エトミドリンの消化管運動に対する作用とその特殊性

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タイトル別名
  • CHARACTERISTIC EFFECT OF ETOMIDOLINE ON CONTRACTILE ACTIVITY IN THE GASTROINTESTINAL TRACT IN CONSCIOUS DOGS

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Atropine and scopolamine have been widely used as an anticholinergic agent in clinic, however, the lack of organ selectivity of these natural belladonna alkaloids has led to intensive efforts to find antimuscarinic drugs with more selective effects. The major development made in this field was to have a quaternary ammonium structure and a typical compound now clinically used is scopolamine butylbromide. Another undesireable effect of these quaternary ammonium compounds is a delay in transport-time of gastrointestinal contents, which could not be overcome.<br>In the present study we investigated the effect of etomidoline, a newly developed antispasmodic drug with an isoindoline ring and a tertiary amine, on gastrointestinal motor activity in conscious dogs. In our system, dogs were chronically implanted with force transducers in the gastric antrum and the upper jejunum and gastrointestinal contractile activity was continuously recorded for long period of time. Etomidoline, dissolved in 0.9% saline, was continuously infused intravenously in a dose of 0.3mg/kg-30min. It was found that gastric and jejunal contractile activity was strongly inhibited for 96.3±0.05min and pentagastin (0.1μg/kg-hr)-stimulated gastric motor activity was also suppressed for 78.5±4.44min during the digestive state. Oral administration of this drug in a dose of 0.6 and 0.4mg/kg of body weight for 30min before each meal resulted in shortening of time for digestion and absorption for 0.9 and 2.2hr, respectively, though contractile force in the gastric antrum was significantly lowered when compared with the control. Its mechanism is not clearly known at present, however, it is noteworthy that time required for digestion and absorption of food was not prolonged by this antimuscarinic agent.

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