Melipramine
Melipramine: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Melipramin
ATX code: N06AA02
Active ingredient: imipramine (imipramine)
Manufacturer: CJSC Pharmaceutical Plant EGIS (Hungary)
Description and photo update: 2019-26-08
Prices in pharmacies: from 229 rubles.
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Melipramine is a drug with an antidepressant effect.
Release form and composition
Dosage forms of release:
- Film-coated tablets: red-brown, biconvex, round, with a matte surface, almost odorless or odorless (50 pcs. In dark glass bottles, 1 bottle in a cardboard box);
- Dragee: lenticular, brown, with a shiny surface, almost no or odorless (50 pieces in dark glass bottles, 1 bottle in a cardboard box);
- Solution for intramuscular administration: transparent, slightly colored (a greenish-yellow tint is possible) or colorless, odorless (2 ml each in colorless glass ampoules, 5 ampoules in blisters, 2 packages in a cardboard box).
Each pack also contains instructions for the use of Melipramine.
The composition of 1 tablet includes:
- Active ingredient: imipramine - 25 mg (as hydrochloride);
- Auxiliary components: talc - 3 mg, lactose monohydrate - 110.5 mg, povidone K25 - 7 mg, magnesium stearate - 1.5 mg, crospovidone - 3 mg;
- Sheath: hypromellose - 2.61 mg, dimethicone (E1049) 39% - 0.35 mg, red-brown cosmetic dye (mixture: dye iron oxide red, yellow and black) - 0.8 mg, magnesium stearate - 0.24 mg.
The composition of 1 tablet contains:
- Active ingredient: imipramine - 25 mg (as hydrochloride);
- Auxiliary components: gelatin, titanium dioxide (E171), glycerol 85%, macrogol 35,000, dye (E172) (red iron oxide), magnesium stearate, sucrose, talc, lactose monohydrate.
The composition of 1 ampoule (2 ml) includes:
- Active ingredient: imipramine - 25 mg (as hydrochloride);
- Auxiliary components: ascorbic acid, sodium disulfite, anhydrous sodium sulfite, sodium chloride (for parenteral dosage forms), water for injection.
Pharmacological properties
Pharmacodynamics
The active substance of Melipramine is imipramine, a dibenzoazepine derivative, a tricyclic antidepressant. The mechanism of its action is explained by the ability to inhibit the synaptic reuptake of serotonin and norepinephrine released during neuron stimulation. As a result, noradrenergic and serotonergic impulse transmission is facilitated.
Also imipramine blocks m-cholinergic receptors and H 1 -histamine receptors, due to which it has anticholinergic and moderate sedative effects.
The antidepressant effect of Melipramine develops gradually. The optimal therapeutic effect is achieved within 2-4 (possibly 6-8) weeks of therapy.
Pharmacokinetics
Once in the gastrointestinal tract, imipramine is well absorbed. Food, when taken simultaneously, does not affect the absorption of the substance.
The drug is extensively metabolized during the first passage through the liver with the formation by demethylation of the main pharmacologically active metabolite of desipramine (dimethyl-imipramine).
Plasma concentrations of both substances are characterized by high individual variability. After 10 days of taking Melipramine 3 times a day at a dose of 50 mg, the plasma concentration of imipramine in an equilibrium state can vary in the range of 33–85 ng / ml, desipramine - 43–109 ng / ml.
In elderly patients, the concentration of the drug in the blood plasma is usually higher than in younger people, which is explained by a decrease in metabolism.
The apparent volume of distribution of imipramine is 10–20 l / kg. Penetrates through the placental barrier, excreted in breast milk.
Imipramine and desipramine are highly protein bound - 60–96% and 73–92%, respectively.
Imipramine is excreted mainly in the form of inactive metabolites: by the kidneys - about 80%, through the intestines - about 20%. Excretion of unchanged imipramine and its active metabolite is no more than 6% of the dose taken.
The half-life of imipramine after a single dose is on average about 19 hours, can vary from 9 to 28 hours, and significantly increases in case of overdose and in the elderly.
Indications for use
- All forms of depression (with and without anxiety), including depressive conditions, major depression, depressive phase of bipolar disorder, atypical depression;
- Panic disorder;
- Nocturnal urinary incontinence in children from 6 years of age (for short-term adjuvant therapy after excluding organic causes).
