Macitentan

Drug #2332

macitentan) is an endothelin receptor antagonist. The chemical name of macitentan is N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'- propylsulfamide. Macitentan is indicated for the treatment of Pulmonary Arterial Hypertension (PAH, WHO GROUP I) to delay disease progression.

← Previous drug Next drug →

Primary Characteristics

It is of Synthetic origin.

Molecular Weight: 588.27 · Solubility in Water: insoluble · Non-proprietary name: Macitentan.

Pharmacokinetics

Distribution: Macitentan has a volume of distribution is 50L. plasma protein binding is greater than 99%.

Elimination: it is metabolised via hepatic, plasma half-life is 16hrs, renal excretion is 50% by urine & 24% by feces.

Indications

Macitentan is primarily indicated in conditions like pulmonary arterial hypertension.

Contraindications

None recorded.

Dosage

Macitentan's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
0 – 10 mg	—	—	PO	Doses higher than 10 mg once daily have not been studied in patients with PAH and are not recommended
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

3 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

Macitentan is known to cause more or less tolerable side effects which are usually transient. These include Bronchitis , Headache, influenza, Nasopharyngitis, Pharyngitis, urinary tract infection.

Warnings / Precautions

Other ERAs cause hepatotoxicity and liver failure. Obtain baseline liver enzymes and monitor as clinically indicated . Decreases in hemoglobin . Pulmonary edema in patients with pulmonary veno-occlusive disease. If confirmed, discontinue treatment. Decreases in sperm count have been observed in patients taking ERA.

Available Brands

None recorded.

Drug Classification

1.12.3.7 — Direct vasodilators