Class
- dual endothelin receptor antagonist
Mechanism of Action
- competitive antagonism of endothelin-1 (pulmonary vasoconstrictor) at the endothelin receptors -> decreases PVR
Pharmaceutics
- tablet
Dose
- 62.5mg BD -> increased monthly
Indications
(1) severe PHT
(2) scleroderma with digital ulcers
Adverse Effects
- liver injury
- teratogenicity
PK
- Absorption – bioavailability = 50%
- Distribution – protein binding 98%
- Metabolism – hepatic
- Elimination – t ½ = 5 hrs
Evidence
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