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. 1983 Nov;16(5):497–502. doi: 10.1111/j.1365-2125.1983.tb02206.x

Effect of chloroquine and primaquine on antipyrine metabolism.

D J Back, H S Purba, B K Park, S A Ward, M L Orme
PMCID: PMC1428067  PMID: 6639836

Abstract

The effects of two antimalarial drugs, chloroquine and primaquine on antipyrine kinetics and metabolism have been studied in volunteers. Chloroquine (250 mg) given 2 h before antipyrine (600 mg orally) had no effect on salivary kinetics of antipyrine or on the urinary recovery of metabolites. Primaquine (45 mg) given 2 h before antipyrine (300 mg orally), increased antipyrine half-life (calculated from 0-24 h) from 12.7 +/- 3.2 (mean +/- s.d.) to 25.3 +/- 3.9 h and decreased clearance from 3.01 +/- 0.67 to 1.32 +/- 0.32 1 h-1. There was no change in the apparent volume of distribution. Antipyrine half life changed with time in the presence of primaquine and when calculated between 24 and 48 h had returned to control. After primaquine, the metabolic clearance (calculated from 0-24 h) of antipyrine to its three main metabolites, 3-hydroxymethylantipyrine, 4-hydroxyantipyrine and norantipyrine was significantly reduced. There was no selective effect on a particular metabolic pathway. There was no change in 6 beta-hydroxycortisol excretion (expressed as a ratio of total 17-hydroxy-corticosteroids) in the period 0-48 h following primaquine administration. The inhibition of hepatic metabolism by primaquine but not the structurally related chloroquine may be an example of a structure activity phenomenon and could be of clinical significance.

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Selected References

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