Antigonadotropin

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Antigonadotropin
Drug class
Class identifiers
UseFor 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)
Legal status
In Wikidata

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.

Contents

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

Related Research Articles

<span class="mw-page-title-main">Antiandrogen</span> Class of pharmaceutical drugs

Antiandrogens, also known as androgen antagonists or testosterone blockers, are a class of drugs that prevent androgens like testosterone and dihydrotestosterone (DHT) from mediating their biological effects in the body. They act by blocking the androgen receptor (AR) and/or inhibiting or suppressing androgen production. They can be thought of as the functional opposites of AR agonists, for instance androgens and anabolic steroids (AAS) like testosterone, DHT, and nandrolone and selective androgen receptor modulators (SARMs) like enobosarm. Antiandrogens are one of three types of sex hormone antagonists, the others being antiestrogens and antiprogestogens.

<span class="mw-page-title-main">Progestogen (medication)</span> Medication producing effects similar to progesterone

A progestogen, also referred to as a progestagen, gestagen, or gestogen, is a type of medication which produces effects similar to those of the natural female sex hormone progesterone in the body. A progestin is a synthetic progestogen. Progestogens are used most commonly in hormonal birth control and menopausal hormone therapy. They can also be used in the treatment of gynecological conditions, to support fertility and pregnancy, to lower sex hormone levels for various purposes, and for other indications. Progestogens are used alone or in combination with estrogens. They are available in a wide variety of formulations and for use by many different routes of administration. Examples of progestogens include natural or bioidentical progesterone as well as progestins such as medroxyprogesterone acetate and norethisterone.

<span class="mw-page-title-main">Sex hormone</span> Type of steroid hormone

Sex hormones, also known as sex steroids, gonadocorticoids and gonadal steroids, are steroid hormones that interact with vertebrate steroid hormone receptors. The sex hormones include the androgens, estrogens, and progestogens. Their effects are mediated by slow genomic mechanisms through nuclear receptors as well as by fast nongenomic mechanisms through membrane-associated receptors and signaling cascades. The polypeptide hormones luteinizing hormone, follicle-stimulating hormone and gonadotropin-releasing hormone – each associated with the gonadotropin axis – are usually not regarded as sex hormones, although they play major sex-related roles.

<span class="mw-page-title-main">Sex hormone-binding globulin</span> Human glycoprotein that binds to androgens and estrogens

Sex hormone-binding globulin (SHBG) or sex steroid-binding globulin (SSBG) is a glycoprotein that binds to androgens and estrogens. When produced by the Sertoli cells in the seminiferous tubules of the testis, it is called androgen-binding protein (ABP).

<span class="mw-page-title-main">Danazol</span> Chemical compound

Danazol, sold as Danocrine and other brand names, is a medication used in the treatment of endometriosis, fibrocystic breast disease, hereditary angioedema and other conditions. It is taken by mouth.

<span class="mw-page-title-main">Gestrinone</span> Chemical compound

Gestrinone, sold under the brand names Dimetrose and Nemestran among others, is a medication which is used in the treatment of endometriosis. It has also been used to treat other conditions such as uterine fibroids and heavy menstrual bleeding and has been investigated as a method of birth control. Gestrinone is used alone and is not formulated in combination with other medications. It is taken by mouth or in through the vagina.

<span class="mw-page-title-main">Trestolone</span> Chemical compound

Trestolone, also known as 7α-methyl-19-nortestosterone (MENT), is an experimental androgen/anabolic steroid (AAS) and progestogen medication which has been under development for potential use as a form of hormonal birth control for men and in androgen replacement therapy for low testosterone levels in men but has never been marketed for medical use. It is given as an implant that is placed into fat. As trestolone acetate, an androgen ester and prodrug of trestolone, the medication can also be given by injection into muscle.

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<span class="mw-page-title-main">Chlormadinone acetate</span> Chemical compound

Chlormadinone acetate (CMA), sold under the brand names Belara, Gynorelle, Lutéran, and Prostal among others, is a progestin and antiandrogen medication which is used in birth control pills to prevent pregnancy, as a component of menopausal hormone therapy, in the treatment of gynecological disorders, and in the treatment of androgen-dependent conditions like enlarged prostate and prostate cancer in men and acne and hirsutism in women. It is available both at a low dose in combination with an estrogen in birth control pills and, in a few countries like France and Japan, at low, moderate, and high doses alone for various indications. It is taken by mouth.

<span class="mw-page-title-main">Medrogestone</span> Chemical compound

Medrogestone, sold under the brand name Colprone among others, is a progestin medication which has been used in menopausal hormone therapy and in the treatment of gynecological disorders. It is available both alone and in combination with an estrogen. It is taken by mouth.

