塩酸グラニセトロン

関: granisetron、Kytril

WordNet

a complex consisting of an organic base in association with hydrogen chloride

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/05/15 18:35:29」(JST)

wiki en

Granisetron is a serotonin 5-HT₃ receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much effect on vomiting due to motion sickness. This drug does not have any effect on dopamine receptors or muscarinic receptors.

Granisetron was developed by chemists working at the British drug company Beecham around 1988 and is available as a generic. It is produced by Roche Laboratories under the trade name Kytril. The drug was approved in the United Kingdom in 1991 and in United States in 1994 by the FDA.

A granisetron transdermal patch with the trade name Sancuso was approved by the US FDA on September 12, 2008.^[1] Sancuso is manufactured by ProStrakan, Inc., a pharmaceutical company headquartered in Bedminster, NJ, with global headquarters in Scotland.

Granisetron breaks down slowly, staying in the body for a long time. One dose usually lasts 4 to 9 hours and is usually administered once or twice daily. This drug is removed from the body by the liver and kidneys.

Indications [edit]

Chemotherapy-induced nausea and vomiting
- 5-HT₃ receptor antagonists are the primary drugs used to treat and prevent chemotherapy-induced nausea and vomiting. Many times they are given intravenously about 30 minutes before beginning therapy.
Post-operative and post-radiation nausea and vomiting
Is a possible therapy for nausea and vomiting due to acute or chronic medical illness or acute gastroenteritis
Treatment of Cyclic vomiting syndrome although there are no formal trials to confirm efficacy.

The proof of efficacy of granisetron to treat post-anesthetic nausea and vomiting has been questioned. Dr. Yoshitaka Fujii published 12 papers on this topic in Canadian Journal of Anesthesia which have since been retracted. A further five papers in the same journal on the same drug by Dr Fujii are considered indeterminate.

Adverse effects [edit]

Granisetron is a well-tolerated drug with few side effects. Headache, dizziness, and constipation are the most commonly reported side effects associated with its use. There have been no significant drug interactions reported with this drug's use. It is broken down by the liver's cytochrome P450 system and it has little effect on the metabolism of other drugs broken down by this system.

APF530 [edit]

A New Drug Application (NDA) for APF530, a sustained-delivery form of Granisetron, was accepted in October 2012.^[2] APF530 will be targeted as an antiemetic, towards patients undergoing radiation therapy and chemotherapy. APF530 contains the 5-HT3 antagonist, granisetron, formulated in the Company's proprietary Biochronomer™ drug delivery system, which allows therapeutic drug levels to be maintained for five days with a single subcutaneous injection.

External links [edit]

Kytril Web site
Sancuso Web site

References [edit]

^ PRNewswire. FDA Approves Sancuso, the First and Only Patch for Preventing Nausea and Vomiting in Cancer Patients Undergoing Chemotherapy. September 12, 2008.
^ Drugs.com A.P. Pharma Announces PDUFA Action Date for APF530 New Drug Application Resubmission. October 16, 2012.

Katzung, Bertram G. Basic and Clinical Pharmacology, 9th ed. (2004). ISBN 0-07-141092-9

UpToDate Contents

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1. 化学療法誘発性悪心および嘔吐の予防および治療 prevention and treatment of chemotherapy induced nausea and vomiting
2. 制吐剤の特性 characteristics of antiemetic drugs
3. 麻酔後ケア病棟における合併症発生の概要 overview of complications occurring in the post anesthesia care unit
4. 放射線療法による悪心および嘔吐：予防と治療 radiotherapy induced nausea and vomiting prophylaxis and treatment
5. 脳腫瘍による頭痛 brain tumor headache

English Journal

Evaluation of the relation between patient characteristics and the state of chemotherapy-induced nausea and vomiting in patients with gynecologic cancer receiving paclitaxel and carboplatin.

