Saquinavir

It is an inhibitor of HIV protease. HIV protease is an enzyme required for the proteolytic cleavage of viral polyprotein precursors into individual functional proteins found in infectious HIV. It is a peptidelike substrate analogue that binds to the protease active site and inhibits the activity of the enzyme. Saquinavir inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature noninfectious virus particles.

Indications

Treatment of HIV infection in combination with other antiretroviral agents.

Dosage

Six 200mg capsules orally, three times a day (1200mg tid) should be taken with a meal or up to 2 hours after a meal. When used in combination with nucleoside analogues, the dosage of Saquinavir should not be reduced as this will lead to greater than dose proportional decreases in saguinavir plasma levels.

Contra-Indications

Hypersensitivity.

Special Precautions

If a serious or severe toxicity occurs discontinue until the etiology of the event is identified or the toxitcity resolves, Hepatic Insufficiency, Hemophilia. Saquinavir should only be used during pregnancy after taking into account the importance of the drug to the mother. Safety and effectiveness of Saquinavir in HIV-infected pediatric patients younger than 16 years of age have not been established. New onset diabetes mellitus, exacerbation of pre-existing diabetes mellitus and hyperglycemia h

Side Effects

Mouth dry, night sweats, sweating increased, allergic reaction, anorexia, appetite decreased, appetite disturbances, asthenia, chest pain, edema, fever, olfactory disorder, pain body, pain pelvic, retrosternal pain, shivering, weakness, ataxia, confusion, convulsions, dizziness, acne, alopecia, chalazion, dermatitis, dehydration, diabetes mellitus, hyperglycemia, hypoglycemia, hypothyroidism, abdominal distention, bowel movements frequent, buccal mucosa, ulceration, agitation, amnesia, anxiety a

Drug Interactions

Astemizole, terfenadine, ergot derivatives, cisapride, midazolam, triazolam, nevirapine, rifabutin, rifampin, clarithromycin, delaviradine, ketoconazole, Indinavir, ritonavir, nelfinavir.