Summary: A series of structurally-related alkaloids that contain the ergoline backbone structure.

Top Publications

  1. Gopal R, Bandgar T, Menon P, Shah N. Remission in Cushing disease with cabergoline. Ann Saudi Med. 2008;28:224-5 pubmed
  2. Youssef M, van Wely M, Hassan M, Al Inany H, Mochtar M, Khattab S, et al. Can dopamine agonists reduce the incidence and severity of OHSS in IVF/ICSI treatment cycles? A systematic review and meta-analysis. Hum Reprod Update. 2010;16:459-66 pubmed publisher
    ..Recently, dopamine agonists were proposed as a prophylactic treatment for ovarian hyperstimulation syndrome (OHSS) in women at high risk in IVF/ICSI treatment cycles...
  3. Ono M, Miki N, Amano K, Kawamata T, Seki T, Makino R, et al. Individualized high-dose cabergoline therapy for hyperprolactinemic infertility in women with micro- and macroprolactinomas. J Clin Endocrinol Metab. 2010;95:2672-9 pubmed publisher
    ..Cabergoline monotherapy could substitute for the conventional combination therapy of pregestational surgery or irradiation plus bromocriptine in macroprolactinomas. ..
  4. Miyoshi T, Otsuka F, Takeda M, Inagaki K, Suzuki J, Ogura T, et al. Effect of cabergoline treatment on Cushing's disease caused by aberrant adrenocorticotropin-secreting macroadenoma. J Endocrinol Invest. 2004;27:1055-9 pubmed
    ..This case demonstrates the efficacy of cabergoline to treat Cushing's disease caused by pituitary macroadenoma secreting aberrant ACTH molecules. ..
  5. Shimon I, Benbassat C, Hadani M. Effectiveness of long-term cabergoline treatment for giant prolactinoma: study of 12 men. Eur J Endocrinol. 2007;156:225-31 pubmed
    ..To review our experience with cabergoline, a D2-selective dopamine agonist, for the treatment of giant prolactinomas...
  6. Zanettini R, Antonini A, Gatto G, Gentile R, Tesei S, Pezzoli G. Valvular heart disease and the use of dopamine agonists for Parkinson's disease. N Engl J Med. 2007;356:39-46 pubmed
    ..These findings should be considered in evaluating the risk-benefit ratio of treatment with ergot derivatives. ..
  7. Manavela M, Danilowicz K, Bruno O. Macrocorticotropinoma shrinkage and control of hypercortisolism under long-term cabergoline therapy: case report. Pituitary. 2012;15 Suppl 1:33-6 pubmed publisher
    ..We show the effectiveness of cabergoline in maintaining long-term biochemical control of hypercortisolism with significant reduction and stabilization of macroadenoma volume in a patient with Cushing's disease. ..
  8. Manno M, Tomei F, Marchesan E, Adamo V. Cabergoline: a safe, easy, cheap, and effective drug for prevention/treatment of ovarian hyperstimulation syndrome?. Eur J Obstet Gynecol Reprod Biol. 2005;122:127-8 pubmed
  9. Jähnichen S, Horowski R, Pertz H. Agonism at 5-HT2B receptors is not a class effect of the ergolines. Eur J Pharmacol. 2005;513:225-8 pubmed
    ..To evaluate whether agonism at 5-HT2B receptors is a phenomenon of the class of the ergolines, we studied 5-HT2B receptor-mediated relaxation in porcine pulmonary arteries to five ergolines which are used ..

More Information


  1. Laloi Michelin M, Ciraru Vigneron N, Meas T. Cabergoline treatment of pregnant women with macroprolactinomas. Int J Gynaecol Obstet. 2007;99:61-2 pubmed
  2. Motazedian S, Babakhani L, Fereshtehnejad S, Mojthahedi K. A comparison of bromocriptine & cabergoline on fertility outcome of hyperprolactinemic infertile women undergoing intrauterine insemination. Indian J Med Res. 2010;131:670-4 pubmed
    ..4%) (P<0.001). Our results suggest that cabergoline treatment in infertile women with prolactinemia is more effective. It lowers prolactin with better tolerability and much more effective in the achievement of pregnancy. ..
  3. Bhansali A, Walia R, Dutta P, Khandelwal N, Sialy R, Bhadada S. Efficacy of cabergoline on rapid escalation of dose in men with macroprolactinomas. Indian J Med Res. 2010;131:530-5 pubmed
    ..This possibly results in delayed normalization of serum prolactin and slow reduction in tumour size. This study was planned to assess the efficacy and safety of rapid escalation of cabergoline doses in men with macroprolactinomas...
  4. Pivonello R, De Martino M, Cappabianca P, De Leo M, Faggiano A, Lombardi G, et al. The medical treatment of Cushing's disease: effectiveness of chronic treatment with the dopamine agonist cabergoline in patients unsuccessfully treated by surgery. J Clin Endocrinol Metab. 2009;94:223-30 pubmed publisher
    ..If this evidence is confirmed by additional studies, this agent may be considered as a useful treatment option in patients with CD who are unsuccessfully treated by neurosurgery. ..
  5. Lila A, Gopal R, Acharya S, George J, Sarathi V, Bandgar T, et al. Efficacy of cabergoline in uncured (persistent or recurrent) Cushing disease after pituitary surgical treatment with or without radiotherapy. Endocr Pract. 2010;16:968-76 pubmed publisher
    ..To evaluate the efficacy of cabergoline therapy in patients with Cushing disease who remained uncured (had persistent or recurrent disease) after a pituitary surgical procedure with or without radiotherapy...
  6. Gibson C, Karmally W, McMahon D, Wardlaw S, Korner J. Randomized pilot study of cabergoline, a dopamine receptor agonist: effects on body weight and glucose tolerance in obese adults. Diabetes Obes Metab. 2012;14:335-40 pubmed publisher
  7. Gomez R, Gonzalez Izquierdo M, Zimmermann R, Novella Maestre E, Alonso Muriel I, Sanchez Criado J, et al. Low-dose dopamine agonist administration blocks vascular endothelial growth factor (VEGF)-mediated vascular hyperpermeability without altering VEGF receptor 2-dependent luteal angiogenesis in a rat ovarian hyperstimulation model. Endocrinology. 2006;147:5400-11 pubmed
    ..Prophylactic administration of cabergoline (5-10 microg/kg x d) decreased the occurrence of OHSS from 65% (controls) to 25% (treatment). Therefore, a specific, safe treatment for OHSS is now available. ..
  8. Roth B. Drugs and valvular heart disease. N Engl J Med. 2007;356:6-9 pubmed
  9. Schade R, Andersohn F, Suissa S, Haverkamp W, Garbe E. Dopamine agonists and the risk of cardiac-valve regurgitation. N Engl J Med. 2007;356:29-38 pubmed
    ..9; 95% CI, 1.5 to 15.6), but not with current use of other dopamine agonists. In this study, use of the dopamine agonists pergolide and cabergoline was associated with an increased risk of newly diagnosed cardiac-valve regurgitation. ..
  10. Zatelli M, Minoia M, Filieri C, Tagliati F, Buratto M, Ambrosio M, et al. Effect of everolimus on cell viability in nonfunctioning pituitary adenomas. J Clin Endocrinol Metab. 2010;95:968-76 pubmed publisher
    ..Everolimus reduced NFA cell viability by inducing apoptosis, with a mechanism likely involving IGF-I signaling but not VEGF secretion, suggesting that it might represent a possible medical treatment of invasive/recurrent NFAs. ..
  11. Vilar L, Naves L, Azevedo M, Arruda M, Arahata C, Moura e Silva L, et al. Effectiveness of cabergoline in monotherapy and combined with ketoconazole in the management of Cushing's disease. Pituitary. 2010;13:123-9 pubmed publisher
    ..Moreover, the addition of relatively low doses of ketoconazole led to normalization of UFC in about two-thirds of patients not achieving a full response to cabergoline. ..
