Description

Simple

A medication used to lower blood pressure in the arteries that connect the heart and lungs.

Clinical

An endothelin receptor antagonist used to manage pulmonary arterial hypertension to delay disease progression.

Overview

Macitentan was approved in October 2013. It is indicated for patients with pulmonary arterial hypertension, and is marketed under the brand name Opsumit. Macitentan is an antagonist/blocker of endothelin receptors on blood vessels and smooth muscle, and, thus, blocks the stimulation of vasculature hypertrophy, inflammation, fibrosis, proliferation, and vasoconstriction. Similar to all drugs acting on the renin-angiotensin system, macitentan is associated with embryo and fetal toxicity, so it should not be used in pregnancy and has special precautions that must be followed for all females of child-bearing age.

Pharmacology

Indication

Macitentan is indicated for patients with pulmonary arterial hypertension.

Pharmacodynamic

Macitentan blocks simulators of hypertrophy, inflammation, fibrosis, proliferation, and vasoconstriction.

Mechanism of action

Macitentan is an antagonist/blocker of endothelin receptors. Endothelin receptors are found in the endothelial cells of blood vessels and smooth muscle. Macitentan binds to the receptors, endothelin A and B (ETA and ETB), which prevents the agonist endothelin -1 (ET-1) from binding and stimulating t... Read more

Absorption

Macitentan is administered orally, and it take about 8 hours for maximum plasma concentrations to be reached.

Protein binding

Macitentan is >99% bound to plasma proteins, which are mainly albumin

Volume of distribution

Macitentan has a volume of distribution of 50L.

Clearance

Clearance data was not found.

Half life

The half life of macitentan is 16 hours, and the half life of it's active metabolite is 48 hours.

Route of elimination

Eliminated 50% through urine and 24% through feces.

Toxicity

Macitentan has a black box warning of embryo-fetal toxicity. Special precautions must be taken for all females of child-bearing age, and women who are pregnant must not be given macitentan.

Adverse Effects

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Pregnancy
      • Drugbank Id: DBCOND0018394

Food Interactions

  • Take with or without food.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
1-benzylimidazole
1-benzylimidazole may decrease the antihypertensive activities of Macitentan.
2,5-Dimethoxy-4-ethylamphetamine
2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Macitentan.
2,5-Dimethoxy-4-ethylthioamphetamine
2,5-Dimethoxy-4-ethylthioamphetamine may decrease the antihypertensive activities of Macitentan.
4-Bromo-2,5-dimethoxyamphetamine
4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Macitentan.
4-Methoxyamphetamine
4-Methoxyamphetamine may decrease the antihypertensive activities of Macitentan.
5-methoxy-N,N-dimethyltryptamine
5-methoxy-N,N-dimethyltryptamine may decrease the antihypertensive activities of Macitentan.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypotensive activities of Macitentan.
Abacavir
Abacavir may decrease the excretion rate of Macitentan which could result in a higher serum level.
Abediterol
Abediterol may decrease the antihypertensive activities of Macitentan.
Acarbose
Acarbose may decrease the excretion rate of Macitentan which could result in a higher serum level.
Acebutolol
The therapeutic efficacy of Macitentan can be increased when used in combination with Acebutolol.
Aceclofenac
The therapeutic efficacy of Macitentan can be decreased when used in combination with Aceclofenac.
Acemetacin
The therapeutic efficacy of Macitentan can be decreased when used in combination with Acemetacin.
Acepromazine
Acepromazine may decrease the antihypertensive activities of Macitentan.
Acetaminophen
Acetaminophen may decrease the excretion rate of Macitentan which could result in a higher serum level.
Acetazolamide
Acetazolamide may increase the excretion rate of Macitentan which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acid
The therapeutic efficacy of Macitentan can be decreased when used in combination with Acetylsalicylic acid.
Aclidinium
Aclidinium may decrease the excretion rate of Macitentan which could result in a higher serum level.
Acrivastine
Macitentan may decrease the excretion rate of Acrivastine which could result in a higher serum level.
Acyclovir
Acyclovir may decrease the excretion rate of Macitentan which could result in a higher serum level.
1 References
  1. 1 . Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, Iglarz M, Meyer S, Rein J, Rey M, Treiber A, Clozel M, Fischli W, Weller T: The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-p ropylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist. J Med Chem. 2012 Sep 13;55(17):7849-61. doi: 10.1021/jm3009103. Epub 2012 Aug 16.PubMed: 22862294