Anti-spasmodics

Reviews of recent developments in synthetic anti-spasmodics have been published by Raymond and by Blicke, and on the pharmacology of antihistamine compounds by Loew. Mention may also be made of the useful description by Henderson and Sweeten of the effeet of atropine on the gastro-intestinal canal and its glands. 

Some starting materials can be unrecognisable even in quite small target molecules. The anti-spasmodic piperldolate (53) is clearly made from (54) which could come from cyclisation of (55), Reconnection of (55) shows that it can be made from furfuraldehyde (56). 

C13 5NO2 Amino ester Anti-spasmodic (20) T296... 

C 21N 2 sN02 Amino ester Anti-spasmodic (53) W486... 

The opiate alkaloid, papaverine, from Papaver somniferum is an anti-spasmodic, vasodilator, and smooth muscle relaxant. Its total synthesis has been studied since Pictet and Gams early work in 1909 and has since been followed up by various industrial syntheses up till the early 1950s using important industrial commodities as vanillin, acetovanillone, veratraldehyde (methylvanillin), and homoveratric acid as starting materials (see Figure 4.50). Table 4.23 summarizes the results of the five synthetic plans for this natural product. All are convergent... 

Omission of the hydroxyl group and one of the cyclic hydrocarbons from the acid moiety is apparently not inconsistent with biological activity. Thus, the ester from 2-phenylbutyryl chloride and diethyl-aminoethoxyethanol, butamirate (71), shows anti-spasmodic activity. In analogous fashion, reaction of the acid chloride from 72 with N-methyl-4-... 

Fixed dose combination of laxatives and/or anti-spasmodic drugs in enzyme preparations. 

Fixed dose combination of dextropropoxyphene with any other drug other than anti-spasmodics and/ or non-steroidal antiinflammatory drugs (NSAIDs). 

The depressant effect of EOs on smooth muscle in the small intestine is consistent with the therapeutic uses of these aromatic plants as gastrointestinal anti-spasmodics and carminatives [224]. In vitro studies showed that EOs produced the inhibition of gastric motility, and are thus the basis of the treatment of some gastrointestinal disorders [225, 226]. 

Nicorandil is a potent vasodilator with anti-spasmodic properties. Its cardiovascular effects are mainly characterised by dilatation of large coronary arteries in combination with reduction of preload and afterload. It has a dual mode of action, activating ATP-dependent K+ channels and a nitrate-like effect. 

Mendelson s syndrome Cytoprotectants Mucosal protective drugs Prokinetic and anti-spasmodic drugs Laxatives Anti-diarrhoeals Nausea and vomiting Pharmacology of anti-emetic drugs Other substances Non-pharmalogical therapy INTRODUCTION... 

Action Uterine tonic, nervine, anti-spasmodic. 

Action Carminative, tonic, diaphoretic, anti-spasmodic. 

Mistletoe leaves are given in hysteria, epilepsy, chorea and other diseases of the nervous system. As an anti-spasmodic and tonic it is used in cardiac dropsy. 

Phrenic, anaesthetic, anti-spasmodic and hypnotic. Unlike opium, it does not constipate the bowels, lessen the appetite, create nausea, produce dry. ness of the tongue, check pulmonary secretions or produce headache. Used with success in hysteria, chorea, gout, neuralgia, acute and sub-acute rheumatism, tetanus, hydrophobia and the like. 

This molecule was actually prepared at the same time as meperidine as an anti-spasmodic agent. Methadone is marketed as a racemic mixture, and again the... 

Ct9nACh-R (mixed n-m properties R) ACh-competitive blocker (mACh-R antagonist) [anticholinergic, anti-spasmodic, antidote to organophosphorous insecticide poisoning, mydriatic, toxic, vasodilatorv]... 

Dl-R ligand (> 10), D2-R ligand (>10), Dl-R ligand (>10) (D-TR, 5HT-TR, O-R) [anti-addictive, anticonvulsant] D-R antagonist (Glu-R antagonist) (Mayan [anti-spasmodic, antiviral, neuroleptic] blue lotus emblem of Nefertem, God of Perfiimes in wine gives tranquil euphoria ... 

Datura stramonium. Jamestown weed. Narcotic anti-spasmodic and anodyne tinct. and infusion as local application. Fol. 4[lb.] 0[oz.]... 

Jamestown weed Datura stramonium anti-spasmodic, anodyne, narcotic likely ... 

Antimuscarinic syndromes consist of tachycardia, dilated pupils, dry, flushed skin, urinary retention, decreased bowel sounds, mild elevation of body temperature, confusion, cardiac arrhythmias and seizures. They are commonly caused by antipsych-otics, tricyclic antidepressants, antihistamines, anti-spasmodics and many plants (see p. 160). 

Many alkaloids have pronounced biological properties, and many of the pharmaceutical agents used today are derived from naturally occurring amines. Morphine and related alkaloids from the opium poppy, for instance, are used for pain relief atropine from the flowering plant Atropa belladonna, commonly called the deadly nightshade, is used as an anti-spasmodic agent for the treatment of colitis and ephedrine from the Chinese p smt Ephedra sinica is used as a bronchodilator and decongestant. 

Atropine is used widely as an antispusmodic because nf its marked dcprcs.sant effect un parasympathctically innervated smooth mu.scle. It appetmt to block all muscarinic receptor subtypes. Atropine i.s. however, the standard by which other similar drugs are measured. Also, atropine has a blocking action on the transmi.ssion of the nerve impulse, rather than a depressant effect directly nn the mu.sculature. This action is termed neuroirnitic, in contrast with the action of an anti-spasmodic such us papaverine, which appears to act by depression uf tiic muscle cells and is termed musculolropic. 

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