Instructions for use. Moclobemide Description of the active ingredient

10 pieces. - cellular contour packings (3) - packs of cardboard.

pharmachologic effect

Antidepressant, selective inhibitor of MAO type A. It inhibits mainly metabolism, as well as norepinephrine and dopamine in the brain, increases their content in the central nervous system.

In clinical conditions, it exhibits moderate thymoanaleptic and distinct psychostimulant properties: it improves mood, increases mental and motor activity, and increases the ability to concentrate. Improves sleep in patients suffering from depression with sleep disorders. In terms of effectiveness in typical endogenous depressions, it is somewhat inferior to tricyclic antidepressants. The clinical effect of moclobemide develops by the end of the 1st week of treatment, usually already in the first days of administration, a pronounced activating effect is noted. The optimal antidepressant effect is observed when MAO is inhibited by 60-80%.

Pharmacokinetics

After oral administration, moclobemide is completely absorbed from the gastrointestinal tract. It undergoes the effect of "first pass" through the liver. Cmax in is achieved 1 hour after ingestion.

Moclobemide is widely distributed in the body. V d is about 1.2 l / kg. Plasma protein binding, mainly to , is 50%.

Almost completely metabolized in the body. Metabolism occurs mainly by oxidation with the participation of the CYP2C9 isoenzyme. At the same dose of moclobemide in individuals with a slow metabolism, the values of C max in blood plasma and AUC can be 1.5 times higher than in individuals with an intensive metabolism.

T 1 / 2 is 1-4 hours. Plasma clearance is about 20-50 l / h. It is excreted by the kidneys mainly in the form of metabolites, less than 1% - unchanged.

Indications

Depression of various etiologies, social phobia.

Contraindications

Acute conditions accompanied by confusion, states of agitation, agitation, pheochromocytoma, pregnancy, lactation, childhood, hypersensitivity to moclobemide.

Dosage

For adults, when taken orally, the initial dose is 300 mg / day in 2 divided doses. If necessary, the daily dose can be gradually increased to 600 mg. The duration of treatment is determined individually.

Side effects

From the side of the central nervous system and peripheral nervous system: restlessness, anxiety, general agitation, sleep disturbances, dizziness, headache, fear, paresthesia, tremor, blurred vision; rarely - confusion.

From the digestive system: dry mouth, nausea, feeling of fullness in the stomach, heartburn, diarrhea, constipation.

Allergic reactions: skin rash, itching, urticaria.

Others: increased sweating.

drug interaction

With simultaneous use with drugs that increase the level of serotonin, there is a possibility of developing serotonin syndrome.

In experimental studies, moclobemide potentiated the effects of opioid receptor agonists.

With simultaneous use with dextropropoxyphene, moderate agitation may develop; with zolmitriptan - an increase in Cmax in blood plasma and AUC of zolmitriptan; c - cases of development of serotonin syndrome are described; with levodopa - headache, nausea, insomnia are possible; with selegiline - increased sensitivity to tyramine; with sumatriptan - increased bioavailability; with fluoxetine, citalopram - the development of serotonin syndrome is possible.

With simultaneous use, cimetidine slows down the metabolism of moclobemide.

special instructions

Use with caution in patients suffering from thyrotoxicosis.

Due to limited clinical experience, it should not be used in patients with comorbid schizophrenia or schizoaffective organic brain disease.

It is necessary to monitor the condition of patients with suicidal tendencies at the beginning of treatment with moclobemide.

During treatment with moclobemide, you should not eat a large amount of food containing.

When used simultaneously with cimetidine, the usual dose of moclobemide should be reduced by 2 times.

Do not use concomitantly with selegiline, with serotonin reuptake inhibitors. Before the use of moclobemide after the end of treatment with serotonin reuptake inhibitors, an interval corresponding to 4-5 half-lives of the drug and / or its active metabolite should be observed.

Moclobemide should not be co-administered with dextromethorphan, which is an ingredient in many cough medicines.

Simultaneous use with pseudoephedrine, phenylpropanolamine should be avoided.

Use with caution simultaneously with drugs that increase the level of serotonin; with morphine, fentanyl (may require correction of the dosing regimen).

Due to the lack of sufficient clinical experience, it should not be used in pediatrics.

Influence on the ability to drive vehicles and control mechanisms

Pregnancy and lactation

Contraindicated in pregnancy and lactation.

