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

  title={A review of the pharmacokinetics, tolerability and pharmacodynamics of amisulpride in healthy volunteers},
  author={Pierre Rosenzweig and M. Canal and Alain A. Patat and Luc Bergougnan and Isabelle Zieleniuk and Gabrio Bianchetti},
  journal={Human Psychopharmacology: Clinical and Experimental},
Amisulpride binds selectively to dopamine D2 and D3 receptors in the limbic system. Low doses of amisulpride preferentially block presynaptic D2/D3‐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… 

Amisulpride: a review of its use in the management of schizophrenia.

Oral amisulpride is an effective and well tolerated option for the first-line treatment of patients with acute schizophrenia as well as for those requiring long-term maintenance therapy and does not seem to be associated with diabetogenic effects.

Amisulpride: a review of its use in the management of schizophrenia.

Its effective alleviation of negative and affective symptoms, its lower association with extrapyramidal symptoms and loss of cognitive function than conventional antipsychotics and its long-term efficacy justifies consideration of the use of higher dosages of amisulpride in this group of patients.

Plasma amisulpride levels in schizophrenia or schizoaffective disorder

Prandial effect on the systemic exposure of amisulpride

A randomized, two-way crossed trial in which a single oral dose of amisulpride was administered on two occasions, with 7-days washout period between each drug administration, to investigate the effect of food on the systemic exposure to amisULpride in healthy volunteers.

Spotlight on Amisulpride in Schizophrenia

In well-controlled trials, the neurological tolerability profile of amisulpride 400 to 1200 mg/day was superior to that of the conventional, and long-term treatment with amisULpride was associated with improvements in quality of life and social functioning.

Clinical Pharmacokinetics of Atypical Antipsychotics

This review of the literature concerning the relationships between plasma concentrations of SGAs and clinical responses is divided by dividing the studies on the basis of the length of their observation periods by indicating a relationship between clinical outcomes and plasma concentrations.

Amisulpride has no effect on plasma clozapine concentrations.

Knowing how clozapine and amisulpride interact could be particularly important as patients with schizophrenia might well profit from such a combination treatment; indeed, a few case reports and studies support this notion.

Update on the management of symptoms in schizophrenia: focus on amisulpride

  • A. Mortimer
  • Psychology, Medicine
    Neuropsychiatric disease and treatment
  • 2009
Amisulpride is efficacious, effective and well tolerated in positive symptoms of schizophrenia: there is extensive evidence that it treats negative symptoms when given in low doses, although relative lack of EPS and an antidepressant effect may contribute.

Characterization of the discriminative stimulus properties of the atypical antipsychotic amisulpride in C57BL/6 mice


Amisulpride: limbic specificity and the mechanism of antipsychotic atypicality

  • H. Möller
  • Psychology
    Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 2003



Effects of 50mg amisulpride on EEG, psychomotor and cognitive functions in healthy sleep‐deprived subjects

The present results demonstrate that 50 mg amisulpride is devoid of detrimental effects on EEG, psychomotor and cognitive performance after sleep deprivation, a situation well‐known to amplify such effects if they exist.

Neurochemical characteristics of amisulpride, an atypical dopamine D2/D3 receptor antagonist with both presynaptic and limbic selectivity.

Amisulpride is characterized as a specific dopamine receptor antagonist with high and similar affinity for the dopamine D2 and D3 receptor with a degree of limbic selectivity and a preferential effect, at low doses, on dopamine D 2/D3 autoreceptors.

Psychopharmacological profile of amisulpride: an antipsychotic drug with presynaptic D2/D3 dopamine receptor antagonist activity and limbic selectivity.

This pharmacological profile of amisulpride, characterized by a preferential blockade of effects involving presynaptic mechanisms and limbic structures, may explain the clinical efficacy of this drug against both negative and positive symptoms of schizophrenia and its low propensity to produce extrapyramidal side effects.

Single oral doses of amisulpride do not enhance the effects of alcohol on the performance and memory of healthy subjects

Amisulpride in single oral doses of 50 and 200 mg did not interact significantly with the effects of high, moderate or low concentrations of ethanol on human skilled and cognitive performance and slightly antagonised ethanol in the digit copying test.

Lack of interaction between amisulpride and lorazepam on psychomotor performance and memory in healthy volunteers

The co‐administration of amisulpride, at both doses of 50 mg and 200 mg, did not potentiate nor antagonize the detrimental effect of lorazepam 2 mg on pharmacodynamic parameters, and was devoid of any clinically relevant impairment psychometric tests, short term and long term memory and mood.

Psychomotor, Cognitive, extrapyramidal, and affective functions of healthy volunteers during treatment with an atypical (amisulpride) and a classic (haloperidol) antipsychotic.

Amisulpride seems to be a well-tolerated drug and its side effects should be much less troublesome to patients using the drug on a long-term basis than those of classic antipsychotics, like haloperidol.

The acute effects of amisulpride (50 mg and 200 mg) and haloperidol (2 mg) on cognitive function in healthy elderly volunteers

The general absence of cognitive impairments with amisulpride at the doses used in this study suggests that this compound does not impair cognitive function in the elderly.

Remoxipride versus haloperidol in healthy volunteers: psychometric performance and subjective tolerance profiles

In healthy subjects, an acute dose of 3 mg haloperidol caused more severe alteration in cognitive functioning, cortical arousal, and psychomotor performance than a clinically equipotent dose of 150 mg remoxipride.

Side effect profiles of new antipsychotic agents.

  • D. Casey
  • Medicine, Psychology
    The Journal of clinical psychiatry
  • 1996
Two new antipsychotic agents, olanzapine and sertindole, are added to the pharmacopeia for treating psychosis and greatly improve the treatment of psychosis by reducing drug-induced morbidity and improving the quality of life for patients.

A comparison of the psychometric effects of remoxipride with those of haloperidol, thioridazine, and lorazepam in healthy volunteers

In this placebo and verum (lorazepam 2 mg) controlled double‐blind crossover study the acute effects of Remoxipride 50 mg and 100 mg; Haloperidol 2·5 mg; and Thioridazine 50 mg were examined in 18