A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers.

Article Details

Citation

Rosenzweig P, Canal M, Patat A, Bergougnan L, Zieleniuk I, Bianchetti G

A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers.

Hum Psychopharmacol. 2002 Jan;17(1):1-13.

PubMed ID
12404702 [ View in PubMed
]
Abstract

Amisulpride binds selectively to dopamine D(2) and D(3) receptors in the limbic system. Low doses of amisulpride preferentially block presynaptic D(2)/D(3)-dopamine autoreceptors, thereby enhancing dopaminergic transmission, whereas higher doses block postsynaptic receptors, thus inhibiting dopaminergic hyperactivity. Amisulpride is clinically effective on the negative symptoms of acute schizophrenia exacerbations at low dosages (50-300 mg/day), and also on the positive symptoms of the disease at high dosages (400-800 mg/day). Nineteen clinical studies involving 358 volunteers have investigated the pharmacokinetics, pharmacodynamics and tolerability of amisulpride. Amisulpride shows linear pharmacokinetics, a bioavailability of 48%, low protein binding (17%) and an elimination half-life of approximately 12 h. It is predominantly eliminated in the urine as the parent compound. It exhibits no significant detrimental effects in psychometric or memory tests up to the dose of 400 mg/day, inducing only mild impairment at high doses, whereas EEG data suggest an alertness-enhancing effect at low doses (

DrugBank Data that Cites this Article

Drugs
Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
AmisulprideDopamine D2 receptorProteinHumans
Yes
Antagonist
Details
AmisulprideDopamine D3 receptorProteinHumans
Yes
Antagonist
Details