitor stem cells to increase red cell production. Binding of erythropoietin to the erythropoietin receptor leads to receptor dimerization, which facilitates activation of JAK-STAT signaling pathways within the cytosol. Activated STAT (signal transducers and activators of transcription) proteins are then translocated to the nucleus where they serve as transcription factors which regulate the activation of specific genes involved in cell division or differentiation.
DosageView
Usual Adult Dose for Anemia Associated with Chronic Renal Failure:
Chronic Kidney Disease (CKD) Patients Not on Dialysis:- Initial dose: 0.45 mcg/kg IV or subcutaneously once every 4 weeks as appropriate
- Comments: Initiate treatment only when hemoglobin is less than 10 g/dL, rate of hemoglobin decline indicates likelihood of requiring RBC transfusion, and reducing risk of alloimmunization and/or other RBC transfusion-related risks is a goal.
- Initial dose: 0.45 mcg/kg IV or subcutaneously once a week or 0.75 mcg/kg once every 2 weeks as appropriate
- Comments: Initiate treatment when hemoglobin is less than 10 g/dL. IV route is recommended for patients on hemodialysis.
Usual Adult Dose for Anemia Associated with Chemotherapy:
- Initial dose: 2.25 mcg/kg subcutaneously once a week or 500 mcg subcutaneously once every 3 weeks
- Duration of therapy: Until completion of chemotherapy course
- Comments: Initiate treatment if hemoglobin is less than 10 g/dL and a minimum of 2 additional months of chemotherapy is planned. Use the lowest dose necessary to avoid RBC transfusions.
- Use: Treatment of anemia in patients with non-myeloid malignancies where anemia is due to the effect of concomitant myelosuppressive chemotherapy.
Side effectsView
Increased Mortality, Myocardial Infarction, Stroke, and Thromboembolism; Increased Mortality and/or Increased Risk of Tumor Progression or Recurrence in Patients with cancer; Hypertension; Seizures; Serious allergic reaction; Severe Cutaneous Reactions
ContraindicationsView
Darbepoetin is contraindicated in patients with:
- Uncontrolled hypertension
- Pure red cell aplasia (PRCA) that begins after treatment with Darbepoetin or other erythropoietin protein drugs
- Serious allergic reactions to Darbepoetin
PrecautionsView
Pregnancy and lactation, children. Hypertension; history of seizures; hepatic impairment; sickle cell anaemia; sudden stabing migraine-like pain (warning sign of hypotensive crisis); exclude other causes of anaemia; ischaemic vascular disease; thrombocytosis; epilepsy; malignant disease; increase in heparin dose may be needed; increased risk of thrombosis when used for anaemia before orthopedic surgery; CV disease including recent MI/cerebrovascular accident. Monitor haemoglobin, BP and electrolytes; platelet count for 1st 8 wk.
InteractionsView
Antagonism of hypotensive effect and increased risk of hyperkalemia with ACE inhibitors and angiotensin II receptor antagonists. Ethanol.
Pregnancy & lactationView
Pregnancy Category C. It is not known whether Darbepoetin Alfa is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Darbepoetin Alfa is administered to a nursing woman.
Pediatric usageView
Pediatric Use:
- Pediatric Patients With CKD: Darbepoetin safety and efficacy were similar between adults and pediatric patients with CKD when Darbepoetin was used for initial treatment of anemia or patients were transitioned from treatment with epoetin alfa to Darbepoetin
- Pediatric Patients With Cancer: The safety and efficacy of Darbepoetin in pediatric patients with cancer have not been established.
Overdose effectsView
Darbepoetin overdosage can cause hemoglobin levels above the desired level, which should be managed with discontinuation or reduction of Darbepoetin dosage and/or with phlebotomy, as clinically indicated. Cases of severe hypertension have been observed following overdose with ESAs
StorageView
Store at 2°C to 8°C. Do not freeze. Do not shake. Protect from light; store Darbepoetin Alfa in the carton until use. Do not use Darbepoetin Alfa that has been shaken or frozen.
Darboren
Darbepoetin Alfa
Darboren
Darbepoetin Alfa
Indications
Anaemia
Indication detailsView
Anemia Due To Chronic Kidney Disease: Darbepoetin Alfa is indicated for the treatment of anemia due to chronic kidney disease (CKD), including patients on dialysis and patients not on dialysis.
Anemia Due To Chemotherapy In Patients With Cancer: Darbepoetin Alfa is indicated for the treatment of anemia in patients with non-myeloid malignancies where anemia is due to the effect of concomitant myelosuppressive chemotherapy, and upon initiation, there is a minimum of two additional months of planned chemotherapy.
Anemia Due To Chemotherapy In Patients With Cancer: Darbepoetin Alfa is indicated for the treatment of anemia in patients with non-myeloid malignancies where anemia is due to the effect of concomitant myelosuppressive chemotherapy, and upon initiation, there is a minimum of two additional months of planned chemotherapy.
Therapeutic classView
Haematopoietic Agents
PharmacologyView
Darbepoetin alfa stimulates erythropoiesis by the same mechanism as endogenous erythropoietin. Erythropoietin interacts with progenitor stem cells to increase red cell production. Binding of erythropoietin to the erythropoietin receptor leads to receptor dimerization, which facilitates activation of JAK-STAT signaling pathways within the cytosol. Activated STAT (signal transducers and activators of transcription) proteins are then translocated to the nucleus where they serve as transcription factors which regulate the activation of specific genes involved in cell division or differentiation.
DosageView
Usual Adult Dose for Anemia Associated with Chronic Renal Failure:
Chronic Kidney Disease (CKD) Patients Not on Dialysis:- Initial dose: 0.45 mcg/kg IV or subcutaneously once every 4 weeks as appropriate
- Comments: Initiate treatment only when hemoglobin is less than 10 g/dL, rate of hemoglobin decline indicates likelihood of requiring RBC transfusion, and reducing risk of alloimmunization and/or other RBC transfusion-related risks is a goal.
- Initial dose: 0.45 mcg/kg IV or subcutaneously once a week or 0.75 mcg/kg once every 2 weeks as appropriate
- Comments: Initiate treatment when hemoglobin is less than 10 g/dL. IV route is recommended for patients on hemodialysis.
Usual Adult Dose for Anemia Associated with Chemotherapy:
- Initial dose: 2.25 mcg/kg subcutaneously once a week or 500 mcg subcutaneously once every 3 weeks
- Duration of therapy: Until completion of chemotherapy course
- Comments: Initiate treatment if hemoglobin is less than 10 g/dL and a minimum of 2 additional months of chemotherapy is planned. Use the lowest dose necessary to avoid RBC transfusions.
- Use: Treatment of anemia in patients with non-myeloid malignancies where anemia is due to the effect of concomitant myelosuppressive chemotherapy.
Side effectsView
Increased Mortality, Myocardial Infarction, Stroke, and Thromboembolism; Increased Mortality and/or Increased Risk of Tumor Progression or Recurrence in Patients with cancer; Hypertension; Seizures; Serious allergic reaction; Severe Cutaneous Reactions
ContraindicationsView
Darbepoetin is contraindicated in patients with:
- Uncontrolled hypertension
- Pure red cell aplasia (PRCA) that begins after treatment with Darbepoetin or other erythropoietin protein drugs
- Serious allergic reactions to Darbepoetin
PrecautionsView
Pregnancy and lactation, children. Hypertension; history of seizures; hepatic impairment; sickle cell anaemia; sudden stabing migraine-like pain (warning sign of hypotensive crisis); exclude other causes of anaemia; ischaemic vascular disease; thrombocytosis; epilepsy; malignant disease; increase in heparin dose may be needed; increased risk of thrombosis when used for anaemia before orthopedic surgery; CV disease including recent MI/cerebrovascular accident. Monitor haemoglobin, BP and electrolytes; platelet count for 1st 8 wk.
InteractionsView
Antagonism of hypotensive effect and increased risk of hyperkalemia with ACE inhibitors and angiotensin II receptor antagonists. Ethanol.
Pregnancy & lactationView
Pregnancy Category C. It is not known whether Darbepoetin Alfa is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Darbepoetin Alfa is administered to a nursing woman.
Pediatric usageView
Pediatric Use:
- Pediatric Patients With CKD: Darbepoetin safety and efficacy were similar between adults and pediatric patients with CKD when Darbepoetin was used for initial treatment of anemia or patients were transitioned from treatment with epoetin alfa to Darbepoetin
- Pediatric Patients With Cancer: The safety and efficacy of Darbepoetin in pediatric patients with cancer have not been established.
Overdose effectsView
Darbepoetin overdosage can cause hemoglobin levels above the desired level, which should be managed with discontinuation or reduction of Darbepoetin dosage and/or with phlebotomy, as clinically indicated. Cases of severe hypertension have been observed following overdose with ESAs
StorageView
Store at 2°C to 8°C. Do not freeze. Do not shake. Protect from light; store Darbepoetin Alfa in the carton until use. Do not use Darbepoetin Alfa that has been shaken or frozen.
Darboren
Darbepoetin Alfa
Darboren
Darbepoetin Alfa
Indications
Anaemia
Indication detailsView
Anemia Due To Chronic Kidney Disease: Darbepoetin Alfa is indicated for the treatment of anemia due to chronic kidney disease (CKD), including patients on dialysis and patients not on dialysis.
