Τόμος 23 (2009) – Τεύχος 2 – Άρθρο 5 – Επιθεώρηση Κλινικής Φαρμακολογίας και Φαρμακοκινητικής-Διεθνής Έκδοση – Volume 23 (2009) – Issue 2 – Article 5 – Epitheorese Klinikes Farmakologias και Farmakokinetikes-International Edition

Title Clinical relevance of bromocriptine
Authors Maria S. Venetikou1 and Eric F. Adams2 

1.       Department of Medical Essential Lessons, Faculty of Health and Caring Professions, Technological Educational Institution of Athens (TEI), Egaleo, Athens, Hellas 

2.      School of Life and Health Sciences, Aston University, Aston Triangle, Birmingham

Citation Venetikou, M.S., Adams, E.F.: Clinical relevance of bromocriptine, Epitheorese Klin. Farmakol. Farmakokinet. 23(2): 77-83 (2009)
Publication Date Accepted for publication (Final Version): July 1, 2009
Full Text Language English
Order – Buy  Ηλεκτρονική Μορφή: pdf (10 €) – Digital Type: pdf (10 €)

pharmakonpress[at]pharmakonpress[.]gr

Keywords Bromocriptine, prolactinomas, prolactin suppression, tumour reduction, dopamine agonist resistance, withdrawal.
Other Terms review article
Summary Subject of this literature review, is the mechanism of prolactin inhibition and the clinical actions of the first dopamine agonist introduced in endocrine practice, bromocriptine. 2Br-a-methyl-ergocriptine (CB154-bromocriptine mesylate) (Parlodel, Provide!) was produced in 1967 and has initially been used in the treatment of hyperprolactinaemia. Bromocriptine was found to inhibit prolactin secretion in all mammals and fishes that have so far been examined, either under physiological conditions or during the phase that the hormone secretion is stimulated with physiological, pharmacological or surgical criteria. The drug acts directly on the pituitary lactotrophs and reduces prolactin secretion without influencing the hormonal synthesis but with reducing the out cellular events. It suppresses post partum lactation and galactorroea of any cause. It restores infertility due to hyperprolactinaemia and it has been so far particularly useful in the treatment of micro and macroprolactinomas. It has also been used as a secondary form of treatment in acromegaly. It has also been useful in the treatment of Parkinson’s disease. Prolactinomas may show resistance to bromocriptine and other dopamine agonists in both prolactin levels and tumour size reduction and this may be due to the fact that some tumours have reduced number of D2 receptors. Another disadvantage of the dopamine agonist therapy is its supposed lifelong requirement, since after discontinuation, prolactin levels increase and tumour size may show clear-cut re-expansion. Newer and stronger dopamine agonists with longer duration of action have been developed through the years to overcome the side effects of bromocriptine and its three daily dosage requirement; till now most of these drugs are being compared with the well known clinical behaviour of bromocriptine.
References 1. Flückiger E., Wagner H.: 2-Br-a-Ergokryptin: influence on fertility and lactation in the rat. Experientia 24: 1130-1131 (1968)

2. Mantegani S., Brabilla E., Varasi M.: Ergoline derivatives. Receptor affinity and selectivity. Farmaco 54: 288-296 (1999)

3. Friesen H.G.: Human prolactin. Ann. R. Coll. Phys. Surg. Can. 11: 275 -281 (1978)

4. Hwang P., Guyda H., Friesen H.A.: Radioimmunoassay for human prolactin. Proc. Natl. Acad. Sci. USA 68: 1902-1906 (1971)

5. Franks S., Murray M.A.F., Jequier AM., Steele S.J., Nabarro J.D.N., Jacobs H.S.: Incidence and significance of hyperprolactinaemia in women with amenorrhoea. Clin. Endocrinol. (Oxf) 4: 587-607 (1975)

6. Franks S., Nabarro J.D.N., Jacobs H.S.: Prevalence and presentation of hyperprolactinaemia in patients with functionless pituitary tumours. Lancet 1: 778-780(1977)

7. Thorner M.O.: Prolactin: Clinical physiology and the significance and management of hyperprolactinaemia. In: Clinical Neuroendocrinology (L. Martini, G.M. Besser, eds). Pp. 285-302, Academic Press, London, 1977