Furukawa N1, Akasaka J, Shigemitsu A, Sasaki Y, Nagai A, Kawaguchi R, Kobayashi H.Author information 1Department of Obstetrics and Gynecology, Nara Medical University, 840 Shijo-cho, Kashihara, Nara, 634-8522, Japan, furunao0813@gmail.com.AbstractPURPOSE: An antiemetic regimen for patients taking paclitaxel and carboplatin (TC) includes dexamethasone (20 mg) to protect against hypersensitivity. Chemotherapy-induced nausea and vomiting (CINV), however, is difficult to adequately control in patients receiving TC. In the present study, we retrospectively investigated risk factors for CINV in patients receiving TC with this antiemetic regimen based on a questionnaire.
Archives of gynecology and obstetrics.Arch Gynecol Obstet.2014 Apr;289(4):859-64. doi: 10.1007/s00404-013-3058-7. Epub 2013 Nov 2.
PURPOSE: An antiemetic regimen for patients taking paclitaxel and carboplatin (TC) includes dexamethasone (20 mg) to protect against hypersensitivity. Chemotherapy-induced nausea and vomiting (CINV), however, is difficult to adequately control in patients receiving TC. In the present study, we retr
PMID 24185939

Aprepitant triple therapy for the prevention of chemotherapy-induced nausea and vomiting following high-dose cisplatin in Chinese patients: a randomized, double-blind, placebo-controlled phase III trial.

Hu Z1, Cheng Y, Zhang H, Zhou C, Han B, Zhang Y, Huang C, Chang J, Song X, Liang J, Liang H, Bai C, Yu S, Chen J, Wang J, Pan H, Chitkara DK, Hille DA, Zhang L.Author information 1Department of Medical Oncology, Sun Yat-sen University Cancer Center, 651 Dongfeng Road East, Guangzhou, 510060, People's Republic of China.AbstractPURPOSE: Aprepitant, an oral neurokinin-1 receptor antagonist, has demonstrated improved control of chemotherapy-induced nausea and vomiting (CINV) in previous studies. This is the first phase III study to evaluate the efficacy and tolerability of aprepitant in patients receiving highly emetogenic chemotherapy (HEC) in Asian countries.
Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer.Support Care Cancer.2014 Apr;22(4):979-87. doi: 10.1007/s00520-013-2043-9. Epub 2013 Nov 26.
PURPOSE: Aprepitant, an oral neurokinin-1 receptor antagonist, has demonstrated improved control of chemotherapy-induced nausea and vomiting (CINV) in previous studies. This is the first phase III study to evaluate the efficacy and tolerability of aprepitant in patients receiving highly emetogenic c
PMID 24276953

Effectiveness of palonosetron for preventing delayed chemotherapy-induced nausea and vomiting following moderately emetogenic chemotherapy in patients with gastrointestinal cancer.

Murakami M1, Hashimoto H, Yamaguchi K, Yamaguchi I, Senba S, Siraishi T.Author information 1Department of Pharmacy, Matsuyama Red Cross Hospital, Bunkyo-cho, Matsuyama-shi, Ehime, 790-8524, Japan, michi@matsuyama.jrc.or.jp.AbstractPURPOSE: Patients with gastrointestinal cancer who were receiving moderately emetogenic chemotherapy (MEC) were switched from granisetron, a first-generation 5-hydroxytryptamine-3 receptor antagonist, to palonosetron at our hospital. In the present study, we compared effectiveness before and after switching antiemetic treatment.
Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer.Support Care Cancer.2014 Apr;22(4):905-9. doi: 10.1007/s00520-013-2046-6. Epub 2013 Nov 16.
PURPOSE: Patients with gastrointestinal cancer who were receiving moderately emetogenic chemotherapy (MEC) were switched from granisetron, a first-generation 5-hydroxytryptamine-3 receptor antagonist, to palonosetron at our hospital. In the present study, we compared effectiveness before and after s
PMID 24240649

Japanese Journal

Preparation and the in Vitro Evaluation of Nanoemulsion System for the Transdermal Delivery of Granisetron Hydrochloride