  12. Stalldecker G, Mallea Gil M, Guitelman M, Alfieri A, Ballarino M, Boero L, et al. Effects of cabergoline on pregnancy and embryo-fetal development: retrospective study on 103 pregnancies and a review of the literature. Pituitary. 2010;13:345-50 pubmed publisher
    ..We registered 2 abnormalities in the development of the children: epilepsy and PDD. Larger series of patients are needed to assess the safety of this drug during pregnancy. ..
  13. Gomez R, Ferrero H, Delgado Rosas F, Gaytan M, Morales C, Zimmermann R, et al. Evidences for the existence of a low dopaminergic tone in polycystic ovarian syndrome: implications for OHSS development and treatment. J Clin Endocrinol Metab. 2011;96:2484-92 pubmed publisher
    ..Deregulation of the VEGF/VEGF receptor (VEGFR)-2 pathway leading to increased risk of ovarian hyperstimulation syndrome has been described in the ovary of patients suffering from polycystic ovarian syndrome (PCOS)...
  14. Zhang W, Murao K, Imachi H, Iwama H, Chen K, Fei Z, et al. Suppression of prolactin expression by cabergoline requires prolactin regulatory element-binding protein (PREB) in GH3 cells. Horm Metab Res. 2010;42:557-61 pubmed publisher
    ..We have demonstrated that PREB is expressed in prolactinomas and that the suppression of PRL expression by cabergoline requires the transcriptional factor PREB. ..
  15. Godbout A, Manavela M, Danilowicz K, Beauregard H, Bruno O, Lacroix A. Cabergoline monotherapy in the long-term treatment of Cushing's disease. Eur J Endocrinol. 2010;163:709-16 pubmed publisher
    ..No long-term response was maintained in four initial partial responders. Cabergoline monotherapy can provide an effective long-term medical therapy for selected patients with CD, but requires close follow-up for dose adjustments. ..
  16. Dos Santos Nunes V, El Dib R, Boguszewski C, Nogueira C. Cabergoline versus bromocriptine in the treatment of hyperprolactinemia: a systematic review of randomized controlled trials and meta-analysis. Pituitary. 2011;14:259-65 pubmed publisher
    ..43 [CI 95% 1.03, 1.98]). The meta-analysis showed new evidence favoring the use of cabergoline in comparison with bromocriptine for the treatment of prolactinomas and idiopathic hyperprolactinemia. ..
  17. Cushing D, Cohen M. Serotonin-induced contraction in porcine coronary artery: use of ergolines to support vascular 5-hydroxytryptamine2-receptor heterogeneity. J Pharmacol Exp Ther. 1993;264:193-200 pubmed
    ..However, the low antagonist affinity of the ergolines (i.e., LY53857 and sergolexole) suggests that heterogeneity of 5-HT2 receptors may exist among species.
  18. Tanaka K, Ogawa N. Dopamine agonist cabergoline inhibits levodopa-induced caspase activation in 6-OHDA-lesioned mice. Neurosci Res. 2005;51:9-13 pubmed
    ..These results indicate that such prevention is attributable mainly to the increase in GSH content and to the inhibition of caspase activities in 6-OHDA-lesioned mice. ..
  19. Di Sarno A, Landi M, Cappabianca P, Di Salle F, Rossi F, Pivonello R, et al. Resistance to cabergoline as compared with bromocriptine in hyperprolactinemia: prevalence, clinical definition, and therapeutic strategy. J Clin Endocrinol Metab. 2001;86:5256-61 pubmed
    ..Therefore, an absence of tumor shrinkage cannot be considered as end point to indicate resistance to CAB, and increasing the dose of CAB higher than 3 mg/wk does not seem to be helpful in controlling PRL hypersecretion. ..
  20. Pivonello R, Ferone D, de Herder W, Kros J, De Caro M, Arvigo M, et al. Dopamine receptor expression and function in corticotroph pituitary tumors. J Clin Endocrinol Metab. 2004;89:2452-62 pubmed
    ..The effectiveness of cabergoline in normalizing cortisol secretion in 40% of cases supports its therapeutic use in the management of Cushing's disease. ..
