Saquinavir

Information about Saquinavir

Saquinavir is an antiretroviral protease inhibitor that is used in the therapy and prevention of human immunodeficiency virus (HIV) infection and the acquired immunodeficiency syndrome (AIDS).

Liver safety of Saquinavir

Saquinavir can cause transient and usually asymptomatic elevations in serum aminotransferase levels and, rarely, can lead to clinically apparent acute liver injury. In HBV or HCV coinfected patients, highly active antiretroviral therapy with saquinavir may result of an exacerbation of the underlying chronic hepatitis B or C.

Mechanism of action of Saquinavir

Saquinavir (sa kwin' a vir) is an antiretroviral protease inhibitor that acts by binding to the catalytic site of the HIV protease, thereby preventing the cleavage of viral polyprotein precursors into mature, functional proteins that are necessary for viral replication.

FDA approval information for Saquinavir

Saquinavir was approved for use in the United States in 1995 and is still widely used in combination with other antiretroviral agents for the prevention and treatment of HIV infection in adults and children. Saquinavir is available under the brand name Invirase in 200 mg capsules and 500 mg tablets. It is usually used in combination with a low dose of ritonavir, which improves its pharmacokinetics and allows for twice daily dosing.

Dosage and administration for Saquinavir

The recommended dose of saquinavir is 1000 mg in combination with 100 mg of ritonavir, both taken twice daily.

Side effects of Saquinavir

The most common side effects of HIV protease inhibitors include gastrointestinal upset, diarrhea, nausea, fatigue and, with long term use, hyperlipidemia and lipodystrophy.

Antiviral agents

Drugs for HIV Infection, in the Subclass Antiretroviral Agents

• Fusion Inhibitors (HIV)
  • Enfuvirtide, Maraviroc

• Integrase Inhibitors (HIV)
  • Dolutegravir, Elvitegravir, Raltegravir

• Monoclonal Antibodies
  • Ibalizumab

• Nonnucleoside Reverse Transcriptase Inhibitors (HIV)
  • Delavirdine, Efavirenz, Etravirine, Nevirapine, Rilpivirine

• Nucleoside Analogues (HIV)
  • Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Tenofovir, Zidovudine

• Protease Inhibitors (HIV)
  • Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Nelfinavir,Ritonavir, Saquinavir, Tipranavir

Drugs for Hepatitis B

• • Alpha Interferon, Adefovir, Emtricitabine, Entecavir, Lamivudine, Telbivudine, Tenofovir

Drugs for Hepatitis C

• Interferon Based Therapies
  • Alpha Interferon and Peginterferon, Ribavirin

HCV NS5A Inhibitors

• Daclatasvir, Elbasvir, Ledipasvir, Ombitasvir, Pibrentasvir, Velpatasvir

HCV NS5B (Polymerase) Inhibitors

• Dasabuvir, Sofosbuvir

HCV Protease Inhibitors

• Asunaprevir, Boceprevir, Glecaprevir, Grazoprevir, Paritaprevir, Simeprevir, Telaprevir, Voxilaprevir

Combination Therapies

• Epclusa, Harvoni, Mavyret, Technive, Viekira Pak, Vosevi, Zepatier

Drugs for Herpes Virus Infections (HSV, CMV, others)

• Acyclovir, Cidofovir, Famciclovir, Foscarnet, Ganciclovir, Valacyclovir, Valganciclovir

Drugs for Influenza

• Amantadine, Oseltamivir, Peramivir, Rimantadine, Zanamivir

• Dailymed label info on Saquinavir
• FDA Saquinavir

Saquinavir

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  Saquinavir structure
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  Saquinavir ball-and-stick model
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  HIV new infections and deaths 1981-2008