Clinical Pharmacology & Therapeutics · 1973 · 50 citations · 0 references
MedicinePharmacokineticsPharmacologyClinical PharmacologyDrug MetabolismPediatric Clinical PharmacologyDrug DispositionDrug Half-lifePediatric PharmacokineticsPediatric PharmacologyChild PharmacokineticsDrug Excretion In ChildrenDrug Half-life In ChildrenDrug Metabolism In ChildrenMaintenance Therapy TrialsUnchanged Drug ExcretionUrinary Excretion Rate
Pharmacokinetic studies in 4 children with hypo glycemia who required diazoxide therapy revealed a half‐life of the drug in blood of 9.5 to 24 hmlrs. The blood level of diazoxide in these children while receiving maintenance therapy was 15 to 50 p.g per milliliter. Hyperglycemia and acidosis developed in one of these patients in the presence of a persistent blood level above 100 ug per milliliter. Twenty‐four hour urinary excretion of unchanged drug in 2 patients was 20 and 33 per cent of the initial dose, and 80 per cent in one patient on maintenance. In order to investigate the fate of the drug better, 3 H‐diazoxide was purified for use in adult volunteers and animals. The half‐life of the drug in plasma of 2 adults was 24 and 36 hours. In these subiects as much as 94 per cent of the radioactive dose was recovered in the urine. About half the radioactivity in urine was present as unchanged drug. The plasma half‐life of 3H‐diazoxide in rats and dogs was much shorter than in man.