  21. Colao A, Vitale G, Cappabianca P, Briganti F, Ciccarelli A, De Rosa M, et al. Outcome of cabergoline treatment in men with prolactinoma: effects of a 24-month treatment on prolactin levels, tumor mass, recovery of pituitary function, and semen analysis. J Clin Endocrinol Metab. 2004;89:1704-11 pubmed
    ..These data demonstrate that cabergoline treatment is as effective and safe in men as in women with prolactinoma and can be successfully used as primary therapy even in men bearing large macroprolactinomas. ..
  22. Corsello S, Ubertini G, Altomare M, Lovicu R, Migneco M, Rota C, et al. Giant prolactinomas in men: efficacy of cabergoline treatment. Clin Endocrinol (Oxf). 2003;58:662-70 pubmed
    ..These data suggest that, in giant, aggressive prolactinomas, CAB represents a first-line therapy effective in reducing PRL levels and determining tumour shrinkage. ..
  23. Liu C, Tyrrell J. Successful treatment of a large macroprolactinoma with cabergoline during pregnancy. Pituitary. 2001;4:179-85 pubmed
    ..PRL levels ranged from 190 to 278 microg/L during the last 10 weeks of pregnancy. She had a C-section electively at 37 weeks gestation and delivered a healthy baby. Management options in this patient and during pregnancy are discussed. ..
  24. Papaleo E, Doldi N, De Santis L, Marelli G, Marsiglio E, Rofena S, et al. Cabergoline influences ovarian stimulation in hyperprolactinaemic patients with polycystic ovary syndrome. Hum Reprod. 2001;16:2263-6 pubmed
  25. Colao A, Lombardi G, Annunziato L. Cabergoline. Expert Opin Pharmacother. 2000;1:555-74 pubmed
    ..CAB was also reported to have some efficacy in patients with Nelson's syndrome and Cushing's disease although these data are available only for limited case reports. ..
  26. Colao A, Di Sarno A, Landi M, Scavuzzo F, Cappabianca P, Pivonello R, et al. Macroprolactinoma shrinkage during cabergoline treatment is greater in naive patients than in patients pretreated with other dopamine agonists: a prospective study in 110 patients. J Clin Endocrinol Metab. 2000;85:2247-52 pubmed
    ..In conclusion, the prevalence of macroprolactinoma shrinkage after CAB treatment at standard doses for 1-3 yr was higher in naive patients (92.3%) than in intolerant (42.1%), resistant (30.3%), and responsive patients (38.4%). Thus, C ..
  27. Leong K, Foy P, Swift A, Atkin S, Hadden D, MacFarlane I. CSF rhinorrhoea following treatment with dopamine agonists for massive invasive prolactinomas. Clin Endocrinol (Oxf). 2000;52:43-9 pubmed
    ..An additional strategy is the withdrawal of dopamine agonist to allow tumour re-growth to stop the leak. ..
  28. Verhelst J, Abs R, Maiter D, Van Den Bruel A, Vandeweghe M, Velkeniers B, et al. Cabergoline in the treatment of hyperprolactinemia: a study in 455 patients. J Clin Endocrinol Metab. 1999;84:2518-22 pubmed
    ..Once PRL secretion was adequately controlled, the dose of cabergoline could often be significantly decreased, which further reduced costs of therapy. ..
  29. Engin Ustun Y, Yılmaz S, Timur H, Ustun Y, Moraloglu O, Deveer R, et al. Comparison of bevacizumab and cabergoline in the treatment of ovarian hyperstimulation syndrome in a rat model. Gynecol Endocrinol. 2013;29:851-4 pubmed publisher
    ..05). This increase was not seen in the OHSS groups treated with either bevacizumab or cabergoline. We demonstrate in this study that bevacizumab can lower VEGF production and ovarian weight in rats treated with gonadotropins. ..
  30. Vilar L, Naves L, Casulari L, Azevedo M, Albuquerque J, Serfaty F, et al. Management of prolactinomas in Brazil: an electronic survey. Pituitary. 2010;13:199-206 pubmed publisher
  31. Heras M, Iglesias P, Fernández Reyes M, Sanchez R, Jiménez M, Muñoz H, et al. Nephrotic-range proteinuria in a patient with a giant prolactinoma. Am J Kidney Dis. 2008;51:1025-8 pubmed publisher
    ..We discuss the possible pathogenic mechanisms of proteinuria that may correspond to PRL level in urine (prolactinuria) or another tumor-related protein. ..