There are no adequate and well-controlled safety studies of moclobemide in human pregnancy. In experimental studies, there was no negative effect of moclobemide on the fetus.

Moclobemide is excreted in breast milk in small concentrations - approximately 1/30 of the maternal dose.

Moclobemide is a drug that belongs to the group of antidepressants and psychostimulants. Despite the convenience of dosing, it can only be used under the supervision of a physician and according to strict indications. Independent change in dosage or drug withdrawal is prohibited.

Indications and pharmacological effect of Moclobemide

The main active ingredient of the drug is moclobemide. Its weight in one tablet is 150 mg. Among the indications for use, the following pathologies are distinguished:

schizophrenia;
chronic course of alcoholism;
depression, which has senile, reactive, involutional and neurotic types.

Against the background of the use of the drug, inhibition of metabolic processes associated with the production of such biologically active components as dopamine and norepinephrine is observed. To a lesser extent, the drug acts on serotonin. Gradually, neurotransmitters accumulate in the synaptic cleft. At the same time, the production of MAO is also inhibited, which achieves an antidepressant effect.

All about the drug and pharmacological properties.

Learn about: the effect of the drug, indications and contraindications.

With regular systematic intake, there is an improvement in mood and an increase in the activity of the patient, a decrease and elimination of lethargy and dysphoria. Attention gradually improves, concentration on ongoing events is ensured. Social phobia is almost completely eliminated, sleep becomes longer without night awakenings.

The drug is rapidly absorbed. The level of bioavailability approaches 100%. The maximum concentration in blood serum occurs within the first hour from the moment of use. The achievement of equilibrium concentration is noted with regular weekly use of the drug.

When released into the blood, the active components bind to plasma proteins only by half. The substance penetrates through various cellular barriers. Excretion is carried out by the organs of the urinary system in an inactive form. Half of the concentration of the drug is excreted 5 hours after its ingestion.

Contraindications and side effects of Moclobemide

The tool is prohibited to use in the presence of the following contraindications:

An acute condition, accompanied by confusion and psychomotor agitation.
Adrenal tumor or pheochromocytoma.
Pregnancy at any gestational age.
breastfeeding period.
Childhood.
An allergic reaction caused by hypersensitivity to any component of the drug.

The medication is taken with extreme caution. This is associated with a high risk of side effects. The most common manifestations include:

Headache that does not subside after taking analgesic drugs.
Agitation (motor restlessness) and dizziness.
with insomnia and subsequent increased suspiciousness and anxiety.
Formation of confusion of consciousness.
Violation of visual function.
Increased irritability.
development of paresthesia.
Violation of the digestive system with heartburn, nausea, dryness of the mucous membranes of the oral cavity.
Dyspeptic disorders with constipation or diarrhea.
Allergic reactions with skin rashes, itching and redness.
Excessive sweating.

With the development of such symptoms, it is required to seek help from a specialist and decide on the possible cancellation of the remedy. Clinical cases of overdose have not been identified. When they appear, you should immediately contact your doctor. If necessary, use symptomatic therapy.

Everything about: composition, pharmacological effect, indications and contraindications.

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Read about: rules for use, recipes for decoctions and tinctures.

Instructions for use

The instructions for taking Moclobemide indicate the optimal dose, as well as the duration of the course. However, the tactics of therapy is carried out on an individual basis by the attending physician on the basis of clinical symptoms and the dynamics of the course of the pathological process. The drug is recommended to be taken after meals. The daily dosage is in the range from 0.3 to 0.6 g of the main active ingredient. It is divided into three doses.

To prevent the symptoms of overdose, as well as the development of side effects, a loading dose is used with an initial use of 0.3 g of the drug and its subsequent increase to achieve a therapeutic effect. The amount should be increased no earlier than one week after the start of treatment. After reaching the clinical effect, the amount of the drug used is gradually reduced.

Important! During the first week, the state of health is monitored for suicidal tendencies against the background of a depressive syndrome.

The medicine can be purchased with a prescription. The price of Moclobemide ranges from 2400 to 2700 rubles. Analogues of the drug have a similar composition. Among them are Trazodone, Eprobemide, Pirlindol. Despite the fact that the reviews about the drug are mostly positive, driving, as well as work requiring attention control, is prohibited during therapy.

