Chloroquine reduces urinary excretion of cloxacillin when it is administered concurrently with ampicillin-cloxacillin combination

Babalola, Chinedum P.; Fashedemi, Titilayo T.; Olaniyi, Ajibola A.

doi:10.4314/tjpr.v2i1.14582

Cited by 2 publications

(8 citation statements)

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“…The pattern of results obtained and the half-life values in this study correlate with in vivo reports in earlier studies [ 4 – 6 ].…”

Section: Discussionsupporting

confidence: 91%

“…The possible effect of chloroquine on the urinary excretion of cloxacillin when co-administered with ampicillin–cloxacillin was also investigated earlier in eight healthy adult volunteers [ 6 ]. A significant reduction (64 %) in the urinary excretion of cloxacillin was reported.…”

Section: Discussionmentioning

confidence: 99%

“…Additionally, the effect of oral co-administration of proguanil with cloxacillin was also evaluated in seven healthy adult volunteers. A 48 % decrease in both rate and extent of absorption of cloxacillin was reported [ 6 ]. A recent study reported a reduction in the mean amount of cloxacillin excreted in urine following the co-administration of artesunate with amoxicillin–cloxacillin [ 7 ].…”

Section: Discussionmentioning

confidence: 99%

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Significant Pharmacokinetic Interactions Between Quinine and Ampicillin–Cloxacillin Combination

et al. 2016

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IntroductionThe co-existence of malaria with bacterial infections is common in the tropics, hence the concurrent use of antimalarials and antibiotics.ObjectiveThis study aimed to investigate the effect on pharmacokinetics and antimicrobial activity of co-administration of quinine and combined ampicillin–cloxacillin.MethodsIn total, 14 healthy adults received single oral doses of ampicillin–cloxacillin combination alone and with quinine in a randomized crossover manner. Urine samples collected at predetermined intervals over 48 h were analysed. The effect of quinine on minimum inhibitory concentrations (MICs) of ampicillin and cloxacillin were determined against Staphylococcus aureus by agar diffusion, agar dilution, and broth dilution.ResultsQuinine significantly reduced the rate and extent of excretion of ampicillin and cloxacillin (p < 0.0002). The total amounts of ampicillin and cloxacillin excreted unchanged (Du∞) alone were 217.10 ± 53.82 and 199.0 ± 64.29 mg versus 126.40 ± 50.63 and 135.20 ± 52.24 mg, respectively, with quinine. Respective maximum excretion rates (dDu/dtmax) for ampicillin and cloxacillin were 43.55 ± 19.41 and 77.64 ± 29.65 mg/h alone versus 18.01 ± 8.52 and 53.16 ± 20.72 mg/h with quinine. This indicates a significant reduction in Du∞and dDu/dtmax by 41.78 and 58.65 % for ampicillin and 32.06 and 31.53 % for cloxacillin. Conversely, the disposition of quinine was unaffected by ampicillin–cloxacillin (p > 0.1). The MIC of antibiotics alone versus with quinine, respectively, were 0.11 ± 0.04 and 0.78 ± 0.1 µg/ml for ampicillin, and 0.18 ± 0.1 and 0.92 ± 0.4 µg/ml for cloxacillin, with a five- to sevenfold increase (p > 0.01); indicating a decrease in antimicrobial activity by quinine.Conclusions Quinine therefore, reduced the bioavailability and the antimicrobial activity of ampicillin–cloxacillin upon co-administration, which may have therapeutic implications. Caution is required with the co-administration of these medicines.

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“…The pattern of results obtained and the half-life values in this study correlate with in vivo reports in earlier studies [ 4 – 6 ].…”

Section: Discussionsupporting

confidence: 91%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Significant Pharmacokinetic Interactions Between Quinine and Ampicillin–Cloxacillin Combination

et al. 2016

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“…The nature of interactions between antimalarials, particularly those belonging to the quinoline class, and antibiotics has been studied extensively in the past two decades (Babalola et al, 2002(Babalola et al, , 2003(Babalola et al, , 2009Abreu et al, 2014;Falade et al, 2016). Malaria is immunosuppressive.…”

Section: Introductionmentioning

confidence: 99%

“…For instance, penicillin antibiotics have been reported to demonstrate in vivo and in vitro interactions with certain antimalarial agents (Babalola et al, 2003(Babalola et al, , 2009Falade et al, 2016). Documented interactions include reduction in bioavailability of penicillins (ampicillin and cloxacillin) by 40-70 % after oral co-administration with quinine and chloroquine in healthy patients (Ali, 1985;Babalola et al, 2003;Falade et al, 2016). Other studies reported similar interactions with proguanil and artesunate (Babalola et al, 2002(Babalola et al, , 2009, suggesting that pharmacokinetic drug interaction is likely occurring at the absorption phase (Palleria et al, 2013).…”

Section: Introductionmentioning

confidence: 99%

Quinoline Antimalarials Increase the Antibacterial Activity of Ampicillin

et al. 2021

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Bacterial and malaria co-infections are common in malaria endemic countries and thus necessitate co-administration of antibiotics and antimalarials. There have long been anecdotal clinical reports of interactions between penicillins and antimalarial agents, but the nature and mechanisms of these interactions remain to be investigated. In this study, we employed antimicrobial interaction testing methods to study the effect of two antimalarials on the antibacterial activity of ampicillin in vitro. Paper strip diffusion, a modified disc diffusion and checkerboard methods were used to determine the nature of interactions between ampicillin and quinoline antimalarials, chloroquine and quinine, against Gram-positive and Gram-negative bacteria. The impact of antimalarials and ampicillin-antimalarial drug combinations on cell integrity of test bacteria were determined by measuring potassium release. The tested antimalarials did not show substantial antibacterial activity but quinine was bactericidal at high concentrations. Chloroquine and quinine increased ampicillin activity, with increasing concentrations extending the antibacterial’s inhibition zones by 2.7-4.4 mm and from 1.1 to over 60 mm, respectively. Observed interactions were largely additive with Fractional Inhibitory Concentration Indices of >0.5-1 for all ampicillin-antimalarial combinations. Quinine and, to a lesser extent, chloroquine increase the activity of ampicillin and potentially other β-lactams, which has implications for combined clinical use.

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Chloroquine reduces urinary excretion of cloxacillin when it is administered concurrently with ampicillin-cloxacillin combination

Abstract: Purpose: To investigate a possible effect of chloroquine on urinary excretion of cloxacillin when chloroquine is administered concurrently with ampicillin-cloxacillin combination. Methods

Cited by 2 publications

References 10 publications

Significant Pharmacokinetic Interactions Between Quinine and Ampicillin–Cloxacillin Combination

Significant Pharmacokinetic Interactions Between Quinine and Ampicillin–Cloxacillin Combination

Quinoline Antimalarials Increase the Antibacterial Activity of Ampicillin

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