Sulpiride: an Antipsychotic with Selective Dopaminergic Antagonist Properties

Caley, Charles F.; Weber, Stanley S.

doi:10.1177/106002809502900210

Cited by 251 publications

(47 citation statements)

References 45 publications

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“…The ECG showed no changes, except benign, nonspecific changes in T waves that occurred in some patients receiving dosages of over 1600 mg/day. Other studies [12,31] also failed to show any clinically relevant influence on cardiovascular parameters; on the whole, sulpiride was well tolerated in this regard.…”

Section: Other Adverse Effectsmentioning

confidence: 90%

“…[16.17] It does not appear to significantly block other types of receptors such as histaminergic, cholinergic, serotonergic, adrenergic and y-aminobutyric acid (GABA) receptors. [12] Although the heuristic value of the dopamine hypothesis of schizophrenia can hardly be denied, a modified version has been recently put forward . This proposes that dopaminergic hyperactivity best explains positive symptoms, while negative symptoms are rather more suggestive of dopaminergic hypofunction.…”

Section: Pharmacodynamics Of Sulpiridementioning

confidence: 99%

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A Risk-Benefit Assessment of Sulpiride in the Treatment of Schizophrenia

et al. 1996

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Sulpiride is a substituted benzamide with a selective action on receptors of the dopamine D2-like family, and clinical and pharmacological data suggest that it could be considered to be an atypical antipsychotic. Sulpiride penetrates the blood-brain barrier poorly because of its low lipid solubility. It is mainly excreted unchanged in the urine, and accumulation of the drug could occur in patients with renal dysfunction and possibly in elderly patients with declining glomerular filtration rate. At low dosages (50 to 150 mg/day), sulpiride produces a disinhibiting and antidepressant effect, which is probably related to its action on D2 presynaptic autoreceptors, thus facilitating dopaminergic neurotransmission. Data have confirmed the efficacy of sulpiride in patients with acute or chronic schizophrenia during both short and long term treatment, but long term, placebo-controlled trials are still lacking. It is still doubtful whether sulpiride is more effective than typical antipsychotics for the treatment of negative symptoms. Data from clinical studies are controversial; the majority of authors indicate that sulpiride produces a better recovery rate from negative than from positive symptoms at low doses, but it shows a similar efficacy either on negative and positive symptoms at higher doses. The safety profile of sulpiride is similar to that of typical antipsychotics, although the frequency of adverse effects seems to be globally lower. Extrapyramidal reactions appear generally to be mild. Autonomic effects occur less frequently with sulpiride than with typical antipsychotics, showing no clinically relevant influence on cardiovascular parameters and, on the whole, good tolerability in elderly patients. Sulpiride is known to induce prolactin elevation in both serum and CSF, which may be associated with impotence in men and diminished gonadal function in women; these effects appear to be dosage-dependent. Sulpiride can be considered to be an atypical antipsychotic, considering its action on negative, defective symptoms, its partial activity against positive symptoms, and its low incidence of extrapyramidal adverse effects. Sulpiride could find its specific therapeutic role in elderly patients with schizophrenia, as it shows a good margin of safety between therapeutic dosages and toxic concentrations.

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Section: Other Adverse Effectsmentioning

confidence: 90%

Section: Pharmacodynamics Of Sulpiridementioning

confidence: 99%

A Risk-Benefit Assessment of Sulpiride in the Treatment of Schizophrenia

et al. 1996

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“…Although some may consider sulpiride an atypical antipsychotic, it elevates prolactin and is not a serotonin-dopamine antagonist and is therefore included here as a conventional agent [45][46]. Literature regarding the simultaneous use of one of the four first-line atypical antipsychotics and a conventional antipsychotic is sparse.…”

Section: Atypical-conventional Antipsychotic Polypharmacymentioning

confidence: 99%

A Critical Review of Atypical Antipsychotic Utilization: Comparing Monotherapy with Polypharmacy and Augmentation

Stahl¹,

Mm²

2004

CMC

159

118

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The atypical antipsychotics risperidone, olanzapine, quetiapine, ziprasidone, and aripiprazole have become first-line treatment for schizophrenia because they reduce the positive symptoms of psychosis but do not have a high incidence of extrapyramidal symptoms. However, these agents, like other antipsychotics, may take as long as 16 or more weeks to produce a response, and even with prolonged treatment are unlikely to evoke responses greater than 50% improvement in symptoms. This has led to the experimental use of high atypical antipsychotic doses, antipsychotic polypharmacy, and augmentation with other psychotropic drugs, all of which occur commonly in clinical practice. This article reviews the current evidence for these increasingly common means of treating schizophrenia and psychosis, with particular emphasis on polypharmacy and augmentation. To date, there are only two controlled studies of antipsychotic polypharmacy involving an atypical antipsychotic; the rest of the data are uncontrolled trials and case reports that describe a mixture of positive and negative findings. One multicenter, double-blind trial shows a faster onset of action when divalproex is added to risperidone or olanzapine than with antipsychotic monotherapy. A small double-blind study demonstrates efficacy when lamotrigine is added to clozapine. The rest of the data on augmentation with anticonvulsants are uncontrolled, and most report adverse effects. With the exception of divalproex, there are currently no compelling data to justify the use of antipsychotic polypharmacy or augmentation. Existing evidence suggests that the best treatments for schizophrenia and psychosis may be long-term trials of a sequence of atypical antipsychotic monotherapies at therapeutic doses.

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“…6,7) After oral administration of 100-400 mg in humans, peak plasma levels of 0.2-1.5 mg/ml are obtained within 1-3 h, and the elimination half life is 7-8 h. [8][9][10] After intravenous administration of sulpiride, 70% of the dose is recovered as unchanged drug in urine, as compared to 15% after oral administration, 11) and the bioavailability of the oral form is 25-36%. 10,11) After oral dosing of 14 C-labeled sulpiride, urinary excretion of radioactivity was 27-52%, and more than 95% of the radioactivity recovered in the urine and feces is unchanged sulpiride.…”

mentioning

confidence: 99%