Influence of Antiretroviral Drugs on the Pharmacokinetics of Prednisolone in HIV-Infected Individuals

Busse, Kristin; Formentini, Elizabeth; Alfaro, Raul M.; Kovacs, Joseph A.; Penzak, Scott R.

doi:10.1097/qai.0b013e31817bebeb

Cited by 21 publications

(17 citation statements)

References 32 publications

(24 reference statements)

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“…26 Finally, cART can also interact with the metabolic pathway of glucocortoids through either inhibition or induction of CYP3A enzymes. 27 …”

Section: Immunosuppressants In Hiv-infected Solid Organ Transplant Rementioning

confidence: 97%

“…28 PIs are known strong inhibitors of CYP3A enzymes and P-gp, but RTV is by far the most powerful CYP3A and Pgp inhibitor currently available requiring dramatic dosage adjustments of numerous CYP3A and Pgp substrates. 38 Glucocortoid clearance, for example, has been reported to be significantly reduced in patients on RTV-boosted PIs resulting in higher serum concentrations and side effects like Cushing syndrome 27 Since glucocortoid levels are not routinely monitored, dosages are mostly adjusted based on patient (in)tolerance and biochemical parameters.…”

Section: Protease Inhibitorsmentioning

confidence: 99%

See 1 more Smart Citation

Drug–Drug Interactions Between Antiretroviral and Immunosuppressive Agents in HIV-Infected Patients After Solid Organ Transplantation: A Review

Maarseveen

Rogers

Trofe‐Clark

et al. 2012

AIDS Patient Care and STDs

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Since the introduction of combination antiretroviral therapy (cART) resulting in the prolonged survival of HIV-infected patients, HIV infection is no longer considered to be a contraindication for solid organ transplantation (SOT). The combined management of antiretroviral and immunosuppressive therapy proved to be extremely challenging, as witnessed by high rates of allograft rejection and drug toxicity, but the profound drug-drug interactions between immunosuppressants and cART, especially protease inhibitors (PIs) also play an important role. Caution and frequent drug level monitoring of calcineurin inhibitors, such as tacrolimus are necessary when PIs are (re)introduced or withdrawn in HIV-infected recipients. Furthermore, the pharmacokinetics of glucocorticoids and mTOR inhibitors are seriously affected by PIs. With the introduction of integrase inhibitors, CCR5-antagonists and fusion inhibitors which cause significantly less pharmacokinetic interactions, have minor overlapping toxicity, and offer the advantage of pharmacodynamic synergy, it is time to revaluate what may be considered the optimal antiretroviral regimen in SOT recipients. In this review we provide a brief overview of the recent success of SOT in the HIV population, and an update on the pharmacokinetic and pharmacodynamic interactions between currently available cART and immunosuppressants in HIV-infected patients, who underwent SOT.

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“…26 Finally, cART can also interact with the metabolic pathway of glucocortoids through either inhibition or induction of CYP3A enzymes. 27 …”

Section: Immunosuppressants In Hiv-infected Solid Organ Transplant Rementioning

confidence: 97%

Section: Protease Inhibitorsmentioning

confidence: 99%

Drug–Drug Interactions Between Antiretroviral and Immunosuppressive Agents in HIV-Infected Patients After Solid Organ Transplantation: A Review

Maarseveen

Rogers

Trofe‐Clark

et al. 2012

AIDS Patient Care and STDs

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“…Our patient was on 100mg of ritonavir daily and also received overthe-counter intramuscular triamcinolone. Glucocorticoids are generally deactivated by CYP3A4 enzymes and therefore when ritonavir is given together with glucocorticoids the systemic levels of glucocorticoids increase dramatically due to inhibition of CYP3A4 [8]. PIs inactivate CYP4503A4 by acting as substrates for the enzyme, leading to the formation of a metabolic intermediate complex, a process called mechanism-based inactivation [11].…”

Section: Discussionmentioning

confidence: 99%

“…It is a potent inhibitor of hepatic cytochrome P450 3A4 (CYP3A4) isoenzyme [5]. Ritonavir reduces the metabolism of systemic steroids, which may lead to clinical Cushing's syndrome and secondary adrenal insufficiency [6][7][8]. Despite occasional reports of Cushing's syndrome occurring with the use of injectable triamcinolone even in the absence of CYP3A4 inhibitors, it is not clear if caution should be exercised when considering the use of local steroid injections in the setting of ritonavir therapy [9,10].…”

Section: Introductionmentioning

confidence: 99%

Iatrogenic Cushing’s Syndrome with Secondary Adrenal Suppression Misdiagnosed as Protease Inhibitor-Induced Lipodystrophy in an HIV Positive Patient: Case Report

Efie¹

2017

HIJ

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“…NNRTIs, namely efavirenz, can result in induction of CYP 3A4, potentially reducing levels of corticosteroids. 26,27 …”

Section: Experience Injectable Steroid-ritonavir Interactionmentioning

confidence: 99%

Iatrogenic Cushing's syndrome after triamcinolone plus ritonavir-boosted atazanavir

Jakeman

Conklin

Bouchonville

et al. 2015

Journal of the American Pharmacists Association

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Influence of Antiretroviral Drugs on the Pharmacokinetics of Prednisolone in HIV-Infected Individuals

Cited by 21 publications

References 32 publications

Drug–Drug Interactions Between Antiretroviral and Immunosuppressive Agents in HIV-Infected Patients After Solid Organ Transplantation: A Review

Drug–Drug Interactions Between Antiretroviral and Immunosuppressive Agents in HIV-Infected Patients After Solid Organ Transplantation: A Review

Iatrogenic Cushing’s Syndrome with Secondary Adrenal Suppression Misdiagnosed as Protease Inhibitor-Induced Lipodystrophy in an HIV Positive Patient: Case Report

Iatrogenic Cushing's syndrome after triamcinolone plus ritonavir-boosted atazanavir

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