Antispasmodics relaxants

N.A. Naphthaquinones, enzymes, flavonoids, volatile oil." Antimicrobial, antispasmodic, Relaxing the muscles of the respiratory tract. 

A similar pathway involving a microwave-driven molybdenum-catalyzed asymmetric allylic alkylation as the key step was elaborated by Moberg and coworkers for the preparation of the muscle relaxant (R)-baclofen (Scheme 6.52) [108]. The racemic form of baclofen is used as a muscle relaxant (antispasmodic) lipophilic derivative of y-aminobutyric acid (GABA). Pharmacological studies have shown that the (R)-enantiomer is the therapeutically useful agonist of the GABAb receptor. Asymmetric alkylation of the allylic carbonate precursor with dimethyl malonate afforded... 

The aforementioned polymer-supported bis-pyridyl ligand has also been applied in microwave-assisted asymmetric allylic alkylation [140], a key step in the enantio-selective synthesis of (R)-baclofen (Scheme 7.118), as reported by Moberg and coworkers. The ( (-enantiomer is a useful agonist of the GABAb (y-aminobutyric acid) receptor, and the racemic form is used as a muscle relaxant (antispasmodic). Under microwave heating, the enantioselectivity could be improved to 89% when using toluene as solvent (see also Scheme 6.52) [140],... 

Colofac is the proprietary preparation of mebeverine, which is an antispasmodic useful in irritable bowel syndrome. Mebeverine is a direct relaxant of the smooth muscle and, unlike hyoscine, is not an antimuscarinic. 

Mebeverine is an antispasmodic that reduces gastric and intestinal motility by direct relaxation of the intestinal smooth muscle. It can be used to relieve pain in irritable bowel syndrome and diverticular disease. Like all antispasmodics, mebeverine is contraindicated in paralytic ileus. 

Nonselective antimuscarinic drugs have been employed in the therapy of peptic ulcers (see Chapter 40) because they can reduce gastric acid secretion they also have been used as adjunctive therapy in the treatment of irritable bowel syndrome. Antimuscarinic drugs can decrease the pain associated with postprandial spasm of intestinal smooth muscle by blocking contractile responses to ACh. Some of the agents used for this disorder have only antimuscarinic activity (e.g., propantheline), while other drugs have additional properties that contribute to their antispasmodic action. Dicyclomine (Bentyl) and oxybutynin (Ditropan) at therapeutic concentrations primarily have a direct smooth muscle relaxant effect with little antimuscarinic action. 

Antispasmodic activity. Gum extract, administered to isolated guinea pig ileum at a dose of 3 mg/mL, produced a decrease of spontaneous contraction to 54 7% of control. Exposure of precontracted ileum by acetylcholine, histamine, and KCl to Ferula gum extract produced a concentration-dependent relaxation. Preincubation with in-domethacin, propanolol, atropine, and chlorpheniramine before exposure to the gum, did not produce any relaxation " . Antitumor activity. Water extract of the dried oleoresin, administered by gastric intubation to mice at a dose of 50 mg/ani-mal daily for 5 days, was active on CA-Ehrlich ascites, 53% increase in life span Water extract administered intra-peritoneally was inactive on Dalton s lymphoma, 4.8% ILS, and CA-Ehrlich ascites, 5.5%... 

Mecfianism of Action A GI antispasmodic and anticholinergic agent that directly acts as a relaxant on smooth muscle. Therapeutic Effect Reduces tone and motility of GI tract. 

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... 

It has got antispasmodic with direct smooth muscle relaxant action. It is used in morning and motion sickness. 

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. 

The aromatic oil extracted from thyme leaves contains thymol and carvacol, which have preservative, antibacterial, and antifungal properties. Thyme is a bronchial antispasmodic that relaxes muscles in the respiratory tract, an effect that makes it a good treatment for bronchitis and whooping cough. Thyme also relaxes smooth muscles in the gastrointestinal tract and the uterus, making it effective as a digestive aid and reliever of menstrual cramps. 

Tertiary amines used for their antispasmodic properties are dicyclomine hydrochloride (Ben-tyl, others), oxyphencyclimine hydrochloride (daricon), flavoxate hydrochloride (Uripas), and oxyburynin chloride (Ditropan). The latter two are indicated specifically for urological disorders. These agents appear to exert some nonspecific direct relaxant effect on smooth muscle. In therapeutic doses they decrease spasm of the gastrointestinal tract, biliary tract, ureter, and uterus characteristic atropine-like effects on the salivary glands and the eye also are seen with oxybutynin. 

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... 

Antispasmodics (see below) are given for abdominal pain, although there is little objective evidence for their efficacy from controlled clinical trials. The generation of evidence is complicated by the variable nature of IBS symptoms, the patients who suffer from them, and the high rate of placebo response in this condition. There are two main classes of antispasmodic, the antimuscarinic drugs and drugs which are direct smooth muscle relaxants. 

A trial of low dose amitryptiline (10-25 mg at night) is worthwhile in patients who do not respond to antispasmodics, and associated depression will be helped by conventional doses of this or other antidepressants. Relaxation therapy, hypnotherapy and cognitive behaviour therapy have a place in selected cases. 

Uremia Antihistamines Antiparkinsonian agents Antispasmodics Ophthalmic preparations OTC sleep/allergy medications Tricyclic antidepressants Other medications Analgesics/NS AIDs Anticonvulsants Corticosteroids (high dose) Digoxin H2 blockers Insulin Muscle relaxants Narcotics Psychotropics (anxiolytic, antidepressant, antipsychotic) Sedative/hypnotic Sulfonylurea... 

Scopolamine (hyoscine N-butylbromide) is available as an antispasmodic product (20 mg ampule for injection and 20 mg tablets) for use in humans. In addition, there is a veterinary product that contains scopolamine and dipyrone approved for use as an antispasmodic/analgesic in animals. In addition to blocking the effects of acetylcholine at the muscarinic receptor, scopolamine affects nicotinic receptors in intestinal ganglia and does not affect the CNS. In horses, scopolamine is used as an antispasmodic and to relax the rectum to facilitate abdominal palpation. In one report, 0.2 mg/kg was as effective as 0.2 mg/kg scopolamine plus 2.5 mg/kg dipyrone in relieving discomfort caused by balloon dilatation of the cecum (Roelvink et al 1991). The analgesic effect tasted for 20 min. 

SMOOTH MUSCLE RELAXANT and ANTISPASMODIC with SOme LOCAL ANAESTHETIC activity. 

ANTIBACTERIAL and ANTHELMINTIC, fenticonazole [ban. inn] (fenticonazole nitrate [usan] Lomexin ) is an (imidazole group) ANTIFUNGAL. Clinically, it can be used topically, fenticonazole nitrate fenticonazole. fentonium bromide [inn] is a quaternary amine, a MUSCARINIC CHOLINOCEPTOR ANTAGONIST, which can be used as an antispasmodic and to treat bladder irritability, fenyramidol [inn] (( )-form = phenyramidol hydrochloride [usan]) is a pyridinylaminobenzenemethanol derivative, with ANALGESIC and SKELETAL MUSCLE RELAXANT properties. 

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