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Powercef
Ceftriaxone Sodium
Powercef
Ceftriaxone Sodium
Indications
Urinary tract infection
Indication detailsView
Ceftriaxone is indicated for the treatment of the following major infections:
- Lower respiratory tract infections
- Acute Bacterial Otitis Media
- Skin and skin structure infections
- Urinary tract infections
- Gonorrhea
- Bacterial Septicemia
- Bone and joint infections
- Meningitis
- Prevention of postoperative infections
- Perioperative prophylaxis of infections associated with surgery
Therapeutic classView
Third generation Cephalosporins
PharmacologyView
Ceftriaxone is a 3rd generation broad-spectrum parenteral cephalosporin antibiotic. It has potent bactericidal activity against a wide range of Gram-positive and Gram-negative organisms. Like other cephalosporins and penicillins, Ceftriaxone kills bacteria by interfering with the synthesis of the bacterial cell wall. Ceftriaxone has a high degree of stability in the presence of beta lactamases. A remarkable feature of Ceftriaxone is its relatively long plasma elimination half-life of about 6 to 9 hours, which makes single or once-daily dosage of the drug appropriate for most patients. Ceftriaxone is not metabolized in the body. About 40-65% of a dose of Ceftriaxone is excreted unchanged in the urine; the remainder is excreted in the bile and ultimately found in the feces as unchanged drug and microbiologically inactive compound. The drug is highly protein bound (95%).
DosageView
Adult: The usual dose is 1 to 2 gm by intravenous or intramuscular administration once a day (or in equally divided doses twice a day).
- Pneumonia, Bronchitis, Acute bacterial otitis media, Skin and skin structure infection, Urinary tract infections, Bacterial Septicemia, Bone and joint infections, Meningitis: 1 to 2 g IV or IM once a day (or in equally divided doses twice a day); Maximum dose: 4 gm/day
- Uncomplicated gonococcal infections: 250 mg IM as a single dose
- Surgical prophylaxis: 1 g IV as a single dose 30 to 120 minutes before surgery
- Pneumonia, Bronchitis, Skin and skin structure infection, Urinary tract infections, Bacterial Septicemia, Bone and joint infections: 50 to 75 mg/kg IV or IM once a day (or in equally divided doses twice a day); Maximum dose: 2 gm/day
- Acute bacterial otitis media: 50 mg/kg IM in single dose; Maximum dose: 1 gm/day
- Meningitis: 100 mg/kg IV or IM in single daily dose or (or in equally divided doses twice a day); Maximum dose: 4 gm/day
AdministrationView
Preparation of Solutions for Intramuscular / Intravenous Injections:
- For Intramuscular Injection: 250 mg or 500 mg Ceftriaxone should be dissolved in 2 ml Lidocaine HCI 1% injection or 1 g Ceftriaxone in 3.5 ml of Lidocaine HCI 1% injection.
- For Intravenous Injection: 250 mg or 500 mg Ceftriaxone should be dissolved in 5 ml of Water for injection or 1 g Ceftriaxone in 10 ml of Water for injection USP or 2 g Ceftriaxone in 20 ml of Water for injection.
Side effectsView
Ceftriaxone is generally well tolerated. A few side effects such as gastro-intestinal effects including diarrhea, nausea and vomiting, stomatitis and glossitis; cutaneous reactions including rash, pruritus, urticaria, edema and erythema multiforme; hematologic reactions including eosinophilia, thrombocytopenia, leucopenia, anemia and neutropenia; hepatic reactions including elevations of SGOT or SGPT, bilirubinemia; CNS reactions including nervousness, confusion, sleep disturbances, headache, hyperactivity, convulsion, hypertonia and dizziness were reported. Local phlebitis occurs rarely following intravenous administration but can be minimized by slow injections over 2-4 minutes.
ContraindicationsView
Ceftriaxone should not be given to patients with a history of hypersensitivity to cephalosporin antibiotics.
PrecautionsView
As with other cephalosporins, anaphylactic shock cannot be ruled out even if a thorough patient history is taken. Anaphylactic shock requires immediate countermeasures such as intravenous epinephrine followed by a glucocorticoid. In rare cases, shadows suggesting sludge have been detected by sonograms of the gallbladder. This condition was reversible on discontinuation or completion of Ceftriaxone therapy. Even if such findings are associated with pain, conservative, nonsurgical management is recommended. During prolonged treatment the blood picture should be checked at regular intervals.
InteractionsView
No drug interactions have been reported.
Pregnancy & lactationView
Its safety in human pregnancy has not been established. Therefore, it should not be used in pregnancy unless absolutely indicated. Low concentrations of Ceftriaxone are excreted in human milk. Caution should be exercised when Ceftriaxone is administered to a lactating mother.
Pediatric usageView
Ceftriaxone must not be given to neonates if the neonates is premature and newborn (up to 28 days of age).
Overdose effectsView
There is no specific antidote. Treatment of overdosage should be symptomatic.
StorageView
Vial store in a cool, dry place (below 30° C), away from light & moisture. Keep out of the reach of children.
Powercef
Ceftriaxone Sodium
Powercef
Ceftriaxone Sodium
Indications
Urinary tract infection
Indication detailsView
Ceftriaxone is indicated for the treatment of the following major infections:
- Lower respiratory tract infections
- Acute Bacterial Otitis Media
- Skin and skin structure infections
- Urinary tract infections
- Gonorrhea
- Bacterial Septicemia
- Bone and joint infections
- Meningitis
- Prevention of postoperative infections
- Perioperative prophylaxis of infections associated with surgery
Therapeutic classView
Third generation Cephalosporins
PharmacologyView
Ceftriaxone is a 3rd generation broad-spectrum parenteral cephalosporin antibiotic. It has potent bactericidal activity against a wide range of Gram-positive and Gram-negative organisms. Like other cephalosporins and penicillins, Ceftriaxone kills bacteria by interfering with the synthesis of the bacterial cell wall. Ceftriaxone has a high degree of stability in the presence of beta lactamases. A remarkable feature of Ceftriaxone is its relatively long plasma elimination half-life of about 6 to 9 hours, which makes single or once-daily dosage of the drug appropriate for most patients. Ceftriaxone is not metabolized in the body. About 40-65% of a dose of Ceftriaxone is excreted unchanged in the urine; the remainder is excreted in the bile and ultimately found in the feces as unchanged drug and microbiologically inactive compound. The drug is highly protein bound (95%).
DosageView
Adult: The usual dose is 1 to 2 gm by intravenous or intramuscular administration once a day (or in equally divided doses twice a day).
- Pneumonia, Bronchitis, Acute bacterial otitis media, Skin and skin structure infection, Urinary tract infections, Bacterial Septicemia, Bone and joint infections, Meningitis: 1 to 2 g IV or IM once a day (or in equally divided doses twice a day); Maximum dose: 4 gm/day
- Uncomplicated gonococcal infections: 250 mg IM as a single dose
- Surgical prophylaxis: 1 g IV as a single dose 30 to 120 minutes before surgery
- Pneumonia, Bronchitis, Skin and skin structure infection, Urinary tract infections, Bacterial Septicemia, Bone and joint infections: 50 to 75 mg/kg IV or IM once a day (or in equally divided doses twice a day); Maximum dose: 2 gm/day
- Acute bacterial otitis media: 50 mg/kg IM in single dose; Maximum dose: 1 gm/day
- Meningitis: 100 mg/kg IV or IM in single daily dose or (or in equally divided doses twice a day); Maximum dose: 4 gm/day
AdministrationView
Preparation of Solutions for Intramuscular / Intravenous Injections:
- For Intramuscular Injection: 250 mg or 500 mg Ceftriaxone should be dissolved in 2 ml Lidocaine HCI 1% injection or 1 g Ceftriaxone in 3.5 ml of Lidocaine HCI 1% injection.
- For Intravenous Injection: 250 mg or 500 mg Ceftriaxone should be dissolved in 5 ml of Water for injection or 1 g Ceftriaxone in 10 ml of Water for injection USP or 2 g Ceftriaxone in 20 ml of Water for injection.
Side effectsView
Ceftriaxone is generally well tolerated. A few side effects such as gastro-intestinal effects including diarrhea, nausea and vomiting, stomatitis and glossitis; cutaneous reactions including rash, pruritus, urticaria, edema and erythema multiforme; hematologic reactions including eosinophilia, thrombocytopenia, leucopenia, anemia and neutropenia; hepatic reactions including elevations of SGOT or SGPT, bilirubinemia; CNS reactions including nervousness, confusion, sleep disturbances, headache, hyperactivity, convulsion, hypertonia and dizziness were reported. Local phlebitis occurs rarely following intravenous administration but can be minimized by slow injections over 2-4 minutes.
ContraindicationsView
Ceftriaxone should not be given to patients with a history of hypersensitivity to cephalosporin antibiotics.
PrecautionsView
As with other cephalosporins, anaphylactic shock cannot be ruled out even if a thorough patient history is taken. Anaphylactic shock requires immediate countermeasures such as intravenous epinephrine followed by a glucocorticoid. In rare cases, shadows suggesting sludge have been detected by sonograms of the gallbladder. This condition was reversible on discontinuation or completion of Ceftriaxone therapy. Even if such findings are associated with pain, conservative, nonsurgical management is recommended. During prolonged treatment the blood picture should be checked at regular intervals.
InteractionsView
No drug interactions have been reported.
Pregnancy & lactationView
Its safety in human pregnancy has not been established. Therefore, it should not be used in pregnancy unless absolutely indicated. Low concentrations of Ceftriaxone are excreted in human milk. Caution should be exercised when Ceftriaxone is administered to a lactating mother.
Pediatric usageView
Ceftriaxone must not be given to neonates if the neonates is premature and newborn (up to 28 days of age).
Overdose effectsView
There is no specific antidote. Treatment of overdosage should be symptomatic.
StorageView
Vial store in a cool, dry place (below 30° C), away from light & moisture. Keep out of the reach of children.
Powercef
Ceftriaxone Sodium
Powercef
Ceftriaxone Sodium
Indications
Urinary tract infection
Indication detailsView
Ceftriaxone is indicated for the treatment of the following major infections:
- Lower respiratory tract infections
- Acute Bacterial Otitis Media
- Skin and skin structure infections
- Urinary tract infections
- Gonorrhea
- Bacterial Septicemia
- Bone and joint infections
- Meningitis
- Prevention of postoperative infections
- Perioperative prophylaxis of infections associated with surgery
Therapeutic classView
Third generation Cephalosporins
PharmacologyView
Ceftriaxone is a 3rd generation broad-spectrum parenteral cephalosporin antibiotic. It has potent bactericidal activity against a wide range of Gram-positive and Gram-negative organisms. Like other cephalosporins and penicillins, Ceftriaxone kills bacteria by interfering with the synthesis of the bacterial cell wall. Ceftriaxone has a high degree of stability in the presence of beta lactamases. A remarkable feature of Ceftriaxone is its relatively long plasma elimination half-life of about 6 to 9 hours, which makes single or once-daily dosage of the drug appropriate for most patients. Ceftriaxone is not metabolized in the body. About 40-65% of a dose of Ceftriaxone is excreted unchanged in the urine; the remainder is excreted in the bile and ultimately found in the feces as unchanged drug and microbiologically inactive compound. The drug is highly protein bound (95%).
DosageView
Adult: The usual dose is 1 to 2 gm by intravenous or intramuscular administration once a day (or in equally divided doses twice a day).
- Pneumonia, Bronchitis, Acute bacterial otitis media, Skin and skin structure infection, Urinary tract infections, Bacterial Septicemia, Bone and joint infections, Meningitis: 1 to 2 g IV or IM once a day (or in equally divided doses twice a day); Maximum dose: 4 gm/day
- Uncomplicated gonococcal infections: 250 mg IM as a single dose
- Surgical prophylaxis: 1 g IV as a single dose 30 to 120 minutes before surgery
- Pneumonia, Bronchitis, Skin and skin structure infection, Urinary tract infections, Bacterial Septicemia, Bone and joint infections: 50 to 75 mg/kg IV or IM once a day (or in equally divided doses twice a day); Maximum dose: 2 gm/day
- Acute bacterial otitis media: 50 mg/kg IM in single dose; Maximum dose: 1 gm/day
- Meningitis: 100 mg/kg IV or IM in single daily dose or (or in equally divided doses twice a day); Maximum dose: 4 gm/day
AdministrationView
Preparation of Solutions for Intramuscular / Intravenous Injections:
- For Intramuscular Injection: 250 mg or 500 mg Ceftriaxone should be dissolved in 2 ml Lidocaine HCI 1% injection or 1 g Ceftriaxone in 3.5 ml of Lidocaine HCI 1% injection.
