酢酸ヒストレリン

関: histrelin

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a salt or ester of acetic acid (同)ethanoate

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/10/19 13:53:53」(JST)

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Histrelin acetate is a nonapeptide analog of gonadotropin-releasing hormone (GnRH) with added potency.^[1] When present in the bloodstream, it acts on particular cells of the pituitary gland called gonadotropes. Histrelin stimulates these cells to release luteinizing hormone and follicle-stimulating hormone. Thus it is considered a gonadotropin-releasing hormone agonist or GnRH agonist.

Histrelin is marketed by Endo Pharmaceuticals under the brand names Vantas and Supprelin LA.

Medical uses

Histrelin is used to treat hormone-sensitive cancers of the prostate in men and uterine fibroids in women. In addition, histrelin has been proven to be highly effective in treating central precocious puberty in children.^[2]^[3]

It is available as a daily intramuscular injection.

Histrelin is also available in a 12-month subcutaneous implant (Vantas) for the palliative treatment of advanced prostate cancer, since 2005 in the US, and since Jan 2010 in the UK.^[4]

A 12-month subcutaneous implant (Supprelin LA) for central precocious puberty (CPP) was approved on May 3, 2007 by the U.S. Food and Drug Administration.

Histrelin is also part of the primary care protocol in transgender children/youth, and is used in suppressing cis-sex puberty, until the patient is ready to begin cross-sex hormonal therapy.^[5]

Adverse effects

Side effects are mainly due to low testosterone levels and include headache, hot flashes, reduced libido, and erectile dysfunction.^[6]

Pharmacology

In a process known as downregulation, daily stimulation of pituitary gonadotropes causes them to become desensitized to the effects of histrelin. As a consequence, levels of LH and FSH fall after a short period of time. From that point forward, as long as histrelin is administered, the levels of LH and FSH in the blood remain low.^[7]^[8]

This prolonged lowering of LH and FSH levels is the rationale for therapy using GnRH agonists. Since LH and FSH stimulate the gonads to produce estrogens and androgens in females and males respectively, histrelin can effectively be used to decrease the sex steroids in the blood of patients.

References

^ Histrelin acetate (Vantas) - New Drug Bulletins
^ Histrelin consumer information
^ Eugster, Erica A.; William Clarke; et al. (2007). "Efficacy and Safety of Histrelin Subdermal Implant in Children with Central Precocious Puberty: A Multicenter Trial". J Clin Endocrinol Metab. 92 (5): 1697–1704. doi:10.1210/jc.2006-2479. PMID 17327379. Retrieved 2007-10-17.
^ "Implant inserted under the skin ends the misery of prostate jabs". Daily Mail. 6 April 2010. p. 48. Archived from the original on 2012-06-23.
^ "Primary Care Protocol for Transgender Patient Care: Hormone Administration". transhealth.ucsf.edu. Archived from the original on 2012-01-17. Retrieved 2015-09-29.
^ Drugs.com: Histrelin Monograph
^ 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.

External links

Central Precocious Puberty

UpToDate Contents

全文を閲覧するには購読必要です。 To read the full text you will need to subscribe.

1. 思春期早発症の治療 treatment of precocious puberty
2. 去勢感受性前立腺癌の初期全身療法 initial systemic therapy for castration sensitive prostate cancer
3. 避妊のための酢酸メドロキシプロゲステロンデポ剤 depot medroxyprogesterone acetate for contraception
4. 資源の限られた状況における子宮頸癌のスクリーニング screening for cervical cancer in resource limited settings
5. βサラセミアの治療 treatment of beta thalassemia

English Journal

Histrelin for central precocious puberty-a single surgeon experience.

Rosati S1, Maarouf R1, Brown K2, Poppe M2, Parrish D1, Haynes J1, Lanning D3.
The Journal of surgical research.J Surg Res.2015 Oct;198(2):355-9. doi: 10.1016/j.jss.2015.03.071. Epub 2015 Mar 30.
BACKGROUND: The most common cause of precocious puberty is idiopathic central precocious puberty (CPP), which is usually treated with monthly injections. An alternative treatment of precious puberty is a subcutaneous implant that contains histrelin acetate, which is continuously released for more th
PMID 25899147

Long-term efficacy and tolerability of abdominal once-yearly histrelin acetate subcutaneous implants in patients with advanced prostate cancer.

Woolen S1, Holzmeyer C1, Nesbitt E1, Siami PF2.
Prostate cancer.Prostate Cancer.2014;2014:490315. doi: 10.1155/2014/490315. Epub 2014 Dec 4.
Objectives. Long-term assessment of the efficacy and tolerability of subcutaneous abdominal histrelin acetate implants that have been inserted for more than two years. Materials and Methods. Retrospective data collected over a six-year period at a single center from charts of 113 patients who receiv
PMID 25548680

Treatment and outcomes of precocious puberty: an update.

