Moclobemide (Moclobemidum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
Read on
Clinical and pharmacological group: & nbsp

Antidepressants

Included in the formulation
АТХ:

N.06.A.G.02   Moclobemide

Pharmacodynamics:

The drug selectively competitively and reversibly inhibits monoamine oxidase type A,inhibits the metabolism of serotonin, dopamine and norepinephrine, which leads to an increase in the concentration of these substances in the central nervous system. Improves mood, increases psychomotor activity. Reduces the symptoms of depression - dysphoria, inhibition, inability to concentrate attention, stop the symptoms of social phobia. Improves sleep in patients with depression with sleep disorders.

Pharmacokinetics:

After oral administration, it is quickly and completely absorbed from the GIT. The maximum concentration is achieved after 1 hour. Bioavailability is 40-80%. The equilibrium concentration in plasma is created after 1 a week constant reception. The connection with plasma proteins is 50%, metabolized in the liver (partially with the participation of isoenzymes CYP2C19 and CYP2D6), half-life is 90 minutes, or 4 hours with liver cirrhosis. The drug is eliminated by the kidneys (1% unchanged).

Indications:

Sociopathy and depression of various etiologies (with manic-depressive psychosis, various forms of schizophrenia, chronic alcoholism, senile and involutional, reactive and neurotic).

ICD-10

V.F00-F09.F06   Other mental disorders due to damage and dysfunction of the brain or somatic disease

V.F00-F09.F06.3   Organic mood disorders [affective]

V.F20-F29.F20   Schizophrenia

V.F30-F39.F31   Bipolar affective disorder

V.F30-F39.F32   Depressive episode

V.F30-F39.F33   Recurrent depressive disorder

V.F30-F39.F34.1   Dysthymia

V.F40-F48.F40.1   Social phobia

V.F40-F48.F41.2   Mixed anxiety and depressive disorder

Contraindications:

Hypesensitivity.

Simultaneous reception of herwhetheron.

Acute impairment of consciousness.

Childhood.

Excitation.

Agitation.

Pheochromocytoma.

Carefully:

Thyrotoxicosis.

Pregnancy and lactation:

Category FDA not determined. Adequate and strictly controlled studies of moclobemide safety in pregnant women have not been conducted. In studies of reproductive performance in animals, no negative effect of moclobemide on the fetus was detected.

Moclobemide is excreted in breast milk in small concentrations.

Application in pregnancy and lactation is possible only if the expected effect of therapy exceeds the risk for the fetus and the baby.

Dosing and Administration:

Orally, after eating for 2-3 doses 300-600 mg.

The initial daily dose should be 300 mg, but in severe cases after 1 week of administration, the dose may be increased to 600 mg.

Side effects:

From the side of the nervous system: headache, dizziness, agitation, sleep disorder, irritability, anxiety, paresthesia, confusion, blurred vision.

From the gastrointestinal tract: heartburn, nausea, dry mouth, diarrhea / constipation, feeling of a full stomach.

Other: skin rashes, dysarthria, apathy, amnesia, dysuria, bradycardia, extrapyramidal disorders, hallucinations, hyperhidrosis.

Overdose:

Amnesia, agitation, dysarthria, drowsiness, disorientation, nausea, hypertension, decreased reflexes, vomiting, convulsions. Treatment is symptomatic.

Interaction:

Alcoholic beverages containing tyramine (beer, ale, wine) - sometimes hypertensive reaction.

Antidepressants (fluoxetine, citalopram) - possibly the development of serotonin syndrome - the development of a potentially lethal serotonin syndrome.

Dextromethorphan - nausea, tremor, dizziness and vomiting, moderate agitation.

Meperidine and, possibly, other opioid analgesics - potentiation of their effects. The combined use of meperidine and moclobemide is contraindicated, and other opioid analgesics should be used with caution.

Sympathomimetics, including epinephrine with local anesthetics, - a sharp increase in systolic pressure. Do not use preparations containing ephedrine, amphetamine or adrenomimetics.

Altrethamine - with combined appointment, severe orthostatic hypotension is possible.

Cimetidine - inhibition of metabolism and increased concentrations and toxicity of moclobemide.

Combination amitriptyline + chlordiazepoxide incompatible with inhibitors MAO (due to the risk of developing serotonin syndrome, including myoclonus, spasms during excitation, delirium and coma). Applying a combination amitriptyline + chlordiazepoxide You can start the day after reversing the reversible inhibitor MAO moclobemide. Application of inhibitors MAO you can start after 2 weeks after combination cancellation amitriptyline + chlordiazepoxide. In either case, u moclobemide, and combination amitriptyline + chlordiazepoxide should be started with small doses, gradually increasing them depending on the effect.

The increase HELL and the emergence of hypertensive crisis after simultaneous application of buspirone and moclobemide (reversible inhibitor MAO); concerning buspirone can not be combined with moclobemide. Must pass at least 14 days after the cancellation of buspirone before the application of moclobemide; but buspirone can be administered 1 day after the abolition of moclobemide.

Moclobemide inhibits MAO and on the background of venlafaxine provokes the development of adverse reactions,

With simultaneous use with zolmitriptan - an increase in the maximum concentration in the blood plasma and AUC of zolmitriptan; with clomipramine - cases of development of serotonin syndrome have been described; with levodopa - there may be a headache, nausea, insomnia; with selegiline - increased sensitivity to tyramine; with sumatriptan - increased bioavailability of sumatriptan; with fluoxetine, citalopram - the development of serotonin syndrome is possible.

Moclobemide enhances the effect of glipizide, diazepam.

Repaglinide - moclobemide inhibits MAO and enhances the hypoglycemic effect.

Moclobemide prolongs and intensifies the anticholinergic effect of diphenhydramine.

Systemic action of ibuprofen may be intensified and prolonged with simultaneous administration of moclobemide.

Carbamazepine - moclobemide, as an inhibitor MAO, increases the likelihood of side effects.

Carvedilol - strengthens the effect on HELL (hypotension) and heart rate (bradycardia).

Clonazepam - potentiation of oppression CNS.

Methyldopa - strengthens the antihypertensive effect; At the same time, cases of development of a hypertonic crisis with psychomotor excitation are described; joint appointment is not recommended.

Metoclopramide - moclobemide inhibits MAO and increases the duration of circulation of catecholamines released by metoclopramide.

Promethazine - moclobemide increases the risk of developing extrapyramidal disorders (inhibits MAO).

Salmeterol, terbutaline - moclobemide as an inhibitor MAO can increase the effect on cardiovascular system.

Moclobemide inhibits MAO and on the background of sertraline can lead to severe, life-threatening reactions, including hyperthermia, rigidity, myoclonus, autonomic disorders, delirium and coma; simultaneous and / or consistent use is contraindicated.

Tramadol - moclobemide inhibits MAO and increases the risk of serotonin syndrome (fever, agitation, tremor and anxiety, seizures).

Moclobemide inhibits MAO, prolongs and intensifies the anticholinergic effects of cyproheptadine and inhibition CNS; combined use is contraindicated.

Special instructions:

The drug should not be used in patients with schizophrenia.

During the administration of the drug, a large number of products containing tyramine should not be eaten.

During the treatment period it is recommended to refrain from potentially dangerous activities related to the need for concentration of attention and increased speed of psychomotor reactions.

Instructions
Up