Effects of Temafloxacin and Ciprofloxacin on the Pharmacokinetics of Caffeine†

Mahr, G.; Sörgel, Fritz; Granneman, G. Richard; Kinzig, Martina; Muth, P.; Patterson, Karen J.; Fuhr, Uwe; Nickel, Peter; Stephan, U

doi:10.2165/00003088-199200221-00015

Cited by 33 publications

(16 citation statements)

References 20 publications

(14 reference statements)

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“…The same study found that OFX had negligible influence on caffeine PK parameters. Another study observed an increase in AUC and terminal phase half-life of caffeine by 145% and 115% respectively when co-administered with 1500 mg CIP [288]. The authors recommended that patients receiving CIP restrict their intake of caffeine.…”

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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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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“…Study 4: In this double-blind placebo-controlled randomised study of the interaction potential of ciprofloxacin and temafloxacin with caffeine, oral temafloxacin 600mg (n = 12) was administered q12h for 7 days (Mahr et al 1992).…”

Section: Studies and Volunteersmentioning

confidence: 99%

Pharmacokinetics of Temafloxacin after Multiple Oral Administration

1992

Clinical Pharmacokinetics

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Four multiple dose studies involving 102 healthy volunteers were reviewed to determine the sources of intersubject variability in the pharmacokinetics of temafloxacin. As a result of the preferential distribution of temafloxacin into muscle, liver and kidney compared with adipose tissue, the best anthropometric explanatory variable was found to be lean body mass, rather than total body mass or body surface area. Single dose studies have confirmed that the distribution volume of temafloxacin is smaller in subjects in whom the lean body mass: total body mass ratio is low, notably in females, the elderly, and those with hepatic impairment. Average creatinine clearance for the volunteers included in this analysis was normal (109 ± 29 mlfmin), and renal function was only a marginally significant covariate; however, renal clearance accounts for 60 to 70% of total clearance (CLT) and has been shown to be a major factor in the elderly, as well as in patients with renal or hepatic impairment. Since temafloxacin is partially reabsorbed renally, urine flow rate was found to be a potentially important secondary factor. Overall, the pharmacokinetics of temafloxacin are essentially linear, with steady-state plasma concentrations at trough (C~in) and 2h postdose (Cl~) averaging slightly more than 0.5 and 1.0 mgjL per 100mg administered every (q) 12h. For example, mean C~in and peak steady-state plasma concentration (C~aJ values after administration of temafloxacin 600mg ql2h were 3.3 ± l.l and 6.2 ± 1.8 mgjL, respectively. Total apparent clearance (CLTjF) and the terminal elimination half-life (tv,) averaged II Ljh (184 mlfmin) per 55kg lean body mass and 8.4h, respectively. Considering that the data reviewed came from 4 studies with doses ranging from 100 to 800mg ql2h, the intersubject coefficients of variation were low for an orally administered drug, ranging from 15.4% for tv" 20.6% for cl~, 21.2% for CLT/F and 25% for C~in.

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“…Ciprofloxacin is a potent inhibitor of CYP1A2 and a weak inhibitor of CYP3A4 [4,5] . Some npg studies have demonstrated a drug-drug interaction when ciprofloxacin was co-administered with other drugs, including theophylline [6,7] , caffeine [8] , clozapine [9] , methadone [10] and zolpidem [11] . Ciprofloxacin is commonly prescribed with analgesics for the management of infection, pain and inflammation.…”

Section: Introductionmentioning

confidence: 99%

Ciprofloxacin blocked enterohepatic circulation of diclofenac and alleviated NSAID-induced enteropathy in rats partly by inhibiting intestinal β-glucuronidase activity

et al. 2016

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Aim: Diclofenac is a non-steroidal anti-inflammatory drug (NSAID), which may cause serious intestinal adverse reactions (enteropathy). In this study we investigated whether co-administration of ciprofloxacin affected the pharmacokinetics of diclofenac and diclofenacinduced enteropathy in rats. Methods: The pharmacokinetics of diclofenac was assessed in rats after receiving diclofenac (10 mg/kg, ig, or 5 mg/kg, iv), with or without ciprofloxacin (20 mg/kg, ig) co-administered. After receiving 6 oral doses or 15 intravenous doses of diclofenac, the rats were sacrificed, and small intestine was removed to examine diclofenac-induced enteropathy. β-Glucuronidase activity in intestinal content, bovine liver and E coli was evaluated. Results: Following oral or intravenous administration, the pharmacokinetic profile of diclofenac displayed typical enterohepatic circulation, and co-administration of ciprofloxacin abolished the enterohepatic circulation, resulted in significant reduction in the plasma content of diclofenac. In control rats, β-glucuronidase activity in small intestinal content was region-dependent: proximal intestine

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Effects of Temafloxacin and Ciprofloxacin on the Pharmacokinetics of Caffeine†

Cited by 33 publications

References 20 publications

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

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

Pharmacokinetics of Temafloxacin after Multiple Oral Administration

Ciprofloxacin blocked enterohepatic circulation of diclofenac and alleviated NSAID-induced enteropathy in rats partly by inhibiting intestinal β-glucuronidase activity

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