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Plasma, erythrocyte and urine concentrations of chlorproguanil and two metabolites in man after different doses

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Standard

Plasma, erythrocyte and urine concentrations of chlorproguanil and two metabolites in man after different doses. / Petersen, E; Flachs, H; Høgh, B; Hanson, A P; Björkman, A; Hvidberg, E F.

I: American Journal of Tropical Medicine and Hygiene, Bind 94, Nr. 3, 06.1991, s. 199-205.

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

Harvard

Petersen, E, Flachs, H, Høgh, B, Hanson, AP, Björkman, A & Hvidberg, EF 1991, 'Plasma, erythrocyte and urine concentrations of chlorproguanil and two metabolites in man after different doses', American Journal of Tropical Medicine and Hygiene, bind 94, nr. 3, s. 199-205.

APA

Petersen, E., Flachs, H., Høgh, B., Hanson, A. P., Björkman, A., & Hvidberg, E. F. (1991). Plasma, erythrocyte and urine concentrations of chlorproguanil and two metabolites in man after different doses. American Journal of Tropical Medicine and Hygiene, 94(3), 199-205.

Vancouver

Petersen E, Flachs H, Høgh B, Hanson AP, Björkman A, Hvidberg EF. Plasma, erythrocyte and urine concentrations of chlorproguanil and two metabolites in man after different doses. American Journal of Tropical Medicine and Hygiene. 1991 jun;94(3):199-205.

Author

Petersen, E ; Flachs, H ; Høgh, B ; Hanson, A P ; Björkman, A ; Hvidberg, E F. / Plasma, erythrocyte and urine concentrations of chlorproguanil and two metabolites in man after different doses. I: American Journal of Tropical Medicine and Hygiene. 1991 ; Bind 94, Nr. 3. s. 199-205.

Bibtex

@article{f0355a91704344fba5d6f1c74ea19c6f,
title = "Plasma, erythrocyte and urine concentrations of chlorproguanil and two metabolites in man after different doses",
abstract = "Failures in the prophylactic effect of the antimalarial biguanide chlorproguanil (Lapudrine) may be caused by insufficient levels of its active metabolite chlorcycloguanil. Concentrations of chlorproguanil, chlorcycloguanil and a second metabolite, dichlorophenylbiguanide, in plasma, erythrocytes and urine, were followed in 13 volunteers, using a HPLC assay. In an initial study the basic kinetics were investigated after an oral dose of 2 mg kg-1. In the main study, the concentration-time curves were followed for 1 week after an oral dose of 20 or 80 mg chlorproguanil, respectively, after either a single dose or one weekly dose for 5 weeks. Higher concentrations of all three compounds were found in erythrocytes than in plasma. The active substance, chlorcycloguanil, was below the probably effective concentration in erythrocytes 24 h after 20 mg chlorproguanil and 72 h after 80 mg. The urinary recovery was about 45% of the dose and t1/2 31-44 h, both higher than previously reported. The apparent clearance was 0.52-0.82 l h-1 kg-1, which is lower than previously found. It is suggested that improved dose regimens, e.g. a higher dose given once a week, should be clinically tested on basis of these kinetic results.",
keywords = "Adult, Aged, Antimalarials/blood, Chromatography, High Pressure Liquid, Erythrocytes/chemistry, Female, Humans, Male, Middle Aged, Proguanil/administration & dosage, Triazines/blood",
author = "E Petersen and H Flachs and B H{\o}gh and Hanson, {A P} and A Bj{\"o}rkman and Hvidberg, {E F}",
year = "1991",
month = jun,
language = "English",
volume = "94",
pages = "199--205",
journal = "American Journal of Tropical Medicine and Hygiene",
issn = "0002-9637",
publisher = "American Society of Tropical Medicine and Hygiene",
number = "3",

}

RIS

TY - JOUR

T1 - Plasma, erythrocyte and urine concentrations of chlorproguanil and two metabolites in man after different doses

AU - Petersen, E

AU - Flachs, H

AU - Høgh, B

AU - Hanson, A P

AU - Björkman, A

AU - Hvidberg, E F

PY - 1991/6

Y1 - 1991/6

N2 - Failures in the prophylactic effect of the antimalarial biguanide chlorproguanil (Lapudrine) may be caused by insufficient levels of its active metabolite chlorcycloguanil. Concentrations of chlorproguanil, chlorcycloguanil and a second metabolite, dichlorophenylbiguanide, in plasma, erythrocytes and urine, were followed in 13 volunteers, using a HPLC assay. In an initial study the basic kinetics were investigated after an oral dose of 2 mg kg-1. In the main study, the concentration-time curves were followed for 1 week after an oral dose of 20 or 80 mg chlorproguanil, respectively, after either a single dose or one weekly dose for 5 weeks. Higher concentrations of all three compounds were found in erythrocytes than in plasma. The active substance, chlorcycloguanil, was below the probably effective concentration in erythrocytes 24 h after 20 mg chlorproguanil and 72 h after 80 mg. The urinary recovery was about 45% of the dose and t1/2 31-44 h, both higher than previously reported. The apparent clearance was 0.52-0.82 l h-1 kg-1, which is lower than previously found. It is suggested that improved dose regimens, e.g. a higher dose given once a week, should be clinically tested on basis of these kinetic results.

AB - Failures in the prophylactic effect of the antimalarial biguanide chlorproguanil (Lapudrine) may be caused by insufficient levels of its active metabolite chlorcycloguanil. Concentrations of chlorproguanil, chlorcycloguanil and a second metabolite, dichlorophenylbiguanide, in plasma, erythrocytes and urine, were followed in 13 volunteers, using a HPLC assay. In an initial study the basic kinetics were investigated after an oral dose of 2 mg kg-1. In the main study, the concentration-time curves were followed for 1 week after an oral dose of 20 or 80 mg chlorproguanil, respectively, after either a single dose or one weekly dose for 5 weeks. Higher concentrations of all three compounds were found in erythrocytes than in plasma. The active substance, chlorcycloguanil, was below the probably effective concentration in erythrocytes 24 h after 20 mg chlorproguanil and 72 h after 80 mg. The urinary recovery was about 45% of the dose and t1/2 31-44 h, both higher than previously reported. The apparent clearance was 0.52-0.82 l h-1 kg-1, which is lower than previously found. It is suggested that improved dose regimens, e.g. a higher dose given once a week, should be clinically tested on basis of these kinetic results.

KW - Adult

KW - Aged

KW - Antimalarials/blood

KW - Chromatography, High Pressure Liquid

KW - Erythrocytes/chemistry

KW - Female

KW - Humans

KW - Male

KW - Middle Aged

KW - Proguanil/administration & dosage

KW - Triazines/blood

M3 - Journal article

C2 - 2051526

VL - 94

SP - 199

EP - 205

JO - American Journal of Tropical Medicine and Hygiene

JF - American Journal of Tropical Medicine and Hygiene

SN - 0002-9637

IS - 3

ER -

ID: 203011961