Sulpiride

Sulpiride is a drug that is used in medicine as an antipsychotic.

1. Mechanism of action: The drug belongs to a group of drugs called antipsychotics or neuroleptics. It works by blocking dopamine receptors in the central nervous system. This helps reduce symptoms of psychosis such as hallucinations, delusions, anxiety and aggression.
2. Use: Sulpiride is commonly used to treat schizophrenia and other psychotic disorders, including acute and chronic psychosis, manic-depressive states, and Guillain-Barré syndrome.
3. Dosage and method of administration: The dosage of sulpiride depends on the severity of the patient's condition and doctor's recommendations. The drug is usually taken orally in the form of tablets or capsules. The dosage may be started with a small dose, which can then be gradually increased depending on the effectiveness of treatment and patient tolerance.
4. Side effects: The drug may cause various side effects such as drowsiness, dizziness, digestive disorders, dry mouth, weight changes, sleep disturbances, decreased sex drive, and extrapyramidal disorders (movement disorders).
5. Contraindications and cautions: Sulpiride is contraindicated in case of allergy to the drug, and is not recommended in acute intoxication with alcohol, in renal and hepatic impairment, in pregnancy and lactation, as well as in severe cardiac rhythm disturbances. When using sulpiride, it is important to follow the doctor's recommendations and regularly monitor the patient's condition.

Indications Sulpiride

1. Schizophrenia: The drug is used to treat schizophrenia, a serious mental disorder characterized by disturbances in thinking, perception, and behavior.
2. Other psychiatric disorders: The drug may also be used in the treatment of other psychiatric disorders such as psychotic states, delusional disorders, manic-depressive syndromes and panic attacks.
3. Anxiety disorders: In some cases, sulpiride may be prescribed for the treatment of anxiety disorders, especially if there are associated symptoms such as panic attacks, phobias, or obsessive-compulsive disorder.
4. Guillain-Barré syndrome: The drug may be used in the treatment of Guillain-Barré syndrome, which is an acute and acute recurrent psychosis characterized by affective disappearances, aggression and panic attacks.
5. Behavioral disorders in children: Sometimes the drug may be prescribed to treat behavioral disorders in children, such as hyperactivity, aggressive behavior, or neurotic symptoms.

Release form

1. Capsules

• Description: The drug is most often available in the form of capsules, which are convenient for oral administration.
• Dosage: Capsules usually contain 50 mg to 200 mg of sulpiride.

2. Pills

• Description: An alternative form to capsules, tablets are also intended for oral administration.
• Dosage: Tablets may contain varying amounts of sulpiride, similar to capsules.

3. Solution for injection

• Description: The drug may also be available as a solution for injection, which is used for more rapid relief of symptoms when oral administration is not possible or is ineffective.
• Dosages: The solution usually contains a certain amount of sulpiride per milliliter and is administered intramuscularly or intravenously in a healthcare facility.

4. Suspension for oral administration

• Description: The oral liquid form of sulpiride is particularly suitable for patients who have difficulty swallowing solid dosage forms.
• Dosage: The content of sulpiride in suspension is similar to capsules and tablets.

Pharmacodynamics

Sulpiride is an antipsychotic drug that exerts its effect primarily by blocking dopamine D2 receptors in the central nervous system. This mechanism is characteristic of typical first-generation antipsychotics, also known as neuroleptics.

Blocking dopamine receptors in various areas of the brain leads to a decrease in dopaminergic activity, which may help in reducing psychotic symptoms such as hallucinations, delusions, and thought disorders.

The drug also has some activity towards serotonin, histamine and some other receptors, which may influence its pharmacological effects.

Pharmacokinetics

1. Absorption: The drug is usually well absorbed from the gastrointestinal tract after oral administration. The maximum concentration is usually reached 2-6 hours after administration.
2. Distribution: It has a medium volume of distribution and can penetrate the blood-brain barrier, reaching the central nervous system.
3. Protein binding: Sulpiride binds to blood plasma proteins at a level of about 40-45%.
4. Metabolism: The drug is metabolized in the liver, where it undergoes glucuronidation and oxidation. The main metabolites are sulfoxide and sulfonylmethyl.
5. Excretion: Most sulpiride is excreted through the kidneys as metabolites, mainly within the first 24 hours after administration.
6. Sulpiride's eliminationhalf-life is about 8-10 hours, which means that most of the drug is eliminated from the body within 24 hours.

Dosing and administration

Ways of application:

Sulpiride may be taken orally in tablet or capsule form, or given by injection (intramuscular or intravenous) if faster action is needed or if oral administration is not possible.

• Oral Use: Tablets or capsules should be taken with water, preferably during or after meals to minimize gastric discomfort.
• Injectionadministration: Sulpiride Injection is administered by healthcare professionals for conditions requiring rapid correction of symptoms.

Dosages:

The dosage of sulpiride depends on the specific disease, its severity and the patient's response to treatment.

Adults:

• Psychiatric disorders (e.g., schizophrenia, depression):

  • Oral: Usually start with 200-400 mg daily, divided into 2-3 doses. Depending on treatment response and tolerance, the dose may be increased to 600-1200 mg daily.
  • Injections: The dosage and regimen are determined by the treating physician.

