Abstract
1 Subcutaneous prostaglandin E2 (2.5 mg/kg) produces profuse diarrhoea in fed rats. 2 Pretreatment of rats with subcutaneous loperamide (1.0 mg/kg) completely prevents prostaglandin-induced diarrhoea. If naloxone is administered prior to loperamide injections the activity of the antidiarrhoeal compound is completely destroyed. 3 These data provide strong evidence that the antidiarrhoeal activity of loperamide is mediated via the opiate receptor.
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Selected References
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- Bianchi C., Goi A. On the antidiarrhoeal and analgesic properties of diphenoxylate, difenoxine and loperamide in mice and rats. Arzneimittelforschung. 1977;27(5):1040–1043. [PubMed] [Google Scholar]
- Clay G. A., Mackerer C. R., Lin T. K. Interaction of loperamide with [3H]naloxone binding sites in guinea pig brain and myenteric plexus. Mol Pharmacol. 1977 May;13(3):533–540. [PubMed] [Google Scholar]
- Colpaert F. C., Niemegeers C. J., Lal H., Janssen P. A. Investigations on drug produced and subjectively experienced discriminative stimuli. 2. Loperamide, an antidiarrheal devoid of narcotic cue producing actions. Life Sci. 1975 Mar 1;16(5):717–727. doi: 10.1016/0024-3205(75)90348-3. [DOI] [PubMed] [Google Scholar]
- Dajani E. Z., Bianchi R. G., East P. F., Bloss J. L., Adelstein G. W., Yen C. H. The pharmacology of SC-27166: a novel antidiarrheal agent. J Pharmacol Exp Ther. 1977 Dec;203(3):512–526. [PubMed] [Google Scholar]
- Karim S. M., Adaikan P. G. The effect of loperamide on prostaglandin induced diarrhoea in rat and man. Prostaglandins. 1977 Feb;13(2):321–331. doi: 10.1016/0090-6980(77)90011-9. [DOI] [PubMed] [Google Scholar]
- Lange A. P., Secher N. J., Amery W. Prostaglandin-induced diarrhoea treated with loperamide or diphenoxylate. A double-blind study. Acta Med Scand. 1977;202(6):449–454. doi: 10.1111/j.0954-6820.1977.tb16863.x. [DOI] [PubMed] [Google Scholar]
- Mackerer C. R., Clay G. A., Dajani E. Z. Loperamide binding to opiate receptor sites of brain and myenteric plexus. J Pharmacol Exp Ther. 1976 Oct;199(1):131–140. [PubMed] [Google Scholar]
- Niemegeers C. J., Lenaerts F. M., Janssen P. A. Loperamide (R 18 553), a novel type of antidiarrheal agent. Part 1: in vivo oral pharmacology and acute toxicity. Comparison with morphine, codeine, diphenoxylate and difenoxine. Arzneimittelforschung. 1974 Oct;24(10):1633–1636. [PubMed] [Google Scholar]
- Stahl K. D., van Bever W., Janssen P., Simon E. J. Receptor affinity and pharmacological potency of a series of narcotic analgesic, anti-diarrheal and neuroleptic drugs. Eur J Pharmacol. 1977 Dec 1;46(3):199–205. doi: 10.1016/0014-2999(77)90334-x. [DOI] [PubMed] [Google Scholar]
- Van Nueten J. M., Janssen P. A., Fontaine J. Loperamide (R 18 553), a novel type of antidiarrheal agent. Part 3: in vitro studies on the peristaltic reflex and other experiments on isolated tissues. Arzneimittelforschung. 1974 Oct;24(10):1641–1645. [PubMed] [Google Scholar]