Gonadorelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which is used in fertility medicine and to treat amenorrhea and hypogonadism.[2][3][4][5][5][6][7] It is also used in veterinary medicine.[3][5] The medication is a form of the endogenous GnRH and is identical to it in chemical structure.[2][3][5][7] It is given by injection into a blood vessel or fat or as a nasal spray.[5][1][7]
Contents
1Medical uses
1.1Available forms
2Pharmacology
2.1Pharmacodynamics
2.2Pharmacokinetics
3History
4Society and culture
4.1Generic names
4.2Brand names
4.3Availability
5See also
6References
Medical uses
Gonadorelin is used as a diagnostic agent to assess pituitary gland function.[1] It is also used in the treatment of primary hypothalamic amenorrhea, hypogonadotropic hypogonadism (e.g., Kallmann syndrome), delayed puberty, cryptorchidism, and infertility.[7][8][1] Unlike other GnRH analogues, it is not used to suppress sex hormone production.[9]
Available forms
Gonadorelin is available in a portable infusion pump that provides pulsatile subcutaneous administration of the drug.[7][8] The usual dosage delivered is 5 to 20 μg of gonadorelin per pulse every 90 to 120 minutes.[7][8] It is also available in solution form for intravenous or subcutaneous injection and as a nasal spray.[7]
Pharmacology
Pharmacodynamics
Gonadorelin is an agonist of the GnRH receptor and is used to induce the secretion of the gonadotropins follicle-stimulating hormone and luteinizing hormone from the pituitary gland and to increase sex hormone production by the gonads.[7][8]
Pharmacokinetics
Gonadorelin has a distribution half-life of 2 to 10 minutes and a very short terminal half-life of 10 to 40 minutes.[1] It is metabolized by hydrolysis into smaller peptide components.[1]
History
Gonadorelin was available for medical use, under the brand name Factrel, as early as 1978.[10]
Society and culture
Generic names
Gonadorelin is the generic name of the drug and its INN, BAN, and JAN, while gonadorelina is its DCIT and gonadoréline is its DCF. The diacetate salt is known as gonadorelin acetate and this is its USAN, BANM, and JAN, while the hydrochloride salt is known as gonadorelin hydrochloride and this is its USAN and BANM.[2][3][5]
Brand names
Free alcohol gonadorelin has been marketed under the brand names Cryptocur, Cystoréline, Fertagyl, GnRH Serono, Gonadorelin, HRF, Kryptocur, LH-RH, Luforan, Pulstim, Relefact, Relisorm L, Stimu-LH, and Wyeth-Ayest HRF.[3][5] Gonadorelin diacetate has been marketed under the brand names Kryptocur, LHRH Ferring, Lutamin, Lutrelef, Lutrepulse, Relisorm L, and Relisorm.[3][5] GnRH hydrochloride has been marketed under the brand names Factrel, HRF, and Luforan.[3][5] Additional brand names of gonadorelin and its salts include Acegon, Conceptyl, Cystorelin, Enagon, Equity Oestrus Control, Fertagyl Cattle, Fertiral, Gonabreed, Gonadorelin Interpharm, Gonasyn, Gonavet Veyx, Hypocrine, Improvest, LH RH Tanabe, LHRH Ferring, LH-RH Ferring, LH-RH Tanabe, Oestracton, OvaCyst, Ovsynch, OVsynch, Ovurelin, Ovarelin, and Relefact LH-RH.[5] The majority of these brand names are for veterinary use.[3][5]
Availability
Gonadorelin is available widely throughout the world for clinical and/or veterinary use, including in the United States, Canada, the United Kingdom, Ireland, elsewhere throughout Europe, South Africa, Australia, New Zealand, Japan, Taiwan, and in many other countries.[3][5][11]
^ abcJ. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 745–. ISBN 978-1-4757-2085-3.
