Melperone hexal

Melperone Hexal is an antipsychotic, part of the butyrophenone derivative group.

The active element of the drug is the substance melperone (under the guise of hydrochloride), included in the category of butyrophenones. This component has a neuroleptic effect characteristic for butyrophenones, which varies from mild to moderate. According to animal tests, it was found that butyrophenones block the effect of dopamine endings, thereby weakening the intensity of the effect of the dopamine neurotransmitter.

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Indications Melperone hexal

It is used for the following violations:

• insomnia, mental confusion, psychosis and agitation of a psychomotor nature (especially in people with mental disorders and the elderly);
• dementia (associated with organic CNS lesions);
• gypopheres;
• neurosis (if it is impossible to use tranquilizers due to hypersensitivity or the risk of addiction);
• alcoholism.

Release form

The release of the drug element is implemented in tablets - 20 pieces inside a blister pack, 2 packs inside a pack.

Pharmacodynamics

In vitro testing determined that melperone has a lower rate of synthesis with D2-termini than with haloperidol (almost 200 times). In addition to dopaminergic activity, the drug exhibits a strong antiserotonergic effect.

It is difficult to evaluate the central and peripheral antihistamine and anticholinergic effects of the drug.

Antipsychotic effects develop only with the introduction of large portions of drugs.

In addition to the effects described above, which are usually observed in neuroleptics with weak activity, melperone can have a muscle relaxant effect and an antiarrhythmic effect.

The drug differs from other neuroleptics in that when it is administered its therapeutic portions, it does not develop a negative effect on the indices of the convulsive threshold of the brain. Conducted relevant tests showed that a small increase in this threshold can be observed when using drugs in medium medication portions.

The impact of melperone on motor extrapyramidal activity is rather weak.

Pharmacokinetics

When ingested inside, melperone is absorbed completely and at high speed into the blood, and then participates in intensive metabolic processes during the 1st intrahepatic passage. Plasma Cmax values are recorded after 60-90 minutes from the moment of oral administration.

Increasing the dosage leads to a non-linear increase in the plasma level of Cmax, which is due to the characteristics of intrahepatic metabolism.

The level of synthesis with intraplasma protein is 50% (18% of them are with serum albumin).

Eating food does not change the intensity of drug absorption and its blood parameters.

The drug is almost fully and at high speed undergoes intrahepatic metabolism. In tests involving animals inside the urine, a number of metabolic components were found.

Unchanged through the kidneys excreted 5-10% of the active ingredient. The term half-life at 1-time reception is approximately 4-6 hours. After repeated use, this indicator increases to approximately 6-8 hours.

Dosing and administration

A portion of Melperon Hexal is required to be selected, taking into account the weight and age of the person, as well as his personal tolerance, and in addition to this, the intensity and type of the disease. In this case, the doctor is most important to be guided by the possibility of minimizing the portion and duration of therapy.

Daily portion should be divided into several uses. A single dose should be taken with food (especially if sedation is required), before bedtime. It is forbidden to use with tea, coffee or milk.

In order to get a weak sedative and enhanced anxiolytic effect, in which there is an improvement in mood, a daily portion of 20-75 mg is often used. To achieve a stronger sedative effect, you can use the maximum dosage (in the evening).

Persons with confusion and agitation are first required to use 0.05-0.1 g of medicine per day. If required, a portion of a few days can be increased to 0.2 g. In some cases with severe disorders, in which aggressiveness, the appearance of hallucinations and illusions is noted, a maximum portion of 0.4 g can be administered.

Restrictions on the term use of drugs is often not available. The required antipsychotic effect may not develop during the 2-3 weeks of treatment. Further, taking into account the personal response of the patient, the portion can be reduced.

Combined use with lithium substances requires a reduction of the portion of both drugs.

Use Melperone hexal during pregnancy

You can not use Melperone Hexal during pregnancy, because the available information about its safety for a newborn baby is too little.

