Bosentan
Bosentan is an endothelin receptor antagonist, used in the treatment of pulmonary arterial hypertension and heart failure.
Primary Characteristics
It is of Synthetic origin.
It belongs to Vasodilators pharmacological group on the basis of mechanism of action.
Molecular Weight: 551.61 · Solubility in Water: poorly soluble · Non-proprietary name: Bosentan.
Pharmacokinetics
Distribution: Bosentan has a plasma protein binding is >98%.
Elimination: it is metabolised via Hepatic, plasma half-life is 5 hrs.
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Indications
Bosentan is primarily indicated in conditions like Nausea and vomiting (palliative care).
Contraindications
Bosentan is contraindicated in conditions like Hepatic impairment, Pregnancy, Breast feeding.
Dosage
Bosentan's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 62.5 mg twice a day | 62.5 mg twice a day | — | PO | This dose should be taken for 4 weeks and then increase to 125 mg two times daily. |
| Paediatric Dosage (20kg) | ||||
| No data. | ||||
| Neonatal Dosage (3kg) | ||||
| No data. | ||||
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Bosentan is known to cause more or less tolerable side effects which are usually transient. These include Anemia, Dyspepsia , Edema, Fatigue, Flushing, Hypotension , Nasopharyngitis, Palpitation, Pruritus .
Warnings / Precautions
Interference in Pathology
Bosentan may interfere in the diagnosis of Elevation in ALT or AST.
Available Brands
Storage Conditions
Drug Classification
- 1.12.3.7 — Direct vasodilators
Manufacturers
Manufacturers of Bosentan in Pakistan: