Lopinavir

Information about Lopinavir

Lopinavir is an antiretroviral protease inhibitor used in combination with ritonavir in the therapy and prevention of human immunodeficiency virus (HIV) infection and the acquired immunodeficiency syndrome (AIDS).

Liver safety of Lopinavir

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

Mechanism of action of Lopinavir

Lopinavir (loe pin' a vir) is a peptidomimetic HIV 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. Lopinavir is usually given in combination with low “booster” doses of ritonavir which improves the pharmacokinetics of lopinavir by slowing its hepatic metabolism.

FDA approval information for Lopinavir

Lopinavir was approved for use in the United States in 2000 for the treatment of HIV infection in adults and children. Lopinavir in fixed combination with ritonavir is available as tablets of 100 mg/25 mg and 200 mg/50 mg and as an oral solution (80/20 mg per mL) for pediatric use generically and under the brand name Kaletra.

Dosage and administration for Lopinavir

The recommended dosage of lopinavir in adults is 800 mg daily in combination with 200 mg of ritonavir, either once daily or in two divided doses. Pediatric doses are based upon body weight or body surface area.

Side effects of Lopinavir

Common side effects include gastrointestinal upset, nausea, diarrhea, fatigue, headache, and, with long term therapy, dyslipidemia 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 Lopinavir
• FDA Lopinavir

Lopinavir

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  Chemical structure of Lopinavir

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  3D model of Lopinavir