Interactions among Drugs for HIV and Opportunistic Infections

Piscitelli, Stephen C.; Gallicano, Keith

doi:10.1056/nejm200103293441307

Cited by 282 publications

(194 citation statements)

References 81 publications

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“…Pharmacokinetics for orally administered drugs includes absorption, distribution, metabolism and elimination. 13 Interactions of metabolism especially affect the following: 14 • Drug absorption due to changes in gastric pH • Cytochrome P450 system • Modulation of P-glycoprotein • Induction of glucoronidation • Renal elimination Most ARVs are well absorbed when administered orally, 15 undergo passive diffusion through the gastro-intestinal system and are then metabolised by cytochrome P450 (CYP)3A and CYP2B6 isoenzymes. 13 Absorption of drugs can be altered by changes in the gastric pH, which has specific implications for the critically ill individual where antacids may decrease drug absorption.…”

Section: Pharmacokinetic Overview Of the Arv Drugs In Clinical Usementioning

confidence: 99%

“…13 Absorption of drugs can be altered by changes in the gastric pH, which has specific implications for the critically ill individual where antacids may decrease drug absorption. 14,15 Lipophilic drugs such as the PIs and NNRTIs are oxidatively metabolised by the P450 system to more polar forms for biliary or renal excretion. 13 These drugs can further be classified according to their effects as cytochrome P450 enzyme inducers or inhibitors.…”

Section: Pharmacokinetic Overview Of the Arv Drugs In Clinical Usementioning

confidence: 99%

“…13 These drugs can further be classified according to their effects as cytochrome P450 enzyme inducers or inhibitors. 14 This means that the plasma concentration of drugs taken concurrently with these ARV drugs can either be increased or decreased, 14 and some drugs may alter their own metabolism over time. However, some drugs like ritonavir and efavirenz may have properties of both induction and inhibition depending on the combination used.…”

Section: Pharmacokinetic Overview Of the Arv Drugs In Clinical Usementioning

confidence: 99%

“…14 Thus, drugs that induce cytochrome enzymes increase the hepatic metabolism of other drugs and lead to lower plasma concentration. 14,15 NRTIs are water soluble (except for zidovudine) and are eliminated renally. 13 However, the NRTIs are prodrugs and require intracellular phosphorylation to be activated.…”

Section: Pharmacokinetic Overview Of the Arv Drugs In Clinical Usementioning

confidence: 99%

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Antiretroviral therapyand anaesthesia

Schulenburg

Roux

2008

Southern African Journal of Anaesthesia and Analgesia

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HIV has reached pandemic proportions in Southern Africa. Great emphasis is placed on the prevention and containment of HIV transmission by suppressing virus replication using highly active anti-retroviral therapy (HAART). HAART has proven to be highly effective if taken correctly, and has lead to increased life expectancy. Increasing numbers of HIV-positive patients on antiretroviral (ARV) therapy or HIV-exposed individuals taking prophylaxis present for surgery and critical care management. The anaesthesiologist should be familiar with the anaesthetic implications of HIV as well as the possible drug interactions while on ARV treatment. This article focuses specifically on the anaesthetic implications of the patient on HAART.HAART is HIV treatment with a combination of three or more ARV drugs from five broad classes. The specific HAART regimen in use in South Africa is considered in detail in this article. The pharmacokinetics of the ARV drugs is complex, and subject to interactions at many different sites. Serious drug interactions are possible, including drugs commonly used in anaesthesia. Drug interactions and recommendations are discussed in detail.ARVs are known to cause multiple systemic side effects, including lactic acidosis, Immune Reconstitution Inflammatory Syndrome (IRIS), premature atherosclerosis and increased cardiovascular risk, hyperlipidaemia, insulin resistance, skeletal disorders, hepatotoxicity, lipodystrophy, mitochondrial abnormalities, allergic reactions and pancreatitis.Non-compliance is common, and leads to the rapid development of resistance. The anaesthesiologist may inadvertently exacerbate this in the perioperative period. Recommendations regarding the interruption of treatment and fasting are made. Alternative routes for HAART administration are also explored. The management of the critically ill patient on a HAART regimen is discussed.

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Section: Pharmacokinetic Overview Of the Arv Drugs In Clinical Usementioning

confidence: 99%

Section: Pharmacokinetic Overview Of the Arv Drugs In Clinical Usementioning

confidence: 99%

Section: Pharmacokinetic Overview Of the Arv Drugs In Clinical Usementioning

confidence: 99%

Section: Pharmacokinetic Overview Of the Arv Drugs In Clinical Usementioning

confidence: 99%

See 2 more Smart Citations

Antiretroviral therapyand anaesthesia

Schulenburg

Roux

2008

Southern African Journal of Anaesthesia and Analgesia

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show abstract

“…Various antiretroviral medications may act as cytochrome p450 substrates, activators, inhibitors, or, as ritonavir, nelfinavir, and efavirenz do, act as a combination of all three (162). The activation of this enzymatic system by the drug may decrease the concentration of steroid hormones, resulting in a decrease in contraceptive efficacy.…”

Section: Contraceptionmentioning

confidence: 99%