Abstract
Darunavir is a new HIV protease inhibitor that has been shown to be highly useful in HIV-infected patients. This drug is primarily metabolized by the liver through the cytochrome P450 3A4 (CYP3A4) isozyme and consequently coadministration with low doses of ritonavir markedly increases exposure and allows both daily doses and pill burden to be reduced. Both darunavir and ritonavir act as inhibitors and substrates of CYP3A4 and may therefore present pharmacological interactions with a large number of drugs commonly used in HIV-infected patients. The present review aims to summarize the main studies that have evaluated drug interactions and to provide recommendations on treatment with darunavir/ritonavir in clinical practice.
MeSH terms
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Anti-HIV Agents / administration & dosage
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Anti-HIV Agents / pharmacology
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Anti-Infective Agents / administration & dosage
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Anti-Infective Agents / pharmacology
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Anti-Ulcer Agents / administration & dosage
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Anti-Ulcer Agents / pharmacology
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Cardiovascular Agents / administration & dosage
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Cardiovascular Agents / pharmacology
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Contraceptives, Oral, Hormonal / administration & dosage
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Contraceptives, Oral, Hormonal / pharmacology
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Cytochrome P-450 CYP3A / metabolism
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Darunavir
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Drug Interactions
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Drug Therapy, Combination
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HIV Infections / drug therapy*
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HIV Infections / metabolism
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HIV Protease Inhibitors / administration & dosage
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HIV Protease Inhibitors / pharmacokinetics
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HIV Protease Inhibitors / pharmacology*
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Humans
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Microsomes, Liver / metabolism
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Phosphodiesterase Inhibitors / administration & dosage
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Phosphodiesterase Inhibitors / pharmacology
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Ritonavir / administration & dosage
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Ritonavir / pharmacokinetics
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Ritonavir / pharmacology
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Selective Serotonin Reuptake Inhibitors / administration & dosage
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Selective Serotonin Reuptake Inhibitors / pharmacology
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Sulfonamides / administration & dosage
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Sulfonamides / pharmacokinetics
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Sulfonamides / pharmacology*
Substances
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Anti-HIV Agents
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Anti-Infective Agents
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Anti-Ulcer Agents
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Cardiovascular Agents
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Contraceptives, Oral, Hormonal
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HIV Protease Inhibitors
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Phosphodiesterase Inhibitors
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Serotonin Uptake Inhibitors
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Sulfonamides
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Cytochrome P-450 CYP3A
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CYP3A4 protein, human
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Ritonavir
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Darunavir