Use of Somatostatin Analogues in Obesity
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- 作者：Dr Themistoklis Tzotzas (1)
Kostas Papazisis (2)
Petros Perros (3)
Gerasimos E. Krassas (1) - 刊名：Drugs
- 出版年：2008
- 出版时间：October 2008
- 年：2008
- 卷：68
- 期：14
- 页码：1963-1973
- 全文大小：132KB
- 参考文献：1. Popkin BM, Doak CM. The obesity epidemic is a worldwide phenomenon. Nutr Rev 1998 Apr; 56 (4 Pt 1): 106-4 CrossRef
2. Tzotzas T, Krassas GE. Prevalence and trends of obesity in children and adults of South Europe. Pediatr Endocrinol Rev 2004 Aug; 1 Suppl. 3: 448-4
3. Atkinson RL. Management of obesity: pharmacotherapy. In: Kopelman PG, Caterson LD, Dietz WH, editors. Clinical obesity in adults and children. Maiden (MA): Blackwell, 2005: 380-3 CrossRef
4. Mancini MC, Halpern A. Investigational therapies in the treatment of obesity. Expert Opin Investig Drugs 2006 Aug; 15(8): 897-15 CrossRef
5. Brazeau P, Vale W, Burgus R, et al. Hypothalamic polypeptide that inhibits the secretion of immunoreactive pituitary growth hormone. Science 1973 Jan; 179(68): 77- CrossRef
6. Patel YC. Molecular pharmacology of somatostatin receptosubtypes. J Endocrinol Invest 1997 Jun; 20(6): 348-7
7. Strowski MZ, Parmar RM, Blake AD, et al. Somatostatin inhibits insulin and glucagon secretion via two receptors subtypes: an in vitro study of pancreatic islets from somatostatin receptor 2 knockout mice. Endocrinology 2000 Jan; 141(1): 111- CrossRef
8. Reisine T, Bell GI. Molecular biology of somatostatin receptors. Endocr Rev 1995 Aug; 16(4): 427-2
9. Lewis I, Bauer W, Albert R, et al. A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. J Med Chem 2003 Jun; 46(12): 2334-4 CrossRef
10. Stewart PM, James RA. The future of somatostatin analogue therapy. Baillieres Best Pract Res Clin Endocrinol Metab 1999 Oct; 13(3): 409-8 CrossRef
11. Krassas GE, Tzotzas T, Papazisis K, et al. The efficacy of somatostatin analogues in the treatment of diabetic retinopathy and thyroid eye disease. Clin Ophthalmol 2007; 1(3): 209-5
12. Lamberts SW, Van der Lely AJ, De Herder WW, et al. Octreotide. N Engl J Med 1996 Jan; 334(4): 246-4 CrossRef
13. Pliquett RU, Führer D, Falk S, et al. The effects of insulin on the central nervous system: focus on appetite regulation. Horm Metab Res 2006 Jul; 38(7): 442- CrossRef
14. Niswender KD, Schwartz MW. Insulin and leptin revisited: adiposity signals with overlapping physiological and intracellular signaling capabilities. Front Neuroendocrinol 2003 Jan; 24(1): 1-0 CrossRef
15. Campfield LA, Smith FJ, Mackie G, et al. Insulin normalization as an approach to the pharmacological treatment of obesity. Obes Res 1995 Nov; 3 Suppl. 4: S591-03
16. Strowski MZ, Kohler M, Chen HY, et al. Somatostatin receptor subtype 5 regulates insulin secretion and glucose homeostasis. Mol Endocrinol 2003 Jan; 17(1): 93-06 CrossRef
17. Hansen JB, Arkhammar PO, Bodvarsdottir TB, et al. Inhibition of insulin secretion as a new drug target in the treatment of metabolic disorders. Curr Med Chem 2004 Jun; 11(12): 1595-15 CrossRef
18. Lustig RH, Hinds PS, Ringwald-Smith K, et al. Octreotide therapy of pediatric hypothalamic obesity: a double-blind, placebo-controlled trial. J Clin Endocrinol Metab 2003 Jun; 88(6): 2586-2 CrossRef
19. Lustig RH, Greenway F, Velasquez-Mieyer P, et al. A multicenter, randomized, double-blind, placebo-controlled, dose-finding trial of a long-acting formulation of octreotide in promoting weight loss in obese adults with insulin hypersecretion. Int J Obes (Lond) 2006 Feb; 30(2): 331-1 CrossRef
