Norfloxacin-Cyclosporine Interaction

Dj, Thomson; Ah, Menkis; Fn, McKenzie

doi:10.1097/00007890-198808000-00024

Cited by 29 publications

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“…In the species other than dogs, some researchers have also reported the inhibitory effects of the antimicrobials on CYP3A activities. Thomson et al (1988) reported an interaction in a human patient between norfloxacin (NFX) and cyclosporine A, a CYP3A substrate in humans. They observed elevated serum concentrations of cyclosporine A in the patient when NFX was co-administered.…”

Section: Introductionmentioning

confidence: 99%

Lack of inhibitory effects of several fluoroquinolones on cytochrome P‐450 3A activities at clinical dosage in dogs

Regmi

El‐Aty

Kubota

et al. 2007

Vet Pharm & Therapeutics

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Inhibitory effects of several fluoroquinolones (FQs) on liver CYP3A activities were examined by in vitro and in vivo tests in dogs. Midazolam (MDZ) hydroxylation rate was used to determine the CYP3A activities in liver microsomes. Enrofloxacin (EFX), ofloxacin (OFX) orbifloxacin (OBFX) and ciprofloxacin (CFX) were tested. None of the FQs changed Vmax, Km or intrinsic clearance (Vmax/Km) of MDZ. For in vivo test, we examined the effects of oral administration of EFX and OFX on the pharmacokinetics of quinidine (QN), a CYP3A substrate. EFX or OFX (10 mg/kg) was administered once a day for 3 days. QN (2 mg/kg) was intravenously injected at 2 h after the final dose of FQs administration. The same dose of QN was intravenously injected 3 weeks before the start of FQs administration for control. Neither EFX nor OFX changed the pharmacokinetic parameters of QN. These in vitro and in vivo consisted results suggest that these FQs lack the inhibitory effects on CYP3A activities in dogs. Hence, given these results, the risk of drug-drug interaction is unlikely to occur between FQs and CYP3A substrates in clinical situation in dogs.

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Section: Introductionmentioning

confidence: 99%

Lack of inhibitory effects of several fluoroquinolones on cytochrome P‐450 3A activities at clinical dosage in dogs

Regmi

El‐Aty

Kubota

et al. 2007

Vet Pharm & Therapeutics

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Management of Drug Interactions With Cyclosporine

Lake

1991

Pharmacotherapy

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Major advances in transplantation and in the treatment of autoimmune disorders have been achieved with the use of cyclosporine (CsA). During the past 10 years a variety of drug interactions have been reported to occur with CsA. These may be classified as either pharmacokinetic or pharmacodynamic in origin. Pharmacokinetic interactions are manifested by either an increase or decrease in the CsA concentration. The predominant mechanism of interaction is alteration in the cytochrome P‐450 metabolism of CsA, however, some of the drugs may also affect its absorption, distribution, and elimination. Pharmacodynamic interactions include enhanced nephrotoxicity. Management of these events mandates proactive measures such as assessing the interactive potential of each new agent, measuring CsA concentrations more frequently when either initiating or discontinuing other agents, adjusting the dosage of CsA as necessary, and monitoring patients' clinical status to ensure efficacy and minimize the risk of toxicity.

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Drug‐Drug Interactions With Fluoroquinolones

Marchbanks

1993

Pharmacotherapy

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Antimicrobials of the fluoroquinolone class are involved in a number of clinically important drug‐drug interactions. Many of these interactions occur with all the available agents and exhibit little interpatient variability. In contrast, others occur only with specific fluoroquinolones and their extent varies markedly among subjects. The oral absorption of all fluoroquinolones is significantly impaired when coadministered with aluminum‐ and magnesium‐containing antacids and sucralfate, as well as with other metal cations such as calcium and iron. Concomitant use of these agents, even when dosed several hours apart, should be avoided. Enoxacin and ciprofloxacin impair the hepatic metabolism of theophylline and caffeine, leading to significantly increased serum concentrations. Ofloxacin and lomefloxacin have only minimal effects on xanthine metabolism. Case reports suggest that concomitant administration of several fluoroquinolones and warfarin, a drug that is also highly metabolized by the liver, leads to increased hypoprothrombinemic effects; prospective studies, however, failed to confirm this interaction. Clinicians must be aware of these and other potential drug‐drug interactions with fluoroquinolones for optimal use of the agents.

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Norfloxacin-Cyclosporine Interaction

Cited by 29 publications

References 0 publications

Lack of inhibitory effects of several fluoroquinolones on cytochrome P‐450 3A activities at clinical dosage in dogs

Lack of inhibitory effects of several fluoroquinolones on cytochrome P‐450 3A activities at clinical dosage in dogs

Management of Drug Interactions With Cyclosporine

Drug‐Drug Interactions With Fluoroquinolones

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