<span class="mw-page-title-main">Allylestrenol</span> Chemical compound

Allylestrenol, sold under the brand names Gestanin and Turinal among others, is a progestin medication which is used to treat recurrent and threatened miscarriage and to prevent premature labor in pregnant women. However, except in the case of proven progesterone deficiency, its use for such purposes is no longer recommended. It is also used in Japan to treat benign prostatic hyperplasia (BPH) in men. The medication is used alone and is not formulated in combination with an estrogen. It is taken by mouth.

<span class="mw-page-title-main">Inborn errors of steroid metabolism</span> Medical condition

An inborn error of steroid metabolism is an inborn error of metabolism due to defects in steroid metabolism.

<span class="mw-page-title-main">Cyproterone acetate</span> Chemical compound

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<span class="mw-page-title-main">Edogestrone</span> Chemical compound

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<span class="mw-page-title-main">Steroidal antiandrogen</span> Class of compounds

A steroidal antiandrogen (SAA) is an antiandrogen with a steroidal chemical structure. They are typically antagonists of the androgen receptor (AR) and act both by blocking the effects of androgens like testosterone and dihydrotestosterone (DHT) and by suppressing gonadal androgen production. SAAs lower concentrations of testosterone through simulation of the negative feedback inhibition of the hypothalamus. SAAs are used in the treatment of androgen-dependent conditions in men and women, and are also used in veterinary medicine for the same purpose. They are the converse of nonsteroidal antiandrogens (NSAAs), which are antiandrogens that are not steroids and are structurally unrelated to testosterone.

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<span class="mw-page-title-main">Pharmacology of cyproterone acetate</span>

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References

  1. ↑ Jonathan S. Berek; Emil Novak (2007). Berek and Novak's Gynecology. Lippincott Williams & Wilkins. p. 212. ISBN   978-0-7817-6805-4 . Retrieved 29 May 2012.
  2. 1 2 de Lignières B, Silberstein S (April 2000). "Pharmacodynamics of oestrogens and progestogens". Cephalalgia: An International Journal of Headache. 20 (3): 200–7. doi:10.1046/j.1468-2982.2000.00042.x. PMID   10997774. S2CID   40392817.
  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 . Retrieved 29 May 2012.
  5. ↑ Singh H, Jindal DP, Yadav MR, Kumar M (1991). "Heterosteroids and drug research". Progress in Medicinal Chemistry. 28: 233–300. doi:10.1016/s0079-6468(08)70366-7. ISBN   9780444812759. PMID   1843548.
  6. ↑ Bercovici JP (September 1987). "[Progestational contraception]". La Revue du Praticien (in French). 37 (38): 2277–8, 2281–4. PMID   3659794.
  7. ↑ Chassard D, Schatz B (2005). "[The antigonadrotropic activity of chlormadinone acetate in reproductive women]". Gynécologie, Obstétrique & Fertilité (in French). 33 (1–2): 29–34. 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.
  9. ↑ Bernard V, Young J, Binart N (June 2019). "Prolactin - a pleiotropic factor in health and disease". Nat Rev Endocrinol. 15 (6): 356–365. doi:10.1038/s41574-019-0194-6. PMID   30899100. S2CID   84846294.
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  11. 1 2 Bawor M, Bami H, Dennis BB, Plater C, Worster A, Varenbut M, Daiter J, Marsh DC, Steiner M, Anglin R, Coote M, Pare G, Thabane L, Samaan Z (April 2015). "Testosterone suppression in opioid users: a systematic review and meta-analysis". Drug Alcohol Depend. 149: 1–9. doi: 10.1016/j.drugalcdep.2015.01.038 . PMID   25702934.
  12. ↑ Coluzzi F, Billeci D, Maggi M, Corona G (December 2018). "Testosterone deficiency in non-cancer opioid-treated patients". J Endocrinol Invest. 41 (12): 1377–1388. doi:10.1007/s40618-018-0964-3. PMC   6244554 . PMID   30343356.
  13. ↑ Smith HS, Elliott JA (July 2012). "Opioid-induced androgen deficiency (OPIAD)". Pain Physician. 15 (3 Suppl): ES145–56. PMID   22786453.
  14. ↑ Tenhola H, Sinclair D, Alho H, Lahti T (February 2012). "Effect of opioid antagonists on sex hormone secretion". J Endocrinol Invest. 35 (2): 227–30. doi:10.3275/8181. PMID   22183092. S2CID   31583157.
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