- For Intravenous Injection: 250 mg or 500 mg Ceftriaxone should be dissolved in 5 ml of Water for injection or 1 g Ceftriaxone in 10 ml of Water for injection USP or 2 g Ceftriaxone in 20 ml of Water for injection.
Side effectsView
Ceftriaxone is generally well tolerated. A few side effects such as gastro-intestinal effects including diarrhea, nausea and vomiting, stomatitis and glossitis; cutaneous reactions including rash, pruritus, urticaria, edema and erythema multiforme; hematologic reactions including eosinophilia, thrombocytopenia, leucopenia, anemia and neutropenia; hepatic reactions including elevations of SGOT or SGPT, bilirubinemia; CNS reactions including nervousness, confusion, sleep disturbances, headache, hyperactivity, convulsion, hypertonia and dizziness were reported. Local phlebitis occurs rarely following intravenous administration but can be minimized by slow injections over 2-4 minutes.
ContraindicationsView
Ceftriaxone should not be given to patients with a history of hypersensitivity to cephalosporin antibiotics.
PrecautionsView
As with other cephalosporins, anaphylactic shock cannot be ruled out even if a thorough patient history is taken. Anaphylactic shock requires immediate countermeasures such as intravenous epinephrine followed by a glucocorticoid. In rare cases, shadows suggesting sludge have been detected by sonograms of the gallbladder. This condition was reversible on discontinuation or completion of Ceftriaxone therapy. Even if such findings are associated with pain, conservative, nonsurgical management is recommended. During prolonged treatment the blood picture should be checked at regular intervals.
InteractionsView
No drug interactions have been reported.
Pregnancy & lactationView
Its safety in human pregnancy has not been established. Therefore, it should not be used in pregnancy unless absolutely indicated. Low concentrations of Ceftriaxone are excreted in human milk. Caution should be exercised when Ceftriaxone is administered to a lactating mother.
Pediatric usageView
Ceftriaxone must not be given to neonates if the neonates is premature and newborn (up to 28 days of age).
Overdose effectsView
There is no specific antidote. Treatment of overdosage should be symptomatic.
StorageView
Vial store in a cool, dry place (below 30° C), away from light & moisture. Keep out of the reach of children.
Powersol
Amino Acid + D-Sorbitol + Electrolytes
Powersol
Amino Acid + D-Sorbitol + Electrolytes
Indications
Protein supply for peritoneal nutrition
Indication detailsView
Amino acid is indicated as a source of amino acids for protein synthesis in patients needing intravenous nutrition. Amino acid is particularly suitable for patients with basal amino acid requirements. Amino acid is also indicated in faster recovery in surgery, burns, renal insufficiency, hepatic insufficiency and effective management of cancer.
Therapeutic classView
Parenteral nutritional preparations
PharmacologyView
This IV solution is a sterile aqueous solution of crystalline Amino Acid and D-Sorbitol with electrolytes, which are necessary as the nitrogen source for parenteral nutrition. Nitrogen provided in the form of essential and non-essential amino acids. This IV solution contains all 18 essential and non-essential amino acids needed for protein synthesis. The amino acid composition is such that positive nitrogen balance can be achieved in the postoperative period and during extended periods of intravenous nutrition. The solution is clear, colorless to pale yellow colored, having a p H lying in the range of 5.0 to 7.0.
DosageView
The nitrogen requirement for maintenance of body protein mass depends on the patient's condition (nutritional state and degree of metabolic stress).
In obese patients, the dose should be based on the estimated ideal weight. Depending upon patients requirements, 1000-2000 ml Amino acids IV may be infused intravenously per 24 hours. Amino acids IV should be infused slowly, at rates 1.4-2.8 ml (30-60 drops) per minute.
In children and infants: The rate of infusion is 28-35 ml/kg body weight per day is recommended, with a step-wise increase in the rate of administration during the frst week.
- No or minor metabolic stress and normal nutritional state: 0.10-0.15 g nitrogen/kg/day,
- Moderate metabolic stress with or without malnutrition: 0.15-0.20 g nitrogen/kg/day,
- Severe catabolism as in burns, sepsis and trauma: up to 0.20-0.25 g nitrogen/kg/day.
In obese patients, the dose should be based on the estimated ideal weight. Depending upon patients requirements, 1000-2000 ml Amino acids IV may be infused intravenously per 24 hours. Amino acids IV should be infused slowly, at rates 1.4-2.8 ml (30-60 drops) per minute.
In children and infants: The rate of infusion is 28-35 ml/kg body weight per day is recommended, with a step-wise increase in the rate of administration during the frst week.
Side effectsView
This preparation is usually well tolerated. Nausea occurs rarely. Vomiting, flushing and sweating have been observed during infusion of Amino acid at rates exceeding the recommended maximal rate. Transient increases liver test during intravenous nutrition have been reported. The reasons are at present unclear. Hypersensitivity reactions have been reported. As with all hypertonic infusion solutions, thrombophlebitis may occur when peripheral veins are used. The incidence may be reduced by the simultaneous infusion of 10% fat emulsion. If given to severely ill, premature infants, hyperphenylalaninemia may occur.
ContraindicationsView
This is contraindicated in patients with inborn errors of amino acids metabolism, severe liver dysfunction and in severe uremia when dialysis facilities are not available. Due to the content of glucose, Amino Acids IV infusion and 10% Glucose with Electrolytes is contraindicated in patients with hyperosmolar nonketotic diabetic coma.
PrecautionsView
IV infusion of amino acids is accompanied by increased urinary excretion of the trace elements copper and in particular zinc, which should be taken into account in the dosing of trace elements, particularly during long-term IV nutrition. Hyperphenylalaninemia may occur in severely ill, premature infants. In these patients, monitoring of the phenylalanine level is recommended and the infusion rate adjusted as needed. Amino Acids IV infusion and 10% Glucose with Electrolytes should be used with caution in patients with diabetes mellitus, severe heart failure or with renal function in combination with fluid restrictions or oliguria/anuria of another origin. In patients with hyperglycemia, administration of exogenous insulin might be necessary. In severely malnourished patients refeeding carbohydrates can trigger thiamine (vitamin B1 ) deficiency syndrome. Those at high risk are patients with a history of alcohol abuse, anorexia nervosa, prolonged fasting or starvation and pregnant women with hyperemesis gravidarum. In this kind of patients, parenteral nutrition containing glucose should be given with caution and parenteral administration of thiamine should be considered before and during the administration of glucose. Monitoring of serum potassium and blood glucose is recommended if Amino Acids IV infusion and 10% Glucose with electrolytes is infused rapidly or in a large quantity. For patients with hypophosphatemia, an additional supply of phosphate is recommended.
InteractionsView
At the recommended dosage the amino acid have no pharmacological effects and is not expected to interact with other medicaments.
Pregnancy & lactationView
Successful and safe administration of amino acid solutions during pregnancy in the human has been reported. Animal reproduction studies have not been carried out with Amino acid.
Overdose effectsView
If Amino Acids IV infusion and 10% Glucose with Electrolytes is administered at a higher rate than recommended, there is an augmented risk for nausea, vomiting and sweating. When peripheral veins are used thrombophlebitis may occur. Osmotic diuresis with dehydration may occur if the dosage recommendations are exceeded. There is also a risk of symptoms related to hyperglycemia with Amino Acids IV infusion and 10% Glucose with Electrolytes. In case of symptoms due to overdose, the infusion should be slowed down or discontinued.
StorageView
Protect from light and store between 15°C to 25°C temperature. Avoid freezing. Keep out of reach of children.
Pradaxa
Dabigatran Etexilate Mesylate
Pradaxa
Dabigatran Etexilate Mesylate
Indications
Stroke
Indication detailsView
Reduction of Risk of Stroke and Systemic Embolism in Non-valvular Atrial Fibrillation: Dabigatran Etexilate Mesylate is indicated to reduce the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation.
Treatment of Deep Venous Thrombosis and Pulmonary Embolism: Dabigatran Etexilate Mesylate is indicated for the treatment of deep venous thrombosis and pulmonary embolism in patients who have been treated with a parenteral anticoagulant for 5-10 days.
Reduction in the Risk of Recurrence of Deep Venous Thrombosis and Pulmonary Embolism: Dabigatran Etexilate Mesylate is indicated to reduce the risk of recurrence of deep venous thrombosis and pulmonary embolism in patients who have been previously treated.
Prophylaxis of Deep Vein Thrombosis and Pulmonary Embolism Following Hip Replacement Surgery: Dabigatran Etexilate Mesylate is indicated for the prophylaxis of deep vein thrombosis and pulmonary embolism, in patients who have undergone hip replacement surgery.
Treatment of Deep Venous Thrombosis and Pulmonary Embolism: Dabigatran Etexilate Mesylate is indicated for the treatment of deep venous thrombosis and pulmonary embolism in patients who have been treated with a parenteral anticoagulant for 5-10 days.
Reduction in the Risk of Recurrence of Deep Venous Thrombosis and Pulmonary Embolism: Dabigatran Etexilate Mesylate is indicated to reduce the risk of recurrence of deep venous thrombosis and pulmonary embolism in patients who have been previously treated.
Prophylaxis of Deep Vein Thrombosis and Pulmonary Embolism Following Hip Replacement Surgery: Dabigatran Etexilate Mesylate is indicated for the prophylaxis of deep vein thrombosis and pulmonary embolism, in patients who have undergone hip replacement surgery.
Therapeutic classView
Anti-coagulants, Anti-platelet drugs, Fibrinolytics (Thrombolytics)
PharmacologyView
Dabigatran and its acyl glucuronides are competitive, direct thrombin inhibitors. Because thrombin (serine protease) enables the conversion of fibrinogen into fibrin during the coagulation cascade, its inhibition prevents the development of a thrombus. Both free and clot-bound thrombin, and thrombin-induced platelet aggregation are inhibited by the active moieties.
At recommended therapeutic doses, dabigatran etexilate prolongs the coagulation markers such as aPTT, ECT, and TT. INR is relatively insensitive to the exposure to dabigatran and cannot be interpreted the same way as used for warfarin monitoring. The aPTT test provides an approximation of Dabigatran Etexilate’s anticoagulant effect. The average time course for effects on aPTT, following approved dosing regimens in patients with various degrees of renal impairment is shown in Figure 2. The curves represent mean levels without confidence intervals; variations should be expected when measuring aPTT. While advice cannot be provided on the level of recovery of aPTT needed in any particular clinical setting, the curves can be used to estimate the time to get to a particular level of recovery, even when the time since the last dose of Dabigatran Etexilate is not precisely known. In the RE-LY trial, the median (10 th to 90 th percentile) trough aPTT in patients receiving the 150 mg dose was 52 (40 to 76) seconds.
At recommended therapeutic doses, dabigatran etexilate prolongs the coagulation markers such as aPTT, ECT, and TT. INR is relatively insensitive to the exposure to dabigatran and cannot be interpreted the same way as used for warfarin monitoring. The aPTT test provides an approximation of Dabigatran Etexilate’s anticoagulant effect. The average time course for effects on aPTT, following approved dosing regimens in patients with various degrees of renal impairment is shown in Figure 2. The curves represent mean levels without confidence intervals; variations should be expected when measuring aPTT. While advice cannot be provided on the level of recovery of aPTT needed in any particular clinical setting, the curves can be used to estimate the time to get to a particular level of recovery, even when the time since the last dose of Dabigatran Etexilate is not precisely known. In the RE-LY trial, the median (10 th to 90 th percentile) trough aPTT in patients receiving the 150 mg dose was 52 (40 to 76) seconds.
DosageView
Reduction in Risk of Stroke and Systemic Embolism in Non-valvular AF-
Reduction of Risk of Stroke and Systemic Embolism in Non-valvular Atrial Fibrillation: For patients with creatinine clearance (CrCl) >30 mL/min, the recommended dose of Dabigatran Etexilate is 150 mg taken orally, twice daily. For patients with severe renal impairment (CrCl 15-30 mL/min), the recommended dose of Dabigatran Etexilate is 75 mg twice daily. Dosing recommendations for patients with a CrCl <15 mL/min or on dialysis cannot be provided.
Treatment of Deep Venous Thrombosis and Pulmonary Embolism: For patients with CrCl >30 mL/min, the recommended dose of Dabigatran Etexilate is 150 mg taken orally, twice daily, after 5-10 days of parenteral anticoagulation. Dosing recommendations for patients with a CrCl ≤30 mL/min or on dialysis cannot be provided.
