Nemonapride
Template:Short description Template:Cs1 config Template:Drugbox Nemonapride, also previously known as emonapride and sold under the brand name Emilace, is an atypical antipsychotic which is used in the treatment of schizophrenia.[1][2][3] It is taken by mouth.[1][2]
Side effects of nemonapride include akathisia, dystonia, hypokinesia, tremor, hypersalivation, and hyperprolactinemia, among others.[1][2] The drug acts as a dopamine D2, D3, and D4 receptor antagonist.[1] To a lesser extent, it is also a serotonin 5-HT1A receptor partial agonist.[4] Structurally, nemonapride is a benzamide derivative and is related to sulpiride and other benzamides.[1]
Nemonapride was introduced for medical use in either 1991[5] or 1997.[1][6] It was developed and marketed by Yamanouchi Pharmaceuticals.[6][7] The drug is approved only in Japan and China.[8]
Medical uses
Nemonapride is used in the treatment of schizophrenia.[1][2] It is described as being effective in treating the positive symptoms of schizophrenia.[1] It is also said to have some antidepressant and anxiolytic effects.[1] However, clinical data on nemonapride are described as being somewhat limited.[1]
Available forms
Nemonapride is available in the form of 3 and 10Script error: No such module "String".mg oral tablets.[2]
Side effects
Side effects of nemonapride include akathisia, dystonia, hypokinesia, tremor, hypersalivation, and hyperprolactinemia, among others.[1][2]
Pharmacology
Pharmacodynamics
Nemonapride has been described both as a typical antipsychotic[1] and as an atypical antipsychotic.[9] It is a potent and selective dopamine D2, D3, and D4 receptor antagonist.[1] Its affinities (Ki) for these receptors are 0.16Script error: No such module "String".nM for the dopamine D2 receptor, 0.26Script error: No such module "String".nM for the dopamine D3 receptor, and 0.31Script error: No such module "String".nM for the dopamine D4 receptor.[1] Antagonism of the dopamine D2 receptor is thought to be responsible for the antipsychotic effects of nemonapride.[2]
In addition to the dopamine D2-like receptors, nemonapride has weaker affinity for the serotonin 5-HT1A and 5-HT2A receptors.[1] Its affinities (Ki) for these receptors are 1.8Script error: No such module "String".nM for the serotonin 5-HT1A receptor (11-fold lower than for the D2 receptor) and 9.4Script error: No such module "String".nM for the serotonin 5-HT2A receptor (59-fold lower than for the D2 receptor).[1] It is a partial agonist of the serotonin 5-HT1A receptor.[10][1][11] It has very weak affinity for sigma receptors (Ki = 80–3,000Script error: No such module "String".nM) as well.[12] Besides these specific receptors, nemonapride is described as having very weak affinity for the dopamine D1, serotonin 5-HT2, adrenergic, and cholinergic receptors.[1]
In animals, nemonapride suppresses conditioned avoidance responses, inhibits methamphetamine- and apomorphine-induced hyperactivity and stereotypy, produces catalepsy, and has slight central depressant effects.[1][2]
Pharmacokinetics
Nemonapride is metabolized primarily by the cytochrome P450 enzyme CYP3A4.[2] Its elimination half-life is 2.3 to 4.5Script error: No such module "String".hours.[2]
Chemistry
Nemonapride is a benzamide derivative and is structurally related to other dopamine antagonists of the benzamide group such as sulpiride.[1]
Structure and stereochemistry
Nemonapride is a cis-2-methyl-3-amino-pyrrolidine derivative,[13] which was later shown to express most of its action as a drug to treat schizophrenia from its homochiral (+)-(2R,3R) form.[14][15]
History
Nemonapride was developed by scientists at Yamanouchi Pharmaceuticals via structural modification of the benzamide antiemetic and gastroprokinetic agent metoclopramide.[6][13] It was first described in the scientific literature by 1980.[16] The name nemonapride was first used by 1989 and this name was designated as its INN in 1991.[17][18] The drug was launched in May 1991.[5] However, other sources state that it was launched in 1997.[1][6]
Society and culture
Names
Nemonapride is the generic name of the drug and its INN and JAN.[8][7][19] It was also previously known as emonapride and by its former developmental code name YM 09151-2.[8][7][19][20] In addition, nemonapride is known by its brand name Emilace (JP: エミレース) in Japan and China.[8][7][19]
Availability
Nemonapride is marketed only in Japan and China.[8][7] It was also under development for use in other countries, such as France, but development in other countries was discontinued.[3][1] There are no further plans for nemonapride to be developed for use in the United States, the United Kingdom, or Europe.[1]
See also
- ENX-104, a deuterated analog under development at low doses for depression
References
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Template:Dopamine receptor modulators Template:Serotonin receptor modulators