Amisulpride versus moclobemide in treatment of clozapine-induced hypersalivation

Kreinin, Anatoly; Miodownik, Chanoch; Sokolik, Shmuel; Shestakova, Diana; Libov, Igor; Bergman, Joseph; Lerner, Vladimir

doi:10.3109/15622975.2010.527370

Cited by 22 publications

(18 citation statements)

References 54 publications

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“…Several other pharmacologic strategies have been explored. The antipsychotics sulpiride and amisulpride have shown promising results in several small trials, as has the monoamine oxidase inhibitor moclobemide. Finally, botulinum toxin injection has been shown to substantially improve antipsychotic‐induced sialorrhea for 8‐16 weeks.…”

Section: Specific Adverse Effectsmentioning

confidence: 99%

Management of common adverse effects of antipsychotic medications

2018

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The benefits of antipsychotic medications are sometimes obscured by their adverse effects. These effects range from relatively minor tolerability issues (e.g., mild sedation or dry mouth) to very unpleasant (e.g., constipation, akathisia, sexual dysfunction) to painful (e.g., acute dystonias) to disfiguring (e.g., weight gain, tardive dyskinesia) to life-threatening (e.g., myocarditis, agranulocytosis). Importantly, adverse effect profiles are specific to each antipsychotic medication and do not neatly fit into first- and second-generation classifications. This paper reviews management strategies for the most frequent side effects and identifies common principles intended to optimize net antipsychotic benefits. Only use antipsychotics if the indication is clear; only continue antipsychotics if a benefit is discernible. If an antipsychotic is providing substantial benefit, and the adverse effect is not life-threatening, then the first management choice is to lower the dose or adjust the dosing schedule. The next option is to change the antipsychotic; this is often reasonable unless the risk of relapse is high. In some instances, behavioral interventions can be tried. Finally, concomitant medications, though generally not desirable, are necessary in many instances and can provide considerable relief. Among concomitant medication strategies, anticholinergic medications for dystonias and parkinsonism are often effective; beta-blockers and anticholinergic medications are useful for akathisia; and metformin may lead to slight to moderate weight loss. Anticholinergic drops applied sublingually reduce sialorrhea. Usual medications are effective for constipation or dyslipidemias. The clinical utility of recently approved treatments for tardive dyskinesia, valbenazine and deutetrabenazine, is unclear.

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Section: Specific Adverse Effectsmentioning

confidence: 99%

Management of common adverse effects of antipsychotic medications

2018

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“…The atypical antipsychotic drug amisulpride has been reported to reduce a troublesome ‘sialorrhea’/drooling in schizophrenic patients under treatment with clozapine, the archetype of atypical antipsychotics (Gardner and Teehan, ), as judged by a ‘hypersalivation rating scale’ (Kreinin et al , , ). In the course of a preclinical investigation on the clozapine‐induced ‘sialorrhea’ and its treatment, using the duct‐cannulated rat parotid and submandibular glands as experimental models, we established a secretory role of clozapine by its agonistic action on muscarinic M1 type of receptors of the secretory cells – besides an antagonistic action on muscarinic M3 and α (1) ‐adrenergic receptors.…”

Section: Introductionmentioning

confidence: 99%

The antipsychotic amisulpride: ultrastructural evidence of its secretory activity in salivary glands

Loy

Isola

et al. 2013

Oral Diseases

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“…As a result of the discomfort, the drug regimen is discontinued. The strategies suggested to abolish clozapine‐induced sialorrhoea include treatment with amisulpride, a substitute benzamide derivate (3, 4). Data from clinical studies which have measured the volume of saliva secreted, are few and contradictory (5–7).…”

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confidence: 99%

Clozapine-induced salivation: interaction with N-desmethylclozapine and amisulpride in an experimental rat model

Godoy

Riva

Ekström

2011

European Journal of Oral Sciences

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Many drugs (e.g. amisulpride) have been used to treat troublesome clozapine-induced salivation; however, varying success has been achieved in this respect, probably because, until recently, the salivatory action of clozapine has been largely unexplained. In the rat, clozapine and its main metabolite, N-desmethylclozapine, were found to exert mixed secretory actions: excitatory, through muscarinic acetylcholine M1-receptors giving rise to a long-lasting, low-level flow of saliva; and inhibitory, through muscarinic M3-receptors and α(1) -adrenoceptors reducing the parasympathetically and sympathetically nerve-evoked flow of saliva. The aim of the present study was to define the interactions between clozapine and N-desmethylclozapine, and clozapine and amisulpride, with respect to the excitatory response. Submandibular glands, sensitized by chronic parasympathetic preganglionic denervation, were studied in pentobarbitone-anaesthetized rats. To prevent clozapine from being metabolized to N-desmethylclozapine by hepatic enzymes, the liver was, under terminal anaesthesia, excluded from the circulation. The weak receptor-stimulating clozapine prevented the strong receptor-stimulating N-desmethylclozapine, at specific ratios in humans and in rats, from exerting its full agonistic action. In conclusion, the contribution of N-desmethylclozapine to the clozapine-induced sialorrhoea was, at most, only partly additive. Furthermore, the present experimental set-up failed to demonstrate any anti-salivatory action of amisulpride on the clozapine-induced flow of saliva.

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Amisulpride versus moclobemide in treatment of clozapine-induced hypersalivation

Abstract: Both medications were safe and effective as treatment of CIS. Although moclobemide exceeded amisulpride in antisalivation activity, treatment of CIS with amisulpride leads to improvement in psychotic symptoms.

Cited by 22 publications

References 54 publications

Management of common adverse effects of antipsychotic medications

Management of common adverse effects of antipsychotic medications

The antipsychotic amisulpride: ultrastructural evidence of its secretory activity in salivary glands

Clozapine-induced salivation: interaction with N-desmethylclozapine and amisulpride in an experimental rat model

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