Hexocyclium inhibits muscarinic action of acetylcholine on postganglionic parasympathetic effector regions. It is used for treating stomach ulcers. A synonym of this drug is tral.
14.1.3 Antiparkinsonian drugs of the quaternary amine series
Drugs that exhibit central anticholinergic properties are used in treating Parkinsonism. It is believed that they do not affect the synthesis, release, or hydrolysis of acetylcholine. Their medicinal efficacy is manifest by the reduction or removal of motor disturbances caused by damage to the extrapyramidal system. They reduce rigidity, and to a somewhat lesser degree, akinesia, and they have little effect on tremors.
The therapeutic value of these drugs is relatively small, and they are used either in combination with levodopa, or in cases of minor Parkinsonism. Drugs described in Chapter 10—trihexyphenidyl (10.2.2), procyclidine (10.2.3), biperiden (10.2.4), benztropine (10.2.6), ethopropazine (10.2.7), and others belong to this group of drugs.
Synthetic antispasmodics of the tertiary series (dicyclomine, oxybutynin, oxyphency-climine) exhibit direct antispastic action on smooth muscle and inhibit muscaric-like action of acetylcholine on smooth muscle.
These drugs have weaker anticholinergic activity than atropine; however, they have a significantly more expressed antispastic action. They are used for treating so-called irritable bowel syndrome and diarrhea.
Dicyclomine: Dicyclomine, diethylaminoethyl ester of 1-cyclohexylcyclohexanecarboxylic acid (14.1.32), is synthesized in two different ways. According to the first, benzyl cyanide undergoes alkylation by 1,5-dibromopentane, which forms 1-cyano-1-phenyl-cyclohexane (14.1.29). This undergoes alcoholysis, which gives the ethyl ester of 1-phenyl-1-cyclohexa-necarboxylic acid (14.1.30), which undergoes transesterification using 2-diethylaminoethanol in the presence of sodium as an alcoholic component, giving the 2-diethylaminoethyl ester of 1-phenylcyclohexanecarboxylic acid (14.1.31), the phenyl group of which is reduced to a cyclohexyl group using hydrogen over platinum oxide [24,25].
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