Products
Saquinavir is commercially available in the form of film-coated tablets (Invirase). It has been approved in many countries since 1996 (United States: 1995).
Structure and properties
Saquinavir (C38H50N6O5, Mr = 670.8 g/mol) is present in the drug as saquinavir mesilate, a white, weakly hygroscopic powder that is practically insoluble in water.
Effects
Saquinavir (ATC J05AE01) has antiviral properties. The effects are due to inhibition of HIV protease, which plays a central role in viral maturation and replication.
Indications
For treatment of infection with HIV (combination antiretroviral therapy).
Dosage
According to the professional information. Tablets are administered twice daily two hours after a meal. Saquinavir must be combined with the pharmacokinetic booster ritonavir. Ritonavir is a CYP inhibitor and inhibits the metabolism of saquinavir.
Contraindications
- Hypersensitivity
- Severe hepatic insufficiency
- Combination with certain drugs
Full precautions can be found in the drug label.
Interactions
Saquinavir is a substrate of CYP3A4. Corresponding drug interactions with CYP substrates, inhibitors, and inducers are possible.
Adverse effects
The most common potential adverse effects include nausea, diarrhea, fatigue, vomiting, flatulence, and abdominal pain.
