Release form
Moclobemide is produced by various trading companies. It is always produced in the form of tablets. The dosage of the active substance in one tablet is 150 mg or 300 mg. The package can contain 30, 100 or 500 tablets. The dosage of the drug is indicated on the packaging.
There is a complete analogue of moclobemide - the drug Aurorix . The latter has the same active ingredient - moclobemide - and differs only in its release under a different trade name. There are no other complete analogues of the product.
pharmachologic effect
Moclobemide is an antidepressant whose mechanism of action is based on the reversible inhibition of monoamine oxidase type A. Monoamines are substances that are responsible for transmitting information about a good mood between nerve cells. The more of these mediators, the better a person’s mood and less anxiety. Monoamines include norepinephrine, dopamine and serotonin.
Depression and phobias occur when there are not enough of these mediators in the brain. Monoamine oxidase (MAO) is an enzyme that breaks down monoamines. MAO type A destroys serotonin and norepinephrine, MAO type B destroys dopamine. Moclobemide blocks MAO type A, thereby increasing the concentration of serotonin and norepinephrine in brain cells. This helps improve mood and reduce anxiety.
special instructions
The drug should be taken with extreme caution in patients who suffer from thyrotoxicosis. Due to limited clinical studies, Moclobemide should not be used in patients with schizophrenia or other psychiatric diseases, unless otherwise indicated in the instructions or recommended by the attending physician.
You should also monitor the behavior of suicidal patients, especially at the beginning of treatment
Due to limited clinical studies, Moclobemide should not be used in patients with schizophrenia or other psychiatric diseases, unless otherwise indicated in the instructions or recommended by the attending physician. You should also monitor the behavior of suicidal patients, especially at the beginning of treatment.
The medicine is not prescribed in childhood, since no research has been conducted on this topic.
In addition, the drug has a negative effect on the reaction
Therefore, during the course of therapy, you should refrain from driving a car or operating other mechanisms, as well as from any dangerous types of work that require constant concentration and increased attention.
Patients with suicidal tendencies, symptoms of schizophrenia or schizoaffective disorders, as well as patients with pheochromacyotoma and thyrotoxicosis should be carefully monitored.
During pregnancy and breastfeeding, medication is prescribed in extreme cases, after weighing all the pros and cons of such treatment.
Indications
Moclobemide is most often used in the practice of psychiatrists and psychotherapists. Its appointment is justified in the following cases:
- Depressive episode of any severity;
- Recurrent depressive disorder;
- Bipolar affective disorder, current episode of depression;
- Symptomatic decrease in mood due to other diseases;
- Persistent decline in mood in old age;
- Anxiety phobic disorder.
The drug is often used to treat depression as a separate pathology and as a symptom of other diseases.
There are two types of anxiety-phobic disorder for which moclobemide has proven effective: social phobia and agoraphobia. Social phobia is the fear of interacting with other people. Agoraphobia is the fear of open areas and crowded spaces. In both diseases, moclobemide can reduce anxiety and help overcome fear.
Drug interactions
During therapy, it is not recommended to consume foods high in tyramine.
When using the drug together with Cimetidine, the standard dose must be reduced by 2 times. It is not permissible to use Aurorix in combination with Selegiline, as well as serotonin reuptake inhibitors. Before using Moclobemide after completing a course of therapy with serotonin reuptake inhibitors, you need to follow a certain interval that will be equal to five half-lives of SSRIs from the body.
The drug does not need to be taken together with dextromethorphan, which is present in many cough suppressants.
It is also necessary to avoid the combined use of Aurorix with ephedrine, pseudoephedrine, phenylpropanalamine
Use with great caution together with drugs that can increase serotonin levels in the body - morphine, fentanyl
The use of Aurorix helps improve and prolong the effect of adrenal stimulants, Ibuprofen and opiates. Moclobemide increases the vasoconstrictor effect of tyramine, which is found in food, so it is advisable to remove it from the diet.
The drug should not be combined with Clomipramine, as the chance of serious reactions from the central nervous system will increase. Therapy with tricyclic antidepressants can be carried out immediately after discontinuation of Aurorix.
Dextromethorphan increases the risk of serious CNS side effects.
Drinking alcoholic beverages during the course of therapy is strictly prohibited!
Side effects
The side effect of the drug is associated with its effect on norepinephrine and serotonin, which, in addition to influencing the emotional sphere, have a number of other functions. Common side effects of moclobemide include dizziness, headache, nausea, insomnia, or drowsiness. At the beginning of treatment, many patients experience a decrease in the production of saliva and tear secretion, a feeling of dryness in the oral and nasal cavities, and dry eyes. Gradually these symptoms disappear.
Less common side effects include constipation, epigastric pain, agitation, hand tremors, and transient visual disturbances. In patients with bipolar affective disorder, exceeding the recommended dosage may cause a phase change to manic. Patients with schizophrenia may develop paranoid syndrome during treatment.
AURORIX
| Film-coated tablets | 1 tab. |
| moclobemide | 150 mg |
10 pieces. – contour cell packaging (3) – cardboard packs.
pharmachologic effect
Antidepressant, selective inhibitor of MAO type A. Inhibits mainly the metabolism of serotonin, 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 psychostimulating properties: improves mood, increases mental and motor activity, and increases the ability to concentrate. Improves sleep in patients suffering from depression and sleep disorders.
