Instruction for use: Moclobemide

Latin name of substance Moclobemide

Moclobemidum (genus. Moclobemidi)

Chemical name

p-Chloro-N- (2-morpholinoethyl) benzamide

Gross formula

C₁₃H₁₇ClN₂O₂

Pharmacological group:

Antidepressant

The nosological classification (ICD-10)

F06 Other mental disorders due to brain damage or dysfunction or somatic disease: Somatogenic depression; Somatogenic psychosis

F06.3 Organic mood disorders [affective]: Secondary affective symptoms; Organic depression; Affective disorders; Depressed mood with elements of anxiety

F20 Schizophrenia: Schizophrenic Conditions; An exacerbation of schizophrenia; Schizophrenia; Chronic schizophrenia; Dementia praecox; Bleuler's disease; Psychotic discordant; Dementia early; The febrile form of schizophrenia; Chronic schizophrenic disorder; Psychosis of the schizophrenic type; Acute form of schizophrenia; Acute schizophrenic disorder; Cerebral Organic Insufficiency in Schizophrenia; Acute attack of schizophrenia; Schizophrenic psychosis; Acute schizophrenia; Sluggish schizophrenia; Sluggish schizophrenia with apathoabulic disorders; Acute stage of schizophrenia with agitation

F32 Depressive episode: Adynamic subdepression; Astheno-adynamic subdepressive states; Asthenoadressive disorder; Astheno-depressive disorder; Asthenodepressive state; Astheno-depressive state; Major Depressive Disorder; Vyaloapatichesky depression with retardation; Double Depression; Depressive pseudodement; Depressive illness; Depressive mood disorder; Depressive disorder; Depressive mood disorder; Depressive state; Depressive disorders; Depressive syndrome; Depressive syndrome larviated; Depressive syndrome in psychoses; Depressed masks; Depression; Depression Depletion; Depression with the phenomena of inhibition within the framework of cyclothymia; Depression is smiling; Involutional depression; Involutionary melancholy; Involutional depression; Manic-depressive disorder; Masked Depression; Melancholic Attack; Neurotic depression; Neurotic depression; Shallow Depression; Organic depression; Organic depressive syndrome; Simple depression; Simple melancholic syndrome; Psychogenic depression; Reactive depression; Reactive depression with moderate psychopathological symptoms; Reactive depressive states; Reactive depression; Recurrent depression; Seasonal depressive syndrome; Severostatic depression; Senile Depression; Symptomatic Depression; Somatogenic depression; Cyclotymic depression; Exogenous depression; Endogenous depression; Endogenous Depressive Conditions; Endogenous Depression; Endogenous depressive syndrome

F34.1 Dysthymia: Dysthymic state within the framework of psychopathic disorders in children and adolescents

F40.1 Social phobia: Social isolation; Social detachment; Social phobia; Social Anxiety Disorder / Social Phobia; Sociophobia; Sociopathy

CAS code

71320-77-9

Characteristics of the substance Moclobemide

Antidepressant (MAO inhibitor).

White or white with a creamy hue of crystalline powder. Easily soluble in water and alcohol.

Pharmacology

Pharmacological action - antidepressive, psychostimulating.

Selectively and reversibly inhibits MAO type A, inhibits the metabolism of serotonin (predominantly), norepinephrine, dopamine, causing their accumulation in the synaptic cleft. The optimal antidepressant effect develops with oppression of MAO by 60-80%. Improves mood, increases psychomotor activity. Reduces the symptoms of depression - dysphoria, inhibition, inability to concentrate attention, reduces symptoms of social phobia, improves sleep.

After oral administration, it is quickly and completely absorbed from the digestive tract. Cmax is achieved after 1 hour. Bioavailability is 40-80%. Equilibrium concentration in the plasma is created after 1 week of constant reception. Binding to blood proteins (mainly albumin) is 50%. Fabric barriers easily pass, the apparent volume of distribution is about 1.2 l / kg. Almost completely biotransformed (oxidized). It is excreted by the kidneys mainly in the form of metabolites (in unchanged form - less than 1%). The total ground clearance is 20-50 l / h. T1 / 2 - 1-4 hours.

Metabolism

It was shown that moclobemide is partially metabolized by CYP2C19 and CYP2D6 isoenzymes. Thus, in the case of slow metabolizers (which can be genetically caused or caused by the intake of drugs - inhibitors of metabolism), the biotransformation of moclobemide can be altered. The results of two studies conducted to study the severity of this effect suggest that the effect is not of great therapeutic value due to the presence of multiple alternative metabolic pathways and does not require correction of the dose of moclobemide.

Application of Moclobemide

Depression of various etiologies: with manic-depressive psychosis, various forms of schizophrenia, chronic alcoholism, senile and involutional, reactive and neurotic, social phobia.

Contraindications

Hypersensitivity, acute impairment of consciousness, simultaneous reception of selegiline, children's age (safety and efficacy in children are not defined).

Application in pregnancy and lactation

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 - about 1/30 of the dose received by the mother.

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

Side effects of Moclobemide

From the nervous system and sensory organs: dizziness, headache, sleep disorder, agitation, anxiety, irritability, confusion, paresthesia, blurred vision.

On the part of the intestine: dry mouth, nausea, heartburn, feeling of overflow of the stomach, diarrhea / constipation.

Other: skin reactions (rash, itching, urticaria, hot flashes).

Interaction

Strengthens and lengthens the effect of sympathomimetics and opiates. Increases the likelihood of adverse reactions from the central nervous system when combined with clomipramine, dextromethorphan. Cimetidine slows the biotransformation of moclobemide.

The simultaneous administration of moclobemide and other antidepressants that increase the serotonin concentration should be conducted with caution. This is due to the fact that in some cases there is an increase in the frequency of symptoms indicative of serotonergic hyperactivity (hyperthermia, confusion, increased reflexes, myoclonus).

In animals, moclobemide enhances and lengthens the effect of opiates, so when used simultaneously with moclobemide, a dose adjustment of these drugs may be required.

With simultaneous use, inhibitors of microsomal oxidation slow down the metabolism of moclobemide.

Contraindicated simultaneous use of moclobemide and selegiline (see Contraindications).

Routes of administration

Inside.

Precautions for the substance Moclobemide

With caution appoint with thyrotoxicosis and pheochromocytoma (possibly the development of hypertensive reactions). It is not recommended for patients in whom excitation is the main clinical manifestation of the disease. In schizophrenic or schizoaffective psychosis, there may be an increase in schizophrenic symptoms (it is necessary in this case to switch to neuroleptics). Patients with elevated blood pressure should refrain from excess consumption of foods containing tyramine.