Macitentan

Macitentan Uses, Dosage, Side Effects, Food Interaction and all others data.

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.

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

Table Of contents

• Macitentan
• Uses
• Dosage
• Side Effect
• Precautions
• Interactions
• Uses during Pregnancy
• Uses during Breastfeeding
• Accute Overdose
• Food Interaction
• Half Life
• Volume of Distribution
• Clearance
• Interaction With other Medicine
• Contradiction
• Storage

Trade Name	Macitentan
Availability	Prescription only
Generic	Macitentan
Macitentan Other Names	Macitentán, Macitentan, Macitentanum
Related Drugs	sildenafil, tadalafil, Revatio, Adempas, Opsumit, ambrisentan
Weight	10mg
Type	Oral tablet
Formula	C19H20Br2N6O4S
Weight	Average: 588.273 Monoisotopic: 585.963349142
Protein binding	Macitentan is >99% bound to plasma proteins, which are mainly albumin
Groups	Approved
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Macitentan is an endothelin receptor antagonist used to manage pulmonary arterial hypertension to delay disease progression.

Macitentan is indicated for patients with pulmonary arterial hypertension.

Macitentan is also used to associated treatment for these conditions: Pulmonary Arterial Hypertension (PAH) (WHO Group 1 PH)

How Macitentan works

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 the ETA and ETB receptors.

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.

Food Interaction

• Take with or without food.

Macitentan Drug Interaction

Moderate: diltiazemUnknown: charcoal, tadalafil, fluticasone / salmeterol, diphenhydramine, fluticasone / vilanterol, rosuvastatin, glucose, ferrous sulfate, clonazepam, furosemide, levothyroxine, metoprolol, metoprolol, acetaminophen, selexipag, liraglutide, cyanocobalamin, cholecalciferol, sertraline

Macitentan Disease Interaction

Major: hepatotoxicity/liver impairmentModerate: anemia, fluid retention

Volume of Distribution

Macitentan has a volume of distribution of 50L.

Elimination Route

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

Half Life

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

Clearance

Clearance data was not found.

Elimination Route

Eliminated 50% through urine and 24% through feces.

Innovators Monograph

You find simplified version here Macitentan