Betamax (Tablets) Instructions for Use

ATC Code

N05AL01 (Sulpiride)

Active Substance

Sulpiride (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antipsychotic drug (neuroleptic)

Pharmacotherapeutic Group

Antipsychotic agent (neuroleptic)

Pharmacological Action

Antipsychotic drug, is an atypical neuroleptic. It also has stimulating, antidepressant, and antiemetic effects.

Antipsychotic action is due to the blockade of dopamine D₂ receptors in the mesolimbic and mesocortical systems. Antipsychotic action manifests at doses above 600 mg/day; at doses up to 600 mg/day, stimulating and antidepressant effects predominate.

It stimulates prolactin secretion, does not significantly affect adrenergic, cholinergic, serotonin, histamine, and GABA receptors.

Antiemetic action is due to the blockade of dopamine D₂ receptors in the trigger zone of the vomiting center. Peripheral action is based on the inhibition of presynaptic receptors. In gastric and duodenal ulcers, by exerting a selective action on the hypothalamus, it suppresses excitation of the sympathetic nervous system centers and improves gastric blood supply, increases mucus secretion in the stomach; accelerates the proliferation of granulation tissue, forms regenerating epithelium, improves capillary proliferation in tissues.

Pharmacokinetics

Absorption

After oral administration, C_max in plasma is reached in 1.5-3 hours. The bioavailability of sulpiride after oral administration is 27%.

Distribution

The binding of sulpiride to plasma proteins is less than 40%. It rapidly penetrates the liver and kidneys, more slowly into brain tissue (the main amount of the drug accumulates in the pituitary gland). The concentration of sulpiride in the CNS is 2-5% of the plasma concentration. Sulpiride is excreted in breast milk (0.1% of the daily dose).

Metabolism and Excretion

In the human body, Sulpiride is not metabolized and is excreted almost unchanged by the kidneys via glomerular filtration (92%). Total clearance is 126 ml/min. T_1/2 is about 7 hours.

Pharmacokinetics in Special Clinical Cases

T_1/2 is significantly increased in patients with moderate and severe renal failure (up to 20-26 hours after IV administration). Such patients should have the dose of sulpiride reduced and/or the interval between doses increased.

Indications

As monotherapy or in combination with other psychotropic drugs

• Acute and chronic schizophrenia;
• Acute delirious states;
• Depression of various etiologies;
• Neuroses;
• Dizziness of various etiologies (vertebrobasilar insufficiency, vestibular neuritis, Ménière’s disease, traumatic brain injury, otitis media);
• Migraine;
• Adjuvant therapy for gastric ulcer, duodenal ulcer, and irritable bowel syndrome.

ICD codes

Dosage Regimen

Tablets

The drug is taken orally in the first half of the day (before 4:00 PM), regardless of meals, with a small amount of liquid.

For acute and chronic schizophrenia, acute delirious psychosis, the initial doses of Betamax depend on the clinical picture of the disease and are 600-1200 mg/day in several doses; maintenance doses are 300-800 mg/day. The maximum recommended daily dose is 1600 mg.

For depression, the drug is prescribed in doses from 150-200 mg to 600 mg/day in several doses.

For neuroses – 400-600 mg/day in several doses.

For dizziness – 150-200 mg/day; in severe conditions, the dose can be increased to 300-400 mg. The duration of treatment is at least 14 days.

For migraine – 100-300 mg/day.

As adjuvant therapy for gastric ulcer, duodenal ulcer, and irritable bowel syndrome – 150 mg/day in 3 doses, for 4-6 weeks.

In patients with impaired renal function, it is recommended to reduce the dose of Betamax and/or increase the interval between individual doses of the drug depending on the CC values (since Sulpiride is excreted from the body mainly by the kidneys).

In elderly patients, the initial dose of Betamax is 1/4-1/2 of the adult dose.

During pregnancy, the drug is prescribed in low doses and not for a long duration.

Adverse Reactions

From the endocrine system: reversible hyperprolactinemia is possible, the most frequent manifestations of which are galactorrhea, menstrual cycle disorders, less often – gynecomastia, impotence, and frigidity.

From the metabolism: increased sweating, weight gain are possible.

From the digestive system: dry mouth, heartburn, nausea, vomiting, constipation, increased activity of hepatic transaminases and alkaline phosphatase.

From the CNS: extrapyramidal syndrome (usually occurs when the drug is prescribed in doses above 400 mg/day), tremor, early and late dyskinesias (spasmodic torticollis, oculomotor disorders, spasm of the masticatory muscles), akathisia (resting posture disorders), insomnia, drowsiness, anxiety, irritability, agitation, sleep disorder, headache, neuroleptic malignant syndrome (pallor of the skin, autonomic disorders, hyperthermia). If hyperthermia develops, the drug should be discontinued!

