Medizinische Universität Graz Austria/Österreich - Forschungsportal - Medical University of Graz
Gewählte Publikation:
SHR Neuro Krebs Kardio Lipid Stoffw Microb
Herbert, MK; Weis, R; Holzer, P.
The enantiomers of tramadol and its major metabolite inhibit peristalsis in the guinea pig small intestine via differential mechanisms.
BMC Pharmacol. 2007; 7(2): 5-5.
Doi: 10.1186/1471-2210-7-5
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- Co-Autor*innen der Med Uni Graz
- Holzer Peter
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- Abstract:
- BACKGROUND: Inhibition of intestinal peristalsis is a major side effect of opioid analgesics. Although tramadol is an opioid-like analgesic, its effect on gut motility is little known. Therefore, the effect of (+)-tramadol, (-)-tramadol and the major metabolite O-desmethyltramadol on intestinal peristalsis in vitro and their mechanisms of action were examined. Distension-induced peristalsis was recorded in fluid-perfused segments of the guinea pig small intestine. The intraluminal peristaltic pressure threshold (PPT) was used to quantify the motor effects of extraserosally administered drugs. RESULTS: Racemic tramadol, its (+)- and (-)-enantiomers and the major metabolite O-desmethyltramadol (0.1-100 microM) concentration-dependently increased PPT until peristalsis was transiently or persistently abolished. The rank order of potency was (-)-tramadol < (+)-tramadol
- Find related publications in this database (using NLM MeSH Indexing)
- Animals -
- Dose-Response Relationship, Drug -
- Female -
- Guinea Pigs -
- Intestine, Small - drug effects
- Male - drug effects
- Peristalsis - drug effects
- Stereoisomerism - drug effects
- Tramadol - analogs and derivatives