1988
DOI: 10.1378/chest.94.5.954
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Near-total Reduction in Verapamil Bioavailability by Rifampin

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Cited by 45 publications
(24 citation statements)
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“…In addition, before our mouse treatment study, we conducted a pharmacologic assessment of the rifampin-verapamil drug-drug interaction. Although it is known that concomitant rifampin administration lowers levels of orally administered verapamil by approximately 90% via induction of CYP3A4 in humans (25,26,32), the earlier 2-month mouse study with multidrug-resistant TB infection did not adjust the verapamil dosing for this interaction. Our pharmacologic assessment revealed that, in mice receiving steady-state rifampin, it is necessary to use a verapamil dose of 9.4 mg/kg to achieve a daily AUC equivalent to that achieved with 40 mg/d of verapamil in humans.…”
Section: Discussionmentioning
confidence: 99%
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“…In addition, before our mouse treatment study, we conducted a pharmacologic assessment of the rifampin-verapamil drug-drug interaction. Although it is known that concomitant rifampin administration lowers levels of orally administered verapamil by approximately 90% via induction of CYP3A4 in humans (25,26,32), the earlier 2-month mouse study with multidrug-resistant TB infection did not adjust the verapamil dosing for this interaction. Our pharmacologic assessment revealed that, in mice receiving steady-state rifampin, it is necessary to use a verapamil dose of 9.4 mg/kg to achieve a daily AUC equivalent to that achieved with 40 mg/d of verapamil in humans.…”
Section: Discussionmentioning
confidence: 99%
“…In humans, rifampin causes up to a 10-fold reduction in plasma levels of orally administered verapamil (25,26). To assess the nature of this interaction in mice, we measured mouse plasma verapamil levels after steady-state induction by rifampin for 10 days.…”
Section: Pharmacokinetic Studies and Dose Selection For Verapamil Trementioning
confidence: 99%
“…In principle, strong SXR activators should lead to higher levels of CYP3A4, which is involved in the clearance of 60% of clinically relevant drugs (Cholerton et al 1992). For example, rifampicin leads to increased clearance of calcium channel blockers such as nifedipine (Holtbecker et al 1996;Ndanusa et al 1997) and verapamil (Barbarash et al 1988), anti-arhythmics such as pirmenol (Stringer et al 1988), and ␤-blockers such as propranolol (Herman et al 1983), in addition to the steroid interactions mentioned above. It should be noted that, although most CYP3A4 inducers are SXR activators, a few such as cyclosporine A fail to activate SXR.…”
Section: Discussionmentioning
confidence: 99%
“…So far, the complex pattern of verapamil oxidative metabolism has been extensively studied ( Fig. Data in parentheses indicate the amount of metabolite excreted in urine (Eichelbaum et al 1978) rail metabolism (Kroemer et al 1992) and characterized some of the respective P 450 enzymes involved (Fuhr et al 1992;Kroemer et al 1993): the identification of the enzymes catalyzing the two main metabolic routes of veraparail, namely the N-demethylation by C Y P 3 A 4 and the Ndealkylation by C Y P 3 A 4 and 1A2, has provided the molecular base for our understanding of the metabolic in vivo interactions of verapamil with other C Y P 3 A 4 or C Y P 1 A 2 substrates like cyclosporine (Lindholm and Henrissons 1987), theophylline (Abemethy et al 1988) and caffeine (Fuhr et al 1992) or inducers like phenobarbital (Rutledge et al 1988) and rifampicin (Barbarash et al 1988). Previous studies of the in vitro metabolism of verapamil have evaluated the contribution of the individual pathways to overall verapa- Fig.…”
Section: Introductionmentioning
confidence: 99%