Prolactin modulator

Drug class

Prolactin modulator

Drug class

Bromocriptine, a D2 receptor agonist, and the most commonly used prolactin inhibitor

Class identifiers
Synonyms| Indirect prolactin modulator; Prolactin inhibitor; Prolactin releaser
Use| Hyperprolactinemia; Hypoprolactinemia
Biological target| D2 receptor (mainly)
Legal status
In Wikidata

A prolactin modulator is a drug which affects the hypothalamic–pituitary–prolactin axis (HPP axis) by modulating the secretion of the pituitary hormone prolactin from the anterior pituitary gland. Prolactin inhibitors suppress and prolactin releasers induce the secretion of prolactin, respectively.[1][2]

## Prolactin inhibitors

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Prolactin inhibitors are mainly used to treat hyperprolactinemia (high prolactin levels).[1] 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.[1] 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.[3] Other dopamine agonists and dopaminergic agents, for instance levodopa (L-DOPA), can also inhibit prolactin secretion.[4] 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.

## Prolactin releasers

[edit]

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.[2] 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.[5][6][7][8]

## References

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1. ^ a b c Thomas L. Lemke; David A. Williams (24 January 2012). Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. pp. 432–. ISBN 978-1-60913-345-0.
2. ^ a b University of Kansas School of Nursing Karen Wambach (15 August 2014). Breastfeeding and Human Lactation. Jones & Bartlett Publishers. pp. 182–. ISBN 978-1-4496-9729-7.
3. ^ George W.A Milne (8 May 2018). Drugs: Synonyms and Properties: Synonyms and Properties. Taylor & Francis. pp. 1579–. ISBN 978-1-351-78989-9.
4. ^ Cacabelos R (March 2017). "Parkinson's Disease: From Pathogenesis to Pharmacogenomics". Int J Mol Sci. 18 (3): 551. doi:10.3390/ijms18030551. PMC 5372567. PMID 28273839.
5. ^ Madhusoodanan S, Parida S, Jimenez C (2010). "Hyperprolactinemia associated with psychotropics--a review". Hum Psychopharmacol. 25 (4): 281–97\. doi:10.1002/hup.1116. PMID 20521318. S2CID 6851723.
6. ^ Torre DL, Falorni A (October 2007). "Pharmacological causes of hyperprolactinemia". Ther Clin Risk Manag. 3 (5): 929–51\. PMC 2376090. PMID 18473017.
7. ^ Amsterdam JD, Garcia-España F, Goodman D, Hooper M, Hornig-Rohan M (November 1997). "Breast enlargement during chronic antidepressant therapy". J Affect Disord. 46 (2): 151–6\. doi:10.1016/s0165-0327(97)00086-4. PMID 9479619.
8. ^ Coker F, Taylor D (July 2010). "Antidepressant-induced hyperprolactinaemia: incidence, mechanisms and management". CNS Drugs. 24 (7): 563–74\. doi:10.2165/11533140-000000000-00000. PMID 20527996. S2CID 20016957.

## External links

[edit]

* Media related to Prolactin modulators at Wikimedia Commons

* v
* t
* e

Prolactin inhibitors and anti-inflammatory products for vaginal administration (G02CB–G02CC)

Prolactin inhibitors|

* Bromocriptine
* Cabergoline
* Ergoloid
* Lisuride
* Metergoline
* Pergolide
* Quinagolide
* Terguride

Anti-inflammatory products
for vaginal administration|

* Benzydamine
* Ibuprofen
* Flunoxaprofen
* Naproxen

* v
* t
* e

Prolactin receptor modulators

Agonists|

* Growth hormone
* Human placental lactogen
* Placental growth hormone (growth hormone variant)
* Prolactin
* S179D-hPRL
* Somatotropin

Antagonists|

* Δ1–9-G129R-hPRL
* Δ1–14-G129R-hPRL
* G120K-hGH
* G129R-hPRL

Indirect
modulators|

| Inhibitors|

* D2 receptor agonists (e.g., bromocriptine, cabergoline, lergotrile, lisuride, metergoline, pergolide, quinagolide, terguride)
* Indirect dopaminergic agents (e.g., levodopa)

|

Releasers|

* D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone)
* Indirect antidopaminergic agents (e.g., reserpine)
* Estrogens (e.g., estradiol)
* Progestogens (e.g., progesterone)
* Thyrotropin-releasing hormone and analogues (e.g., protirelin, taltirelin)
* Vasoactive intestinal peptide

* v
* t
* e

Breastfeeding

Anatomy, physiology
and immunology|

* Anti inflammatory agents in breast milk
* Areola
* Areolar gland (gland of Montgomery)
* Breast
* Breast anatomy
* Breast crawl
* Breast milk
* Breastfeeding and medications
* Dysphoric milk ejection reflex
* Frenulum of tongue
* Galactose
* Human milk oligosaccharide
* Hypothalamic–pituitary–prolactin axis
* Latching on
* Lactation suppression
* Lactiferous duct
* Lactose
* Milk
* Overactive let-down
* Oxytocin
* Passive immunity
* Prolactin
* Prolactin modulator
* Colostrum
* Lactation
* Nipple
* Mammary gland
* Mammary alveoli
* Mammary lobule

Disorders
and difficulties|

* Blocked milk duct
* Breastfeeding difficulties
* Breast engorgement
* Low milk supply
* Fissure of the nipple
* Inverted nipple
* Cracked nipple
* Mastitis
* Nipple bleb
* Nipple vasospasm
* Neonatal jaundice
* Nipple pain in breastfeeding
* Breastfeeding infertility
* Breastfeeding and HIV
* Prolactinoma
* Breastfeeding and mental health

Culture and
support|

* Breastfeeding advocacy
* Breastfeeding in art
* Breastfeeding in Islam
* Breastfeeding in public
* Breastfeeding in the United States
* Breastfeeding organizations
* Breastfeeding promotion
* Child's Right to Nurse Act
* Diana West (lactation consultant)
* History and culture of breastfeeding
* Human-animal breastfeeding
* Human milk bank
* Human milk banking in North America
* International Breastfeeding Symbol
* Jack Newman (doctor)
* International Breast Milk Project
* La Leche League
* Lactation room
* Lactivism
* Mothers' rights
* Pat Shelly
* Amy Spangler
* Mary Rose Tully
* World Breastfeeding Week

Roles|

* Doula
* Midwifery
* Lactation consultant
* Lactation counselor
* List of breastfeeding activists
* Wet nurse

Equipment used
with breastfeeding|

* Breast pump
* Nipple shield
* Nursing bra
* Nursing chair
* Supplemental nursing system

Other topics|

* Baby-led weaning
* Weaning
* Extended breastfeeding
* Nipple confusion
* Breastfeeding and fertility
* Breastfeeding and medications
* Breastfeeding contraindications
* Breastfeeding and mental health

*[GnRH]: gonadotropin-releasing hormone
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