[Clinical-pharmacological and pharmacokinetic studies with naproxen].
d-2-(6'-Methoxy-2'-naphthyl)-propionic acid (naproxen) is bound in blood to a high degree to plasma protein. After oral application naproxen is absorbed rapidly and completely. The mean biological half-life in man is fourteen hours. This gives us the possibility of controlling the symptoms of disease with two daily doses. In man, 99% of naproxen is excreted in the urine, either unchanged or glucuronized and as its 6-des-methyl metabolite. There is a linear increase of plasma levels with daily doses of up to 500 mg. Higher naproxen doses do not produce higher blood levels but lead to a faster excretion. This probably depends in part on a saturation of the binding sites in plasma. Differences in affinity of some compounds for binding sites in plasma are responsible for a potential interaction between naproxen and other agents, such as warfarin, acetyl salicylic acid (ASA) and sulfonylureas. These interactions are discussed. In a double-blind trial the influence of naproxen and ASA on the gastric mucosa of healthy volunteers has been compared. The results of gastroscopic findings as well as laboratory tests are reported.
D000284:Administration, Oral; D000818:Animals; D000863:Antacids / Q000494:pharmacology; D001241:Aspirin / Q000494:pharmacology; D001682:Biological Availability; D002986:Clinical Trials as Topic; D003374:Coumarins / Q000494:pharmacology; D004347:Drug Interactions; D005753:Gastric Mucosa / Q000187:drug effects; D006207:Half-Life; D006801:Humans; D007275:Injections, Intravenous; D007700:Kinetics; D008954:Models, Biological; D009280:Naphthaleneacetic Acids / Q000097:blood*; D009288:Naproxen / Q000008:administration & dosage / Q000097:blood* / Q000494:pharmacology; D011485:Protein Binding / Q000187:drug effects; D051381:Rats; D013453:Sulfonylurea Compounds / Q000494:pharmacology; D014859:Warfarin / Q000494:pharmacology
D000863:Antacids; D003374:Coumarins; D009280:Naphthaleneacetic Acids; D013453:Sulfonylurea Compounds; D009288:Naproxen; D014859:Warfarin; D001241:Aspirin
Klinisch-pharmakologische und pharmakokinetische Studien mit Naproxen