In terms of effectiveness for typical endogenous depression, 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 suppressed by 60-80%.
Pharmacokinetics
After oral administration, moclobemide is completely absorbed from the gastrointestinal tract. Subject to a “first pass” effect through the liver. Cmax in plasma is achieved 1 hour after oral administration.
Moclobemide is widely distributed in the body. Vd is about 1.2 l/kg. Binding to plasma proteins, 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, plasma Cmax and AUC values in slow metabolizers may be 1.5 times higher than in extensive metabolizers.
T1/2 is 1-4 hours. Plasma clearance is about 20-50 l/hour. 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.
From the central nervous system and peripheral nervous system:
feeling of 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.
Other:
increased sweating.
Drug interactions
When used simultaneously with drugs that increase serotonin levels, there is a possibility of developing serotonin syndrome.
In experimental studies, moclobemide potentiated the effects of opioid agonists.
When used simultaneously with dextropropoxyphene, moderate agitation may develop; with zolmitriptan - increased plasma Cmax and AUC of zolmitriptan; with clomipramine – cases of serotonin syndrome have been described; with levodopa – possible headache, nausea, insomnia; with selegiline – increased sensitivity to tyramine; with sumatriptan – increasing the bioavailability of sumatriptan; 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 concomitant schizophrenia or schizoaffective organic brain diseases.
It is necessary to monitor the condition of patients with suicidal tendencies when starting treatment with moclobemide.
During treatment with moclobemide, you should not eat large amounts of foods containing tyramine.
When used simultaneously with cimetidine, the usual dose of moclobemide should be reduced by 2 times.
It should not be used simultaneously with selegiline and serotonin reuptake inhibitors. Before using moclobemide after finishing 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 used concomitantly with dextromethorphan, which is included in many antitussive drugs.
Avoid simultaneous use with ephedrine, pseudoephedrine, and phenylpropanolamine.
Use with caution simultaneously with drugs that increase serotonin levels; with morphine, fentanyl (dosage regimen adjustment may be required).
Due to the lack of sufficient clinical experience, it should not be used in pediatrics.
Impact on the ability to drive vehicles and operate machinery
During the treatment period, it is recommended to refrain from potentially hazardous activities associated with the need for concentration and increased speed of psychomotor reactions.
Pregnancy and lactation
Contraindicated during pregnancy and lactation.
There have been no adequate and strictly controlled studies of the safety of moclobemide during pregnancy in humans. Experimental studies have not revealed a negative effect of moclobemide on the fetus.
Moclobemide is excreted into breast milk in small concentrations - approximately 1/30 of the maternal dose.
Use in childhood
Contraindicated in children.
The description of the drug AURORIX is based on the officially approved instructions for use and approved by the manufacturer.
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Source: https://health.mail.ru/drug/moclobemide/
Instructions for use
The drug is taken after meals with a small amount of water. The initial dosage of moclobemide is 300 mg per day. The required dose is divided into two doses - one tablet in the morning and one in the evening. Then the concentration of the product is gradually increased.
After just a week, it is recommended to reach an average dose of 450 mg. In this case, two tablets of 150 mg are taken in the morning, one in the same dosage in the evening. After a few more days, you can increase the concentration to 600 mg. In this dosage, the drug is taken twice a day, 150 mg.
When treating anxiety-phobic disorder, it is recommended to start with 300 mg in two doses, and on the fourth day of treatment increase the dose to 600 mg. The duration of the course of therapy is regulated by the attending physician.
Moclobemide
Moclobemide
Moclobemide
- an antidepressant, selectively and reversibly inhibits MAO type A, inhibits the metabolism of serotonin (mainly), norepinephrine and dopamine, causing their accumulation in the synaptic cleft.
Possessing an antidepressant effect, it improves mood and concentration, eliminates increased fatigue, dysphoria, nervous exhaustion, psychomotor retardation, and improves sleep. The optimal antidepressant effect develops when MAO is suppressed by 60–80%.
The effect manifests itself by the end of the 1st week of treatment, usually already in the first days of administration a pronounced activating effect is noted. Does not have a negative effect on the reaction rate.
After oral administration, it is quickly and completely absorbed from the gastrointestinal tract. Maximum plasma concentration (Cmax) is achieved 1 hour after oral administration.
Distribution
Equilibrium concentration (Css) is created by the end of 1 week of treatment. Bioavailability (depending on the dose taken) is 40–80%. Moclobemide is widely distributed in the body. The volume of distribution (Vd) is approximately 1.2 l/kg. Communication with plasma proteins (albumin) - 80%.
Biotransformation
Metabolized in the liver during oxidative reactions by isoenzymes CYP2C9 and CYP2D6. At the same dose of moclobemide in persons with slow metabolism, plasma Cmax and AUC values ( Area Under Curve
- area under the concentration-time curve) can be 1.5 times higher than in individuals with intensive metabolism.