Anemia Due To Chemotherapy In Patients With Cancer: Darbepoetin Alfa is indicated for the treatment of anemia in patients with non-myeloid malignancies where anemia is due to the effect of concomitant myelosuppressive chemotherapy, and upon initiation, there is a minimum of two additional months of planned chemotherapy.
Anemia Due To Chemotherapy In Patients With Cancer: Darbepoetin Alfa is indicated for the treatment of anemia in patients with non-myeloid malignancies where anemia is due to the effect of concomitant myelosuppressive chemotherapy, and upon initiation, there is a minimum of two additional months of planned chemotherapy.
Therapeutic classView
Haematopoietic Agents
PharmacologyView
Darbepoetin alfa stimulates erythropoiesis by the same mechanism as endogenous erythropoietin. Erythropoietin interacts with progenitor stem cells to increase red cell production. Binding of erythropoietin to the erythropoietin receptor leads to receptor dimerization, which facilitates activation of JAK-STAT signaling pathways within the cytosol. Activated STAT (signal transducers and activators of transcription) proteins are then translocated to the nucleus where they serve as transcription factors which regulate the activation of specific genes involved in cell division or differentiation.
DosageView
Usual Adult Dose for Anemia Associated with Chronic Renal Failure:
Chronic Kidney Disease (CKD) Patients Not on Dialysis:- Initial dose: 0.45 mcg/kg IV or subcutaneously once every 4 weeks as appropriate
- Comments: Initiate treatment only when hemoglobin is less than 10 g/dL, rate of hemoglobin decline indicates likelihood of requiring RBC transfusion, and reducing risk of alloimmunization and/or other RBC transfusion-related risks is a goal.
- Initial dose: 0.45 mcg/kg IV or subcutaneously once a week or 0.75 mcg/kg once every 2 weeks as appropriate
- Comments: Initiate treatment when hemoglobin is less than 10 g/dL. IV route is recommended for patients on hemodialysis.
Usual Adult Dose for Anemia Associated with Chemotherapy:
- Initial dose: 2.25 mcg/kg subcutaneously once a week or 500 mcg subcutaneously once every 3 weeks
- Duration of therapy: Until completion of chemotherapy course
- Comments: Initiate treatment if hemoglobin is less than 10 g/dL and a minimum of 2 additional months of chemotherapy is planned. Use the lowest dose necessary to avoid RBC transfusions.
- Use: Treatment of anemia in patients with non-myeloid malignancies where anemia is due to the effect of concomitant myelosuppressive chemotherapy.
Side effectsView
Increased Mortality, Myocardial Infarction, Stroke, and Thromboembolism; Increased Mortality and/or Increased Risk of Tumor Progression or Recurrence in Patients with cancer; Hypertension; Seizures; Serious allergic reaction; Severe Cutaneous Reactions
ContraindicationsView
Darbepoetin is contraindicated in patients with:
- Uncontrolled hypertension
- Pure red cell aplasia (PRCA) that begins after treatment with Darbepoetin or other erythropoietin protein drugs
- Serious allergic reactions to Darbepoetin
PrecautionsView
Pregnancy and lactation, children. Hypertension; history of seizures; hepatic impairment; sickle cell anaemia; sudden stabing migraine-like pain (warning sign of hypotensive crisis); exclude other causes of anaemia; ischaemic vascular disease; thrombocytosis; epilepsy; malignant disease; increase in heparin dose may be needed; increased risk of thrombosis when used for anaemia before orthopedic surgery; CV disease including recent MI/cerebrovascular accident. Monitor haemoglobin, BP and electrolytes; platelet count for 1st 8 wk.
InteractionsView
Antagonism of hypotensive effect and increased risk of hyperkalemia with ACE inhibitors and angiotensin II receptor antagonists. Ethanol.
Pregnancy & lactationView
Pregnancy Category C. It is not known whether Darbepoetin Alfa is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Darbepoetin Alfa is administered to a nursing woman.
Pediatric usageView
Pediatric Use:
- Pediatric Patients With CKD: Darbepoetin safety and efficacy were similar between adults and pediatric patients with CKD when Darbepoetin was used for initial treatment of anemia or patients were transitioned from treatment with epoetin alfa to Darbepoetin
- Pediatric Patients With Cancer: The safety and efficacy of Darbepoetin in pediatric patients with cancer have not been established.
Overdose effectsView
Darbepoetin overdosage can cause hemoglobin levels above the desired level, which should be managed with discontinuation or reduction of Darbepoetin dosage and/or with phlebotomy, as clinically indicated. Cases of severe hypertension have been observed following overdose with ESAs
StorageView
Store at 2°C to 8°C. Do not freeze. Do not shake. Protect from light; store Darbepoetin Alfa in the carton until use. Do not use Darbepoetin Alfa that has been shaken or frozen.
Darifen ER
Darifenacin
Darifen ER
Darifenacin
Indications
Urinary frequency and urgency
Indication detailsView
Darifenacin is indicated for the treatment of overactive bladder with symptoms of urge urinary incontinence, urgency and frequency.
Therapeutic classView
BPH/ Urinary retention/ Urinary incontinence
PharmacologyView
Darifenacin is a potent, competitive and selective muscarinic receptor antagonist which has greater binding affinity for muscarinic M3 receptors. M3 receptors are involved in the contraction of the detrusor muscle of the bladder, GI smooth muscle, saliva production, and iris sphincter function. Darifenacin may increase volume threshold in patients with involuntary detrusor contraction, thus increase bladder capacity.
DosageView
Darifenacin 7.5 mg once daily; may increase dose to 15 mg once daily if no adequate response after 2 wk of therapy. Darifenacin should be taken with liquid. It can be taken with or without food, and should be swallowed whole and not chewed, divided or crushed.
For patients with moderate hepatic impairment or when co-administered with potent CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, nelfinavir, clarithromycin and nefazadone), the daily dose of Darifenacin should not exceed 7.5 mg.
For patients with moderate hepatic impairment or when co-administered with potent CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, nelfinavir, clarithromycin and nefazadone), the daily dose of Darifenacin should not exceed 7.5 mg.
Side effectsView
The most common side effects are dry mouth & constipation. Other less commonly reported side effects include- abnormal vision, back pain, dry skin, hypertension, vomiting, peripheral edema, weight gain, arthralgia, bronchitis, pharyngitis, rhinitis, sinusitis, rash, pruritus, urinary tract disorder and vaginitis.
ContraindicationsView
Patient with urinary retention, gastric retention, uncontrolled narrow-angle glaucoma, and in patients who are at risk for these conditions.
PrecautionsView
Darifenacin should be used with caution in the patient at risk for urinary retention & decreased gastrointestinal motility, with impaired renal & hepatic impairment.
InteractionsView
Darifenacin has known drug-drug interaction with CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, ritonavir, nelfinavir etc.). The concomitant use of Darifenacin with other anticholinergic agents may increase the frequency and/or severity of dry mouth, constipation, blurred vision and other anticholinergic pharmacological effects.
Pregnancy & lactationView
Pregnancy Category C. Darifenacin should be used during pregnancy only if the benefit to the mother outweighs the potential risk to the fetus.
Lactation: It is not known whether Darifenacin is excreted into human milk and therefore caution should be exercised before Darifenacin is administered to a nursing woman.
Lactation: It is not known whether Darifenacin is excreted into human milk and therefore caution should be exercised before Darifenacin is administered to a nursing woman.
Overdose effectsView
Overdosage with antimuscarinic agents can result in severe antimuscarinic effects. ECG monitoring is recommended when event of overdosage is occurred. Darifenacin has been administered in clinical trials at doses up to 75 mg (five times the maximum therapeutic dose) and signs of overdose were limited to abnormal vision.
StorageView
Store at 25° C. Protect from light.
Darma
Fluconazole
Darma
Fluconazole
Indications
Vaginal candidiasis or thrush
Indication detailsView
Fluconazole is indicated for the treatment of vaginal candidiasis, oropharyngeal & esophageal candidiasis and cryptococcal meningitis. It is also effective for the treatment of urinary tract infection caused by candida, peritonitis and systemic candida infections (including candidemia, disseminated candidiasis and pneumonia).
Therapeutic classView
Drugs for subcutaneous and mycoses
PharmacologyView
Fluconazole is a triazole antifungal agent. It is a potent inhibitor of fungal cytochrome P-450 dependent enzymes. Cytochrome P-450 enzyme system is essential component of fungal cell membrane which is responsible for the synthesis of ergosterol.
DosageView
Adult (oral)-
Intravenous-
- Vaginal candidiasis: 150 mg as a single dose.
- Oropharyngeal candidiasis: 200 mg on the first day, followed by 100 mg once daily. Clinical evidence of this infection generally resolves within several days, but treatment should be continued for at least 2 weeks to decrease the likelihood of relapse.
- Esophageal candidiasis: 200 mg on the first day, followed by 100 mg once daily. Doses up to 400 mg/day may be used. Patients should be treated for a minimum of three weeks and for at least two weeks following resolution of symptoms.
- Systemic candida infections: Optimal therapeutic dosage and duration of therapy have not been established. Sometimes, doses of up to 400 mg daily have been used.