In connection with the lack of information regarding the volume of the active ingredient excreted in breast milk, when the need for the use of drugs during lactation, breastfeeding should be abandoned during therapy.

Contraindications

The main contraindications:

• severe intolerance towards melperone, other butyrphenones, or other components of drugs;
• acute poisoning or coma, triggered by opiates, alcohol, hypnotics and other psychotropics that weaken the function of the central nervous system (anti-depressants with neuroleptics, as well as lithium salts, among them);
• failure of the liver in the severe stage.

Side effects Melperone hexal

Therapeutic portions of drugs often do not affect (or have a weak effect) regarding the processes of blood circulation, respiration, urination, digestion of food and the liver.

At the initial stage of therapy, fatigue may develop or (at times) orthostatic disregulation / reduction in blood pressure, or reflex increase in heart rate values. People with cardiopathy need to regularly monitor ECG readings, because sometimes they develop arrhythmia.

The use of large portions of Melperon Hexal, taking into account the personal response of the body, can lead to a breakdown of the forms of involuntary movements (the appearance of extrapyramidal disorders). Among the signs are dyskinesia of an early nature (spasm of the pharyngeal muscles, spastic tongue bite, torticollis, ocular crisis, spasm affecting the jaw muscles, and stiffness of the cervical muscles) and manifestations of trembling paralysis (rigidity or shivering) and akatisia (appearance of hyperkinesia)

The development of the early stage of dyskinesia and signs of trembling paralysis is controlled by reducing the amount of drugs or introducing cholinolytic anti-parkinsonic drugs. The abolition of neuroleptic completely eliminates these symptoms. But akathisia is more difficult to cure. First, you can try to reduce the dose of the medication, and in the absence of a result, prescribe treatment with the introduction of bipyriden, sedatives or hypnotic drugs, or substances that block the action of β-adrenergic receptors.

Sometimes there is a temporary connection between the appearance of an early variety of dyskinesia and the use of melperone. But in all such cases, together with this drug or before its introduction, they used other medicines that can provoke such a side symptom. Therapy has not yet been developed for him.

Occasionally, intrahepatic cholestasis or jaundice occurs, and the effect of intrahepatic enzymes also increases temporarily.

With the introduction of butyrophenones, epidermal signs of allergy (rash) were rarely observed.

Sometimes the use of melperone leads to disorders associated with the blood system - pancyto-, leuco-or thrombocytopenia. Agranulocytosis is only observed.

Occasionally, especially with the introduction of highly active neuroleptics in large portions, it is possible to develop potentially lethal ZNS (with temperature indices of more than 40 ° C, suppression of consciousness reaching coma, rigidity, and also decompensation of a vegetative nature with an increase in blood pressure and tachycardia), requiring immediate termination of the drug. As in the case of intoxication, such negative manifestations require emergency medical care.

Sometimes there is galactorrhea, weight loss, dysmenorrhea and impaired sexual function.

It is also possible to develop thermoregulation or accommodation disorders, headaches, olfactory disorders (due to nasal congestion), xerostomia, constipation, vomiting with nausea, and in addition loss of appetite, upset urine and increased IOP levels.

As in the case of the introduction of other sedative psychotropes, the use of the drug causes the likelihood of venous thrombosis in the pelvis and legs - this factor must be taken into account in the case of bed rest, prolonged immobility or susceptibility to this violation.

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Overdose

In connection with a wide range of therapeutic dosages of melperone, poisoning is detected only in the case of a significant overdose. During intoxication, not all of the manifestations indicated below were noted, but none of them can be excluded.