Contraindications
- Violation of intracardiac conduction;
- Recently transferred myocardial infarction;
- Manic episodes;
- Heart rhythm disorder;
- Severe violations of liver and / or kidney function;
- Closed-angle glaucoma;
- Retention of urine;
- Galactose intolerance, congenital lactase deficiency, galactose and glucose malabsorption syndrome;
- Simultaneous use with monoamine oxidase inhibitors;
- Age up to 18 years (depression and panic disorder) and up to 6 years (therapy for bedwetting);
- Pregnancy and lactation;
- Hypersensitivity to the components of Melipramine or other tricyclic antidepressants from the dibenzoazepine group.
Melipramine, instructions for use: method and dosage
Tablets and pills
Melipramine is taken orally.
The dosage regimen is determined by the doctor individually and depends on the degree and nature of the symptoms. As a rule, it takes at least 2-4 weeks to achieve a therapeutic effect (in some cases, up to 8 weeks). Therapy should be started with low doses of Melipramine, gradually increasing them to select the minimum effective maintenance dose. Particular care should be taken when titrating the dose in children, adolescents and elderly patients.
The recommended dosage regimen for Melipramine in the treatment of depression:
- 18-60 years old (outpatient treatment): standard single dose - 25 mg, frequency of administration - 1-3 times a day. If necessary, it is possible to gradually increase the dose to 150-200 mg per day (by the end of the first week). The standard maintenance daily dose is 50-100 mg;
- 18-60 years old (inpatient treatment): the initial daily dose in especially severe cases is 75 mg. It is possible to increase it by 25 mg per day up to 200 mg (in exceptional cases - up to 300 mg);
- Patients from 60 years of age: Treatment should be started with the lowest possible doses, since patients in this age group may have a pronounced response to the above doses. The initial dose can be gradually (over 10 days) increased to 50-75 mg per day (it is not recommended to increase it in the future).
Patients with panic disorder have an increased incidence of side effects, so therapy should be started with the lowest possible dose. At the beginning of treatment, there may be a transient increase in anxiety, which can be prevented or stopped with benzodiazepines (as their dose improves, they gradually decrease). The daily dose of Melipramine is gradually increased to 75-100 mg (in some cases, up to 200 mg). The minimum duration of therapy is six months. At the end of treatment, it is recommended to cancel the drug gradually.
Children from 6 years of age with panic disorders are prescribed Melipramine only as a temporary adjuvant therapy for nocturnal enuresis after excluding organic pathology. Recommended dosing regimen (daily dose):
- 6-8 years (body weight 20-25 kg) - 25 mg;
- 9-12 years old (body weight 25-35 kg) - 25-50 mg;
- From 12 years old (body weight from 35 kg) - 50-75 mg.
The use of higher doses is possible only in cases where a satisfactory response to therapy is not observed after 7 days of taking Melipramine. The maximum daily dose is 2.5 mg / kg.
Melipramine is recommended to be taken once after a meal in the evening (before bedtime). In cases when nocturnal enuresis is noted in the early evening hours, the daily dose can be divided into 2 doses (day and night). The duration of the course should not exceed 3 months. The maintenance dose can be reduced (depending on changes in the clinical picture of the disease). After completion of treatment, Melipramine should be withdrawn gradually.
Solution for intramuscular injection
Melipramine can only be administered intramuscularly.
The initial single dose is 25 mg, the frequency of use is 3 times a day. If necessary, it is possible to increase the dose up to a maximum of 100 mg.
After 6 days of treatment, the dose is gradually reduced, replacing one injection with the oral form of the drug. After 12 days, the patient is completely transferred to oral administration of Melipramine (4 times a day, 25 mg).
In the event of a relapse of the disease, it is possible to reapply the drug in the form of a solution for intramuscular administration.
Side effects
The side effects listed below are not necessarily observed in all patients. Some of them are difficult to distinguish from signs of depression (for example, agitation, fatigue, anxiety, sleep disturbance, dry mouth), others are dose-dependent and disappear when it is reduced or spontaneously during therapy.
It should be borne in mind that the occurrence of severe mental or neurological reactions requires a temporary cancellation of Melipramine.
Elderly patients in particular are sensitive to neurological, m-anticholinergic, cardiovascular or mental effects. The ability to eliminate and metabolize Melipramine in them may be reduced, which increases the risk of increasing plasma concentrations of the active substance.
