Contraception
Volume 80, Issue 1 , Pages 53-62 , July 2009

Selective effect of chlormadinone acetate on brain allopregnanolone and opioids content

Received 25 June 2008 ,Revised 14 January 2009 ,Accepted 14 January 2009.

References 

  1. Wiegratz I, Kuhl H. Progestogen therapies: differences in clinical effects?. Trends Endocrinol Metab. 2004;15:277–285
  2. Schumacher M, Guennoun R, Ghoumari A, et al. Novel perspectives for progesterone in hormone replacement therapy, with special reference to the nervous system. Endocr Rev. 2007;28:387–439
  3. Mani S. Mini review: progestin receptor subtypes in the brain: the known and the unknown. Endocrinology. 2008;1:1
  4. Brinton RD, Thompson RF, Foy MR, et al. Progesterone receptors: form and function in brain. Front Neuroendocrinol. 2008;29:313–339
  5. Corpéchot C, Young J, Calvel M, et al. Neurosteroids: 3 alpha-hydroxy-5 alpha-pregnan-20-one and its precursors in the brain, plasma, and steroidogenic glands of male and female rats. Endocrinology. 1993;133:1003–1009
  6. Wang JM, Liu L, Irwin RW, Chen S, Brinton RD. Regenerative potential of allopregnanolone. Brain Res Rev. 2008;14(57):398–409
  7. Schumacher M, Weill-Engerer S, Liere P, et al. Steroid hormones and neurosteroids in normal and pathological aging of the nervous system. Prog Neurobiol. 2003;71:3–29
  8. Bodnar RJ, Klein GE. Endogenous opiates and behavior: 2005. Peptides. 2006;27:3391–3478
  9. Charmandari E, Tsigos C, Chrousos G. Endocrinology of the stress response. Annu Rev Physiol. 2005;67:259–284
  10. Ribeiro C, Kennedy SE, Smith YR, Stohler CS, Zubieta JK. Interface of physical and emotional stress regulation through the endogenous opioid system and mu-opioid receptors. Prog Neuropsychopharmacol Biol Psychiatry. 2005;29:1264–1280
  11. Argiolas A. Neuropeptides and sexual behaviour. Neurosci Biobehav Rev. 1999;23:1127–1142
  12. Bancroft J. The endocrinology of sexual arousal. J Endocrinol. 2005;186:411–427
  13. Bernardi F, Pluchino N, Pieri M, et al. Progesterone and medroxyprogesterone acetate effects on central and peripheral allopregnanolone and beta-endorphin levels. Neuroendocrinology. 2006;83:348–359
  14. Genazzani AR, Pluchino N, Begliuomini S, et al. Drospirenone increases central and peripheral beta-endorphin in ovariectomized female rats. Menopause. 2007;14:63–73
  15. Pluchino N, Lenzi E, Casarosa E, et al. Dydrogesterone increases allopregnanolone in selected brain areas and in serum of female rats. Fertil Steril. 2007;
  16. Pluchino N, Luisi M, Lenzi E, et al. Progesterone and progestins: effects on brain, allopregnanolone and beta-endorphin. J Steroid Biochem Mol Biol. 2006;102:205–213[Electronic publication 2006 Oct 18]
  17. Bouchard P. Chlormadinone acetate (CMA) in oral contraception — a new opportunity. Eur J Contracept Reprod Health Care. 2005;10(Suppl):7–11
  18. Bernardi F, Salvestroni C, Casarosa E, et al. Aging is associated with changes in allopregnanolone concentrations in brain, endocrine glands and serum in male rats. Eur J Endocrinol. 1998;138:316–321
  19. Genazzani AR, Stomati M, Bernardi F, et al. Conjugated equine estrogens reverse the effects of aging on central and peripheral allopregnanolone and beta-endorphin levels in female rats. Fertil Steril. 2004;81:757–766
  20. Rupprecht R, Hauser CA, Trapp T, Holsboer F. Neurosteroids: molecular mechanisms of action and psychopharmacological significance. J Steroid Biochem Mol Biol. 1996;56163–56168
  21. Karavolas HJ, Hodges DR. Neuroendocrine metabolism of progesterone and related progestins. Ciba Found Symp. 1990;153:22–44
  22. Bernardi F, Pluchino N, Stomati M, Pieri M, Genazzani AR. CNS: sex steroids and SERMs. Ann NY Acad Sci. 2003;997:378–388
  23. Cheng YJ, Karavolas HJ. Conversion of progesterone to 5α-pregnane-3,20-dione and 3α-hydroxy-5α-pregnan-20-one by rat medial basal hypothalamus and the effects of estradiol and stage of estrus cycle on the conversion. Endocrinology. 1973;93:1157–1162
  24. Schramm G, Steffens D. Contraceptive efficacy and tolerability of chlormadinone acetate 2mg/ethinylestradiol 0.03 mg (Belara)®. Clin Drug Invest. 2002;22:221–231
  25. Schramm G, Steffens D. A 12-month evaluation of the CMA containing oral contraceptive Belara®: efficacy, tolerability and antiandrogenic properties. Contraception. 2003;67:305–312
  26. Genazzani AR, Bernardi F, Pluchino N, et al. Endocrinology of menopausal transition and its brain implications. CNS Spectr. 2005;10:449–457
  27. Bernardi F, Pluchino N, Begliuomini S, et al. Disadaptive disorders in women: allopregnanolone, a sensitive steroid. Gynecol Endocrinol. 2004;19:344–353
  28. Frye CA, Walf AA. Changes in progesterone metabolites in the hippocampus can modulate open field and forced swim test behavior of proestrous rats. Horm Behav. 2002;41:306–315
  29. Uzunova V, Ceci M, Kohler C, Uzunov DP, Wrynn AS. Region-specific dysregulation of allopregnanolone brain content in the olfactory bulbectomized rat model of depression. Brain Res. 2003;20(976):1–8
  30. Mains RE, Eipper BA. Synthesis and secretion of corticotropins, melanotropins, and endorphins by rat intermediate pituitary cells. J Biol Chem. 1979;25:7885–7894

 This work was partially supported by the Fondazione Cassa di Risparmio di S. Miniato, S. Miniato, Pisa.

PII: S0010-7824(09)00007-9

doi: 10.1016/j.contraception.2009.01.005

Contraception
Volume 80, Issue 1 , Pages 53-62 , July 2009