- Urinary tract infections caused by candida and peritonitis: 50-200 mg daily have been used.
- Cryptococcal meningitis: 400 mg on the first day, followed by 200 mg once daily.
- Prophylaxis in patients undergoing bone marrow transplantation: 400 mg once daily.
- Doses of 3-6 mg/kg daily have been used. Doses up to 12 mg/kg is recommended.
Intravenous-
- Adult: Invasive candidal infections including candidaemia and disseminated candidiasis and cryptococcal infections including meningitis, by IV, 400 mg initially then 200 mg daily, increased if necessary to 400 mg daily, treatment continued according to response (at least 6-8 weeks for cryptococcal meningitis)
- Child: 6-12 mg/kg daily (every 72 hours in neonate up to 2 weeks old, every 48 hours in neonate 2-4 weeks old); maximum 400 mg daily. Prevention of relapse of cryptococcal meningitis, by IV, 100-200 mg daily.
Side effectsView
Fluconazole is well tolerated. Most common side effects of using Fluconazole includes nausea, vomiting, abdominal pain, diarrhoea, headache and skin rash.
ContraindicationsView
Fluconazole should not be used in patients with known hypersensitivity to Fluconazole or to related triazole compounds.
PrecautionsView
Fluconazole should be administered with caution to patients having proarrhythmic conditions.
InteractionsView
Concomitant use of cyclosporin or phenytoin with Fluconazole increases the plasma level of cyclosporin or phenytoin. Concomitant use of Fluconazole & warfarin prolongs the prothrombin time. Rifampicin level is decreased when used with Fluconazole.
Pregnancy & lactationView
US FDA Pregnancy category of Fluconazole is C. So, Fluconazole should be avoided in pregnancy and lactation unless the potential benefits to the other outweigh the possible risks to the fetus.
StorageView
Keep in a dry place away from light and heat. Keep out of the reach of children.
Darven
Cilnidipine
Darven
Cilnidipine
Indications
Hypertension
Indication detailsView
Cilnidipine is indicated for the management of hypertension for end-organ protection. It is reported to be useful in elderly patients and in those with diabetes and albuminuria. Cilnidipine has been increasingly used in patients with chronic kidney disease
Hypertension is the term used to describe the presence of high blood pressure. The blood pressure is generated by the force of the blood pumped from the heart against the blood vessels. Thus hypertension is caused when there is too much pressure on the blood vessels and this effect can damage the blood vessel
Hypertension is the term used to describe the presence of high blood pressure. The blood pressure is generated by the force of the blood pumped from the heart against the blood vessels. Thus hypertension is caused when there is too much pressure on the blood vessels and this effect can damage the blood vessel
Therapeutic classView
Calcium-channel blockers
PharmacologyView
Cilnidipine is a dihydropyridine calcium-channel blocker. Cilnidipine binds to the dihydropy-ridine binding sites of the L-type voltage dependent calcium channel and inhibits Ca2+ influx across the cell membranes of vascular smooth muscle cells via this channel, consequently vascular smooth muscle is relaxed, causing vasodilation. Cilnidipine inhibits Ca2+ influx via N-type voltage dependent calcium channels in the sympathetic nerve cell membrane. The inhibition of Ca2+ influx via N-type voltage dependent calcium channel was observed over a similar range of drug concentrations to those inhibiting L-type voltage dependent Ca2+ channels. Consequently, release of norepinephrine from sympathetic nerve terminals would be inhibited. Cilnidipine is considered to suppress the reflex increase in heart rate after blood pressure reduction.
DosageView
Adults: 5-10 mg once daily after breakfast. Maximum dose: 20 mg once daily.
Pediatric use: The safety of Cilnidipine in pediatric patients has not been established.
Elderly use: Since the elderly may be more susceptible to hypotension, therapy should be initiated with the lowest possible dose (5 mg).
Pediatric use: The safety of Cilnidipine in pediatric patients has not been established.
Elderly use: Since the elderly may be more susceptible to hypotension, therapy should be initiated with the lowest possible dose (5 mg).
Side effectsView
The most common side effects of Cilnidipine are: Dizziness; flushing; headache; hypotension; peripheral oedema; palpitations; GI disturbances; increased micturition frequency; lethargy; eye pain; depression.
ContraindicationsView
Cilnidipine is contraindicated in patients with known sensitivity to Cilnidipine or any of the excipients or patients having cardiogenic shock, recent MI or acute unstable angina and severe aortic stenosis.
PrecautionsView
Cilnidipine should be administered with care in the following patients: patients with serious hepatic dysfunction, patients with a history of serious adverse reactions to calcium antagonists. During the discontinuation, the dosage should be gradually decreased under close observation.
InteractionsView
Other anti-hypertensive, antipsychotics that cause hypotension, quinidine, carbamazepine, phenytoin, rifampicin, cimetidine, erythromycin.
Pregnancy & lactationView
Cilnidipine should not be administered in pregnant woman or woman having possibilities of being pregnant. It is also advisable to avoid the administration of Cilnidipine to nursing mothers. However, if the administration is indispensable, the patient should be instructed to discontinue lactation.
StorageView
Store below 30°C, protected from light and moisture. Keep away from reach out of the children.
Darven
Cilnidipine
Darven
Cilnidipine
Indications
Hypertension
Indication detailsView
Cilnidipine is indicated for the management of hypertension for end-organ protection. It is reported to be useful in elderly patients and in those with diabetes and albuminuria. Cilnidipine has been increasingly used in patients with chronic kidney disease
Hypertension is the term used to describe the presence of high blood pressure. The blood pressure is generated by the force of the blood pumped from the heart against the blood vessels. Thus hypertension is caused when there is too much pressure on the blood vessels and this effect can damage the blood vessel
Hypertension is the term used to describe the presence of high blood pressure. The blood pressure is generated by the force of the blood pumped from the heart against the blood vessels. Thus hypertension is caused when there is too much pressure on the blood vessels and this effect can damage the blood vessel
Therapeutic classView
Calcium-channel blockers
PharmacologyView
Cilnidipine is a dihydropyridine calcium-channel blocker. Cilnidipine binds to the dihydropy-ridine binding sites of the L-type voltage dependent calcium channel and inhibits Ca2+ influx across the cell membranes of vascular smooth muscle cells via this channel, consequently vascular smooth muscle is relaxed, causing vasodilation. Cilnidipine inhibits Ca2+ influx via N-type voltage dependent calcium channels in the sympathetic nerve cell membrane. The inhibition of Ca2+ influx via N-type voltage dependent calcium channel was observed over a similar range of drug concentrations to those inhibiting L-type voltage dependent Ca2+ channels. Consequently, release of norepinephrine from sympathetic nerve terminals would be inhibited. Cilnidipine is considered to suppress the reflex increase in heart rate after blood pressure reduction.
DosageView
Adults: 5-10 mg once daily after breakfast. Maximum dose: 20 mg once daily.
Pediatric use: The safety of Cilnidipine in pediatric patients has not been established.
Elderly use: Since the elderly may be more susceptible to hypotension, therapy should be initiated with the lowest possible dose (5 mg).
Pediatric use: The safety of Cilnidipine in pediatric patients has not been established.
Elderly use: Since the elderly may be more susceptible to hypotension, therapy should be initiated with the lowest possible dose (5 mg).
Side effectsView
The most common side effects of Cilnidipine are: Dizziness; flushing; headache; hypotension; peripheral oedema; palpitations; GI disturbances; increased micturition frequency; lethargy; eye pain; depression.
ContraindicationsView
Cilnidipine is contraindicated in patients with known sensitivity to Cilnidipine or any of the excipients or patients having cardiogenic shock, recent MI or acute unstable angina and severe aortic stenosis.
PrecautionsView
Cilnidipine should be administered with care in the following patients: patients with serious hepatic dysfunction, patients with a history of serious adverse reactions to calcium antagonists. During the discontinuation, the dosage should be gradually decreased under close observation.
InteractionsView
Other anti-hypertensive, antipsychotics that cause hypotension, quinidine, carbamazepine, phenytoin, rifampicin, cimetidine, erythromycin.
Pregnancy & lactationView
Cilnidipine should not be administered in pregnant woman or woman having possibilities of being pregnant. It is also advisable to avoid the administration of Cilnidipine to nursing mothers. However, if the administration is indispensable, the patient should be instructed to discontinue lactation.
StorageView
Store below 30°C, protected from light and moisture. Keep away from reach out of the children.
Darvoni
Daclatasvir + Sofosbuvir
Darvoni
Daclatasvir + Sofosbuvir
Indications
Direct acting antiviral agent (DAA) against the hepatitis C virus
Indication detailsView
Sofosbuvir directly targets the Hepatitis C virus to stop it from making copies of itself in the liver. Sofosbuvir attaches itself to the genetic information, called RNA, to block the virus from multiplying. And Daclatasvir is a direct-acting antiviral agent (DAA) against the hepatitis C virus.
