Melipramine

Melipramine is an analgesic, antidiuretic and anxiolytic substance; the drug has a sedative, anticholinergic and α-adrenergic blocking effect on the body.

The active element of the drug increases the level of norepinephrine inside the synapses, and in addition increases the serotonin levels inside the central nervous system. This therapeutic effect is realized by slowing down the processes of capturing neurotransmitter molecules located on the presynaptic walls.

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Indications Melipramine

It is used in case of occurrence of such disorders:

• depression of endogenous origin;
• asthenodepressive syndrome;
• depression associated with changes due to menopause;
• depressive states developing in connection with psychopathy or neuroses;
• depression, which has a reactive, alcoholic or involutional form;
• narcolepsy;
• behavioral disorders;
• withdrawal syndrome that occurs after stopping the use of cocaine-containing substances;
• migraine pain;
• panic disorders;
• neuralgia of postherpetic origin;
• chronic pain;
• neuropathy of diabetic origin;
• narcolepsy accompanied by catalepsy;
• stress urinary incontinence and urge to urinate;
• bulimia, which has a nervous nature;
• headaches.

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Release form

The drug is produced in the form of injection liquid (inside 2 ml ampoules, 5 pieces inside a pack), and also in tablets (50 pieces inside a bottle).

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Pharmacodynamics

The drug reduces the speed of ventricular conduction, which helps stop the occurrence of arrhythmia. Long-term use leads to a slowdown in the functional activity of the endings of β-adrenergic receptors and serotonin. The introduction of the drug helps restore the functional balance of serotonergic and adrenergic transmission, the disorders of which cause the occurrence of depression.

Melipramine can block the activity of histamine H2-endings inside gastric cells, reducing acid secretion, and in addition, it has an antiulcer effect. The substance reduces pain in people with ulcers, and also increases the rate of ulcer regeneration, having an m-anticholinergic effect. The anticholinergic effect has a positive effect on the treatment of nocturnal enuresis. The drug increases the extensibility of the bladder walls, as well as the tone of the sphincter.

The analgesic effect of central origin is associated with the effect on monoamine levels and the effect on the opiate ending system. Administration in the case of general anesthesia is considered justified because the drug has hypotonic activity and leads to the development of hypothermia.

No slowing of MAO activity is observed. The effect on α2- and β-adrenergic endings in the locus coeruleus leads to the development of an anxiolytic effect. The drug eliminates movement inhibition, helps to get rid of insomnia, improves mood and stabilizes digestive function.

At the initial stage of treatment, a sedative effect may be observed. Antidepressant drug activity develops after 2-3 weeks of therapy.

Dosing and administration

The drug is taken in the morning or during the day, so as not to lead to the development or strengthening of insomnia. The tablets should be taken with food or after food. At first, 0.075-0.2 g of the substance is used per day. The portion can be gradually increased by 25 mg daily until a daily dosage of 0.2-0.3 g is obtained. The daily portion should be divided into 3-4 uses. The entire cycle lasts 1-1.5 months.

After the therapy cycle, maintenance treatment is performed, during which reduced doses of the drug are used. The dosage is reduced by 25 mg daily. During the maintenance cycle, 0.025-0.1 g of the drug is used per day. The maintenance course lasts no more than 1.5 months. The maintenance dose is taken in the evening.

In outpatient settings, an adult can be administered no more than 0.2 g per day, and in hospital settings, a maximum of 0.3 g.

An elderly person should initially be administered 10 mg of the substance per day. The dosage should be increased to 30-50 mg. Elderly people should not use more than 0.1 g of the drug per day.

Children should take a dose of Melipramine 60 minutes before bedtime (1 time), or divide it into 2 doses, taken during the day and in the evening.

For people aged 6-8 years with depression, 10 mg is prescribed at first, and then the dose is increased to 20 mg. For nocturnal enuresis, 25 mg of the substance is taken per day.

For patients aged 8-14 years in case of depression, 10 mg of the drug is first administered, and then the dosage is increased to 20-25 mg. In case of nocturnal enuresis, a dose of 25-75 mg is required.

For teenagers over 14 years of age, during depression, 10 mg of the substance is initially used, and then the dose is increased to 0.05-0.1 g per day. In case of enuresis, a dose of 50-75 mg is required.

Children are allowed to take no more than 2.5 mg/kg of medication per day.

Use Melipramine during pregnancy

Prescribing imipramine-containing drugs during pregnancy is permitted only in the case of strict indications.

Contraindications

Main contraindications:

• severe hypersensitivity associated with imipramine and excipients of the drug;
• use of MAOIs;
• conduction disorder in the ventricular region of the myocardium;
• myocardial infarction;
• acute ethyl alcohol poisoning;
• breast-feeding;
• sleeping pill intoxication;
• drug poisoning;
• suppression of the central nervous system;
• closed-angle glaucoma.

It should be used with caution in the following disorders:

• BA;
• chronic stage of alcoholism;
• liver or kidney failure;
• neuroblastoma;
• pheochromocytoma;
• cardiac pathologies;
• suppression of hematopoietic processes;
• bipolar disorder;
• vascular diseases;
• stroke;
• gastrointestinal motility disorders;
• hyperthyroidism;
• prostatic hyperplasia accompanied by anuria;
• epilepsy or schizophrenia;
• old age.

