Antispasmodic drugs

TABLE 50-3. Anticholinergic/Antispasmodic Drugs Recommended For Urge Urinary Incontinence... 

Muscle relaxants and antispasmodics methocarbamol (Robaxin), carisoprodol (Soma), chlorzoxazone (Paraflex), metaxalone (Skelaxin), cyclobenzaprine (Flexeril), and oxybutynin (Ditropan) Do not consider the extended-release Ditropan XL Most muscle relaxants and antispasmodic drugs are poorly tolerated by elderly patients, because these cause anticholinergic adverse effects, sedation, and weakness. Additionally, their effectiveness at doses tolerated by elderly patients is questionable. High... 

If patients are on antispasmodic drugs, formulas that stabilize and bind should be used with caution. 

Tritium-labelled 7V-(4-phenylphenacyl)heliotridanium bromide (55) has been prepared. The absorption, tissue distribution, and excretion of this radioactive antispasmodic drug in rats were then studied.84... 

Angelico et al. (1992) reported in vivo effects of different antispasmodic drugs on the rat bladder contractions induced by topically applied KC1. 

Andersson KE, Mattiasson A, Sjogren S (1983) Electrically induced relaxation of the noradrenaline contracted isolated urethra from rabbit and man. J Urol 129 210-214 Andersson KE, Pascual AG, Persson K et al. (1992) Electrically-induced, nerve-mediated relaxation of rabbit urethra involves nitric oxide. J Urol 147 253-259 Angelico P, Guameri L, Fredella B, Testa R (1992) In vivo effects of different antispasmodic drugs on the rat bladder contractions induced by topically applied KC1.1 Pharmacol Meth 27 33-39... 

The antispasmodic drug biperidin is made by the Grignard addition reaction shown here. What is the structure of the drug Do not be put off by the apparent complexity of the compounds-—the chemistry is the same as that you have seen in this chapter. How would you suggest that the drug procyclidine should be made ... 

Symptomatic diverticular disease often responds to an increase in dietary fibre, and addition of a stool bulking agent. Antispasmodic drugs are helpful in controlling the pain of colon spasm but antimotility drugs encourage stasis of bowel contents, increase intracolonic pressure, and should be avoided. Diverticulitis requires treatment with broad spectrum antimicrobials for 7-10 days (e.g. 

Ketobemidone is an opioid receptor agonist, with pharmacokinetics and potency similar to morphine. Combined with the antispasmodic drug, A,A-dimethyl-3,3-diphenyl-l-methylallylamine chloride, ketobemidone is often used in Scandinavia. 

Mebeverine is an antispasmodic drug that is claimed to act directly on the colonic mnscle and is virtnally free of systemic adverse reactions. It has been nsed to treat irritable bowel syndrome, bnt its therapentic effect is poor. 

Hyoscyamine, an anticholinergic and antispasmodic drug related to atropine, has also been suggested for treating UUI, but data are insufficient to recommend its use. " ... 

Dipyrone is a water-soluble pyrazolone derivative available in oral, rectal, and injectable forms. It has been recogifized as an effective analgesic, antipyretic, and antispasmodic drug. Some antiinflammatory properties have also been recogifized in pharmacological models, although it is stiU questionable whether this is of any clinical relevance. Dipyrone is indicated in severe pain, particularly, pain associated with smooth-muscle spasm or colic affecting the GI, biliary, or urinary tract. It is also useful in fever that is refractory to other treatment. 

Total reduction of a benzene to a cyclohexane ring requires pressure and active catalysts and is more easily done industrially than in the lab. The antispasmodic drug Dicyclomine (20) can be made this way" and this synthesis illustrates that six-membered rings can be made by methods other than the three presented in this chapter. Disconnection of the ester reveals acid (21) with one ring that could have been aromatic (22). Note that this is FGA logic (Chapters 24 and 28). Acid (22) can be made by simple alkylation, using cyanide (23) cf. Chapter 35). 

Another important natural product lead compound is the tropane alkaloid ester atropine [( )-hyoscyamine], from the piant Atropa belladonna (deadiy nightshade) Atropine has served as a prototype moiecuie for severai antichoiinergic and antispasmodic drugs. One recentiy introduced exampie cf an antichoiinergic compound modeied on atropine is tiotropium bromide, which is used fcr the maintenance treatment of bronchospasm associated with chronic obstructive puimcnary disease (54). 

Memantine might modify the effects of antispasmodic drugs such as dantrolene or baclofen and dosage adjustment might be required. ... 

Khellin (33), an antispasmodic drug that comprises approximately 1% of the dry weight of plants of Ammi visnaga (Apiaceae), has a pyrone structure reminiscent of that of many linear furanocoumarins (Fig. 9.6). This compound acts directly on smooth muscle, is a bronchial dilator, and is used in the treatment of asthma (Sneader, 1985). 

Goei R, Nix M, Kessels AH et al (1995) Use of antispasmodic drugs in double contrast barium enema examination glucagon or buscopan Clin Radiol 50 553-557 Gollub MJ, Jhaveri S, Schwartz E et al (2005) CT colonography features of sigmoid diverticular disease. Clin Imaging 29 200-206... 

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