Therapeutic classView
Hepatic viral infections (Hepatitis C)
PharmacologyView
Sofosbuvir is an inhibitor of the hepatitis C virus (HCV) NS5B ribonucleic acid (RNA)-dependent RNA polymerase, which is essential for viral replication. Sofosbuvir is a nucleotide prodrug that undergoes intracellular metabolism to form the pharmacologically active uridine analog triphosphate (GS-461203), which can be incorporated into HCV RNA by the NS5B polymerase and acts as a chain terminator. In a biochemical assay, GS-461203 inhibited the polymerase activity of the recombinant NS5B from HCV genotype 1b, 2a, 3a and 4a with a 50% inhibitory concentration (IC50) value ranging from 0.7-2.6 micrometer. GS-461203 (the active metabolite of sofosbuvir) is not an inhibitor of human deoxyribonucleic acid (DNA) and RNA polymerases, nor an inhibitor of mitochondrial RNA polymerase.
Daclatasvir stops HCV viral RNA replication and protein translation by directly inhibiting HCV protein NS5A. NS5A is critical for HCV viral transcription and translation.
Daclatasvir stops HCV viral RNA replication and protein translation by directly inhibiting HCV protein NS5A. NS5A is critical for HCV viral transcription and translation.
Dasacent
Dasatinib
Dasacent
Dasatinib
Indications
Chronic myeloid leukaemia
Indication detailsView
Dasatinib is indicated for the treatment of adults with:
- Newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase.
- Chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.
- Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy.
Therapeutic classView
Targeted Cancer Therapy
PharmacologyView
Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.
DosageView
The recommended starting dosage of Dasatinib for:
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
- Chronic phase CML is 100 mg administered orally once daily.
- Accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL is 140 mg administered orally once daily.
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
Side effectsView
Reversible myelosuppression, neutropenia, anaemia, thrombocytopenia, fluid retention, pulmonary arterial HTN, QT prolongation, cardiac failure, arrhythmias, HTN, musculoskeletal pain, GI disturbances, headache, chills, fatigue, asthenia, myalgia, chest pain, arthralgia, pyrexia, mucositis, flushing, colitis, electrolyte disturbances, appetite and wt disturbances, rash, dermatitis, hyperhidrosis, pruritus, acne.
ContraindicationsView
Concomitant use with CYP3A4 inhibitors (e.g. atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole or grapefruit juice); CYP3A4 inducers (e.g. carbamazepine, dexamethasone, phenytoin, phenobarbital, rifampicin or St John's wort); antacid. Pregnancy.
PrecautionsView
Patients with predisposing factors for QT prolongation (e.g. congenital long QT syndrome, hypokalaemia, hypomagnesaemia, on antiarrhythmic therapy, or receiving cumulative high doses of anthracyclines). Hepatic impairment. Lactation.
InteractionsView
Concomitant use with drugs that have narrow therapeutic index (e.g. alfentanil, cisapride, ciclosporin, fentanyl, pimozide, quinidine, simvastatin, sirolimus, tacrolimus, ergot alkaloids) as it may increase the serum levels of these drugs. Increased risk of bleeding and thrombocytopenia with antiplatelet drugs, anticoagulants, and NSAIDs.
Pregnancy & lactationView
Pregnancy category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Pediatric usageView
Pediatric Use: The safety and efficacy of Dasatinib in patients less than 18 years of age have not been established.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Overdose effectsView
Symptoms: Significant platelet count reduction. Management: Closely monitor for myelosuppression. Supportive and symptomatic treatment.
StorageView
Dasatinib tablets should be stored at 20°C to 25°C
Dasacent
Dasatinib
Dasacent
Dasatinib
Indications
Chronic myeloid leukaemia
Indication detailsView
Dasatinib is indicated for the treatment of adults with:
- Newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase.
- Chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.
- Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy.
Therapeutic classView
Targeted Cancer Therapy
PharmacologyView
Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.
DosageView
The recommended starting dosage of Dasatinib for:
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
- Chronic phase CML is 100 mg administered orally once daily.
- Accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL is 140 mg administered orally once daily.
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
Side effectsView
Reversible myelosuppression, neutropenia, anaemia, thrombocytopenia, fluid retention, pulmonary arterial HTN, QT prolongation, cardiac failure, arrhythmias, HTN, musculoskeletal pain, GI disturbances, headache, chills, fatigue, asthenia, myalgia, chest pain, arthralgia, pyrexia, mucositis, flushing, colitis, electrolyte disturbances, appetite and wt disturbances, rash, dermatitis, hyperhidrosis, pruritus, acne.
ContraindicationsView
Concomitant use with CYP3A4 inhibitors (e.g. atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole or grapefruit juice); CYP3A4 inducers (e.g. carbamazepine, dexamethasone, phenytoin, phenobarbital, rifampicin or St John's wort); antacid. Pregnancy.
PrecautionsView
Patients with predisposing factors for QT prolongation (e.g. congenital long QT syndrome, hypokalaemia, hypomagnesaemia, on antiarrhythmic therapy, or receiving cumulative high doses of anthracyclines). Hepatic impairment. Lactation.
InteractionsView
Concomitant use with drugs that have narrow therapeutic index (e.g. alfentanil, cisapride, ciclosporin, fentanyl, pimozide, quinidine, simvastatin, sirolimus, tacrolimus, ergot alkaloids) as it may increase the serum levels of these drugs. Increased risk of bleeding and thrombocytopenia with antiplatelet drugs, anticoagulants, and NSAIDs.
Pregnancy & lactationView
Pregnancy category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Pediatric usageView
Pediatric Use: The safety and efficacy of Dasatinib in patients less than 18 years of age have not been established.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Overdose effectsView
Symptoms: Significant platelet count reduction. Management: Closely monitor for myelosuppression. Supportive and symptomatic treatment.
StorageView
Dasatinib tablets should be stored at 20°C to 25°C
Dasanix
Dasatinib
Dasanix
Dasatinib
Indications
Chronic myeloid leukaemia
Indication detailsView
Dasatinib is indicated for the treatment of adults with:
- Newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase.
- Chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.
- Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy.
Therapeutic classView
Targeted Cancer Therapy
PharmacologyView
Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.
DosageView
The recommended starting dosage of Dasatinib for:
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
- Chronic phase CML is 100 mg administered orally once daily.
- Accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL is 140 mg administered orally once daily.
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
Side effectsView
Reversible myelosuppression, neutropenia, anaemia, thrombocytopenia, fluid retention, pulmonary arterial HTN, QT prolongation, cardiac failure, arrhythmias, HTN, musculoskeletal pain, GI disturbances, headache, chills, fatigue, asthenia, myalgia, chest pain, arthralgia, pyrexia, mucositis, flushing, colitis, electrolyte disturbances, appetite and wt disturbances, rash, dermatitis, hyperhidrosis, pruritus, acne.
ContraindicationsView
Concomitant use with CYP3A4 inhibitors (e.g. atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole or grapefruit juice); CYP3A4 inducers (e.g. carbamazepine, dexamethasone, phenytoin, phenobarbital, rifampicin or St John's wort); antacid. Pregnancy.
PrecautionsView
Patients with predisposing factors for QT prolongation (e.g. congenital long QT syndrome, hypokalaemia, hypomagnesaemia, on antiarrhythmic therapy, or receiving cumulative high doses of anthracyclines). Hepatic impairment. Lactation.
InteractionsView
Concomitant use with drugs that have narrow therapeutic index (e.g. alfentanil, cisapride, ciclosporin, fentanyl, pimozide, quinidine, simvastatin, sirolimus, tacrolimus, ergot alkaloids) as it may increase the serum levels of these drugs. Increased risk of bleeding and thrombocytopenia with antiplatelet drugs, anticoagulants, and NSAIDs.
Pregnancy & lactationView
Pregnancy category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Pediatric usageView
Pediatric Use: The safety and efficacy of Dasatinib in patients less than 18 years of age have not been established.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Overdose effectsView
Symptoms: Significant platelet count reduction. Management: Closely monitor for myelosuppression. Supportive and symptomatic treatment.
StorageView
Dasatinib tablets should be stored at 20°C to 25°C
Dasanix
Dasatinib
Dasanix
Dasatinib
Indications
Chronic myeloid leukaemia
Indication detailsView
Dasatinib is indicated for the treatment of adults with:
- Newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase.
- Chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.
- Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy.
Therapeutic classView
Targeted Cancer Therapy
PharmacologyView
Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.
DosageView
The recommended starting dosage of Dasatinib for:
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
- Chronic phase CML is 100 mg administered orally once daily.
- Accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL is 140 mg administered orally once daily.
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
Side effectsView
Reversible myelosuppression, neutropenia, anaemia, thrombocytopenia, fluid retention, pulmonary arterial HTN, QT prolongation, cardiac failure, arrhythmias, HTN, musculoskeletal pain, GI disturbances, headache, chills, fatigue, asthenia, myalgia, chest pain, arthralgia, pyrexia, mucositis, flushing, colitis, electrolyte disturbances, appetite and wt disturbances, rash, dermatitis, hyperhidrosis, pruritus, acne.
ContraindicationsView
Concomitant use with CYP3A4 inhibitors (e.g. atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole or grapefruit juice); CYP3A4 inducers (e.g. carbamazepine, dexamethasone, phenytoin, phenobarbital, rifampicin or St John's wort); antacid. Pregnancy.
PrecautionsView
Patients with predisposing factors for QT prolongation (e.g. congenital long QT syndrome, hypokalaemia, hypomagnesaemia, on antiarrhythmic therapy, or receiving cumulative high doses of anthracyclines). Hepatic impairment. Lactation.
