Human plasma and urine quinine levels following tablets, capsules, and intravenous infusion

Hall, Anthony; Czerwinski, Anthony W.; Madonia, Eugene C.; Evensen, Kenneth

doi:10.1002/cpt1973144part1580

Cited by 36 publications

(12 citation statements)

References 5 publications

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“…Quinine is metabolized primarily via the cytochrome P450 enzyme CYP3A4, and the more polar metabolites are eliminated mainly by renal excretion (13)(14)(15). The major metabolite, 3-hydroxyquinine, contributes approximately 10% of the antimalarial activity of the parent compound (16).…”

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confidence: 99%

Population Pharmacokinetic and Pharmacodynamic Properties of Intramuscular Quinine in Tanzanian Children with Severe Falciparum Malaria

Hendriksen

Maiga

Lemnge

et al. 2013

Antimicrob Agents Chemother

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f Although artesunate is clearly superior, parenteral quinine is still used widely for the treatment of severe malaria. A loading-dose regimen has been recommended for 30 years but is still often not used. A population pharmacokinetic study was conducted with 75 Tanzanian children aged 4 months to 8 years with severe malaria who received quinine intramuscularly; 69 patients received a loading dose of 20 mg quinine dihydrochloride (salt)/kg of body weight. Twenty-one patients had plasma quinine concentrations detectable at baseline. A zero-order absorption model with one-compartment disposition pharmacokinetics described the data adequately. Body weight was the only significant covariate and was implemented as an allometric function on clearance and volume parameters. Population pharmacokinetic parameter estimates (and percent relative standard errors [%RSE]) of elimination clearance, central volume of distribution, and duration of zero-order absorption were 0.977 liters/h (6.50%), 16.7 liters (6.39%), and 1.42 h (21.5%), respectively, for a typical patient weighing 11 kg. Quinine exposure was reduced at lower body weights after standard weight-based dosing; there was 18% less exposure over 24 h in patients weighing 5 kg than in those weighing 25 kg. Maximum plasma concentrations after the loading dose were unaffected by body weight. There was no evidence of dose-related drug toxicity with the loading dosing regimen. Intramuscular quinine is rapidly and reliably absorbed in children with severe falciparum malaria. Based on these pharmacokinetic data, a loading dose of 20 mg salt/kg is recommended, provided that no loading dose was administered within 24 h and no routine dose was administered within 12 h of admission. (This study has been registered with Current Controlled Trials under registration number ISRCTN 50258054.)

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confidence: 99%

Population Pharmacokinetic and Pharmacodynamic Properties of Intramuscular Quinine in Tanzanian Children with Severe Falciparum Malaria

Hendriksen

Maiga

Lemnge

et al. 2013

Antimicrob Agents Chemother

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“…Bioavailability of the sulphate salt is of the order of 80-90% [22]. In the present study, 600 mg quinine sulphate was given postprandially to previously untreated subjects in an attempt to reproduce a common clinical situation in which the pharmacokinetic and pharmacodynamic properties of quinine could best be studied.…”

Section: Discussionmentioning

confidence: 99%

The pharmacokinetics and pharmacodynamics of quinine in the diabetic and non‐diabetic elderly.

Dyer

Davis

Giele

et al. 1994

Brit J Clinical Pharma

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1 Quinine is a front-line antimalarial drug but is prescribed most commonly in nonmalarious countries for cramps. Postural hypotension, hearing loss and hyperinsulinaemic hypoglycaemia occur in malaria and overdose but little is known of quinine kinetics and toxicity in the elderly. 2 We studied 12 non-insulin-dependent diabetics and 10 non-diabetic controls aged 51-79 years. Subjects attended on two occasions >7 days apart. On each test day, subjects were given a 600 Cal meal at 18.00 h (0 h) and, on one occasion, quinine sulphate 600 mg at 22.00 h (4 h). Venous blood samples for glucose, insulin and quinine assay were drawn pre-prandially and then regularly over the next 38 h. Supine and erect blood pressures were taken and audiometry was performed at 4, 6, 8 and 14 h. A one-compartment open pharmacokinetic model was fitted to serum quinine concentrations. 3 Absorption and elimination half-times, volume of distribution and oral clearance of quinine were comparable in the two groups (P > 0.2) and there was a mean absorption lag-time of approximately 1 h. Basal and immediate post-prandial (< 4 h) serum glucose and insulin concentrations on both test days were similar in the diabetics and also in the non-diabetics, but quinine produced a mean reduction in serum glucose of 1.0 mmol 1-1 from 3-5 h post-dose in both groups without affecting serum insulin concentrations. Quinine administration did not alter postural blood pressure changes or produce significant hearing loss in either group. 4 These data suggest that a nocturnal post-prandial dose of quinine lowers early morning plasma glucose concentrations in both non-diabetic and diabetic subjects. Other potentially significant toxic effects in elderly patients were not observed.

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“…Oral and intramuscular bioavailability exceed 80% (Hall et al 1973). The decline in plasma concentrations following intravenous administration is biexponential (White et al 1983a).…”

Section: Quininementioning

confidence: 99%

Antiparasitic Drugs in Children

White

1989

Clinical Pharmacokinetics

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Many of the children living in tropical areas of the world are infected by a variety of human parasites. As a group, the antiparasitic drugs can claim to be the least studied of all compounds in current clinical use. There is little information on the disposition of these drugs in children, and most treatment recommendations are either empirical or by extrapolationjrom observations in adults. Many of the older drugs used in systemic parasitic infections have narrow therapeutic ratios and could be better used if treatment regimens were based on detailed pharmacokinetic and pharmacodynamic information. This review summarises existing information on these drugs and suggests provisional recommendations for antiparasitic treatment.

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Human plasma and urine quinine levels following tablets, capsules, and intravenous infusion

Cited by 36 publications

References 5 publications

Population Pharmacokinetic and Pharmacodynamic Properties of Intramuscular Quinine in Tanzanian Children with Severe Falciparum Malaria

Population Pharmacokinetic and Pharmacodynamic Properties of Intramuscular Quinine in Tanzanian Children with Severe Falciparum Malaria

The pharmacokinetics and pharmacodynamics of quinine in the diabetic and non‐diabetic elderly.

Antiparasitic Drugs in Children

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