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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/09/30 08:06:55」(JST)

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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]

References

^ ^a ^b ^c ^d Jasek, W, ed. (2007). Austria-Codex (in German) (62nd ed.). Vienna: Österreichischer Apothekerverlag. pp. 7832–7. ISBN 978-3-85200-181-4.
^ ^a ^b 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.

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1. 去勢感受性前立腺癌の初期全身療法 initial systemic therapy for castration sensitive prostate cancer
2. 月経前症候群および月経前不快気分障害の治療 treatment of premenstrual syndrome and premenstrual dysphoric disorder
3. 慢性偽性腸閉塞 chronic intestinal pseudo obstruction
4. 思春期遅発症の診断および治療 diagnosis and treatment of delayed puberty
5. 子宮内膜症の長期治療を目的としたゴナドトロピン放出ホルモンアゴニスト gonadotropin releasing hormone agonists for long term treatment of endometriosis

English Journal

In vitro fertility rate of 129 strain is improved by buserelin (gonadotropin-releasing hormone) administration prior to superovulation.

Vasudevan K, Sztein JM.SourceAssisted Reproduction Technologies and Cryopreservation Unit, CMB, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, Maryland, USA.
Laboratory animals.Lab Anim.2012 Oct;46(4):299-303. doi: 10.1258/la.2012.012073.
The 129 mice are well recognized for their low fertility and it is speculated that this lack of fertility may be due to the oocyte condition. In this study we investigated superovulation regimens for the 129S1/SvImJ mouse strain to improve the oocyte quality and fertility rate of in vitro fertilizat
PMID 23097563

Comparison of the GnRH-stimulation test and a semiquantitative quick test for LH to diagnose presence of ovaries in the female domestic cat.

Rohlertz M, Ström Holst B, Axnér E.SourceDivision of Reproduction, Department of Clinical Sciences, Swedish University of Agricultural Sciences, Faculty of Veterinary Medicine and Animal Health, Uppsala, Sweden.
Theriogenology.Theriogenology.2012 Sep 11. pii: S0093-691X(12)00397-4. doi: 10.1016/j.theriogenology.2012.06.027. [Epub ahead of print]
It is generally recommended that female cats not intended for planned breeding are spayed to reduce the population of feral cats and also because spaying is beneficial for the long-term health of the individual. For female cats of unknown origin or with estrous symptoms after spaying there is a need
PMID 22979964

Japanese Journal

Effects of a single use of the GnRH analog buserelin on the induction of ovulation and endocrine profiles in heavy draft mares

Ｊｏｕｒｎａｌ　ｏｆ　Ｅｑｕｉｎｅ　Ｓｃｉｅｎｃｅ 27(4), 149-156, 2016
NAID 130005250231

Effect of Postbreeding Intramuscular Administration of Deslorelin Acetate on Plasma LH and Progesterone Concentrations and Conception Rate in Mares

Journal of Equine Science 25(1), 23-27, 2014
NAID 130004840487

Is it Possible to Predict the Onset of Side Effects in Patients Treated with Subcutaneous Buserelin?

Shimane journal of medical science 28(1), 21-26, 2011-12-01
NAID 120005586310

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リンク元

「ブセレリン」

Buserelin
Clinical data
Trade names	Etilamide
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Pregnancy; category	X;
Routes of; administration	implant, intranasal
Legal status
Legal status	℞ (Prescription only);
Pharmacokinetic data
Biological half-life	72 to 80 minutes
Excretion	Renal
Identifiers
CAS Number	57982-77-1
ATC code	L02AE01 (WHO) QH01CA90 (WHO)
PubChem	CID 50225
IUPHAR/BPS	3860
DrugBank	DB06719
ChemSpider	45545
UNII	PXW8U3YXDV
ChEMBL	CHEMBL1909304
Synonyms	D-Ser(Tbu)6EA10LHRH
Chemical data
Formula	C60H86N16O13
Molar mass	1239.42 g/mol
	SMILES 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 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 ; Key:CUWODFFVMXJOKD-UVLQAERKSA-N ;
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英: buserelin
化: 酢酸ブセレリン buserelin acetate
商: イトレリン、スプレキュア、フセット、ブセレキュア
関: GnRHアゴニスト; その他のホルモン剤

LH-RH作動薬;前立腺癌および閉経前乳癌治療;子宮内膜症治療

[Austria-Codex-1] Jasek, W, ed. (2007). Austria-Codex (in German) (62nd ed.). Vienna: Österreichischer Apothekerverlag. pp. 7832–7. ISBN 978-3-85200-181-4.

[Mutschler-2] Mutschler, Ernst; Schäfer-Korting, Monika (2001). Arzneimittelwirkungen (in German) (8 ed.). Stuttgart: Wissenschaftliche Verlagsgesellschaft. pp. 372–3. ISBN 3-8047-1763-2.

[3] 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.

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buserelin