20. Boehm BO, Lustig RH. Use of somatostatin receptor ligands in obesity and diabetic complications. Best Pract Res Clin Gastroenterol 2002 Jun; 16(3): 493-09 CrossRef
21. Mlinar B, Marc J, Janez A, et al. Molecular mechanisms of insulin resistance and associated diseases. Clin Chim Acta 2007 Jan; 375(1-): 20-5 CrossRef
22. Rizza RA, Mandarino LJ, Genest J, et al. Production of insulin resistance by hyperinsulinaemia in man. Diabetologia 1985 Feb; 28(2): 70-
23. Sigal RJ, El-Hashimy M, Martin BC, et al. Acute postchallenge hyperinsulinemia predicts weight gain: a prospective study. Diabetes 1997 Jun; 46(6): 1025- CrossRef
24. Le Stunff C, Bougneres P. Early changes in postprandial insulin secretion, not in insulin sensitivity, characterize juvenile obesity. Diabetes 1994 May; 43(5): 696-02 CrossRef
25. Howard BV, Klimes I, Vasquez B, et al. The antilipolytic action of insulin in obese subjects with resistance to its glucoregulatory action. J Clin Endocrinol Metab 1984 Mar; 58(3): 544- CrossRef
26. Schade DS, Eaton RP. Dose response to insulin in man: differential effects on glucose and ketone body regulation. J Clin Endocrinol Metab 1977 Jun; 44(6): 1038-3 CrossRef
27. Frayn KN, Karpe F, Fielding BA, et al. Integrative physiology of human adipose tissue. Int J Obes Relat Metab Disord 2003 Aug; 27(8): 875-8 CrossRef
28. Badman MK, Flier JS. The gut and energy balance: visceral allies in the obesity wars. Science 2005 Mar; 307(5717): 1909-4 CrossRef
29. Pinkney J, Wilding J, Williams G, et al. Hypothalamic obesity in humans: what do we know and what can be done? Obes Rev 2002 Feb; 3(1): 27-4 CrossRef
30. Inoue S, Bray GA. An autonomic hypothesis for hypothalamic obesity. Life Sci 1979 Aug; 25(7): 561- CrossRef
31. Bray GA, York DA. The MONA LISA hypothesis in the time of leptin. Recent Prog Horm Res 1998; 53: 95-17
32. King BM, Frohman LA. The role of vagally-medicated hyperinsulinemia in hypothalamic obesity. Neurosci Biobehav Rev 1982; 6(2): 205-4 CrossRef
33. Gurrath M. Peptide-binding G protein-coupled receptors: new opportunities for drug design. Curr Med Chem 2001 Nov; 8(13): 1605-8 CrossRef
34. Hsu WH, Xiang HD, Rajan AS, et al. Somatostatin inhibits insulin secretion by a G-protein-mediated decrease in Ca2+ entry through voltage-dependent Ca2+ channels in the beta cell. J Biol Chem 1991 Jan; 266(2): 837-3
35. Bertoli A, Magnaterra R, Borboni P, et al. Dose-dependent effect of octreotide on insulin secretion after OGTT in obesity. Horm Res 1998; 49(1): 17-1 CrossRef
36. Giustina A, Bussi AR, Pizzocolo G, et al. Acute effects of octreotide, a long-acting somatostatin analogue, on the insulinemic and glycemie responses to a mixed meal in patients with essential obesity: a dose-response study. Diabetes Nutr Metab 1994; 7: 735-1
37. Vance ML, Harris AG. Long-term treatment of 189 acromegalic patients with the somatostatin analog octreotide: results of the International Multicenter Acromegaly Study Group. Arch Intern Med 1991 Aug; 151(8): 1573- CrossRef
38. Koop BL, Harris AG, Ezzat S. Effect of octreotide on glucose tolerance in acromegaly. Eur J Endocrinol 1994 Jun; 130(6): 581- CrossRef
39. Baldelli R, Battista C, Leonetti F, et al. Glucose homeostasis in acromegaly: effects of long-acting somatostatin analogues treatment. Clin Endocrinol (Oxf) 2003 Oct; 59(4): 492- CrossRef
