Topral (Tablets) Instructions for Use

Marketing Authorization Holder

Alkaloid AD (Macedonia)

ATC Code

N05AL02 (Sultopride)

Active Substance

Sultopride (Rec.INN registered by WHO)

Dosage Form

Topral

Tablets 400 mg: 20 pcs.

Dosage Form, Packaging, and Composition

20 pcs. – dark glass bottles (1) – cardboard packs.

Clinical-Pharmacological Group

Antipsychotic drug (neuroleptic)

Pharmacotherapeutic Group

Antipsychotic (neuroleptic) agent

Pharmacological Action

Antipsychotic agent (neuroleptic) from the group of substituted benzamides. It has a moderate antipsychotic, as well as antidepressant effect combined with an activating action. The mechanism of antipsychotic action is associated with selective blockade of central dopamine D₂ receptors.

The sedative effect is weak, alpha-adrenergic blocking activity is low, and it practically does not cause antimuscarinic effects. It rarely causes extrapyramidal disorders, therefore it is classified as an atypical neuroleptic.

Pharmacokinetics

After oral administration of a 400 mg dose, C_max of sultopride in plasma is reached after 2 hours; after a single IM injection of a 200 mg dose – after 25 minutes, with repeated administration of the same dose – after 1 hour. The bioavailability of sultopride after oral administration is 80-90%. There is a linear relationship between the dose and the concentration of the active substance in plasma.

C_ss in plasma is achieved from the first day of treatment. The distribution of sultopride occurs quickly (within 2 hours) and evenly. Sultopride freely penetrates the blood-brain barrier, placental barrier, and is excreted in breast milk (the ratio of concentrations in milk and plasma is 3:5). It does not accumulate in body tissues.

It undergoes minor metabolism.

T_1/2 is 3-5 hours, total clearance is 390 ml/min, renal clearance is 325 ml/min. 77-90% is excreted unchanged in the urine, 4% as an inactive metabolite; 5-10% is excreted through the intestines.

Indications

Acute manic syndrome, acute stage of schizophrenia with agitation, state of agitation in alcoholism, chronic psychoses with behavioral disorders, aggressiveness, behavioral instability in patients with mental illnesses.

ICD codes

Dosage Regimen

Determine the dosage individually based on the clinical presentation and severity of symptoms.

For oral administration, initiate therapy with a daily dose of 400 mg to 800 mg.

Divide the total daily dose into three or four separate administrations.

Maintain an interval of at least 6 hours between consecutive doses.

If clinically warranted, titrate the dose upward. The recommended therapeutic range is 0.4 g to 1.6 g (400 mg to 1600 mg) per day.

For intramuscular injection, administer a total daily dose of 0.4 g to 1.2 g (400 mg to 1200 mg).

Divide the total daily IM dose into several injections throughout the day.

Do not exceed the maximum daily dose of 1.6 g (1600 mg) for intramuscular administration in adults.

Adjust the dosage carefully in elderly patients and in patients with cardiovascular comorbidities.

Adverse Reactions

From the central nervous system lethargy, drowsiness, early dyskinesias (spasmodic torticollis, spasms of masticatory and oculomotor muscles), extrapyramidal syndrome. With long-term treatment, the development of tardive dyskinesia, neuroleptic malignant syndrome is possible.

From the cardiovascular system cardiac rhythm disturbances (including torsades de pointes type arrhythmia), bradycardia, orthostatic hypotension.

From the endocrine system amenorrhea, galactorrhea, hyperprolactinemia, gynecomastia, impotence, frigidity.

From metabolism increased body weight.

Contraindications

Hypersensitivity to sultopride; bradycardia, pheochromocytoma, hypokalemia; lactation period (breastfeeding); simultaneous use of clonidine, beta-blockers, cardiac glycosides, class I and III antiarrhythmic drugs, tricyclic antidepressants.

Use in Pregnancy and Lactation

If it is necessary to use during pregnancy (especially in the III trimester), the dose and duration of treatment should be reduced, followed by monitoring of the newborn’s condition. Contraindicated for use during lactation (breastfeeding).

Geriatric Use

In elderly patients, the risk of developing sedative and hypotensive effects is increased.

Special Precautions

Use with caution in patients with epilepsy (due to a possible decrease in the seizure threshold), parkinsonism. In elderly patients, the risk of developing sedative and hypotensive effects is increased. In severe cardiovascular diseases, the likelihood of developing arterial hypotension and cardiac rhythm disturbances increases.

Avoid alcohol consumption during treatment.

Effect on ability to drive vehicles and mechanisms

During the use of sultopride, patients should exercise caution when driving vehicles and mechanisms, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

With simultaneous use of drugs that have a depressant effect on the central nervous system (including opioid analgesics, centrally acting antitussives, antihistamines, barbiturates, benzodiazepines, other tranquilizers), ethanol, an increase in the depressant effect on the central nervous system and mutual enhancement of effects is possible.

With simultaneous use with phenothiazine derivatives, the risk of developing cardiac rhythm disturbances increases; with tricyclic antidepressants – the development of slow dyskinesias is possible; with antihypertensive drugs – an increase in the hypotensive effect and the development of orthostatic hypotension are possible.

With simultaneous use with clonidine, beta-blockers, cardiac glycosides, class I and III antiarrhythmic drugs, an increase in the manifestations of side effects (bradycardia, arterial hypotension, arrhythmia) is possible.

With simultaneous use with levodopa, mutual weakening of effects occurs.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.