Moclobemide ( Moclobemide , active ingredient: 4-chloro-N- (2-morpholinoethyl) -benzamide, trade name: "Aurorix") - a drug related to antidepressants - MAO inhibitors of reversible action and affecting mainly MAO type A. By structure differs from befol in that in the side chain it contains an ethyl group instead of a propyl group.
Moclobemide | |
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Moclobemidum | |
Chemical compound | |
IUPAC | 4-chloro- N - (2-morpholin-4-ylethyl) benzamide |
Gross formula | C 13 H 17 ClN 2 O 2 |
Molar mass | 268,739 |
Cas | |
PubChem | |
Drugbank | |
Classification | |
ATX | |
Pharmacokinetics | |
Bioavailable | 60% after the first application,> 80% after the first week of application |
Metabolism | Liver |
The half-life. | from 1 to 2 hours |
Excretion | Bud |
Dosage Forms | |
Tablets 150 mg, 300 mg | |
Route of administration | |
Inside | |
Other names | |
Aurorix | |
Content
Pharmacological action and application
A single dose of 300 mg inhibits about 80% of type A monoamine oxidase (MAO-A) and 30% of type B monoamine oxidase (MAO-B), thus blocking the destruction of norepinephrine, serotonin and, to a lesser extent, dopamine. Reuptake inhibition of the aforementioned neurotransmitters is not observed.
Used for depression of various etiologies, as well as sociophobia . The therapeutic dose is 300-600 mg per day.
Pharmacokinetics
Absorption is fast and complete after oral administration. TCmax - 1 hour after a single dose. Css is created by the end of the 1st week of treatment. Bioavailability (depending on the size of the dose) is 40–80%. Distribution volume - 1.2 l / kg. Communication with plasma proteins (albumin) - 80%. Tissue barriers easily pass, the apparent volume of distribution is about 1.2 l / kg.
It is metabolized in the liver during oxidative reactions by the isoenzymes of CYP2C9 and CYP2D6. In the form of metabolites (unchanged 1%) is rapidly excreted by the kidneys, the total clearance of 333-833.3 ml / min, T1 / 2 1-4 hours.
Side Effects
The most common side effects of moclobemide are dry mucous membranes (especially the oral cavity), dizziness, headaches, drowsiness, nausea, and insomnia. More rare side effects include constipation, discomfort in the stomach, and very rare - muscle twitching, visual impairment. In patients with bipolar depression, the depressive phase can be changed to manic [1] .
Agitation is also possible, in patients with paranoid syndrome - its aggravation; fatigue, tremor , sweating, tachycardia [2] . There have been cases of the occurrence of serotonin syndrome during moclobemide monotherapy [3] .
Contraindications
Hepatic and renal failure, diseases of the hematopoietic system , pheochromocytoma , pregnancy and lactation, age less than 15 years, hypersensitivity to the drug [2] .
Interactions
When treating with reversible MAO inhibitors, such as moclobemide, although rarely (much less often than with irreversible MAO inhibitors), tyramine adverse reactions may occur due to interaction with certain foods and drugs - tyramine syndrome . Therefore, patients (especially those with hypertension ) should avoid large amounts of food containing tyramine ; it is also necessary to avoid taking sympathomimetics ( ephedrine , pseudoephedrine , phenylpropanolamine ) [4] . The use of opioid analgesics , maprotiline , levodopa , methyldopa, and furazolidone in combination with moclobemide can also lead to a dangerous increase in blood pressure [5] .
It is also necessary to avoid drugs whose interaction with MAOI can lead to serotonin syndrome: SSRIs antidepressants [6] , cyclic antidepressants [7] (including clomipramine , imipramine [6] ), venlafaxine [8] , cold medicines containing dextromethorphan [ 6] , meperidine [7] [8] , nefazodona [8] [9] , lithium preparations [9] , herbal antidepressants, containing St. John's wort [10] , 5-hydroxytryptophan [11] and tryptophan [7] .
When combined with antipsychotics, moclobemide enhances antipsychotic extrapyramidal disorders [2] . The combination with clozapine leads to a toxic effect on the central nervous system. Moclobemide enhances the toxicity of phenothiazine derivatives [5] .
The combined use of moclobemide with other MAO inhibitors is unacceptable, it can lead to fever , convulsions and death [5] .
Dextromethorphan in combination with moclobemide increases the risk of side effects from the central nervous system [5] .
Moclobemide enhances the effect of indapamide , enhances the hypotensive effect of diuretics , the hypoglycemic effect of insulin and oral hypoglycemic drugs [5] .
Cimetidine slows down the biotransformation of moclobemide [5] .
Notes
- ↑ Minutko V.L. Depression. - Moscow: GEOTAR-Media, 2006 .-- 320 p. - 2000 copies. - ISBN 5-9704-0205-2 .
- ↑ 1 2 3 Podkorytov V.S., Chaika Yu. Yu. Depression. Modern therapy. - Kharkov: Tornado, 2003 .-- 352 p. - ISBN 966-635-495-0 .
- ↑ Volkov V.P. Iatrogenic psychoneurosomatic syndromes. - Tver: Triad, 2014 .-- 320 p.
- ↑ Reference guide for psychopharmacological and antiepileptic drugs approved for use in Russia / Ed. S. N. Mosolova. - 2nd, rev. - M .: "BINOM Publishing House", 2004. - 304 p. - 7000 copies. - ISBN 5-9518-0093-5 .
- ↑ 1 2 3 4 5 6 Drug Interactions and the Effectiveness of Pharmacotherapy / L. V. Derimedved, I. M. Pertsev, E. V. Shuvanova, I. A. Zupanets, V. N. Khomenko; under the editorship of prof. I. M. Pertseva. - Kharkov: Publishing house "Megapolis", 2001. - 784 p. - 5,000 copies. - ISBN 996-96421-0-X.
- ↑ 1 2 3 Mosolov C. N., Kostyukova E. G., Serditov O. V. Serotonin syndrome in the treatment of depression // International Journal of Medical Practice. - MediaSfera, 2000. - No. 8 . Archived February 1, 2015.
- ↑ 1 2 3 Arana J., Rosenbaum J. Pharmacotherapy of mental disorders. Per. from English - M .: Publishing house BINOM, 2004 .-- 416 p. - ISBN 5-9518-0098-6 .
- ↑ 1 2 3 Janichak F.J., Davis J.M., Predkorn Sh. H., Aid F.J. Jr. Principles and practice of psychopharmacotherapy . - 3rd. - M. , 1999 .-- 728 p. - ISBN 966-521-031-9 . (inaccessible link)
- ↑ 1 2 Schlienger RG, Shear NH. Serotonin Syndrome // British Journal of Psychiatry. - 1996 .-- T. 169 (suppl.31) . - S. 15-20 . Translation: Serotonin Syndrome // Review of Modern Psychiatry. - 1998. - Vol. 1 .
- ↑ Antidepressant Therapy and Other Treatments for Depressive Disorders: CINP Working Group Report Based on a Survey of Evidence / Editors T. Bagai, H. Grunze, N. Sartorius. A translation into Russian was prepared at the Moscow Scientific Research Institute of Psychiatry of the Russian Health Ministry, edited by V.N. Krasnova. - Moscow, 2008 .-- 216 p. Archived March 4, 2016. Archived March 4, 2016 on Wayback Machine
- ↑ Drug Interactions: SSRIs . iHerb.Com. Archived March 15, 2012.