Generic Name: Saquinavir
Product Name: Fortovase
Used, in combination with other anti-retroviral agents, in the treatment of HIV infection.
Saquinavir is a highly selective HIV protease inhibitor, with only a weak affinity for human proteases. Saquinavir exerts synergistic effects against HIV in double and triple combination regimens with reverse transcriptase inhibitors (e.g. zidovudine, zalcitabine, didanosime, lamivudine, stavudine, nevipramine) in the absence of increased toxicity. Cross resistance between saquinavir and reverse transcriptase inhibitors is unlikely due to their different enzyme targets. HIV strains with reduced susceptibility to saquinavir have been isolated in vitro.
Saquinavir absorption and bioavailability is improved in the presence of food. Saquinavir is rapidly and almost completely metabolised by the CYP450 isoenzyme CYP3A4 in the liver. Systemic clearance is rapid, and most of the oral dose is recovered in the faeces within five days of dosing.
Six 200 mg capsules, three times daily (i.e. 1.2 g three times daily)
Use in pregnancy (Category B1)
Caution should be exercised is using the drug in pregnant women. Animal studies suggest that placental transfer is low, and the Saquinavir has no effect on the growth and development of the foetus.
Use in lactation
Lactating women taking Saquinavir should not breast feed. It is not known if the drug is excreted in breast milk.
Use in children
Safety and efficacy in children < 16 years has not been established.
Common side effects
- Nausea, diarrhoea, abdominal discomfort, flatulence
- Increased likelihood of infections (e.g. bacterial, viral, fungal)
Uncommon side effects
- Abnormalities of liver enzymes, electrolytes and haematological laboratory values.
- Dry mouth, unpleasant taste, decreased appetite, constipation, frequent bowel movements.
- Night sweats, increased sweating.
- Dizziness, light-headedness, tremor.
- Rash, eczema.
- Thirst, dehydration.
- Pain (e.g. back pain, muscle pain, facial pain, jaw pain, leg pain, joint pain)
- Decreased libido, sexual dysfunction.
For further information talk to your doctor.