Macitentan


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Pulmonary arterial hypertension
Adult: As mono- or in combination therapy, in patients with WHO functional class II and III PAH (idiopathic, heritable, associated with connective tissue diseases or with corrected simple congenital heart disease): 10 mg once daily.
Hepatic Impairment
Severe: Contraindicated.
Cách dùng
May be taken with or without food. Swallow whole, do not chew/split/crush.
Chống chỉ định
Severe hepatic impairment (with or without cirrhosis) or clinically significant elevated baseline values of hepatic aminotransferases (>3 times the upper limit of normal). Women of childbearing potential who are not using reliable contraception. Pregnancy and lactation.
Thận trọng
Patient with pulmonary veno-occlusive disease, anaemia, severe chronic heart disease. Severe renal (including patients on dialysis) and moderate hepatic impairment.
Phản ứng phụ
Significant: Increased serum liver aminotransferases, hepatotoxicity, liver failure, fluid retention, peripheral oedema, decreased Hb and haematocrit, anaemia, decreased sperm count.
Blood and lymphatic system disorders: Leucopenia, thrombocytopenia.
Infections and infestations: Influenza.
Nervous system disorders: Headache.
Renal and urinary disorders: UTI.
Respiratory, thoracic and mediastinal disorders: Nasopharyngitis, pharyngitis, bronchitis, nasal congestion.
Vascular disorders: Hypotension.
Thông tin tư vấn bệnh nhân
This drug may cause headache or hypotension, if affected, do not drive or operate machinery.
MonitoringParameters
Obtain pregnancy test prior to initiation of therapy, monthly during treatment, and 1 month after stopping treatment. Monitor ALT and AST, Hb and haematocrit levels prior to treatment and as clinically indicated. Monitor for signs of hepatic injury, significant peripheral oedema.
Quá liều
Symptoms: Headache, nausea, vomiting. Management: Supportive treatment.
Tương tác
Decreased serum concentrations with strong CYP3A4 inducers (e.g. carbamazepine, phenytoin, rifampicin). Increased serum concentrations with strong CYP3A4 inhibitors (e.g. clarithromycin, ketoconazole, ritonavir).
Food Interaction
Reduced serum concentration with St. John’s wort.
Tác dụng
Description: Macitentan inhibits the binding of endothelin (ET)-1 from binding to both type A (ETA) and type B (ETB) receptors. ET-1 is a potent vasoconstrictor which plays a pathogenic role in pulmonary arterial hypertension (PAH). Blockade of ET-1 leads to vasodilatation, inhibition of smooth muscle proliferation and improved exercise capacity.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: Approx 8 hours.
Distribution: Widely distributed into tissues. Volume of distribution: Approx 50 L (active metabolite: 40 L). Plasma protein binding: >99%, mainly to albumin and to a lesser extent to α1-acid glycoprotein.
Metabolism: Extensively metabolised, mainly by CYP3A4 and to a lesser extent by CYP2C8, CYP2C9, and CYP2C19 via several metabolic pathways, including oxidative depropylation of the sulfamide to form the active metabolite ACT-132577.
Excretion: Mainly via urine (approx 50%); faeces (approx 24%). Elimination half-life: Approx 16 hours (macitentan); approx 48 hours (ACT-132577)
Đặc tính

Chemical Structure Image
Macitentan

Source: National Center for Biotechnology Information. PubChem Database. Macitentan, CID=16004692, https://pubchem.ncbi.nlm.nih.gov/compound/Macitentan (accessed on Jan. 21, 2020)

Bảo quản
Store between 15-30°C.
Phân loại MIMS
Phân loại ATC
C02KX04 - macitentan ; Belongs to the class of other antihypertensives. Used in the treatment of pulmonary arterial hypertension.
References
Anon. Macitentan. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 05/05/2020.

Anon. Macitentan. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 05/05/2020.

Buckingham R (ed). Macitentan. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/05/2020.

Joint Formulary Committee. Macitentan. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 05/05/2020.

Opsumit (Johnson & Johnson Sdn Bhd). MIMS Malaysia. http://www.mims.com/malaysia.

Opsumit Tablet, Film Coated (Actelion Pharmaceuticals US, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 05/05/2020.

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