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NERVOUS SYSTEM › PSYCHOLEPTICS › ANTIPSYCHOTICS › Benzamides
levosulpiride
N05AL07
Forms & Strengths
- Tablet: 25 mg
- Oral drops: 25 mg/mL
- Syrup: 5 mg/mL
- Injection: 25 mg/2 mL
Adult Dosing
- Gastrointestinal disorders: 25 mg orally 3 times daily before meals
- Psychiatric disorders (anxiety/depression/somatization): 25 mg to 50 mg orally 3 times daily
Pediatric Dosing
- Safety and efficacy not well established in children; use generally not recommended
Indications
- Functional dyspepsia
- Gastroparesis and diabetic neuropathy-related GI symptoms
- Irritable bowel syndrome (IBS)
- Short-term management of anxiety and depressive disorders
Mechanism of Action
- Selective dopamine D2 receptor antagonist in both the central nervous system and the gastrointestinal tract
- Prokinetic effect mediated via enteric nervous system stimulation enhancing upper GI motility
- Central antidopaminergic action contributes to antiemetic, anxiolytic, and antidepressant properties
- Enantiomer (l-isomer) responsible for high binding affinity to dopamine D2 and D3 receptors
Contraindications
- Known hypersensitivity to levosulpiride or substituted benzamides
- Pheochromocytoma (risk of hypertensive crisis)
- Epilepsy and states with history of seizures
- Mania and acute psychotic states
- Prolactin-dependent tumors (e.g., pituitary prolactinoma, breast cancer)
- Concurrent use with drugs that prolong QT interval or cause extrapyramidal reactions
- Gastrointestinal hemorrhage, mechanical obstruction, or perforation
Adverse Reactions
- Somnolence and fatigue
- Weight gain
- Hyperprolactinemia (galactorrhea, gynecomastia, amenorrhea)
- Extrapyramidal symptoms (acute dystonia, parkinsonism, tardive dyskinesia with prolonged use)
- Orthostatic hypotension
- QT interval prolongation
Drug Interactions
- Levodopa and dopamine agonists: Mutual antagonism of therapeutic effects
- Anticholinergic agents: May antagonize the gastrointestinal prokinetic effects of levosulpiride
- CNS depressants (alcohol, opioids, sedatives): Enhanced sedation and central nervous system depression
- QT-prolonging drugs (antiarrhythmics, antipsychotics, certain antibiotics): Increased risk of ventricular arrhythmias
- Antihypertensive agents: Potential for additive hypotensive effects
Curated Content: Needs Vetting Before Put to Clinical Use