Saquinavir

Indications
 Oral
HIV infection
Adult: Combined with other antiretrovirals: >16 yr: 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 wk if tolerated.
Contraindications
 Lactation; hypersensitivity; severe hepatic impairment.
Warnings / Precautions
 Pregnancy; adolescents <16 yr; elderly; renal or hepatic impairment; DM; haemophilia; underlying hepatitis B, cirrhosis or other underlying liver abnormalities. Diarrhoea may cause malabsorption.
Adverse Reactions
 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.
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.
See Below for More saquinavir Drug Interactions
Lab Interactions
 May cause abnormal laboratory test results e.g. raised liver enzymes and bilirubin, raised creatinine phosphokinase and raised blood lipids.
Food Interactions
 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.
Mechanism of Actions
 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 hr.
Administration
 Should be taken with food. (Take w/ meals or up to 2 hr after meals.)
Storage Conditions
 Oral: Store at 25°C.
ATC Classification
 J05AE01 - saquinavir ; Belongs to the class of protease inhibitors. Used in the systemic treatment of viral infections.
Storage
 Oral: Store at 25°C.
Available As
  • Saquinavir 500 mg

    • Subscribe for latest updates

    Subscribe to our e-mail newsletter to receive updates.

    No comments yet.

    Post Review about Saquinavir


    Saquinavir Containing Brands

    We are Developing Our database, More results coming soon.

    Saquinavir is used in following diseases

    We are Developing Our database, More results coming soon.

    Drug - Drug Interactions of Saquinavir

    We are Developing Our database, More results coming soon.