Dopamine receptor agonists for treating prolactinomas
- 1 June 2002
- journal article
- review article
- Published by Informa Healthcare in Expert Opinion on Investigational Drugs
- Vol. 11 (6), 787-800
- https://doi.org/10.1517/13543784.11.6.787
Abstract
Prolactinomas are the most common hormone-secreting pituitary tumours and cause infertility and gonadal and sexual dysfunction in both sexes. The approach to prolactinomas has changed in the last 25 years thanks to the availability of dopaminergic drugs characterised by a potent prolactin-inhibitory effect, a tumour shrinking effect associated with a satisfactory tolerability. In more recent years, cabergoline (1-[(6-allelylergolin-8β-yl)carbonyl]-1-[3-(dimethylamino) propyl]-3-ethyl-urea), an ergoline derivative with potent, selective and long-lasting inhibitory activity on prolactin release, has been used to suppress prolactin secretion in women with hyperprolactinaemia. Cabergoline was shown to be significantly more effective than bromocriptine in inducing a complete biochemical response and clinical efficacy and was better tolerated than bromocriptine in the majority of patients. Notable tumour shrinkage until tumour disappearance was observed during cabergoline treatment in most patients with macroprolactinoma and it was also proven effective in patients resistant to or with a poor response to bromocriptine. In view of the limited data on cabergoline-associated pregnancies and the long half-life of the drug, it is currently recommended that women hoping to become pregnant, once ovulatory cycles have been established, should discontinue cabergoline therapy 1 month before they intend to conceive. However, no data concerning negative effects on pregnancy or offspring have been reported. The great efficacy of this compound together with its excellent tolerability makes this drug the current treatment of choice for the majority of patients with hyperprolactinaemic disorders.Keywords
This publication has 92 references indexed in Scilit:
- In vivo Effect of Cabergoline, a Dopamine Agonist, on Estrogen-Induced Rat Pituitary Tumors.Endocrine Journal, 1995
- Recurrent myocardial infarction in a postpartum patient receiving bromocriptineClinical Cardiology, 1992
- Mechanisms of signal transduction at the dopamine D2 receptorTrends in Pharmacological Sciences, 1989
- Hormonal effects of CV 205–502, a novel octahydrobenzo [g] quinoline with potent dopamine agonist propertiesLife Sciences, 1988
- Increase in Bone Mass after Treatment of Hyperprolactinemic AmenorrheaThe New England Journal of Medicine, 1986
- Resolution and absolute configuration of the potent dopamine agonist N,N-diethyl-N'-[(3.alpha.,4a.alpha.,10a.beta.)-1,2,3,4,4a,5,10,10a-octahydro-6-hydroxy-1-propyl-3-benzo[g]quinolinyl]sulfamideJournal of Medicinal Chemistry, 1985
- Low Doses of Dopamine Agonists in the Long-Term Treatment of MacroprolactinomasThe New England Journal of Medicine, 1985
- Microadenomas of the Pituitary and Abnormal Sellar Tomograms in an Unselected Autopsy SeriesThe New England Journal of Medicine, 1981
- Decreased Bone Density in Hyperprolactinemic WomenThe New England Journal of Medicine, 1980
- Side Effects of BromocriptineThe New England Journal of Medicine, 1980