During therapy, the following disorders may develop (≥1 / 10 - very often; ≥1 / 100 and <1/10 - often; ≥1 / 1000 and <1/100 - infrequently; ≥1 / 10,000 and <1/1000 - rarely; <1/10 000 - very rarely; if it is impossible to estimate the frequency of occurrence from the available data - with an unknown frequency):
- Central nervous system: very often - tremor; often - headache, paresthesia, dizziness, disorientation, hallucinations, delirious confusion (especially in elderly patients with Parkinson's disease), transition from depression to mania or hypomania, anxiety, agitation, sleep disturbances, increased anxiety, insomnia, fatigue, violations of potency and libido; infrequently - activation of psychotic symptoms, convulsions; rarely - ataxia, extrapyramidal symptoms, myoclonus, aggressiveness, speech disorders;
- Cardiovascular system: very often - changes in the electrocardiogram and sinus tachycardia (of no clinical significance) in patients with normal heart function, hot flashes, orthostatic hypotension; often - arrhythmias, conduction disturbances (blockade of the His bundle, widening of the PR interval and QRS complex), palpitations; rarely - increased blood pressure, decompensation of cardiac activity, peripheral vasospastic reactions;
- Endocrine system: rarely - galactorrhea, enlargement of the mammary glands, syndrome of inadequate secretion of antidiuretic hormone, change (decrease or increase) in the concentration of glucose in the blood plasma;
- Digestive system: very often - dry mouth, constipation; often - vomiting, nausea; rarely - lesion of the tongue, paralytic ileus, stomatitis, indigestion, hepatitis not accompanied by jaundice;
- Urinary system: often - urination disorders;
- Hematopoietic system: rarely - leukopenia, eosinophilia, agranulocytosis, purpura and thrombocytopenia;
- The organ of hearing and vision: very often - blurred vision, violation of accommodation; rarely - mydriasis, glaucoma; with an unknown frequency - ringing in the ears;
- Skin: very often - increased sweating; often - allergic skin reactions (in the form of urticaria, skin rash); rarely - generalized or localized edema, hair loss, photosensitivity, petechiae, itching;
- Metabolism and nutrition: very often - weight gain; often - anorexia; rarely - weight loss;
- Laboratory tests: often - an increase in the activity of transaminases;
- Other: rarely - weakness, hyperpyrexia, systemic anaphylactic reactions, including a decrease in blood pressure, allergic alveolitis (pneumonitis), with or without eosinophilia; in patients over 50 years old - an increase in the frequency of bone fractures.
During therapy and in the early stages after discontinuation of Melipramine, cases of suicidal behavior and suicidal thoughts have been reported.
Overdose
Possible symptoms of Melipramine overdose:
- from the central nervous system: muscular rigidity, increased reflexes, stupor, lethargy, dizziness, agitation, anxiety, ataxia, chorea-like and athetoid movements, convulsions, coma;
- from the cardiovascular system: conduction disturbances, arrhythmia, tachycardia, decreased blood pressure, heart failure, shock; extremely rare - cardiac arrest;
- other: cyanosis, fever, mydriasis, sweating, vomiting, anuria or oliguria, respiratory depression.
Overdose symptoms may occur within 4-6 days. Children are more sensitive to acute overdose than adults, so it should be considered more dangerous and potentially lethal in childhood.
If an overdose is suspected, the patient should be immediately hospitalized and monitored in the hospital for at least 72 hours. Imipramine has no specific antidote; treatment is aimed primarily at eliminating the symptoms that have arisen and maintaining the functions of vital body systems.
Due to the m-anticholinergic effect of Melipramine, gastric emptying may be delayed (by 12 hours or more), therefore, it is necessary to induce vomiting as soon as possible (if the patient is conscious) or install a gastric tube and inject activated charcoal. Cardiovascular activity, blood gas and electrolyte composition should be continuously monitored.
As symptomatic therapy, the following can be prescribed:
- the use of anticonvulsants (intravenous diazepam, muscle relaxants, inhalation anesthetics, phenobarbital);
- intravenous drip of plasma-replacing fluids, dobutamine or dopamine;
- installation of a temporary pacemaker;
- artificial lung ventilation;
- cardiopulmonary resuscitation (rarely required).
Hemodialysis, peritoneal dialysis, and forced diuresis are ineffective.
It is not recommended to use physostigmine in case of an overdose of Melipramine, since it can cause asystole, severe bradycardia, and epileptic convulsions.
special instructions
Before starting therapy and regularly during the use of Melipramine, it is recommended to monitor such indicators as:
- Blood pressure (especially in patients with arterial hypotension or unstable blood circulation);
- Peripheral blood indicators (with laryngitis or fever, control should be carried out immediately, since these symptoms may indicate the development of agranulocytosis and leukopenia; in other cases, the indicators are monitored before starting therapy and regularly during its course);
- Liver function (especially in liver disease);
- Electrocardiogram (for heart disease and in the elderly).
