Bosentan


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Pulmonary arterial hypertension
Adult: To improve exercise capacity and symptoms, and to decrease clinical deterioration in patients with WHO functional class II-IV symptoms: <40 kg: 62.5 mg bid. ≥40 kg: Initially, 62.5 mg bid for 4 weeks. Maintenance dose: 125 mg bid. Dose reduction, interruption, or discontinuation may be required according to individual safety or tolerability (refer to detailed product guidelines).
Child: To improve pulmonary vascular resistance (PVR) in paediatric patients with idiopathic or congenital PAH: ≥3-≤12 years ≥ 4-8 kg: 16 mg bid; >8-16 kg: 32 mg bid; >16-24 kg: 48 mg bid; >24-40 kg: 64 mg bid. >12 years Same as adult dose. Dosing recommendations may vary among individual products and between countries (refer to specific product guidelines).

Oral
Systemic sclerosis with ongoing digital ulcer disease
Adult: To reduce the number of new digital ulcers: Initially, 62.5 mg bid for 4 weeks. Maintenance dose: 125 mg bid. Treatment recommendations may vary among individual products and between countries (refer to specific product guidelines).
Nhóm bệnh nhân đặc biệt
Patient with ALT/AST levels of >3 times but ≤5 times ULN: If the result is confirmed by another aminotransferase test, reduce the daily dose or interrupt treatment. Monitor aminotransferase levels at least every 2 weeks. May continue or reintroduce treatment if aminotransferase levels return to pre-treatment values.

Patient with ALT/AST levels of >5 times but ≤8 times ULN: If the result is confirmed by another aminotransferase test, stop treatment and monitor aminotransferase levels at least every 2 weeks. May reintroduce treatment if aminotransferase levels return to pre-treatment values.

Patient with ALT/AST levels of >8 times ULN: Stop treatment and do not reintroduce.
Suy gan
Pulmonary arterial hypertension
Moderate to severe (Child-Pugh class B and C) and/or baseline transaminase >3 times upper limit of normal (ULN): Contraindicated.
Cách dùng
May be taken with or without food.
Hướng dẫn pha thuốc
Disperse tablets for oral susp in a minimal amount of water immediately before administration.
Chống chỉ định
Women of childbearing potential who are not using reliable methods of contraception. Moderate to severe hepatic impairment (Child-Pugh class B or C). Pregnancy. Concomitant use with ciclosporin and glibenclamide.
Thận trọng
Patient with underlying heart failure due to potential complications from fluid retention. Children. Lactation.
Tác dụng không mong muốn
Significant: Fluid retention, peripheral oedema, decreased haematocrit/Hb (dose-related), elevated transaminase (ALT or AST ≥3 times ULN), hypersensitivity reactions (e.g. anaphylaxis, angioedema, rash, drug reaction with eosinophilia and systemic symptoms). Rarely, unexplained liver cirrhosis in patients with multiple comorbidities and drug therapies (prolonged use); liver failure.
Blood and lymphatic system disorders: Anaemia.
Cardiac disorders: Palpitations.
Gastrointestinal disorders: GERD, diarrhoea.
Nervous system disorders: Headache, syncope.
Respiratory, thoracic and mediastinal disorders: Nasal congestion.
Skin and subcutaneous tissue disorders: Erythema.
Vascular disorders: Flushing, hypotension.
Thông tin tư vấn bệnh nhân
Women of childbearing potential must use 2 reliable methods of contraception.
Chỉ số theo dõi
Monitor serum transaminases (ALT, AST) and bilirubin at baseline then monthly thereafter, or as clinically necessary; Hb and haematocrit at baseline, after 1 and 3 months of treatment, and every 3 months thereafter. Obtain pregnancy tests prior to initiation of therapy, monthly during treatment, and 1 month after treatment discontinuation. Monitor for signs and symptoms of liver injury and fluid retention.
Quá liều
Symptoms: Nausea, vomiting, dizziness, headache, sweating, blurred vision, hypotension. Management: Supportive treatment (e.g. blood pressure support).
Tương tác
May increase plasma concentration with CYP2C9 inhibitors (e.g. fluconazole, amiodarone), CYP3A4 inhibitors (e.g. ketoconazole, itraconazole, ritonavir, erythromycin, diltiazem), tacrolimus and sirolimus. May decrease plasma concentration of hormonal contraceptives, warfarin, simvastatin, tadalafil and sildenafil. Decreased plasma concentration with rifampicin.
Potentially Fatal: Increased plasma concentration with ciclosporin. Enhanced hepatotoxic effect with glibenclamide.
Tác dụng
Description: Bosentan, an endothelin receptor antagonist, improves exercise capacity and haemodynamic in patients with pulmonary arterial hypertension (PAH) by blocking endothelin-1 (ET-1) receptors, ETA and ETB (with a slightly higher affinity for subtype A) on vascular endothelium and smooth muscle, thus promoting vasodilation.
Pharmacokinetics:
Absorption: Absorbed from the gastrointestinal tract. Bioavailability: Approx 50%. Time to peak plasma concentration: 3-5 hours.
Distribution: Volume of distribution: Approx 18 L. Plasma protein binding: >98%, mainly to albumin.
Metabolism: Metabolised in the liver by CYP2C9 and CYP3A4.
Excretion: Via faeces (as metabolites); urine (<3% as unchanged drug). Elimination half-life: Approx 5 hours.
Đặc tính

Chemical Structure Image
Bosentan

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 104865, Bosentan. https://pubchem.ncbi.nlm.nih.gov/compound/Bosentan. Accessed June 27, 2022.

Bảo quản
Store between 20-25°C. Store divided dispersible tab pieces in the opened blister for up to 7 days.
Phân loại MIMS
Thuốc trị tăng huyết áp khác
Phân loại ATC
C02KX01 - bosentan ; Belongs to the class of other antihypertensives. Used in the treatment of pulmonary arterial hypertension.
Tài liệu tham khảo
Anon. Bosentan. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 07/02/2022.

Anon. Bosentan. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/02/2022.

Bosentan Cipla 62.5 mg Film-coated Tablets (Cipla [EU] Limited). MHRA. https://products.mhra.gov.uk. Accessed 07/02/2022.

Buckingham R (ed). Bosentan. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/02/2022.

Janssen-Cilag (New Zealand) Ltd. Tracleer - Bosentan (as Monohydrate) 62.5 mg & 125 mg Tablets data sheet 27 May 2019. Medsafe. http://www.medsafe.govt.nz. Accessed 07/02/2022.

Joint Formulary Committee. Bosentan. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/02/2022.

Tracleer (Actelion Pharmaceuticals US, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 07/02/2022.

Tracleer 62.5 mg Film-coated Tablets, Tracleer 125 mg Film-coated Tablets (Johnson & Johnson Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 07/02/2022.

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