Studies on the pharmacokinetics of primaquine

A sensitive and specific assay for primaquine in plasma and urine using gas chromatography/mass spectrometry has been developed and used to study the plasma kinetics of primaquine. Preliminary studies on the effects of single and multiple oral doses have been carried out. In both cases the drug was completely, or almost completely, removed from the plasma in 24 h. The concentration of primaquine in the plasma usually reached a peak 1-2 hours after oral administration. The plasma elimination half-life was about 4 h. Less than 1% of the dose was detected in the urine collected over a 24-h period following drug ingestion. When Caucasian volunteers were given primaquine and chloroquine concurrently, some of them developed significant methaemoglobinaemia. Primaquine was not detectable in the plasma of any of the volunteers, 24 h after each daily dose.