40. Hizuka N. Divergent effects of octreotide on glucose tolerance in patients with acromegaly. Intern Med 1997 May; 36(5): 319-0 CrossRef
41. Lamers CB. Clinical and pathophysiological aspects of somatostatin and the gastrointestinal tract. Acta Endocrinol Suppl (Copenh) 1987; 286: 19-5
42. Gillis JC, Noble S, Goa KL. Octreotide long-acting release (LAR): a review of its pharmacological properties and therapeutic use in the management of acromegaly. Drugs 1997; 53(4): 681-9 CrossRef
43. Barkan AL, Dimaraki EV, Jessup SK, et al. Ghrelin secretion in humans is sexually dimorphic, suppressed by somatostatin, and not affected by the ambient growth hormone levels. J Clin Endocrinol Metab 2003 May; 88(5): 2180- CrossRef
44. Foxx-Orenstein A, Camilleri M, Stephens D, et al. Effect of a somatostatin analogue on gastric motor and sensory functions in healthy humans. Gut 2003 Nov; 52(11): 1555-1 CrossRef
45. Cremonini F, Camilleri M, Gonenne J, et al. Effect of somatostatin analog on postprandial satiation in obesity. Obes Res 2005 Sep; 13(9): 1572- CrossRef
46. Lotter EC, Krinsky R, McKay JM, et al. Somatostatin decreases food intake of rats and baboons. J Comp Physiol Psychol 1981 Apr; 95(2): 278-7 CrossRef
47. Levine AS, Morley JE. Peripherally administered somatostatin reduces feeding by a vagal mediated mechanism. Pharmacol Biochem Behav 1982 Jun; 16(6): 897-02 CrossRef
48. Campbell RM, Scanes CG. Inhibition of growth hormone-stimulated lipolysis by somatostatin, insulin, and insulin-like growth factors (somatomedins) in vitro. Proc Soc Exp Biol Med 1988 Dec; 189(3): 362-
49. Bray GA, Gallagher TF. Manifestations of hypothalamic obesity in man: a comprehensive investigation of eight patients and a review of the literature. Medicine 1975 Jul; 54(4): 301-0 CrossRef
50. Karavitaki N, Cudlip S, Adams CB, et al. Craniopharyngiomas. Endocr Rev 2006 Jun; 27(4): 371-7 CrossRef
51. Bunin GR, Surawicz TS, Witman PA, et al. The descriptive epidemiology of craniopharyngioma. J Neurosurg 1998 Oct; 89(4): 547-1 CrossRef
52. Muller HL, Emser A, Faldum A, et al. Longitudinal study on growth and body mass index before and after diagnosis of childhood craniopharyngioma. J Clin Endocrinol Metab 2004 Jul; 89(7): 3298-05 CrossRef
53. Ahmet A, Blaser S, Stephens D, et al. Weight gain in craniopharyngioma: a model for hypothalamic obesity. J Pediatr Endocrinol Metab 2006 Feb; 19(2): 121- CrossRef
54. Clement K. Genetics of human obesity. C R Biol 2006 Aug; 329(8): 608-2 CrossRef
55. Goldstone AP. The hypothalamus, hormones, and hunger: alterations in human obesity and illness. Prog Brain Res 2006; 153: 57-3 CrossRef
56. Zhang S, Bertrais S, Hercberg S, et al. Melanocortin 4 receptor mutations in a large cohort of severely obese adults: prevalence, functional classification, genotype-phenotype relationship, and lack of association with binge eating. J Clin Endocrinol Metab 2006 May; 91(5): 1811- CrossRef
57. Lustig RH. Obesity in childhood cancer survivors. Pediatr Endocrinol Rev 2006 Apr; 3 Suppl. 2: 306-1
58. Valassi E, Scacchi M, Cavagnini F. Neuroendocrine control ol food intake. Nutr Metab Cardiovasc Dis 2008 Feb; 18(2): 158-8 CrossRef
59. Preeyasombat C, Bacchetti P, Lazar AA, et al. Racial and etiopathologic dichotomies in insulin hypersecretion and resistance in obese children. J Pediatr 2005 Apr; 146(4): 474-1 CrossRef