Reduction in the Risk of Recurrence of Deep Venous Thrombosis and Pulmonary Embolism: For patients with CrCl >30 mL/min, the recommended dose of Dabigatran Etexilate is 150 mg taken orally, twice daily after previous treatment. Dosing recommendations for patients with a CrCl ≤30 mL/min or on dialysis cannot be provided.
Prophylaxis of Deep Vein Thrombosis and Pulmonary Embolism Following Hip Replacement Surgery: For patients with CrCl >30 mL/min, the recommended dose of Dabigatran Etexilate is 110 mg taken orally 1-4 hours after surgery and after hemostasis has been achieved, then 220 mg taken once daily for 28-35 days. If Dabigatran Etexilate is not started on the day of surgery, after hemostasis has been achieved initiate treatment with 220 mg once daily. Dosing recommendations for patients with a CrCl ≤30 mL/min or on dialysis cannot be provided
- CrCl >30 mL/min: 150 mg twice daily
- CrCl 15 to 30 mL/min: 75 mg twice daily
- CrCl <15 mL/min or on dialysis: Dosing recommendations cannot be provided
- CrCl 30 to 50 mL/min with concomitant use of P-gp inhibitors: Reduce dose to 75 mg twice daily if given with P-gp inhibitors dronedarone or systemic ketoconazole.
- CrCl <30 mL/min with concomitant use of P-gp inhibitors: Avoid co-administration
- CrCl >30 mL/min: 150 mg twice daily
- CrCl ≤30 mL/min or on dialysis: Dosing recommendations cannot be provided
- CrCl <50 mL/min with concomitant use of P-gp inhibitors: Avoid co-administration
- CrCl >30 mL/min: 110 mg for first day, then 220 mg once daily
- CrCl ≤30 mL/min or on dialysis: Dosing recommendations cannot be provided
- CrCl <50 mL/min with concomitant use of P-gp inhibitors: Avoid co-administration.
Reduction of Risk of Stroke and Systemic Embolism in Non-valvular Atrial Fibrillation: For patients with creatinine clearance (CrCl) >30 mL/min, the recommended dose of Dabigatran Etexilate is 150 mg taken orally, twice daily. For patients with severe renal impairment (CrCl 15-30 mL/min), the recommended dose of Dabigatran Etexilate is 75 mg twice daily. Dosing recommendations for patients with a CrCl <15 mL/min or on dialysis cannot be provided.
Treatment of Deep Venous Thrombosis and Pulmonary Embolism: For patients with CrCl >30 mL/min, the recommended dose of Dabigatran Etexilate is 150 mg taken orally, twice daily, after 5-10 days of parenteral anticoagulation. Dosing recommendations for patients with a CrCl ≤30 mL/min or on dialysis cannot be provided.
Reduction in the Risk of Recurrence of Deep Venous Thrombosis and Pulmonary Embolism: For patients with CrCl >30 mL/min, the recommended dose of Dabigatran Etexilate is 150 mg taken orally, twice daily after previous treatment. Dosing recommendations for patients with a CrCl ≤30 mL/min or on dialysis cannot be provided.
Prophylaxis of Deep Vein Thrombosis and Pulmonary Embolism Following Hip Replacement Surgery: For patients with CrCl >30 mL/min, the recommended dose of Dabigatran Etexilate is 110 mg taken orally 1-4 hours after surgery and after hemostasis has been achieved, then 220 mg taken once daily for 28-35 days. If Dabigatran Etexilate is not started on the day of surgery, after hemostasis has been achieved initiate treatment with 220 mg once daily. Dosing recommendations for patients with a CrCl ≤30 mL/min or on dialysis cannot be provided
Side effectsView
The following clinically significant adverse reactions are described elsewhere in the labeling:
- Increased Risk of Thrombotic Events after Premature Discontinuation
- Risk of Bleeding
- Spinal/Epidural Anesthesia or Puncture
- Thromboembolic and Bleeding Events in Patients with Prosthetic Heart Valves
- Increased Risk of Thrombosis in Patients with Triple-Positive Antiphospholipid Syndrome
ContraindicationsView
Dabigatran Etexilate is contraindicated in patients with:
- Active pathological bleeding.
- History of a serious hypersensitivity reaction to Dabigatran Etexilate (e.g., anaphylactic reaction or anaphylactic shock).
- Mechanical prosthetic heart valve.
PrecautionsView
Bleeding: Dabigatran Etexilate can cause serious and fatal bleeding
Bioprosthetic heart valves: Dabigatran Etexilate use not recommended
Increased Risk of Thrombosis in Patients with Triple-Positive Antiphospholipid Syndrome: Dabigatran Etexilate use not recommended
Bioprosthetic heart valves: Dabigatran Etexilate use not recommended
Increased Risk of Thrombosis in Patients with Triple-Positive Antiphospholipid Syndrome: Dabigatran Etexilate use not recommended
InteractionsView
Reduction of Risk of Stroke and Systemic Embolism in Non-valvular Atrial Fibrillation: The concomitant use of Dabigatran Etexilate with P-gp inducers (e.g., rifampin) reduces exposure to dabigatran and should generally be avoided. P-gp inhibition and impaired renal function are the major independent factors that result in increased exposure to dabigatran. Concomitant use of P-gp inhibitors in patients with renal impairment is expected to produce increased exposure of dabigatran compared to that seen with either factor alone. In patients with moderate renal impairment (CrCl 30-50 mL/min), reduce the dose of Dabigatran Etexilate to 75 mg twice daily when administered concomitantly with the P-gp inhibitors dronedarone or systemic ketoconazole. The use of the P-gp inhibitors verapamil, amiodarone, quinidine, clarithromycin, and ticagrelor does not require a dose adjustment of Dabigatran Etexilate. These results should not be extrapolated to other P-gp inhibitors. The concomitant use of Dabigatran Etexilate and P-gp inhibitors in patients with severe renal impairment (CrCl 15-30 mL/min) should be avoided.
Treatment and Reduction in the Risk of Recurrence of Deep Venous Thrombosis and Pulmonary Embolism: Avoid use of Dabigatran Etexilate and P-gp inhibitors in patients with CrCl <50 mL/min.
Prophylaxis of Deep Vein Thrombosis and Pulmonary Embolism Following Hip Replacement Surgery: In patients with CrCl ≥50 mL/min who have concomitant administration of P-gp inhibitors such as dronedarone or systemic ketoconazole, it may be helpful to separate the timing of administration of dabigatran and the P-gp inhibitor by several hours. The concomitant use of Dabigatran Etexilate and P-gp inhibitors in patients with CrCl <50 mL/min should be avoided.
Treatment and Reduction in the Risk of Recurrence of Deep Venous Thrombosis and Pulmonary Embolism: Avoid use of Dabigatran Etexilate and P-gp inhibitors in patients with CrCl <50 mL/min.
Prophylaxis of Deep Vein Thrombosis and Pulmonary Embolism Following Hip Replacement Surgery: In patients with CrCl ≥50 mL/min who have concomitant administration of P-gp inhibitors such as dronedarone or systemic ketoconazole, it may be helpful to separate the timing of administration of dabigatran and the P-gp inhibitor by several hours. The concomitant use of Dabigatran Etexilate and P-gp inhibitors in patients with CrCl <50 mL/min should be avoided.
Pregnancy & lactationView
Pregnancy: The limited available data on Dabigatran Etexilate use in pregnant women are insufficient to determine drug-associated risks for adverse developmental outcomes. There are risks to the mother associated with untreated venous thromboembolism in pregnancy and a risk of hemorrhage in the mother and fetus associated with the use of anticoagulant
Lactation: There are no data on the presence of dabigatran in human milk, the effects on the breastfed child, or on milk production. Dabigatran and/or its metabolites were present in rat milk. Breastfeeding is not recommended during treatment with Dabigatran Etexilate.
Lactation: There are no data on the presence of dabigatran in human milk, the effects on the breastfed child, or on milk production. Dabigatran and/or its metabolites were present in rat milk. Breastfeeding is not recommended during treatment with Dabigatran Etexilate.
Pediatric usageView
Pediatric Use: The safety and effectiveness of Dabigatran Etexilate in pediatric patients have not been established.
Geriatric Use: Of the total number of patients in the RE-LY study, 82% were 65 and over, while 40% were 75 and over. The risk of stroke and bleeding increases with age, but the risk-benefit profile is favorable in all age groups.
Geriatric Use: Of the total number of patients in the RE-LY study, 82% were 65 and over, while 40% were 75 and over. The risk of stroke and bleeding increases with age, but the risk-benefit profile is favorable in all age groups.
Overdose effectsView
Accidental overdose may lead to hemorrhagic complications. In the event of hemorrhagic complications, initiate appropriate clinical support, discontinue treatment with Dabigatran Etexilate, and investigate the source of bleeding. A specific reversal agent (idarucizumab) is available. Dabigatran is primarily eliminated by the kidneys with a low plasma protein binding of approximately 35%. Hemodialysis can remove dabigatran; however, data supporting this approach are limited. Using a high-flux dialyzer, blood flow rate of 200 mL/min, and dialysate flow rate of 700 mL/min, approximately 49% of total dabigatran can be cleared from plasma over 4 hours. At the same dialysate flow rate, approximately 57% can be cleared using a dialyzer blood flow rate of 300 mL/min, with no appreciable increase in clearance observed at higher blood flow rates. Upon cessation of hemodialysis, a redistribution effect of approximately 7% to 15% is seen. The effect of dialysis on dabigatran’s plasma concentration would be expected to vary based on patient specific characteristics. Measurement of aPTT or ECT may help guide therapy
StorageView
Store Dabigatran Etexilate at room temperature 20°C to 25°C. After opening the bottle, use Dabigatran Etexilate within 4 months. Safely throw away any unused Dabigatran Etexilate after 4 months. Keep Dabigatran Etexilate in the original bottle or blister package to keep it dry (protect the capsules from moisture). Do not put Dabigatran Etexilate in pill boxes or pill organizers. Tightly close your bottle of Dabigatran Etexilate right away after you take your dose. Keep Dabigatran Etexilate and all medicines out of the reach of children.
Pradaxa
Dabigatran Etexilate Mesylate
Pradaxa
Dabigatran Etexilate Mesylate
Indications
Stroke
Indication detailsView
Reduction of Risk of Stroke and Systemic Embolism in Non-valvular Atrial Fibrillation: Dabigatran Etexilate Mesylate is indicated to reduce the risk of stroke and systemic embolism in patients with non-valvular atrial fibrillation.
Treatment of Deep Venous Thrombosis and Pulmonary Embolism: Dabigatran Etexilate Mesylate is indicated for the treatment of deep venous thrombosis and pulmonary embolism in patients who have been treated with a parenteral anticoagulant for 5-10 days.
Reduction in the Risk of Recurrence of Deep Venous Thrombosis and Pulmonary Embolism: Dabigatran Etexilate Mesylate is indicated to reduce the risk of recurrence of deep venous thrombosis and pulmonary embolism in patients who have been previously treated.
Prophylaxis of Deep Vein Thrombosis and Pulmonary Embolism Following Hip Replacement Surgery: Dabigatran Etexilate Mesylate is indicated for the prophylaxis of deep vein thrombosis and pulmonary embolism, in patients who have undergone hip replacement surgery.
Treatment of Deep Venous Thrombosis and Pulmonary Embolism: Dabigatran Etexilate Mesylate is indicated for the treatment of deep venous thrombosis and pulmonary embolism in patients who have been treated with a parenteral anticoagulant for 5-10 days.
Reduction in the Risk of Recurrence of Deep Venous Thrombosis and Pulmonary Embolism: Dabigatran Etexilate Mesylate is indicated to reduce the risk of recurrence of deep venous thrombosis and pulmonary embolism in patients who have been previously treated.
Prophylaxis of Deep Vein Thrombosis and Pulmonary Embolism Following Hip Replacement Surgery: Dabigatran Etexilate Mesylate is indicated for the prophylaxis of deep vein thrombosis and pulmonary embolism, in patients who have undergone hip replacement surgery.
Therapeutic classView
Anti-coagulants, Anti-platelet drugs, Fibrinolytics (Thrombolytics)
PharmacologyView
Dabigatran and its acyl glucuronides are competitive, direct thrombin inhibitors. Because thrombin (serine protease) enables the conversion of fibrinogen into fibrin during the coagulation cascade, its inhibition prevents the development of a thrombus. Both free and clot-bound thrombin, and thrombin-induced platelet aggregation are inhibited by the active moieties.
