Lisuride — a new drug for treatment of hyperprolactinaemic disorders

  • R. Horowski
  • R. Dorow
  • A. Scholz
  • L. De Cecco
  • W. H. F. Schneider


Lisuride (Dopergin®), a highly active dopaminergic ergot derivative with prolactin-lowering properties, has an outstanding affinity as an agonist for dopamine receptors. It is concentrated by a factor of 5–10 above lisuride plasma levels within the pituitary where it acts on dopamine receptors which inhibit prolactin release. In rats, oral lisuride is 10–30 times more active on a weight basis as a prolactin-lowering agent than bromocriptine. In carcinogenicity studies in rodents, no endometrial carcinomas could be found after 2 years of treatment; on the contrary, development of pituitary tumours was prevented almost completely and there was a dose-dependent reduction in the incidence of mammary tumours. Studies in rats, rabbits and monkeys revealed no teratogenic potential of the drug. On acute administration, doses as low as 0.1mg of lisuride p.o. decrease prolactin plasma levels in humans; this effect is enhanced and prolongated on repeated administration. Its effect is highly specific and no other hormonal systems are affected with the exception of growth hormone. Lisuride can be used in all clinical conditions where a dopaminergic or prolactin-lowering effect is needed, and its activity is unsurpassed by any other form of treatment. In the prevention of post-partum lactation, controlled studies point to a lower incidence of rebound lactation than observed with other treatments. Lisuride effectively restores normal cycles and fertility in hyperprolactinaemic women. In the pregnancies documented so far, which were induced by lisuride treatment, no evidence for any particular abnormality was observed. In healthy males, lisuride treatment did not affect spermatogenesis. In hyperprolactinaemic men suffering from prolac-tin-producing tumours, testosterone synthesis as well as libido, potency and fertility can be restored with lisuride. In the case of macroprolactinomas, treatment with lisuride not only lowered prolactin levels but also led to a sometimes dramatic reduction of tumour volume.

All these data suggest that lisuride is a highly effective drug in the treatment of menstrual cycle and fertility disorders and related situations, and a valuable alternative to bromocriptine.