Signs of poisoning:

• drowsiness, which can develop into a coma, and sometimes there is a confused consciousness of a delirious character and excitement;
• anticholinergic symptoms (glaucoma, urinary retention, visual clouding or intestinal peristalsis disorders);
• cardiovascular disorders (bradycardia or tachycardia, insufficiency of blood flow processes, decrease in blood pressure, ventricular tachyarrhythmia, or HF);
• hypo or hyperthermia;
• severe stages of extrapyramidal disorders (visual spasms, acute dystonic or dyskinetic manifestations, spasms affecting the larynx or pharynx, as well as the defeat of the glossopharyngeal nerve);
• single lesions associated with respiratory activity (aspiration, cyanosis, pneumonia, respiratory arrest or suppression).

Standard symptomatic actions are carried out, which are often used in cases of poisoning; but in this case there are some features, because the drug is rapidly absorbed. Perform gastric lavage is possible only with an early determination of poisoning. Dialysis with forced diuresis will be ineffective.

In the case of severe extrapyramidal disorders, anti-parkinsonic agents are used (for example, intravenous injection of biperiden).

To prevent spasm of the pharyngeal muscles, intubation is performed or a muscle relaxant is injected with a short type of effect.

In the case of a decrease in blood pressure, in order to prevent its paradoxical increase, it is required to use drugs similar to norepinephrine (or norepinephrine), but it is prohibited to use substances similar to epinephrine (or adrenaline). The use of β-adrenoreceptor agonists is prohibited, because they lead to vasodilation.

Anticholinergic features are eliminated with physostigmine salicylate (administration of 1-2 mg with the possibility of repeated use). It is impossible to use the standard dosing regimen, because it can provoke severe side effects.

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Interactions with other drugs

The use of drugs with alcohol can cause increased alcohol exposure.

Introduction in combination with drugs that suppress the action of the central nervous system (painkillers, sleeping pills, antihistamines or other psychotropics), can provoke an increase in sedation or respiratory depression.

Use with tricyclics may trigger reciprocal activity enhancement.

The effect of antihypertensive drugs can be enhanced in the case of a combination with melperone hexal.

The combination with dopamine antagonists (for example, with levodopa) causes a decrease in the therapeutic activity of the dopamine agonist.

The use of neuroleptics simultaneously with other dopamine antagonists (for example, with metoclopramide) can provoke a potentiation of the intensity of motor extrapyramidal signs.

The combined use of melperon and drugs with an anticholinergic effect (for example, with atropine) causes the potentiation of this effect. Symptoms are dysopia, xerostomia, an increase in IOP values or heart rate indicators, urinary disorders, constipation, hypersalivation, partial loss of memory, speech problems and hypohydrosis. The intensity of the effect of drugs may weaken due to a decrease in its absorption inside the gastrointestinal tract.

Butyrophenones are capable of forming poorly dissolvable combinations with tea, coffee or milk, which makes the absorption of the drug more difficult.

Although the use of Melperon Hexal causes only a rather weak and short-term increase in the level of prolactin, the effect of prolactin inhibitors (for example, gonadorelin) may decrease. Such interaction has not yet been noted, but its development cannot be completely ruled out.

Although the development of drug interactions with the following medicines was not registered before, they cannot be completely excluded, because melperone has α-adrenergic activity.

Amphetamine-type stimulants: there is a weakening of the antipsychotic effect of melperone and the stimulating activity of amphetamine.

Epinephrine (or adrenaline) leads to tachycardia or a paradoxical decrease in blood pressure.

Combination with phenylephrine causes a decrease in the effect of this drug.

The use of dopamine causes the expansion of peripheral vessels (for example, the arteries of the kidneys). The introduction of large portions of dopamine causes vasoconstriction by melperon. The use of melperone may have an antagonistic effect on the expansion of peripheral vessels (for example, kidney arteries) or, at a high dosage of dopamine, vasoconstriction.

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Storage conditions

Melperone Hexal must be kept in a place inaccessible to small children. Temperature values - not more than 25 ° С.

Shelf life

Melperone Hexal can be used for a 3-year term since the sale of the medication.

Application for children

You can not prescribe medication to persons under the age of 12 years.

Analogs

Analogues of the drug are the substances Galomond, Halopril with Haloperdol and Senorm.