Removal
The half-life (T½) is 1–4 hours. General clearance - 20–50 l/h. It is excreted by the kidneys mainly in the form of metabolites, less than 1% - unchanged.
- Depression of various etiologies (with manic-depressive psychosis, various forms of schizophrenia, chronic alcoholism, senile and involutional, reactive and neurotic);
- social phobia.
- Hypersensitivity to moclobemide;
- acute conditions accompanied by “confusion” of consciousness;
- states of agitation, excitement;
- pheochromocytoma;
- pregnancy;
- breast-feeding;
- childhood.
- Thyrotoxicosis;
- simultaneous use with drugs that increase serotonin levels; with morphine, fentanyl (dosage regimen adjustment may be required).
FDA category of effect on the fetus is N.
Adequate and strictly controlled studies on the safety of moclobemide during pregnancy have not been conducted.
Animal reproduction studies have not revealed any negative effects of moclobemide on the fetus.
Use during pregnancy is contraindicated, except in cases of extreme necessity, when the expected benefit of therapy for the mother outweighs the potential risk to the fetus.
Use during breastfeeding
No special studies have been conducted on the safety of moclobemide during breastfeeding.
Moclobemide is excreted in breast milk in small concentrations - approximately 1/30 of the dose received by the mother.
It is necessary to stop breastfeeding if you use the drug.
For adults, when taken orally, the initial dose is 300 mg/day in 3 divided doses. In severe depressive conditions and ineffective therapy, after 7 days the daily dose can be increased to 600 mg. The duration of treatment is determined individually.
If the effect is obtained, the dose can be reduced to 150 mg/day. If you have liver disease or are taking medications that are inhibitors of microsomal enzymes, the dose of the drug should be reduced by 30–50% of the average therapeutic dose.
Social phobia: 600 mg/day in 2 doses, initial dose - 300 mg/day, from day 4 the dose is increased to 600 mg/day. Taking 300 mg/day for more than 3 days is not recommended.
Strengthens and prolongs the effect of adrenergic stimulants, opiates and ibuprofen.
Strengthens the vasoconstrictor effect of tyramine contained in food products, which (if possible) requires its exclusion from the diet.
It is not recommended to combine with clomipramine (the likelihood of severe reactions from the central nervous system increases).
Treatment with tricyclics and other antidepressants can be started immediately after discontinuation of moclobemide.
Does not change the pharmacodynamics and pharmacokinetics of indirect anticoagulants, digoxin and ethanol.
Cimetidine and other microsomal oxidation inhibitors slow down metabolism.
Dextromethorphan increases the risk of severe side effects from the central nervous system.
Concomitant use of selegiline is contraindicated.
In patients with schizophrenia, it can cause aggravation of the course of the disease (prescription is possible only under the guise of antipsychotic drugs).
Against the background of thyrotoxicosis or pheochromocytoma, as well as in patients with initially high blood pressure (especially those receiving large amounts of tyramine from food), a significant increase in blood pressure is possible.
During treatment with moclobemide, you should not eat large amounts of foods containing tyramine.
When used simultaneously with cimetidine, the usual dose of moclobemide should be reduced by 2 times.
It should not be used simultaneously with selegiline and serotonin reuptake inhibitors. Before using moclobemide after finishing 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 used concomitantly with dextromethorphan, which is included in many antitussive drugs.
Avoid simultaneous use with ephedrine, pseudoephedrine, and phenylpropanolamine.
During the treatment period, it is recommended to refrain from potentially hazardous activities associated with the need for concentration and increased speed of psychomotor reactions.
Information about the active substance Moclobemide is intended for medical and pharmaceutical professionals for informational purposes only. The instructions are not intended to be a substitute for professional medical advice, diagnosis or treatment. The information contained here may change over time. The most accurate information about the use of drugs containing the active substance Moclobemide is contained in the manufacturer's instructions included with the package.
Source: https://medum.ru/moklobemid
Reviews
Oleg S .: “I have suffered from agoraphobia since childhood. At first I was only afraid of large squares, stadiums, and busy streets. Gradually the disease progressed, and over time it became difficult for me to simply leave the house and go outside. Then I realized that I needed to see a doctor. I was treated with moclobemide, taking 600 mg twice a day. I began to notice a decrease in fear after two weeks. Now I continue to take the drug and walk around the city calmly.”
Doctor's review : “Moclobemide is an antidepressant from the group of MAO inhibitors. Its advantage lies in its simultaneous antidepressant and anti-anxiety effects. Moclobemide is often used in patients with various combinations of depression and anxiety disorders. The advantage of the drug is its effectiveness, good tolerability and relative safety.”
Content
Point of view
Most often, Aurorix is taken by patients with sophiophobia or depression, and judging by the reviews, some are very pleased with the result, but there are also those who did not see the proper therapeutic effect.
I use 400 mg per day. I don’t feel drowsiness and apathy, as it seems to me it’s more serotonin. I don’t notice any extra motivation for anything yet. But overall I feel a little better.
Alexey, 31
She was treated for social phobia for about 3 years. It got better, socialization seemed to be a success. I haven’t used it for 2 years now, but it hasn’t gotten any worse.
Alina, 21
