Cabergoline in the Treatment of Hyperprolactinemia: A Study in 455 Patients

Verhelst, Johan; Abs, Roger; Maiter, Dominique; Bruel, Annick Van den; Vandeweghe, Mark; Velkeniers, Brigitte; Mockel, Jean; Lamberigts, G.; Pétrossians, Patrick; Coremans, Peter; Mahler, C.; Stevenaert, Achille; Verlooy, Jan; Raftopoulos, Christian; Beckers, Albert

doi:10.1097/00006254-200001000-00018

Cited by 52 publications

(83 citation statements)

References 6 publications

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“…Further evidence of the inexistence of the detrimental effects of DRD2-A for eutopic endometrial angiogenesis is provided by the fact that women receiving high doses of Cb2 become pregnant uneventfully (Verhelst et al 1999). Given its different mechanism of action, DRD2-As are unlikely to interfere with the menstrual cycle and thus possesses an important advantage over GNRH agonists and aromatase inhibitors, which induce osteoporosis and hot flushes as a result of hypoestrogenic milieu (Gregoriou et al 1997, Walch et al 2009).…”

Section: Discussionmentioning

confidence: 99%

The effects of ergot and non-ergot-derived dopamine agonists in an experimental mouse model of endometriosis

Delgado-Rosas¹,

Gómez²,

Ferrero³

et al. 2011

Reproduction

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Implantation of a retrogradely shed endometrium during menstruation requires an adequate blood supply, which allows the growth of endometriotic lesions. This suggests that the development of endometriosis can be impaired by inhibiting angiogenesis. The growth of endometriotic foci is impaired by commercial oncological antiangiogenic drugs used to block vascular endothelial growth factor (VEGF) signaling. The dopamine agonist cabergoline (Cb2) inhibits the growth of established endometriosis lesions by exerting antiangiogenic effects through VEGFR2 inactivation. However, the use of ergot-derived Cb2 is associated with an increased incidence of cardiac valve regurgitation. To evaluate the potential usage of non-ergot-derived dopamine agonists for the treatment of human endometriosis, we compared the efficacy of quinagolide with that of Cb2 in preventing angiogenesis and vascularization in a heterologous mouse model of endometriosis. Nude mice whose peritoneum had been implanted with eutopic human endometrial fragments were treated with vehicle, 50 mg/kg per day oral Cb2, or 50 or 200 mg/kg per day quinagolide during a 14-day period. At the end of the treatment period, the implants were excised in order to assess lesion size, cell proliferation, degree of vascularization, and angiogenic gene expression. Neoangiogenesis was inhibited and the size of active endometriotic lesions, cellular proliferation index, and angiogenic gene expression were significantly reduced by both dopamine agonists when compared with the placebo. Given that Cb2 and quinagolide were equally effective in inhibiting angiogenesis and reducing lesion size, these experiments provide the rationale for pilot studies to explore the use of non-ergot-derived dopamine agonists for the treatment of endometriosis in humans.

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Section: Discussionmentioning

confidence: 99%

The effects of ergot and non-ergot-derived dopamine agonists in an experimental mouse model of endometriosis

Delgado-Rosas¹,

Gómez²,

Ferrero³

et al. 2011

Reproduction

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“…agonists, specially cabergoline, may be related to dopamine-receptor expression in the adenomatous tissue (7)(8)(9)(10), although tumor aggressiveness may be related to AIP mutations in young patients (12,13). Mutations on AIP may be involved in cell proliferation in several ways: multiple protein-protein interactions may lead in particular to AHR stabilization in the cytoplasm, thereby enhancing its ligand-induced nuclear translocation, and modulation of specific phosphodiesterases in some pituitary cells (16,20,21).…”

Section: Discussionmentioning

confidence: 99%

“…Clinical factors associated with tumor aggressiveness and resistance to dopamine agonists include young age at onset, male gender, large tumor size or cavernous sinus invasion at diagnosis (7)(8)(9)(10).…”

Section: Introductionmentioning

confidence: 99%

Aggressive prolactinoma in a child related to germline mutation in the ARYL hydrocarbon receptor interacting protein (AIP) gene