At recommended therapeutic doses, dabigatran etexilate prolongs the coagulation markers such as aPTT, ECT, and TT. INR is relatively insensitive to the exposure to dabigatran and cannot be interpreted the same way as used for warfarin monitoring. The aPTT test provides an approximation of Dabigatran Etexilate’s anticoagulant effect. The average time course for effects on aPTT, following approved dosing regimens in patients with various degrees of renal impairment is shown in Figure 2. The curves represent mean levels without confidence intervals; variations should be expected when measuring aPTT. While advice cannot be provided on the level of recovery of aPTT needed in any particular clinical setting, the curves can be used to estimate the time to get to a particular level of recovery, even when the time since the last dose of Dabigatran Etexilate is not precisely known. In the RE-LY trial, the median (10 th to 90 th percentile) trough aPTT in patients receiving the 150 mg dose was 52 (40 to 76) seconds.
At recommended therapeutic doses, dabigatran etexilate prolongs the coagulation markers such as aPTT, ECT, and TT. INR is relatively insensitive to the exposure to dabigatran and cannot be interpreted the same way as used for warfarin monitoring. The aPTT test provides an approximation of Dabigatran Etexilate’s anticoagulant effect. The average time course for effects on aPTT, following approved dosing regimens in patients with various degrees of renal impairment is shown in Figure 2. The curves represent mean levels without confidence intervals; variations should be expected when measuring aPTT. While advice cannot be provided on the level of recovery of aPTT needed in any particular clinical setting, the curves can be used to estimate the time to get to a particular level of recovery, even when the time since the last dose of Dabigatran Etexilate is not precisely known. In the RE-LY trial, the median (10 th to 90 th percentile) trough aPTT in patients receiving the 150 mg dose was 52 (40 to 76) seconds.
DosageView
Reduction in Risk of Stroke and Systemic Embolism in Non-valvular AF-
Reduction of Risk of Stroke and Systemic Embolism in Non-valvular Atrial Fibrillation: For patients with creatinine clearance (CrCl) >30 mL/min, the recommended dose of Dabigatran Etexilate is 150 mg taken orally, twice daily. For patients with severe renal impairment (CrCl 15-30 mL/min), the recommended dose of Dabigatran Etexilate is 75 mg twice daily. Dosing recommendations for patients with a CrCl <15 mL/min or on dialysis cannot be provided.
Treatment of Deep Venous Thrombosis and Pulmonary Embolism: For patients with CrCl >30 mL/min, the recommended dose of Dabigatran Etexilate is 150 mg taken orally, twice daily, after 5-10 days of parenteral anticoagulation. Dosing recommendations for patients with a CrCl ≤30 mL/min or on dialysis cannot be provided.
Reduction in the Risk of Recurrence of Deep Venous Thrombosis and Pulmonary Embolism: For patients with CrCl >30 mL/min, the recommended dose of Dabigatran Etexilate is 150 mg taken orally, twice daily after previous treatment. Dosing recommendations for patients with a CrCl ≤30 mL/min or on dialysis cannot be provided.
Prophylaxis of Deep Vein Thrombosis and Pulmonary Embolism Following Hip Replacement Surgery: For patients with CrCl >30 mL/min, the recommended dose of Dabigatran Etexilate is 110 mg taken orally 1-4 hours after surgery and after hemostasis has been achieved, then 220 mg taken once daily for 28-35 days. If Dabigatran Etexilate is not started on the day of surgery, after hemostasis has been achieved initiate treatment with 220 mg once daily. Dosing recommendations for patients with a CrCl ≤30 mL/min or on dialysis cannot be provided
- CrCl >30 mL/min: 150 mg twice daily
- CrCl 15 to 30 mL/min: 75 mg twice daily
- CrCl <15 mL/min or on dialysis: Dosing recommendations cannot be provided
- CrCl 30 to 50 mL/min with concomitant use of P-gp inhibitors: Reduce dose to 75 mg twice daily if given with P-gp inhibitors dronedarone or systemic ketoconazole.
- CrCl <30 mL/min with concomitant use of P-gp inhibitors: Avoid co-administration
- CrCl >30 mL/min: 150 mg twice daily
- CrCl ≤30 mL/min or on dialysis: Dosing recommendations cannot be provided
- CrCl <50 mL/min with concomitant use of P-gp inhibitors: Avoid co-administration
- CrCl >30 mL/min: 110 mg for first day, then 220 mg once daily
- CrCl ≤30 mL/min or on dialysis: Dosing recommendations cannot be provided
- CrCl <50 mL/min with concomitant use of P-gp inhibitors: Avoid co-administration.
Reduction of Risk of Stroke and Systemic Embolism in Non-valvular Atrial Fibrillation: For patients with creatinine clearance (CrCl) >30 mL/min, the recommended dose of Dabigatran Etexilate is 150 mg taken orally, twice daily. For patients with severe renal impairment (CrCl 15-30 mL/min), the recommended dose of Dabigatran Etexilate is 75 mg twice daily. Dosing recommendations for patients with a CrCl <15 mL/min or on dialysis cannot be provided.
Treatment of Deep Venous Thrombosis and Pulmonary Embolism: For patients with CrCl >30 mL/min, the recommended dose of Dabigatran Etexilate is 150 mg taken orally, twice daily, after 5-10 days of parenteral anticoagulation. Dosing recommendations for patients with a CrCl ≤30 mL/min or on dialysis cannot be provided.
Reduction in the Risk of Recurrence of Deep Venous Thrombosis and Pulmonary Embolism: For patients with CrCl >30 mL/min, the recommended dose of Dabigatran Etexilate is 150 mg taken orally, twice daily after previous treatment. Dosing recommendations for patients with a CrCl ≤30 mL/min or on dialysis cannot be provided.
Prophylaxis of Deep Vein Thrombosis and Pulmonary Embolism Following Hip Replacement Surgery: For patients with CrCl >30 mL/min, the recommended dose of Dabigatran Etexilate is 110 mg taken orally 1-4 hours after surgery and after hemostasis has been achieved, then 220 mg taken once daily for 28-35 days. If Dabigatran Etexilate is not started on the day of surgery, after hemostasis has been achieved initiate treatment with 220 mg once daily. Dosing recommendations for patients with a CrCl ≤30 mL/min or on dialysis cannot be provided
Side effectsView
The following clinically significant adverse reactions are described elsewhere in the labeling:
- Increased Risk of Thrombotic Events after Premature Discontinuation
- Risk of Bleeding
- Spinal/Epidural Anesthesia or Puncture
- Thromboembolic and Bleeding Events in Patients with Prosthetic Heart Valves
- Increased Risk of Thrombosis in Patients with Triple-Positive Antiphospholipid Syndrome
ContraindicationsView
Dabigatran Etexilate is contraindicated in patients with:
- Active pathological bleeding.
- History of a serious hypersensitivity reaction to Dabigatran Etexilate (e.g., anaphylactic reaction or anaphylactic shock).
- Mechanical prosthetic heart valve.
PrecautionsView
Bleeding: Dabigatran Etexilate can cause serious and fatal bleeding
Bioprosthetic heart valves: Dabigatran Etexilate use not recommended
Increased Risk of Thrombosis in Patients with Triple-Positive Antiphospholipid Syndrome: Dabigatran Etexilate use not recommended
Bioprosthetic heart valves: Dabigatran Etexilate use not recommended
Increased Risk of Thrombosis in Patients with Triple-Positive Antiphospholipid Syndrome: Dabigatran Etexilate use not recommended
InteractionsView
Reduction of Risk of Stroke and Systemic Embolism in Non-valvular Atrial Fibrillation: The concomitant use of Dabigatran Etexilate with P-gp inducers (e.g., rifampin) reduces exposure to dabigatran and should generally be avoided. P-gp inhibition and impaired renal function are the major independent factors that result in increased exposure to dabigatran. Concomitant use of P-gp inhibitors in patients with renal impairment is expected to produce increased exposure of dabigatran compared to that seen with either factor alone. In patients with moderate renal impairment (CrCl 30-50 mL/min), reduce the dose of Dabigatran Etexilate to 75 mg twice daily when administered concomitantly with the P-gp inhibitors dronedarone or systemic ketoconazole. The use of the P-gp inhibitors verapamil, amiodarone, quinidine, clarithromycin, and ticagrelor does not require a dose adjustment of Dabigatran Etexilate. These results should not be extrapolated to other P-gp inhibitors. The concomitant use of Dabigatran Etexilate and P-gp inhibitors in patients with severe renal impairment (CrCl 15-30 mL/min) should be avoided.
Treatment and Reduction in the Risk of Recurrence of Deep Venous Thrombosis and Pulmonary Embolism: Avoid use of Dabigatran Etexilate and P-gp inhibitors in patients with CrCl <50 mL/min.
Prophylaxis of Deep Vein Thrombosis and Pulmonary Embolism Following Hip Replacement Surgery: In patients with CrCl ≥50 mL/min who have concomitant administration of P-gp inhibitors such as dronedarone or systemic ketoconazole, it may be helpful to separate the timing of administration of dabigatran and the P-gp inhibitor by several hours. The concomitant use of Dabigatran Etexilate and P-gp inhibitors in patients with CrCl <50 mL/min should be avoided.
Treatment and Reduction in the Risk of Recurrence of Deep Venous Thrombosis and Pulmonary Embolism: Avoid use of Dabigatran Etexilate and P-gp inhibitors in patients with CrCl <50 mL/min.
Prophylaxis of Deep Vein Thrombosis and Pulmonary Embolism Following Hip Replacement Surgery: In patients with CrCl ≥50 mL/min who have concomitant administration of P-gp inhibitors such as dronedarone or systemic ketoconazole, it may be helpful to separate the timing of administration of dabigatran and the P-gp inhibitor by several hours. The concomitant use of Dabigatran Etexilate and P-gp inhibitors in patients with CrCl <50 mL/min should be avoided.
Pregnancy & lactationView
Pregnancy: The limited available data on Dabigatran Etexilate use in pregnant women are insufficient to determine drug-associated risks for adverse developmental outcomes. There are risks to the mother associated with untreated venous thromboembolism in pregnancy and a risk of hemorrhage in the mother and fetus associated with the use of anticoagulant
Lactation: There are no data on the presence of dabigatran in human milk, the effects on the breastfed child, or on milk production. Dabigatran and/or its metabolites were present in rat milk. Breastfeeding is not recommended during treatment with Dabigatran Etexilate.
Lactation: There are no data on the presence of dabigatran in human milk, the effects on the breastfed child, or on milk production. Dabigatran and/or its metabolites were present in rat milk. Breastfeeding is not recommended during treatment with Dabigatran Etexilate.
Pediatric usageView
Pediatric Use: The safety and effectiveness of Dabigatran Etexilate in pediatric patients have not been established.
Geriatric Use: Of the total number of patients in the RE-LY study, 82% were 65 and over, while 40% were 75 and over. The risk of stroke and bleeding increases with age, but the risk-benefit profile is favorable in all age groups.
Geriatric Use: Of the total number of patients in the RE-LY study, 82% were 65 and over, while 40% were 75 and over. The risk of stroke and bleeding increases with age, but the risk-benefit profile is favorable in all age groups.
Overdose effectsView
Accidental overdose may lead to hemorrhagic complications. In the event of hemorrhagic complications, initiate appropriate clinical support, discontinue treatment with Dabigatran Etexilate, and investigate the source of bleeding. A specific reversal agent (idarucizumab) is available. Dabigatran is primarily eliminated by the kidneys with a low plasma protein binding of approximately 35%. Hemodialysis can remove dabigatran; however, data supporting this approach are limited. Using a high-flux dialyzer, blood flow rate of 200 mL/min, and dialysate flow rate of 700 mL/min, approximately 49% of total dabigatran can be cleared from plasma over 4 hours. At the same dialysate flow rate, approximately 57% can be cleared using a dialyzer blood flow rate of 300 mL/min, with no appreciable increase in clearance observed at higher blood flow rates. Upon cessation of hemodialysis, a redistribution effect of approximately 7% to 15% is seen. The effect of dialysis on dabigatran’s plasma concentration would be expected to vary based on patient specific characteristics. Measurement of aPTT or ECT may help guide therapy
StorageView
Store Dabigatran Etexilate at room temperature 20°C to 25°C. After opening the bottle, use Dabigatran Etexilate within 4 months. Safely throw away any unused Dabigatran Etexilate after 4 months. Keep Dabigatran Etexilate in the original bottle or blister package to keep it dry (protect the capsules from moisture). Do not put Dabigatran Etexilate in pill boxes or pill organizers. Tightly close your bottle of Dabigatran Etexilate right away after you take your dose. Keep Dabigatran Etexilate and all medicines out of the reach of children.