From the cardiovascular system: increased blood pressure; rarely – decreased blood pressure, orthostatic hypotension, dizziness, tachycardia, QT interval prolongation, torsades de pointes arrhythmia.

Allergic reactions: skin rash, eczematous eruptions, itching are possible.

From the organ of vision: impaired visual acuity.

Side effects developing with sulpiride intake are similar to those observed with other psychotropic drugs, but their frequency is generally lower.

Contraindications

• Acute poisoning with alcohol, hypnotics, opioid analgesics;
• Manic psychosis;
• Convulsive seizures;
• Parkinson’s disease;
• Pheochromocytoma;
• Prolactin-dependent tumors (including breast cancer);
• Hyperprolactinemia;
• Affective disorders, aggressive behavior;
• Arterial hypertension of II-III degree;
• Lactation period (breastfeeding);
• Children and adolescents under 18 years of age;
• Hypersensitivity to the components of the drug.

With caution, the drug should be used in epilepsy, arterial hypertension, dysmenorrhea, severe heart disease, angina pectoris, hepatic insufficiency, history of neuroleptic malignant syndrome, in glaucoma, prostatic hyperplasia, urinary retention, in elderly patients, in patients with impaired renal function (since up to 95% of sulpiride is excreted by the kidneys), in patients with parkinsonism, young women with irregular menstrual cycle.

Use in Pregnancy and Lactation

Use of the drug during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus. In this case, it is recommended, as far as possible, to limit the dose and duration of the course of treatment.

The drug is contraindicated during lactation (breastfeeding).

Use in Hepatic Impairment

With caution, the drug should be used in hepatic insufficiency.

Use in Renal Impairment

With caution, the drug should be used in patients with impaired renal function (since up to 95% of sulpiride is excreted by the kidneys).

Pediatric Use

Contraindicated: children and adolescents under 18 years of age.

Geriatric Use

With caution, the drug should be used in elderly patients.

Special Precautions

If hyperthermia occurs during treatment, the drug should be discontinued (hyperthermia is a symptom of developing neuroleptic malignant syndrome).

When prescribing the drug to patients with epilepsy, a preliminary clinical and electrophysiological examination should be performed before starting treatment, because the drug lowers the threshold for convulsive activity.

With simultaneous use with drugs that increase the risk of ventricular arrhythmias, regular ECG monitoring is recommended.

QT interval prolongation with the use of Betamax is a dose-dependent effect.

Ethanol consumption while taking the drug is contraindicated.

Effect on the ability to drive vehicles and mechanisms

During the treatment period, patients should exercise caution when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: dyskinesias (spasm of the masticatory muscles, spasmodic torticollis), extrapyramidal disorders; in some cases – severe parkinsonism, coma.

Treatment: symptomatic. Use of centrally acting anticholinergics.

Drug Interactions

With simultaneous use with levodopa, the effectiveness of sulpiride decreases; with antihypertensive drugs – their hypotensive effect is enhanced and the risk of orthostatic hypotension increases.

With simultaneous use with drugs that depress the CNS (opioid analgesics, hypnotic and anxiolytic drugs, clonidine, centrally acting antitussives), their depressant effect on the CNS is enhanced.

Sucralfate, antacids containing magnesium and/or aluminum ions, reduce the bioavailability of sulpiride by 20-40%.

Antagonism with dopamine receptor agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ropinirole) and neuroleptics.

For neuroleptic-induced extrapyramidal syndrome, dopamine receptor agonists are not used; instead, anticholinergic drugs are prescribed.

If it is necessary to treat patients with Parkinson’s disease while using dopamine receptor agonists, the dose of the latter should be gradually reduced until complete withdrawal (abrupt withdrawal can lead to the development of neuroleptic malignant syndrome).

With simultaneous use with sultopride, the risk of ventricular arrhythmias (including atrial fibrillation) increases.

The risk of developing torsades de pointes ventricular arrhythmia increases with the simultaneous use of sulpiride with class I A antiarrhythmic drugs (quinidine, hydroquinidine, disopyramide) and class III antiarrhythmic drugs (amiodarone, sotalol, dofetilide, ibutilide), some neuroleptics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, cyamemazine, amisulpride, tiapride, haloperidol, droperidol, pimozide); with drugs causing bradycardia (diltiazem, verapamil, beta-blockers, clonidine, guanfacine, digitalis preparations, donepezil, rivastigmine, tacrine, ambenonium chloride, galantamine, pyridostigmine, neostigmine); with drugs causing hypokalemia (potassium-wasting diuretics, some laxatives, intravenous amphotericin B, corticosteroids, tetracosactide); with other drugs (including bepridil, cisapride, diphemanil, intravenous erythromycin, mizolastine, intravenous vincamine, halofantrine, pentamidine, sparfloxacin, moxifloxacin).

Storage Conditions

The drug should be stored out of the reach of children, in a dry place at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 2 years.

Dispensing Status

The drug is dispensed by prescription.

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.