[Antidepressive action, pharmacokinetic characteristics and biochemical properties of cimoxatone, a new reversible MAO-A inhibitor].
Cimoxatone is a new monoamine oxidase inhibitor (MAOI) in comparison to the existing non-selective and irreversible MAOIs used in the therapy of depression. A clinical study has been carried out in 10 depressed patients. Cimoxatone was given from 0.32 to 0.78 mg/kg/day for 28 days. The drug was shown to be effective against depression and well tolerated at the given doses. The inhibition of monoamine oxidase and its reversibility were assessed by urinary excretion of 3-methoxy-4-hydroxy- phenylethyleneglycol sulphate. The treatment had no effect on the plasma prolactin levels. The plasma concentrations of cimoxatone reached a plateau after 3 to 4 days of therapy. The study confirmed earlier findings in healthy volunteers that the principal metabolite is also active as a type A MAOI. The plasma elimination of cimoxatone and its metabolite is almost complete 4 days after the last dosing.
D000328:Adult; D002986:Clinical Trials as Topic; D003866:Depressive Disorder / Q000188:drug therapy*; D005260:Female; D006801:Humans; D007700:Kinetics; D008297:Male; D008734:Methoxyhydroxyphenylglycol / Q000031:analogs & derivatives / Q000652:urine; D008875:Middle Aged; D008996:Monoamine Oxidase Inhibitors / Q000097:blood / Q000378:metabolism / Q000627:therapeutic use*; D010080:Oxazoles / Q000097:blood / Q000378:metabolism / Q000627:therapeutic use*; D023303:Oxazolidinones; D011388:Prolactin / Q000097:blood
D008996:Monoamine Oxidase Inhibitors; D010080:Oxazoles; D023303:Oxazolidinones; C030284:3-methoxy-4-hydroxyphenylglycol sulfate; D008734:Methoxyhydroxyphenylglycol; C038383:MD 770222; D011388:Prolactin; C026234:cimoxatone
Activité antidépressive, caractéristiques pharmacocinétiques et propriétés biochimiques de la cimoxatone, un nouvel IMAO-A réversible.