Adult: In patients with World Health Organization (WHO) functional class II-III pulmonary arterial hypertension (PAH): As monotherapy or in combination with tadalafil: Initially, 5 mg once daily, may be increased to 10 mg once daily based on clinical response and tolerability. Treatment recommendations may vary among countries and between individual products (refer to specific product or local guidelines). Child: In patients with WHO functional class II-III PAH: As monotherapy or in combination with other PAH therapies: 8-17 years Patients weighing ≥20-<35 kg: Initially, 2.5 mg once daily, may be increased to 5 mg once daily; ≥35-<50 kg: Initially, 5 mg once daily, may be increased to 7.5 mg once daily; ≥50 kg: Same as adult dose. Increase dose based on clinical response and tolerability. Treatment recommendations may vary among countries and between individual products (refer to specific product or local guidelines).
What are the brands available for Ambrisentan in Malaysia?
Patients concurrently taking ciclosporin:
Adult: Max: 5 mg once daily.
Child: 8-17 years Patients weighing ≥20-<50 kg: Max: 2.5 mg once daily; ≥50 kg: Max: 5 mg once daily.
Hepatic Impairment
Severe (with or without cirrhosis) or baseline ALT or AST >3 times ULN: Contraindicated. Treatment recommendations may vary among countries and between individual products (refer to specific product or local guidelines).
Administration
Ambrisentan May be taken with or without food. Swallow whole, do not split/chew/crush.
Contraindications
Idiopathic pulmonary fibrosis (with or without secondary pulmonary hypertension). Severe hepatic impairment (with or without cirrhosis) or baseline ALT or AST >3 times ULN. Pregnancy.
Special Precautions
Patient with pulmonary veno-occlusive disease. Patients concurrently taking ciclosporin. Initiation of therapy is not recommended in patients with clinically significant anaemia. Mild to moderate hepatic impairment and severe renal impairment (CrCl <30 mL/min). Children. Breastfeeding during treatment is not recommended.
Adverse Reactions
Significant: Decreased haematocrit and Hb levels; fluid retention, peripheral oedema; increased liver aminotransferases (ALT, AST); may reduce sperm counts. Cardiac disorders: Palpitation, cardiac failure. Ear and labyrinth disorders: Tinnitus. Eye disorders: Blurred vision, visual impairment. Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain, constipation. General disorders and administration site conditions: Chest pain or discomfort, fatigue, asthenia. Immune system disorders: Hypersensitivity reactions (e.g. angioedema, rash, pruritus). Nervous system disorders: Headache (including sinus headache and migraine), dizziness. Respiratory, thoracic and mediastinal disorders: Dyspnoea, cough, upper respiratory (e.g. nasal, sinus) congestion, nasopharyngitis, epistaxis, rhinitis, sinusitis. Vascular disorders: Flushing, syncope, hypotension. Potentially Fatal: Pulmonary oedema (particularly in patients with pulmonary veno-occlusive disease).
PO: Z (Endothelin receptor antagonists (e.g. ambrisentan) are teratogenic and contraindicated during pregnancy.)
Patient Counseling Information
This drug may cause dizziness, fatigue or blurred vision, if affected, do not drive or operate machinery. Women of childbearing potential must use proven birth control methods before treatment initiation, during therapy and for 1 month after the last dose.
Monitoring Parameters
Verify pregnancy status and exclude pregnancy before treatment initiation in women of childbearing potential; monthly pregnancy tests are recommended during therapy. Monitor Hb and haematocrit levels (at baseline, after 1 and 3 months of starting treatment, and periodically thereafter); LFTs (before treatment, monthly during therapy and as clinically indicated). Assess for signs or symptoms of liver problems and significant peripheral oedema.
Overdosage
Symptoms: Headache, dizziness, nausea, flushing, nasal congestion, and potential hypotension.
Management: Symptomatic and supportive treatment. In case of profound hypotension, active CV support may be needed.
Drug Interactions
Increased ambrisentan exposure with ciclosporin. Concomitant use with rifampicin resulted in transient increase in ambrisentan exposure, which resolved when rifampicin reached steady state.
Action
Description: Overview: Ambrisentan, a vasodilator, is a selective propionic-acid endothelin-1 (ET-1) type A receptor antagonist. Mechanism of Action: Ambrisentan selectively blocks ETA receptors, which are predominantly located on vascular smooth muscle cells and cardiac myocytes, thereby inhibiting endothelin-mediated activation of second messenger pathways that lead to vasoconstriction and smooth muscle cell proliferation. By selectively inhibiting ETA receptors, it is expected to retain ETB receptor-mediated vasodilation and ET-1 clearance. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Time to peak plasma concentration: Approx 2 hours. Distribution: Plasma protein binding: Approx 99%. Metabolism: Metabolised in the liver via glucuronidation by several UGT isoenzymes (UGT1A9S, UGT2B7S and UGT1A3S) forming ambrisentan glucuronide; also undergoes oxidative metabolism primarily by CYP3A4 and to a lesser extent by CYP3A5 and CYP2C19 isoenzymes to form 4-hydroxymethyl ambrisentan, which is further metabolised into 4-hydroxymethyl ambrisentan glucuronide. Excretion: Mainly via bile; urine (approx 22%; 3.3% as unchanged drug). Elimination half-life: Approx 9 hours; 15 hours (terminal).
Chemical Structure
Ambrisentan Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6918493, Ambrisentan. https://pubchem.ncbi.nlm.nih.gov/compound/Ambrisentan. Accessed Feb. 24, 2026.
Storage
Store between 15-30°C. Follow applicable procedures for receiving, handling, administration, and disposal.
C02KX02 - ambrisentan ; Belongs to the class of other antihypertensives. Used in the treatment of pulmonary arterial hypertension.
References
Ambrisentan. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 02/12/2025.Ambrisentan. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 02/12/2025.Ambrisentan. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 02/12/2025.Brayfield A, Cadart C (eds). Ambrisentan. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/12/2025.GlaxoSmithKline NZ Limited. Volibris 5 mg and 10 mg Film-coated Tablets data sheet 28 April 2025. Medsafe. http://www.medsafe.govt.nz. Accessed 02/12/2025.Joint Formulary Committee. Ambrisentan. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 02/12/2025.Letairis Tablet, Film Coated (Gilead Sciences, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 02/12/2025.Paediatric Formulary Committee. Ambrisentan. BNF for Children [online]. London. BMJ Group, Pharmaceutical Press, and RCPCH Publications. https://www.medicinescomplete.com. Accessed 02/12/2025.Volibris 5 mg and 10 mg Film-coated Tablets (GlaxoSmithKline Pharmaceutical Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 02/12/2025.Volibris 5 mg Film-coated Tablets (GlaxoSmithKline UK Limited). MHRA. https://products.mhra.gov.uk. Accessed 02/12/2025.
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