8. Corrodi H., Fuxe K., Hokfelt T., Lidbrink P., Ungerstedt U.: Effect of ergot drugs on central catecholamine neurons: evidence for a stimulation of central dopamine neurons. J. Pharmacol. 25: 409-412 (1973)

9. Fuxe K., Corrodi H., Hokfelt T., Lidbrink P., Ungerstedt U.: Ergocornine and 2-Br-a-ergocryptine. Evidence for prolonged dopamine receptor stimulation. Med. Biol. 52: 121-132 (1974)

10. Schally .V., Dupont A., Arimura A., Takahara J., Redding T. W., Clemens J., Shaar C.J.: Purification of catecholamine-rich fraction with prolactin release-inhibiting factor (PIF) activity from porcine hypothalami. Acta Endocrinol. (Khb) 82: 1-14 (1976)

11. Flückiger E.: The pharmacology of bromocriptine. In: Pharmacological and clinical aspects of bromocriptine (Parlodel) (R.I.S. Bayliss, P. Turner, W.P. Maclay, eds) pp. 12-26, MCS Consultants, Turnbridge Wells, Kent, UK, 1976

12. Pasteels J.L., Danguy A., Fretotte M., Ectors F.: Inhibition de la secretion de prolactine par l’ergocornine et la 2-Br-a-ergocryptine. Action direct sur l’hypophyse en culture. Ann. Endocrinol. (Paris) 32: 188-192 (1971)

13. Schams D.: Prolactin release effects of TRH in the bovine and their depression by a prolactin inhibitor. Horm. Metab. Res. 4: 405 (1972)

14. Flückiger E., Marko M., Doepfner W., Niederer W.: Effects of ergot -alkaloids on the hypothalamic-pituitary axis. Postgr. Med. J. 52 (suppl 1): 57 – 61 (1976)

15. Flückiger E.: Ergot alkaloids and the modulation of hypothalamic function. In: Pharmacology of the Hypothalamus (B. Cox, I.D. Morris, A.H. Weston, eds). Pp. 137-160, MacMillan, London, 1978

16. Yanai R., Nagasawa, H.: Effect of 2-Br-a ergocryptine on pituitary synthesis and release of prolactin and growth hormone in rats. Horm. Res. 5: 1-5 (1974)

17. Hausler A., Rohr H.P., Marbach P., Flückiger E.: Changes in prolactin secretion in lactating rats assessed by correlative morphometric and biochemical methods. J. Ultrastruct. Res. 64: 74-84 (1978)

18. Yanai R., Nagasawa H.: Effects of ergocornine and 2-Br-a-ergo-cryptine (CB154) on the formation of mammary hyperplastic alveolar nodules and the pituitary prolactin levels in mice. Experientia 26: 649 – 650 (1970)

19. Lloyd H.M., Jacoby J.M., Meares J.D.: DNA synthesis and depletion of prolactin in the pituitary gland of the male rat. J. Endocrinol. 77: 129 -136(1978)

20. Lloyd H.M., Meares J.D., Jacobi J.M.: Effects of oestrogen and bromocriptine on in vivo secretion and mitosis in prolactin cells. Nature 255: 497-498(1975)

21. Nagasawa H., Yanai R.: Promotion of pituitary prolactin release in rats by dibutyryl-adenosine-3’5′-monophosphate. J. Endocrinol. 55: 215-217 (1972)

22. Nagasawa H., Yanai R., Fluckiger E.: Counteraction by 2-Br-a-ergocryptine of pituitary prolactin release promoted by dibutyryl-adenosine 3’5′ monophospate. In: Human Prolactin (J.L. Pasteels, C. Robyn, eds). Pp 313-315, Experta Medica, Amsterdam, 1973

23. Kimura H., Calabro M.A., MacLeod R.M.: Suppression of prolactin secretion and cAMP accumulation by dopamine in the pituitary. Fed. Proc. 35: 305 (1976)

24. Markstein R., Herrling PL., Wagner H.: Bromocriptine mimics dopamine effects on the cyclic-AMP system of rat

pituitary gland (abstract). Seventh International Congress of Pharmacology, Pergamon Press, Paris, 1978

25. Schmidt M.J., Hill L.E.: Effects of ergots on adenylate cyclase activity in the corpus stiatum and pituitary. Life Sci. 20: 789-798 (1977)

