Restful

Restful is a drug from the antipsychotic group. Its active ingredient (sulpiride) as a dopamine mimetic has an effect on the dopaminergic neuronal transmission inside the brain, resulting in its activation. When used in large doses, sulpiride demonstrates an antireproductive 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 for aggressiveness and agitation in individuals with mental disorders in chronic or active form ( schizophrenia or chronic types of non-schizophrenic disorders - hallucinatory form of psychosis in the chronic stage or paranoid state).

Release form

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

Pharmacokinetics

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

Sulpiride undergoes high-speed distribution within tissues: the apparent distribution volume under steady-state conditions is 0.94 l/kg. Plasma protein synthesis is 40%. Small amounts of the substance are excreted in breast milk and can cross the placenta. [ 2 ]

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

Excretion is mainly realized through the kidneys by means of KF processes. The intrarenal clearance rate of Restful is 126 ml/minute. The half-life is 7 hours.

Dosing and administration

The medication is administered intramuscularly; the medication may only be prescribed to adults.

It is always necessary to use the minimum effective dosage. If the patient's clinical condition allows such a regimen, therapy begins with a dose of 0.1 g, and then it is allowed to gradually titrate it. The daily dosage is 0.4-0.8 g; such therapy lasts for 14 days.

• Application for children

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

Use Restful during pregnancy

Animal testing has shown decreased fertility due to the pharmacological parameters of the drug (prolactin-mediated effects). Animal testing data do not indicate any direct or indirect harmful effects on pregnancy, embryonic/fetal development, or postnatal development.

There is limited information available in humans regarding the effects of drugs during pregnancy. Almost always, when fetal or postnatal developmental disorders were reported in cases of sulpiride use during pregnancy, alternative causes were given that seemed more appropriate.

Restful should not be used during pregnancy. The introduction of antipsychotics, including this drug, in the 3rd trimester can provoke side effects, 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 are reports of hypertension, RDS syndrome, tremor, agitation, drowsiness and hypotension. Because of this, the condition of newborns must be closely monitored.

Because sulpiride is excreted in breast milk, it should not be used during breastfeeding.

Contraindications

Main contraindications:

• severe intolerance associated with sulpiride or any of the auxiliary components of the drug;
• prolactin-related neoplasms (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 quinagolide), mechitazine, escitalopram, citalopram, levodopa or antiparkinsonian drugs (including ropinorole).

Side effects Restful

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

• akathisia;
• Parkinsonism and the symptoms that arise against its background: hypokinesia, tremor, hypersalivation and hypertension;
• akinetic manifestations, in which the development of hypertonia is observed (or not). Their severity can be partially reduced by using anticholinergic antiparkinsonian agents;
• motor activity of an excitatory type that has a hyperkinetic-hypertonic character;
• late stage dyskinesia, in which rhythmic movements of an involuntary type are observed (for example, of the face or tongue), observed during long-term treatment cycles using any neuroleptics; in this case, anticholinergic antiparkinsonian drugs will be ineffective and may even worsen clinical symptoms;
• calming effect or drowsiness, as well as insomnia;
• convulsions.

Systemic disorders: weight gain or potentially fatal NMS.

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

Cardiac dysfunction: prolongation of the QT interval, ventricular arrhythmias, including torsades de pointes type 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 blood system: neutro- or leukopenia, and agranulocytosis. The administration of antipsychotics has occasionally caused the development of venous thromboembolism (sometimes fatal), deep venous thrombosis, and pulmonary embolism.

Symptoms related to digestive activity: increased activity of intrahepatic enzymes.

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

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

There are reports of anaphylaxis, with the development of palpitations, dyspnea, convulsive syndrome and decreased blood pressure, as well as a feeling of shortness of breath and the appearance of drip hemorrhages and redness in the injection area.

Overdose

There are limited data on sulpiride poisoning. Dyskinetic disorders with trismus, cervical dystonia and tongue protrusion may occur. Life-threatening parkinsonism or coma may develop in some patients.

Some of the drug is excreted via 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 prolongation of the QT interval and the appearance of ventricular arrhythmias) - this must be done until the patient has fully recovered. If extrapyramidal syndrome occurs in a severe degree, the administration of anticholinergic agents is required.

Interactions with other drugs

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

Levodopa exhibits an antagonistic effect relative to neuroleptics 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 should be stored in a dark place, out of the reach of small children. Temperature indicators should not exceed 25°C.

Shelf life

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

Analogues

Analogues of the drug are Tiaprilan, Betamax and Sulpiride with Solex, as well as Solian with Eglonil and Soleron.