[Pharmacology, toxicology and pharmacokinetics of mofebutazone].
The difference between mofebutazone and phenylbutazone is shown by means of toxicological, pharmacological and pharmacokinetic studies as well as by the protein binding. In spite of a certain chemical similarity both substances differ distinctly. Mofebutazone is approx. 5-6 times less toxic than phenylbutazone but its analgesic and antiphlogistic effects are weaker than those of phenylbutazone. The half life time of mofebutazone of 1.9 h is considerably shorter than that of phenylbutazone (54-99 h). Mofebutazone, in contrast to phenylbutazone, is mainly glucuronidised and to 94% eliminated within 24 h, phenylbutazone on the other hand to only 88% within 21 days. In spite of a high plasma protein binding quota of 99%, mofebutazone is classed among those substances with a medium binding potential. Conclusions may only be drawn with great reservation with regard to a category of substances from the effect and side effects of one substance on the basis of the present studies.
D000328:Adult; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000097:blood / Q000633:toxicity*; D001711:Biotransformation; D004305:Dose-Response Relationship, Drug; D004487:Edema / Q000188:drug therapy; D006801:Humans; D007249:Inflammation / Q000188:drug therapy; D007700:Kinetics; D008297:Male; D008657:Metabolic Clearance Rate; D051379:Mice; D010146:Pain / Q000188:drug therapy; D010653:Phenylbutazone / Q000031:analogs & derivatives* / Q000097:blood / Q000633:toxicity; D011485:Protein Binding
D000893:Anti-Inflammatory Agents; D010653:Phenylbutazone; C002374:mofebutazone
Zur Pharmakologie, Toxikologie und Pharmakokinetik von Mofebutazon.