Antidepressant - a reversible MAO-A inhibitor. It inhibits the metabolism of noradrenaline, Dopamine and serotonin, which leads to an increase in their concentration in the extracellular space. It is completely absorbed from the gastrointestinal tract, reaching Cmax within the first hour after administration. The first-pass effect of the liver reduces the bioavailability of the drug; this phenomenon is more severe after a single dose (bioavailability 60%) than after several doses (bioavailability 80%). About 50% is bound to plasma proteins. It is almost completely metabolised, mainly by oxidation reaction of fragments of the molecule. CYP2C19 and CYP2D6 isoenzymes are involved in the metabolism. Metabolites are excreted via the kidney. Less than 1% of the dose is excreted unchanged by the kidneys. Medium T0,5 in the elimination phase after several doses (300 mg 2 times a day) is about 3 hours.
Contraindications:
Hypersensitivity to the components of the preparation. acute confusion. Phaeochromocytoma tumor. Children (no clinical trials). Do not use with pethidine or selegiline. Do not use with dextromethorphan. Do not use with serotonin reuptake inhibitors (including tricyclic antidepressants) - between discontinuation of serotonin reuptake inhibitors and administration of the preparation should take a period of 4-5 times longer than the half-life of the drug discontinued.
Precautions:
Use with caution in patients with epilepsy. In patients with thyrotoxicosis, caution should be exercised when initiating treatment with moclobemide (risk of hypertensive reaction). In depressed patients in whom excitement predominates in the clinical picture should not be administered or should be used only in combination with sedatives (eg benzodiazepines); sedatives should not be used for longer than 2-3 weeks. In cases of depression in patients with bipolar disorder, episodes may occur. Due to the lack of adequate clinical data, moclobemide should not be used in patients with concomitant schizophrenia or with schizoaffective organic diseases. All patients treated with moclobemide should be monitored for signs of suicidal ideation and behavior (especially in early recovery and after dose adjustment); this applies especially to patients under the age of 25 years and patients with a history of suicidal behavior or thoughts. When treating patients with other mental disorders, the same precautions should be taken as when treating patients with major depressive disorder. If drowsiness, confusion or convulsions occur during therapy with moclobemide, the risk of hyponatremia (especially in elderly patients) should be considered. If symptoms suggestive of a serotonin syndrome occur during treatment, care should be provided (if necessary in a hospital setting) and appropriate treatment. It is possible that pharmacogenetically determined abnormalities in the metabolism of mephenytoin may affect the metabolism of moclobemide; the clinical significance of this fact is unknown. Due to the lactose content, the preparation should not be used in patients with rare congenital galactose intolerance, Lapp lactase deficiency or poor absorption of Glucose and galactose.
Pregnancy and lactation:
Before using the drug during pregnancy or breastfeeding, the relationship between the benefit from use and the potential risk to the fetus or child should be evaluated.
Side effects:
The following may occur: sleep disturbances, agitation, anxiety, confusion, suicidal thoughts and behaviors (during treatment, and also shortly after discontinuation of moclobemide), dizziness, headache, paresthesia, irritability, dryness of the oral mucosa, nausea, diarrhea, constipation, vomiting, fromsight disorders, skin reactions (eg rash, pruritus, urticaria), swelling, redness (especially of the face).Rare: increase in liver enzymes (without clinical sequelae).Very rare: hyponatremia.
Dosage:
Orally, after finishing the meal. Adults.Depressive disordersThe recommended dose is 300-600 mg daily in 2-3 divided doses. The initial dose is 300 mg a day and in the case of severe depression it can be increased to 600 mg a day. Do not increase the dose before the first week of treatment because the bioavailability of moclobemide increases during this period. The dose of the drug can be reduced depending on the patient's individual response. The effectiveness of therapy can be fully assessed after 4-6 weeks of treatment.Social phobiaThe recommended dose is 600 mg daily in 2 divided doses. The effectiveness of therapy can be assessed after 8-12 weeks of treatment. If it is effective, consider continuing treatment. Clinical trials confirm the effectiveness of a long-term formulation. The need for further treatment should be periodically assessed.Special groups of patients. In patients whose hepatic metabolism is disturbed by liver disease or drugs that inhibit the activity of microsomal monooxygenase (eg cimetidine), the dose should be reduced by half or to 1/3. Patients with decreased renal function or elderly do not require dose adjustment.
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