60. Danielsson P, Janson A, Norgren S, et al. Impact sibutramine therapy in children with hypothalamic obesity or obesity with aggravating syndromes. J Clin Endocrinol Metab 2007 Nov: 92(11): 4101- CrossRef
61. Hoybye C, Hilding A, Jacobsson H, et al. Growth hormone treatment improves body composition in adults with Prader-Willi syndrome. Clin Endocrinol (Oxf) 2003 May; 58(5): 653-1 CrossRef
62. Geffner M, Lundberg M, Koltowska-Haggstrom M, et al. Changes in height, weight, and body mass index in children with craniopharyngioma after three years of growth hormone therapy: analysis of KIGS (Pfizer International Growth Database). J Clin Endocrinol Metab 2004 Nov; 89(11): 5435-0 CrossRef
63. Smith DK, Sarfeh J, Howard L. Truncal vagotomy in hypothalamic obesity. Lancet 1983 Jun; I(8337): 1330- CrossRef
64. Fobi MA. Operations that are questionable for control of obesity. Obes Surg 1993 May; 3(2): 197-00 CrossRef
65. Lustig RH, Rose SR, Burghen GA, et al. Hypothalamic obesity caused by cranial insult in children: altered glucose and insulin dynamics and reversal by a somatostatin agonist. J Pediatr 1999 Aug; 135 (2 Pt 1): 162- CrossRef
66. Nicholls RD, Saitoh S, Horsthemke B. Imprinting in Prader-Willi and Angelman syndromes. Trends Genet 1998 May; 14(5): 194-00 CrossRef
67. Holland AJ, Treasure J, Coskeran P, et al. Measurement ol excessive appetite and metabolic changes in Prader-Willi syndrome. Int J Obes Relat Metab Disord 1993 Sep; 17(9): 527-2
68. Cummings DE, Clement K, Purneil JQ, et al. Elevated plasma ghrelin levels in Prader Willi syndrome. Nat Med 2002 Jul; 8(7): 643- CrossRef
69. Norrelund H, Hansen TK, Orskov H, et al. Ghrelin immunoreactivity in human plasma is suppressed by somatostatin. Clin Endocrinol (Oxf) 2002 Oct; 57(4): 539-6 CrossRef
70. Silva AP, Bethmann K, Raulf F, et al. Regulation of ghrelin secretion by somatostatin analogs in rats. Eur J Endocrinol 2005 Jun; 152(6): 887-4 CrossRef
71. Haqq AM, Stadler DD, Rosenfeld RG, et al. Circulating ghrelin levels are suppressed by meals and octreotide therapy in children with Prader-Willi syndrome. J Clin Endocrinol Metab 2003 Aug; 88(8): 3573- CrossRef
72. Tan TM, Vanderpump M, Khoo B, et al. Somatostatin infusion lowers plasma ghrelin without reducing appetite in adults with Prader-Willi syndrome. J Clin Endocr Metabol 2004 Aug; 89(8): 4162- CrossRef
73. Goldstone AP, Thomas EL, Brynes AE, et al. Visceral adipose tissue and metabolic complications of obesity are reduced in Prader-Willi syndrome female adults: evidence for novel influences on body fat distribution. J Clin Endocrinol Metab 2001 Sep; 86(9): 4330- CrossRef
74. Kennedy L, Bittel DC, Kibiryeva N, et al. Circulating adiponectin levels, body composition and obesity-related variables in Prader-Willi syndrome: comparison with obese subjects. Int J Obes Relat Metab Disord 2006 Feb; 30(2): 382- CrossRef
75. Goldstone AP, Patterson M, Kalingag N, et al. Fasting and postprandial hyperghrelinemia in Prader-Willi syndrome is partially explained by hypoinsulinemia, and is not due to peptide YY3-36 deficiency or seen in hypothalamic obesity due to craniopharyngioma. J Clin Endocrinol Metab 2005 May; 90(5): 2681-0 CrossRef
76. Holsen LM, Zarcone JR, Brooks WM, et al. Neural mechanisms underlying hyperphagia in Prader-Willi syndrome. Obesity (Silver Spring) 2006 Jun; 14(6): 1028-7 CrossRef
77. Hinton EC, Holland AJ, Gellatly MS, et al. Neural representations of hunger and satiety in Prader-Willi syndrome. Int J Obes (Lond) 2006 Feb; 30(2): 313-1 CrossRef
