Pharmacokinetic study of the interaction between rifabutin and delavirdine mesylate in HIV-1 infected patients

Borin, Marie T.; Chambers, J. H.; Carel, Barbara J.; Freimuth, William W.; Aksentijevich, Sophia; Piergies, Antoni A.

doi:10.1016/s0166-3542(97)00011-9

Cited by 38 publications

(5 citation statements)

References 17 publications

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“…Although this study was conducted with a 900-mg total daily dose of delavirdine mesylate and the currently recommended dose is 1,200 mg (400 mg three times daily), results of several pharmacokinetic studies have demonstrated that due to the high intersubject variability in the pharmacokinetics of delavirdine, there is considerable overlap in drug concentrations between these dosing regimens. Overall, the mean steady-state trough delavirdine level for a dosage of 900 mg/day in the present study (about 12 M) is similar to the value reported for patients receiving a dosage of 1,200 mg/day (about 14 M) (5,6). Thus, the findings from this study should be applicable to the recommended delavirdine mesylate dosage regimen.…”

Section: Discussionsupporting

confidence: 87%

Effect of fluconazole on the steady-state pharmacokinetics of delavirdine in human immunodeficiency virus-positive patients

Borin¹,

Cox²,

Herman³

et al. 1997

Antimicrob Agents Chemother

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Fluconazole, an inhibitor of certain human cytochrome P-450 isozymes, is used for the prevention and treatment of a broad range of fungal infections that predominantly affect immunocompromised individuals. This study evaluated the influence of fluconazole on the steady-state pharmacokinetics of delavirdine, a nonnucleoside inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase, in 13 HIV-1-infected patients with CD4 counts ranging from 186 to 480/mm3. Both the control group (n = 5) and the fluconazole group (n = 8) received 300 mg of delavirdine mesylate every 8 h for 30 days; subjects in the fluconazole group took a 400-mg, once-daily dose of fluconazole on study days 16 to 30. Harvested plasma from serial blood samples collected on days 15, 16, and 30 were assayed for concentrations of delavirdine and its N-desalkyl metabolite by a reversed-phase high-pressure liquid chromatography (HPLC) method. Blood samples obtained on days 16 and 30 were also assayed for fluconazole by HPLC. Delavirdine mesylate alone and in combination with fluconazole was well tolerated. There were no significant differences (P > 0.16) in delavirdine pharmacokinetic parameters between treatment groups on day 15 or day 30. After coadministration of fluconazole and delavirdine mesylate for 2 weeks (day 30), no significant differences (P > 0.058) were observed in any delavirdine pharmacokinetic parameters relative to those after receiving delavirdine mesylate alone (day 15) after in the fluconazole group. Fluconazole pharmacokinetic parameters were similar to those previously reported for healthy volunteers and HIV-positive patients. On the basis of these findings, fluconazole and delavirdine mesylate may be taken concurrently without adjustment of the dose of either drug.

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Section: Discussionsupporting

confidence: 87%

Effect of fluconazole on the steady-state pharmacokinetics of delavirdine in human immunodeficiency virus-positive patients

Borin¹,

Cox²,

Herman³

et al. 1997

Antimicrob Agents Chemother

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“…RIF co-administration resulted in a 2700% increase of oral clearance, leading to nearly negligible delavirdine concentrations [72]. RFB increased the oral clearance by 500% [73]. Co-administration of didanosine with RFB resulted in a 20% AUC increase of didanosine [74].…”

Section: Resultsmentioning

confidence: 99%

Pharmacokinetic Drug Interactions of Antimicrobial Drugs: A Systematic Review on Oxazolidinones, Rifamycines, Macrolides, Fluoroquinolones, and Beta-Lactams

et al. 2011

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Like any other drug, antimicrobial drugs are prone to pharmacokinetic drug interactions. These drug interactions are a major concern in clinical practice as they may have an effect on efficacy and toxicity. This article provides an overview of all published pharmacokinetic studies on drug interactions of the commonly prescribed antimicrobial drugs oxazolidinones, rifamycines, macrolides, fluoroquinolones, and beta-lactams, focusing on systematic research. We describe drug-food and drug-drug interaction studies in humans, affecting antimicrobial drugs as well as concomitantly administered drugs. Since knowledge about mechanisms is of paramount importance for adequate management of drug interactions, the most plausible underlying mechanism of the drug interaction is provided when available. This overview can be used in daily practice to support the management of pharmacokinetic drug interactions of antimicrobial drugs.

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“…The use of rifabutin with NNRTIs should be approached cautiously. Rifabutin reduces delavirdine levels by 80%, and should not be used [53]. For patients treated with efavirenz, the rifabutin daily dose should be increased from 300 to 450 mg.…”

Section: O -A D M I N I S T R a T I O N O F A N T I -T B A N D A N mentioning

confidence: 99%

Tuberculosis in HIV-infected patients: a comprehensive review

Aaron

Saadoun

Calatroni

et al. 2004

Clinical Microbiology and Infection

276

169

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The incidence of tuberculosis (TB) is currently increasing in HIV-infected patients living in Africa and Asia, where TB endemicity is high, reflecting the susceptibility of this group of patients to mycobacteria belonging to the TB group. In this population, extension of multiple resistance to anti-tuberculous drugs is also a matter of anxiety. HIV-induced immunosuppression modifies the clinical presentation of TB, resulting in atypical signs and symptoms, and more frequent extrapulmonary dissemination. The treatment of TB is also more difficult to manage in HIV-infected patients, particularly with regard to pharmacological interactions secondary to inhibition or induction of cytochrome P450 enzymes by protease inhibitors with rifampicin or rifabutin, respectively. Finally, immune restoration induced by highly active anti-retroviral therapy (HAART) in developed countries may be responsible for a paradoxical worsening of TB manifestations.

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Pharmacokinetic study of the interaction between rifabutin and delavirdine mesylate in HIV-1 infected patients

Cited by 38 publications

References 17 publications

Effect of fluconazole on the steady-state pharmacokinetics of delavirdine in human immunodeficiency virus-positive patients

Effect of fluconazole on the steady-state pharmacokinetics of delavirdine in human immunodeficiency virus-positive patients

Pharmacokinetic Drug Interactions of Antimicrobial Drugs: A Systematic Review on Oxazolidinones, Rifamycines, Macrolides, Fluoroquinolones, and Beta-Lactams

Tuberculosis in HIV-infected patients: a comprehensive review

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