Pradox
Pralidoxime Chloride
Pradox
Pralidoxime Chloride
Indications
Organophosphorous poisoning
Indication detailsView
Pralidoxime chloride is indicated as an antidote:
- In the treatment of poisoning due to those pesticides and chemicals (e.g., nerve agents) of the organophosphate class which have anticholinesterase activity and
- In the control of overdosage by anticholinesterase drugs used in the treatment of myasthenia gravis.
Therapeutic classView
Antidote preparations
PharmacologyView
Pralidoxime reactivates cholinesterase outside the CNS that had been inactivated by phosphorylation due to exposure to certain organophosphates by displacing the enzyme from its receptor sites. It removes the phosphoryl group from the active site of the inactivated enzyme by nucleophilic attack, regenerating active cholinesterase and forming an oxime complex. It also detoxifies certain organophosphates by direct chemical reaction.
DosageView
Intramuscular-
Organophosphorus poisoning:- Adult: Mild: 600 mg, repeat 1-2 times at 15 min intervals as needed. Severe: 1.8 g given as 3 inj of 600 mg in rapid succession. Persistent: May repeat the entire series (1.8 g) beginning 1 hr after admin of the last inj.
- Child: <40 kg: Mild: 15 mg/kg, repeat as needed every 15 min. Max: 45 mg/kg. Severe: 15 mg/kg, repeat twice in rapid succession to a total dose of 45 mg/kg. Persistent: May repeat the entire series (45 mg/kg) beginning 1 hr after admin of the last inj; ≥40 kg: Same as adult dose.
Intravenous-
Organophosphorus poisoning:- Adult: In combination with atropine: Loading dose: 1-2 g by infusion over 15-30 min or slow inj over at least 5 min, may repeat dose after 1 hr then 10-12 hrly, as needed. Administer as soon as the effects of atropine are observed. Maintain atropinisation for at least 48 hr.
- Child: ≤16 yr Loading dose: 20-50 mg/kg (max: 2 g/dose) by inj over 15-30 min followed by 10-20 mg/kg/hr as continuous infusion. Alternatively, a repeat bolus of 20-50 mg/kg after 1 hr and repeated 10-12 hrly as needed; >16 yr Same as adult dose.
- Adult: Initially, 1-2 g, followed by 0.5-1 g/hr as infusion. Alternatively, the initial dose may be repeated after 1 hr and then 3-8 hrly as needed.
Side effectsView
Drowsiness, dizziness, visual disturbances, nausea, HTN, tachycardia, headache, hyperventilation, muscle weakness, impaired renal function, elevated liver enzymes, transient increase in creatine phosphokinase, transient neuromuscular blockade; mild to moderate pain at inj site.
ContraindicationsView
There are no known absolute contraindications for the use of Pralidoxime Chloride. Relative contraindications include known hypersensitivity to the drug and other situations in which the risk of its use clearly outweighs possible benefit.
PrecautionsView
Patient with myasthenia gravis receiving anticholinesterase agents. Not indicated in the treatment of poisoning due to phosphorous, inorganic phosphates, or organophosphates without anticholinesterase activity and carbamate pesticides. Renal impairment. Pregnancy and lactation.
Pregnancy & lactationView
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Overdose effectsView
Manifestations of Overdosage: Observed in normal subjects only: dizziness, blurred vision, diplopia, headache, impaired accommodation, nausea, slight tachycardia. In therapy it has been difficult to differentiate side effects due to the drug from those due to the effects of the poison.
ReconstitutionView
Intramuscular: Dilute 1 g with 3.3 mL sterile water for inj to a final concentration of 300 mg/mL.
Intravenous: Dilute 1 g with 20 mL of sterile water for inj to make a concentration of 50 mg/mL to be administered in fluid-restricted patients or when rapid admin is required; for all other patients, further dilute with normal saline to a final concentration of 20 mg/mL.
Intravenous: Dilute 1 g with 20 mL of sterile water for inj to make a concentration of 50 mg/mL to be administered in fluid-restricted patients or when rapid admin is required; for all other patients, further dilute with normal saline to a final concentration of 20 mg/mL.
StorageView
Store between 20-25° C.
Pralidot
Pralidoxime Chloride
Pralidot
Pralidoxime Chloride
Indications
Organophosphorous poisoning
Indication detailsView
Pralidoxime chloride is indicated as an antidote:
- In the treatment of poisoning due to those pesticides and chemicals (e.g., nerve agents) of the organophosphate class which have anticholinesterase activity and
- In the control of overdosage by anticholinesterase drugs used in the treatment of myasthenia gravis.
Therapeutic classView
Antidote preparations
PharmacologyView
Pralidoxime reactivates cholinesterase outside the CNS that had been inactivated by phosphorylation due to exposure to certain organophosphates by displacing the enzyme from its receptor sites. It removes the phosphoryl group from the active site of the inactivated enzyme by nucleophilic attack, regenerating active cholinesterase and forming an oxime complex. It also detoxifies certain organophosphates by direct chemical reaction.
DosageView
Intramuscular-
Organophosphorus poisoning:- Adult: Mild: 600 mg, repeat 1-2 times at 15 min intervals as needed. Severe: 1.8 g given as 3 inj of 600 mg in rapid succession. Persistent: May repeat the entire series (1.8 g) beginning 1 hr after admin of the last inj.
- Child: <40 kg: Mild: 15 mg/kg, repeat as needed every 15 min. Max: 45 mg/kg. Severe: 15 mg/kg, repeat twice in rapid succession to a total dose of 45 mg/kg. Persistent: May repeat the entire series (45 mg/kg) beginning 1 hr after admin of the last inj; ≥40 kg: Same as adult dose.
Intravenous-
Organophosphorus poisoning:- Adult: In combination with atropine: Loading dose: 1-2 g by infusion over 15-30 min or slow inj over at least 5 min, may repeat dose after 1 hr then 10-12 hrly, as needed. Administer as soon as the effects of atropine are observed. Maintain atropinisation for at least 48 hr.
- Child: ≤16 yr Loading dose: 20-50 mg/kg (max: 2 g/dose) by inj over 15-30 min followed by 10-20 mg/kg/hr as continuous infusion. Alternatively, a repeat bolus of 20-50 mg/kg after 1 hr and repeated 10-12 hrly as needed; >16 yr Same as adult dose.
- Adult: Initially, 1-2 g, followed by 0.5-1 g/hr as infusion. Alternatively, the initial dose may be repeated after 1 hr and then 3-8 hrly as needed.
Side effectsView
Drowsiness, dizziness, visual disturbances, nausea, HTN, tachycardia, headache, hyperventilation, muscle weakness, impaired renal function, elevated liver enzymes, transient increase in creatine phosphokinase, transient neuromuscular blockade; mild to moderate pain at inj site.
ContraindicationsView
There are no known absolute contraindications for the use of Pralidoxime Chloride. Relative contraindications include known hypersensitivity to the drug and other situations in which the risk of its use clearly outweighs possible benefit.
PrecautionsView
Patient with myasthenia gravis receiving anticholinesterase agents. Not indicated in the treatment of poisoning due to phosphorous, inorganic phosphates, or organophosphates without anticholinesterase activity and carbamate pesticides. Renal impairment. Pregnancy and lactation.
Pregnancy & lactationView
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Overdose effectsView
Manifestations of Overdosage: Observed in normal subjects only: dizziness, blurred vision, diplopia, headache, impaired accommodation, nausea, slight tachycardia. In therapy it has been difficult to differentiate side effects due to the drug from those due to the effects of the poison.
ReconstitutionView
Intramuscular: Dilute 1 g with 3.3 mL sterile water for inj to a final concentration of 300 mg/mL.
Intravenous: Dilute 1 g with 20 mL of sterile water for inj to make a concentration of 50 mg/mL to be administered in fluid-restricted patients or when rapid admin is required; for all other patients, further dilute with normal saline to a final concentration of 20 mg/mL.
Intravenous: Dilute 1 g with 20 mL of sterile water for inj to make a concentration of 50 mg/mL to be administered in fluid-restricted patients or when rapid admin is required; for all other patients, further dilute with normal saline to a final concentration of 20 mg/mL.
StorageView
Store between 20-25° C.
Pralidox
Pralidoxime Chloride
Pralidox
Pralidoxime Chloride
Indications
Organophosphorous poisoning
Indication detailsView
Pralidoxime chloride is indicated as an antidote:
- In the treatment of poisoning due to those pesticides and chemicals (e.g., nerve agents) of the organophosphate class which have anticholinesterase activity and
- In the control of overdosage by anticholinesterase drugs used in the treatment of myasthenia gravis.
Therapeutic classView
Antidote preparations
PharmacologyView
Pralidoxime reactivates cholinesterase outside the CNS that had been inactivated by phosphorylation due to exposure to certain organophosphates by displacing the enzyme from its receptor sites. It removes the phosphoryl group from the active site of the inactivated enzyme by nucleophilic attack, regenerating active cholinesterase and forming an oxime complex. It also detoxifies certain organophosphates by direct chemical reaction.
DosageView
Intramuscular-
Organophosphorus poisoning:- Adult: Mild: 600 mg, repeat 1-2 times at 15 min intervals as needed. Severe: 1.8 g given as 3 inj of 600 mg in rapid succession. Persistent: May repeat the entire series (1.8 g) beginning 1 hr after admin of the last inj.
- Child: <40 kg: Mild: 15 mg/kg, repeat as needed every 15 min. Max: 45 mg/kg. Severe: 15 mg/kg, repeat twice in rapid succession to a total dose of 45 mg/kg. Persistent: May repeat the entire series (45 mg/kg) beginning 1 hr after admin of the last inj; ≥40 kg: Same as adult dose.
Intravenous-
Organophosphorus poisoning:- Adult: In combination with atropine: Loading dose: 1-2 g by infusion over 15-30 min or slow inj over at least 5 min, may repeat dose after 1 hr then 10-12 hrly, as needed. Administer as soon as the effects of atropine are observed. Maintain atropinisation for at least 48 hr.
- Child: ≤16 yr Loading dose: 20-50 mg/kg (max: 2 g/dose) by inj over 15-30 min followed by 10-20 mg/kg/hr as continuous infusion. Alternatively, a repeat bolus of 20-50 mg/kg after 1 hr and repeated 10-12 hrly as needed; >16 yr Same as adult dose.
- Adult: Initially, 1-2 g, followed by 0.5-1 g/hr as infusion. Alternatively, the initial dose may be repeated after 1 hr and then 3-8 hrly as needed.
Side effectsView
Drowsiness, dizziness, visual disturbances, nausea, HTN, tachycardia, headache, hyperventilation, muscle weakness, impaired renal function, elevated liver enzymes, transient increase in creatine phosphokinase, transient neuromuscular blockade; mild to moderate pain at inj site.
ContraindicationsView
There are no known absolute contraindications for the use of Pralidoxime Chloride. Relative contraindications include known hypersensitivity to the drug and other situations in which the risk of its use clearly outweighs possible benefit.
PrecautionsView
Patient with myasthenia gravis receiving anticholinesterase agents. Not indicated in the treatment of poisoning due to phosphorous, inorganic phosphates, or organophosphates without anticholinesterase activity and carbamate pesticides. Renal impairment. Pregnancy and lactation.
Pregnancy & lactationView
Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Overdose effectsView
Manifestations of Overdosage: Observed in normal subjects only: dizziness, blurred vision, diplopia, headache, impaired accommodation, nausea, slight tachycardia. In therapy it has been difficult to differentiate side effects due to the drug from those due to the effects of the poison.
ReconstitutionView
Intramuscular: Dilute 1 g with 3.3 mL sterile water for inj to a final concentration of 300 mg/mL.
Intravenous: Dilute 1 g with 20 mL of sterile water for inj to make a concentration of 50 mg/mL to be administered in fluid-restricted patients or when rapid admin is required; for all other patients, further dilute with normal saline to a final concentration of 20 mg/mL.
Intravenous: Dilute 1 g with 20 mL of sterile water for inj to make a concentration of 50 mg/mL to be administered in fluid-restricted patients or when rapid admin is required; for all other patients, further dilute with normal saline to a final concentration of 20 mg/mL.
StorageView
Store between 20-25° C.