Dopamine Receptor Dopamine Agonist Prolactin Level Fertility Control Ergot Derivative 
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  1. 1.
    Horowski, R. and Wachtel, H. (1976). Direct dopaminergic action of lisuride hydrogen maleate, an ergot derivative, in mice. Eur. J. Pharmacol, 36, 373PubMedCrossRefGoogle Scholar
  2. 2.
    Podvalovà, I. and Dlabac, A. (1972). Lysenyl, a new antiserotonin agent. Res. Clin. Stud. Headache, 3, 325Google Scholar
  3. 3.
    Pieri, L., Keller, H. H., Burkard, W. and Da Prada, M. (1978). Effects of lisuride and LSD on cerebral monoamine systems and hallucinosis. Nature (Lond.), 272, 278CrossRefGoogle Scholar
  4. 4.
    Reynolds, G. P. and Riederer, P. (1981). The effects of lisuride and some other dopaminergic agonists on receptor binding in human brain. J. Neural Transm., 51, 107PubMedCrossRefGoogle Scholar
  5. 5.
    Peroutka, S. J., Lebovitz, R. M. and Snyder, S. H. (1981). Two distinct central serotonin receptors with different physiological functions. Science, 212, 827PubMedCrossRefGoogle Scholar
  6. 6.
    Rogawski, M. A. and Aghajanian, G. K. (1979). Response of central monoaminergic neurons to lisuride: comparison with LSD. Life Sci., 24, 1289PubMedCrossRefGoogle Scholar
  7. 7.
    Horowski, R. (1982). Role of monoaminergic mechanisms in the mechanism of action of ergot derivatives used in migraine. In Rose, F. C. (ed.). Advances in Migraine, pp. 187–198. (New York: Raven Press)Google Scholar
  8. 8.
    Loos, D., Halbhubner, K. and Herken, H. (1977). Lisuride, a potent drug in the treatment of muscular rigidity in rats. Naunyn-Schmiedeberg’s Arch. Pharmacol., 300, 195CrossRefGoogle Scholar
  9. 9.
    Horowski, R. (1978). Differences in the dopaminergic effects of the ergot derivatives bromocriptine, lisuride and d-LSD as compared with apomorphine. Eur. J. Pharmacol , 51, 157PubMedCrossRefGoogle Scholar
  10. 10.
    Calne, D., Horowski, R., McDonald, R. J. and Wuttke, W. (eds.) (1983). lisuride and Other Dopamine Agonists. (New York: Raven Press)Google Scholar
  11. 11.
    Horowski, R. and Dorow, R. (1981). Influence of estradiol and other gonadal steroids on central effects of lisuride and comparable ergot derivatives. In Wuttke, W. and Horowski, R. (eds.). Gonadal Steroids and Brain Function, pp. 169–181. (Berlin: Springer Verlag)Google Scholar
  12. 12.
    Ahlenius, S., Larsson, K. and Svensson, L. (1980). Stimulating effects of lisuride on masculine sexual behaviour of rats. Eur.J. Pharmacol, 64, 47PubMedCrossRefGoogle Scholar
  13. 13.
    Cronin, M. J., Valdenegro, C. A., Perkins, S. N. and MacLeod, R. M. (1981). The 7315a pituitary tumor is refractory to dopaminergic inhibition of prolactin release but contains dopamine receptors. Endrocrinology, 109, 2160CrossRefGoogle Scholar
  14. 14.
    Ausková, M., Rezábek, K., Zikán, V. and Semonsky, M. (1974). Suppression of lactation in rats with lysenyl(R) SPOFA (N-(D-6-methyl-8-isoergolenyl) N’, N’-diethylcarbamide hydrogen maleate). Endocrinol Exp., 8, 51PubMedGoogle Scholar
  15. 15.
    Horowski, R. (1982). Some aspects of the dopaminergic action of ergot derivatives and their role in the treatment of migraine. In Critchley, M., et al. (eds.). Advances in Neurology, Vol. 33, pp. 325–340. (New York: Raven Press)Google Scholar
  16. 16.
    Hümpel, M., Nieuweboer, B., Hasan, S. H. and Wendt, H. (1981). Radioimmunoassay of plasma lisuride in man following intravenous and oral administration of lisuride hydrogen maleate; effects on plasma prolactin level. Eur. J. Clin. Pharmacol, 20, 47PubMedCrossRefGoogle Scholar
  17. 17.
    Hardt, W., Schmid-Gollwitzer, M. and Horowski, R. (1979). Suppression of lactation with lisuride. Gynecol. Obstet. Invest., 10, 95PubMedCrossRefGoogle Scholar
  18. 18.
    van Dam, L. H. and Rolland, R. (1981). Lactation-inhibiting and prolactin-lowering effect of lisuride and bromocriptine: A comparative study. Eur. J. Obstet. Gynecol. Reprod. Biol., 12, 323PubMedCrossRefGoogle Scholar
  19. 19.
    De Cecco, L., Venturini, P. L., Ragni, N., Valenzano, M., Constantini, S. and Horowski, R. (1983). Dopaminergic ergots in lactation and cycle disturbances. In Calne, D. B., Horowski, R., McDonald, R. J. and Wuttke, W. (eds.). Lisuride and Other Dopamine Agonists, pp. 291–299. (New York: Raven Press)Google Scholar
  20. 20.
    Schwibbe, M., Becker, D. and Wuttke, W. (1983). EEG and psychological effects of lisuride in women with premenstrual tension. In Calne, D. B., Horowski, R., McDonald, R. J. and Wuttke, W. (eds.). Lisuride and Other Dopamine Agonists, pp. 345–355. (New York: Raven Press)Google Scholar
  21. 21.
    Verde, G., Chiodini, P. G., Liuzzi, A., et al. (1980). Effectiveness of the dopamine agonist lisuride in the treatment of acromegaly and pathological hyperprolacti-nemic states. J. Endocrinol. Invest., 4, 405Google Scholar
  22. 22.
    Chiodini, P., Liuzzi, A., Cozzi, R., et al. (1981). Size reduction of macroprolactinomas by bromocriptine or lisuride treatment. J. Clin. Endocrinol. Metab., 53, 737PubMedCrossRefGoogle Scholar

Copyright information

© MTP Press Limited 1984

Authors and Affiliations

  • R. Horowski
  • R. Dorow
  • A. Scholz
  • L. De Cecco
  • W. H. F. Schneider

There are no affiliations available

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