Disposition of the Antimalarial, Mefloquine, in the Isolated Perfused Rat Liver

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Abstract:

Mefloquine is a relatively new antimalarial compound that is highly effective against chloroquine-resistant Plasmodium falciparum malaria. The pharmacokinetics of mefloquine have been studied in dogs 1, rats 2 and humans 1, 3-6. Mefloquine exhibits a large volume of distribution, is concentrated in soft tissues, is metabolized slowly, and undergoes considerable biliary excretion in vivo 1-3. Mefloquine also inhibits hepatic metabolism of aminopyrine in vitro in rat microsomes 7. Therefore, to investigate more fully the hepatic handling of mefloquine, we have chosen the isolated perfused rat liver IPRL preparation. This experimental model excludes the influence of other organs and routes of elimination present in the intact animal and has been of value in studies of the disposition of a number of compounds, e.g. cimetidine, propranolol, suramin and the antimalarial primaquine 8-11. Reprints.

Author(s):
Coleman, Michael D. ; Fleckenstein, Lawrence ; Shipley, Lisa A. ; Heiffer, Melvin H.
Author Organization(s):
WALTER REED ARMY INST OF RESEARCH WASHINGTON DC
Descriptive Note:
Manuscript rept.
Supplementary Note:
Pub. in Biochemical Pharmacology, v37 n2 p235-239 1988.
Pagination:
0006

Security Markings

DOCUMENT & CONTEXTUAL SUMMARY

Distribution:
Approved For Public Release
Distribution Statement:
Approved For Public Release; Distribution Is Unlimited.

RECORD

Collection: TR
Identifying Numbers
Monitor Series:
WRAIR
 Subject Terms
Joint Capability Areas:
JCA_5_Command and Control; JCA_4.2_Supply; JCA_5.3_Planning; JCA_4.2.2_Inventory Management; JCA_1.2.5_Lessons Learned; JCA_1.2.7_Experimentation; JCA_1_Force Support; JCA_5.5_Direct
Communities of Interest:
Biomedical
Descriptor(s):
*PHARMACOKINETICS, *RATS, *LIVER, *ANTIMALARIALS, *PLASMODIUM FALCIPARUM, MALARIA, HANDLING, ORGANS(ANATOMY), RESISTANCE(BIOLOGY), SOFT TISSUES, METABOLISM, DISTRIBUTION, MODELS, CHLOROQUINE, REPRINTS, VOLUME
Field(s)/Group(s):
Pharmacology
Keyword(s):
*MEFLOQUINE
Report Date:
1987 Jan 01