Pramax
Pantoprazole Sodium Sesquihydrate
Pramax
Pantoprazole Sodium Sesquihydrate
Indications
Zollinger-Ellison syndrome
Indication detailsView
Pantoprazole is indicated where suppression of acid secretion has therapeutic benefit; i.e
- Peptic ulcer diseases
- Gastroesophageal reflux diseases
- Ulcer induced by non-steroidal anti-inflammatory drugs (NSAIDs)
- Eradication of Helicobacter pylori (in combination with antibiotics)
- Zollinger-Ellison Syndrome
Therapeutic classView
Proton Pump Inhibitor
PharmacologyView
Pantoprazole is a proton pump inhibitor that suppresses the final step in gastric acid production by covalently binding to the H+/K+ATPase enzyme system at the surface of the gastric parietal cell. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus that persists longer than 24 hours.
DosageView
Oral:
IV Injection:
- Benign gastric ulcer: 40 mg daily in the morning for 4 weeks, continued for further 4 weeks, if not fully healed.
- Gastro-esophageal reflux disease: 20-40 mg daily in the morning for 4 weeks, continued for further 4 weeks, if not fully healed; maintenance dose is 20 mg daily, which may be increased to 40 mg daily.
- Duodenal ulcer: 40 mg daily in the morning for 2 weeks, continued for further 2 weeks if not fully healed.
- Duodenal ulcer associated with Helicobacter pylori: Pantoprazole is recommended at a dose of 40 mg twice daily in association with antimicrobial agents as detailed below: Amoxycillin 1 g and Clarithromycin 500 mg both twice daily for one week, or Clarithromycin 250 mg and Metronidazole 400 mg both twice daily for one week.
- Prophylaxis of NSAID-associated gastric or duodenal ulcer: 20 mg daily for those require long-term NSAID treatment.
- Zollinger-Ellison Syndrome: Initially 80 mg once daily adjusted according to response (elderly max. 40 mg daily); daily doses above 80 mg given in 2 divided doses.
IV Injection:
- Duodenal ulcer and gastric ulcer: 40 mg once daily for 7-10 days
- Gastroesophageal reflux disease associated with a history of erosive esophagitis: 40 mg once daily for 7-10 days
- Prevention of rebleeding in peptic ulcer: IV 80 mg, followed by 8 mg/hour infusion for 72 hours
- Prophylaxis of acid aspiration: 80 mg IV every 12 h for 24 h, followed by 40mg every 12 hour
- Long-term management of Zollinger-Ellison Syndrome and other pathological hypersecretory conditions: 80 mg IV every 12 hours, may increase to 80 mg every 8 hours if needed, may titrate to higher doses depending on acid output.
Side effectsView
Pantoprazole is well tolerated in both short-term and long-term treatment. Headache and diarrhea are the common side effects and rarely included side effects are abdominal pain, flatulence, rash, insomnia and hyperglycemia.
ContraindicationsView
Pantoprazole is contraindicated in patients with known hypersensitivity to any of the components of the formulation.
PrecautionsView
Patients should be cautioned that Pantoprazole tablet should not be split, chewed or crushed. Long-term therapy of Pantoprazole may lead to malabsorption of cyanocobalamin (Vitamin B12) or may increase the risk of osteoporosis related disorders.
InteractionsView
No significant drug interactions have been observed in clinical studies.
Pregnancy & lactationView
US FDA Pregnancy Category of Pantoprazole is B. There are, however, no adequate and well-controlled studies in pregnant woman. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. Pantoprazole has been shown to be excreted in human milk. So, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the benefit of the drug to the mother.
Overdose effectsView
There are no known symptoms of overdosage in humans. Since Pantoprazole is highly protein bound, it is not readily dialyzable. Apart from symptomatic and supportive management, no specific therapy is recommended.
ReconstitutionView
Direction for use of IV injection: Pantoprazole lyophilized powder and 0.9% Sodium Chloride Injection is for intravenous administration only and must not be given by any other route. Pantoprazole IV injection should be given as a slow intravenous injection. The solution for IV injection is obtained by adding 10 ml 0.9% Sodium Chloride Injection to the vial containing powder. After reconstitution the injection should be given slowly over a period of at least 2 to 5 minutes. Use only freshly prepared solution. The reconstituted solution may be stored at room temperature (up to 30° C) for a maximum 4 hours.
Direction for use of IV infusion: Pantoprazole IV infusion should be given as an intravenous infusion over a period of approximately 15 minutes. Pantoprazole IV infusion should be reconstituted with 10 ml of 0.9% Sodium Chloride Injection and further diluted (admixed) with 0.9% Sodium Chloride Injection or 5% Dextrose or Lactated Ringer's Injection to a final volume of 100 ml. The reconstituted solution may be stored at room temperature (up to 30° C) for a maximum 4 hours prior to further dilution. The admixed solution may be stored at room temperature (up to 30° C) and must be used within 24 hours from the time of initial reconstitution.
Direction for use of IV infusion: Pantoprazole IV infusion should be given as an intravenous infusion over a period of approximately 15 minutes. Pantoprazole IV infusion should be reconstituted with 10 ml of 0.9% Sodium Chloride Injection and further diluted (admixed) with 0.9% Sodium Chloride Injection or 5% Dextrose or Lactated Ringer's Injection to a final volume of 100 ml. The reconstituted solution may be stored at room temperature (up to 30° C) for a maximum 4 hours prior to further dilution. The admixed solution may be stored at room temperature (up to 30° C) and must be used within 24 hours from the time of initial reconstitution.
StorageView
Keep in a dry place, away from light and heat. Keep out of the reach of children.
Pramax
Pantoprazole Sodium Sesquihydrate
Pramax
Pantoprazole Sodium Sesquihydrate
Indications
Zollinger-Ellison syndrome
Indication detailsView
Pantoprazole is indicated where suppression of acid secretion has therapeutic benefit; i.e
- Peptic ulcer diseases
- Gastroesophageal reflux diseases
- Ulcer induced by non-steroidal anti-inflammatory drugs (NSAIDs)
- Eradication of Helicobacter pylori (in combination with antibiotics)
- Zollinger-Ellison Syndrome
Therapeutic classView
Proton Pump Inhibitor
PharmacologyView
Pantoprazole is a proton pump inhibitor that suppresses the final step in gastric acid production by covalently binding to the H+/K+ATPase enzyme system at the surface of the gastric parietal cell. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus that persists longer than 24 hours.
DosageView
Oral:
IV Injection:
- Benign gastric ulcer: 40 mg daily in the morning for 4 weeks, continued for further 4 weeks, if not fully healed.
- Gastro-esophageal reflux disease: 20-40 mg daily in the morning for 4 weeks, continued for further 4 weeks, if not fully healed; maintenance dose is 20 mg daily, which may be increased to 40 mg daily.
- Duodenal ulcer: 40 mg daily in the morning for 2 weeks, continued for further 2 weeks if not fully healed.
- Duodenal ulcer associated with Helicobacter pylori: Pantoprazole is recommended at a dose of 40 mg twice daily in association with antimicrobial agents as detailed below: Amoxycillin 1 g and Clarithromycin 500 mg both twice daily for one week, or Clarithromycin 250 mg and Metronidazole 400 mg both twice daily for one week.
- Prophylaxis of NSAID-associated gastric or duodenal ulcer: 20 mg daily for those require long-term NSAID treatment.
- Zollinger-Ellison Syndrome: Initially 80 mg once daily adjusted according to response (elderly max. 40 mg daily); daily doses above 80 mg given in 2 divided doses.
IV Injection:
- Duodenal ulcer and gastric ulcer: 40 mg once daily for 7-10 days
- Gastroesophageal reflux disease associated with a history of erosive esophagitis: 40 mg once daily for 7-10 days
- Prevention of rebleeding in peptic ulcer: IV 80 mg, followed by 8 mg/hour infusion for 72 hours
- Prophylaxis of acid aspiration: 80 mg IV every 12 h for 24 h, followed by 40mg every 12 hour
- Long-term management of Zollinger-Ellison Syndrome and other pathological hypersecretory conditions: 80 mg IV every 12 hours, may increase to 80 mg every 8 hours if needed, may titrate to higher doses depending on acid output.
Side effectsView
Pantoprazole is well tolerated in both short-term and long-term treatment. Headache and diarrhea are the common side effects and rarely included side effects are abdominal pain, flatulence, rash, insomnia and hyperglycemia.
ContraindicationsView
Pantoprazole is contraindicated in patients with known hypersensitivity to any of the components of the formulation.
PrecautionsView
Patients should be cautioned that Pantoprazole tablet should not be split, chewed or crushed. Long-term therapy of Pantoprazole may lead to malabsorption of cyanocobalamin (Vitamin B12) or may increase the risk of osteoporosis related disorders.
InteractionsView
No significant drug interactions have been observed in clinical studies.
Pregnancy & lactationView
US FDA Pregnancy Category of Pantoprazole is B. There are, however, no adequate and well-controlled studies in pregnant woman. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. Pantoprazole has been shown to be excreted in human milk. So, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the benefit of the drug to the mother.
Overdose effectsView
There are no known symptoms of overdosage in humans. Since Pantoprazole is highly protein bound, it is not readily dialyzable. Apart from symptomatic and supportive management, no specific therapy is recommended.
ReconstitutionView
Direction for use of IV injection: Pantoprazole lyophilized powder and 0.9% Sodium Chloride Injection is for intravenous administration only and must not be given by any other route. Pantoprazole IV injection should be given as a slow intravenous injection. The solution for IV injection is obtained by adding 10 ml 0.9% Sodium Chloride Injection to the vial containing powder. After reconstitution the injection should be given slowly over a period of at least 2 to 5 minutes. Use only freshly prepared solution. The reconstituted solution may be stored at room temperature (up to 30° C) for a maximum 4 hours.
Direction for use of IV infusion: Pantoprazole IV infusion should be given as an intravenous infusion over a period of approximately 15 minutes. Pantoprazole IV infusion should be reconstituted with 10 ml of 0.9% Sodium Chloride Injection and further diluted (admixed) with 0.9% Sodium Chloride Injection or 5% Dextrose or Lactated Ringer's Injection to a final volume of 100 ml. The reconstituted solution may be stored at room temperature (up to 30° C) for a maximum 4 hours prior to further dilution. The admixed solution may be stored at room temperature (up to 30° C) and must be used within 24 hours from the time of initial reconstitution.
Direction for use of IV infusion: Pantoprazole IV infusion should be given as an intravenous infusion over a period of approximately 15 minutes. Pantoprazole IV infusion should be reconstituted with 10 ml of 0.9% Sodium Chloride Injection and further diluted (admixed) with 0.9% Sodium Chloride Injection or 5% Dextrose or Lactated Ringer's Injection to a final volume of 100 ml. The reconstituted solution may be stored at room temperature (up to 30° C) for a maximum 4 hours prior to further dilution. The admixed solution may be stored at room temperature (up to 30° C) and must be used within 24 hours from the time of initial reconstitution.
StorageView
Keep in a dry place, away from light and heat. Keep out of the reach of children.
Pramin
Imipramine Hydrochloride
Pramin
Imipramine Hydrochloride
Indications
Urinary incontinence
Indication detailsView
Imipramine Hydrochloride is indicated in-
- Depressive illness
- Nocturnal enuresis in children.
Therapeutic classView
Tricyclic & related anti-depressant drugs, Tricyclic Anti-depressant
PharmacologyView
Imipramine works by inhibiting the neuronal reuptake of the neurotransmitters norepinephrine and serotonin. It binds the sodium-dependent serotonin transporter and sodium-dependent norepinephrine transporter reducing the reuptake of norepinephrine and serotonin by neurons. Depression has been linked to a lack of stimulation of the post-synaptic neuron by norepinephrine and serotonin. Slowing the reuptake of these neurotransmitters increases their concentration in the synaptic cleft, producing knock-on effects in protein kinase signaling which is thought to contribute to changes in neurotransmission and brain physiology which relieves symptoms of depression.
DosageView
Depression:
- Initially up to 75 mg daily in divided doses increased gradually to 150-200 mg (up to 300 mg in hospital patients)
- Up to 150 mg may be given as a single dose at bedtime
- Elderly initially 10 mg daily, increased gradually to 30-50 mg daily
- Child not recommended for depression
- Child 7-8 years: 25 mg
- 8-11 years: 25-50 mg
- Over 11 years: 50-75 mg at bedtime; max
Side effectsView
The most frequent of side effects are dry mouth, constipation, urinary retention, increased heart rate, sedation, irritability, dizziness, and decreased coordination. Dry mouth, if severe to the point of causing difficulty speaking or swallowing, may be managed by dosage reduction or temporary discontinuation of the drug. Imipramine usage has been linked to both increases and decreases in blood pressure and heart rate. Heart attacks, congestive heart failure, and strokes have been reported. Confusion, disorientation, delusions, insomnia, and anxiety have also been reported as side effects in a small percentage of people taking imipramine. Problems associated with the skin (loss of sensation, numbness and tingling, rashes, spots, itching and puffiness), seizures, and ringing in the ears have also been reported. Nausea, vomiting, loss of appetite, diarrhea, and abdominal cramping are all side effects associated with imipramine usage in a small number of people.
