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Rabeprazole /ˌræ.ˈbɛp.ræ.zɔːl/ is an antiulcer drug in the class of proton pump inhibitors. It was developed by Eisai Co. and is marketed by Janssen-Cilag as the sodium salt under the brand names AcipHex (/ˈæsɨfɛks/, referring to pH) in the US, Pariet in Europe, Brazil, Canada, Japan, Russia and Australia, Acigard, Cyra, Rabium, Esoon,Orporo, Parit, Rabemac, Rabiloz, Razo, Rabifast, Rablet and Rabsiv in India, and Zechin in Pakistan.

Indications and usage[edit source | edit]

Short-term treatment in healing and symptomatic relief of duodenal ulcers and erosive or ulcerative gastroesophageal reflux disease (GERD); maintaining healing and reducing relapse rates of heartburn symptoms in patients with GERD; treatment of daytime and nighttime heartburn and other symptoms associated with GERD; long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome and in combination with amoxicillin and clarithromycin to eradicate Helicobacter pylori.

Gastric ulcer (GU)
Peptic ulcer disease (PUD)
Maintenance of healing of erosive or ulcerative GERD
Healing of erosive and ulcerative GERD
Healing of duodenal ulcers.
Treatment of symptomatic GERD
Treatment of pathological hypersecretory conditions (Zollinger-Ellison syndrome)
Helicobacter pylori eradication to reduce risk of duodenal ulcer recurrence

Contraindications[edit source | edit]

hypersensitivity to rabeprazole, substituted benzimidazoles or any of components of its pharmaceutical forms.
pregnancy: FDA Pregnancy Ratings: B
lactation: Thomson Lactation Ratings: Infant risk cannot be ruled out.

Restriction of usage[edit source | edit]

Bottle of rabeprazole 20 mg tablets.

acute hepatic failure
pediatric use in patients under 18 years of age (there are insufficient data about safety and efficiency of rabeprazole in this group of patients)

Side effects[edit source | edit]

Rabeprazole adverse reactions/side effects include^{[citation needed]}:

In clinical trials the most common side effect assessed as possibly or probably related to AcipHex was headache in 2.4% of patients vs 1.6% taking placebo.
abdominal pains
anxiety
arthralgia
asthenia
constipation
diarrhea
dry mouth
erythema
granulocytopenia
headache
increased or decreased appetite
insomnia
leukocytopenia
meteorism
muscle or bone pain
myalgia
nausea
skin eruption
thrombocytopenia
vertigo
vomiting

Antacid preparations such as rabeprazole by suppressing acid mediated break down of proteins, leads to an elevated risk of developing food or drug allergies. This happens due to undigested proteins then passing into the gastrointestinal tract where sensitisation occurs. It is unclear whether this risk occurs with only long-term use or with short-term use as well.^[1]

Drug interactions[edit source | edit]

Rabeprazole decreases the concentration of ketoconazole in the plasma (in 33%), increases the concentration of digoxin (in 22%), and does not interact with liquid antacids. Rabeprazole is compatible with any medicine metabolized by the CYP450 (theophylline, warfarin, diazepam, phenytoin).

Overdosage[edit source | edit]

Studies in mice and rats indicated the symptoms of acute toxicity due to overdose included: hypoactivity, labored respiration, convulsion, diarrhea, tremor, and coma. A study in dogs indicated that a dose of 2000mg/kg was not lethal.

Formulations and brand names[edit source | edit]

Rabeprazole as "CYRA" (Systopic Labs Pvt Ltd), "Elpizole" (Orchid Chemicals & Pharmaceuticals), Elpizole-20 (Orchid Chemicals & Pharmaceuticals), Rablet (Lupin), Acigard (3D), AcipHex, Rabeloc, Pariet, Rabider (Duta Formulations) Rabsiv 20 (Saharsh Biologicals) is supplied in:

Tablet, enteric-coated; 10 mg
Tablet, enteric-coated; 20 mg

References[edit source | edit]

^ Pali-Schöll I, Jensen-Jarolim E (April 2011). "Anti-acid medication as a risk factor for food allergy". Allergy 66 (4): 469–77. doi:10.1111/j.1398-9995.2010.02511.x. PMID 21121928.

Morii M, Takata H, Fujisaki H, Takeguchi N., The potency of substituted benzimidazoles such as E3810, omeprazole, Ro 18-5364 to inhibit gastric H+, K(+)-ATPase is correlatedwith the rate of acid-activation of the inhibitor, Biochem. Pharmacol. 1990 Feb 15;39(4):661-7.
Prakash A, Faulds D., Rabeprazole, Drugs. 1998 Feb;55(2):261-7; discussion 268.

