VIETNAM

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  • Macitentan - MIMS.com
Macitentan

Tác Động
Description: Macitentan, an endothelin receptor antagonist, blocks both type A (ETA) and type B (ETB) receptors. Endothelin is a potent vasoconstrictor which plays a pathogenic role in pulmonary arterial hypertension (PAH). Blockade of endothelin receptor leads to vasodilatation, inhibition of smooth muscle proliferation and improve exercise capacity.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: Approx 8 hour.
Distribution: Widely distributed to tissues. Volume of distribution: 50 L; 40 L (active metabolite). Plasma protein binding: >99%, primarily to albumin and to a lesser extent a1-acid glycoprotein.
Metabolism: Extensively metabolised in the liver by CYP3A4 (major enzyme) and CYP2C19 to its active metabolite.
Excretion: Via urine (approx 50%); faeces (approx 24%). Elimination half-life: Approx 16 hour (macitentan); approx 48 hour (active metabolite).


Phân loại MIMS
Thuốc trị tăng huyết áp khác Other Antihypertensives

Phân loại ATC
C02KX04 -  macitentan;  Belongs to the class of other antihypertensives. Used in the treatment of pulmonary arterial hypertension.; 

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