Saquinavir
- Atc Codes:J05AE01
- CAS Codes:149845-06-7
- PHARMGKB ID:149845-06-7
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Invirase; Belgium: Invirase; Bulgaria: Invirase; Czech Republic: Invirase; Denmark: Invirase; Estonia: Invirase; Finland: Invirase; France: Invirase; Germany: Invirase; Greece: Invirase; Hungary: Invirase; Ireland: Invirase; Italy: Invirase; Latvia: Invirase; Lithuania: Invirase; Luxembourg: Invirase; Malta: Invirase; Netherlands: Invirase; Poland: Invirase; Portugal: Invirase; Romania: Invirase; Slovakia: Invirase; Slovenia: Invirase; Spain: Invirase; Sweden: Invirase; UK: Invirase.
North America
Canada: Invirase; USA: Invirase.
Latin America
Argentina: Fortovase, Proteovir; Brazil: Fortovase (d), Invirase (d), Svir; Mexico: Invirase.
Asia
Japan: Fortovase, Invirase.
Drug combinations
Chemistry
Saquinavir Mesylate: C~38~H~50~N~6~O~5~. CH~4~O~3~S. Mw: 766.95. (1) Butanediamide, N^1^-[3-[3-[[(1,1-dimethylethyl)amino]carbonyl]octahydro-2(1H)-isoquinolinyl]-2-hydroxy-1-(phenylmethyl)propyl]-2-[(2-quinolinylcarbonyl)amino]-, [3S-[2[1R*(R*),2S*],3α,4aβ,8aβ]]-, monomethanesulfonate; (2)(S)-N-[(αS)-α-[(1R)-2-[(3S,4aS,8aS)-3-(tert-Butylcarbamoyl)octahydro-2(1H)-isoquinolyl]-1-hydroxyethyl]phenethyl]-2-quinaldamidosuccinamide monomethanesulfonate. CAS-149845-06-7. (1994)
Pharmacologic Category
Antiretrovirals; HIV Protease Inhibitors. (ATC-Code: J05AE01).
Mechanism of action
Binds to site of HIV-1 protease activity and inhibits cleavage of viral Gag-Pol polyprotein precursors into individual functional proteins required for infectious HIV, resulting in formation of immature, noninfectious viral particles. Active against HIV-1 and HIV-2. Inhibits replication of HIV-1 and HIV-2 by interfering with HIV protease.
Therapeutic use
HIV infection (used in combination with at least two other antiretroviral agents). Postexposure chemoprophylaxis following occupational exposure to HIV.
Pregnancy and lactiation implications
Adverse events not observed in animals; saquinavir crosses human placenta in minimal amounts. Pregnancy and protease inhibitors both associated with increased risk of hyperglycemia. Excretion in breast milk unknown. HIV-infected women should not breast-feed due to risk of HIV transmission and risk of adverse effects in the infant.
Unlabeled use
Contraindications
Hypersensitivity to saquinavir or any component of the formulation. Severe hepatic impairment. Concomitant use with drugs highly dependent on CYP3A4 for metabolism and for which elevated plasma concentrations are associated with serious and/or life-threatening events (e.g. amiodarone, cisapride, ergot alkaloids, flecainide, midazolam, propafenone, quinidine, rifampin, pimozide, triazolam).
Warnings and precautions
May cause fat redistribution. Patients may develop immune reconstitution syndrome (occurrence of inflammatory response to indolent or residual opportunistic infection). Increases in total cholesterol and triglycerides reported. Changes in glucose tolerance, hyperglycemia, exacerbation of diabetes, DKA, and new-onset diabetes mellitus reported in patients receiving protease inhibitors. Use with caution in hemophilia A or B (increased bleeding during protease inhibitor therapy reported). May cause hepatitis and/or exacerbate pre-existing hepatic dysfunction (caution in underlying hepatic disease, such as hepatitis B or C or cirrhosis). Use with caution in patients taking strong CYP3A4 inhibitors, moderate or strong CYP3A4 inducers and major CYP3A4 substrates. May be used only if combined with ritonavir. St. John’s wort, lovastatin, simvastatin should not be used concurrently with saquinavir/ritonavir.