৳ 50/unit
Pack: ৳ 500
৳ 50/unit
Pack: ৳ 500
At a glance
Bosentan is an endothelin receptor antagonist used in the treatment of pulmonary arterial hypertension (PAH). It dilates pulmonary blood vessels, improves blood flow, and delays disease progression.
Indications
- Pulmonary arterial hypertension (PAH) - WHO functional class II and III
Pharmacology
Bosentan is a dual endothelin receptor antagonist (ERA) with affinity for both ETA and ETB receptors. It blocks the vasoconstrictive, pro-fibrotic, and pro-inflammatory effects of endothelin-1 (ET-1). Bosentan decreases pulmonary and systemic vascular resistance, increasing cardiac output. It is metabolized in the liver by CYP2C9 and CYP3A4 and eliminated via biliary excretion. Bioavailability is approximately 50%, plasma protein binding is >98%, and peak plasma concentration is reached within 3-5 hours.
Dosage
Adults (>12 years, >40 kg):
First 4 weeks: 62.5 mg twice daily
Maintenance dose: 125 mg twice daily
Children (≥2 years): 2 mg/kg twice daily (optimal maintenance dose not established in controlled studies)
Elderly (≥65 years): No dose adjustment needed
Hepatic impairment: Mild (Child-Pugh A): No dose adjustment; Moderate-severe (Child-Pugh B/C): Contraindicated
Renal impairment: No dose adjustment needed; dialysis patients also require no adjustment
Discontinuation: Do not stop abruptly (withdraw gradually over 3-7 days by reducing to half the dose to minimize risk of clinical deterioration)
Side effects
Common side effects:
Headache, ankle swelling (edema), diarrhea, anemia (hemoglobin decrease), respiratory tract infection.
Hepatic: Dose-dependent elevations in liver aminotransferases, hepatitis, jaundice, rare cases of liver cirrhosis and liver failure.
Other: Thrombocytopenia, neutropenia, leukopenia, hypersensitivity reactions, syncope, palpitations, flushing, hypotension, gastroesophageal reflux disease, erythema.
Use in pregnancy
Highly unsafe during pregnancy (Category X). Studies on pregnant women and animals have shown significant harmful effects to the developing baby. Women of reproductive potential must use reliable contraception during treatment and for 1 month after stopping.
Pregnancy Category: X — always consult a doctor before taking during pregnancy.
Precautions & warnings
- Liver aminotransferases (AST/ALT) must be measured prior to initiation and monthly during treatment; measure 2 weeks after any dose increase.
- Monitor hemoglobin for anemia.
- Do not stop abruptly (withdraw gradually over 3-7 days by reducing to half the dose to minimize risk of clinical deterioration).
- Consider discontinuation if pulmonary edema occurs.
- Highly unsafe during pregnancy (Category X); women of reproductive potential must use reliable contraception during and for 1 month after stopping treatment.
- May cause dizziness; know your response before driving or operating machinery.
- Inform your doctor if you notice yellowing of skin/eyes, dark urine, stomach pain, weight gain, swelling of arms/legs, or difficulty breathing.
Overdose effects
Overdose may cause severe hypotension, headache, nausea, and elevated liver enzymes. Consult your doctor if overdose is suspected.
Storage conditions
Store below 30°C in a cool, dry place, protected from light. Keep out of reach of children.