Opiate-induced constipation related to activation of small intestine opioid μ2-receptors

Chen, Wency; Chung, Hsien-Hui

doi:10.3748/wjg.v18.i12.1391

Cited by 34 publications

(24 citation statements)

References 30 publications

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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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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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“…Loperamide is a popularly prescribed to reduce the bowel motility that causes diarrhea. It induces intestinal relaxation by activating opioid μ2 receptors via the cAMP-PKA pathway, which in turn prevents the exocytosis of acetylcholine from the parasympathetic nerves of the ileum, as demonstrated in mice (Chen et al 2012). In the large intestine, Lop suppresses the release of 5-hydroxytryptamine (5-HT), an enhancer of colonic motility, from the colonic mucosa, in a process triggered by the NK3 receptor, probably by activating κ-and δ-opioid receptors, as shown in guinea pigs (Kojima et al 2005).…”

Section: Groupmentioning

confidence: 99%

Enhanced intestinal 2-deoxy-2-[¹⁸F]fluoro-D-glucose uptake under metformin is not fully suppressed by loperamide

Nobashi

Saga

Nakamoto

et al. 2018

Endocrine Regulations

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Objective. This study investigated whether the metformin (Met)-induced enhanced intestinal uptake of 2-deoxy-2-[18F]fluoro-D-glucose (18F-FDG) is reduced by loperamide, a long-acting anti-diarrheal agent. Methods. Mean 18F-FDG uptake in the mouse small intestine and colon with Met exposure was compared with that in control mice. In the Met group, high-dose (1.0 mg/kg body weight) and low-dose (0.1 mg/kg body weight) loperamide were introduced, and 18F-FDG uptake in the small intestine and colon was compared with that of control mice administered high-dose loperamide. The percent injected dose of 18F-FDG per gram of tissue (%ID/g) in the extracted tissues was then determined. Results. 18F-FDG uptake increased significantly in the small intestine (0.64±0.06 vs. 1.01±0.15, p=0.040) and, especially, the colon (0.46±0.13 vs. 2.16±0.51, p<0.001) after Met exposure. Neither high-dose nor low-dose loperamide significantly reduced 18F-FDG uptake in the small intestine (0.82±0.31 vs. 0.84±0.22, p=0.93 and 0.78±0.25 vs. 0.70±0.15, p=0.13, respectively) or colon (2.13±0.41 vs. 1.67±0.55, p=0.063 and 1.77±0.39 vs. 1.80±0.25, p=0.56, respectively). The colonic %ID/g was significantly higher in Met groups irrespective of loperamide introduction than in control group, whereas the significant difference in the small intestine was observed only between Met and control groups. Conclusion. Metformin increased 18F-FDG uptake in intestines especially in colon. Loperamide administration partially, but not sufficiently, suppresses the Met-induced increased colonic uptake of 18F-FDG.

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“…This lack of tolerance differs from other adverse effects of opioid analgesics and could possibly be related to the actions associated with μ-opioid receptor subtypes (eg, tolerance develops for activities that are μ-1 dependent versus other subtypes). [26][27][28] Given the lack of tolerance development to OIC, it is important that OIC be anticipated and be treated as appropriate in patients receiving opioid analgesics. 4 The strength of this placebo crossover analysis is that the design allowed patients to serve as their own controls when comparing the efficacy and safety of methylnaltrexone versus placebo.…”

Section: Discussionmentioning

confidence: 99%

(451) Efficacy and safety of methylnaltrexone for opioid-induced constipation in patients with chronic noncancer pain: a placebo crossover analysis

Viscusi¹,

Barrett²,

Paterson³

et al. 2014

The Journal of Pain

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Opiate-induced constipation related to activation of small intestine opioid μ2-receptors

Abstract: Loperamide induces intestinal relaxation by activation of opioid μ-2 receptors via the cAMP-PKA pathway to open K(ATP) channels, relates to OIC.

Cited by 34 publications

References 30 publications

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

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

Enhanced intestinal 2-deoxy-2-[¹⁸F]fluoro-D-glucose uptake under metformin is not fully suppressed by loperamide

(451) Efficacy and safety of methylnaltrexone for opioid-induced constipation in patients with chronic noncancer pain: a placebo crossover analysis

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Opiate-induced constipation related to activation of small intestine opioid μ2-receptors

Abstract: Loperamide induces intestinal relaxation by activation of opioid μ-2 receptors via the cAMP-PKA pathway to open K(ATP) channels, relates to OIC.

Cited by 34 publications

References 30 publications

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

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

Enhanced intestinal 2-deoxy-2-[18F]fluoro-D-glucose uptake under metformin is not fully suppressed by loperamide

(451) Efficacy and safety of methylnaltrexone for opioid-induced constipation in patients with chronic noncancer pain: a placebo crossover analysis

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Enhanced intestinal 2-deoxy-2-[¹⁸F]fluoro-D-glucose uptake under metformin is not fully suppressed by loperamide