Update on Rifampin Drug Interactions

Borcherding, Shawn M; Baciewicz, Anne M.; Self, Timothy H.

doi:10.1001/archinte.1987.00370030169033

Cited by 121 publications

(23 citation statements)

References 60 publications

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“…Quinine is widely used to treat malaria in endemic phylline, antipyrine, hexobarbitone and cyclosporine malaria areas where Plasmodium falciparum is resist- [2][3][4][5][6][7][8]. It has been shown that rifampicin decreases the ant to chloroquine.…”

Section: Introductionmentioning

confidence: 99%

Marked enhancement by rifampicin and lack of effect of isoniazid on the elimination of quinine in man.

Wanwimolruk

Kang

Coville

et al. 1995

Brit J Clinical Pharma

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The effect of rifampicin and isoniazid pretreatment on the pharmacokinetics of quinine after a single oral dose (600 mg quinine sulphate) was studied in nine healthy young Thai male volunteers using a three-way randomized crossover design. Subjects were studied over three 2 day periods, during which they received no pretreatment, or pretreatment with daily 600 mg p.o. rifampicin for 2 weeks, or isoniazid 300 mg p.o. daily for 1 week, prior to quinine administration. The mean (+ s.d.) clearance (CL/F) of quinine coadministered with rifampicin (0.87 ± 0.35 1 h-1 kg-') was significantly greater than that of quinine alone (0.14 ± 0.05 1 h-1 kg-'). The mean difference in clearance from the control treatment was 0.73 1 h-1 kg-', with 95% confidence interval (C.I.) of 0.48 to 0.98. The unbound clearance (CLu/F) of quinine, which reflects the activity of the drug-metabolizing enzymes, was considerably greater (6.9-fold) in subjects when rifampicin was coadministered with quinine than that of quinine alone (6.9 ± 3.6 vs 1.0 ± 0.5 1 h-1 kg-'; the 95% C.I. for the mean difference was 3.3 to 8.5). The mean elimination half-life of quinine when coadministered with rifampicin (5.5 ± 3.0 h) was significantly shorter than when quinine was given alone (11.1 ± 3.0 h; the 95% C.I. for the mean difference was -8.6 to -2.6). In contrast to rifampicin, pretreatment for 1 week with 300 mg oral isoniazid had no significant effects on the pharmacokinetics of quinine. These results indicate that rifampicin pretreatment caused a marked increase (6.2-fold) in the clearance of quinine, possibly due to enzyme induction. The extent to which the elimination of quinine is enhanced by the concomitant administration of rifampicin is likely to have important clinical consequences. Although the clinical significance of these findings is unknown, they indicate the need for caution in the administration of quinine to patients who are concurrently taking rifampicin as an anti-tuberculosis medication.

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Section: Introductionmentioning

confidence: 99%

Marked enhancement by rifampicin and lack of effect of isoniazid on the elimination of quinine in man.

Wanwimolruk

Kang

Coville

et al. 1995

Brit J Clinical Pharma

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“…Drug-drug interactions involving drug-metabolizing enzymes and transporters are of increasing interest due to reports of adverse reactions and loss of efficacy (Baciewicz et al, 1987;Spina et al, 1996). During drug development, in vitro assays can be used to avoid inducers, and characterize drug-drug interaction potential due to increased drug clearance by the liver.…”

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confidence: 99%

Induction of Drug Metabolism Enzymes and MDR1 Using a Novel Human Hepatocyte Cell Line

Mills¹,

Rose²,

Sadagopan³

et al. 2004

J Pharmacol Exp Ther

135

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Induction of drug-metabolizing enzymes and transporters can cause drug-drug interactions and loss of efficacy. In vitro induction studies traditionally use primary hepatocyte cultures and enzyme activity with selected marker compounds. We investigated the use of a novel human hepatocyte clone, the Fa2N-4 cell line, as an alternative reagent, which is readily available and provides a consistent, reproducible system. We used the Invader assay to monitor gene expression in these cells. This assay is a robust, yet simple, high-throughput system for quantification of mRNA transcripts. CYP1A2, CYP3A4, CYP2C9, UGT1A, and MDR1 transcripts were quantified from total RNA extracts from Fa2N-4 cells treated with a panel of known inducers and compared with vehicle controls. In addition, we used enzyme activity assays to monitor the induction of CYP1A2, CYP2C9, and CYP3A4. The Fa2N-4 cells responded in a similar manner as primary human hepatocytes. Treatment with 10 M rifampin resulted in increases in CYP3A4 mRNA (17-fold) and activity (6-␤-hydroxytestoterone formation, 9-fold); and in CYP2C9 mRNA (4-fold) and activity (4Ј-hydroxydiclofenac formation, 2-fold). Treatment with 50 M ␤-naphthoflavone resulted in increases in CYP1A2 mRNA (15-fold) and activity (7-ethoxyresorufin O-dealkylation, 27-fold). UGT1A mRNA was induced by ␤-naphthoflavone (2-fold), and MDR1 (P-glycoprotein) mRNA was induced by rifampin (3-fold). These preliminary data using a few prototypical inducers show that Fa2N-4 cells can be a reliable surrogate for primary human hepatocytes, and, when used in conjunction with the Invader technology, could provide a reliable assay for assessment of induction of drug-metabolizing enzymes and transporters.

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“…Our limited experience has suggested that a 2-mg dose may be less effective if rifamycin derivatives are given concomitantly, presumably because of the enhanced hepatic metabolism of the steroid (1).…”

Section: Discussionmentioning

confidence: 99%

“…Two patients underwent necropsy, which showed lymphoma, MAC, and interstitial pneumonia for patient 1 and cytomegalovirus and pyogenic pneumonia for patient 3. Patient 2 died of an undetermined type of pneumonia.…”

mentioning

confidence: 99%

Low-dose dexamethasone as adjunctive therapy for disseminated Mycobacterium avium complex infections in AIDS patients

Wormser

Horowitz

Dworkin

1994

Antimicrob Agents Chemother

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Five human immunodeficiency virus-infected patients with disseminated Mycobacterium avium complex infection had progressive weight loss and persistent fever despite multidrug antimycobacterial therapy. These patients were given daily low-dose oral dexamethasone (typically 2 mg/day) as adjunctive therapy. All had substantial and sustained weight gain (12 to 50%o of pre-steroid treatment body weight [P < 0.03]), reduction in fever, and an improved sense of well-being. The serum albumin level increased during dexamethasone therapy (from 3.06 ± 0.59 g/dl [mean + standard deviation] to 3.9 ± 0.22 g/dl [P < 0.01]), while the serum alkaline phosphatase level fell (from 368 ± 247 U/liter to 128 + 43.6 U/liter [P < 0.04]). Further studies of the potential role for corticosteroids in the management of disseminated M. avium complex infections in human immunodeficiency virus-infected patients are warranted.

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Update on Rifampin Drug Interactions

Cited by 121 publications

References 60 publications

Marked enhancement by rifampicin and lack of effect of isoniazid on the elimination of quinine in man.

Marked enhancement by rifampicin and lack of effect of isoniazid on the elimination of quinine in man.

Induction of Drug Metabolism Enzymes and MDR1 Using a Novel Human Hepatocyte Cell Line

Low-dose dexamethasone as adjunctive therapy for disseminated Mycobacterium avium complex infections in AIDS patients

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