Document Detail

Role of opioid antagonists in the treatment of women with glucoregulation abnormalities.
MedLine Citation:
PMID:  16533167     Owner:  NLM     Status:  MEDLINE    
Beta-endorphin were detected in the endocrine pancreas and seem able to influence insulin and glucagon release. Hence, endogenous opioids could have a role in glucoregulation and in the pathogenesis of obesity beyond the previously detected effects on appetite. Metabolic abnormalities, such as hyperinsulinemia, insulin-resistance and obesity, are common features of polycystic ovary syndrome (PCOS), and seem to have a pathogenetic role in this disorder. A link between opioids and PCOS-related hyperinsulinism is suggested by the finding of altered central opioid tone and elevated beta-endorphins levels, directly correlated with body weight, in these patients. Furthermore, naloxone and naltrexone significantly reduce the insulin response to glucose load only in hyperinsulinemic PCOS patients. This effect is obtained chiefly through an improvement of insulin clearance. Naltrexone is also able to ameliorate the abnormal gonadotrophins secretion and to improve the ovarian responsiveness in obese PCOS women undergoing ovulation induction with exogenous GnRH. Such effects are believed to be obtained through an amelioration of hyperinsulinemia. Gonadal steroids modulate the opioid system both centrally and in peripheral districts. Nevertheless, the decline of ovarian function does not abolish the opioidergic control of glucoregulation. Post-menopausal period is characterised by a high prevalence of hyperinsulinemia and insulin-resistance. In particular, an association between hyperinsulinemia and increased opioid activity was found in postmenopausal women showing a central body fat distribution. Both naloxone and naltrexone ameliorate the metabolic imbalance also when it appears in the climacteric period, and mainly by increasing insulin clearance. The benefits of naltrexone may represent in the future a useful tool for the treatment of women with hyperinsulinism in the clinical practice.
M Guido; D Romualdi; A Lanzone
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Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Current pharmaceutical design     Volume:  12     ISSN:  1381-6128     ISO Abbreviation:  Curr. Pharm. Des.     Publication Date:  2006  
Date Detail:
Created Date:  2006-03-14     Completed Date:  2007-03-29     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  9602487     Medline TA:  Curr Pharm Des     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  1001-12     Citation Subset:  IM    
Department of Obstetrics and Gynaecology, Università Cattolica del Sacro Cuore, Roma, Italy.
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MeSH Terms
Clinical Trials as Topic
Endorphins / antagonists & inhibitors*,  metabolism
Hyperinsulinism / drug therapy*,  metabolism
Insulin Resistance*
Menopause / metabolism
Naloxone / therapeutic use
Naltrexone / therapeutic use*
Narcotic Antagonists / therapeutic use*
Obesity / drug therapy,  metabolism
Polycystic Ovary Syndrome / drug therapy*,  metabolism
Reg. No./Substance:
0/Endorphins; 0/Narcotic Antagonists; 16590-41-3/Naltrexone; 465-65-6/Naloxone

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