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Inhibitory potency of quinolone antibacterial agents against cytochrome P450IA2 activity in vivo and in vitro.
Inhibition of cytochrome P450IA2 activity is an important adverse effect of quinolone antibacterial agents. It results in a prolonged half-life for some drugs that are coadministered with quinolones,Expand
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Biotransformation of caffeine and theophylline in mammalian cell lines genetically engineered for expression of single cytochrome P450 isoforms.
Primary steps in the metabolism of caffeine and theophylline are cleavage of methyl groups and/or hydroxylation at position 8, mediated by cytochromes P450. V79 Chinese hamster cells geneticallyExpand
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Inhibitory effect of grapefruit juice and its bitter principal, naringenin, on CYP1A2 dependent metabolism of caffeine in man.
1. The effects of grapefruit juice and naringenin on the activity of the human cytochrome P450 isoform CYP1A2 were evaluated using caffeine as a probe substrate. 2. In vitro naringin was a potentExpand
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Evaluation of caffeine as a test drug for CYP1A2, NAT2 and CYP2E1 phenotyping in man by in vivo versus in vitro correlations.
Caffeine is used to phenotype subjects in vivo for the cytochrome P450 isoforms CYP1A2 and CYP2E1, and for N-acetyltransferase type 2 (NAT2). However, how much of the variation in phenotypingExpand
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Quinolone inhibition of cytochrome P-450-dependent caffeine metabolism in human liver microsomes.
Inhibitory effects of the quinolone antibiotics ofloxacin, lomefloxacin, pipemidic acid, ciprofloxacin, and enoxacin on caffeine metabolism were examined in vitro with human liver microsomes of fourExpand
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Variation of CYP1A2-dependent caffeine metabolism during menstrual cycle in healthy women.
BACKGROUND AND OBJECTIVES The activity of the human cytochrome P450 CYP1A2 is decreased by female sex hormones during pregnancy or treatment with oral contraceptives. However, the influence ofExpand
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Decrease of caffeine elimination in man during co-administration of 4-quinolones.
The single dose pharmacokinetics of caffeine (220-230 mg per dose) were investigated in 12 healthy male volunteers before and during treatment with ofloxacin (200 mg bd), ciprofloxacin (250 mg bd)Expand
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Investigation of nifedipine absorption in different regions of the human gastrointestinal (GI) tract after simultaneous administration of 13C- and 12C-nifedipine
Objective: To evaluate the absorption of nifedipine in man from four different sites of the gastrointestinal tract.Methods:On separate occasions, nifedipine solution was administered locally to theExpand
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Ciprofloxacin absorption in different regions of the human gastrointestinal tract. Investigations with the hf-capsule.
1. The absorption of ciprofloxacin from different regions of the human gastrointestinal tract was investigated in four healthy males using a remote-controlled drug delivery device (hf-capsule). 2.Expand
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Lacking effect of grapefruit juice on theophylline pharmacokinetics.
Grapefruit juice inhibits the biotransformation of several drugs, including caffeine (23% clearance reduction), which is metabolized by the cytochrome P450 isoform CYP1A2. Since CYP1A2 alsoExpand
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