InteractionsView
Concomitant use with drugs that have narrow therapeutic index (e.g. alfentanil, cisapride, ciclosporin, fentanyl, pimozide, quinidine, simvastatin, sirolimus, tacrolimus, ergot alkaloids) as it may increase the serum levels of these drugs. Increased risk of bleeding and thrombocytopenia with antiplatelet drugs, anticoagulants, and NSAIDs.
Pregnancy & lactationView
Pregnancy category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Pediatric usageView
Pediatric Use: The safety and efficacy of Dasatinib in patients less than 18 years of age have not been established.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Overdose effectsView
Symptoms: Significant platelet count reduction. Management: Closely monitor for myelosuppression. Supportive and symptomatic treatment.
StorageView
Dasatinib tablets should be stored at 20°C to 25°C
Dasanix
Dasatinib
Dasanix
Dasatinib
Indications
Chronic myeloid leukaemia
Indication detailsView
Dasatinib is indicated for the treatment of adults with:
- Newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase.
- Chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.
- Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy.
Therapeutic classView
Targeted Cancer Therapy
PharmacologyView
Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.
DosageView
The recommended starting dosage of Dasatinib for:
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
- Chronic phase CML is 100 mg administered orally once daily.
- Accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL is 140 mg administered orally once daily.
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
Side effectsView
Reversible myelosuppression, neutropenia, anaemia, thrombocytopenia, fluid retention, pulmonary arterial HTN, QT prolongation, cardiac failure, arrhythmias, HTN, musculoskeletal pain, GI disturbances, headache, chills, fatigue, asthenia, myalgia, chest pain, arthralgia, pyrexia, mucositis, flushing, colitis, electrolyte disturbances, appetite and wt disturbances, rash, dermatitis, hyperhidrosis, pruritus, acne.
ContraindicationsView
Concomitant use with CYP3A4 inhibitors (e.g. atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole or grapefruit juice); CYP3A4 inducers (e.g. carbamazepine, dexamethasone, phenytoin, phenobarbital, rifampicin or St John's wort); antacid. Pregnancy.
PrecautionsView
Patients with predisposing factors for QT prolongation (e.g. congenital long QT syndrome, hypokalaemia, hypomagnesaemia, on antiarrhythmic therapy, or receiving cumulative high doses of anthracyclines). Hepatic impairment. Lactation.
InteractionsView
Concomitant use with drugs that have narrow therapeutic index (e.g. alfentanil, cisapride, ciclosporin, fentanyl, pimozide, quinidine, simvastatin, sirolimus, tacrolimus, ergot alkaloids) as it may increase the serum levels of these drugs. Increased risk of bleeding and thrombocytopenia with antiplatelet drugs, anticoagulants, and NSAIDs.
Pregnancy & lactationView
Pregnancy category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Pediatric usageView
Pediatric Use: The safety and efficacy of Dasatinib in patients less than 18 years of age have not been established.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Overdose effectsView
Symptoms: Significant platelet count reduction. Management: Closely monitor for myelosuppression. Supportive and symptomatic treatment.
StorageView
Dasatinib tablets should be stored at 20°C to 25°C
Dasatab
Dasatinib
Dasatab
Dasatinib
Indications
Chronic myeloid leukaemia
Indication detailsView
Dasatinib is indicated for the treatment of adults with:
- Newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase.
- Chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.
- Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy.
Therapeutic classView
Targeted Cancer Therapy
PharmacologyView
Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.
DosageView
The recommended starting dosage of Dasatinib for:
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
- Chronic phase CML is 100 mg administered orally once daily.
- Accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL is 140 mg administered orally once daily.
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
Side effectsView
Reversible myelosuppression, neutropenia, anaemia, thrombocytopenia, fluid retention, pulmonary arterial HTN, QT prolongation, cardiac failure, arrhythmias, HTN, musculoskeletal pain, GI disturbances, headache, chills, fatigue, asthenia, myalgia, chest pain, arthralgia, pyrexia, mucositis, flushing, colitis, electrolyte disturbances, appetite and wt disturbances, rash, dermatitis, hyperhidrosis, pruritus, acne.
ContraindicationsView
Concomitant use with CYP3A4 inhibitors (e.g. atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole or grapefruit juice); CYP3A4 inducers (e.g. carbamazepine, dexamethasone, phenytoin, phenobarbital, rifampicin or St John's wort); antacid. Pregnancy.
PrecautionsView
Patients with predisposing factors for QT prolongation (e.g. congenital long QT syndrome, hypokalaemia, hypomagnesaemia, on antiarrhythmic therapy, or receiving cumulative high doses of anthracyclines). Hepatic impairment. Lactation.
InteractionsView
Concomitant use with drugs that have narrow therapeutic index (e.g. alfentanil, cisapride, ciclosporin, fentanyl, pimozide, quinidine, simvastatin, sirolimus, tacrolimus, ergot alkaloids) as it may increase the serum levels of these drugs. Increased risk of bleeding and thrombocytopenia with antiplatelet drugs, anticoagulants, and NSAIDs.
Pregnancy & lactationView
Pregnancy category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Pediatric usageView
Pediatric Use: The safety and efficacy of Dasatinib in patients less than 18 years of age have not been established.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Overdose effectsView
Symptoms: Significant platelet count reduction. Management: Closely monitor for myelosuppression. Supportive and symptomatic treatment.
StorageView
Dasatinib tablets should be stored at 20°C to 25°C
Dasatab
Dasatinib
Dasatab
Dasatinib
Indications
Chronic myeloid leukaemia
Indication detailsView
Dasatinib is indicated for the treatment of adults with:
- Newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase.
- Chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.
- Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy.
Therapeutic classView
Targeted Cancer Therapy
PharmacologyView
Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.
DosageView
The recommended starting dosage of Dasatinib for:
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
- Chronic phase CML is 100 mg administered orally once daily.
- Accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL is 140 mg administered orally once daily.
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
Side effectsView
Reversible myelosuppression, neutropenia, anaemia, thrombocytopenia, fluid retention, pulmonary arterial HTN, QT prolongation, cardiac failure, arrhythmias, HTN, musculoskeletal pain, GI disturbances, headache, chills, fatigue, asthenia, myalgia, chest pain, arthralgia, pyrexia, mucositis, flushing, colitis, electrolyte disturbances, appetite and wt disturbances, rash, dermatitis, hyperhidrosis, pruritus, acne.
ContraindicationsView
Concomitant use with CYP3A4 inhibitors (e.g. atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole or grapefruit juice); CYP3A4 inducers (e.g. carbamazepine, dexamethasone, phenytoin, phenobarbital, rifampicin or St John's wort); antacid. Pregnancy.
PrecautionsView
Patients with predisposing factors for QT prolongation (e.g. congenital long QT syndrome, hypokalaemia, hypomagnesaemia, on antiarrhythmic therapy, or receiving cumulative high doses of anthracyclines). Hepatic impairment. Lactation.
InteractionsView
Concomitant use with drugs that have narrow therapeutic index (e.g. alfentanil, cisapride, ciclosporin, fentanyl, pimozide, quinidine, simvastatin, sirolimus, tacrolimus, ergot alkaloids) as it may increase the serum levels of these drugs. Increased risk of bleeding and thrombocytopenia with antiplatelet drugs, anticoagulants, and NSAIDs.
Pregnancy & lactationView
Pregnancy category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Pediatric usageView
Pediatric Use: The safety and efficacy of Dasatinib in patients less than 18 years of age have not been established.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Overdose effectsView
Symptoms: Significant platelet count reduction. Management: Closely monitor for myelosuppression. Supportive and symptomatic treatment.
StorageView
Dasatinib tablets should be stored at 20°C to 25°C
Dasatin
Dasatinib
Dasatin
Dasatinib
Indications
Chronic myeloid leukaemia
Indication detailsView
Dasatinib is indicated for the treatment of adults with:
- Newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase.
- Chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.
- Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy.
Therapeutic classView
Targeted Cancer Therapy
PharmacologyView
Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.
DosageView
The recommended starting dosage of Dasatinib for:
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
- Chronic phase CML is 100 mg administered orally once daily.
- Accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL is 140 mg administered orally once daily.
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
Side effectsView
Reversible myelosuppression, neutropenia, anaemia, thrombocytopenia, fluid retention, pulmonary arterial HTN, QT prolongation, cardiac failure, arrhythmias, HTN, musculoskeletal pain, GI disturbances, headache, chills, fatigue, asthenia, myalgia, chest pain, arthralgia, pyrexia, mucositis, flushing, colitis, electrolyte disturbances, appetite and wt disturbances, rash, dermatitis, hyperhidrosis, pruritus, acne.
ContraindicationsView
Concomitant use with CYP3A4 inhibitors (e.g. atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole or grapefruit juice); CYP3A4 inducers (e.g. carbamazepine, dexamethasone, phenytoin, phenobarbital, rifampicin or St John's wort); antacid. Pregnancy.
PrecautionsView
Patients with predisposing factors for QT prolongation (e.g. congenital long QT syndrome, hypokalaemia, hypomagnesaemia, on antiarrhythmic therapy, or receiving cumulative high doses of anthracyclines). Hepatic impairment. Lactation.