• Dyspeptic disorders (e.g., delayed gastric emptying):

  • Oral: Usually 50 mg 3 times daily before meals.
  • Injections: May be used for quick relief of symptoms, dosage to be determined by a physician.

Elderly patients:

• The dose for elderly patients should be reduced due to possible slowing of metabolic processes and risk of side effects. The initial dose may be 1/2 of the adult dose.

Special Instructions:

• Renal insufficiency: In renal insufficiency, the dose should be adjusted downward because sulpiride is excreted by the kidneys.
• Duration of treatment: The duration of use and the possibility of discontinuation of treatment should be determined by the attending physician.
• Side effects: Extrapyramidal symptoms such as tremor, rigidity, bradykinesia, and possible endocrine disorders (e.g., gynecomastia, menstrual disorders) should be monitored.

Use Sulpiride during pregnancy

The use of sulpiride during pregnancy should be carried out only on strict medical indications and under medical supervision. The effect of sulpiride on pregnancy has not been fully studied and its safety for the fetus has not been established.

During pregnancy, sulpiride should be prescribed only when the benefits to the mother significantly outweigh the potential risks to the fetus. The physician should carefully evaluate the indications for use and have a discussion with the patient to make an informed decision about whether the drug should be used in this situation.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to sulpiride or other components of the drug should avoid its use due to the risk of allergic reactions.
2. Parkinsonism: The drug is contraindicated in parkinsonism and patients with other extrapyramidal disorders, as it may aggravate symptoms and worsen the condition.
3. Severe hepatic or renal impairment: In patients with severe hepatic or renal impairment, use of sulpiride with caution or under medical supervision is recommended because its metabolism may be impaired.
4. Cardiovascular diseases: The drug should be used with caution in patients with cardiovascular diseases such as arterial hypertension, heart failure or arteriosclerosis.
5. Seizure syndrome: In seizure disorders, including a history of epilepsy, the use of sulpiride may increase the risk of seizures.
6. Contraindicated drugs: The drug is contraindicated in concomitant use with certain drugs such as monoamine oxidase inhibitors (MAOIs) and antiparkinsonian drugs.
7. Pregnancy and lactation: The use of sulpiride during pregnancy and lactation may be undesirable unless the potential benefits are judged to exceed the possible risks.
8. Children and adolescents: Data on the safety and efficacy of sulpiride in children and adolescents may be limited, therefore its use in this group of patients requires special attention and strict prescribing by a physician.

Side effects Sulpiride

1. Extrapyramidal symptoms: This group includes tremors, gesticulation, muscle cramping, akinesia (impaired motor activity) and dyskinesia (unusual, involuntary movements). These symptoms may be particularly severe in elderly patients.
2. Drowsiness and fatigue: The drug may cause drowsiness and decreased activity, which may affect the ability to drive a car or operate machinery.
3. Dry mouth: Patients may experience a dry mouth sensation, which may lead to discomfort and reduced salivation.
4. Digestive disorders: Gastrointestinal disorders such as nausea, vomiting, diarrhea, constipation or increased appetite may occur.
5. Erectile dysfunction and urinary disorders: Some men may experience erectile problems and decreased libido, as well as urinary disorders such as urinary retention or urinary frequency.
6. Elevation of prolactin: Long-term use of sulpiride may result in an increase in prolactin levels in the blood, which can lead to gynecomastia (enlargement of the mammary glands in men) and galactorrhea (discharge of milk from the mammary glands in men and women).
7. Allergic reactions: In rare cases, allergic reactions such as skin rash, itching, urticaria or angioedema may occur.

Overdose

An overdose of sulpiride can cause serious side effects such as seizures, hyperthermia, extrapyramidal symptoms (movement disorders), decreased blood pressure, tachycardia, coma, arrhythmias, and even death.

Interactions with other drugs

1. Drugs affecting the central nervous system (CNS): The drug may increase the effects of other drugs that affect the CNS, such as alcohol, sleeping pills, sedatives, antidepressants, and some antihistamines. This may result in increased sedation and decreased response of the external world.
2. Antiparkinsonian drugs: Sulpiride may reduce the efficacy of antiparkinsonian drugs such as levodopa, carbidopa or other antiparkinsonian agents. This is due to the antagonistic effect of sulpiride on dopamine receptors.
3. Anticonvulsants: The drug may increase the effect of anticonvulsants such as phenytoin or carbamazepine, which may lead to an increased risk of seizures.
4. Antihypertensive drugs: Sulpiride may increase the hypotensive effect of antihypertensive drugs such as beta-adrenoblockers or angiotensin-converting enzyme inhibitors (ACEIs), which may lead to an increased risk of hypotensive reactions.
5. Drugs affecting the rhythm of the heart: The drug may increase the cardiotoxicity of drugs affecting the rhythm of the heart, such as antiarrhythmic drugs, antidepressants or antihistamines, which may lead to an increased risk of arrhythmias.