Macitent

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

Macitent was approved in October 2013. It is indicated for patients with pulmonary arterial hypertension, and is marketed under the brand name Opsumit. Macitent 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.

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

Trade Name Macitent
Availability Prescription only
Generic Macitentan
Macitentan Other Names Macitentán, Macitentan, Macitentanum
Related Drugs sildenafil, tadalafil, Revatio, Adempas, Opsumit, ambrisentan
Weight 10mg
Type 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 Msn Laboratories
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Macitent
Macitent

Uses

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

Macitent is indicated for patients with pulmonary arterial hypertension.

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

How Macitent works

Macitent is an antagonist/blocker of endothelin receptors. Endothelin receptors are found in the endothelial cells of blood vessels and smooth muscle. Macitent 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

Macitent 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.

Volume of Distribution

Macitent has a volume of distribution of 50L.

Elimination Route

Macitent 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 Macitent

*** Taking medicines without doctor's advice can cause long-term problems.
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