Depression is associated with an increased risk of suicidal ideation, suicide, and self-harm. This risk usually persists until significant remission occurs. Since an improvement in the condition is observed several weeks after the start of treatment, the patient's condition must be carefully monitored. The risk of suicide, according to clinical experience, may be increased in the early stages of recovery. In children and young people under 24, the frequency of suicides increases.
Other mental conditions in which the use of Melipramine is indicated may also be associated with a high risk of suicidal events. In this regard, when prescribing the drug for other indications, the above precautions should also be observed.
In the presence of a history of suicidal events or with significantly pronounced suicidal ideation, careful monitoring of the condition must be carried out before starting treatment.
If clinical deterioration or unusual changes in behavior appear, you should immediately consult a specialist.
Abrupt withdrawal of Melipramine can lead to the development of withdrawal symptoms (in the form of nausea, headache, fatigue, anxiety, anxiety, sleep disorders, arrhythmias, extrapyramidal symptoms), therefore, treatment must be withdrawn gradually.
In patients with bipolar depression, Melipramine may contribute to the development of mania; the drug should not be used during manic episodes.
Imipramine lowers the threshold of convulsive readiness, therefore, in case of epilepsy and spasmophilia or a history of epilepsy, careful medical supervision and adequate anticonvulsant therapy should be carried out.
During treatment, it is necessary to take into account the likelihood of developing serotonin syndrome.
Melipramine increases the risk associated with electroconvulsive therapy, and therefore it is not recommended to use the drug in electroconvulsive therapy.
In patients with panic disorder, anxiety may increase in the first few days of therapy. As a rule, this disorder resolves spontaneously within 1-2 weeks of therapy, if necessary, benzodiazepine derivatives may be prescribed for its treatment.
With psychosis, at the beginning of drug therapy, there may be an increase in anxiety, agitation and anxiety.
Careful medical supervision is required when prescribing Melipramine for glaucoma, severe constipation, prostatic hyperplasia (therapy can lead to an increase in the severity of these symptoms).
Caution must be observed when prescribing Melipramine to patients with coronary heart disease, diabetes mellitus, functional disorders of the kidneys and liver, adrenal tumors.
Decreased production of tear fluid in patients who use contact lenses can lead to the accumulation of mucous secretions and damage to the corneal epithelium.
When using Melipramine in patients with hyperthyroidism and patients using thyroid hormones, careful medical supervision is necessary, which is associated with an increased risk of developing adverse reactions from the cardiovascular system.
Before carrying out surgery, the anesthesiologist must be informed about taking Melipramine.
In some cases, during treatment, the development of leukopenia, eosinophilia, agranulocytosis, purpura, thrombocytopenia was observed (regular monitoring of blood counts should be carried out).
Long-term therapy with antidepressants can lead to the development of dental caries, and therefore it is recommended to conduct regular check-ups with the dentist.
In young and elderly patients, the side effects of Melipramine may be more severe, therefore, especially at the beginning of treatment, they should be prescribed lower doses.
Melipramine can cause photosensitivity; exposure to intense sunlight should be avoided during therapy.
In the presence of a predisposition and / or in elderly patients, imipramine can cause delirious (m-anticholinergic) syndrome, which stops within several days after discontinuation of Melipramine.
It is prohibited to consume alcoholic beverages during treatment.
Influence on the ability to drive vehicles and complex mechanisms
At the beginning of the use of Melipramine, driving a car and working with mechanisms is prohibited. The doctor determines the duration of these restrictions individually.
Application during pregnancy and lactation
During pregnancy, the use of Melipramine is contraindicated, since there are known cases of intrauterine fetal development disorders under the influence of tricyclic antidepressants.
Imipramine passes into breast milk, therefore, the drug is contraindicated in women who are breastfeeding.
Pediatric use
For panic disorder and depression, Melipramine should not be used under the age of 18.
With bedwetting (in the absence of organic pathology), the drug is prescribed only from the age of 6, since in younger patients there is not enough clinical experience with imipramine. Melipramine is used in accordance with age recommendations for the dosage regimen, preferably in the lowest dose from the specified dose range. Increasing the dose is possible only in cases where, after 1 week of treatment with the drug in low doses, there is no satisfactory clinical response to therapy. The maximum permissible daily dose for children is 2.5 mg / kg of body weight.
With impaired renal function
Melipramine should be used with caution in patients with impaired renal function.
In severe renal failure, the drug is contraindicated.
For violations of liver function
Melipramine should be used with caution in patients with impaired liver function.