InteractionsView
Concomitant use with drugs that have narrow therapeutic index (e.g. alfentanil, cisapride, ciclosporin, fentanyl, pimozide, quinidine, simvastatin, sirolimus, tacrolimus, ergot alkaloids) as it may increase the serum levels of these drugs. Increased risk of bleeding and thrombocytopenia with antiplatelet drugs, anticoagulants, and NSAIDs.
Pregnancy & lactationView
Pregnancy category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Pediatric usageView
Pediatric Use: The safety and efficacy of Dasatinib in patients less than 18 years of age have not been established.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Overdose effectsView
Symptoms: Significant platelet count reduction. Management: Closely monitor for myelosuppression. Supportive and symptomatic treatment.
StorageView
Dasatinib tablets should be stored at 20°C to 25°C
Dasinib
Dasatinib
Dasinib
Dasatinib
Indications
Chronic myeloid leukaemia
Indication detailsView
Dasatinib is indicated for the treatment of adults with:
- Newly diagnosed Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in chronic phase.
- Chronic, accelerated, or myeloid or lymphoid blast phase Ph+ CML with resistance or intolerance to prior therapy including imatinib.
- Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) with resistance or intolerance to prior therapy.
Therapeutic classView
Targeted Cancer Therapy
PharmacologyView
Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.
DosageView
The recommended starting dosage of Dasatinib for:
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
- Chronic phase CML is 100 mg administered orally once daily.
- Accelerated phase CML, myeloid or lymphoid blast phase CML, or Ph+ ALL is 140 mg administered orally once daily.
In clinical studies, treatment with Dasatinib was continued until disease progression or until no longer tolerated by the patient. The effect of stopping treatment on long-term disease outcome after the achievement of a cytogenetic response (including complete cytogenetic response [CCyR]) or major molecular response (MMR) is not known.
Side effectsView
Reversible myelosuppression, neutropenia, anaemia, thrombocytopenia, fluid retention, pulmonary arterial HTN, QT prolongation, cardiac failure, arrhythmias, HTN, musculoskeletal pain, GI disturbances, headache, chills, fatigue, asthenia, myalgia, chest pain, arthralgia, pyrexia, mucositis, flushing, colitis, electrolyte disturbances, appetite and wt disturbances, rash, dermatitis, hyperhidrosis, pruritus, acne.
ContraindicationsView
Concomitant use with CYP3A4 inhibitors (e.g. atazanavir, clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, telithromycin, voriconazole or grapefruit juice); CYP3A4 inducers (e.g. carbamazepine, dexamethasone, phenytoin, phenobarbital, rifampicin or St John's wort); antacid. Pregnancy.
PrecautionsView
Patients with predisposing factors for QT prolongation (e.g. congenital long QT syndrome, hypokalaemia, hypomagnesaemia, on antiarrhythmic therapy, or receiving cumulative high doses of anthracyclines). Hepatic impairment. Lactation.
InteractionsView
Concomitant use with drugs that have narrow therapeutic index (e.g. alfentanil, cisapride, ciclosporin, fentanyl, pimozide, quinidine, simvastatin, sirolimus, tacrolimus, ergot alkaloids) as it may increase the serum levels of these drugs. Increased risk of bleeding and thrombocytopenia with antiplatelet drugs, anticoagulants, and NSAIDs.
Pregnancy & lactationView
Pregnancy category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).
Pediatric usageView
Pediatric Use: The safety and efficacy of Dasatinib in patients less than 18 years of age have not been established.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Geriatric Use: No differences in confirmed Complete Cytogenetic Response (cCCyR) and MMR were observed between older and younger patients. Of the 2712 patients in clinical studies of Dasatinib, 617 (23%) were 65 years of age and older, and 123 (5%) were 75 years of age and older. While the safety profile of Dasatinib in the geriatric population was similar to that in the younger population, patients aged 65 years and older are more likely to experience the commonly reported adverse reactions of fatigue, pleural effusion, diarrhea, dyspnea, cough, lower gastrointestinal hemorrhage, and appetite disturbance, and more likely to experience the less frequently reported adverse reactions of abdominal distention, dizziness, pericardial effusion, congestive heart failure, hypertension, pulmonary edema, and weight decrease, and should be monitored closely.
Hepatic Impairment: No dosage adjustment is necessary in patients with hepatic impairment. Caution is recommended when administering Dasatinib to patients with hepatic impairment.
Renal Impairment: There are currently no clinical studies with Dasatinib in patients with impaired renal function. Less than 4% of dasatinib and its metabolites are excreted via the kidney.
Overdose effectsView
Symptoms: Significant platelet count reduction. Management: Closely monitor for myelosuppression. Supportive and symptomatic treatment.
StorageView
Dasatinib tablets should be stored at 20°C to 25°C
Daunobin
Daunorubicin
Daunobin
Daunorubicin
Indications
Leukemia
Indication detailsView
Daunorubicin in combination with other approved anticancer drugs is indicated for remission induction in acute nonlymphocytic leukemia (myelogenous, monocytic, erythroid) of adults and for remission induction in acute lymphocytic leukemia of children and adults.
Therapeutic classView
Cytotoxic Chemotherapy
PharmacologyView
Daunorubicin has antimitotic and cytotoxic activity through a number of proposed mechanisms of action. It forms complexes with DNA by intercalation between base pairs. It inhibits topoisomerase II activity by stabilizing the DNA- topoisomerase II complex, preventing the religation portion of the ligation- religation reaction that topoisomerase II catalyzes. Single strand and double-strand DNA breaks result. It may also inhibit polymerase activity, affect the regulation of gene expression, and produce free radical damage to DNA. It possesses an antitumor effect against a wide spectrum of animal tumors, either grafted or spontaneous.
Distribution: Daunorubicin is rapidly and widely distributed in tissues, with the highest levels in the spleen, kidneys, liver, lungs and heart. The drug binds to many cellular components, particularly nucleic acids. There is no evidence that it crosses the blood-brain barrier, but the drug apparently crosses the placenta.
Metabolism and Elimination: Daunorubicin is extensively metabolized in the liver and other tissues, mainly by cytoplasmic aldo-keto reductases, producing daunorubicinol, the major metabolite which has antineoplastic activity. Approximately 40% of the drug in the plasma is present as daunorubicinol within 30 minutes and 60% in 4 hours after a dose of Daunorubicin. Further metabolism via reduction cleavage of the glycosidic bond, 4-O demethylation, and conjugation with both sulfate and glucuronide have been demonstrated. Simple glycosidic cleavage of Daunorubicin or Daunorubicinol is not a significant metabolic pathway in man. Twenty-five percent of an administered dose of Daunorubicin is eliminated in an active form by urinary excretion and an estimated 40% by biliary excretion.
Distribution: Daunorubicin is rapidly and widely distributed in tissues, with the highest levels in the spleen, kidneys, liver, lungs and heart. The drug binds to many cellular components, particularly nucleic acids. There is no evidence that it crosses the blood-brain barrier, but the drug apparently crosses the placenta.
Metabolism and Elimination: Daunorubicin is extensively metabolized in the liver and other tissues, mainly by cytoplasmic aldo-keto reductases, producing daunorubicinol, the major metabolite which has antineoplastic activity. Approximately 40% of the drug in the plasma is present as daunorubicinol within 30 minutes and 60% in 4 hours after a dose of Daunorubicin. Further metabolism via reduction cleavage of the glycosidic bond, 4-O demethylation, and conjugation with both sulfate and glucuronide have been demonstrated. Simple glycosidic cleavage of Daunorubicin or Daunorubicinol is not a significant metabolic pathway in man. Twenty-five percent of an administered dose of Daunorubicin is eliminated in an active form by urinary excretion and an estimated 40% by biliary excretion.
DosageView
Parenteral drug products should be inspected visually for particulate matter prior to administration.
Representative Dose Schedules and Combination for the Approved Indication of Remission Induction in Adult Acute Nonlymphocytic Leukemia: In Combination: For patients under age 60, Daunorubicin 45 mg/m2/day IV on days 1, 2, and 3 of the first course and on days 1, 2 of subsequent courses AND cytosine arabinoside 100 mg/m2/day IV infusion daily for 7 days for the first course and for 5 days for subsequent courses. For patients 60 years of age and above, Daunorubicin 30 mg/m2/day IV on days 1, 2, and 3 of the first course and on days 1, 2 of subsequent courses AND cytosine arabinoside 100 mg/m2/day IV infusion daily for 7 days for the first course and for 5 days for subsequent courses. This Daunorubicin dose-reduction is based on a single study and may not be appropriate if optimal supportive care is available.
Representative Dose Schedule and Combination for the Approved Indication of Remission Induction in Pediatric Acute Lymphocytic Leukemia: In Combination: Daunorubicin 25 mg/m2 IV on day 1 every week, Vincristine 1.5 mg/m2 IV on day 1 every week, prednisone 40 mg/m2 PO daily. Generally, a complete remission will be obtained within four such courses of therapy; however, if after four courses the patient is in partial remission, an additional one or, if necessary, two courses may be given in an effort to obtain a complete remission. In children less than 2 years of age or below 0.5 m2 body surface area, it has been recommended that the Daunorubicin dosage calculation should be based on weight (1 mg/kg) instead of body surface area.
