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Macitentan

Vasodilator · Antihypertensive

VasodilatorAntihypertensive
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 12
  • AmprenavirSevereDatabaseDDInter
  • ApalutamideSevereDatabaseDDInter
  • AtazanavirSevereDatabaseDDInter
  • BoceprevirSevereDatabaseDDInter

Mechanism

Macitentan is a dual endothelin receptor antagonist. It was developed by modifying the structure of bosentan, which is a nonselective ET receptor antagonist. It blocks both the initial transient depressor (ETB) and the prolonged pressor (ETA) responses to endothelin.

Indications

Pulmonary arterial hypertensionimproved time to disease progression or death in PAHimproved symptoms, functional capacity, and pulmonary hemodynamic measurementsmoderate PAH (functional class II–III)

Dosing

Adult
reduce blood pressure rapidly after the first dose and should be introduced with caution. Doxazosin, indoramin p. 827, and terazosin have properties similar to those of prazosin. Hypertension 155 Alpha-blockers can be used with other antihypertensive drugs in the treatment of resistant hypertension. . receiving high-dose vasodilator therapy; . known renovascular disease.…

Pharmacokinetics

Half-life
16 h (parent compound), 48 h (active metabolite)
Metabolism
Metabolized by CYPs, including CYP3A4, to an active metabolite.

Side effects

Common
headachepulmonary edemaperipheral edemaanemianasal congestion/pharyngitisnasopharyngitis
Serious
  • embryo-fetal toxicity (potent teratogen, FDA-mandated REMS program)
  • testicular atrophy
  • infertility

Drug interactions

Amprenavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Apalutamide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Atazanavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Boceprevir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Carbamazepine
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Ceritinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Clarithromycin
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Cobicistat
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Conivaptan
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Delavirdine
Severe
Database

Clinical effect not specified

Source: DDInter

Enzalutamide
Severe
Database

Clinical effect not specified

Source: DDInter

Erythromycin
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

Other Vasodilator drugs

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Sources: Goodman & Gilman 14e, BNF·Verified: 2026-05-13 · House clinical team