Zheng Wen-wu,Zhao Ling,Wei Yu-meng [他],Ye Yun,Xiao Shun-han
Chemical and Pharmaceutical Bulletin 58(8), 1015-1019, 2010
… The objective of this study was to develop and evaluate nanoemulsion system for transdermal delivery of granisetron hydrochloride. … The effects of the content of IPM as an oil phase and n-methyl pyrrolidone (NMP) as transdermal enhancer on rat skin permeation of granisetron hydrochloride nanoemulsion were studied in vitro. …
NAID 130000299807

症例肺癌化学療法時の制吐管理が塩酸グラニセトロンよりも塩酸ラモセトロンの方が有効であった1例

田尻守拡,森松嘉孝,相沢久道
癌の臨床 52(2), 71-75, 2006-00-00
NAID 40015393319

Antiemetic Activity of FK1052, a 5-HT3- and 5-HT4-Receptor Antagonist, in Suncus murinus and Ferrets

Nakayama Hiroe,Yamakuni Hisashi,Higaki Mika [他],Ishikawa Hirofumi,Imazumi Katsunori,Matsuo Masahiko,Mutoh Seitaro
Journal of Pharmacological Sciences 98(4), 396-403, 2005
… We investigated the effect of FK1052 [(+)-8,9-dihydro-10-methyl-7-[(5-methyl-1H-imidazol-4-yl)methyl]pyrido[1,2-a]indol-6(7H)-one hydrochloride], a 5-HT3- and 5-HT4-receptor antagonist, on the emesis induced by motion stimuli, copper sulfate, or cisplatin in either Suncus murinus …
NAID 130000074270

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★リンクテーブル★

リンク元	「グラニセトロン」
関連記事	「hydrochloride」

「グラニセトロン」

Granisetron
Systematic (IUPAC) name
	1-methyl-N-((1R,3r,5S)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl)-1H-indazole-3-carboxamide
Clinical data
Trade names	Kytril
AHFS/Drugs.com	monograph
MedlinePlus	a601211
Pregnancy cat.	B1 (Au),
Legal status	S4 (Au), POM (UK), ℞-only (U.S.)
Routes	Oral, intravenous, transdermal
Pharmacokinetic data
Bioavailability	60%
Protein binding	65%
Metabolism	Hepatic
Half-life	3–14 hours
Excretion	Renal 11–12%, faecal 38%
Identifiers
CAS number	109889-09-0
ATC code	A04AA02
PubChem	CID 3510
IUPHAR ligand	2300
DrugBank	DB00889
ChemSpider	10482033
UNII	WZG3J2MCOL
KEGG	D04370
ChEMBL	CHEMBL519643
Chemical data
Formula	C18H24N4O
Mol. mass	312.41 g/mol
	SMILES CN4[C@@H]1CCC[C@H]4C[C@H](C1)NC(=O)c3nn(C)c2ccccc23;
	InChI InChI=1S/C18H24N4O/c1-21-13-6-5-7-14(21)11-12(10-13)19-18(23)17-15-8-3-4-9-16(15)22(2)20-17/h3-4,8-9,12-14H,5-7,10-11H2,1-2H3,(H,19,23)/t12-,13+,14- ; Key:MFWNKCLOYSRHCJ-BTTYYORXSA-N ;
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　　[★]

英: granisetron
化: 塩酸グラニセトロン granisetron hydrochloride
商: カイトリル Kytril
関: 鎮吐薬

「hydrochloride」

　　[★] 塩酸塩、ハイドロクロライド　

[1] PRNewswire. FDA Approves Sancuso, the First and Only Patch for Preventing Nausea and Vomiting in Cancer Patients Undergoing Chemotherapy. September 12, 2008.

[2] Drugs.com A.P. Pharma Announces PDUFA Action Date for APF530 New Drug Application Resubmission. October 16, 2012.

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案内

granisetron hydrochloride