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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/10/31 16:14:47」(JST)

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Nafarelin 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). Nafarelin may be used in the treatment of estrogen-dependent conditions (such as endometriosis or uterine fibroids), to treat central precocious puberty, and to control ovarian stimulation in IVF.

It is normally delivered via a nasal spray.

Nafarelin acetate is marketed by Searle (now part of Pfizer) under the brand name Synarel.

Side effects

Side effects of nafarelin are mostly related to the low estrogen state. Side effects include hot flashes, vaginal dryness, headaches, mood changes, and decreased interest in sex. Some patients may experience acne, muscle pain, reduced breast size, and irritation of the tissue inside the nose. These side effects should disappear after stopping the medication.

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UpToDate Contents

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1. 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
2. アンドロゲン過剰症および男性型多毛症治療におけるGnRHアゴニストの使用 use of gnrh agonists in the treatment of hyperandrogenism and hirsutism
3. 子宮内膜症の治療の概要 overview of the treatment of endometriosis
4. 子宮平滑筋腫（子宮筋腫）の治療の概要 overview of treatment of uterine leiomyomas fibroids
5. 思春期における子宮内膜症の診断および治療 diagnosis and treatment of endometriosis in adolescents

English Journal

Spontaneous reports of seizure in association with leuprolide (lupron depot), goserelin (zoladex implant), and naferelin (synarel nasal spray).

Gatti J, Brinker A, Avigan M.
Obstetrics and gynecology.Obstet Gynecol.2013 May;121(5):1107. doi: 10.1097/AOG.0b013e31828c9cb3.
PMID 23635751

A mathematical model of the human menstrual cycle for the administration of GnRH analogues.

Röblitz S, Stötzel C, Deuflhard P, Jones HM, Azulay DO, van der Graaf PH, Martin SW.Author information Computational Systems Biology Group, Zuse Institute Berlin (ZIB), Berlin, Germany. susanna.roeblitz@zib.deAbstractThe paper presents a differential equation model for the feedback mechanisms between gonadotropin-releasing hormone (GnRH), follicle-stimulating hormone (FSH), luteinizing hormone (LH), development of follicles and corpus luteum, and the production of estradiol (E2), progesterone (P4), inhibin A (IhA), and inhibin B (IhB) during the female menstrual cycle. Compared to earlier human cycle models, there are three important differences: The model presented here (a) does not involve any delay equations, (b) is based on a deterministic modeling of the GnRH pulse pattern, and (c) contains less differential equations and less parameters. These differences allow for a faster simulation and parameter identification. The focus is on modeling GnRH-receptor binding, in particular, by inclusion of a pharmacokinetic/pharmacodynamic (PK/PD) model for a GnRH agonist, Nafarelin, and a GnRH antagonist, Cetrorelix, into the menstrual cycle model. The final mathematical model describes the hormone profiles (LH, FSH, P4, E2) throughout the menstrual cycle of 12 healthy women. It correctly predicts hormonal changes following single and multiple dose administration of Nafarelin or Cetrorelix at different stages in the cycle.
Journal of theoretical biology.J Theor Biol.2013 Mar 21;321:8-27. doi: 10.1016/j.jtbi.2012.11.020. Epub 2012 Dec 1.
The paper presents a differential equation model for the feedback mechanisms between gonadotropin-releasing hormone (GnRH), follicle-stimulating hormone (FSH), luteinizing hormone (LH), development of follicles and corpus luteum, and the production of estradiol (E2), progesterone (P4), inhibin A (Ih
PMID 23206386

Restart of steroidogenesis in dogs during recrudescence of testicular function following downregulation with a GnRH-agonist implant.