26. Enjalbert A., Bockaert J.: Pharmacological characterization of the dopamine receptor negatively coupled with adenylate cyclase in rat anterior pituitary. Mol. Pharmacol. 23: 576-584 (1983)

27. Vallar L., Melddesi J.: Mechanisms of signal transduction at the dopamine D2 receptor. Trends Pharmacol. Sci. 10: 74-77 (1989)

28. Wood D.F., Johnston J.M., Johnston D.G.: Dopamine, the dopaminergic D2 receptor and pituitary tumours. Clin. Endocrinol. (Oxf) 35: 455-466 (1991)

29. Caccavelli L, Cussac D., Pellegrini I., Audinot V., Jaquet P., Enjalbert A.: D2 dopaminergic receptors: normal and abnormal transduction mechanisms. Horm. Res. 38: 78-83 (1992)

30. Bunzow J.R., Van Toll H.H., Grandy D.K., Albert P., Salon J., Christie M., Machida C.A., Neve K.A., Civelli O.: Cloning and expression of a rat D2 dopamine receptor cDNA. Nature 336: 783-787 (1988)

31. Giros B., Sokoloff S.,, Martres MP, Riou J.F., Emorcine L.J., Schaartz L.C.: Alternative splicing directs the expression of two D2 dopamine receptors isoforms. Nature 342: 783-787 (1989)

32. Missale C, Nash S.R., Robinson S.W., Jaber M., Caron M.G.: Dopamine receptors: from structure to function. Physiol. Rev. 78: 189-225 (1998)

33. Colao A., diSarno A., Pivonello S., diSomma C, Lombardi G.: Dopamine receptor agonists for treating prolactinomas. Expert. Opin. Invstig. Drugs 11: 787-800 (2002)

34. Bevan J.S., Webster J., Burke C.W., Scanlon M.F.: Dopamine agonists and pituitary tumour shrinkage. Endocr. Rev., 13: 220-240 (1992)

35. Trouillas J., Chevalier P., Claustrat B., Hooghe-Peters E., Dubray C, Rousset B., Girod C.: Inhibitory effects of the dopamine agonists quinagolide (CV 205-502) and bromocriptine on prolactin secretion and growth of SMtTW pituitary tumours in the rat. Endocrinology 134: 401-410 (1994)

36. Wass J.A.H., Thorner M.O., Charlesworth M., Moult P.J.A., Dacie J.E., Jones A.E., Besser G.M.: Reduction of pituitary tumour size in patients with prolactinomas and acromegaly treated with bromocriptine with or without radiotherapy. Lancet 2: 66-69 (1979)

37. Thorner M.O., Perryman R.L., Rogol A.D., Conway BP., MacLeod R.M., Login I.V., Morris J.L.: Rapid changes of prolactinoma volume after withdrawal and reinstitution of bromocriptine. J. Clin. Endocrinol. Metab. 53: 480-483 (1981)

38. Molitch M.E.: Dopamine resistance to prolactinomas. Pituitary 6: 19-2 (2003)

39. Pellegrini I., Rasolonjanahary R., Gunz G., Bertrand P., Delivet S., Jedynac CP., Kordon C, Peillon F., Jaquet P., Enjallbert A.: Resistance to bromocriptine in prolactinomas. J. Clin. Endocrinol. Metab. 69: 500-509(1989)

40. Kukskas L.A, Domec C., Bacles L., Bonnet J., Verrier D., Israel J.M., Vincent J.D.: Different expression of the two dopaminergic D2 receptors D2415 and D2444, in the two types of lactotroph each characterized by their response to dopamine, and modification of expression by sex steroids. Endocrinology 129:1101-1103 (1991)

41. Missale C., Boroni F., Losa M., Giovanelli M., Zanellato A., Dal Toso M., Balsari A., Spano P.: Nerve growth factor suppresses the transforming of human prolactinomas. Proc. Natl. Acad. Sci. USA 90: 7961-7965 (1993)

42. Caccavelli L., Feron F., Morange I., Rouer E., Benarous R., Dewailly D., Jaquet P., Kordon C., Enjalbert A.: Decreased expression of the two D2 dopamine receptor isoforms in bromocriptine-resistant prolactinomas. Neuroendocrinology 60: 314-322 (1994)