In severe hepatic impairment, the drug is contraindicated.
Use in the elderly
Elipramine should be used with caution in elderly patients. It should be borne in mind that in patients of this category, imipramine can cause the development of m-anticholinergic (delirious) syndrome. It stops within a few days after stopping therapy.
Prescribing Melipramine, especially at the beginning of treatment, is recommended in low doses, since side effects in the elderly can be more severe.
Drug interactions
When Melipramine is used together with certain drugs, the following effects may occur:
- Inhibitors of liver microsomal enzymes (including methylphenidate, cimetidine, phenothiazines, other antidepressants, flecainide, propafenone): a decrease in the metabolism of imipramine and an increase in its concentration in blood plasma;
- Monoamine oxidase (MAO) inhibitors: enhancement of peripheral noradrenergic effects with the possible achievement of toxic levels, manifested by the development of hypertensive crisis, hyperpyrexia, myoclonus, agitation, seizures, delirium, coma (the combination is recommended to be avoided, the use of Melipramine can be started 3 weeks after the end of therapy with MAO inhibitors, after applying moclobemide, an interval of 24 hours is sufficient; the same scheme should be followed when prescribing MAO inhibitors after Melipramine);
- Oral contraceptives, estrogens: a decrease in the effectiveness of Melipramine, the development of its toxic effects (joint administration requires caution and dose adjustment of one of the drugs);
- Antipsychotic drugs: an increase in the concentration of Melipramine in the blood plasma and, accordingly, its side effects (a dose reduction may be required);
- Inducers of microsomal liver enzymes (barbiturates, meprobamate, nicotine, alcohol, antiepileptic drugs, etc.): increased metabolism of imipramine and a decrease in its concentration in blood plasma and, accordingly, the antidepressant effect;
- Drugs that depress the central nervous system (narcotic analgesics, barbiturates, benzodiazepines, drugs for general anesthesia, alcohol): a pronounced increase in the effects and side effects of these drugs;
- Medicines with m-anticholinergic properties (blockers of H 1 -histamine receptors, phenothiazines, atropine, drugs for the treatment of parkinsonism, biperiden): increased antimuscarinic effects and side effects (when used together, monitoring the patient's condition and careful selection of doses is required);
- Thyroid hormone preparations: increasing the antidepressant effect of Melipramine and its side effects on the heart (the combination requires caution);
- Sympathomimetics: enhancing their cardiovascular effects;
- Sympatholytics: decrease in antihypertensive action;
- Quinidine: increased risk of conduction disturbances and arrhythmias (simultaneous use with class Ia antiarrhythmic drugs is not recommended);
- Phenytoin: a decrease in its anticonvulsant effect;
- Hypoglycemic agents: change in the concentration of glucose in the blood plasma (at the beginning of treatment, at the end of treatment and changes in the dosage regimen, it is necessary to monitor the concentration of glucose in the blood);
- Indirect anticoagulants: an increase in their half-life, which increases the risk of bleeding (combined use is possible under close medical supervision and control of prothrombin content).
Analogs
Analogues of Melipramine are: Ketilept, Anafranil, Tranquezipam, Phenobarbital, Vernison, Bromizoval.
Terms and conditions of storage
Keep out of reach of children at a temperature of 15-25 ° C.
Shelf life:
- Film-coated tablets, pills - 3 years;
- Solution for intramuscular injection - 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Melipramine
Patients leave mostly positive reviews about Melipramine on various thematic forums and sites. The drug is used for various indications: for depression, panic disorder, obsessive-compulsive disorder. The effect of the intake develops gradually, so a pronounced effect is noted only a few weeks after the start of therapy.
There are many reports from parents whose children have been prescribed Melipramine for the treatment of nocturnal enuresis. The reviews are mostly positive.
The negative statements contain complaints about the development of side effects, the most common of which are drowsiness and nausea. However, most patients note that negative reactions are moderately expressed and disappear on their own after a dose reduction.
The cost of the drug is generally estimated to be affordable.
Price for Melipramine in pharmacies
Approximate prices for Melipramine: 25 mg film-coated tablets, 50 pcs. in the package - 325–388 rubles; dragee 25 mg, 50 pcs. in the package - 336-399 rubles. The cost of the solution is approximately 380 rubles, but at the moment it is not available for sale.
Melipramine: prices in online pharmacies
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Drug name Price Pharmacy |
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Melipramine 25 mg film-coated tablets 50 pcs. 229 r Buy |
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Melipramine tablets p.o. 25mg 50 pcs. 376 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
