Melperon

Melperon is a drug from the subgroup of butyrophenones and demonstrates their characteristic antipsychotic effect.

The drug blocks the activity of dopamine endings, which leads to a weakening of the intensity of the influence of the dopamine neurotransmitter. Along with this, the drug demonstrates a powerful antiserotonergic effect, while the antipsychotic effect develops only with the introduction of large portions of drugs. [1]

Melperon can lead to the development of antiarrhythmic activity and muscle relaxation. [2]

Indications Melperon

It is used for such violations:

• dysomnia, psychomotor agitation or agitation and confusion in the elderly and people with mental disorders;
• dementia , neuroses or psychosis, as well as oligophrenia associated with brain lesions of the organic type.

Release form

The release of the drug substance is made in the form of a liquid for oral administration - 5 mg / ml inside bottles with a volume of 0.2 or 0.3 liters. Inside the pack - 1 such bottle and a dosage cup.

Pharmacodynamics

Melperone hydrochloride is butyrophene. Its synthesis index with D2 endings is almost 200 times lower than that of haloperidol. In addition to the dopaminergic effect, the drug also exhibits a powerful antiserotonergic effect.

After the introduction of melperon, affective relaxation, which tends to decrease drowsiness, is observed tied to the dose size of the drug. Antipsychotic activity in relation to delusions, hallucinations and autism develops only with the use of large dosages of the medication.

In addition to the above-described basic properties that are characteristic of antipsychotics with a weak effect, the drug has antiarrhythmic and muscle relaxant effects.

Melperon differs from other antipsychotics in that it does not affect the cerebral convulsive threshold in therapeutic portions. A slight increase in this threshold will probably be observed with the use of medium therapeutic doses of the drug.

The activity of the drug in relation to extrapyramidal motor activity is rather weak.

Pharmacokinetics

When administered orally, the drug is fully absorbed and at high speed, undergoing intensive metabolic processes during the 1st intrahepatic passage.

Plasma level Cmax is noted after 60-90 minutes from the moment of drug administration.

In the case of an increase in dosage, a nonlinear increase in plasma parameters Cmax of melperon occurs - due to the peculiarities of intrahepatic metabolic processes.

The level of protein synthesis is 50% (18% is synthesized with intra-serum albumin).

Eating food does not change drug absorption and blood counts.

Melperon at high speed, almost fully participates in intrahepatic metabolism; 5-10% of the unchanged active element is excreted through the kidneys. The half-life for a single administration is approximately 4-6 hours. In case of repeated administration, this value increases to approximately 6-8 hours.

The metabolic processes of the drug do not change under the action of substances that induce intrahepatic enzymes (phenytoin with phenobarbital and carbamazepine), which distinguishes it from other butyrophenone derivatives.

Dosing and administration

The selection of the dosage is made taking into account the age, personal sensitivity, weight and severity of the manifestations of the disease.

To obtain a mild sedative effect, in which there is an improvement in mood, the medication is used in a daily portion, which is in the range of 20-75 mg.

Persons with confusion and agitation should first use the drug in a portion of 0.05-0.1 g per day. If necessary, with the appointment of a doctor, this portion can be increased to 0.2 g. The maximum permissible dosage per day is 0.4 g.

• Application for children

Not assigned to persons under 12 years of age.

Use Melperon during pregnancy

Melperon should not be administered to pregnant women.

If you need to use it during hepatitis B, you need to stop breastfeeding for the period of therapy.

Contraindications

Among the contraindications:

• severe intolerance to melperone, other butyrophenones or other elements of the drug;
• acute poisoning or coma provoked by opiates, alcohol, sleeping pills and other psychotropics that weaken the activity of the central nervous system (antidepressants with neuroleptics and lithium salts);
• severe liver failure;
• a history of ZNS.

Side effects Melperon

The main side symptoms:

• a decrease in blood pressure values, fatigue, a reflex increase in heart rate indicators, as well as orthostatic dysregulation;
• signs of paralysis (stiffness and trembling), voluntary movement disorders (extrapyramidal manifestations) and hyperkinesia;
• weakening of the outflow of bile, a temporary increase in the activity of liver enzymes and jaundice;
• epidermal signs of allergies;
• thrombocyto-, leuko- or pancytopenia.

Overdose

Poisoning with a drug can lead to the potentiation of negative symptoms.

Symptomatic actions are performed.

Interactions with other drugs

The use of the drug together with ethyl alcohol causes an increase in the activity of the latter.

Administration in combination with substances that suppress the activity of the central nervous system (among them analgesics, antihistamines, hypnotics and other psychotropics), can provoke an increase in the sedative effect or respiratory depression.

The use of drugs together with tricyclics can provoke a mutual enhancement of drug activity.

Combination with medication can enhance the activity of antihypertensive medications.

The use together with dopamine antagonists (for example, levodopa) can provoke a decrease in the therapeutic effect of the dopamine agonist.

The use of antipsychotics in combination with other dopamine antagonists (for example, with metoclopramide) can provoke an increase in the intensity of extrapyramidal disorders.

The use of Melperon simultaneously with substances with anticholinergic activity (for example, atropine) can potentiate the anticholinergic effect. In this case, visual disturbance, an increase in the level of IOP, constipation, xerostomia, an increase in heart rate, salivation, urinary disorders, hypohidrosis, difficulty in speech processes and partial amnesia can develop. The intensity of the effect of melperon can be weakened by decreasing its absorption inside the gastrointestinal tract.

Butyrophenones are able to form compounds with tea, coffee and milk, which reduce their solubility; this makes it difficult for the drug to be absorbed.

Despite the fact that melperon leads only to a rather weak and short-term increase in prolactin indicators, the effect of drugs that slow down the action of prolactin (for example, gonadorelin) may decrease. Such interaction has not yet developed, but it should not be completely ruled out.

Amphetamine stimulants can reduce the antipsychotic effect of a drug.

Epinephrine can cause the development of tachycardia and a paradoxical decrease in blood pressure.

The introduction together with melperon can reduce the drug effect of phenylephrine.

The combination with dopamine can antagonize peripheral vasodilation (for example, renal arteries) or, with the introduction of a large dose of dopamine, vasoconstriction.

It is necessary to exclude the combined use of medications that can prolong the QT-interval (among them macrolides, antiarrhythmic substances of type IA or III, as well as antihistamines), lead to the appearance of hypokalemia (for example, diuretics) or slow down the intrahepatic disintegration of the drug (among them fluoxetine with cimetidine ).

Storage conditions

Melperon must be kept in a place out of the reach of children. Temperature level - no more than 25 ° С.

Shelf life

Melperon is allowed to be used within a 36-month term from the date of manufacture of the drug. The opened bottle has a shelf life of 2 months.

Analogs

The analogs of the drug are the substances Halopril with Galomond, Senorm and Haloperidol with Droperidol.