macitentan/tadalafil (Opsynvi)

Indications

• pulmonary arterial hypertension

Contraindications

• pregnancy
• lactation (do not breast feed)
• chronic renal failure stage 4 or 5
• severe hepatic impairment

*for all female patients, OPSYNVI is available only through Macitentan-Containing Products Risk Evaluation & Mitigation Strategy (REM), a restricted program.

Dosage

• one tablet taken orally once daily with or without food

*

Tablets: 10 mg macitentan/20 mg tadalafil or 10 mg macitentan/40 mg tadalafil

Monitor

• baseline serum transaminases & as clinically indicated

Adverse effects

• most common >= 10%
  • edema/fluid retention, anemia, headache/migraine
• macitentan
  • hepatotoxicity
  • decreased sperm count
• tadalafil
  • hypotension
  • non-arteritic ischemic optic neuropathy
  • priapism
  • hearing impairment
• other
  • pulmonary edema due to pulmonary vaso-occlusive disease

Drug interactions

• avoid use with other phosphodiesterase-5 inhibitors
• avoid use with strong CYP3A4 inhibitors & inducers

Mechanism of action

• combination of macitentan, an endothelin receptor antagonist & tadalafil, a phosphodiesterase-5 inhibitor
• macitentan reduces risk of clinical worsening events & hospitalization
• tadalafil improves exercise ability

More general terms

• pharmacologic combination

Components

• macitentan (Opsumit)
• tadalafil (Cialis, Adcirca, 'weekend Viagra')