EFFECTS OF FOOD ON THE PHARMACOKINETICS OF AMODIAQUINE IN HEALTHY VOLUNTEERS

SOYINKA J O, ODUNFA O. ADEMISOYE AA

Abstract


Amodiaquine (AQ) is a 4-aminoquinoline derivative which
is intrinsically more active than the other 4-
aminoquinoline, chloroquine, against Plasmodium
falciparum parasites. The pharmacokinetic parameters of
amodiaquine and its active metabolite following the
administration of amodiaquine to healthy volunteers under
fasted conditionS were compared with those when it was
co-administered with food.
In an open, two-way crossover study, 16 healthy
volunteers fasted overnight and were randomized to
receive a single oral administration of 600 mg (3 tablets)
of amodiaquine in the absence or presence of a
standardized high-fat breakfast, administered 30 min
before drug administration. Blood samples were collected
up to 192 h and amodiaquine and desethyl amodiaquine
were assayed by a validated HPLC method.
Relative to the fasting state, the administration of a single
dose of amodiaquine after a high-fat breakfast resulted in
delayed median Tmax values (20 min for amodiaquine and
3 h for desethylamodiaquine). The geometric mean ratios
(GMR) of fed to fasting conditions indicated increased
Cmax values for amodiaquine (GMR 1.40) (90% CI: 1.12-
1.48) and desethylamodiaquine (GMR 1.48) (90% CI: 1.09-
1.52) and increased AUC0-t values for amodiaquine (GMR
1.62) (90% CI: 1.42-1.86) and for desethylamodiaquine
(GMR 1.26) (90% CI: 1.12-1.36).
Intake of AQ with a high fat meal resulted in a statistically
significant increase in blood levels of amodiaquine and
desethylamodiaquine which may affect its safety and
tolerability. The findings of this study suggest that
amodiaquine should not be administered with a high-fat
meal.


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