  32. Davie M. Pathological gambling associated with cabergoline therapy in a patient with a pituitary prolactinoma. J Neuropsychiatry Clin Neurosci. 2007;19:473-4 pubmed
  33. Rasmussen V, Poulsen S, Dupont E, Østergaard K, Safikhany G, Egeblad H. Heart valve disease associated with treatment with ergot-derived dopamine agonists: a clinical and echocardiographic study of patients with Parkinson's disease. J Intern Med. 2008;263:90-8 pubmed
    ..Clinical screening for valve disease was inadequate and it seems advisable to offer EDDA patients control with echocardiography. ..
  34. Sayyah Melli M, Tehrani Gadim S, Dastranj Tabrizi A, Gatrehsamani F, Morteza G, Ouladesahebmadarek E, et al. Comparison of the effect of gonadotropin-releasing hormone agonist and dopamine receptor agonist on uterine myoma growth. Histologic, sonographic, and intra-operative changes. Saudi Med J. 2009;30:1024-33 pubmed
  35. Ouattara B, Hoyer D, Gregoire L, Morissette M, Gasparini F, Gomez Mancilla B, et al. Changes of AMPA receptors in MPTP monkeys with levodopa-induced dyskinesias. Neuroscience. 2010;167:1160-7 pubmed publisher
    ..In conclusion, the elevated values of AMPA receptors in dyskinetic monkeys (and their prevention through treatments) were only observed in subregions of the striatum. ..
  36. Soares S, Gomez R, Simon C, Garcia Velasco J, Pellicer A. Targeting the vascular endothelial growth factor system to prevent ovarian hyperstimulation syndrome. Hum Reprod Update. 2008;14:321-33 pubmed publisher
    ..Ovarian hyperstimulation syndrome (OHSS) typically occurs when ovaries are primed with FSH/LH and subsequently exposed to hCG. The ultimate pathophysiological step underlying this clinical picture is increased vascular permeability (VP)...
  37. Markert A, Steffan N, Ploss K, Hellwig S, Steiner U, Drewke C, et al. Biosynthesis and accumulation of ergoline alkaloids in a mutualistic association between Ipomoea asarifolia (Convolvulaceae) and a clavicipitalean fungus. Plant Physiol. 2008;147:296-305 pubmed publisher
    ..The association between the fungus and the plant very likely is a symbiotum in which ergoline alkaloids play an essential role...
  38. Orer H, Gebber G, Barman S. Role of serotonergic input to the ventrolateral medulla in expression of the 10-Hz sympathetic nerve rhythm. Am J Physiol Regul Integr Comp Physiol. 2008;294:R1435-44 pubmed publisher
    ..These results support the view that serotonergic inputs to the VLM play an important role in expression of the 10-Hz rhythm in SND. ..
  39. Troxler T, Enz A, Hoyer D, Langenegger D, Neumann P, Pfäffli P, et al. Ergoline derivatives as highly potent and selective antagonists at the somatostatin sst 1 receptor. Bioorg Med Chem Lett. 2008;18:979-82 pubmed
    ..In functional assays, these ergolines act as antagonists at human recombinant sst(1) receptors...
  40. Ratner L, Gonzalez B, Ahtiainen P, Di Giorgio N, Poutanen M, Calandra R, et al. Short-term pharmacological suppression of the hyperprolactinemia of infertile hCG-overproducing female mice persistently restores their fertility. Endocrinology. 2012;153:5980-92 pubmed publisher
  41. Kvernmo T, Hartter S, Burger E. A review of the receptor-binding and pharmacokinetic properties of dopamine agonists. Clin Ther. 2006;28:1065-1078 pubmed publisher
    ..Fibrosis (including VHD) seemed to be a class effect of the ergot-derived DAs. Each of the DAs except pramipexole has the potential to interact with other drugs via the CYP enzyme system. ..