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Side effects Melipramine

Side effects of the drug include:

• nightmares, confusion, depersonalization, hallucinations, accommodative paresis, psychosis, insomnia, headaches and delirium, as well as anxiety, impaired attention, dizziness, manic syndrome and drowsiness, as well as psychomotor agitation and hypomanic states. In addition, yawning, tinnitus, disorientation, potentiation of depression, changes in blood pressure values, aggression and orthostatic collapse appear;
• asthenia, arrhythmia, potentiation of epileptic seizures, tachycardia, hypohidrosis, changes in EEG and ECG values, as well as paresthesia, extrapyramidal disorders, ataxia and conduction disorders in the ventricular region of the myocardium;
• heartburn, nausea, diarrhea, dry mouth, paralytic intestinal obstruction, vomiting, as well as constipation, dysarthria, weight change, darkening of the tongue, taste disturbance, stomatitis and gastralgia;
• delay or difficulty in urination or its increase in frequency, swelling of the testicles, hypoproteinemia, changes in libido and weakening of potency;
• glaucoma, blurred vision, and mydriasis;
• eosinophilia, thrombocytopenia or leukopenia and agranulocytosis;
• myoclonus or tremor;
• swelling affecting the face or tongue, itching, purpura, epidermal rashes, photosensitivity, alopecia and urticaria;
• hepatitis, intrahepatic cholestasis and potentiation of ADH release;
• galactorrhea or gynecomastia;
• hyponatremia or -glycemia, as well as hyperglycemia or -pyrexia.

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Overdose

In case of intoxication, anuria, confusion, psychomotor agitation, dry oral mucosa, mydriasis, tachycardia, convulsions, respiratory disorders and coma are observed.

It is necessary to hospitalize the patient in a hospital, where doctors will observe him and conduct symptomatic procedures. Diuresis with dialysis will be ineffective.

Interactions with other drugs

The use of imipramine with adrenergic blockers increases antihypertensive activity.

Administration together with α- or β-adrenergic agonists leads to potentiation of the psychostimulating effect of Melipramine.

Substances containing ethyl alcohol enhance the psychostimulating effect of the drug and increase the intolerance associated with ethanol.

Combination with opiates causes the development of lethargy, which can be dangerous for the patient.

Hormonal contraception potentiates depressive manifestations.

Use in combination with zolpidem enhances the sedative properties of the drug.

The use of MAOIs causes an increase in psychostimulant activity.

The introduction of antihistamines leads to a potentiation of the antihistamine effect.

Combination with antidepressants leads to suppression of the respiratory process and central nervous system function, as well as to a decrease in blood pressure values.

Use of benzodiazepines can result in respiratory depression, low blood pressure, and life-threatening sluggishness.

Delirium may develop when disulfiram is administered.

The use of clozapine results in the development of toxic activity in relation to the central nervous system.

When combined with levodopa, a hypertensive effect develops.

Use with methyldopa weakens its medicinal effect.

Taking it together with clonidine can cause an increase in blood pressure, which can lead to a hypertensive crisis.

Lithium substances lead to a decrease in the seizure threshold.

Combination with m-anticholinergics increases the anticholinergic effect of the drug.

Administration together with cimetidine potentiates the negative effects of Melipramine.

Use in combination with furazolidone causes a sharp increase in blood pressure.

Thyroid drugs contribute to the enhancement of the psychostimulant effect of imipramine, heart palpitations and potentiation of toxic activity.

Quinidine may cause irregular heartbeats.

Administration together with nicotine results in increased activity of the drug.

Systemic anesthetics result in depression of central nervous system function.

Taking it in combination with procainamide leads to disturbances in heart rhythm.

Use with phenytoin causes a weakening of its therapeutic effectiveness.

Combination with amanatadine or biperiden potentiates the anticholinergic activity of the drug.

Use together with atropine potentiates the anticholinergic effect of the drug and may lead to the development of paralytic intestinal obstruction.

Anticoagulants with indirect activity increase the anticoagulant effect.

Administration together with GCS potentiates symptoms of depression.

Combination with carbamazepine leads to weakening of the medicinal properties of imipramine.

Use in combination with fluoxetine increases intraplasmic levels of imipramine.

Use with phenothiazines may result in NMS.

The combination of Melipramine with reserpine weakens the antihypertensive effect of the drug.

Taking it together with fluvoxamine increases the drug's plasma levels.

Use with cocaine may cause arrhythmia.

Combined use with pimozide leads to potentiation of existing arrhythmia, and administration together with probucol causes potentiation of its symptoms.

Combination with epinephrine causes an increased effect on the cardiovascular system.

Concomitant administration with phenylephrine may cause hypertensive crisis or myocardial dysfunction.

Use with neuroleptics may cause hyperpyrexia.

The combination of the drug and hematotoxic substances potentiates hematotoxic activity.

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Storage conditions

Melipramine in tablets should be stored at a temperature not exceeding 20°C, and the substance in ampoules can be kept at temperatures in the range of 15-25°C.

Shelf life

Melipramine in tablets can be used for a 3-year period from the date of release of the pharmaceutical product. The shelf life of the solution is 24 months.

Application for children

In pediatrics, it can be prescribed to persons over 6 years of age.

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Analogues

Analogues of the drug are Abilify, Lamolep, Ziprexa, Adepress with Sedalit, Clopixol and Lamotrigine with Convulsan, and in addition to Lerivon, Velafax MV and Lamictal. In addition, the list includes Velaxin, Prosulpin, Rispaksol with Stimuloton, Clofranil and Cipramil with Leponex, as well as Ludiomil and Quetiax.

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Reviews

Medipramine receives good reviews from doctors and patients - it is considered to be very effective in case of panic attacks or depression, as well as enuresis. Negative manifestations develop only occasionally, in case of incorrect dosage selection.

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