Benzamides Metoclopramide

Chlorpromazine Prochlorperazine Fluphenazine Butyrophenones Droperidol Domperidone Antihistamines Promethazine Diphenhydramine Benzamides Metoclopramide Serotonin antagonists Ondansetron Granisetron Tropisetron... 

Other examples of secondary benzamides include the therapeutic class of orthopramides, which are, again, markedly resistant to hydrolysis. Thus, hydrolysis of the amide bond is a minor metabolic pathway in humans for the antiemetic drug metoclopramide (4.76) [49]. Clebopride (4.77), an anti-dopaminergic agent, was found to be hydrolyzed to a limited extent in rabbit liver homogenates and in dogs to 4-amino-5-chloro-2-methoxybenzoic acid (4.78) and to the amine 4.79 [48] [50], Attempts to detect in vivo formation of this metabolite in rats, rabbits, or humans were not successful [50],... 

Benzamides are heterocyclic neuroleptics. These include the gastroenterologic agents metoclopramide and cisapride, which have antiserotonergic as well as anti-D2 receptor dopaminergic actions and also the antipsychotic agents sulpiride and tiapride. Tachyarrhythmias have resulted in the withdrawal of cisapride from general use. 

Substituted benzamides include metoclopramide and trimethobenzamide. Their primary mechanism of antiemetic action is believed to be dopamine-receptor blockade. Trimethobenzamide... 

Sulpiride is a member of a series of neuroleptics, the benzamides, of which the antiemetic drug metoclopramide is another example. The benzamides have a lower propensity to cause extrapyramidal side effects, probably because they show a high degree of selectivity for the D2 dopamine receptors. 

Alizapride is a substituted benzamide related to some neuroleptic drugs. In one study alizapride, in doses that were less effective than normal doses of metoclopramide, was equally likely to cause extrapyramidal effects and more likely to cause hypotension (SED-12, 939) (SEDA-17, 413). 

The primary benzamides used to enhance gastrointestinal motility are metoclopramide and cisapride. Each drug has its benefits and hazards, and recently cisapride was withdrawn from the market because of its potential to cause fatal cardiac arrhythmias in humans. 

Metoclopramide is a first-generation benzamide. The drug acts presynaptically, mainly as a 5-hydroxytryptamine (5-HT serotonin) 5-HT4 receptor agonist and 5-HT3 receptor antagonist but it is also an antagonist at dopamine 1 (Dj) and 2 (D2) receptors (MacDonald 1991). The net effect of the interactions with these receptors is to facilitate acetylcholine release from enteric neurons and promote smooth muscle contrachon. Metoclopramide... 

ML 10302 (RS 70678) is a substituted benzamide and analogue of metoclopramide, and is a (5-HT4-subtype) -HYDROXYTRYPTAMINE RECEPTOR AGONIST. 

Hanocq M, Topart J, van Damme M and Molle L, Determination of ionization constants for some substituted N-(2-diediylaminoethyl) benzamides, /. Pharm. Beige, 28, 649-662 (1975). Cited in Pitre D, Stradi R, Metoclopramide hydrochloride, APDS, 16,327-360 (1987). 

A 15-year, prospective cohort study of 2991 elderly patients evaluated the risk of developing Parkinson s disease and previous neuroleptic exposure [37. After adjustment for gender and past occupation, previous exposure to neuroleptics was associated with incident Parkinson s disease (relative risk, 3.16 95% confidence interval [Cl], 1.65-6.04), with a relative risk for benzamides (sulpiride, metoclopramide) of 3.65 (95% Cl, 1.41-9.45) and for phenothiazines (flunarizine, aceprometazine, levomepromazine, cyamemazine, thioridazine, athioproperazine) of 2.59 (95% Cl, 1.23-5.43). Of note, approximately a third of subjects had presented with transient Parkinsonism during drug exposure. 

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