Representative Dose Schedules and Combination for the Approved Indication of Remission Induction in Adult Acute Lymphocytic Leukemia: In Combination: Daunorubicin 45 mg/m2/day IV on days 1, 2, and 3 and Vincristine 2 mg IV on days 1, 8, and 15; prednisone 40 mg/m2/day PO on days 1 through 22, then tapered between days 22 to 29; L-asparaginase 500 IU/kg/day x 10 days IV on days 22 through 32. Or, as directed by the registered physicians.
Representative Dose Schedules and Combination for the Approved Indication of Remission Induction in Adult Acute Nonlymphocytic Leukemia: In Combination: For patients under age 60, Daunorubicin 45 mg/m2/day IV on days 1, 2, and 3 of the first course and on days 1, 2 of subsequent courses AND cytosine arabinoside 100 mg/m2/day IV infusion daily for 7 days for the first course and for 5 days for subsequent courses. For patients 60 years of age and above, Daunorubicin 30 mg/m2/day IV on days 1, 2, and 3 of the first course and on days 1, 2 of subsequent courses AND cytosine arabinoside 100 mg/m2/day IV infusion daily for 7 days for the first course and for 5 days for subsequent courses. This Daunorubicin dose-reduction is based on a single study and may not be appropriate if optimal supportive care is available.
Representative Dose Schedule and Combination for the Approved Indication of Remission Induction in Pediatric Acute Lymphocytic Leukemia: In Combination: Daunorubicin 25 mg/m2 IV on day 1 every week, Vincristine 1.5 mg/m2 IV on day 1 every week, prednisone 40 mg/m2 PO daily. Generally, a complete remission will be obtained within four such courses of therapy; however, if after four courses the patient is in partial remission, an additional one or, if necessary, two courses may be given in an effort to obtain a complete remission. In children less than 2 years of age or below 0.5 m2 body surface area, it has been recommended that the Daunorubicin dosage calculation should be based on weight (1 mg/kg) instead of body surface area.
Representative Dose Schedules and Combination for the Approved Indication of Remission Induction in Adult Acute Lymphocytic Leukemia: In Combination: Daunorubicin 45 mg/m2/day IV on days 1, 2, and 3 and Vincristine 2 mg IV on days 1, 8, and 15; prednisone 40 mg/m2/day PO on days 1 through 22, then tapered between days 22 to 29; L-asparaginase 500 IU/kg/day x 10 days IV on days 22 through 32. Or, as directed by the registered physicians.
Side effectsView
Dose-limiting toxicity includes myelosuppression and cardiotoxicity. Other reactions include:
- Cutaneous: Reversible alopecia occurs in most patients. Rash, contact dermatitis and urticaria have occurred rarely.
- Gastrointestinal: Acute nausea and vomiting occur but are usually mild. Antiemetic therapy may be of some help. Mucositis may occur 3 to 7 days after administration. Diarrhea and abdominal pain have occasionally been reported.
- Local: If extravasation occurs during administration, severe local tissue necrosis, severe cellulitis, thrombophlebitis or painful induration can result.
- Acute Reactions: Rarely, anaphylactoid reaction, fever, and chills can occur. Hyperuricemia may occur, especially in patients with leukemia, and serum uric acid levels should be monitored.
ContraindicationsView
It is contraindicated in patients with known hypersensitivity to Daunorubicin or any other components of this product.
PrecautionsView
Therapy with Daunorubicin requires close patient observation and frequent complete blood-count determinations. Cardiac, renal, and hepatic function should be evaluated prior to each course of treatment. Appropriate measures must be taken to control any systemic infection before beginning therapy with Daunorubicin. It may transiently impart a red coloration to the urine after administration, and patients should be advised to expect this.
Daunorubicin Hydrochloride Injection must be given into a rapidly flowing intravenous infusion. It must never be given by the intramuscular or subcutaneous route. Severe local tissue necrosis will occur if there is extravasation during administration.
Myocardial toxicity manifested in its most severe form by potentially fatal congestive heart failure may occur either during therapy or months to years after termination of therapy. The incidence of myocardial toxicity increases after a total cumulative dose exceeding 400 to 550 mg/m2 in adults, 300 mg/m2 in children more than 2 years of age, or 10 mg/kg in children less than 2 years of age.
Severe myelosuppression occurs when used in therapeutic doses; this may lead to infection or hemorrhage.
It is recommended that Daunorubicin Hydrochloride be administered only by physicians who are experienced in leukemia chemotherapy and in facilities with laboratory and supportive resources adequate to monitor drug tolerance and protect and maintain a patient compromised by drug toxicity. The physician and institution must be capable of responding rapidly and completely to severe hemorrhagic conditions and/or overwhelming infection.
Dosage should be reduced in patients with impaired hepatic or renal function.
Daunorubicin Hydrochloride Injection must be given into a rapidly flowing intravenous infusion. It must never be given by the intramuscular or subcutaneous route. Severe local tissue necrosis will occur if there is extravasation during administration.
Myocardial toxicity manifested in its most severe form by potentially fatal congestive heart failure may occur either during therapy or months to years after termination of therapy. The incidence of myocardial toxicity increases after a total cumulative dose exceeding 400 to 550 mg/m2 in adults, 300 mg/m2 in children more than 2 years of age, or 10 mg/kg in children less than 2 years of age.
Severe myelosuppression occurs when used in therapeutic doses; this may lead to infection or hemorrhage.
It is recommended that Daunorubicin Hydrochloride be administered only by physicians who are experienced in leukemia chemotherapy and in facilities with laboratory and supportive resources adequate to monitor drug tolerance and protect and maintain a patient compromised by drug toxicity. The physician and institution must be capable of responding rapidly and completely to severe hemorrhagic conditions and/or overwhelming infection.
Dosage should be reduced in patients with impaired hepatic or renal function.
InteractionsView
The use of Daunorubicin in a patient who has previously received Doxorubicin increases the risk of cardiotoxicity. Daunorubicin should not be used in patients who have previously received the recommended maximum cumulative doses of Doxorubicin or Daunorubicin. Cyclophosphamide used concurrently with Daunorubicin may also result in increased cardiotoxicity. Dosage reduction of Daunorubicin may be required when used concurrently with other myelosuppressive agents. Hepatotoxic medications, such as high-dose Methotrexate, may impair liver function and increase the risk of toxicity.
Pregnancy & lactationView
Pregnancy Category D. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Daunorubicin, mothers should be advised to discontinue nursing during Daunorubicin therapy.
ReconstitutionView
The sterile vial contents provide 20 mg of Daunorubicin, with 5 mg of Daunorubicin per ml. The desired dose is withdrawn into a syringe containing 10 ml to 15 ml of 0.9% sodium chloride injection, USP and then injected into the tubing or sidearm in a rapidly flowing IV infusion of 5% Dextrose injection, USP or 0.9% Sodium Chloride Injection, USP. Daunorubicin Hydrochloride should not be administered mixed with other drugs or heparin.
StorageView
Store unopened vials in the refrigerator, 2°-8°C. Contains no preservatives. Discard unused portions. Protect from light. If Daunorubicin contacts the skin or mucosae, the area should be washed thoroughly with soap and water. Procedures for proper handling and disposal of anticancer drugs should be considered.
Davycal
Calcium Orotate
Davycal
Calcium Orotate
Indications
Calcium suppliment
Indication detailsView
This medication is used to prevent or treat low blood calcium levels in people who do not get enough calcium from their diets. To fulfill the calcium deficiency or meet extra need of calcium, it may be used in conditions like osteoporosis osteomalacia, rickets, latent tetany, postmenopausal osteoporosis, senile osteoporosis, juvenile osteoporosis, drug (phenytoin, phenobarbital, or prednisone) induced osteoporosis, pregnancy and lactation, premenstrual syndrome (PMS), hypoparathyroidism and hip joint plastic surgery.
Calcium Orotate acts against a number of inflammatory diseases like arthritis, psoriasis, lupus, spondylitis, various cardiovascular ailments, encephalitis, retinitis, phlebitis, colitis, and multiple sclerosis. Calcium Orotate helps in controlling weight by suppressing the habit of frequent appetite of chronic overeaters. It is also beneficial in reducing the effects of mood swings and is proved to be quite effective in cognitive enhancement. Calcium Orotate protects the heart by enhancing the efficiency of cardiac muscles. Recent studies on calcium orotate indicate its potential to minimize the risk of colon cancer.
Calcium Orotate acts against a number of inflammatory diseases like arthritis, psoriasis, lupus, spondylitis, various cardiovascular ailments, encephalitis, retinitis, phlebitis, colitis, and multiple sclerosis. Calcium Orotate helps in controlling weight by suppressing the habit of frequent appetite of chronic overeaters. It is also beneficial in reducing the effects of mood swings and is proved to be quite effective in cognitive enhancement. Calcium Orotate protects the heart by enhancing the efficiency of cardiac muscles. Recent studies on calcium orotate indicate its potential to minimize the risk of colon cancer.
