Effect of chloroquine and primaquine on antipyrine metabolism.

Back, DJ; Purba, HS; Park, BK; Ward, SA; Orme, ML

doi:10.1111/j.1365-2125.1983.tb02206.x

Cited by 49 publications

(17 citation statements)

References 21 publications

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“…It has been shown previously that PQ (45 mg) inhibits the metabolism of antipyrine in man (Back et al, 1983a), as seen by an increase in the half-life of antipyrine elimination, and by a decrease in the clearance to metabolites following PQ administration. In contrast to this finding, CQ (250 mg) was found to have no significant effect on antipyrine metabolism in man.…”

Section: -Bis(trifluoromethyl)-4-quinolinemethanoli Is a New Antimalmentioning

confidence: 88%

The pharmacokinetics of mefloquine in man: lack of effect of mefloquine on antipyrine metabolism.

Riviere¹,

Back²,

Breckenridge³

et al. 1985

Brit J Clinical Pharma

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1 A method is described for the determination of the new antimalarial agent, mefloquine, in plasma and urine. 2 After oral administration of 750 mg mefloquine to six volunteers, absorption was apparently slow, with plasma mefloquine concentrations at 24 h (559 + 181 ng ml-1; mean + s.d.) higher than at 6 h (459 + 166 ng ml-1). The elimination half-life was 373 + 249 h, oral clearance was 5.09 + 2.71 h-1, and apparent volume of distribution was 35.7 ± 30.71 kg-1 (assuming 100% bioavailability). 3 Mefloquine (750 mg) had no significant effect on salivary kinetics of antipyrine or on the metabolic clearance of antipyrine to its three main metabolites, 3-hydroxymethylantipyrine, 4-hydroxyantipyrine and norantipyrine, when antipyrine was administered either 2 h or 2 weeks after dosing with mefloquine.

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Section: -Bis(trifluoromethyl)-4-quinolinemethanoli Is a New Antimalmentioning

confidence: 88%

The pharmacokinetics of mefloquine in man: lack of effect of mefloquine on antipyrine metabolism.

Riviere¹,

Back²,

Breckenridge³

et al. 1985

Brit J Clinical Pharma

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“…It has recently been shown that primaquine is a potent inhibitor of mixed function oxidase (M.F.O.) activity in both animals and man (Back et al, 1983a(Back et al, 1983bMihaly et al, 1985b).…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of primaquine in man. II. Comparison of acute vs chronic dosage in Thai subjects.

Ward¹,

Mihaly²,

Edwards³

et al. 1985

Brit J Clinical Pharma

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3 Repeated dosing with primaquine had no effect on the mean pharmacokinetic parameters calculated for this drug. In contrast, individual pharmacokinetic parameters for some subjects exhibited gross and unpredictable changes after chronic dosage. 4 The carboxylic acid metabolite of primaquine accumulated in plasma after repeated dosing such that by day 14 of chronic dosing the mean AUC (0,24) for this metabolite was 74% greater than that obtained after acute administration of primaquine.

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“…The propensity of most antimalarial drugs to inhibit hepatic drug metabolizing enzymes had previously been reported in various studies (Back et al, 1983a;Back et al, 1983b;Mihaly et al, 1985;Riviere and Back, 1985;Na-Bangchang et al, 1992). Clinically relevant drug interaction was of a great concern when PQ is to be given concurrently with other antimalarial drugs.…”

Section: Referencementioning

confidence: 95%

“…The propensitity of such pharmacokinetic interaction has been raised when PQ is given at repeated dosing (auto-inhibition of hepatic drug metabolism) as well as in combination with other antimalarial drugs as a tissue schizontocide or gametocytocide. Previous studies demonstrated the potential of PQ as a potent inhibitor of cytochrome P450 in both animals and humans (Back et al, 1983a;Back et al, 1983b;Mihaly et al, 1985;Na-Bangchang et al, 1992). It is thought that the synergistic effects on radical curative activity between PQ and the standard blood schizontocidal antimalarial drugs CQ and quinine (Alving et al, 1980) could be linked to these pharmacokinetic drug interactions (cytochrome P450 inhibition) which result in elevated plasma concentrations of both CQ and quinine.…”

Section: General Pharmacokinetic Propertiesmentioning

confidence: 99%

“…Clinically relevant drug interaction was of a great concern when PQ is to be given concurrently with other antimalarial drugs. Moreover, malaria infection was also reported to alter hepatic drug metabolism and pharmacokinetics of several antimalarial drugs both in vitro and in vivo (Back et al, 1983b;Mansor et al, 1990;Edwards et al, 1993). The issues of pharmacokinetic drug interactions between PQ and the concurrently administered antimalarial drugs and influence of malaria infection on the pharmacokinetics of PQ were clarified in the following four studies conducted in Thai subjects (Edwards et al, 1993;Mansor et al, 1990;Hanboonkunupakarn et al, 2014;Jittamala et al, 2015).…”

Section: Referencementioning

confidence: 99%

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A review of clinical pharmacokinetics of chloroquine and primaquine and their application in malaria treatment in Thai population

Chukanchitipat¹,

Na‐Bangchang²

2017

Afr. J. Pharm. Pharmacol.

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The blood schizontocidal chloroquine (CQ) and the tissue schizontocidal and gametocytocidal primaquine (PQ) remain the mainstay treatment of Plasmodium vivax and Plasmodium ovale infections for more than six decades. The review focuses on the clinical pharmacokinetic studies of both drugs in Thai population that have provided useful information for clinical application in the treatment of malaria. There appears to be no major differences in the pharmacokinetics of both drugs with respect to the influences of ethinicity, acute phase malaria infection, and G6PD status. The increase in systemic exposure of CQ and/or its metabolite mono-desethylchlorooquine (DECQ) following oral administration could be due to change in the absorption kinetics during acute phase infection. The high clinical efficacy of CQ for treatment of P. vivax infection in Thailand supports this benefitial pharmacokinetic change. Transiently high and toxic plasma/whole blood concentrations of CQ following intravenous infusion at high rate is explained by the pharmacokinetic characteristics of CQ. Pharmacokinetics of PQ following repeated dosing in most studies appears to be similar to that following a single dosing. This suggests that auto-inhibition of PQ metabolism during multiple dosing is unlikely. Coadministration of CQ, dihydroartemisinin-piperaquine (DHA-PIP), and pyronaridine-artesunate (PYR-ARS) significantly altered the pharmacokinetics of PQ. In the presence of these drugs, PQ exposure was significantly increased. The apparent volume of distribution of PQ was reduced when coadministered with PYR-ARS. In addition, plasma concentrations of CPQ were significantly increased in the presence of CQ. Clinical relevance of these interactions needs to be confirmed.

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Effect of chloroquine and primaquine on antipyrine metabolism.

Cited by 49 publications

References 21 publications

The pharmacokinetics of mefloquine in man: lack of effect of mefloquine on antipyrine metabolism.

The pharmacokinetics of mefloquine in man: lack of effect of mefloquine on antipyrine metabolism.

Pharmacokinetics of primaquine in man. II. Comparison of acute vs chronic dosage in Thai subjects.

A review of clinical pharmacokinetics of chloroquine and primaquine and their application in malaria treatment in Thai population

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