Prolactin modulator#Prolactin inhibitors

Prolactin inhibitors are mainly used to treat hyperprolactinemia (high prolactin levels). Agonists of the dopamine D₂ receptor such as bromocriptine and cabergoline are able to strongly suppress pituitary prolactin secretion and thereby decrease circulating prolactin levels, and so are most commonly used as prolactin inhibitors. D₂ receptor agonists that are described as prolactin inhibitors include the approved medications bromocriptine, cabergoline, lisuride, metergoline, pergolide, quinagolide, and terguride and the never-marketed agent lergotrile.{{cite book|author=George W.A Milne|title=Drugs: Synonyms and Properties: Synonyms and Properties|url=https://books.google.com/books?id=xUlaDwAAQBAJ&pg=PT1579|date=8 May 2018|publisher=Taylor & Francis|isbn=978-1-351-78989-9|pages=1579–}} Other dopamine agonists and dopaminergic agents, for instance levodopa (L-DOPA), can also inhibit prolactin secretion.{{cite journal | vauthors = Cacabelos R | title = Parkinson's Disease: From Pathogenesis to Pharmacogenomics | journal = Int J Mol Sci | volume = 18 | issue = 3 | date = March 2017 | page = 551 | pmid = 28273839 | pmc = 5372567 | doi = 10.3390/ijms18030551 | url = | doi-access = free }} Antiestrogens such as aromatase inhibitors and GnRH analogues are also able to inhibit the secretion of prolactin, though not nearly as robustly as D₂ receptor agonists, and as such, they are not usually used as prolactin inhibitors.

Whereas D₂ receptor agonists suppress prolactin secretion, dopamine D₂ receptor antagonists like domperidone and metoclopramide have the opposite effect, strongly inducing the pituitary secretion of prolactin, and are sometimes used as prolactin releasers, for instance to correct hypoprolactinemia (low prolactin levels) in the treatment of lactation failure. When such drugs are used not for the purpose of inducing prolactin secretion, increased prolactin levels may be unwanted, and can result in various side effects including mammoplasia (breast enlargement), mastodynia (breast pain/tenderness), galactorrhea (inappropriate or excessive milk production/secretion), gynecomastia (breast development in males), hypogonadism (low sex hormone levels), amenorrhea (cessation of menstrual cycles), reversible infertility, and sexual dysfunction. Indirect dopaminergic agents such as levodopa can also suppress prolactin levels. Other prolactin releasers besides D₂ receptor antagonists include estrogens (e.g., estradiol), progestogens (e.g., progesterone), thyrotropin-releasing hormone and analogues (e.g., protirelin, taltirelin), and vasoactive intestinal peptide. Serotonergic agents such as serotonin precursors (e.g., tryptophan), serotonin reuptake inhibitors, serotonin releasing agents (e.g., fenfluramine, MDMA), monoamine oxidase inhibitors, and serotonin receptor agonists have also been associated with increases in prolactin levels.{{cite journal | vauthors = Madhusoodanan S, Parida S, Jimenez C | title = Hyperprolactinemia associated with psychotropics--a review | journal = Hum Psychopharmacol | volume = 25 | issue = 4 | pages = 281–97 | date = 2010 | pmid = 20521318 | doi = 10.1002/hup.1116 | s2cid = 6851723 | url = }}{{cite journal | vauthors = Torre DL, Falorni A | title = Pharmacological causes of hyperprolactinemia | journal = Ther Clin Risk Manag | volume = 3 | issue = 5 | pages = 929–51 | date = October 2007 | pmid = 18473017 | pmc = 2376090 | doi = | url = }}{{cite journal | vauthors = Amsterdam JD, Garcia-España F, Goodman D, Hooper M, Hornig-Rohan M | title = Breast enlargement during chronic antidepressant therapy | journal = J Affect Disord | volume = 46 | issue = 2 | pages = 151–6 | date = November 1997 | pmid = 9479619 | doi = 10.1016/s0165-0327(97)00086-4 | url = | doi-access = free }}{{cite journal | vauthors = Coker F, Taylor D | title = Antidepressant-induced hyperprolactinaemia: incidence, mechanisms and management | journal = CNS Drugs | volume = 24 | issue = 7 | pages = 563–74 | date = July 2010 | pmid = 20527996 | doi = 10.2165/11533140-000000000-00000 | s2cid = 20016957 | url = }}

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Category:Breastfeeding