Saquinavir information from DrugsUpdate
P - Caution when used during pregnancy
L - Contraindicated in lactation
FI - Food *
LI - Lab *
Saquinavir is an antiretroviral drug used in HIV therapy. It falls in the protease inhibitor class. Two formulations have been marketed:
A hard-gel capsule formulation of the mesylate, with trade name Invirase, which requires combination with ritonavir to increase the saquinavir bioavailability.
A soft-gel capsule formulation of saquinavir, with trade name Fortovase.
Both formulations are generally used as a component of highly active antiretroviral therapy (HAART).
Pharmacodynamics
Pharmacokinetics
Saquinavir is a selectively competitive reversible inhibitor of HIV protease. It interferes with the formation of essential proteins and enzymes, leading to the formation of immature and non-infectious viruses.
Absorption
About 30% is absorbed after oral doses. Bioavailability: About 4% when taken with food.
Distribution
98% bound to plasma proteins. Extensively distributed into the tissues.
Metabolism
Rapidly metabolised by CYP3A4.
Excretion
Excreted mainly in the faeces. Terminal half-life: About 13.2 hours.
Saquinavir Indications / Saquinavir Uses
Information Not Available
Saquinavir Adverse Reactions / Saquinavir Side Effects
Nausea, vomiting and diarrhoea. Taste disturbances, abdominal pain, anorexia, increased appetite, flatulence, asthenia, fatigue, sleep disturbances, headache, dizziness, paraesthesia, hypoaesthesia, myalgia, arthralgia, alopecia, pruritus and renal insufficiency. Myositis and rhabdomyolysis. Lipodystrophy; hyperglycaemia, onset or exacerbation of DM; hypersensitivity; blood disorders; ingrowing toenails and paronychia of the great toes. Irregular, prolonged heavy menstruation. Acute paranoid reactions. Sexual dysfunction.
Potentially Fatal: Hypersensitivity, Stevens-Johnson syndrome; photosensitivity; nephrolithiasis; pancreatitis; haemorrhage, haemolytic anaemia, intracranial haemorrhage and respiratory disorder.
Precautions
Monitor
Monitor WBC and differential. Note any significant changes. Monitor Hct and Hgb frequently (severe anemia may require blood transfusions). Perform clinical chemistry, viral load, and CD4 count prior to therapy and at appropriate intervals thereafter. Periodically monitor triglyceride levels during therapy.
Special Precautions
Pregnancy; adolescents <16 years; elderly; renal or hepatic impairment; DM; haemophilia; underlying hepatitis B, cirrhosis or other underlying liver abnormalities. Diarrhoea may cause malabsorption.
Other Drug Interactions
Concomitant use of ritonavir, indinavir, nelfinavir, rifabutin, delavirdine, nevirapine, substrate of CYP3A4 enzyme. Concomitant use with sildenafil, nucleoside reverse transcriptase inhibitors (NRTI), pimozide may cause serious arrhythmogenic, neurologic or other toxicities. Oestrogens: May require alternative or additional contraceptive methods. May increase serum levels of digoxin and maraviroc. May decrease serum levels of methadone. Serum levels may be increased by fluconazole, ranitidine and omeprazole.
Potentially Fatal: Concurrent use with astemizole, terfenadine, ergot derivatives, cisapride, midazolam or triazolam may lead to serious adverse effects e.g. cardiac arrhythmias. Severe hepatocellular toxicity when rifampicin is used with saquinavir and ritonavir. Increased risk of myopathy when used with HMG-CoA reductase inhibitors that are metabolised by the CYP3A4 pathway.
Other Interactions
Food Interaction
Coadmin with St. John's wort may lead to decreased serum levels of saquinavir, resulting in loss of efficacy and increasing risk of emergence of resistance to the drug.
Dosage
Oral
HIV infection
Adult: Combined with other antiretrovirals: >16 years: 1 g bid when taken with ritonavir 100 mg bid. Alternatively, 400 mg bid with ritonavir 400 mg bid.
Oral
Postexposure prophylaxis during occupational exposure to HIV
Adult: 1 g bid with ritonavir 100 mg bid, combined with other antiretrovirals. Should be started as soon as possible and continued for 4 weeks if tolerated.
Food(before/after)
Should be taken with food. (Take with meals or up to 2 hours after meals.)
List of Contraindications
Saquinavir and Pregnancy
Caution when used during pregnancy
Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).
Saquinavir and Lactation
Contraindicated in lactation
Saquinavir and Children
Not recommended for children younger than 16 years of age.
Saquinavir and Geriatic
Use with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.
Saquinavir and Other Contraindications
Lactation; hypersensitivity; severe hepatic impairment.
Storage
Oral
Store at 25°C
Lab interference
Oral
Store at 25°C
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