Spasmolytic effect

The simplification of the local anesthetic phaimacophore of cocaine to an aryl substituted ester of ethanolamine has been described previously. Atropine (S2) is a structurally closely related natural product whose main biologic action depends on inhibition of the parasympathetic nervous system. Among its many other actions, the compound exerts useful spasmolytic effects. 

Inclusion of a second nitrogen atom in the side chain seemingly increases the spasmolytic effect of the benzhydrol derivatives. Alkylation of the benzdryl chloride (9) with the sodium... 

DHPs are potent arterial vasodilators. They act on resistance vessels and therefore reduce peripheral vascular resistance, lower arterial blood pressure, and antagonize vasospasms in coronary or peripheral arteries. By reducing afterload, DHPs also reduce cardiac oxygen demand. Together with their vascular spasmolytic effect, this explains most of the beneficial actions of DHPs in angina pectoris. Most DHPs are only licensed for the therapy of hypertension, some of them also for the treatment of angina pectoris and vasospastic (Prinzmetal) angina. 

The answer is a. (Hardman, pp 228-229.) Phentolamine is a non-selective a-adrenergic receptor blocker (i.e., it has affinity for both - and ct2-adrenergic receptor sites). It also has a prominent direct relaxant (musculotropic spasmolytic) effect on arterioles, which results in vasodilation and reflex tachycardia. In addition, phentolamine can block the effects of serotonin and will increase hydrochloric acid and pepsin secretion from the stomach. Phentolamine is used for the short-term control of hypertension in patients with pheochromocytoma (i.e., a type of secondary hypertension) because of the high incidence of tachycardia associated with the compound, it is not used chronically for the treatment of essential hypertension... 

Three phenylethylamines with complex sympatholytic or spasmolytic effects 31... 

Hernandez-Romero Y Rojas J-I, Castillo R, Rojas A, MataR, Spasmolytic effects, mode of action, and structure-activity relationships of stilbenoids from Nidema boothii, J Nat Prod 67 160—167, 2004. 

Bolus The onset of action is generally 0.5 to 1 hour after an intrathecal bolus dose. Peak spasmolytic effect is seen at about 4 hours after dosing and effects may last 4 to 8 hours. Onset, peak response, and duration of action may vary with individual patients depending on the dose and severity of symptoms. 

Coriander Coriandrum sativum) Uses t Appetite, treat D, dyspep-sia, flatulence Action Stimulates gastric secretions, spasmolytic effects Available forms Tine 10-30 gtts PO OD Contra w/ PRG or lactation Notes/SE N/V, fatty liver tumors, allergic skin Rxns Interactions T Effects OF oral hypoglycemics EMS T Risk of photosensitivity Rxns may cause hypoglycemia Cranberry [Vaeeinium macreearpon) Uses Prevention UTI urinary deodorizer in urinary incontinence Actions Interferes w/ bacterial adherence to epithelial cells of the bladder Available forms Caps 300-500 mg PO bid-qid unsweetened juice 8-16 oz daily tine 3-5 mL or tincture 1/2-1 tsp up to 3X/d, tea 2-3 tsps of dried flowers/cup creams apply topically 2-3X/d PO SE D, irritation, nephrolithiasis if T urinary Ca oxalate Interactions T Effects OF warfarin ... 

The tetraethyl homologue of papaverine (Perparin , Perperine , Ethaverine , Diquinol ) is more active than papaverine and is used for its spasmolytic effects on the uterus, ileum, and circulatory system. 

Anileridine, ethyl l-(4-amino phenethyl)-4 phenylisonipecotate is available in the form of its dihydrochloride for oral administration and as the phosphate for injection (Leritine ). Its analgesic potency is intermediate between that of meperidine and morphine. Similar to meperidine, it exerts mild antihistaminic and spasmolytic effects, but it is devoid of the constipating effect of opiates. Sedative and direct hypnotic effects are similar to those of meperidine but less than those of morphine. 

Obaberine Weak spasmolytic effect (rabbit intestine) antiinflammatory (rat) not adrenolytic 370... 

Papaverine dehydroepiandrosterone-3-monophosphate (151) had a much more rapid coronary vasodilator action on the isolated cat heart than papaverine the effect of papaverine was, however, of longer duration. Both compounds inhibited histamine bronchospasms. The spasmolytic effect of papaverine dehydroepiandrosterone-3-mono-phosphate on histamine-induced contractions of the small intestine of guinea pigs was twice as strong as that of papaverine but less toxic than papaverine. 

Mercier el al. (330) administered i.v. infusions of sodium salicylate to dogs and determined the lethal dose to be 1 g/kg. Simultaneous administration of papaverine resulted in a slight increase in the toxicity. Lettr6 et al. (331) studied the synergism of mitotic poisons and found that papaverine intensified the mitotic effect of colchicine on the growth of fibroblasts in vitro. The spasmolytic effect of khelline was augmented by small doses of papaverine (332). Therapeutic doses of khelline did not produce a hypotensive effect upon dogs, but in combination with barbiturates and papaverine a hypotensive effect was observed. 