  42. Riahi G, Morissette M, Parent M, Di Paolo T. Brain 5-HT(2A) receptors in MPTP monkeys and levodopa-induced dyskinesias. Eur J Neurosci. 2011;33:1823-31 pubmed publisher
    ..These results confirm the involvement of serotonergic pathways and the glutamate/serotonin interactions in LID. They also support targeting 5-HT(2A) receptors as a potential treatment for LID...
  43. Alonso Navarro H, Ruiz Ezquerro J, Adeva Bartolomé T, Jimenez Jimenez F. [Association between amytrophic lateral sclerosis and Parkinson's disease]. Med Clin (Barc). 2007;129:478-9 pubmed
  44. Goetz C, Poewe W, Rascol O, Sampaio C. Evidence-based medical review update: pharmacological and surgical treatments of Parkinson's disease: 2001 to 2004. Mov Disord. 2005;20:523-39 pubmed
    ..We consider a 3-year period a reasonable time frame for published updates and are working to establish a Web-based mechanism to update the report in an ongoing manner. ..
  45. Burley S, Lam V, Lakner F, Bergdahl B, Parker M. New route to the ergoline skeleton via cyclization of 4-unsubstituted indoles. Org Lett. 2013;15:2598-600 pubmed publisher
    ..Key steps include Negishi coupling of a three-carbon chain to a bromonicotinate ester, Fischer indole synthesis to facilitate incorporation of substituents via phenylhydrazines, and Pd-catalyzed cyclization to form the ergoline C ring. ..
  46. Martinkova J, Trejbalova L, Sasikova M, Benetin J, Valkovic P. Impulse control disorders associated with dopaminergic medication in patients with pituitary adenomas. Clin Neuropharmacol. 2011;34:179-81 pubmed publisher
    ..This study demonstrates the importance of systematic screening for ICDs in patients taking dopaminergic medication regardless of their primary condition. ..
  47. Kanzato N, Nishihira T, Murao H, Takara H. [Case of juvenile parkinsonism in pregnancy]. Rinsho Shinkeigaku. 2006;46:400-3 pubmed
    ..Motor disability may worsen during pregnancy, and appropriate childcare support should be prepared. ..
  48. Vallette S, Serri K, Serri O. Cabergoline therapy for prolactinomas: is valvular heart disease a real safety concern?. Expert Rev Cardiovasc Ther. 2010;8:49-54 pubmed publisher
    ..The clinical significance of the present findings has yet to be confirmed by future larger prospective studies with rigorous echocardiographic protocols and prolonged duration of follow-up...
  49. Sandret L, Maison P, Chanson P. Place of cabergoline in acromegaly: a meta-analysis. J Clin Endocrinol Metab. 2011;96:1327-35 pubmed publisher
    ..Cabergoline is widely considered to be poorly effective in acromegaly...
  50. Colao A, Martino E, Cappabianca P, Cozzi R, Scanarini M, Ghigo E. First-line therapy of acromegaly: a statement of the A.L.I.C.E. (Acromegaly primary medical treatment Learning and Improvement with Continuous Medical Education) Study Group. J Endocrinol Invest. 2006;29:1017-20 pubmed
  51. Delgrange E, Gustin T. Cystic macroprolactinoma: primary medical treatment?. Intern Med J. 2005;35:687; author reply 688 pubmed
  52. England G, Freeman S, Russo M. Treatment of spontaneous pyometra in 22 bitches with a combination of cabergoline and cloprostenol. Vet Rec. 2007;160:293-6 pubmed
    ..Eleven of the 21 successfully treated bitches were mated at the next oestrus, and seven became pregnant; their litters were smaller than the published breed averages. In four of the bitches the pyometra recurred after the next oestrus. ..
  53. Cheng J, Coyle C, Panaccione D, O Connor S. A role for Old Yellow Enzyme in ergot alkaloid biosynthesis. J Am Chem Soc. 2010;132:1776-7 pubmed publisher
    ..This reduction, which yields dihydrochanoclavine aldehyde, facilitates an intramolecular reaction between a secondary amine and aldehyde to form the D ring of the ergot alkaloid structural framework. ..