Melipramin

Melipramine is an anesthetic, antidiuretic, and anxiolytic; The drug has a sedative, anticholinergic and α-adrenoceptor 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 capture of neurotransmitter molecules located on the presynaptic walls.

[1], [2], [3]

Indications Melipramine

It is used in case of such disorders:

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

[4], [5],

Release form

The release of drugs is in the form of injection fluid (inside ampoules with a volume of 2 ml, 5 pieces inside a pack), and besides this in tablets (50 pieces inside a bottle).

[6], [7], [8]

Pharmacodynamics

The drug reduces the rate of ventricular conduction, which allows you to stop the appearance of arrhythmias. Prolonged use leads to a slowdown in the functional activity of the endings of β-adrenoreceptors and serotonin. Drug administration helps to restore the functional balance of serotonergic and adrenergic transmission, disorders of which cause depression.

Melipramine can block the activity of histamine H2-terminations inside gastric cells, reducing the secretion of acid, and in addition has an anti-ulcer effect. The substance reduces pain in persons with ulcers, as well as increases the rate of regeneration of ulcerations, providing m-anticholinergic blocking effect. Cholinolytic effect has a positive effect on the treatment of nocturnal enuresis. The drug increases the elasticity of the bladder walls, as well as the tone of the sphincter.

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

There is no slowdown in the activity of MAO. Impact on α2- and β-adrenergic endings in the blue spot area leads to the development of an anxiolytic effect. The drug eliminates the inhibition of movements, helps get rid of insomnia, improves mood and stabilizes digestive function.

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

Dosing and administration

The use of drugs is made in the morning or afternoon, so as not to lead to the development or strengthening of insomnia. Tablets should be taken with or after meals. At first, 0.075-0.2 g of the substance is applied per day. A gradual increase in servings per 25 mg may be performed daily until a daily dosage of 0.2-0.3 g is obtained. Divide the daily portion into 3-4 uses. The whole cycle lasts 1-1.5 months.

After the cycle of therapy, maintenance treatment is performed, during which reduced portions of drugs are used. Dosage reduction is performed on 25 mg daily. During the maintenance cycle, 0.025-0.1 g of the drug is applied per day. The supporting course lasts no more than 1.5 months. The supporting portion is consumed in the evening.

In the outpatient mode, an adult can enter no more than 0.2 g per day, and a maximum of 0.3 g at the hospital.

An elderly person must first enter 10 mg of a substance per day. Increase the dosage should be up to 30-50 mg. Older people do not use more than 0.1 g of drugs per day.

Children should eat a portion of Melipramine 60 minutes before bedtime (1-fold), or divide it into 2 uses with a reception in the afternoon and evening.

Persons of 6-8 years old with depression are prescribed at first 10 mg each, and then increase the portion to 20 mg. With nocturnal enuresis take 25 mg of the substance per day.

In the case of depression, patients of 8–14 years of age are first given 10 mg of the drug, and then increase the dosage to 20–25 mg. In the case of nocturnal enuresis, a portion of 25-75 mg is required.

Adolescents older than 14 years of age during depressions first use 10 mg of the substance, and then increase the portion to 0.05-0.1 g per day. In the case of enuresis, a portion of 50-75 mg is required.

During the day, children are allowed to use no more than 2.5 mg / kg of the drug.

Use Melipramine during pregnancy

The prescription of imipramine-containing drugs during pregnancy is allowed only if there are strict indications.

Contraindications

The main contraindications:

• strong sensitivity associated with imipramine and auxiliary elements of drugs;
• using IMAO;
• conduction disorder in the area of the ventricular myocardium;
• myocardial infarction;
• acute poisoning with ethyl alcohol;
• breast-feeding;
• intoxication with sleeping pills;
• poisoning with narcotic substances;
• suppression of the central nervous system;
• glaucoma, having a closed angle shape.

With caution should be used in such disorders:

• AND;
• chronic stage of alcoholism;
• failure of the liver or kidneys;
• neuroblastoma;
• pheochromocytoma;
• cardiac pathology;
• suppression of hematopoietic processes;
• bipolar disorder;
• vascular diseases;
• stroke;
• motility disorders of the digestive tract;
• hyperthyroidism;
• prostatic hyperplasia accompanied by anuria;
• epilepsy or schizophrenia;
• elderly age.