David and Gyarmati (350) carried out a comparison between the spasmolytic effect of papaverine, perparine, dihydroisoperparine, and tetrahydroperparine upon contractions in rats induced by oxytocin. The most effective was dihydroisoperparine. The significance of the phenylisopropylamine group was studied by Leuschner et al. (351). They found that 1-benzylisoquinoline, papaverine, and A-allyl-... 

Unstable angina although the therapy of choice for unstable angina rests on the use of beta-blockers and aspirin, calcium antagonists may add further value due to their spasmolytic effects. 

In conclusion, all dihydropyridines show a potent calcium channel antagonist activity, which is in turn translated into direct arteriolar spasmolytic effect that results in a beneficial vasodilatory activity. This is useful in some cardiovascular diseases, such as hypertension and angina, in which the peripheral resistances are raised due to increased calcium entry into the cells. Many analogues of nifedipine have been synthesized and introduced into the market, and each of these presents some common features and some peculiar differences. In particular ... 

Dipyrone (metamizole) is a pyrazolone derivative. It produces strong analgesia, even in pain of colic, and has an additional spasmolytic effect. The antipyretic effect is marked. The usual dosage is about 500 mg Luellmann, Color Atlas of Pharmacology All rights reserved. Usage subject to terms... 

Carisoprodol is a precursor of meprobamate, an oral anxiolytic with similarities to benzodiazepines. The spasmolytic effect of carisoprodol is thought to be due to interruption of neuronal communication within the reti-cnlar formation and spinal cord. Major adverse effects are sedation and drowsiness. 

Vincamine is an alkaloid extracted from the plant Vinca minor. Ethyl apovincaminate is a related synthetic ethyl ester of vincaminic acid. These drugs have spasmolytic effects similar to those of reserpine, but also have metabolic effects, including, in high doses, inhibition of phosphodiesterase. Although increased cerebral blood flow has been reported after the intravenous administration of vincamine, there have been no reliable studies of blood flow after oral medication. Improvement in scores on some psychometric tests have been obtained in some patients with cerebrovascular disease, but no clear-cut practical benefit has been demonstrated. 

Roberts M C, Clarke L L, Johnson C M 1989 Castor-oil induced diarrhoea in ponies a model for acute colitis. Equine Veterinary Journal Supplement 7 60-67 Roelvink M E, Goossens L, Kalsbeek H C et al 1991 Analgesic and spasmolytic effects of dipyrone, hyoscine-/V-butylbromide and a combination of the two in ponies. Veterinary Record 129 378-380 Roger T, Bardon T, Ruckebusch Y 1985 Colonic motor responses in the pony relevance of colonic stimulation by opiate antagonists. American Journal of Veterinary Research 46 31-35... 

Dicyclomine hydrochloride has one eighth of the neii-rotropic activity of atropine and approximately twice the musculotropic activity of papaverine. This preparation. liN introduced in 1950. has minimized the adverse effects asso. dated with the atropine-type compounds. It is used for its spasmolytic effect on variou.s smtxrth muscle spa.snts. particularly those associated with the GI tract. It is also useful in dysmenorrhea. pylorospa.sm. and biliary dysfunction. 

Matricaria chamomilla L. -camomila Nervous disturbances Flower (infusion) Afro-Brazilians (Northeast Brazil) [45,46] Flavonoids [104,105] essential oil [106] acylglycerols, linoleic and linolenic acids [107] coumarins [108,109] sesquiterpene lactone [110] inhibits both development of morphine dependence and expression of abstinence syndrome [255,256] anxiolytic effect [257] sedative as well as spasmolytic effects [258]... 

The enantiomers of trimetoquinol have been synthesized and their activities in /8-adrenoceptor systems compared. A number of new 1- and 3-benzylisoquinoline analogues of papaverine were found to have up to a third of the muscle-relaxing activity of papaverine. Also compared with papaverine, N butylpapaverinium bromide had the same spasmolytic effect and an N-benzylpapaverinium salt had a more prolonged antiarrhythmic effect. Other new... 

In essence, this identifies the rhamnosylated 4-hydroxy-benzyl isothiocyanates, carbamates and thiocarbamates as the pharmacologically active principles of the extracts. The effects of all of these compounds have been found to be similar, reversible and dose-dependent. Nitriles do not show any hypotensive effect however. Investigations on organs of several animals indicate spasmolytic properties of thiocarbamates in vitro along with the hypotensive effects (29). Nevertheless, with these studies no specific mechanism can be supposed for the hypotensive and spasmolytic effects of these thio-carbamates (57). 

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