Buserelin
 | |
| Clinical data | |
|---|---|
| Trade names | Etilamide |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
| Pregnancy category |
|
| Routes of administration | implant, intranasal |
| ATC code | L02AE01 (WHO) QH01CA90 (WHO) |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Biological half-life | 72 to 80 minutes |
| Excretion | Renal |
| Identifiers | |
| Synonyms | D-Ser(Tbu)6EA10LHRH |
| CAS Number |
57982-77-1  |
| PubChem (CID) | 50225 |
| IUPHAR/BPS | 3860 |
| DrugBank |
DB06719  |
| ChemSpider |
45545 |
| UNII |
PXW8U3YXDV |
| ChEMBL |
CHEMBL1909304 |
| ECHA InfoCard | 100.055.493 |
| Chemical and physical data | |
| Formula | C60H86N16O13 |
| Molar mass | 1239.42 g/mol |
| 3D model (Jmol) | Interactive image |
| |
| |
| (what is this?) (verify) | |
Buserelin (INN) is a gonadotropin-releasing hormone agonist (GnRH agonist). The drug's effects are dependent on the frequency and time course of administration. GnRH is released in a pulsatile fashion in the postpubertal adult. Initial interaction of any GnRH agonist, such as buserelin, with the GnRH receptor induces release of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) by gonadotrophes. Long-term exposure to constant levels of buserelin, rather than endogenous pulses, leads to downregulation of the GnRH receptors and subsequent suppression of the pituitary release of LH and FSH.[1][2][3]
Like other GnRH agonists, buserelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction.[2]
It is normally delivered via a nasal spray, but is also available as an injection.[1]
Buserelin acetate is marketed by Sanofi-Aventis under the brand name Suprefact[1] and a generic form of buserelin is now produced by CinnaGen under the brand name CinnaFact.
Buserelin is also marketed under the brand name Metrelef. Metrelef is approved to treat patients with endometriosis by suppression of ovarian hormone production. In ovulation induction It is used as a pituitary blockade as an adjunct to gonadotrophin administration.
Deslorelin is a similar GnRH agonist used in veterinary medicine.
Adverse effects
During the initial phase of the therapy, before GnRH receptors have been significantly down-regulated, testosterone levels are increased. This can lead to transient tumour activation with bone pain (in patients with metastases) and urinary retention. Side effects that occur later during the treatment are mainly due to low testosterone levels and include headache, hot flashes, reduced libido, and erectile dysfunction.[1]
See also
References
- 1 2 3 4 Jasek, W, ed. (2007). Austria-Codex (in German) (62nd ed.). Vienna: Österreichischer Apothekerverlag. pp. 7832–7. ISBN 978-3-85200-181-4.
- 1 2 Mutschler, Ernst; Schäfer-Korting, Monika (2001). Arzneimittelwirkungen (in German) (8 ed.). Stuttgart: Wissenschaftliche Verlagsgesellschaft. pp. 372–3. ISBN 3-8047-1763-2.
- ↑ Wuttke, W; Jarry, H; Feleder, C; Moguilevsky, J; Leonhardt, S; Seong, J. Y.; Kim, K (1996). "The neurochemistry of the GnRH pulse generator". Acta neurobiologiae experimentalis. 56 (3): 707–13. PMID 8917899.