<p>Spironolactone is deacetylated to 7α-thiospironolactone.<sup class="text-reference-group"><a class="reference-popover-link" data-content="LaCagnin LB, Lutsie P, Colby HD: Conversion of spironolactone to 7 alpha-thiomethylspironolactone by hepatic and renal microsomes. Biochem Pharmacol. 1987 Oct 15;36(20):3439-44. (PubMed ID 3675606)" href="#reference-A178069">2</a>,<a class="reference-popover-link" data-content="Los LE, Pitzenberger SM, Ramjit HG, Coddington AB, Colby HD: Hepatic metabolism of spironolactone. Production of 3-hydroxy-thiomethyl metabolites. Drug Metab Dispos. 1994 Nov-Dec;22(6):903-8. (PubMed ID 7895608)" href="#reference-A178072">3</a></sup> 7α-thiospironolactone is S-methylated to 7α-thiomethylspironolactone or undergoes an elimination reaction to canrenone.<sup class="text-reference-group"><a class="reference-popover-link" data-content="LaCagnin LB, Lutsie P, Colby HD: Conversion of spironolactone to 7 alpha-thiomethylspironolactone by hepatic and renal microsomes. Biochem Pharmacol. 1987 Oct 15;36(20):3439-44. (PubMed ID 3675606)" href="#reference-A178069">2</a>,<a class="reference-popover-link" data-content="Los LE, Pitzenberger SM, Ramjit HG, Coddington AB, Colby HD: Hepatic metabolism of spironolactone. Production of 3-hydroxy-thiomethyl metabolites. Drug Metab Dispos. 1994 Nov-Dec;22(6):903-8. (PubMed ID 7895608)" href="#reference-A178072">3</a></sup> 7α-thiomethylspironolactone is reduced to 3α-hydroxythiomethylspironolactone or 3β-hydroxythiomethylspironolactone.<sup class="text-reference-group"><a class="reference-popover-link" data-content="LaCagnin LB, Lutsie P, Colby HD: Conversion of spironolactone to 7 alpha-thiomethylspironolactone by hepatic and renal microsomes. Biochem Pharmacol. 1987 Oct 15;36(20):3439-44. (PubMed ID 3675606)" href="#reference-A178069">2</a>,<a class="reference-popover-link" data-content="Los LE, Pitzenberger SM, Ramjit HG, Coddington AB, Colby HD: Hepatic metabolism of spironolactone. Production of 3-hydroxy-thiomethyl metabolites. Drug Metab Dispos. 1994 Nov-Dec;22(6):903-8. (PubMed ID 7895608)" href="#reference-A178072">3</a></sup></p><p>Canrenone was originally thought to be the primary circulating metabolite, however more recent studies have demonstrated that the primary metabolite is actually 7α-thiomethylspironolactone.<sup class="text-reference-group"><a class="reference-popover-link" data-content="Sica DA: Pharmacokinetics and pharmacodynamics of mineralocorticoid blocking agents and their effects on potassium homeostasis. Heart Fail Rev. 2005 Jan;10(1):23-9. doi: 10.1007/s10741-005-2345-1. (PubMed ID 15947888)" href="#reference-A11837">8</a>,<a class="reference-popover-link" data-content="Gardiner P, Schrode K, Quinlan D, Martin BK, Boreham DR, Rogers MS, Stubbs K, Smith M, Karim A: Spironolactone metabolism: steady-state serum levels of the sulfur-containing metabolites. J Clin Pharmacol. 1989 Apr;29(4):342-7. (PubMed ID 2723123)" href="#reference-A178207">9</a></sup></p><p class="d-none d-sm-block"><strong>Hover over products below to view reaction partners</strong></p>