[9]

Side effects Melipramine

Among the adverse symptoms of medication:

• nightmares, confusion, depersonalization, hallucinations, accommodative paresis, psychosis, insomnia, headaches and delirium, and also anxiety, worsening of attention, dizziness, manic syndrome and drowsiness, as well as arousal of psychomotor nature and hypomania. In addition, yawning, ear noise, disorientation, potentiation of depression, changes in blood pressure values, aggressiveness and orthostatic collapse appear;
• asthenia, arrhythmia, potentiation of epileptic seizures, tachycardia, hypohydrosis, changes in EEG and ECG values, and in addition, paresthesia, extrapyramidal disorders, ataxia, and ventricular myocardial disorder;
• heartburn, nausea, diarrhea, dry mouth mucous membranes, paralytic intestinal blockage, the urge to vomit, and also constipation, dysarthria, weight change, darkening of the tongue, taste disturbance, stomatitis and gastralgia;
• delay or difficulty of urination or its increased frequency, swelling of the testicles, hypoproteinemia, changes in libido and weakening of potency;
• glaucoma, visual impairment, and mydriasis;
• eosinophilia, thrombocyte or leukopenia and agranulocytosis;
• myoclonus or tremor;
• swelling of 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, and hyperglycemia or pyrexia.

[10]

Overdose

During intoxication, anuria, confusion, agitation of a psychomotor nature, dry oral mucous membranes, mydriasis, tachycardia, convulsions, respiratory disorders and a comatose state are noted.

It is required to hospitalize the patient in a hospital where doctors will observe him and carry out symptomatic procedures. Diuresis with dialysis will be ineffective.

Interactions with other drugs

Using imipramine with adrenergic blockers increases antihypertensive activity.

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

Substances containing ethanol, enhance the psychogogic effects of drugs and increase the intolerance associated with ethanol.

Combination with opiates causes the development of inhibition, which may be dangerous for the patient.

Hormonal contraception potentiates depressive manifestations.

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

The use of MAOI causes an increase in psychostimulating activity.

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

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

The use of benzodiazepines can lead to the suppression of respiration, a decrease in blood pressure and the appearance of life-threatening lethargy.

With the introduction of disulfiram may develop delirium.

The use of clozapine leads to toxic activity against the central nervous system.

When combined with levodopa develops hypertensive effects.

Using together with methyldopa weakens its medicinal effect.

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

Lithium substances lead to a decrease in the convulsive threshold.

The combination with m-anticholinergic increases the anticholinergic effect of the drug.

The introduction together with cimetidine potentiates the negative manifestations of Melipramine.

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

Thyroid medications contribute to the enhancement of the psychostimulant effects of imipramine, heartbeat and potentiation of toxic activity.

Quinidine can lead to heartbeat disorders.

Introduction together with nicotine leads to increased activity of the drug.

Systemic anesthetics suppress CNS function.

Reception in combination with procainamide leads to heart rhythm disorder.

Use with phenytoin causes a decrease in its therapeutic efficacy.

The combination with amantadin or biperidenom potentiates the anticholinergic activity of drugs.

Use together with atropine potentiates the cholinolytic effect of the drug and may lead to the appearance of paralytic intestinal blockage.

Indirect anticoagulants increase the anticoagulant effect.

Introduction together with GCS potentiates the symptoms of depression.

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

Use in combination with fluoxetine increases intraplasma values of imipramine.

Use together with phenothiazines may cause NNS.

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

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

Concurrent use with cocaine can cause arrhythmia.

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

Combination with epinephrine causes an increase in influence in relation to the CAS.

Simultaneous administration with phenylephrine may cause a hypertensive crisis or myocardial dysfunction.

Use together with neuroleptics may cause hyperpyrexia.

The combination of drugs and hematotoxic substances potentiates hematotoxic activity.

[11], [12]

Storage conditions

Melipramine tablets should be maintained at a temperature not higher than 20 ° C, and the substance in ampoules can be contained at temperature values in the range of 15-25 ° C.

Shelf life

Melipramine tablets can be used for a 3-year term since the release of the pharmaceutical product. The shelf life of the solution is 24 months.

Application for children

Prescribed in pediatrics can be older than 6 years.

[13]

Analogs

Analogs of drugs are the substances Abilifay, Lamolep, Zipreksa, Adepress with Sedalit, Klopiksol and Lamotrigine with Convulsan, and in addition Lerivon, Velafax MB and Lamiktal. In addition, Velaksin, Prosulpin, Rispaxol with Stimuloton, Klofranil and Tsipramil with Leponeks, as well as Lyudiomil and Quentiax, are on the list.

[14]

Reviews

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

[15]