Premium
Blood to plasma ratio of mefloquine: Interpretation and pharmacokinetic implications
Author(s) -
Tajerzadeh H.,
Cutler D. J.
Publication year - 1993
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510140109
Subject(s) - mefloquine , pharmacokinetics , pharmacology , blood plasma , red blood cell , chemistry , blood proteins , medicine , plasmodium falciparum , biochemistry , malaria , immunology
The blood to plasma ratio of the antimalarial mefloquine has been reported to be close to 1, while other reports indicate extensive accumulation in erythrocytes. This apparent contradiction has been resolved by a quantitative examination of the compensating effects of plasma protein binding of mefloquine which almost exactly matches the extent of mefloquine accumulation in erythrocytes. The observed blood to plasma ratio of about 1 arises as the result of a balance between extensive red cell uptake and extensive plasma protein binding. Some pharmacokinetic implications of the distribution of mefloquine within blood are outlined.