Fuqua JS1.
The Journal of clinical endocrinology and metabolism.J Clin Endocrinol Metab.2013 Jun;98(6):2198-207. doi: 10.1210/jc.2013-1024. Epub 2013 Mar 20.
Precocious puberty is a common problem affecting up to 29 per 100,000 girls per year. The earliest identified neuroendocrine change in early puberty thus far is increased kisspeptin secretion from the arcuate nucleus and the anteroventral paraventricular nucleus of the hypothalamus. The regulation o
PMID 23515450

「ヒストレリン」

Histrelin
Systematic (IUPAC) name
	5-oxo-L-prolyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-1-benzyl-D-histidyl-L-leucyl-N5-(diaminomethylene)-L-ornithyl-N-ethyl-L-prolinamide
Clinical data
AHFS/Drugs.com	Monograph
MedlinePlus	a601146
Pregnancy; category	US: X (Contraindicated); ;
Routes of; administration	Subcutaneous implant
Legal status
Legal status	US: ℞-only;
Pharmacokinetic data
Bioavailability	92%
Protein binding	70%
Metabolism	Hepatic
Biological half-life	4.0 hours
Excretion	Undetermined
Identifiers
CAS Number	76712-82-8
ATC code	L02AE05 (WHO)
PubChem	CID 25077993
IUPHAR/BPS	3884
ChemSpider	10482012
UNII	H50H3S3W74
KEGG	D02369
ChEMBL	CHEMBL1201255
Chemical data
Formula	C66H86N18O12
Molar mass	1323.5 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](CC2=CN(C=N2)CC3=CC=CC=C3)NC(=O)[C@H](CC4=CC=C(C=C4)O)NC(=O)[C@H](CO)NC(=O)[C@H](CC5=CNC6=CC=CC=C65)NC(=O)[C@H](CC7=CNC=N7)NC(=O)[C@@H]8CCC(=O)N8 ;
	InChI InChI=1S/C66H86N18O12/c1-4-70-64(95)55-17-11-25-84(55)65(96)48(16-10-24-71-66(67)68)76-58(89)49(26-38(2)3)77-62(93)53(30-43-34-83(37-74-43)33-40-12-6-5-7-13-40)81-59(90)50(27-39-18-20-44(86)21-19-39)78-63(94)54(35-85)82-60(91)51(28-41-31-72-46-15-9-8-14-45(41)46)79-61(92)52(29-42-32-69-36-73-42)80-57(88)47-22-23-56(87)75-47/h5-9,12-15,18-21,31-32,34,36-38,47-55,72,85-86H,4,10-11,16-17,22-30,33,35H2,1-3H3,(H,69,73)(H,70,95)(H,75,87)(H,76,89)(H,77,93)(H,78,94)(H,79,92)(H,80,88)(H,81,90)(H,82,91)(H4,67,68,71)/t47-,48-,49-,50-,51-,52-,53+,54-,55-/m0/s1 ; Key:HHXHVIJIIXKSOE-QILQGKCVSA-N ;
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英: histrelin
化: 酢酸ヒストレリン histrelin acetate

「酢酸ヒストレリン」

　　[★]

英: histrelin acetate
関: ヒストレリン

[def-1] Histrelin acetate (Vantas) - New Drug Bulletins

[2] Histrelin consumer information

[3] Eugster, Erica A.; William Clarke; et al. (2007). "Efficacy and Safety of Histrelin Subdermal Implant in Children with Central Precocious Puberty: A Multicenter Trial". J Clin Endocrinol Metab. 92 (5): 1697–1704. doi:10.1210/jc.2006-2479. PMID 17327379. Retrieved 2007-10-17.

[4] "Implant inserted under the skin ends the misery of prostate jabs". Daily Mail. 6 April 2010. p. 48. Archived from the original on 2012-06-23.

[5] "Primary Care Protocol for Transgender Patient Care: Hormone Administration". transhealth.ucsf.edu. Archived from the original on 2012-01-17. Retrieved 2015-09-29.

[6] Drugs.com: Histrelin Monograph

[Mutschler-7] Mutschler, Ernst; Schäfer-Korting, Monika (2001). Arzneimittelwirkungen (in German) (8 ed.). Stuttgart: Wissenschaftliche Verlagsgesellschaft. pp. 372–3. ISBN 3-8047-1763-2.

[8] 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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histrelin acetate