European Journal of Clinical Pharmacology

, Volume 20, Issue 6, pp 413–416

Reduction of menopausal hot flushes by methyldopa

A double blind crossover trial
  • B. -I. Nesheim
  • T. Sætre


In a double-blind study, methyldopa was shown to be significantly more effective than placebo in reducing menopausal hot flushes. The median reduction in the number of hot flushes was 38% with placebo and 65% with methyldopa. The active metabolite of methyldopa, alpha-methylnoradrenaline, is an alpha2-adrenoceptor agonist. Since the alpha2-adrenoceptor agonist clonidine also reduces hot flushes, while the alpha2-adrenoceptor antagonist yohimbine produces flushes, it is speculated that menopausal hot flushes might result from a reduced stimulation of alpha2-adrenoceptors, probably in the CNS.

Key words

methyldopa menopause hot flushes alpha2-adrenoceptor agonist 


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  1. 1.
    Hutton JD, Murray MAF, Jacobs HS, James VHT (1978) Relation between plasma oestrone and oestradiol and climacteric symptoms. Lancet 1: 678–681Google Scholar
  2. 2.
    Clayden JR, Bell JW, Pollard P (1974) Menopausal flushing: Double-blind trial of a non-hormonal medication. Br Med J 1: 409–412Google Scholar
  3. 3.
    Starke K, Endo T (1976) Presynaptic α-adrenoceptors. Gen Pharmacol 7: 307–312Google Scholar
  4. 4.
    Starke K, Borowski E, Endo T (1975) Preferential blockade of presynaptic α-adrenoceptors by yohimbine. Eur J Pharmacol 34: 385–388Google Scholar
  5. 5.
    Garfield SL, Gershon S, Sletten I, Sundland D, Ballon S (1967) Chemically induced anxiety. Int J Neuropsychiatry 3: 426–433Google Scholar
  6. 6.
    Coope J, Thomson JM, Poller L (1975) Effects of “natural oestrogen” replacement therapy on menopausal symptoms and blood clotting. Br Med J 4: 139–143Google Scholar
  7. 7.
    Baumgardner SB, Condrea H, Daane TA et al (1978) Replacement estrogen therapy for menopausal vasomotor flushes. Obstet Gynaecol 51: 445–452Google Scholar
  8. 8.
    Coope J, Williams S, Patterson JS (1978) A study of the effectiveness of propranolol in menopausal hot flushes. Br J Obstet Gynaecol 85: 472–475Google Scholar
  9. 9.
    Heritage AS, Stumpf WE, Sar M, Grant LD (1980) Brainstem catecholamine neurons are target sites for sex steroid hormones. Science 207: 1377–1379Google Scholar
  10. 10.
    Fishman J, Norton B (1975) Catechol estrogen formation in the central nervous system of the rat. Endocrinology 96: 1054–1059Google Scholar
  11. 11.
    Ball P, Knuppen R, Haupt M et al. (1972) Interactions between estrogens and catecholamines. J Clin Endocrinol 34: 736–746Google Scholar
  12. 12.
    Lloyd T, Weisz J, Breakfield XO (1978) The catechol estrogen, 2-hydroxyestradiol, inhibits catechol-O-methyltransferase activity in neuroblastoma cells. J Neurochem 31: 245–250Google Scholar

Copyright information

© Springer-Verlag 1981

Authors and Affiliations

  • B. -I. Nesheim
    • 1
  • T. Sætre
    • 1
  1. 1.Department of Gynaecology and Obstetrics, Akershus Central HospitalUniversity of OsloNorway

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