Triptorelin (acetate or palmoate) is a gonadotropin releasing hormone agonist (GnRH agonist). By causing constant stimulation of the pituitary, it decreases pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Like other GnRH agonists, triptorelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, precocious puberty, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction. Triptorelin is marketed under the brand names Decapeptyl® (Ferring Pharmaceuticals) and Diphereline® and Gonapeptyl®. Triptorelin is sold by Pfizer in the United States as Trelstar®.
During the treatment of prostate cancer it does cause a surge of testosteron (an initial uplevel of testosterone levels). In men a reduction of serum testosterone levels into the range normally seen after surgical castration occurs appr. 2 to 4 weeks after initiation of therapy. In contrast gonadotropin releasing hormone Receptor antagonists does not cause a surge, but a sudden shut-down of testosterone level.
Systematic IUPAC Name: [d-Trp6]GnRH
Additional recommended knowledge
References
- Pharmacokinetics and pharmacodynamics of GnRH agonists: clinical implications in pediatrics. J Pediatr Endocrinol Metab. 2000 Jul;13 Suppl 1:723-37. Review. PMID 10969915
- GnRH analogues—agonists and antagonists A.M. Padula,
University of Melbourne [1]
Sex hormones and related agents (primarily G03, also L02, H01C) - human endogenous in CAPS |
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Progestogens: (receptor) | PROGESTERONE, Desogestrel, Drospirenone, Dydrogesterone, Ethisterone, Etonogestrel, Ethynodiol diacetate, Gestodene, Gestonorone, Levonorgestrel, Lynestrenol, Medroxyprogesterone, Megestrol, Norelgestromin,
Norethisterone, Norethynodrel, Norgestimate, Norgestrel, Norgestrienone, Tibolone Selective progesterone receptor modulator: Asoprisnil, CDB-4124 Antiprogestogen: Mifepristone |
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Androgens: (receptor) | TESTOSTERONE, Androstanolone, Fluoxymesterone, Mesterolone, Methyltestosterone, (see also anabolic steroids) Antiandrogens: Bicalutamide, Cyproterone, Flutamide, Nilutamide, Spironolactone |
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Estrogens: (receptor) | ESTRADIOL, ESTRIOL, ESTRONE, Chlorotrianisene, Dienestrol, Diethylstilbestrol, Ethinylestradiol, Fosfestrol, Mestranol, Polyestradiol phosphate Selective estrogen receptor modulator: Bazedoxifene, Clomifene, Fulvestrant, Lasofoxifene, Raloxifene, Tamoxifen, Toremifene Aromatase inhibitor: Aminogluthetimide, Anastrozole, Exemestane, Formestane, Letrozole, Vorozole |
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Gonadotropins: (FSHR/LHCGR) | ovulation stim.: Clomifene, Urofollitropin Antigonadotropins:
Danazol, Gestrinone |
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GnRH: (receptor) | agonist: Buserelin, Goserelin, Histrelin, Leuprorelin, Nafarelin, Triptorelin antagonist:
Abarelix, Cetrorelix, Ganirelix |
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