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 |
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.
Macitent 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
Macitent Disease Interaction
Major: hepatotoxicity/liver impairmentModerate: anemia, fluid retention
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