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{{Editor Help}}
{{Drugbox
| Verifiedfields = changed
| verifiedrevid = 477165149
| image = Buserelin.png


<!--Clinical data-->
| tradename = Etilamide
| Drugs.com = {{drugs.com|CONS|buserelin}}
| pregnancy_category = X
| legal_status = ℞-only
| routes_of_administration = [[Implant (medicine)|implant]], intranasal


{{drugbox |
<!--Pharmacokinetic data-->
| image = Buserelin.svg
| elimination_half-life = 72 to 80 minutes
| excretion = [[Kidney|Renal]]
 
<!--Identifiers-->
| CASNo_Ref = {{cascite|correct|CAS}}
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 57982-77-1
| CAS_number = 57982-77-1
| ATC_prefix = L02  
| ATC_prefix = L02
| ATC_suffix =AE01
| ATC_suffix = AE01
| PubChem = 50225  
| ATC_supplemental =  {{ATCvet|H01|CA90}}
| DrugBank = HMDB03170
| PubChem = 50225
| C=62 | H=90| N=16| O=15|
| DrugBank_Ref = {{drugbankcite|changed|drugbank}}
| DrugBank = DB06719
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 1909304
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| ChemSpiderID = 45545
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = PXW8U3YXDV
 
<!--Chemical data-->
| C=62 | H=90 | N=16 | O=15  
| molecular_weight = 1299.48 g/mol
| molecular_weight = 1299.48 g/mol
| InChI = 1/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
| InChIKey = CUWODFFVMXJOKD-UVLQAERKBG
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| StdInChI = 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
| StdInChIKey_Ref = {{stdinchicite|correct|chemspider}}
| StdInChIKey = CUWODFFVMXJOKD-UVLQAERKSA-N
| synonyms = D-Ser(Tbu)<sup>6</sup>EA<sup>10</sup>LHRH
| synonyms = D-Ser(Tbu)<sup>6</sup>EA<sup>10</sup>LHRH
| elimination_half-life = 72 to 80 minutes
| excretion = [[Kidney|Renal]]
| pregnancy_category = X
| legal_status = ℞-only
| routes_of_administration = [[Implant (medicine)|implant]], intranasal
}}
}}
{{SI}}
__NOTOC__
'''Buserelin''' 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, 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 [[Reproductive technology|assisted reproduction]].
{{CMG}}; {{AE}} {{AV}}
 
==Overview==
 
'''Buserelin''' ([[International Nonproprietary Name|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 FSH and 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.
 
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 [[Reproductive technology|assisted reproduction]].
 
It is normally delivered via a [[nasal spray]], but is also available as an injection.
 
Buserelin acetate is marketed by [[Sanofi-Aventis]] under the brand name '''Suprefact''' 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]] '''Metrelef''' is used as a [[pituitary]] blockade as an adjunct to [[gonadotrophin]] administration.


It is normally delivered via a nasal spray but is also available as an injection.
==See also==
* [[Leuprorelin]]


Buserelin acetate is marketed by [[Sanofi-Aventis]] under the brand name '''Suprefact'''.
==References==
{{Reflist|2}}


{{Sex hormones}}
[[Category:drug]]
{{SIB}}
[[Category:chemotherapeutic agents]]
[[Category:GnRH agonists]]
[[Category:Endocrinology]]
[[de:Buserelin]]
[[sv:Buserelinacetat]]
{{WikiDoc Help Menu}}
{{WikiDoc Sources}}

Latest revision as of 18:03, 4 February 2015

Buserelin
Clinical data
Trade namesEtilamide
SynonymsD-Ser(Tbu)6EA10LHRH
AHFS/Drugs.comMicromedex Detailed Consumer Information
Pregnancy
category
  • X
Routes of
administration		implant, intranasal
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Elimination half-life72 to 80 minutes
ExcretionRenal
Identifiers
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
E number{{#property:P628}}
ECHA InfoCard{{#property:P2566}}Lua error in Module:EditAtWikidata at line 36: attempt to index field 'wikibase' (a nil value).
Chemical and physical data
FormulaC62H90N16O15
Molar mass1299.48 g/mol
 ☒N☑Y (what is this?)  (verify)

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Aparna Vuppala, M.B.B.S. [2]

Overview

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 FSH and 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.

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.

It is normally delivered via a nasal spray, but is also available as an injection.

Buserelin acetate is marketed by Sanofi-Aventis under the brand name Suprefact 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 Metrelef is used as a pituitary blockade as an adjunct to gonadotrophin administration.

See also

References

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