Naves

Jaffrain-Rea

Vencio

et al. 2010

Arq Bras Endocrinol Metab

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SUMMARYThe objective of this study was to describe a familial screening for AIP mutations in the context of aggressive prolactinoma in childhood. A 12-year-old boy, presented headaches and bilateral hemianopsia. He had adequate height and weight for his age (50 th percentile), Tanner stage G1 P1. His bone age was 10 years. Prolactin was 10.560 ng/mL (3-25), FSH and LH were undetectable, IGF-1, TSH, Free T4, ACTH, and cortisol were within normal ranges. MRI showed a pituitary macroadenoma, 5.3 X 4.0 X 3.5 cm with compression of the optic chiasm, bilateral cavernous sinus invasion, encasement of carotids, and extension to clivus. Surgical debulking was performed. Resistance to cabergoline was characterized and he was submitted to two surgeries and radiotherapy. Immunohistochemical evaluation included prolactin, ACTH, GH, FSH, LH,AIP, c-erb B2, Ki-67, and p53. Genomic DNA was isolated from the index case and 48 relatives, PCR and sequencing were performed. A germline A195V mutation in AIP was identified in the index case and in five asymptomatic relatives. Germline mutations in the AIP gene may be involved in the predisposition to pituitary adenoma formation, as cause or co-factor in pathogenesis of aggressive tumors in young patients. Arq Bras Endocrinol Metab. 2010;54(8):761-7 SUMÁRIOO objetivo deste estudo foi descrever o rastreamento familiar para mutações AIP em paciente portador de prolactinoma agressivo e resistente na infância. Um menino de 12 anos foi avaliado com queixa de cefaleia e hemianopsia bitemporal. Apresentava peso e altura adequados para a idade (percentil 50), estádio puberal Tanner G1 P1 e idade óssea de 10 anos. Prolactina 10.560 ng/mL (3-25), FSH e LH indetectáveis, IGF-1, TSH, T4 livre, ACTH, e cortisol normais. A ressonância magnética de sela evidenciou macroadenoma hipofisário, 53 X 40 X 35 mm com compressão de quiasma ótico, invasão de seios cavernosos, envolvimento de carótidas internas e extensão para o clivus. Foi realizada descompressão cirúrgica por via transesfenoidal e caracterizada resistência a doses máximas de cabergolina, sendo o paciente operado por mais duas vezes e submetido à radioterapia. Realizou-se imuno-histoquímica para prolactina, ACTH, GH, FSH, LH, AIP, c-erb B2, Ki-67 e p53. O DNA genômico foi extraído do caso índice e de 48 familiares, e PCR e sequenciamento. Uma mutação A195V na AIP foi detectada no paciente e em cinco parentes assintomáticos. As mutações no gene da AIP podem estar envolvidas na predisposição à formação de adenomas, como causa ou cofator na patogênese de tumores agressivos em jovens. Arq Bras Endocrinol Metab. 2010;54(8):761-7

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“…A média da dose de cabergolina foi 1,10 mg/semana, com variação de 0,5 a 1,75 mg/semana. Esta média foi semelhante às utilizadas em estudos sobre o uso de cabergolina em macroprolactinomas 22,23 . Os resultados relativos aos efeitos adversos com os agonistas dopaminérgicos confirmam os da literatura que descrevem menos efeitos colaterais com a cabergolina 24 .…”

Section: Discussionunclassified

Aspectos clínicos e terapêuticos de prolactinomas em homens

Braucks

Naliato

Tabet

et al. 2003

Arq. Neuro-Psiquiatr.

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RESUMO -Em homens, macroprolactinomas predominam em relação aos microprolactinomas e têm maior invasividade que nas mulheres. O tratamento clínico é a primeira opção tanto em macro como em microadenomas, independente do sexo. Comparamos apresentação clínica, níveis de prolactina, invasividade neurorradiológica e resposta da prolactinemia em 42 homens com prolactinomas, 23 com terapia clínica (grupo 1) e 19 que também utilizaram tratamento cirúrgico e/ou radioterápico (grupo 2). Os dados obtidos foram submetidos a análise estatística utilizando-se os testes de qui-quadrado ou exato de Fisher para comparações de proporções. Para comparar médias foi aplicado o teste t de Student ou, na ausência de distribuição normal ou com número pequeno de eventos, o não paramétrico de Mann-Whitney. O nível de significância adotado foi de 5% (p<0,05). Os grupos foram similares para idade (p=0,23), período entre primeiro sintoma e diagnóstico (p=0,82), níveis de prolactina pré tratamento (p=0,41) e proporção de macroadenomas invasivos (p=0,096). Ocorreu percentual significativamente maior de cefaléia (p=0,009), deficit visual (p=0,025), tempo de terapia (p=0,007) e período de acompanhamento (p=0,0005) no grupo 2. Variações dos níveis de prolactina antes e após terapia não apresentaram diferença significativa nos grupos (p=0,49), nem o percentual de normalização da prolactina após tratamento (p=0,20). Concluímos, enfatizando a importância do diagnóstico precoce do prolactinoma em homens, tendo em vista a morbidade demonstrada, e reforçamos a necessidade do uso do agonista dopaminérgico como opção terapêutica inicial independente do tamanho do adenoma. PALAVRAS-CHAVE: prolactinoma, bromocriptina, agonistas de dopamina, glândula pituitária, masculino. Clinical and therapeutic aspects of prolactinoma in menABSTRACT -Macroprolactinomas predominate in males in comparison to microprolactinomas, with greater trend to invasiveness than in females. The clinical treatment has been the first option to prolactinomas, in both macro and microadenomas, irrespective the sex. We compared clinical presentation, prolactin levels, neuroradiologic invasiveness and prolactinemia response of 23 men with prolactinomas subjected to clinical therapy (group 1) with 19 who went also through surgical and/or radiotherapic treatment (group 2). The statistical analysis was done by the tests of chi-square or exact of Fisher, in order to compare proportions, and by t of Student or Mann-Whitney, in order to compare means. The level of significance adopted was 5% (p<0.05). The two groups were similar regarding age (p=0.23), period between start of the first symptom and diagnosis (p=0.82), prolactin levels before treatment (p=0.41) and invasive macroadenomas proportion (p=0.096). There was significantly greater percentage of headache (p=0.009) and visual deficit (p=0.025) in group 2, as well as the drug usage (p=0.007) and observation (p=0.0005) periods were superior in this group. The variations of prolactin levels before and after therapy (p=0.49) as well as the per...

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Cabergoline in the Treatment of Hyperprolactinemia: A Study in 455 Patients

Cited by 52 publications

References 6 publications

The effects of ergot and non-ergot-derived dopamine agonists in an experimental mouse model of endometriosis

The effects of ergot and non-ergot-derived dopamine agonists in an experimental mouse model of endometriosis

Aggressive prolactinoma in a child related to germline mutation in the ARYL hydrocarbon receptor interacting protein (AIP) gene

Aspectos clínicos e terapêuticos de prolactinomas em homens

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