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Cimetidine, a Histamine H₂ Receptor Antagonist, Occupies Androgen Receptors^*

Medical Research Centre, Prince Henry's Hospital Melbourne, Australia, 3004

Address all correspondence and requests for reprints to: Dr. J. W. Funder, Medical Research Centre, Prince Henrya's Hospital, St. Kilda Road, Melbourne, Victoria, Australia, 3004.

The histamine H₂ receptor antagonist cimetidine is in increasing usage in the medical management of peptic ulcer. In clinical trials, its most frequent side effect is gynecomastia. Such estrogenic/antiandrogenic manifestations are well known side effects of treatment with digitoxin or spirolactones. Both of these drugs share a common skeleton with the steroid hormones and have been shown to occupy estrogen and/or androgen receptors. Cimetidine has no measurable affinity for rat uterine estradiol receptors, but competes for tritiated dihydrotestosterone-binding sites in mouse kidney preparations with a displacement curve parallel to that for unlabeled dihydrotestosterone. Steroid receptor-mediated side effects, therefore, may not be confined to molecules with a common skeleton, such as steroids, spirolactones, and cardiac glycosides, but may extend to such apparently unrelated molecules as histamine antagonists and androgens. (J Clin Endocrinol Metab 48: 189, 1979)

^* This work was supported by the National Health and Medical Research Council of Australia.

Received May 15, 1978.

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