The role of mineralocorticoid receptor function in treatment-resistant depression

J Psychopharmacol. 2013 Dec;27(12):1169-79. doi: 10.1177/0269881113499205. Epub 2013 Jul 31.

Abstract

Background: Treatment-resistant depression patients show both reduced glucocorticoid receptor function and a hyperactive hypothalamic-pituitary-adrenal axis. However, few studies have examined the role of the mineralocorticoid receptor. This study aimed to evaluate the functional activity of the mineralocorticoid receptor system in regulating the hypothalamic-pituitary-adrenal axis in well-defined treatment-resistant depression patients.

Material and method: We recruited 24 subjects divided into: (a) treatment-resistant depression; (b) healthy controls. We evaluated: (a) the effect of combined glucocorticoid receptor/mineralocorticoid receptor stimulation with prednisolone; (b) the effect of prednisolone with the mineralocorticoid receptor antagonist spironolactone; and (c) the effect of spironolactone alone. The response of the hypothalamic-pituitary-adrenal axis was measured using salivary cortisol and plasma levels of drugs were also measured.

Results: Treatment-resistant depression patients had higher cortisol compared with controls after all challenges. In controls, spironolactone increased cortisol compared to placebo. The co-administration of spironolactone with prednisolone in controls decreases the suppressive effects of prednisolone. In contrast, in treatment-resistant depression, spironolactone did not increase cortisol compared to placebo and spironolactone with prednisolone had no effect on the suppressive effects of prednisolone. Patients with treatment-resistant depression had a reduction in the conversation of spironolactone to the active metabolite canrenone.

Conclusion: Our data confirmed that treatment-resistant depression is associated with hypercortisolism and these patients no longer show an hypothalamic-pituitary-adrenal response to the administration of a mineralocorticoid receptor antagonist, suggesting that there is a mineralocorticoid receptor malfunctioning, such as a down regulation, however, pharmacokinetics and pharmacodynamics in these subjects could also have had an effect on the lack of mineralocorticoid receptor response.

Keywords: Cortisol; hypothalamic-pituitary-adrenal axis; mineralocorticoid receptor; mineralocorticoid receptor antagonist; prednisolone; treatment resistant depression.

Publication types

  • Controlled Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Canrenone / metabolism
  • Case-Control Studies
  • Depressive Disorder, Treatment-Resistant / physiopathology*
  • Female
  • Humans
  • Hydrocortisone / metabolism
  • Hypothalamo-Hypophyseal System / metabolism
  • Male
  • Middle Aged
  • Mineralocorticoid Receptor Antagonists / administration & dosage
  • Mineralocorticoid Receptor Antagonists / pharmacokinetics
  • Mineralocorticoid Receptor Antagonists / pharmacology
  • Pituitary-Adrenal System / metabolism
  • Prednisolone / administration & dosage
  • Prednisolone / pharmacology*
  • Receptors, Glucocorticoid / drug effects
  • Receptors, Glucocorticoid / metabolism*
  • Receptors, Mineralocorticoid / drug effects
  • Receptors, Mineralocorticoid / metabolism*
  • Saliva / chemistry
  • Single-Blind Method
  • Spironolactone / administration & dosage
  • Spironolactone / pharmacokinetics
  • Spironolactone / pharmacology

Substances

  • Mineralocorticoid Receptor Antagonists
  • Receptors, Glucocorticoid
  • Receptors, Mineralocorticoid
  • Spironolactone
  • Canrenone
  • Prednisolone
  • Hydrocortisone