Black Box Warnings .
restricted distribution program (Opsumit REMS) for all female pts due to fetal harm risk; prescribers, pharmacies, and female pts must enroll at 1-866-228-3546 or www.opsumitrems.com
contraindicated in pregnancy; exclude pregnancy in females of reproductive potential prior to tx start, then qmo during tx and x1mo after D/C; use acceptable methods of contraception during tx and x1mo after D/C
Adult Dosing .
Dosage forms: 10
Restricted Distribution in US
- [1-866-228-3546 or www.opsumitrems.com for more info]
- Info: female pts may only receive tx through Opsumit REMS program
pulmonary arterial HTN
- [10 mg PO qd]
- Max: 10 mg/day; Info: do not cut/crush/chew tab
- [see below]
- CrCl >15: no adjustment; CrCl <15: not defined; HD: not defined
- [no adjustment]
Peds Dosing .
Peds dosing is currently unavailable or not applicable for this drug.
- hypersens. to drug/class/compon.
- pulmonary veno-occlusive dz
Drug Interactions .
endothelin receptor antagonist
- CYP3A4 substrate
- St. John's wort
Adverse Reactions .
- embryo-fetal toxicity
- ALT, AST elevated
- sperm count decr.
Lactation: Safety Unknown
use 2 reliable forms of contraception (one non-hormonal) during tx and x1mo after D/C in women of childbearing potential; no additional contraception needed if tubal sterilization hx or current IUD or contraceptive implant use
pregnancy test at baseline, then qmo during tx, and 1mo after D/C; Hgb, LFTs at baseline, then as clinically indicated
Metabolism: liver; CYP450: 3A4 (primary), 2C19 substrate; Info: active metabolite
Excretion: urine 50%, feces 24%; Half-life: 16h (parent drug), 48h (active metabolite)
Subclass: Pulmonary Arterial HTN
Mechanism of Action
binds to endothelin receptors, blocking vasoconstrictive effects of endothelin-1; reduces pulmonary vascular resistance (endothelin receptor antagonist)
Manufacturer: Actelion Pharmaceuticals US, Inc.
Approximate Retail Price
This information is currently not available for this drug.
Join Now to View Patient Handouts!
Create a FREE Epocrates Online account to access patient medication instructions. Your patients and caregivers will appreciate you printing these friendly handouts, available in English and Spanish. Each handout addresses common concerns such as how to take the medication, and possible side effects.
Current Members: Sign In.