Absolute bioavailability of quinine formulations in Nigeria.

This study compared the absolute bioavailability of quinine sulphate as capsule and as tablet against the intravenous (i.v.) infusion of the drug in twelve male volunteers.

Evidence for increased metabolism of chloroquine during the early third trimester of human pregnancy.

Objective: To examine the possibility of a different extent of chloroquine (CQ) metabolism in human pregnancy by determining blood level profiles of the drug and its major metabolite, desethylchloroquine (CQM).

Methods: Five women in the early third trimester of pregnancy and five non-pregnant women received each a single 600 mg oral dose of CQ and blood samples were collected at pre-determined intervals following drug administration. Plasma concentrations of CQ and CQM were analysed by an established HPLC method.

Polymorphic oxidative metabolism of proguanil in a Nigerian population.

Objective: The genetic polymorphic metabolic oxidation of proguanil was investigated in 126 healthy, unrelated Nigerian subjects as an indication of the phenotypic status of CYP2C19 in Nigerians.

Methods: The proguanil oxidation capacity was determined using the 8-h urinary metabolic ratio of the parent drug and its metabolite (cycloguanil) after a single oral dose of 200 mg proguanil.

Results: The frequency distribution of the proguanil metabolic ratio ranged from 0.

Pharmacokinetic aspects of chloroquine-induced pruritus: influence of dose and evidence for varied extent of metabolism of the drug.

The significance of a pharmacokinetics basis in chloroquine (CQ)-induced pruritus was investigated by determining the disposition of the drug in two groups of volunteers; pruritus positive and pruritus negative. Single oral dose of 600 mg CQ was administered to each of 36 volunteers, 18 for each of the two groups. After a washout period of 9 months, 150 mg single oral dose of the drug was given to 12 of the same volunteers, six each from the two groups.

Pharmacokinetics of quinine in African patients with acute falciparum malaria.

The pharmacokinetics of quinine were studied in six Nigerian patients during acute uncomplicated falciparum malaria and convalescent periods. An oral dose of 10 mg/kg quinine dihydrochloride administered 8-hourly for 7 days gave parasite and fever clearance times of 36.0 +/- 16.