ContraindicationsView
Imipramine should not be given in conjunction with, or within 14 days of treatment with a MAO inhibitor. The combined therapy of this type could lead to the appearance of serious interactions such as hypertensive crises, hyperactivity, hyperpyrexia, spasticity, severe convulsions or coma and death may occur. Imipramine is contraindicated in patients with existing severe hepatic or renal damage, and those with a history of blood dyscrasias. Imipramine is contraindicated in patients who have shown hypersensitivity to the drug or hypersensitivity to tricyclic antidepressants belonging to the dibenzazepine group. Imipramine is contraindicated for use during the acute recovery phase following myocardial infarction. It should not be used in patients with convulsive disorders or glaucoma.
PrecautionsView
Imipramine should be used cautiously and with close physician supervision in people, especially the elderly, who have benign prostatic hypertrophy, urinary retention, and glaucoma, especially angle-closure glaucoma. The sedative effect is increased when imipramine is taken with other central nervous system depressants, such as alcoholic beverages, sleeping medications, other sedatives, or antihistamines. Imipramine may increase heart rate and stress on the heart. It may be dangerous for people with cardiovascular disease, especially those who have recently had a heart attack, to take this drug or other antidepressants in the same pharmacological class. Older people and persons with a history of heart disease may develop heart arrhythmias, heart conduction abnormalities, congestive heart failure, heart attack, abnormally rapid heart rates and strokes. Until a therapeutic dosage has been determined, people starting imipramine should be closely watched for signs of suicide. The risk of suicide is increased when imipramine is taken in overdose or combined with alcohol. Manic episodes and the emergence of symptoms of pre-existing psychotic states have been reported when imipramine therapy is started.
InteractionsView
Methylphenidate may increase the effects of imipramine. This is usually avoided by reducing the dosage of imipramine. Imipramine may increase the depressant action of alcohol. Dangerously high blood pressure has resulted from the combination of imipramine, and members of monoamine oxidase (MAO) inhibitors. Because of this, imipramine should never be taken in combination with MAO inhibitors. Patients taking any MAO inhibitors, for example phenelzine sulfate or tranylcypromine sulfate, should stop the MAO inhibitor then wait at least 14 days before starting imipramine or any other tricyclic antidepressant. The same holds true when discontinuing imipramine and starting an MAO inhibitor. The anticholinergic (drying out) effects of imipramine are additive with other anticholinergic drugs such as benztropine, biperiden, trihexyphenidyl, and antihistamines.
Pregnancy & lactationView
Pregnancy category D. Limited data suggest that imipramine is likely to be excreted in human breast milk. Known risk of damage to fetus.
Overdose effectsView
Children have been reported to be more sensitive than adults to an acute overdosage of imipramine. An acute overdose in infants or young children must be considered serious and potentially fatal.
StorageView
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
Prandil
Repaglinide
Prandil
Repaglinide
Indications
Type 2 DM
Indication detailsView
Repaglinide is indicated as an adjunct to diet and exercise to lower the blood glucose in patients with type 2 diabetes mellitus (NIDDM) whose hyperglycemia cannot be controlled satisfactorily by diet and exercise alone. It is also indicated for use in combination with Metformin to lower blood glucose in patients whose hyperglycemia cannot be controlled by exercise, diet, and either Repaglinide or Metformin alone.
Therapeutic classView
Meglitinide Analogues
PharmacologyView
Repaglinide binds to specific receptors in the cell membrane leading to the closure of ATP dependent K+ channels and the depolarisation of cell membrane. This in turn, leads to Ca++ influx, increased intracellular Ca++ and the stimulation of insulin secretion.
DosageView
- For patients not previously treated or whose HbA1c is <8%, the starting dose should be 0.5 mg before each meal.
- For patients previously treated with blood glucose-lowering drugs and whose HbA1c is >8%, the initial dose is 1 or 2 mg before each meal.
- Repaglinide should be taken immediately or up to 30 minutes before each meal.
- Dosage should be adjusted according to response at intervals of 1-2 weeks; up to 4 mg may be given as a single-dose, maximum 16 mg daily.
Side effectsView
The most common side effects of Repaglinide are hypoglycemia and related symptoms. Others include upper respiratory tract infections, diarrhea, constipation, nausea and vomiting. Hypersensitivity reactions include rashes and urticaria.
ContraindicationsView
Repaglinide is contraindicated in patients with:
- Diabetic ketoacidosis, with or without coma.
- Type 1 diabetes mellitus and
- Known hypersensitivity to the drug or its inactive ingredients.
PrecautionsView
Insulin should be substituted during concurrent illness (such as myocardial infarction, coma, infection, and trauma) and during surgery. All oral blood glucose-lowering drugs are capable of producing hypoglycemia. Repaglinide should be administered with meals to lessen the risk of hypoglycemia.
InteractionsView
The dose of Repaglinide may need to be adjusted, if taken with other medications. The possible interactions of Repaglinide with other drugs are:
- Inhibitors of the cytochrome P450 enzyme system (azole antifungals and macrolides) may lead to lower Repaglinide clearance and longer half life.
- Inducers of the cytochrome P450 enzyme system (Rifampin, Phenobarbital, Carbamazepine, Troglitazone, etc.) may accelerate Repaglinide metabolism and shorten its effect.
- Cimetidine has no significant effect on Repaglinide absorption or clearance.
- Repaglinide has no significant effect on Digoxin, Theophyllin, or Warfarin.
- Highly protein bound drugs (e.g., NSAIDs) may increase the plasma level of unbound Repaglinide and potentiate its glucose lowering effect. Thus, co-administration of these drugs with Repaglinide may increase the risk of hypoglycaemia.
- The risk of hypoglycaemia may also be increased when hypoglycaemic agents are co-administered with certain drugs such as salicylates, sulphonamides, Chloramphenicol, coumarins, Probenecid, monoamine oxidase (MAO) inhibitors, and adrenergic blockers.
Pregnancy & lactationView
Safety in pregnant women has not been established. Repaglinide should be used during pregnancy only if it is clearly needed. It is not known whether Repaglinide 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 Repaglinide, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the mother.
Overdose effectsView
Patients receiving up to 80 mg of Repaglinide developed few adverse effects other than lowering of blood glucose. Hypoglycemia did not occur when meals were given with these high doses. Severe hypoglycemic reactions with coma, seizure or other neurological impairment occur infrequently.
StorageView
Do not store above 30°C. Keep away from light and out of the reach of children.
Prapid
Prasugrel Hydrochloride
Prapid
Prasugrel Hydrochloride
Indications
Unstable angina
Indication detailsView
Prasugrel is indicated to reduce the rate of thrombotic cardiovascular (CV) events (including stent thrombosis) in patients with acute coronary syndrome (ACS) who are to be managed with percutaneous coronary intervention (PCI) as follows:
- Patients with unstable angina (UA) or non-ST-elevation myocardial infarction (NSTEMI).
- Patients with ST-elevation myocardial infarction (STEMI) when managed with primary or delayed PCI.
Therapeutic classView
Anti-platelet drugs
PharmacologyView
Prasugrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets.
DosageView
Treatment should be initiated with a single 60 mg oral loading dose. Continue at 10 mg once daily with or without food. Consider 5 mg once daily for patients <60 kg. Patients should also take aspirin (75 mg to 325 mg) daily.
Side effectsView
- Bleeding
- Thrombotic thrombocytopenic purpura
- Other side effects (Headache, back pain, dyspnea, nausea, hypertension, bradycardia, rash etc)
ContraindicationsView
- Active pathological bleeding such as peptic ulcer or intracranial haemorrhage.
- Patient with a history of prior transient ischemic attack or stroke
PrecautionsView
- CABG-related bleeding: Risk increases in patients receiving Prasugrel who undergo CABG.
- Discontinuation of Prasugrel: Premature discontinuation increases risk of stent thrombosis, MI, and death
InteractionsView
- Coadministration of Prasugrel and warfarin increases the risk of bleeding.
- Coadministration of Prasugrel and NSAIDs (used chronically) may increase the risk of bleeding.
- Prasugrel can be administered with drugs that are inducers or inhibitors of cytochrome P450 enzymes. Prasugrel can be administered with aspirin (75 mg to 325 mg per day), heparin, GPIIb/IIIa inhibitors, statins, and drugs that elevate gastric pH, including proton pump inhibitors and H2 blockers.
Pregnancy & lactationView
There are no adequate and well-controlled studies of Prasugrel use in pregnant women. Reproductive and developmental toxicology studies in rats and rabbits at doses of up to 30 times the recommended therapeutic exposures in humans revealed no evidence of fetal harm; however, animal studies are not always predictive of a human response.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
Pediatric usageView
Pediatric Use: Safety and effectiveness in pediatric patients have not been established.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Overdose effectsView
In rats, lethality was observed after administration of 2000 mg/kg. Platelet transfusion may restore clotting ability. The prasugrel active metabolite is not likely to be removed by dialysis.
StorageView
Keep in dry place and away from light and heat. Keep out of the reach of children.
Prapid
Prasugrel Hydrochloride
Prapid
Prasugrel Hydrochloride
Indications
Unstable angina
Indication detailsView
Prasugrel is indicated to reduce the rate of thrombotic cardiovascular (CV) events (including stent thrombosis) in patients with acute coronary syndrome (ACS) who are to be managed with percutaneous coronary intervention (PCI) as follows:
- Patients with unstable angina (UA) or non-ST-elevation myocardial infarction (NSTEMI).
- Patients with ST-elevation myocardial infarction (STEMI) when managed with primary or delayed PCI.
Therapeutic classView
Anti-platelet drugs
PharmacologyView
Prasugrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets.
DosageView
Treatment should be initiated with a single 60 mg oral loading dose. Continue at 10 mg once daily with or without food. Consider 5 mg once daily for patients <60 kg. Patients should also take aspirin (75 mg to 325 mg) daily.
Side effectsView
- Bleeding
- Thrombotic thrombocytopenic purpura
- Other side effects (Headache, back pain, dyspnea, nausea, hypertension, bradycardia, rash etc)
ContraindicationsView
- Active pathological bleeding such as peptic ulcer or intracranial haemorrhage.
- Patient with a history of prior transient ischemic attack or stroke
PrecautionsView
- CABG-related bleeding: Risk increases in patients receiving Prasugrel who undergo CABG.
- Discontinuation of Prasugrel: Premature discontinuation increases risk of stent thrombosis, MI, and death
InteractionsView
- Coadministration of Prasugrel and warfarin increases the risk of bleeding.
- Coadministration of Prasugrel and NSAIDs (used chronically) may increase the risk of bleeding.
- Prasugrel can be administered with drugs that are inducers or inhibitors of cytochrome P450 enzymes. Prasugrel can be administered with aspirin (75 mg to 325 mg per day), heparin, GPIIb/IIIa inhibitors, statins, and drugs that elevate gastric pH, including proton pump inhibitors and H2 blockers.
Pregnancy & lactationView
There are no adequate and well-controlled studies of Prasugrel use in pregnant women. Reproductive and developmental toxicology studies in rats and rabbits at doses of up to 30 times the recommended therapeutic exposures in humans revealed no evidence of fetal harm; however, animal studies are not always predictive of a human response.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
Pediatric usageView
Pediatric Use: Safety and effectiveness in pediatric patients have not been established.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Overdose effectsView
In rats, lethality was observed after administration of 2000 mg/kg. Platelet transfusion may restore clotting ability. The prasugrel active metabolite is not likely to be removed by dialysis.
StorageView
Keep in dry place and away from light and heat. Keep out of the reach of children.
Prasulet
Prasugrel Hydrochloride
Prasulet
Prasugrel Hydrochloride
Indications
Unstable angina
Indication detailsView
Prasugrel is indicated to reduce the rate of thrombotic cardiovascular (CV) events (including stent thrombosis) in patients with acute coronary syndrome (ACS) who are to be managed with percutaneous coronary intervention (PCI) as follows:
- Patients with unstable angina (UA) or non-ST-elevation myocardial infarction (NSTEMI).
- Patients with ST-elevation myocardial infarction (STEMI) when managed with primary or delayed PCI.
Therapeutic classView
Anti-platelet drugs
PharmacologyView
Prasugrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets.
