Antigonadotropin

Short description: Drug

Antigonadotropin

Drug class
Class identifiers
Use| For the treatment of androgen and estrogen-related medical conditions.
ATC code| G03XA
Biological target| GnRH receptor, gonadotropin receptors (FSHR, LHR), sex steroid receptors (AR, ER, PR)

An antigonadotropin is a drug which suppresses the activity and/or downstream effects of one or both of the gonadotropins, follicle-stimulating hormone (FSH) and luteinizing hormone (LH). This results in an inhibition of the hypothalamic-pituitary-gonadal (HPG) axis, and thus a decrease in the levels of the androgen, estrogen, and progestogen sex steroids in the body. Antigonadotropins also inhibit ovulation in women and spermatogenesis in men. They are used for a variety of purposes, including for the hormonal birth control, treatment of hormonally-sensitive cancers, to delay precocious puberty and puberty in transgender youth, as a form of chemical castration to reduce the sex drives of individuals with hypersexuality or pedophilia, and to treat estrogen-associated conditions in women such as menorrhagia and endometriosis, among others. High-dose antigonadotropin therapy has been referred to as medical castration.

The best-known and widely used antigonadotropins are the gonadotropin-releasing hormone (GnRH) analogues (both agonists and antagonists).[1] However, many other drugs have antigonadotropic properties as well, including compounds acting on sex steroid hormone receptors such as progestogens, androgens, and estrogens (due to negative feedback on the HPG axis),[2][3] as well as steroid synthesis inhibitors such as danazol and gestrinone.[4][5] Since progestins have relatively little effect on sexual differentiation compared to the other sex steroids, potent ones such as cyproterone acetate, medroxyprogesterone acetate, and chlormadinone acetate are often used at high doses specifically for their antigonadotropic effects.[2][6][7]

Danazol, gestrinone, and paroxypropione have all been classified specifically as antigonadotropins.[8]

Prolactin has antigonadotropic effects and hyperprolactinemia can cause hypogonadism.[9][10]

Opioids have antigonadotropic effects and can reduce luteinizing hormone and testosterone levels in men.[11][12][13] A 2015 systematic review and meta-analysis found that opioid therapy decreased testosterone levels in men by about 165 ng/dL (5.7 nmol/L) on average, which was a reduction in testosterone level of almost 50%.[11] In contrast to opioids, opioid antagonists, like naltrexone, have progonadotropic effects, and can increase luteinizing hormone and testosterone levels.[14]

## See also

* Progonadotropin
* CYP17A1 inhibitor
* Steroidogenesis inhibitor
* Antiandrogen
* Antiestrogen
* Antiprogestogen
* Neurosteroidogenesis inhibitor

