Human plasma and urine quinine levels following tablets, capsules, and intravenous infusion

Abstract
Using a crossover design, 12 healthy male volunteers received 3 forms of quinine in 3 day courses in random sequence at weekly intervals. Enteric‐coated tablets and gelatin capsules of quinine sulfate (540 mg base) were given orally every 8 hours for 3 days (1.62 gm base daily), and quinine dihydrochloride (490 mg base) was given as a continuous intravenous infusion every 8 hours for 3 days (1.47 gm base daily). Drug‐related toxicity included headache, tinnitus, and liver dysfunction. Form‐related toxicities were nausea, abdominal pain, and diarrhea with oral administration and ephemeral thrombophlebitis at the needle site with intravenous administration in 2 of 12 infusions. The plasma quinine levels were maximal at 72 hours with mean levels of 5.3,3.7, and 4.1 mg per liter for infusions, capsules, and tablets, respectively. Quinine by infusion resulted in significantly higher plasma levels than oral quinine. The plasma quinine concentrations during administration of capsules and tablets were not significantly different. Recovery of quinine in the urine was 18%, 14%, and 10% for intravenous, capsule, and tablet forms, respectively.