Human pharmacokinetics of proguanil and its metabolites

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Standard

Human pharmacokinetics of proguanil and its metabolites. / Bygbjerg, Ib Christian; Ravn, P; Rønn, A; Flachs, H; Hvidberg, E F.

I: Tropical Medicine and Parasitology, Bind 38, Nr. 2, 01.06.1987, s. 77-80.

Publikation: Bidrag til tidsskrift › Tidsskriftartikel › Forskning › fagfællebedømt

Harvard

Bygbjerg, IC, Ravn, P, Rønn, A, Flachs, H & Hvidberg, EF 1987, 'Human pharmacokinetics of proguanil and its metabolites', Tropical Medicine and Parasitology, bind 38, nr. 2, s. 77-80.

APA

Bygbjerg, I. C., Ravn, P., Rønn, A., Flachs, H., & Hvidberg, E. F. (1987). Human pharmacokinetics of proguanil and its metabolites. Tropical Medicine and Parasitology, 38(2), 77-80.

Vancouver

Bygbjerg IC, Ravn P, Rønn A, Flachs H, Hvidberg EF. Human pharmacokinetics of proguanil and its metabolites. Tropical Medicine and Parasitology. 1987 jun. 1;38(2):77-80.

Author

Bygbjerg, Ib Christian ; Ravn, P ; Rønn, A ; Flachs, H ; Hvidberg, E F. / Human pharmacokinetics of proguanil and its metabolites. I: Tropical Medicine and Parasitology. 1987 ; Bind 38, Nr. 2. s. 77-80.

Bibtex

@article{9b7ee6372b48492bbb765c3630e8c2fe,
title = "Human pharmacokinetics of proguanil and its metabolites",
abstract = "The pharmacokinetics of proguanil and its metabolites cycloguanil and p-chlorophenylbiguanide were studied in five healthy volunteers taking 200 mg orally for 14 days. A highly sensitive and specific high-performance liquid chromatographic assay was applied, clearly identifying all three compounds in plasma extracts as separate peaks. In four subjects peak plasma concentrations of proguanil (500 to 600 nmol/l) were reached after two to three hours, while cycloguanil and p-chlorophenylbiguanide showed a plateau after three and six hours, respectively. In the fifth subject peak concentrations of proguanil and cycloguanil appeared after seven hours. Trough concentrations (pre-dose in the morning) of proguanil and cycloguanil were about 200 and 100 nmol/l, respectively. Mean half-life of proguanil was estimated to approximately 20 h. The active metabolite cycloguanil constituted 30% of the total plasma drug concentration. The concentration of proguanil was higher in erythrocytes than in plasma, while that of cycloguanil was lower. Relevant clinical studies correlating plasma concentrations to the suppressive activity against malaria will be possible to perform based on the applied method and presented kinetic data.",
keywords = "Adult, Biguanides, Chemical Phenomena, Chemistry, Chromatography, High Pressure Liquid, Erythrocytes, Female, Half-Life, Humans, Kinetics, Male, Proguanil, Triazines",
author = "Bygbjerg, {Ib Christian} and P Ravn and A R{\o}nn and H Flachs and Hvidberg, {E F}",
year = "1987",
month = jun,
day = "1",
language = "English",
volume = "38",
pages = "77--80",
journal = "Tropical Medicine and Parasitology",
issn = "0177-2392",
publisher = "Wiley-Blackwell",
number = "2",

}

RIS

TY - JOUR

T1 - Human pharmacokinetics of proguanil and its metabolites

AU - Bygbjerg, Ib Christian

AU - Ravn, P

AU - Rønn, A

AU - Flachs, H

AU - Hvidberg, E F

PY - 1987/6/1

Y1 - 1987/6/1

N2 - The pharmacokinetics of proguanil and its metabolites cycloguanil and p-chlorophenylbiguanide were studied in five healthy volunteers taking 200 mg orally for 14 days. A highly sensitive and specific high-performance liquid chromatographic assay was applied, clearly identifying all three compounds in plasma extracts as separate peaks. In four subjects peak plasma concentrations of proguanil (500 to 600 nmol/l) were reached after two to three hours, while cycloguanil and p-chlorophenylbiguanide showed a plateau after three and six hours, respectively. In the fifth subject peak concentrations of proguanil and cycloguanil appeared after seven hours. Trough concentrations (pre-dose in the morning) of proguanil and cycloguanil were about 200 and 100 nmol/l, respectively. Mean half-life of proguanil was estimated to approximately 20 h. The active metabolite cycloguanil constituted 30% of the total plasma drug concentration. The concentration of proguanil was higher in erythrocytes than in plasma, while that of cycloguanil was lower. Relevant clinical studies correlating plasma concentrations to the suppressive activity against malaria will be possible to perform based on the applied method and presented kinetic data.

AB - The pharmacokinetics of proguanil and its metabolites cycloguanil and p-chlorophenylbiguanide were studied in five healthy volunteers taking 200 mg orally for 14 days. A highly sensitive and specific high-performance liquid chromatographic assay was applied, clearly identifying all three compounds in plasma extracts as separate peaks. In four subjects peak plasma concentrations of proguanil (500 to 600 nmol/l) were reached after two to three hours, while cycloguanil and p-chlorophenylbiguanide showed a plateau after three and six hours, respectively. In the fifth subject peak concentrations of proguanil and cycloguanil appeared after seven hours. Trough concentrations (pre-dose in the morning) of proguanil and cycloguanil were about 200 and 100 nmol/l, respectively. Mean half-life of proguanil was estimated to approximately 20 h. The active metabolite cycloguanil constituted 30% of the total plasma drug concentration. The concentration of proguanil was higher in erythrocytes than in plasma, while that of cycloguanil was lower. Relevant clinical studies correlating plasma concentrations to the suppressive activity against malaria will be possible to perform based on the applied method and presented kinetic data.

KW - Adult

KW - Biguanides

KW - Chemical Phenomena

KW - Chemistry

KW - Chromatography, High Pressure Liquid

KW - Erythrocytes

KW - Female

KW - Half-Life

KW - Humans

KW - Kinetics

KW - Male

KW - Proguanil

KW - Triazines

M3 - Journal article

C2 - 3629140

VL - 38

SP - 77

EP - 80

JO - Tropical Medicine and Parasitology

JF - Tropical Medicine and Parasitology

SN - 0177-2392

IS - 2

ER -

ID: 33891665