The enantiomers of tramadol and its major metabolite inhibit peristalsis in the guinea pig small intestine via differential mechanisms

Herbert, M. K.; Weis, Rebecca; Holzer, Peter

doi:10.1186/1471-2210-7-5

Cited by 16 publications

(13 citation statements)

References 27 publications

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“…Our study demonstrate that the tramadol impaired intestinal peristalsis movement in a concentration -dependent manner as deduced from an increase in the peristaltic pressure threshold and this result agreement with others study that suggest that tramadol impaired intestinal peristalsis contraction in a concentration -dependent (Herbert et al, 2007).…”

Section: Discussionsupporting

confidence: 93%

The Effect of Tramadol on the Peristaltic Movement Small Intestine in Rabbit

Jameel¹,

Taqa²,

AL-Fathee³

2011

RJS

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Tramadol is an opium analgesic drug that is used to relieve moderate to relatively severe pain. The major side effect of opium analgesic drugs is inhibit the intestinal peristalsis motility, and the effect of tramadol on gut motility is unknown quitely, therefore the effect of tramadol on intestinal peristalsis in vitro was examined in segments of the rabbit small intestine. Our study demonstrated that the low concentration of tramadol (0.1, 0.2, 0.3 , 0.4 , 0.5) ml , escort to activation peristalsis movement while increase the concentration (0.6, 0.7, 0.8, 0.9, 1.0) ml lead to decrease the contraction but when increase the concentration to 1ml lead to inhibited the peristalsis movement and complete relaxation. There for the study was concluded that the tramadol uses on rabbit small intestine decrease the peristalsis movement and this inhibition depend on concentration manner.

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Section: Discussionsupporting

confidence: 93%

The Effect of Tramadol on the Peristaltic Movement Small Intestine in Rabbit

Jameel¹,

Taqa²,

AL-Fathee³

2011

RJS

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“…The reduction of body weight induced by opioid and tramadol was attributed to the reduction of androgen synthesis that might be associated with reduction of its metabolism (Yilmaz et al, 1999) and to the major metabolite of tramadol (O-desmethyl tramadol) that affects the intestinal motility and inhibited peristalsis of small intestine more than the parent compound (Herbert et al, 2007). Moreover, presence of μ-opioid receptors in the intestinal tract that leads to inhibition of the peristaltic action (Chen et al, 2012).…”

Section: Discussionmentioning

confidence: 99%

Effects of Brown Heroin and Tramadol Dependency on Reproductive Axis in Adult Male Albino Rats

Mesallam

El-Sheikh

AbdEl-Fatah

et al. 2018

Ain Shams Journal of Forensic Medicine and Clinical Toxicology

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Objective: Drugs addiction is considered a general major problem all over the world causing massive detrimental effects for the addict, communities and governments. The study was designed to assess the dependency impact of concurrent brown heroin and Tramadol administration on reproduction in rats. Material and methods: Sixty adult male albino rats were divided into untreated control (I), vehicles groups citric acid (II), saline (III), brown heroin (IV), tramadol (V) and concurrent brown heroin and tramadol (VI) groups. The animals were treated daily for forty days by oral (saline and tramadol) and intra-peritoneal (citric acid and heroin) routes. The body weights, the reproductive hormonal assay (luteinizing hormone LH, follicle stimulating hormone FSH, free Testosterone, Estradiol E2 and prolactin PRL) and the hormones related gene expression (brain FSH-B gene, LH-B gene and testicular cytochrome 19 gene CYP-19) were evaluated. The histopathological changes of the brain and testis were demonstrated. Results: The brown heroin, tramadol and the concurrent brown heroin and tramadol administration reduced the rats' body weight, serum LH, FSH and Testosterone and increased the serum E2 and PRL levels. Moreover, both heroin and tramadol produced down regulation of brain LH-B and FSH-B with up regulation of testicular CYP-19 genes expression and induced histopathological alterations in both of the brain and testicular structures. Conclusion: The concurrent brown heroin and tramadol dependency affect the reproductive axis and impaired fertility in adult male albino rats via altering the circulating reproductive hormones and its related genes expression, moreover, affecting the histology of the brain and testis. Recommendation: Health education for the purpose of increasing public awareness regarding hazards of tramadol and heroin addiction, periodic urine screening for early detection and proper management which could be done for university students, employee in different community services….etc

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“…In this light, antimuscarinic effects may explain dry mouth, which is a common adverse effect reported in patients treated with tramadol (Scott & Perry, 2000). Tramadol has also been shown to inhibit the contractility of isolated smooth muscles like rabbit aorta (Kaya et al, 2003), guinea-pig small intestine (Herbert et al, 2007) and caprine (goat) detrusor muscle (Kumar et al, 2012). To our knowledge, the effect of tramadol on the contractility of isolated myometrium has not been studied.…”

Section: Introductionmentioning

confidence: 91%

Tramadol inhibits the contractility of isolated human myometrium

Shah

Thomas

Jose

et al. 2013

Auton Autocoid Pharmacol

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This study was conducted to determine whether the atypical opioid analgesic tramadol inhibits the contractility of isolated non-pregnant human myometrium. Ten strips of non-pregnant human myometrium stimulated with 55 mm potassium chloride (KCl) were treated with three concentrations (30, 100 and 300 μm) of tramadol to test for any inhibitory effect of tramadol. The effects of concurrent administration of the ß adrenoceptor antagonist propranolol (1 μm), the guanylyl cyclase and nitric oxide synthase inhibitor methylene blue (20 μm) and the opioid receptor antagonist naloxone (100 μm) with tramadol were also studied. Tramadol caused a concentration-dependent inhibition of KCl-induced myometrial contractility, which was statistically significant at all three concentrations of tramadol used. Propranolol significantly reversed the inhibitory effect of 100 μm tramadol on KCl-induced myometrial contractility but not that of 300 μm tramadol. Neither methylene blue nor naloxone reversed the inhibitory effect of tramadol on KCl-induced myometrial contractility. These results suggest that tramadol inhibits KCl-induced contractility of isolated human myometrium. They also suggest that tramadol relaxes the myometrium due to stimulation of ß1 adrenoceptors. However, the concentrations of tramadol required to relax the myometrium were high and likely to be attained at toxic doses, rather than therapeutic doses, of tramadol.

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The enantiomers of tramadol and its major metabolite inhibit peristalsis in the guinea pig small intestine via differential mechanisms

Cited by 16 publications

References 27 publications

The Effect of Tramadol on the Peristaltic Movement Small Intestine in Rabbit

The Effect of Tramadol on the Peristaltic Movement Small Intestine in Rabbit

Effects of Brown Heroin and Tramadol Dependency on Reproductive Axis in Adult Male Albino Rats

Tramadol inhibits the contractility of isolated human myometrium

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