Ketorolac Tromethamine Pharmacokinetics and Metabolism After Intravenous, Intramuscular, and Oral Administration in Humans and Animals

摘要: In humans, ketorolac is completely bioavailable and its kinetics are linear. It absorbed rapidly (half-life for absorption 3.8 min) after oral (fasting) intramuscular administration; food delays but does not reduce absorption. The drug highly protein bound in humans (greater than 99%). mean plasma elimination half-life 5-6 hours, extensively distributed outside the vascular compartment (Vd beta 15 L). Virtually all of drug-related material circulating form 96%), with only metabolite pharmacologically inactive p-hydroxyketorolac (PHK). Humans excrete about 90% administered dose urine. About 60% recovered from urine ketorolac, 12% PHK, 28% represents polar, glucuronide conjugates ketorolac. animal models which ketorolac's metabolism most similar to those mouse monkey, respectively.