N06AG02 (Moclobemide)

Before using the drug MOCLOBEMIDE you should consult with your doctor. These instructions for use are for informational purposes only. For more information, please refer to the manufacturer's annotation.

Clinical and pharmacological group

02.002 (Antidepressant)

pharmachologic effect

Antidepressant, selective inhibitor of MAO type A. It inhibits mainly the metabolism of serotonin, as well as norepinephrine and dopamine in the brain, increases their content in the central nervous system.

Pharmacokinetics

After oral administration, moclobemide is completely absorbed from the gastrointestinal tract. It undergoes the effect of "first pass" through the liver. Cmax in plasma is achieved 1 hour after ingestion.

Moclobemide is widely distributed in the body. Vd is about 1.2 l/kg. Plasma protein binding, mainly albumin, is 50%.

Almost completely metabolized in the body. Metabolism occurs mainly by oxidation with the participation of the CYP2C9 isoenzyme. At the same dose of moclobemide in individuals with a slow metabolism, the values of Cmax in blood plasma and AUC can be 1.5 times higher than in individuals with an intensive metabolism.

T1 / 2 is 1-4 hours. Plasma clearance is about 20-50 l / h. It is excreted by the kidneys mainly in the form of metabolites, less than 1% - unchanged.

MOCLOBEMIDE: DOSAGE

drug interaction

With simultaneous use with drugs that increase the level of serotonin, there is a possibility of developing serotonin syndrome.

In experimental studies, moclobemide potentiated the effects of opioid receptor agonists.

With simultaneous use with dextropropoxyphene, moderate agitation may develop; with zolmitriptan - an increase in Cmax in blood plasma and AUC of zolmitriptan; with clomipramine - cases of the development of serotonin syndrome are described; with levodopa - headache, nausea, insomnia are possible; with selegiline - increased sensitivity to tyramine; with sumatriptan; with fluoxetine, citalopram - the development of serotonin syndrome is possible.

Pregnancy and lactation

There are no adequate and well-controlled safety studies of moclobemide in human pregnancy. In experimental studies, there was no negative effect of moclobemide on the fetus.

Moclobemide is excreted in breast milk in small concentrations - approximately 1/30 of the maternal dose.

MOCLOBEMIDE: SIDE EFFECTS

From the side of the central nervous system and peripheral nervous system: anxiety, anxiety, general agitation, sleep disturbances, dizziness, headache, fear, paresthesia, tremor, blurred vision; rarely - confusion.

From the digestive system: dry mouth, nausea, feeling of stomach fullness, heartburn, diarrhea, constipation.

Allergic reactions: skin rash, itching, urticaria.

Other: increased sweating.

Indications

Depression of various etiologies, social phobia.

Contraindications

Acute conditions accompanied by confusion, states of agitation, agitation, pheochromocytoma, pregnancy, lactation, childhood, hypersensitivity to moclobemide.

special instructions

Use with caution in patients suffering from thyrotoxicosis.

Due to limited clinical experience, it should not be used in patients with comorbid schizophrenia or schizoaffective organic brain disease.

It is necessary to monitor the condition of patients with suicidal tendencies at the beginning of treatment with moclobemide.

During the period of treatment with moclobemide, you should not eat a large amount of food containing tyramine.

When used simultaneously with cimetidine, the usual dose of moclobemide should be reduced by 2 times.

Moclobemide should not be co-administered with dextromethorphan, which is an ingredient in many cough medicines.

Simultaneous use with ephedrine, pseudoephedrine, phenylpropanolamine should be avoided.

Use with caution simultaneously with drugs that increase the level of serotonin; with morphine, fentanyl (may require correction of the dosing regimen).

Due to the lack of sufficient clinical experience, it should not be used in pediatrics.

Influence on the ability to drive vehicles and control mechanisms

"Moclobemide (Moclobemide)" used in the treatment and / or prevention of the following diseases (nosological classification - ICD-10):

Molecular formula: C13-H17-Cl-N2-O2

CAS Code: 71320-77-9

Description

Characteristic: White or off-white crystalline powder. Easily soluble in water and alcohol.

pharmachologic effect

Pharmacology: Pharmacological action - antidepressant, psychostimulant. Selectively and reversibly inhibits MAO type A, inhibits the metabolism of serotonin (mainly), norepinephrine, dopamine, causing their accumulation in the synaptic cleft. The optimal antidepressant effect develops when MAO is inhibited by 60-80%. Improves mood, increases psychomotor activity. Reduces symptoms of depression - dysphoria, lethargy, inability to concentrate, relieves symptoms of social phobia, improves sleep.