## References

1. ↑ Jonathan S. Berek; Emil Novak (2007). Berek and Novak's Gynecology. Lippincott Williams & Wilkins. p. 212. ISBN 978-0-7817-6805-4. https://books.google.com/books?id=P3erI0J8tEQC&pg=PA212. Retrieved 29 May 2012.
2. ↑ 2.0 2.1 "Pharmacodynamics of oestrogens and progestogens". Cephalalgia: An International Journal of Headache 20 (3): 200–7. April 2000. doi:10.1046/j.1468-2982.2000.00042.x. PMID 10997774.
3. ↑ Gooren L (October 1989). "Androgens and estrogens in their negative feedback action in the hypothalamo-pituitary-testis axis: site of action and evidence of their interaction". Journal of Steroid Biochemistry 33 (4B): 757–61. doi:10.1016/0022-4731(89)90488-3. PMID 2689784.
4. ↑ Jonathan S. Berek; Emil Novak (2007). Berek and Novak's Gynecology. Lippincott Williams & Wilkins. p. 1167. ISBN 978-0-7817-6805-4. https://books.google.com/books?id=P3erI0J8tEQC&pg=PA1167. Retrieved 29 May 2012.
5. ↑ "Heterosteroids and drug research". Progress in Medicinal Chemistry 28: 233–300. 1991. doi:10.1016/s0079-6468(08)70366-7. ISBN 9780444812759. PMID 1843548.
6. ↑ Bercovici JP (September 1987). "[Progestational contraception]" (in fr). La Revue du Praticien 37 (38): 2277–8, 2281–4. PMID 3659794.
7. ↑ "[The antigonadrotropic activity of chlormadinone acetate in reproductive women]" (in fr). Gynécologie, Obstétrique & Fertilité 33 (1–2): 29–34. 2005. doi:10.1016/j.gyobfe.2004.12.002. PMID 15752663.
8. ↑ George W.A. Milne (8 May 2018). Drugs: Synonyms and Properties: Synonyms and Properties. Taylor & Francis. pp. 674–. ISBN 978-1-351-78989-9. https://books.google.com/books?id=xUlaDwAAQBAJ&pg=PT674.
9. ↑ "Prolactin - a pleiotropic factor in health and disease". Nat Rev Endocrinol 15 (6): 356–365. June 2019. doi:10.1038/s41574-019-0194-6. PMID 30899100.
10. ↑ "Prolactin Biology and Laboratory Measurement: An Update on Physiology and Current Analytical Issues". Clin Biochem Rev 39 (1): 3–16. February 2018. PMID 30072818.
11. ↑ 11.0 11.1 "Testosterone suppression in opioid users: a systematic review and meta-analysis". Drug Alcohol Depend 149: 1–9. April 2015. doi:10.1016/j.drugalcdep.2015.01.038. PMID 25702934.
12. ↑ "Testosterone deficiency in non-cancer opioid-treated patients". J Endocrinol Invest 41 (12): 1377–1388. December 2018. doi:10.1007/s40618-018-0964-3. PMID 30343356.
13. ↑ "Opioid-induced androgen deficiency (OPIAD)". Pain Physician 15 (3 Suppl): ES145–56. July 2012. PMID 22786453.
14. ↑ "Effect of opioid antagonists on sex hormone secretion". J Endocrinol Invest 35 (2): 227–30. February 2012. doi:10.3275/8181. PMID 22183092.

## External links

* v
* t
* e

GnRH and gonadotropins

GnRH modulators
(incl. analogues)|

| Agonists|

* Peptide: Azagly-nafarelin
* Buserelin
* Deslorelin
* Fertirelin
* Gonadorelin
* Goserelin
* Histrelin
* Lecirelin
* Leuprorelin (leuprolide)
* Nafarelin
* Peforelin
* Triptorelin

|

Antagonists|

* Peptide: Abarelix
* Cetrorelix
* Degarelix
* Ganirelix

* Non-peptide: Elagolix
* Linzagolix†
* Relugolix†

Gonadotropins|

| Preparations|

* Follicle-stimulating hormone
* Human chorionic gonadotropin
* Luteinizing hormone
* Menotropin
* Urofollitropin

|

Others
(indirect)|

| Progonadotropins|

* Sex steroid antagonists (via disinhibition of the HPG axis): Antiandrogens (e.g., flutamide, bicalutamide, enzalutamide)
* Antiestrogens/SERMs (e.g., tamoxifen, Chemistry:Clomifene

|

Antigonadotropins|

* Sex steroid agonists (via negative feedback on the HPG axis): Androgens/anabolic steroids (e.g., testosterone, nandrolone esters, oxandrolone)
* D2 receptor antagonists (prolactin releasers) (incl., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, sulpiride)
* Estrogens (incl., bifluranol, estradiol, estradiol esters, ethinylestradiol, diethylstilbestrol, paroxypropione)
* Progestogen|Progestogens (incl. progestins, e.g., Chemistry:Chlormadinone acetate

* #WHO-EM
* ‡Withdrawn from market
* Clinical trials:
* †Phase III
* §Never to phase III

See also
GnRH and gonadotropin receptor modulators
Androgens and antiandrogens
Estrogens and antiestrogens
Progestogens and antiprogestogens

0.00

(0 votes)

Original source: https://en.wikipedia.org/wiki/Antigonadotropin. Read more

|

Retrieved from "https://handwiki.org/wiki/index.php?title=Chemistry:Antigonadotropin&oldid=875551"
*[v]: View this template
*[t]: Discuss this template
*[e]: Edit this template
*[GnRH]: gonadotropin-releasing hormone
*[HPG]: hypothalamic–pituitary–gonadal
*[SERMs]: Selective estrogen receptor modulators