78. Velasquez-Mieyer PA, Cowan PA, Arheart KL, et al. Suppression of insulin secretion is associated with weight loss and altered macronutrient intake and preference in a subset of obese adults. Int J Obes Relat Metab Disord 2003 Feb; 27(2): 219-6 CrossRef
79. Velasquez-Mieyer PA, Umpierrez GE, Lustig RH, et al. Race affects insulin and GLP-1 secretion and response to a longacting somatostatin analogue in obese adults. Int J Obes Relat Metab Disord 2004 Feb; 28(2): 330-
80. Prelevic GM, Würzburger MI, Balint-Peric L, et al. Effects of the somatostatin analogue, octreotide, in polycystic ovary syndrome. Metabolism 1992 Sep; 41 Suppl. 2: 76- CrossRef
81. Gambineri A, Patton L, De Iasio R, et al. Efficacy of octreotide-LAR in dieting women with abdominal obesity and polycystic ovary syndrome. J Clin Endocrinol Metab 2005 Jul; 90(7): 3854-2 CrossRef
82. Pasquali R, Gambineri A. Insulin-sensitizing agents in polycystic ovary syndrome. Eur J Endocrinol 2006 Jul; 86 Suppl. 1: S28-
83. Lustig RH, Mietus-Snyder ML, Bacchetti P, et al. Insulin dynamics predict body mass index and z-score response to insulin suppression or sensitization pharmacotherapy in obese children. J Pediatr 2006 Jan; 148(1): 23- CrossRef - 作者单位：Dr Themistoklis Tzotzas (1)
Kostas Papazisis (2)
Petros Perros (3)
Gerasimos E. Krassas (1)
1. Department of Endocrinology, Diabetes and Metabolism, Panagia General Hospital, Thessaloniki, Greece
2. Department of Oncology, Theagenion Medical Institute, Thessaloniki, Greece
3. Department of Endocrinology, Freeman Hospital, Newcastle Upon Tyne, UK
文摘
Obesity is a condition that results from dysregulation of energy balance. Insulin, a component of the efferent pathway of the energy-regulatory circuit, promotes storage of energy substrates in adipose tissue and is, therefore, a potential target for pharmacotherapy. Somatostatin and its analogues (octreotide and lanreotide) bind to somatostatin subtype 5 receptors on the β-cell membrane, which limits insulin release and, consequently, may decrease adipogenesis. Somatostatin and its analogues have been used in trials in patients with paediatric hypothalamic obesity. These children have hypothalamic dysfunction, mainly due to brain tumours such as craniopharyngiomas, which are thought to generate increased vagal output, leading to hyperinsulinaemia and weight gain. Two small trials, each of 6 months-duration, in children with paediatric hypothalamic obesity showed either a minimal weight loss or stabilization of bodyweight. In children with Prader-Willi syndrome, the most common genetic hypothalamic disorder associated with hyperphagia, hyperghrelinaemia, massive obesity and other endocrine disturbances, somatostatin failed to control hyperphagia and weight gain in a small number of patients, although it lowered the levels of the anorexigenic hormone ghrelin. Long-acting release octreotide was recently used in hyperinsulinaemic obese adults without cranial pathology. Insulin suppression was associated with small decreases in the body mass indexes of obese subjects receiving the higher dosages of the drug, with an acceptable safety profile, similar to that in previous studies. In conclusion, somatostatin and its analogues, by suppressing β-cell insulin secretion, can retard weight gain in children with hypothalamic obesity and induce a small amount of weight loss in some adults with hyperinsulinaemic obesity.