Brand Name :
Opsumit
Synonyms :
macitentan
Class :
Endothelin Antagonists
Dosage Forms & Strengths
Tablet
10mg
pulmonary Arterial Hypertension
Indicated for pulmonary arterial hypertension (PAH) :
10 mg once daily, taken orally with or without food.
Note:
Do not take more or less of the medication than directed, and do not stop taking it without first consulting your healthcare provider.
Safety and efficacy not established
Refer to adult dosing
CYP3A strong enhancers of the small intestine may reduce the bioavailability of macitentan
may enhance the serum concentration of CYP3A4 inhibitors
may decrease the serum concentration of macitentan
may decrease the serum concentration of macitentan
may decrease the serum concentration of macitentan
may decrease the serum concentration of macitentan
may decrease the serum concentration of macitentan
may enhance the serum concentration of macitentan
may enhance the serum concentration of macitentan
may enhance the serum concentration of macitentan
may enhance the serum concentration of macitentan
may enhance the serum concentration of macitentan
It may enhance the serum concentration when combined with CYP3A4 Inhibitors (Moderate)
It may enhance the serum concentration when combined with CYP3A4 Inhibitors (Moderate)
It may enhance the serum concentration when combined with CYP3A4 Inhibitors (Moderate)
It may enhance the serum concentration when combined with CYP3A4 Inhibitors (Moderate)
It may enhance the serum concentration when combined with CYP3A4 Inhibitors (Moderate)
It may diminish the metabolism when combined with Endothelin antagonists
It may diminish the metabolism when combined with Endothelin antagonists
It may diminish the metabolism when combined with Endothelin antagonists
It may diminish the metabolism when combined with Endothelin antagonists
It may diminish the metabolism when combined with Endothelin antagonists
It may diminish the metabolism when combined with Endothelin receptor antagonists
It may diminish the metabolism when combined with Endothelin receptor antagonists
bazedoxifene/conjugated estrogens
It may diminish the metabolism when combined with Endothelin receptor antagonists
It may diminish the metabolism when combined with Endothelin receptor antagonists
It may diminish the metabolism when combined with Endothelin receptor antagonists
It may diminish the metabolism when combined with Endothelin receptor antagonists
It may diminish the metabolism when combined with Endothelin receptor antagonists
It may diminish the metabolism when combined with Endothelin receptor antagonists
may decrease the serum concentration of CYP3A4 Inducers
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Ergot alkaloids
It may diminish the metabolism when combined with Estrogens
It may diminish the metabolism when combined with Estrogens
bazedoxifene/conjugated estrogens
It may diminish the metabolism when combined with Estrogens
It may diminish the metabolism when combined with Estrogens
It may diminish the metabolism when combined with Estrogens
Frequency Defined
>10%
Bronchitis (12%)
Nasopharyngitis (20%)
Anemia (13%)
Headache (14%)
1-10%
Hemoglobin <10 g/dL (8.7%)
Urinary tract infection (9%)
Influenza (6%)
Elevated aminotransferases >8 x ULN (2.1%)
Elevated aminotransferases >3 x ULN (3.4%)
Pregnancy warnings:
Pregnancy: N/A
Lactation:
Excreted into human milk is unknown
Pregnancy Categories:
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Patient information leaflet
Generic Name: macitentan
Why do we use macitentan?
macitentan is an Endothelin Antagonists. Macitentan is a medication that is used to treat pulmonary arterial hypertension (PAH). Macitentan is an endothelin receptor antagonist, which means it works by blocking the action of a substance called endothelin that can constrict blood vessels and increase blood pressure in the pulmonary arteries.
By blocking the action of endothelin, macitentan can help to relax the blood vessels in the lungs and reduce blood pressure, which can improve symptoms and increase the ability to exercise in people with PAH.