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[Pharmacological effects of the combination of a spasmolytic (otilonium) with a benzodiazepine (diazepam)].

The pharmacological effects of an association represented by a myolitic agent (otilonium bromide) and a benzodiazepine (diazepam) were investigated on different in vitro preparations and on one in vivo test. In the isolated preparations both drugs administered alone showed a remarkable inhibitory effect on the motility of different areas of the digestive system both spontaneous and evoked by different stimulatory agents. Association of the two compounds gave rise to additive effects or actually to a potentiating effect according to the different tissues and animal species. Negative interference was never observed. The same was true also in the in vivo preparation ("in situ" rat pylorus). The significance and the importance of these observations are discussed also in the light of the relevant clinical implications.

Acetylcholine↗

[Spasmolytic and anti-inflammatory activity of 8-hydroxyquinolines].

It has been shown that quinozole (aqueous solution), enteroseptol and nitroxoline (suspension with Tween-80) in a concentration of 0.2 X 10(-6)-1.10(-5) decrease the tone of the rat and guinea-pig ileum and diminish their peristalsis. When administered in the same concentrations quinozole removes or prevents the spasmogenic effects of barium chloride (1 X 10(-5)-4.10(-5), of histamine (2 X 10(-5) and -6) but not of acetylcholine (1 X 10(-6)). When administered orally in a dose 50 mg/kg to rats enteroseptol and nitroxoline inhibit the serotonin-, agar- and carrageenin-induced edemas of the rat paws without changing the response to subplantar injection of histamine. The data obtained should be taken into consideration during the use of 8-hydroxyquinolines as antimicrobial substances.

Animals↗

[3-Benzyl-1,2-benzoisothiazoles: spasmolytic properties of the aminoalkyl derivatives].

The synthesis and chemical and pharmacological properties of 3-benzyl-1,2-benzisothiazoleaminoalkyl derivatives are reported. These compounds were studied because 4-dimethyl-2-phenyl-2-(1,2-benzisotiazol-3-yl)-butyramide and N,N-dimethyl-3-phenyl-3-(1,2-benzisothiazol-3-yl)propylamine were recently found to have antispasmodic properties. Most of the compounds studied aspecifically inhibited the contracturant effects of acetylcholine, histamine and BaCl2. Three of them showed mixed antagonism (competitive and non-competitive) versus acetylcholine and histamine, showing both antimuscarinic and antihistaminic properties. However the antimuscarinic action prevailed over the others, as shown by pA2 and pD'2 calculated values. On the basis of the results obtained, the structure-activity relationships is discussed.

Acetylcholine↗

Lack of effect of a new spasmolytic agent, rociverine, on intraocular pressure, pupil size and iridocorneal angle in patients with angle-closure glaucoma.

Twenty patients with angle-closure glaucoma (38 glaucomatous eyes - 17 surgically operated, 21 non-operated) were treated with rociverine (60 mg orally per day for 7 days), a new direct myolitic and mildly anticholinergic antispasmodic drug. Intraocular pressure, pupil size, iridocorneal angle, blood pressure and heart rate were checked before and during treatment. No clinically significant variations were observed in the parameters tested. It is suggested, therefore, that rociverine may be administered, if necessary, even to patients with angle-closure glaucoma.

Adult↗