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Related Experiment Videos

Prolactin responses to cimetidine

W L Burland, R I Gleadle, R M Lee

    British Journal of Clinical Pharmacology
    |January 1, 1979
    PubMed
    Summary
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    Intravenous cimetidine significantly increases prolactin levels in men, an effect blocked by bromocriptine. Oral cimetidine did not raise prolactin, suggesting dose-dependent effects and potential idiosyncratic responses.

    Area of Science:

    • Pharmacology
    • Endocrinology

    Background:

    • Cimetidine, a histamine H2 receptor antagonist, is widely used.
    • Elevated prolactin (hyperprolactinemia) can cause endocrine disturbances.

    Purpose of the Study:

    • To investigate the effect of intravenous and oral cimetidine on serum prolactin levels in healthy males.
    • To explore the role of prolactin in cimetidine-associated side effects like gynecomastia.

    Main Methods:

    • Four healthy males received a 400 mg intravenous injection of cimetidine.
    • A separate group of healthy males received an 800 mg oral dose of cimetidine.
    • Serum prolactin levels were measured, and bromocriptine pretreatment was used in one experiment.

    Main Results:

    • Intravenous cimetidine caused a threefold increase in serum prolactin.

    Related Experiment Videos

  • Bromocriptine pretreatment prevented the prolactin increase induced by intravenous cimetidine.
  • Oral cimetidine (800 mg) did not elevate prolactin levels, with peak concentrations less than 20% of IV dose.
  • Hyperprolactinemia was observed in 3 of 7 patients experiencing gynecomastia or galactorrhea during cimetidine treatment.

    • Conclusions:

    • Intravenous cimetidine can acutely increase prolactin levels in healthy males.
    • The prolactin-elevating effect of cimetidine appears to be dose-dependent.
    • Hyperprolactinemia may contribute to idiosyncratic side effects like gynecomastia and galactorrhea at therapeutic oral doses.