SULPIRIDE 200 BIOTECH

Indications

• Schizophrenia
• Psychoses

Dosage

Children: For children, sulpiride should only be used under expert supervision, and specific dosing guidance is to be referred from the BNF for Children.

Adults: The initial dose for adults is typically 400mg daily, which may be increased based on clinical response and tolerability, with regular monitoring for side effects.

Mechanism of action

Sulpiride selectively antagonizes dopamine D2 and D3 receptors, with in silico studies indicating interactions with specific amino acid residues in these receptors. Optimal treatment is achieved with 65-80% occupancy of D2 receptors, which helps in minimizing adverse effects while providing therapeutic benefits.

Pharmacodynamics

As a substituted benzamide derivative, sulpiride has a short duration of action, necessitating administration twice daily. It exhibits a wide therapeutic window, with instances of patients surviving doses as high as 16g. However, it may lead to increased motor agitation, extrapyramidal reactions, and neuroleptic malignant syndrome, necessitating careful monitoring.

Pharmacokinetics

Sulpiride is absorbed well after oral administration and has a relatively long half-life, allowing for flexible dosing regimens. It undergoes minimal metabolism in the liver, and its elimination is primarily renal, necessitating dose adjustments in patients with renal impairment. Due to its pharmacokinetic profile, monitoring blood concentrations may be beneficial in specific clinical scenarios.

Contra-indications

• CNS depression
• comatose states
• history of arrhythmias
• history or family history of congenital QT prolongation
• phaeochromocytoma

Adverse effects

• acute dystonias
• breast abnormalities
• hypersalivation
• muscle tone increased
• orgasm abnormal
• decreased appetite
• depression
• fatigue
• headache
• hyperhidrosis
• restlessness
• sebaceous gland complaints

Interactions

• sulpiride + dopaminereceptor agonists: Severe (decreases effects)
• sulpiride + levodopa: Unknown (decreases effects)
• sucralfate + sulpiride: Unknown (decreases absorption)

Precautions

• Elderly patients should start with lower initial doses, increased gradually according to response
• Monitor for increased motor agitation and extrapyramidal symptoms
• Use caution in aggressive or excited patients as even low doses may aggravate symptoms
• Dose adjustments are necessary in severe renal impairment due to increased cerebral sensitivity

Pregnancy

Sulpiride should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult specific guidelines for further details.

Breast-feeding

Sulpiride is excreted in breast milk. Caution is advised if it is administered to nursing mothers.

Storage

Store in a cool, dry place away from light. Keep out of reach of children.

Formulations

• Sulpiride 200 mg tablets
• Sulpiride 400 mg tablets
• Sulpiride 200 mg/5 ml oral solution

Mechanism of action

Sulpiride is a selective dopamine D2 and D3 receptor antagonist. _In silico_ studies show that sulpiride may interact with the Asp-119 and Phe-417 amino acid residues of these receptors. It is estimated that D2 receptors should be 65-80% occupied for optimal treatment and minimal adverse effects.

Pharmacodynamics

Sulpiride is a substituted benzamide derivative and a selective dopamine D2 antagonist indicated to treat acute and chronic schizophrenia. It has a short duration of action as it is given twice daily, and a wide therapeutic window as patients have survived single doses as high as 16g. Patients should be counselled regarding increased motor agitation, extrapyramidal reactions, and neuroleptic malignant syndrome.