Ambrisentan
- Atc Codes:C02KX02
- CAS Codes:177036-94-1
- PHARMGKB ID:177036-94-1
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Volibris; Belgium: Volibris; Czech Republic: Volibris; Denmark: Volibris; Estonia: Volibris; Finland: Volibris; France: Volibris; Germany: Volibris; Greece: Volibris; Hungary: Volibris; Ireland: Volibris; Italy: Volibris; Latvia: Volibris; Luxembourg: Volibris; Netherlands: Volibris; Poland: Volibris; Portugal: Volibris; Romania: Volibris; Slovakia: Volibris; Spain: Volibris; Sweden: Volibris; UK: Volibris.
North America
Canada: Volibris; USA: Letairis.
Drug combinations
Chemistry
Ambrisentan: C~22~H~22~N~2~O~4~. Mw: 378.42. (+)-(2S)-2-[(4,6-Dimethylpyrimidin-2-yl)oxy]-3-methoxy-3,3-diphenylpropanoic acid. CAS-177036-94-1.
Pharmacologic Category
Vasodilating Agents, Miscellaneous; Endothelin Antagonists. (ATC-Code: C02KX02).
Mechanism of action
Blocks endothelin receptor ET~A~ and ET~B~ on vascular endothelium and smooth muscle.
Therapeutic use
Treatment of pulmonary artery hypertension.
Pregnancy and lactiation implications
Contraindicated during pregnancy. Use not recommended during lactation.
Unlabeled use
Contraindications
Pregnancy.
Warnings and precautions
Peripheral edema/fluid retention might occur. A reduction in hematocrit/hemoglobin may occur within the first few weeks of therapy. Avoid use in moderate-to-severe hepatic impairment (transaminase (ALT or AST) elevations). Use caution in mild hepatic impairment. Use caution in patients taking strong inhibitors or inducers of CYP3A4 or CYP2C19, inhibitors of P-glycoprotein (cyclosporine), or agents which affect glucuronidation metabolism via uridine 5′-diphosphate glucuronosyltransferase (UGT) enzymes. Use in pregnancy is contraindicated (pregnancy should be excluded prior to initiating therapy and monthly thereafter during therapy.)