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Pharmacotherapeutic Group: Antipsychotics: benzamides. ATC Code: N05AL 01.
Pharmacology: Pharmacodynamics: Sulpiride specifically antagonises D2 and D3 antidopaminergic receptors. In patients with psychotic symptoms that cause negative symptoms, sulpiride is effective at doses of 150 to 600 mg/day. In this dosage range, sulpiride has practically no effect on positive symptoms. Doses of 600 to 1,600 mg/day improve positive symptoms in patients with acute or chronic psychosis. Only very high doses of sulpiride induce sedative effects.
Pharmacokinetics: Absorption: After intramuscular injection of 100 mg sulpiride, peak plasma concentrations of 2.2 mg/l were reached after 30 minutes (C_max).
When taken orally, sulpiride is absorbed within 4.5 hours after administration. The C_max corresponding to one oral dose (tablet) of 200 mg varies between 0.5 and 1.8 mg/l and between 0.1 and 0.6 mg/l after the administration of one 50 mg capsule. After one dose of 50 mg oral solution the C_max was 0.28 mg/l.
Distribution: The bioavailability of the oral forms varies between 25% and 35%, with extensive inter-individual variations. Plasma levels of sulpiride are proportional to the dose.
Sulpiride is distributed rapidly to body tissues, in particular to the liver and kidneys. There is scarce distribution in the brain.
Less than 40% of the drug binds to plasma proteins. The red blood cell/plasma distribution ratio is 1.
Metabolism: Sulpiride is not actively metabolised in humans.
Elimination: Sulpiride is primarily excreted by the kidneys, by glomerular filtration. Renal clearance is usually equal to the total clearance. Ninety-two per cent (92%) of the intramuscular dose is excreted unchanged in urine.
The amount excreted in human milk has been estimated at 1/1,000 of the daily dose.
The plasma elimination half-life is 7 hours. The distribution volume at steady state is 0.94 l/kg (from 0.6 to 1.5 l/kg). The total clearance is 126 ml/min.
Toxicology: Preclinical safety data: Experimental studies in animals showed no direct or indirect evidence of teratogenic effects on embryo-foetal development, childbirth or postnatal development.
A decrease in fertility related to the pharmacological effects of the drug (effect mediated by prolactin) has been observed in animals treated with sulpiride. This effect is reversible after treatment is discontinued.