Restful

Restful is a medication from the group of antipsychotics. Its active element (sulpiride) as a dopaminomimetic has an effect of relatively dopaminergic neuronal transmission within the brain, as a result of which its activation occurs. When used in large portions, sulpiride has an anti-reproductive effect.

It has a moderate neuroleptic effect, and at the same time a stimulating and thymoleptic effect. The drug is a selective serotonin and dopamine antagonist. In addition, it demonstrates antiemetic activity. [1]

Indications Restful

It is used for short- term therapy with aggressiveness and agitation in persons with mental disorders in a chronic or active form ( schizophrenia or chronic types of disorders of the non-schizophrenic type - a hallucinatory form of psychosis in a chronic stage or a paranoid state).

Release form

The release of the therapeutic substance is realized in the form of an injection liquid - inside ampoules with a volume of 2 ml. Inside the cell pack contains 6 ampoules; inside the box - 1 or 6 such packs.

Pharmacokinetics

When using a dosage of 0.1 g, the plasma Cmax values of sulpiride are 2.2 mg / l and are noted after half an hour.

Sulpiride undergoes distribution inside tissues at high speed: the indicator of the visible distribution volume under stationary conditions is 0.94 l / kg. Plasma protein synthesis is 40%. Small volumes of the substance are excreted in breast milk and can cross the placenta. [2]

Sulpiride almost does not participate in metabolic processes; 92% of the used drug dosage is excreted in the urine unchanged. [3]

Excretion is mainly carried out through the kidneys using CF processes. Indicators of intrarenal clearance of Restful are equal to 126 ml / minute. The half-life is 7 hours.

Dosing and administration

The medication is injected by the intramuscular method; prescribing medication is allowed only to adults.

Always use the lowest effective dosage. When the patient's clinical condition allows such a regimen, therapy begins with a portion of 0.1 g, and then it is allowed to gradually titrate. The dosage amount per day is 0.4-0.8 g; this therapy lasts for a period of 14 days.

• Application for children

The medication in the indicated form of release cannot be used in pediatrics.

Use Restful during pregnancy

When tested with the participation of animals, a decrease in fertility caused by the pharmacological parameters of the drug (prolactin-mediated effect) was noted. The data from animal tests do not contain information on the presence of an indirect or direct negative impact on the course of pregnancy, the development of the embryo / fetus, or postpartum development.

In humans, there is only limited information regarding drug exposure during pregnancy. Almost always, for disorders of fetal or postnatal development in the case of the use of sulpiride during pregnancy, alternative reasons were given that looked more suitable.

You should not use Restful during pregnancy. The introduction of antipsychotics, among which the indicated medical drug, in the 3rd trimester can provoke side symptoms, including withdrawal syndrome, as well as extrapyramidal syndrome, which can change the duration and severity of side effects in the postnatal period in newborns. There is information about the appearance of hypertension, RDS syndrome, tremor, agitation, drowsiness and hypotension. Because of this, the condition of newborns must be closely monitored.

Due to the fact that sulpiride is excreted in mother's milk, it cannot be used during periods of breastfeeding.

Contraindications

The main contraindications:

• severe intolerance associated with sulpiride or any of the auxiliary components of the drug;
• neoplasms associated with the action of prolactin (for example, prolactinoma or breast carcinoma);
• suspicion of the development of pheochromocytoma or its diagnosed presence;
• active porphyria;
• combined use with non-antiparkinsonian dopamine agonists (this includes rotigotine with cabergoline and kinagolide), mechitazine, escitalopram, citalopram, levodopa or antiparkinsonian drugs (among them ropinorol).

Side effects Restful

Among the disorders associated with the activity of the NS: the early stage of development of dyskinesia (cervical dystonia, OGK and trismus), which is weakened in the case of the use of anticholinergic antiparkinsonian substances, as well as extrapyramidal disorders and related manifestations:

• akathisia;
• parkinsonism and signs that arise against its background: hypokinesia, tremor, hypersalivation and hypertension;
• akinetic manifestations, in which there is (or not) the development of hypertonicity. Their severity can be partially reduced by using anticholinergic antiparkinsonian agents;
• having a hyperkinetic-hypertensive nature of the motor activity of the exciting type;
• late stage of dyskinesia, in which rhythmic movements of an involuntary type (for example, of the face or tongue) are noted, observed with prolonged treatment cycles using any antipsychotics; at the same time, anticholinergic antiparkinsonian drugs will be ineffective and may even worsen clinical symptoms;
• sedative effect or drowsiness, as well as insomnia;
• convulsions.

Systemic disorders: weight gain or potentially fatal NMS.

Problems associated with the endocrine system: short-term hyperprolactinemia, which disappears when therapy is canceled; the disease can cause gynecomastia, frigidity, amenorrhea, impotence and galactorrhea, as well as pain and enlargement of the mammary glands.

Violations of cardiac function: prolongation of the QT-interval, ventricular arrhythmias, including torsades de pointes tachycardia, and in addition, ventricular tachycardia, which can cause ventricular fibrillation or cardiac arrest, and sudden death.

Vascular disorders: orthostatic collapse.

Lesions affecting the lymph with the circulatory system: neutro- or leukopenia, as well as agranulocytosis. Administration of antipsychotics has sometimes caused venous thromboembolism (sometimes fatal), DVT, and pulmonary embolism.

Digestive symptoms: increased activity of intrahepatic enzymes.

Diseases of the subcutaneous layers and epidermis: urticaria or maculopapular rashes.

Conditions associated with pregnancy, peri- and postnatal periods: the development of a withdrawal syndrome in a newborn.

There is information about the appearance of anaphylaxis, with the development of palpitations, dyspnea, convulsive syndrome and a decrease in blood pressure, and in addition, with a feeling of lack of air and the appearance of drip hemorrhages and redness in the injection area.

Overdose

There are only limited data on sulpiride poisoning. The appearance of dyskinetic disorders with trismus, cervical dystonia and protrusion of the tongue is possible. Some patients may develop life-threatening signs of parkinsonism or coma.

Some of the drug is excreted through hemodialysis. Sulpiride has no antidote.

Symptomatic procedures are performed; if necessary, resuscitation is performed, during which the work of the heart and respiratory activity are closely monitored (there is a risk of lengthening the QT interval and the appearance of ventricular arrhythmias) - this must be done until the patient is fully recovered. When extrapyramidal syndrome appears in a severe degree, the administration of anticholinergic agents is required.

Interactions with other drugs

When using the medication, it is forbidden to consume alcoholic beverages or substances that contain alcohol (this increases its sedative effect).

Levodopa demonstrates antagonistic effects with respect to antipsychotics and vice versa. Persons with extrapyramidal signs using Restful are prohibited from administering levodopa.

When combined with antihypertensive drugs, the likelihood of developing orthostatic collapse increases.

Morphine derivatives (antitussive drugs with a central type of activity and analgesics), substances that block the activity of histamine H1-endings, as well as clonidine, barbiturates with benzodiazepines and other sedative drugs potentiate the suppressive effect of the drug on the central nervous system.

Storage conditions

Restful must be kept in a dark place, closed from the penetration of small children. Temperature indicators - no more than 25 ° C.

Shelf life

Restful can be applied within a 5-year term from the date of sale of the pharmaceutical product.

Analogs

The analogues of the drug are Tiaprilan, Betamax and Sulpiride with Solex, and in addition, Solian with Eglonil and Soleron.