Gentil M, Hoffmann B, Spang A, Failing K, Goericke-Pesch S.Author information Clinic for Obstetrics, Gynecology and Andrology of Large and Small Animals, Justus-Liebig-University Giessen, Germany. schulzmichaela@gmx.deAbstractTo date, no details are available concerning the restart of steroidogenesis following the downregulation of testicular endocrine and germinative function by gonadotrophin-releasing hormone (GnRH)-agonist implants. This restart was assessed by determining the expression of steroidogenic acute regulatory (StAR) protein, cytochrome P450 side-chain cleavage enzyme (P450scc) and cytochrome P450 17α-hydroxylase,17,20-lyase (P450c17). The re-establishment of steroidogenesis was initiated by the removal of the GnRH-agonist implant (18.5 mg azagly nafarelin, Gonazon) at 5 months after treatment. Testes were removed at 3-week intervals (weeks 0-24) and four groups were formed according to the stage of spermatogenesis as revealed by the most developed germ cells observed (developmental group [DG] spermatocytes to DG elongated spermatids). Five dogs served as untreated controls. Positive immunostaining for StAR, P450scc and P450c17 was restricted to Leydig cells. Western blot indicated the specifity of the respective antibodies with hints of a expression of canine-specific P450scc and P450c17 proteins. A significant effect of group was observed for a percentage of the immunopositive area (PIA) as an indicator of active Leydig cells for StAR (P<0.05), P450scc (P<0.001) and P450c17 (P<0.001), with PIA being lowest for the DG spermatocytes. With regard to the strength of the immunopositive signal, a significant effect of group was found for P450scc (P<0.01) and P450c17 (P<0.05), with the lowest intensity being observed in DG spermatocytes. At the mRNA level, the upregulation from DG spermatocytes to DG round spermatids was clearly evident but was only significant for P450scc (P<0.05). Thus, downregulation affects the whole cascade of steroidogenesis, whereas withdrawal of inhibition results in a rapid restart, in part indicating a rebound phenomenon.
Cell and tissue research.Cell Tissue Res.2012 Dec;350(3):513-23. doi: 10.1007/s00441-012-1506-5. Epub 2012 Oct 9.
To date, no details are available concerning the restart of steroidogenesis following the downregulation of testicular endocrine and germinative function by gonadotrophin-releasing hormone (GnRH)-agonist implants. This restart was assessed by determining the expression of steroidogenic acute regulat
PMID 23053053

Japanese Journal

GnRHアナログによるうつ病の1例

日本農村医学会雑誌 60(5), 627-630, 2012
NAID 130004451246

酢酸ナファレリンを用いてのIVF-ETのための過排卵刺激法の試み

日本不妊学会雑誌 = Japanese journal of fertility and sterility 43(3), 275-279, 1998-07-01
NAID 10008351966

Comparison of buserelin and nafarelin in IVF cycles and in subsequent frozen-thawed embryo transfer cycles

Acta Obstet Gynecol Scand 77, 854-859, 1998
NAID 30013471604

Related Pictures

★リンクテーブル★

リンク元	「ナファレリン」
拡張検索	「nafarelin acetate」

「ナファレリン」

Nafarelin
Systematic (IUPAC) name
	(2R)-N-[(2R)-5-carbamimidamido-1-[(2S)-2-[(carbamoylmethyl)carbamoyl]pyrrolidin-1-yl]-1-oxopentan-2-yl]-2-[(2R)-2-[(2R)-2-[(2R)-3-hydroxy-2-[(2S)-2-[(2S)-3-(1H-imidazol-4-yl)-2-{[(2R)-5-oxopyrrolidin-2-yl]formamido}propanamido]-3-(1H-indol-3-yl)propanamido]propanamido]-3-(4-hydroxyphenyl)propanamido]-3-(naphthalen-2-yl)propanamido]-4-methylpentanamide
Clinical data
Trade names	Synarel
AHFS/Drugs.com	monograph
MedlinePlus	a601082
Pregnancy cat.	X
Legal status	℞-only
Routes	Nasal spray
Pharmacokinetic data
Half-life	2.6 to 4 hours
Excretion	renal
Identifiers
CAS number	76932-56-4
ATC code	H01CA02
PubChem	CID 25077649
DrugBank	DB00666
ChemSpider	10482014
UNII	1X0094V6JV
ChEMBL	CHEMBL1201309
Chemical data
Formula	C66H83N17O13
Mol. mass	1321.6344 g/mol
	InChI InChI=1S/C66H83N17O13/c1-36(2)25-48(58(89)76-47(13-7-23-71-66(68)69)65(96)83-24-8-14-54(83)64(95)73-33-55(67)86)77-60(91)50(28-38-15-18-39-9-3-4-10-40(39)26-38)78-59(90)49(27-37-16-19-43(85)20-17-37)79-63(94)53(34-84)82-61(92)51(29-41-31-72-45-12-6-5-11-44(41)45)80-62(93)52(30-42-32-70-35-74-42)81-57(88)46-21-22-56(87)75-46/h3-6,9-12,15-20,26,31-32,35-36,46-54,72,84-85H,7-8,13-14,21-25,27-30,33-34H2,1-2H3,(H2,67,86)(H,70,74)(H,73,95)(H,75,87)(H,76,89)(H,77,91)(H,78,90)(H,79,94)(H,80,93)(H,81,88)(H,82,92)(H4,68,69,71)/t46-,47-,48-,49-,50+,51-,52-,53-,54-/m0/s1 ; Key:RWHUEXWOYVBUCI-ITQXDASVSA-N ;
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