Antispasmodic agent

Ethanolpyridines are used mainly for vinylpyridine manufacture. However, 2-ethanolpyridine (22) is used to make the psychotropic agent thioridazine [50-52-2] (106), and the antispasmodic agent triquizium bromide [71731-58-3] (107). 

L-Dopa and Trimethoprim are two other dmgs that can be made from vanillin. u-Dopa is used for the treatment of Parkinson s disease Trimethoprim is an antiinfective agent used mainly for urinary tract infections and certain venereal diseases. Also, Mebeverine, an antispasmodic agent, and Verazide, a generic antitubercular agent, are dmgs that can be made from vanillin or its derivatives. 

Substitution of an alicyclic ring for one of the aromatic rings in the amino alcohols such as 32 or 39 produces a series of useful antispasmodic agents that have found some use in the treatment of the symptoms of Parkinson s disease. Mannich reaction of acetophenone with formaldehyde and piperidine affords the amino-ketone, 44a. Reaction of the ketone with cyclohexylmagnesium... 

The antispasmodic agent, chlorzoxazone (56), is obtained by cyclization of the o-hydroxybenzformamide (55), a general method... 

A great many organic quaternary bases can inhibit the action of acetyl choline in organ systems activated by that neurotransmitter and thus possess anticholinergic-antispasmodic activity. One such agent is methantheline bromide (4), used in the treatment of peptic ulcer and as an antispasmodic agent in intestinal disorders. Its synthesis Involves Friedel-Crafts cyclization of o-... 

Reduction of the exocyclic double bond generally decreases neuroleptic activity in this series. Some of these compounds, however, show other activities. Methixene (44), for example, is used as an antispasmodic agent. It is prepared by alkylation of the sodium salt of thioxanthene (43) with w-methyl-3-chloromethyl-piperidine. ... 

Substitution of somewhat more complex side chains on the imidazole nitrogen of the purines leads to CNS stimulant drugs that have also been used as vasodilators and antispasmodic agents. Thus, alkylation of theophyline (2) with ethyl bromoacetate followed by saponification of the product gives acephylline (9). Alkylation with l-bromo-2-chloroethane gives the 2-chloroethyl derivative (10). Reaction of that intermediate with amphetamine yields fenethylline (11). ... 

Antispasmodic agents such as dicyclomine or hyoscyamine have been among the most frequently used medications for treating abdominal pain in patients with IBS (Table 18-5). 

Antispasmodic agents such as oxybutynin 5 mg by mouth two to three times daily may be used for bladder spasms. In patients with refractory pain, opioid analgesics should be titrated to adequate pain control. 

Mechanism of Action A urinary antispasmodic agent that acts as a direct antagonist at muscarinic receptor sites in cholinergically innervated organs. Blockade of the receptors limits bladder contractions. Therapeutic Effect Reduces symptoms of bladder irritability and overactivity improves bladder capacity. 

Methylchromone (Tricromyl or Crodimyl) possesses muscle relaxant properties and exerts a vasodilator effect on coronary blood vessels, whilst the flavone derivative Flavoxate (Urispas) (725) is an antispasmodic agent which reduces smooth muscle spasm in the urinary tract. The isofiavone Formononetin (726) is a diuretic and Dimeffine (Remeflin) (727) is a respiratory stimulant. 

Aniseed is used in folk medicine as an antispasmodic agent. Tirapelli et al. (2007) report that ethanokwater (40 60) extract of aerial parts of anise (50pg/ml) inhibited acetylcholine-induced contraction in rat smooth muscle. 

Teratogenic activity has been attributed to doxylamine, a constituent of many combinations with vitamin B6 and antispasmodic agents, and used in the treatment of hyperemesis gravidarum. However, extensive studies and reviews have suggested that the incidence of malformations is not higher in children whose mothers have taken formulations containing antihistamines as a group, and in particular the combination of doxylamine/pyridoxine with or without dicycloverine (100-102). 

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