Therapeutic classView
Minerals in bone formation, Specific mineral preparations
PharmacologyView
This contains Calcium Orotate, a calcium supplement with a functional amino acid chelating ligand- orotic acid. Orotic acid assists the transport of calcium through cellular membrane structures, thus facilitating the intracellular uptake of calcium, particularly in bone. Calcium Orotate also helps in the maintenance of healthy cartilage. Furthermore, Orotate is involved in the synthesis of DNA (deoxyribonucleic acid) and RNA (ribonucleic acid) of the various calcium supplements on the market, Calcium Orotate gets high marks because of the compound's ability to penetrate complex cell membranes so that it can be metabolized in cartilage.
DosageView
Calcium Orotate 400 mg: As an addition to the daily diet, 2-3 tablets are usually recommended with meal or as directed by a physician.
Calcium Orotate 740 mg: As an addition to the daily diet, 1-2 tablets are usually recommended with meal or as directed by a physician.
Calcium Orotate 740 mg: As an addition to the daily diet, 1-2 tablets are usually recommended with meal or as directed by a physician.
Side effectsView
Bloating and swelling in the abdomen are common side effects of Calcium Orotate. Loss of appetite, upset stomach, constipation, nausea, vomiting, unusual weight loss, increased thirst/urination, weakness, unusual tiredness, formation of kidney stones may occur infrequently.
ContraindicationsView
Calcium Orotate is contraindicated in conditions like incomplete or infrequent bowel movements, kidney stone, kidney disease, increased activity of the parathyroid gland, high amount of Calcium in urine, high amount of Calcium in the blood, extreme loss of body water.
PrecautionsView
Before taking Calcium Orotate, precaution is needed if the patient is allergic to Calcium Orotate. This drug may contain inactive ingredients, which can cause allergic reactions or other problems. Precaution is needed before using this drug in kidney disease, kidney stones, little or no stomach acid (achlorhydria), heart disease, disease of the pancreas, sarcoidosis difficulty absorbing nutrition from food (malabsorption syndrome).
InteractionsView
Calcium can decrease absorption of the following drugs when taken together: biphosphonates (e.g., alendronate), quinolone antibiotics (e.g., ciprofloxacin, levofloxacin), and tetracycline antibiotics (e.g., doxycycline, minocycline), levothyroxine, phenytoin (an anticonvulsant), and tiludronate disodium (to treat Paget's disease). Thiazide-type diuretics can interact with Calcium supplements, increasing the risks of hypercalcemia and hypercalciuria. Both aluminum- and magnesium-containing antacids increase urinary calcium excretion. Mineral oil and stimulant laxatives decrease calcium absorption. Glucocorticoids, such as prednisone, can cause calcium depletion and eventually osteoporosis when they are used for months. Oral contraceptives as well as estrogen compounds reduce calcium. Anti-inflammatories such as NSAIDs, Aspirin, Ibuprofen deplete calcium. Corticosteroids deplete calcium.
Pregnancy & lactationView
Women who are pregnant and breast-feeding need more calcium. Pregnancy related high blood pressure is a common and serious risk for women and their babies, and taking supplemental forms of Calcium Orotate can help to reduce this risk.
StorageView
Keep out of the reach of children. Keep in a cool & dry place. Protect from light.
Daxetin
Dapoxetine Hydrochloride
Daxetin
Dapoxetine Hydrochloride
Indications
Premature ejaculation
Indication detailsView
Indicated for the treatment of premature ejaculation (PE) in men 18 to 64 years of age, who have all of the following:
- Persistent or recurrent ejaculation with minimal sexual stimulation before, on or shortly after penetration and before the patient wishes.
- Marked personal distress or interpersonal difficulty as a consequence of PE and poor control over ejaculation.
Therapeutic classView
Drugs for Erectile Dysfunction
PharmacologyView
The mechanism of action is thought to be related to inhibition of neuronal reuptake of serotonin and subsequent potentiation of serotonin activity. The central ejaculatory neural circuit comprises spinal and cerebral areas that form a highly interconnected network. The sympathetic, parasympathetic, and somatic spinal centers, under the influence of sensory genital and cerebral stimuli integrated and processed at the spinal cord level, act in synergy to command physiologic events occurring during ejaculation. Experimental evidence indicates that serotonin (5-HT), throughout brain descending pathways, exerts an inhibitory role on ejaculation. To date, three 5-HT receptor subtypes 5-HT(1A), 5-HT(1B), and 5-HT(2C) have been postulated to mediate 5-HT's modulating activity on ejaculation.
DosageView
Adult (18 to 64 years of age): The recommended starting dose for all patients is 30 mg, taken as needed approximately 1 to 3 hours prior to sexual activity. If the effect of 30 mg is insufficient and the side effects are acceptable, the dose may be increased to the maximum recommended dose of 60 mg. The maximum recommended dosing frequency is one dose every 24 hours.
Side effectsView
Dizziness, Headache, Somnolence, Tremor, Blurred vision, Tinnitus, Sinus congestion, Nausea, Diarrhea, Abdominal pain, Dry mouth, Fatigue, Insomnia, Hypertension.
ContraindicationsView
- Patients with known hypersensitivity to Dapoxetine Hydrochloride.
- Patients with significant pathological cardiac conditions such as heart failure (NYHA class II-IV), conduction abnormalities (second or third degree AV block or sick sinus syndrome) not treated with a permanent pacemaker, significant ischemic heart disease of significant valvular disease.
- Concomitant treatment with monoamine oxidase inhibitors (MAOIs), thioridazine. Similarly, MAOIs or thioridazine should not be administered within 7 days after Dapoxetine has been discontinued.
- Concomitant treatment with serotonin reuptake inhibitors (SSRIs), serotonin-norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs) or other medicinal/herbal products with serotonergic effects or within 14 days of discontinuing treatment with these medicinal/herbal products.
PrecautionsView
Patient with bleeding disorders, epilepsy, susceptibility to angle-closure glaucoma or raised intraocular pressure. Not intended for use in women. Known CYP2D6 poor metabolisers.
InteractionsView
CNS active medicinal products: The use of Dapoxetine in combination with CNS active medicinal products has not been systematically evaluated in patients with premature ejaculation. Consequently, caution is advised if the concomitant administration of Dapoxetine and such medicinal products is required.
PDE5 inhibitors: Tadalafil did not affect the pharmacokinetics of Dapoxetine. Sildenafil caused slight changes in Dapoxetine pharmacokinetics, which are not expected to be clinically significant. However, Dapoxetine should be prescribed with caution in patients who use PDE5 inhibitors due to possible reduced orthostatic tolerance.
Tamsulosin: Concomitant administration of single or multiple doses of 30 mg or 60 mg Dapoxetine to patients receiving daily doses of Tamsulosin did not result in changes in the pharmacokinetics of Tamsulosin. However, Dapoxetine should be prescribed with caution in patients who use alpha adrenergic receptor antagonists due to possible reduced orthostatic tolerance.
Warfarin: There are no data evaluating the effect of chronic use of Warfarin with Dapoxetine; therefore, caution is advised when Dapoxetine is used in patients taking Warfarin chronically.
Ethanol: Concomitant use of alcohol and Dapoxetine could increase the chance or severity of adverse reactions such as dizziness, drowsiness, slow reflexes, or altered judgment. Combining alcohol with Dapoxetine may increase these alcohol-related effects and may also enhance neurocardiogenic adverse events such as syncope, thereby increasing the risk of accidental injury; therefore, patients should be advised to avoid alcohol while taking Dapoxetine.
PDE5 inhibitors: Tadalafil did not affect the pharmacokinetics of Dapoxetine. Sildenafil caused slight changes in Dapoxetine pharmacokinetics, which are not expected to be clinically significant. However, Dapoxetine should be prescribed with caution in patients who use PDE5 inhibitors due to possible reduced orthostatic tolerance.
Tamsulosin: Concomitant administration of single or multiple doses of 30 mg or 60 mg Dapoxetine to patients receiving daily doses of Tamsulosin did not result in changes in the pharmacokinetics of Tamsulosin. However, Dapoxetine should be prescribed with caution in patients who use alpha adrenergic receptor antagonists due to possible reduced orthostatic tolerance.
Warfarin: There are no data evaluating the effect of chronic use of Warfarin with Dapoxetine; therefore, caution is advised when Dapoxetine is used in patients taking Warfarin chronically.
Ethanol: Concomitant use of alcohol and Dapoxetine could increase the chance or severity of adverse reactions such as dizziness, drowsiness, slow reflexes, or altered judgment. Combining alcohol with Dapoxetine may increase these alcohol-related effects and may also enhance neurocardiogenic adverse events such as syncope, thereby increasing the risk of accidental injury; therefore, patients should be advised to avoid alcohol while taking Dapoxetine.
Pregnancy & lactationView
Dapoxetine is not indicated for use by women. It is not known either dapoxetine or its metabolites are excreted through human breast milk.
Overdose effectsView
There were no unexpected adverse events in a clinical pharmacology study of Dapoxetine with daily doses up to 240 mg. In general, symptoms of overdose with SSRIs include serotonin-mediated adverse reactions such as somnolence, gastrointestinal disturbances such as nausea and vomiting, tachycardia, tremor, agitation and dizziness. In cases of overdose, standard supportive measures should be adopted as required.
StorageView
Store below 30°C. Protect from light and moisture. Keep out of reach of children