[Metabolism and pharmacokinetics of acemetacin in man (author's transl)].
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Dell HD, Doersing M, Fischer W, Jacobi H, Kamp R, Kohler G, Schollnhammer G
[Metabolism and pharmacokinetics of acemetacin in man (author's transl)].
Arzneimittelforschung. 1980;30(8A):1391-8.
- PubMed ID
- 7191306 [ View in PubMed]
- Abstract
Metabolism and pharmacokinetics of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetoxy]-acetic acid (acemetacin, TV 1322, Rantudil) in comparison to equimolar doses of indometacin was investigated in human volunteers after a single oral application and in rheumatic patients after multiple application. After multiple application (t.i.d. for 10 days) of equimolar doses of acemetacin and indometacin, mean blood level curves. The bioavailability of acemetacin derived from these data, corresponds to that of indometacin, i.e., approx. 100%, whereas after a single dose bioavailability of acemetcin is found to be smaller (66% from blood level, 64% from urine). This difference between single and multiple application is explained by slow filling-up of compartments. Degradation of acemetacin occurs by esterolytic cleavage to indometacin, by O-demethylation and N-desacylation and by partial conjugation of all these compounds to glucuronic acid. Blood level ratios of acemetacin and indometacin are equal after single and after multiple application of acemetacin. Therefore, degradation of acemetacin is not induced after multiple application. After a steady-state has been reached half-life of elimination is 4.5 +/- 2.8 h, which is longer than for indometacin (2.2 +/- 0.5 h). Interindividual differences are in the same range as described for indometacin.
DrugBank Data that Cites this Article
- Drugs
- Drug Interactions
Drugs Interaction Integrate drug-drug
interactions in your softwareFosphenytoinAcemetacin The serum concentration of Fosphenytoin can be increased when it is combined with Acemetacin. PhenytoinAcemetacin The serum concentration of Phenytoin can be increased when it is combined with Acemetacin.