After oral administration, it is rapidly and completely absorbed from the gastrointestinal tract. C_max achieved after 1 hour Bioavailability is 40-80%. Equilibrium plasma concentration is created after 1 week of continuous administration. Binding to blood proteins (mainly albumin) is 50%. Easily passes tissue barriers, the apparent volume of distribution is about 1.2 l / kg. Almost completely biotransformed (oxidized). It is excreted by the kidneys mainly as metabolites (less than 1% unchanged). The total clearance is 20-50 l / h. T_1/2 - 1-4 hours.

Indications for use

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

Contraindications

Contraindications: Hypersensitivity, acute impairment of consciousness, concomitant use of selegiline, pregnancy, breast-feeding, childhood (safety and efficacy in children have not been determined).

Side effects

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

On the part of the digestive tract: dry mouth, nausea, heartburn, feeling of fullness in the stomach, diarrhea / constipation.

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

Interaction: Enhances and prolongs the effect of sympathomimetics and opiates. Increases the likelihood of adverse reactions from the central nervous system when combined with clomipramine, dextromethorphan. Cimetidine slows down the biotransformation of moclobemide.

Dosage and method of application

Dosage and administration: Inside, after eating - 300-600 mg, for 2-3 doses. The initial daily dose is 300 mg, with severe depression it can be increased to 600 mg. It is recommended to increase the dose no earlier than 1 week after the start of therapy. When the clinical effect is achieved, the dose is reduced.

Precautions: With caution prescribed for thyrotoxicosis and pheochromocytoma (possible development of hypertensive reactions). It is not recommended for patients in whom arousal is the main clinical manifestation of the disease. With schizophrenic or schizoaffective psychosis, schizophrenic symptoms may increase (it is necessary in this case to switch to antipsychotics). Patients with high blood pressure should refrain from excessive consumption of foods containing tyramine.

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

Contraindications

Hypersensitivity to the drug.

Acute cases of confusion.

Pregnancy, breast-feeding (stop for the duration of treatment).

Children, since there is no clinical experience with the use of the drug in them. Co-administration of moclobemide with selegiline.

Dosage and administration

It is applied inside, after eating.

The initial dose is 300 mg per day, in two or three divided doses.

In severe depression, the dose may be increased to 600 mg per day as needed. It is recommended to increase the dose no earlier than 1 week after the start of therapy. When the clinical effect is achieved, the dose is reduced.

In severe disorders of hepatic metabolism, the daily dose of moclobemide should be reduced to half or one third.

Minimum dose: 1 tablet x 2 times a day = 300 mg.

Average dose: 2 tablets in the morning + 1 tablet in the afternoon = 450 mg.

Maximum dose: 2 tablets x 2 times a day = 600 mg.

Release form

Tablets of 150 and 300 mg.

Side effects

From the nervous system and sensory organs

Dizziness, headache, sleep disturbance, agitation, anxiety, irritability, confusion, paresthesia, blurred vision.

From the digestive tract

Dry mouth, nausea, heartburn, fullness, diarrhea/constipation.

Other

Skin reactions (rash, itching, urticaria, hot flashes).

Cautions

For patients in whom arousal or agitation is the main clinical manifestation of the disease, moclobemide is either not given or given in combination with a sedative (eg, a drug from the benzodiazepine group).

Patients with suicidal tendencies, patients with schizophrenic symptoms or schizoaffective disorders, patients with thyrotoxicosis or pheochromacytoma should be carefully observed. Co-administration of moclobemide with clomipramine or dextromethorphan should be avoided. In pregnant women and nursing mothers, the benefit of treatment should be weighed against the possible risk to the fetus and child. Patients with high blood pressure should refrain from excessive consumption of foods containing tyramine.

Interaction with other drugs

Cimetidine slows down the metabolism of moclobemide.

Treatment with tricyclic or other antidepressants can be started immediately after withdrawal, i.e. without waiting period, the same is valid for the opposite case.

Enhances and prolongs the effect of sympathomimetics and opiates.

Increases the likelihood of adverse reactions from the central nervous system when combined with clomipramine, dextromethorphan.