^ abcdefghiIndex Nominum 2000: International Drug Directory. Taylor & Francis. 2000. pp. 499–. ISBN 978-3-88763-075-1.
^I.K. Morton; Judith M. Hall (6 December 2012). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 136–. ISBN 978-94-011-4439-1.
^Shao WM, Bai WJ, Chen YM, Liu L, Wang YJ (2014). "[Micropump infusion of gonadorelin in the treatment of hypogonadotropic hypogonadism in patients with pituitary stalk interruption syndrome: cases analysis and literature review]". Beijing Da Xue Xue Bao (in Chinese). 46 (4): 642–5. PMID 25131486.
^ abcdefghGautam N Allahbadia; Monika Malhotra Chawla; Rita Basuray Das; Esther Velilla Garcia, Goral Gandhi, Rubina Merchant (17 July 2017). The Art & Science of Assisted Reproductive Techniques (ART). JP Medical Ltd. pp. 731–. ISBN 978-93-86322-82-1.CS1 maint: multiple names: authors list (link)
^ abcdDavid A. Williams; William O. Foye; Thomas L. Lemke (2002). Foye's Principles of Medicinal Chemistry. Lippincott Williams & Wilkins. pp. 128–. ISBN 978-0-683-30737-5.
^Louis Sanford Goodman; Alfred Goodman Gilman (January 1996). Goodman & Gilman's the Pharmacological Basis of Therapeutics. McGraw-Hill, Health Professions Division. p. 1379. ISBN 978-0-07-026266-9.
^Bain J, Moskowitz JP, Clapp JJ (1978). "LH and FSH response to gonadotropin releasing hormone (GnRH) in normospermic, oligospermic and azoospermic men". Arch. Androl. 1 (2): 147–52. PMID 367302.
^Sweetman, Sean C., ed. (2009). "Sex hormones and their modulators". Martindale: The Complete Drug Reference (36th ed.). London: Pharmaceutical Press. p. 2106–2108. ISBN 978-0-85369-840-1.
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)
Ovulation and fertility response to commercially available GnRH products in lactating cows synchronized with the Double-Ovsynch protocol.
Luchterhand M, Gamarra CA, Gennari RS, Carvalho PD, Barletta RV, Souza AH.
Animal reproduction science. 2019 Mar;202()42-48.
This study was designed to evaluate whether commonly used gonadorelin products that are commercially available in the United States results in comparable ovulation and pregnancy per AI (P/AI) in synchronized lactating dairy cows. A total of 1411 Holstein cows receiving a Double-Ovsynch protocol (DOV
Impact of phase of the estrous cycle and season on LH surge profile and fertility in dairy cows treated with different GnRH analogs (gonadorelin vs. buserelin).
Armengol-Gelonch R, Mallo JM, Ponté D, Jimenez A, Valenza A, Souza AH.
Theriogenology. 2017 Mar;91()121-126.
Our aim was to assess the GnRH-induced LH surge profile in dairy cows receiving two GnRH products (gonadorelin vs buserelin) given at proestrus or diestrus phase and to investigate whether season could alter LH surge profile in dairy cows. In Experiment 1, dairy cows at 108.2 ± 2.3 DIM, producing
Estrous synchronization strategies to optimize beef heifer reproductive performance after reproductive tract scoring.
Kasimanickam RK, Whittier WD, Hall JB, Kastelic JP.
Theriogenology. 2016 Aug;86(3)831-8.
Three experiments comparing four estrous synchronization protocols were conducted to determine estrous expression rate and artificial insemination pregnancy rate (AI-PR) in heifers with a range (1-5) of reproductive tract scores (RTSs). At enrollment (Day 0), 1783 Angus cross beef heifers from six l
Gonadorelin Acetate Drug Information from Drugs.com. Includes Gonadorelin Acetate side effects, interactions and indications. ... Gonadorelin (Systemic) JAN: Gonadorelin acetate—Gonadorelin diacetate VA CLASSIFICATION ...