COMPARISON OF THE INFLUENCES OF CHLOROQUINE AND CIMETIDINE ON THE PHARMACOKINETICS OF PARACETAMOL IN HEALTHY HUMAN SUBJECTS

COMPARISON OF THE INFLUENCES OF CHLOROQUINE AND CIMETIDINE ON THE PHARMACOKINETICS OF PARACETAMOL IN HEALTHY HUMAN SUBJECTS

Abstract:

Malaria is very prevalent in the world especially in Africa and chloroquine is still a leading drug in the treatment of this ailment. Patients go to hospital with multiple illnesses, malaria inclusive. Thus other drugs are frequently prescribed with chloroquine. This work is designed to find out the interaction of chloroquine with other drugs with which it is commonly prescribed. This effect is compared with that of cimetidine on paracetamol absorption. Paracetamol (1g) was given orally alone as control (first stage). Cimetidine (400mg) was given concurrently with paracetamol (1g) orally (second stage) and then cimetidine was given orally one and a half hours before paracetamol (third stage). Chloroquine sulphate (0.8g) was given orally one and a half hours before paracetamol (fourth stage). All pharmacokinetic parameters of paracetamol were determined statistically for all the different stages of the study. They were then compared with control and those of chloroquine treated compared with those of cimetidine treated (delayed and concurrent administration). Oral administration of 400mg cimetidine an hour before paracetamol significantly (P<0.05) decreased Cmax, Tmax, T½ab, Kab, T½el, Kel, Lagtime, Clearance. With the concurrent administration, cimetidine insignificantly (P>0.10) decreased all the pharmacokinetic parameters. Chloroquine significantly (P<0.05) decreased Cmax, Tmax, T½ab, Kab, Lagtime. When the influences of Chloroquine (delayed) and cimetidine (delayed) on paracetamol kinetics were compared, only clearance, Cmax and AUCo-oo in chloroquine treated were significantly (P<0.05) decreased, while all other parameters were insignificantly (P<0.10) decreased.

COMPARISON OF THE INFLUENCES OF CHLOROQUINE AND CIMETIDINE ON THE PHARMACOKINETICS OF PARACETAMOL IN HEALTHY HUMAN SUBJECTS