Modification of pharmacokinetics of norfloxacin following oral administration of curcumin in rabbits

Pavithra, B. H.; Prakash, N.; Jayakumar, K.

doi:10.4142/jvs.2009.10.4.293

Cited by 37 publications

(27 citation statements)

References 18 publications

(27 reference statements)

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“…Pavithra et al [22] reported that prior treatment of curcumin (60 mg kg -1 , PO) for 3 days significantly increased elimination half-life and volume of distribution of norfloxacin, a reported CYP1A2 inhibitor, in rabbits.…”

Section: Resultsmentioning

confidence: 98%

Curcumin Pretreatment Decreases Absorption of Phenacetin (Cytochrome P450 1A2 Substrate), Without Altering its Disposition Kinetics in Rats

Prasad¹,

Vivek

Rao³

et al. 2016

Proc. Natl. Acad. Sci., India, Sect. B Biol. Sci.

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Many drugs used in the therapeutic regimen for various ailments undergo metabolism via cytochrome P450 1A2 (CYP1A2), so the agents or conditions altering the expression and/or activity of this enzyme play a significant role in therapeutic efficacy/failure of its substrates. Though curcumin is reported to be an inhibitor of CYP1A2, influence of curcumin on the pharmacokinetics of CYP1A2 probe phenacetin in rats has not yet been published to the best of our knowledge. Hence an attempt has been made to investigate the same. Two groups of wistar albino rats were taken, of which, one group received curcumin at 400 mg kg -1 , per os (PO) followed by phenacetin (150 mg kg -1 , PO) and the other received only phenacetin. Plasma concentrations of phenacetin, a known CYP1A2 substrate and its metabolite paracetamol were determined by high performance liquid chromatography. Based on plasma concentrations, the pharmacokinetic parameters were determined by compartmental methods. Curcumin pretreatment significantly (P \ 0.05) decreased peak plasma concentration (C max ) of phenacetin in rats. None of the other pharmacokinetic parameters of either phenacetin or paracetamol were affected. To conclude, curcumin pretreatment decreases C max of phenacetin but has no role on the disposition kinetics of either phenacetin or its metabolite paracetamol in rats. This implies that single dose of curcumin has no effect on CYP1A2 mediated metabolism in rats.

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Section: Resultsmentioning

confidence: 98%

Curcumin Pretreatment Decreases Absorption of Phenacetin (Cytochrome P450 1A2 Substrate), Without Altering its Disposition Kinetics in Rats

Prasad¹,

Vivek

Rao³

et al. 2016

Proc. Natl. Acad. Sci., India, Sect. B Biol. Sci.

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“…After oral curcumin pretreatment for 3 days in rabbits, single oral dose norfloxacin pharmacokinetics were significantly modified compared with those in the non-pretreated group. Mean absorption half-life was decreased (by 23%) while increases were seen in the absorption rate constant (by 41%), t½ (by 19%), AUC (by 52%), AUC (first moment) (by 69%), mean residence time (by 12%), and Vd (area) (by 31%) (all p < 0.05) [308].…”

Section: Metabolism Interactionsmentioning

confidence: 95%

Quinolones

Guay¹

2011

Drug Interactions in Infectious Diseases

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Fluoroquinolone (FQ) antimicrobials are among the most commonly used agents in the outpatient and institutional patient care environments. Due to this high frequency of utilization, the potential for deleterious drug-drug interactions with nonantimicrobials is also high. The majority of interactions with the FQs involve deleterious effects on the FQ component. These are also the most clinically-important interactions with these agents. Multivalent cations such as Mg , and other minerals as well as drugs such as sucralfate, lanthanum, sevelamer, and didanosine (the cation-supplemented version of the latter) can substantially reduce FQ bioavailability, leading the subtherapeutic drug concentrations at the infection site and clinical failure. Separation of dose administrations may or may not reduce the magnitude of these interactions. Ciprofloxacin, norfloxacin, and two experimental FQs in clinical trials (pazufloxacin and prulifloxacin) act as moderate cytochrome P450 enzyme inhibitors and may increase serum concentrations of theophylline and caffeine. Warfarin pharmacodynamics are variably affected by the FQs. The pharmacodynamic interactions between NSAIDs and FQs are only relevant if fenbufen is used concurrently with enoxacin or, possibly, prulifloxacin. Caution is warranted if sparfloxacin or moxifloxacin is used concurrently with other medications prolonging the QTc interval or if patients have other risk factors for prolongation of the QTc interval (e.g. abnormal QTc interval pre-treatment, electrolyte abnormalities, use of starvation-liquid diets, or history of heart disease). Fluoroquinolone antimicrobials can be used effectively and safely in the vast majority of patients if the clinician remembers those few drug-drug interactions that are clinically-important.

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“…Thus, the modulation of P-gp or CYPs or UGTs may affect the pharma- Curcumin has been demonstrated to down regulate the P-gp levels in rat, 16,26) and the cell-based assay using rhodamine 123 indicated that curcumin significantly inhibited the activity of P-gp with a decrease in P-gp protein and multidrug resistance gene MDR1 mRNA levels. Referring to the studies, 22,27) pretreatment with curcumin could alter the oral bioavailability of docetaxel and norfloxacin, which are substrates of P-gp. Therefore, the improved absorption of losartan caused by inhibition of P-gp is likely to result in higher increased AUC and C max .…”

Section: Discussionmentioning

confidence: 99%

Pre-treatment with Curcumin Enhances Plasma Concentrations of Losartan and Its Metabolite EXP3174 in Rats

Liu

Zhao

Xing

et al. 2012

Biological & Pharmaceutical Bulletin

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The study was carried out in the Wistar rats to investigate the effect of curcumin pre-treatment on the pharmacokinetics of the hypertension-treating drug losartan and its metabolite EXP3174 following single oral administration. In the treatment group, rats were gavaged with losartan 10 mg/kg after repeat oral doses of curcumin (100 mg/kg, for 7 d), while rats in the control group were administrated only with the same dose losartan. The results showed that curcumin significantly increased the plasma concentrations of losartan and its metabolite EXP3174. The present study implicated the existence of herb-drug interaction between curcumin and losartan, and further evaluation of the possible interaction during curcumin administration needs to be considered.

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Modification of pharmacokinetics of norfloxacin following oral administration of curcumin in rabbits

Cited by 37 publications

References 18 publications

Curcumin Pretreatment Decreases Absorption of Phenacetin (Cytochrome P450 1A2 Substrate), Without Altering its Disposition Kinetics in Rats

Curcumin Pretreatment Decreases Absorption of Phenacetin (Cytochrome P450 1A2 Substrate), Without Altering its Disposition Kinetics in Rats

Quinolones

Pre-treatment with Curcumin Enhances Plasma Concentrations of Losartan and Its Metabolite EXP3174 in Rats

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