Drug
Anantigonadotropin is adrug which suppresses the activity and/or downstream effects of one or both of thegonadotropins ,follicle-stimulating hormone (FSH) andluteinizing hormone (LH). This results in an inhibition of thehypothalamic-pituitary-gonadal (HPG) axis , and thus a decrease in the levels of theandrogen ,estrogen , andprogestogen sex steroids in the body. Antigonadotropins also inhibitovulation in women andspermatogenesis in men. They are used for a variety of purposes, including for thehormonal birth control , treatment ofhormonally -sensitivecancers , to delayprecocious puberty andpuberty intransgender youth , as a form ofchemical castration to reduce thesex drives of individuals withhypersexuality orpedophilia , and to treat estrogen-associated conditions in women such asmenorrhagia andendometriosis , among others. High-dose antigonadotropin therapy has been referred to asmedical castration .
The best-known and widely used antigonadotropins are thegonadotropin-releasing hormone (GnRH)analogues (bothagonists andantagonists ).[ 1] negative feedback on the HPG axis),[ 2] [ 3] synthesis inhibitors such asdanazol andgestrinone .[ 4] [ 5] sexual differentiation compared to the other sex steroids,potent ones such ascyproterone acetate ,medroxyprogesterone acetate , andchlormadinone acetate are often used at high doses specifically for their antigonadotropic effects.[ 2] [ 6] [ 7]
Danazol ,gestrinone , andparoxypropione have all been classified specifically as antigonadotropins.[ 8]
Prolactin has antigonadotropic effects andhyperprolactinemia can causehypogonadism .[ 9] [ 10]
Opioids have antigonadotropic effects and can reduce luteinizing hormone and testosterone levels in men.[ 11] [ 12] [ 13] systematic review andmeta-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] opioid antagonists , likenaltrexone , haveprogonadotropic effects, and can increase luteinizing hormone and testosterone levels.[ 14]
^ Jonathan S. Berek; Emil Novak (2007).Berek and Novak's Gynecology ISBN 978-0-7817-6805-4 . Retrieved29 May 2012 . ^a b 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 . ^ 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 . ^ Jonathan S. Berek; Emil Novak (2007).Berek and Novak's Gynecology ISBN 978-0-7817-6805-4 . Retrieved29 May 2012 . ^ 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 . ^ Bercovici JP (September 1987). "[Progestational contraception]".La Revue du Praticien (in French).37 (38):2277– 8,2281– 4.PMID 3659794 . ^ 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 . ^ George W.A. Milne (8 May 2018).Drugs: Synonyms and Properties: Synonyms and Properties ISBN 978-1-351-78989-9 ^ 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 . ^ Saleem M, Martin H, Coates P (February 2018)."Prolactin Biology and Laboratory Measurement: An Update on Physiology and Current Analytical Issues" .Clin Biochem Rev .39 (1):3– 16.PMC 6069739 PMID 30072818 . ^a b 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 . ^ 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 . ^ Smith HS, Elliott JA (July 2012). "Opioid-induced androgen deficiency (OPIAD)".Pain Physician .15 (3 Suppl): ES145–56.PMID 22786453 . ^ 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 .
GnRH modulators analogues )
Gonadotropins
Others
Progonadotropins Antigonadotropins Sex steroid agonists (via negative feedback on theHPG 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 )Progestogens (incl.progestins , e.g.,chlormadinone acetate ,cyproterone acetate ,hydroxyprogesterone caproate ,gestonorone caproate ,medroxyprogesterone acetate ,megestrol acetate )
GnRH Tooltip Gonadotropin-releasing hormone receptor Gonadotropin
LH/hCG Tooltip Luteinizing hormone/choriogonadotropin receptor FSH Tooltip Follicle-stimulating hormone receptor
Media related toAntigonadotropins at Wikimedia Commons