Ritonavir-boosted protease inhibitors in HIV therapy. 2011

Mark W Hull, and Julio S G Montaner
Division of AIDS, Department of Medicine, University of British Columbia, Vancouver, Canada.

The advent of combination antiretroviral therapy has led to significant improvement in the care of HIV-infected patients. Originally designed as a protease inhibitor (PI), ritonavir is currently exclusively used as a pharmacokinetic enhancer of other protease inhibitors, predominantly due to ritonavir's potent inhibition of the cytochrome P450 3A4 isoenzyme. Ritonavir-boosting of PIs decrease pill burden and frequency of dosing. Boosted PIs are recommended for first-line therapy in treatment and play a key role in the management of treatment-experienced patients. Potential problems associated with PIs include metabolic abnormalities (e.g. dyslipidemia), increased cardiovascular risk, and drug interactions.

UI MeSH Term Description Entries
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D004359 Drug Therapy, Combination Therapy with two or more separate preparations given for a combined effect. Combination Chemotherapy,Polychemotherapy,Chemotherapy, Combination,Combination Drug Therapy,Drug Polytherapy,Therapy, Combination Drug,Chemotherapies, Combination,Combination Chemotherapies,Combination Drug Therapies,Drug Polytherapies,Drug Therapies, Combination,Polychemotherapies,Polytherapies, Drug,Polytherapy, Drug,Therapies, Combination Drug
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D015658 HIV Infections Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS). HTLV-III Infections,HTLV-III-LAV Infections,T-Lymphotropic Virus Type III Infections, Human,HIV Coinfection,Coinfection, HIV,Coinfections, HIV,HIV Coinfections,HIV Infection,HTLV III Infections,HTLV III LAV Infections,HTLV-III Infection,HTLV-III-LAV Infection,Infection, HIV,Infection, HTLV-III,Infection, HTLV-III-LAV,Infections, HIV,Infections, HTLV-III,Infections, HTLV-III-LAV,T Lymphotropic Virus Type III Infections, Human
D017320 HIV Protease Inhibitors Inhibitors of HIV PROTEASE, an enzyme required for production of proteins needed for viral assembly. HIV Protease Inhibitor,Inhibitor, HIV Protease,Inhibitors, HIV Protease,Protease Inhibitor, HIV,Protease Inhibitors, HIV
D051544 Cytochrome P-450 CYP3A A cytochrome P-450 suptype that has specificity for a broad variety of lipophilic compounds, including STEROIDS; FATTY ACIDS; and XENOBIOTICS. This enzyme has clinical significance due to its ability to metabolize a diverse array of clinically important drugs such as CYCLOSPORINE; VERAPAMIL; and MIDAZOLAM. This enzyme also catalyzes the N-demethylation of ERYTHROMYCIN. CYP3A,CYP3A4,CYP3A5,Cytochrome P-450 CYP3A4,Cytochrome P-450 CYP3A5,Cytochrome P-450IIIA,Cytochrome P450 3A,Cytochrome P450 3A4,Cytochrome P450 3A5,Erythromycin N-Demethylase,Taurochenodeoxycholate 6-alpha-Monooxygenase,3A5, Cytochrome P450,6-alpha-Monooxygenase, Taurochenodeoxycholate,Cytochrome P 450 CYP3A,Cytochrome P 450 CYP3A4,Cytochrome P 450 CYP3A5,Cytochrome P 450IIIA,Erythromycin N Demethylase,N-Demethylase, Erythromycin,P-450 CYP3A, Cytochrome,P-450 CYP3A4, Cytochrome,P-450 CYP3A5, Cytochrome,P-450IIIA, Cytochrome,P450 3A, Cytochrome,P450 3A5, Cytochrome,Taurochenodeoxycholate 6 alpha Monooxygenase
D019438 Ritonavir An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A. ABT 538,ABT-538,Norvir,ABT538
D065692 Cytochrome P-450 CYP3A Inhibitors Drugs and compounds which inhibit or antagonize the biosynthesis or actions of CYTOCHROME P-450 CYP3A. CYP3A Inhibitor,CYP3A5 Inhibitor,CYP3A7 Inhibitor,Cyp3A4 Inhibitor,Cytochrome P-450 CYP3A Inhibitor,Cytochrome P-450 CYP3A4 Inhibitor,Cytochrome P-450 CYP3A5 Inhibitor,Cytochrome P-450 CYP3A7 Inhibitor,P450 CYP3A Inhibitor,P450 CYP3A4 Inhibitor,P450 CYP3A5 Inhibitor,P450 CYP3A7 Inhibitor,CYP3A Inhibitors,CYP3A4 Inhibitors,CYP3A5 Inhibitors,CYP3A7 Inhibitors,Cytochrome P-450 CYP3A4 Inhibitors,Cytochrome P-450 CYP3A5 Inhibitors,Cytochrome P-450 CYP3A7 Inhibitors,P450 CYP3A Inhibitors,P450 CYP3A4 Inhibitors,P450 CYP3A5 Inhibitors,P450 CYP3A7 Inhibitors,CYP3A Inhibitor, P450,CYP3A4 Inhibitor, P450,CYP3A5 Inhibitor, P450,CYP3A5 Inhibitors, P450,CYP3A7 Inhibitor, P450,CYP3A7 Inhibitors, P450,Cytochrome P 450 CYP3A Inhibitor,Cytochrome P 450 CYP3A Inhibitors,Cytochrome P 450 CYP3A4 Inhibitor,Cytochrome P 450 CYP3A4 Inhibitors,Cytochrome P 450 CYP3A5 Inhibitor,Cytochrome P 450 CYP3A5 Inhibitors,Cytochrome P 450 CYP3A7 Inhibitor,Cytochrome P 450 CYP3A7 Inhibitors,Inhibitor, CYP3A,Inhibitor, CYP3A5,Inhibitor, CYP3A7,Inhibitor, Cyp3A4,Inhibitor, P450 CYP3A,Inhibitor, P450 CYP3A4,Inhibitor, P450 CYP3A5,Inhibitor, P450 CYP3A7,Inhibitors, CYP3A,Inhibitors, CYP3A4,Inhibitors, CYP3A5,Inhibitors, CYP3A7,Inhibitors, P450 CYP3A,Inhibitors, P450 CYP3A4,Inhibitors, P450 CYP3A7

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