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Journal of Andrology, Vol 1, Issue 3 111-114, Copyright © 1980 by The American Society of Andrology

Competition of the Histamine H2 Antagonist Cimetidine for Androgen Binding Sites in Man

STEPHEN J. WINTERS 1, JUDY LEE 1, AND PHILIP TROEN 1

1 Department of Medicine, University of Pittsburgh School of Medicine, Montefiore Hospital, Pittsburgh, Pennsylvania

Gynecomastia and impotence have been described as side-effects of cimetidine therapy. It has previously been shown that cimetidine possesses antiandrogenic properties and competes for dihydrotestosterone (DHT) binding to the cytosol and nuclear fractions of the rat prostate. Because this interaction may be relevant to the clinical findings in man, the authors analyzed the effects of cimetidine on androgen binding to the human prostate, testis, and serum. Cimetidine competed for DHT binding sites in the human prostate with a displacement curve parallel to that of nonlabeled DHT, whereas no binding to the testis or serum was apparent. Neither histamine nor the H1 antagonist diphenhydramine was capable of inhibiting androgen binding to the human prostate. Thus, androgen antagonism may be the mechanism of the endocrine side-effects of cimetidine in man.

     Key words: cimetidine, androgen binding, prostate, testis

Submitted on October 30, 1979
Revised on December 28, 1979
Accepted on January 4, 1980






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Copyright © 1980 by The American Society of Andrology.