43. Kovacs K., Stefaneanu L., Horvath E., Buchfelder M., Fahlbusch R., Becker W.: Prolactin-producing pituitary tumour resistance to dopamine agonist therapy. Case report. J. Neurosurg. 82: 886-890 (1995)

44. Colao A., Di Sarno A., Samacchiaro F., Ferone D., Di Renzo G., Merda B., Annunziato L., Lombardi G.: Prolactinoma resistant to standard dopamine agonists responds to chronic cabergoline treatment. J. Endocrinol. Metab. 82: 876-883 (1997)

45. Verhelst J., Abs R., Maiter D., Van den Bruel A., Vandeweghe M., Velkeniers B., Mockel J., Lambergts G., Petrossians P., Coremans P., Mahler C, Stevenaert A., Verlooy J., Raftopoulos C., Beckers A.: Cabergoline in the treatment of hyperprolactinaemia : a study of 455 patients. J. Clin. Endocrinol. Metab. 84: 2518-2522 (1999)

46. Argonz J., Del Castillo E.B.: A syndrome characterized by oestrogen insufficiency, galactorrhoea and decreased urinary gonadotrophin. J. Clin. Endocrinol. Metab. 13: 79-87 (1953)

47. Bevan J.S., Adams C.B., Burke C.W., Morton K.E., Molyneux A.J., Moo R.A., Esiri M.M.: Factors in the outcome of transphenoidal surgery for prolactinoma and non-functioning pituitary tumour including pre-operative bromocriptine therapy. Clin. Endocrinol. (Oxf) 26: 547-556 (1987)

48. Losa M., Mortini P., Bazzghi R., Gioia L, Giovanelli M.: Surgical treatment of prolactin-secreting pituitary adenomas: early results and long term outcome. J. Clin. Endocrinol. Metab. 87: 3180-3186 (2002)

49. Schlechte J.A., Sherman B.M., Chapter F.K., Van Gilder J.: Long-term follow-up of women with surgically treated prolactin-secreting pituitary tumours. J. Clin. Endocrinol. Metab. 62: 1296-1301 (1986)

50. Jonhston D.G., Prescott R.W., Kendall-Taylor P., Hall K., Crombis A.L., Hall R., McGregor A., Watson M.J., Cook D.: Hyperprolactinaemia: long-term effects of bromocriptine. Am. J. Med. 75: 868-874 (1983)

51. Bengh T., Nillius S.J., Wide L.: Menstrual function and serum prolactin levels after long-term bromocriptine treatment of hyperprolactinaemic amenorrhea. Clin. Endocrinol. (Oxf) 16: 587-593 (1982)

52. Jonhston D.G., Hall K, Kendall-Taylor P., Patrick D., Watson M.J., Cook D.B.: Effect of dopamine agonist withdrawal after long-term therapy in prolactinomas. Studies with high-definition computerized tomography. Lancet 2: 187-192(1984)

53. Mason W.S., Dudzinski M., Handwerger S.H., Hammond C.B.: Hyperprolactinaemic response after bromocriptine withdrawal in women with prolactin-secreting pituitary tumours. Fertil. Steril. 41: 218-223 (1984)

54. Biswas M., Smith J., Jadon D., Mc Ewan P., Rees D.A., Evans L.M., Scalon M.F., Davies J.S.: Long term remission following withdrawal of dopamine agonist therapy in subjects with microprolactinomas. Clin. Endocrinol. (Oxf) 63: 26-31 (2005)

55. Wang C., Lam K.S., Ma J.T., Chan T., Liu M.Y., Yeung R.T.: Long term treatment of hyperprolactinaemia with bromocriptine. Effect of drug withdrawal. Clin. Endocrinol. (Oxf) 27: 363-371 (1987)

56. Moriondo P., Tavaglini P., Nissim M., Conti A., Faglia G.: Bromocriptine treatment of microprolactinomas: evidence of stable prolactin decrease after drug withdrawal. J. Clin. Endocrinol. Metab. 60: 764-772 (1985)

57. Passos V.Q., Souza J.J., Musolino NR., Bronstein M.D.: Long term follow-up of prolactinoma: normoprolactinaemia after bromocriptine withdrawal. J. Clin. Endocrinol. Metab. 87: 3578-3582 (2002)

