Buserelin

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Buserelin
Buserelin.svg
Clinical data
Trade names Etilamide
AHFS/Drugs.com Micromedex Detailed Consumer Information
Pregnancy
category
  • X
Legal status
  • ℞ (Prescription only)
Routes of
administration		 implant, intranasal
Pharmacokinetic data
Biological half-life 72 to 80 minutes
Excretion Renal
Identifiers
CAS Number 57982-77-1 YesY
ATC code L02AE01 (WHO) QH01CA90 (WHO)
PubChem CID: 50225
IUPHAR/BPS 3860
DrugBank DB06719 N
ChemSpider 45545 YesY
UNII PXW8U3YXDV YesY
ChEMBL CHEMBL1909304 N
Synonyms D-Ser(Tbu)6EA10LHRH
Chemical data
Formula C60H86N16O13
Molecular mass 1239.42 g/mol
  • CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](COC(C)(C)C)NC(=O)[C@H](Cc2ccc(cc2)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc3c[nH]c4c3cccc4)NC(=O)[C@H](Cc5cnc[nH]5)NC(=O)[C@@H]6CCC(=O)N6
  • InChI=1S/C60H86N16O13/c1-7-64-57(87)48-15-11-23-76(48)58(88)41(14-10-22-65-59(61)62)69-51(81)42(24-33(2)3)70-56(86)47(31-89-60(4,5)6)75-52(82)43(25-34-16-18-37(78)19-17-34)71-55(85)46(30-77)74-53(83)44(26-35-28-66-39-13-9-8-12-38(35)39)72-54(84)45(27-36-29-63-32-67-36)73-50(80)40-20-21-49(79)68-40/h8-9,12-13,16-19,28-29,32-33,40-48,66,77-78H,7,10-11,14-15,20-27,30-31H2,1-6H3,(H,63,67)(H,64,87)(H,68,79)(H,69,81)(H,70,86)(H,71,85)(H,72,84)(H,73,80)(H,74,83)(H,75,82)(H4,61,62,65)/t40-,41-,42-,43-,44-,45-,46-,47+,48-/m0/s1 YesY
  • Key:CUWODFFVMXJOKD-UVLQAERKSA-N YesY
 NYesY (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. ↑ 1.0 1.1 1.2 1.3 Lua error in package.lua at line 80: module 'strict' not found.
  2. ↑ 2.0 2.1 Lua error in package.lua at line 80: module 'strict' not found.
  3. ↑ Lua error in package.lua at line 80: module 'strict' not found.
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