DosageView
Treatment should be initiated with a single 60 mg oral loading dose. Continue at 10 mg once daily with or without food. Consider 5 mg once daily for patients <60 kg. Patients should also take aspirin (75 mg to 325 mg) daily.
Side effectsView
- Bleeding
- Thrombotic thrombocytopenic purpura
- Other side effects (Headache, back pain, dyspnea, nausea, hypertension, bradycardia, rash etc)
ContraindicationsView
- Active pathological bleeding such as peptic ulcer or intracranial haemorrhage.
- Patient with a history of prior transient ischemic attack or stroke
PrecautionsView
- CABG-related bleeding: Risk increases in patients receiving Prasugrel who undergo CABG.
- Discontinuation of Prasugrel: Premature discontinuation increases risk of stent thrombosis, MI, and death
InteractionsView
- Coadministration of Prasugrel and warfarin increases the risk of bleeding.
- Coadministration of Prasugrel and NSAIDs (used chronically) may increase the risk of bleeding.
- Prasugrel can be administered with drugs that are inducers or inhibitors of cytochrome P450 enzymes. Prasugrel can be administered with aspirin (75 mg to 325 mg per day), heparin, GPIIb/IIIa inhibitors, statins, and drugs that elevate gastric pH, including proton pump inhibitors and H2 blockers.
Pregnancy & lactationView
There are no adequate and well-controlled studies of Prasugrel use in pregnant women. Reproductive and developmental toxicology studies in rats and rabbits at doses of up to 30 times the recommended therapeutic exposures in humans revealed no evidence of fetal harm; however, animal studies are not always predictive of a human response.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
Pediatric usageView
Pediatric Use: Safety and effectiveness in pediatric patients have not been established.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Overdose effectsView
In rats, lethality was observed after administration of 2000 mg/kg. Platelet transfusion may restore clotting ability. The prasugrel active metabolite is not likely to be removed by dialysis.
StorageView
Keep in dry place and away from light and heat. Keep out of the reach of children.
Prasulet
Prasugrel Hydrochloride
Prasulet
Prasugrel Hydrochloride
Indications
Unstable angina
Indication detailsView
Prasugrel is indicated to reduce the rate of thrombotic cardiovascular (CV) events (including stent thrombosis) in patients with acute coronary syndrome (ACS) who are to be managed with percutaneous coronary intervention (PCI) as follows:
- Patients with unstable angina (UA) or non-ST-elevation myocardial infarction (NSTEMI).
- Patients with ST-elevation myocardial infarction (STEMI) when managed with primary or delayed PCI.
Therapeutic classView
Anti-platelet drugs
PharmacologyView
Prasugrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets.
DosageView
Treatment should be initiated with a single 60 mg oral loading dose. Continue at 10 mg once daily with or without food. Consider 5 mg once daily for patients <60 kg. Patients should also take aspirin (75 mg to 325 mg) daily.
Side effectsView
- Bleeding
- Thrombotic thrombocytopenic purpura
- Other side effects (Headache, back pain, dyspnea, nausea, hypertension, bradycardia, rash etc)
ContraindicationsView
- Active pathological bleeding such as peptic ulcer or intracranial haemorrhage.
- Patient with a history of prior transient ischemic attack or stroke
PrecautionsView
- CABG-related bleeding: Risk increases in patients receiving Prasugrel who undergo CABG.
- Discontinuation of Prasugrel: Premature discontinuation increases risk of stent thrombosis, MI, and death
InteractionsView
- Coadministration of Prasugrel and warfarin increases the risk of bleeding.
- Coadministration of Prasugrel and NSAIDs (used chronically) may increase the risk of bleeding.
- Prasugrel can be administered with drugs that are inducers or inhibitors of cytochrome P450 enzymes. Prasugrel can be administered with aspirin (75 mg to 325 mg per day), heparin, GPIIb/IIIa inhibitors, statins, and drugs that elevate gastric pH, including proton pump inhibitors and H2 blockers.
Pregnancy & lactationView
There are no adequate and well-controlled studies of Prasugrel use in pregnant women. Reproductive and developmental toxicology studies in rats and rabbits at doses of up to 30 times the recommended therapeutic exposures in humans revealed no evidence of fetal harm; however, animal studies are not always predictive of a human response.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
Pediatric usageView
Pediatric Use: Safety and effectiveness in pediatric patients have not been established.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Overdose effectsView
In rats, lethality was observed after administration of 2000 mg/kg. Platelet transfusion may restore clotting ability. The prasugrel active metabolite is not likely to be removed by dialysis.
StorageView
Keep in dry place and away from light and heat. Keep out of the reach of children.
Prasurel
Prasugrel Hydrochloride
Prasurel
Prasugrel Hydrochloride
Indications
Unstable angina
Indication detailsView
Prasugrel is indicated to reduce the rate of thrombotic cardiovascular (CV) events (including stent thrombosis) in patients with acute coronary syndrome (ACS) who are to be managed with percutaneous coronary intervention (PCI) as follows:
- Patients with unstable angina (UA) or non-ST-elevation myocardial infarction (NSTEMI).
- Patients with ST-elevation myocardial infarction (STEMI) when managed with primary or delayed PCI.
Therapeutic classView
Anti-platelet drugs
PharmacologyView
Prasugrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets.
DosageView
Treatment should be initiated with a single 60 mg oral loading dose. Continue at 10 mg once daily with or without food. Consider 5 mg once daily for patients <60 kg. Patients should also take aspirin (75 mg to 325 mg) daily.
Side effectsView
- Bleeding
- Thrombotic thrombocytopenic purpura
- Other side effects (Headache, back pain, dyspnea, nausea, hypertension, bradycardia, rash etc)
ContraindicationsView
- Active pathological bleeding such as peptic ulcer or intracranial haemorrhage.
- Patient with a history of prior transient ischemic attack or stroke
PrecautionsView
- CABG-related bleeding: Risk increases in patients receiving Prasugrel who undergo CABG.
- Discontinuation of Prasugrel: Premature discontinuation increases risk of stent thrombosis, MI, and death
InteractionsView
- Coadministration of Prasugrel and warfarin increases the risk of bleeding.
- Coadministration of Prasugrel and NSAIDs (used chronically) may increase the risk of bleeding.
- Prasugrel can be administered with drugs that are inducers or inhibitors of cytochrome P450 enzymes. Prasugrel can be administered with aspirin (75 mg to 325 mg per day), heparin, GPIIb/IIIa inhibitors, statins, and drugs that elevate gastric pH, including proton pump inhibitors and H2 blockers.
Pregnancy & lactationView
There are no adequate and well-controlled studies of Prasugrel use in pregnant women. Reproductive and developmental toxicology studies in rats and rabbits at doses of up to 30 times the recommended therapeutic exposures in humans revealed no evidence of fetal harm; however, animal studies are not always predictive of a human response.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
Pediatric usageView
Pediatric Use: Safety and effectiveness in pediatric patients have not been established.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Overdose effectsView
In rats, lethality was observed after administration of 2000 mg/kg. Platelet transfusion may restore clotting ability. The prasugrel active metabolite is not likely to be removed by dialysis.
StorageView
Keep in dry place and away from light and heat. Keep out of the reach of children.
Prasurel
Prasugrel Hydrochloride
Prasurel
Prasugrel Hydrochloride
Indications
Unstable angina
Indication detailsView
Prasugrel is indicated to reduce the rate of thrombotic cardiovascular (CV) events (including stent thrombosis) in patients with acute coronary syndrome (ACS) who are to be managed with percutaneous coronary intervention (PCI) as follows:
- Patients with unstable angina (UA) or non-ST-elevation myocardial infarction (NSTEMI).
- Patients with ST-elevation myocardial infarction (STEMI) when managed with primary or delayed PCI.
Therapeutic classView
Anti-platelet drugs
PharmacologyView
Prasugrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets.
DosageView
Treatment should be initiated with a single 60 mg oral loading dose. Continue at 10 mg once daily with or without food. Consider 5 mg once daily for patients <60 kg. Patients should also take aspirin (75 mg to 325 mg) daily.
Side effectsView
- Bleeding
- Thrombotic thrombocytopenic purpura
- Other side effects (Headache, back pain, dyspnea, nausea, hypertension, bradycardia, rash etc)
ContraindicationsView
- Active pathological bleeding such as peptic ulcer or intracranial haemorrhage.
- Patient with a history of prior transient ischemic attack or stroke
PrecautionsView
- CABG-related bleeding: Risk increases in patients receiving Prasugrel who undergo CABG.
- Discontinuation of Prasugrel: Premature discontinuation increases risk of stent thrombosis, MI, and death
InteractionsView
- Coadministration of Prasugrel and warfarin increases the risk of bleeding.
- Coadministration of Prasugrel and NSAIDs (used chronically) may increase the risk of bleeding.
- Prasugrel can be administered with drugs that are inducers or inhibitors of cytochrome P450 enzymes. Prasugrel can be administered with aspirin (75 mg to 325 mg per day), heparin, GPIIb/IIIa inhibitors, statins, and drugs that elevate gastric pH, including proton pump inhibitors and H2 blockers.
Pregnancy & lactationView
There are no adequate and well-controlled studies of Prasugrel use in pregnant women. Reproductive and developmental toxicology studies in rats and rabbits at doses of up to 30 times the recommended therapeutic exposures in humans revealed no evidence of fetal harm; however, animal studies are not always predictive of a human response.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
Pediatric usageView
Pediatric Use: Safety and effectiveness in pediatric patients have not been established.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Overdose effectsView
In rats, lethality was observed after administration of 2000 mg/kg. Platelet transfusion may restore clotting ability. The prasugrel active metabolite is not likely to be removed by dialysis.
StorageView
Keep in dry place and away from light and heat. Keep out of the reach of children.
Prasuva
Prasugrel Hydrochloride
Prasuva
Prasugrel Hydrochloride
Indications
Unstable angina
Indication detailsView
Prasugrel is indicated to reduce the rate of thrombotic cardiovascular (CV) events (including stent thrombosis) in patients with acute coronary syndrome (ACS) who are to be managed with percutaneous coronary intervention (PCI) as follows:
- Patients with unstable angina (UA) or non-ST-elevation myocardial infarction (NSTEMI).
- Patients with ST-elevation myocardial infarction (STEMI) when managed with primary or delayed PCI.
Therapeutic classView
Anti-platelet drugs
PharmacologyView
Prasugrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets.
DosageView
Treatment should be initiated with a single 60 mg oral loading dose. Continue at 10 mg once daily with or without food. Consider 5 mg once daily for patients <60 kg. Patients should also take aspirin (75 mg to 325 mg) daily.
Side effectsView
- Bleeding
- Thrombotic thrombocytopenic purpura
- Other side effects (Headache, back pain, dyspnea, nausea, hypertension, bradycardia, rash etc)
ContraindicationsView
- Active pathological bleeding such as peptic ulcer or intracranial haemorrhage.
- Patient with a history of prior transient ischemic attack or stroke
PrecautionsView
- CABG-related bleeding: Risk increases in patients receiving Prasugrel who undergo CABG.
- Discontinuation of Prasugrel: Premature discontinuation increases risk of stent thrombosis, MI, and death
InteractionsView
- Coadministration of Prasugrel and warfarin increases the risk of bleeding.
- Coadministration of Prasugrel and NSAIDs (used chronically) may increase the risk of bleeding.
- Prasugrel can be administered with drugs that are inducers or inhibitors of cytochrome P450 enzymes. Prasugrel can be administered with aspirin (75 mg to 325 mg per day), heparin, GPIIb/IIIa inhibitors, statins, and drugs that elevate gastric pH, including proton pump inhibitors and H2 blockers.
Pregnancy & lactationView
There are no adequate and well-controlled studies of Prasugrel use in pregnant women. Reproductive and developmental toxicology studies in rats and rabbits at doses of up to 30 times the recommended therapeutic exposures in humans revealed no evidence of fetal harm; however, animal studies are not always predictive of a human response.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
It is not known whether Prasugrel is excreted in human milk. Because many drugs are excreted in human milk, Prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.
Pediatric usageView
Pediatric Use: Safety and effectiveness in pediatric patients have not been established.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Geriatric Use: Patients > 75 years of age who received Prasugrel had an increased risk of fatal bleeding events (1.0%) compared to patients who received Clopidogrel (0.1%).
Renal Impairment: No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
Overdose effectsView
In rats, lethality was observed after administration of 2000 mg/kg. Platelet transfusion may restore clotting ability. The prasugrel active metabolite is not likely to be removed by dialysis.
StorageView
Keep in dry place and away from light and heat. Keep out of the reach of children.