58. Winkelmann W., Allolio B., Deuss U., Heesen D., Kaulen D.: Persisting normoprolactinaemia after withdrawal of bromocriptine long term therapy in patients with prolactinoma. In: (MacLeod R.M., Thorner M.O., Scapagnini U. (eds) Basic and Clinical Correlates. Pp. 817-822, Liviana Press, Padova Italy, 1985

59. Zarate A., Canales E.S., Cano C, Pilonieta C.J.: Follow-up of patients with prolactinomas after discontinuation of long-term therapy with bromocriptine. Acta Endocrinol. (Copenh) 104: 139-142 (1983)

60. Van’t Verlaat J.W., Crough R.J.: Withdrawal of bromocriptine after long-term therapy for macroprolactinomas; effect on plasma prolactin and tumour size. Clin. Endocrinol. (Oxf) 34: 175-178 (1991)

61. Vance M.L., Evans W.S., Thorner M.O.: Drugs five years later: bromocriptine. Ann. Intern. Med. 100: 78-91 (1984)

62. Grottaz B., Usk A., Reymind M.J., Rey A., Siegel R.A., Brownell J., Gomez F.: CV 205-502 treatment of macroprolactinomas. J. Endocrinol. Invest. 14: 757-762 (1991)

63. Thorner M.O., Pern/man R.L., Rogol A.D., Conway BP., MacLeod R.M., Login I.S., Morris J.L.: Rapid changes of prolactinoma volume after withdrawal and reinstitution of bromocriptine. J. Clin. Endocrinol. Metab. 53: 480-483 (1981)

64. Venetikou M.S.: Investigation of the actions of two novel dopaminergic drugs CV 205-502 and CQP 201-403 in the secretion of prolactin and growth hormone. Medical Thesis (Diatrivi), University of Athens, Medical School, Athens Greece (1994)

65. Venetikou M.S., Burrin J.M., Woods C.A., Yeo T.H., Adams E.F.: The novel dopaminergic drugs CV 205-502 and CQP 201-403 suppress prolactin and growth hormone in the normal and tumorous pituitary. J. Endocrinol. 112 (Suppl.): 150 (1987)

66. Venetikou M.S., Burrin J.M., Woods C.A., Yeo T.H., Brownwell J., Adams E.F.: Effects of two novel dopaminergic drugs, CV 205-502 and CQP 201-502 on prolactin and growth hormone secretion by human pituitary tumours. Acta Endocrinol. (Copenh) 116: 287-292 (1987)

Relative Papers

Online ISSN 1011-6575

Άρθρα Δημοσιευμένα σε αυτό το Περιοδικό Καταχωρούνται στα:

Articles published in this Journal are Indexed or Abstracted in: • Chemical Abstracts • Elsevier’s Bibliographic Databases: Scopus, EMBASE, EMBiology, Elsevier BIOBASE SCImago Journal and Country Rank Factor

Τι είναι η Επιθεώρηση Κλινικής Φαρμακολογίας και Φαρμακοκινητικής-Διεθνής Έκδοση-Οδηγίες προς τους Συγγραφείς – 
What is Epitheorese Klinikes Farmakologias 
και Farmakokinetikes-International Edition-Instrunctions to Authors

Άρθρα Δημοσιευμένα στην Επιθεώρηση Κλινικής Φαρμακολογίας και Φαρμακοκινητικής-Διεθνής Έκδοση – 
Articles Published in Epitheorese Klinikes Farmakologias 
και Farmakokinetikes-International Edition

Συντακτικη Επιτροπή-Editorial Board

ΕΤΗΣΙΑ ΣΥΝΔΡΟΜΗ 2009 – ANNUAL SUBSCRIPTION 2009
Γλώσσα Πλήρους Κειμένου – Full Text Language Αγγλικά – English
Παραγγελία – Αγορά – Order – Buy Ηλεκτρονική Μορφή: pdf (70 €) – Digital Type: pdf (70 €)

pharmakonpress[at]pharmakonpress[.]gr

Έντυπη Μορφή (70 € + έξοδα αποστολής) – Printed Type (70 € + shipping)

pharmakonpress[at]pharmakonpress[.]gr

 

 

 

 

Bookmark the permalink.

Comments are closed.