Buserelin: Difference between revisions

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{{drugbox |
{{Drugbox2
| Verifiedfields = changed
| verifiedrevid = 477165149
| image = Buserelin.svg
| image = Buserelin.svg
<!--Clinical data-->
| tradename = Etilamide
| Drugs.com = {{drugs.com|CONS|buserelin}}
| pregnancy_category = X
| legal_status = ℞-only
| routes_of_administration = [[Implant (medicine)|implant]], intranasal
<!--Pharmacokinetic data-->
| 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}}
'''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]].


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


Buserelin acetate is marketed by [[Sanofi-Aventis]] under the brand name '''Suprefact'''.
It is normally delivered via a [[nasal spray]], but is also available as an injection.


{{Sex hormones}}
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==
* [[Leuprorelin]]
 
==References==
{{Reflist|2}}
 
 
{{Gonadotropins and GnRH}}
{{Peptidergics}}


[[Category:GnRH agonists]]
[[Category:GnRH agonists]]
[[Category:Endocrinology]]
 
[[de:Buserelin]]
 
[[sv:Buserelinacetat]]
{{pharmacology-stub}}
{{WikiDoc Help Menu}}
{{WikiDoc Sources}}

Revision as of 19:28, 3 February 2015


Template:Px
Buserelin
Systematic (IUPAC) name
?
Identifiers
CAS number 57982-77-1
ATC code L02AE01 Template:ATCvet
PubChem 50225
DrugBank DB06719
Chemical data
Formula Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox 
Mol. mass 1299.48 g/mol
Synonyms D-Ser(Tbu)6EA10LHRH
Pharmacokinetic data
Bioavailability ?
Metabolism ?
Half life 72 to 80 minutes
Excretion Renal
Therapeutic considerations
Pregnancy cat.

X

Legal status

℞-only

Routes implant, intranasal

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


Template:Gonadotropins and GnRH


Template:Pharmacology-stub

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