External links[edit source | edit]

AcipHex official product site
Rabeprazole bound to proteins in the PDB

UpToDate Contents

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1. 酸関連疾患治療のためのプロトンポンプ阻害剤の概要および比較 overview and comparison of the proton pump inhibitors for the treatment of acid related disorders
2. ヘリコバクターピロリ菌の治療レジメン treatment regimens for helicobacter pylori
3. 抗潰瘍剤の薬理学 pharmacology of antiulcer medications
4. ゾリンジャー - エリソン症候群（ガストリノーマ）のマネージメントおよび予後 management and prognosis of the zollinger ellison syndrome gastrinoma
5. 食道由来の胸痛 chest pain of esophageal origin

English Journal

Retention behavior of proton pump inhibitors using immobilized polysaccharide-derived chiral stationary phases with organic-aqueous mobile phases.

Cirilli R, Ferretti R, Gallinella B, Zanitti L.SourceIstituto Superiore di Sanità, Dipartimento del Farmaco, Viale Regina Elena 299, 00161 Rome, Italy. Electronic address: rcirilli@iss.it.
Journal of chromatography. A.J Chromatogr A.2013 Aug 23;1304:147-53. doi: 10.1016/j.chroma.2013.07.021. Epub 2013 Jul 11.
In the present study, the chromatographic behavior of two immobilized polysaccharide-derived chiral stationary phases (CSPs), the Chiralpak ID-3 and Chiralpak IE-3, under aqueous mobile phases conditions is presented. Four proton pump inhibitors (PPIs) (omeprazole, lansoprazole, pentaprazole and rab
PMID 23880466

Randomised clinical trial: rabeprazole improves symptoms in patients with functional dyspepsia in Japan.

Iwakiri R, Tominaga K, Furuta K, Inamori M, Furuta T, Masuyama H, Kanke K, Nagahara A, Haruma K, Kinoshita Y, Higuchi K, Takahashi S, Kusano M, Iwakiri K, Kato M, Hongo M, Hiraishi H, Watanabe S, Miwa H, Naito Y, Fujimoto K, Arakawa T.SourceDepartment of Internal Medicine & Gastrointestinal Endoscopy, Saga Medical School, Saga, Japan.
Alimentary pharmacology & therapeutics.Aliment Pharmacol Ther.2013 Aug 20. doi: 10.1111/apt.12444. [Epub ahead of print]
BACKGROUND: The efficacy of proton pump inhibitors (PPIs) for treating functional dyspepsia (FD) is not well established.AIM: This study, named the SAMURAI study, aimed to assess the efficacy and dose-response relationship of rabeprazole in Japanese patients with FD in a multicentre, double-blinded,
PMID 23957383

Low-dose amitriptyline combined with proton pump inhibitor for functional chest pain.

Park SW, Lee H, Lee HJ, Park JC, Shin SK, Lee SK, Lee YC, Kim JE.SourceSe Woo Park, Hyuk Lee, Hyun Jik Lee, Jun Chul Park, Sung Kwan Shin, Sang Kil Lee, Yong Chan Lee, Department of Internal Medicine, Institute of Gastroenterology, Yonsei University College of Medicine, Seoul 120-752, South Korea.
World journal of gastroenterology : WJG.World J Gastroenterol.2013 Aug 14;19(30):4958-65. doi: 10.3748/wjg.v19.i30.4958.
AIM: To investigate the efficacy of amitriptyline with proton pump inhibitor (PPI) for the treatment of functional chest pain (FCP).METHODS: This was a randomized, open-label trial investigating the addition of low dose amitriptyline (10 mg at bedtime) to a conventional dose of rabeprazole (20 mg/d)
PMID 23946601

Japanese Journal

低用量アスピリンとGERD

杉本光繁,西野眞史,魚谷貴洋 [他]
呼吸器内科 21(5), 445-452, 2012-05
NAID 40019334072

P017 胃食道逆流症合併喘息におけるrabeprazoleの効果(成人気管支喘息,ポスターセッション,第24回日本アレルギー学会春季臨床大会)

美甘真史,櫻井章吾,小川喜子,宍戸雄一郎,秋田剛史,森田悟,朝田和博,藤井雅人,白井敏博,須田隆文,千田金吾
アレルギー 61(3・4), 511, 2012-04-10
NAID 110009482886

A large-scale nationwide multicenter prospective observational study of triple therapy using rabeprazole, amoxicillin, and clarithromycin for Helicobacter pylori eradication in Japan

FUJIOKA Toshio,AOYAMA Nobuo,SAKAI Kyoko,MIWA Yoshiyuki,KUDO Mineo,KAWASHIMA Junichi,MATSUBARA Yasuo,MIWA Jun,YAKABI Koji
Journal of gastroenterology 47(3), 276-283, 2012-03-01
NAID 10030560048

Related Pictures

★リンクテーブル★

リンク元	「プロトンポンプ阻害薬」「ラベプラゾール」
拡張検索	「sodium rabeprazole」

「プロトンポンプ阻害薬」

Rabeprazole
Systematic (IUPAC) name
	(RS)-2-([4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methylsulfinyl)-1H-benzo[d]imidazole
Clinical data
Trade names	Aciphex
AHFS/Drugs.com	monograph
MedlinePlus	a699060
Licence data	US FDA:link
Pregnancy cat.	B (US)
Legal status	POM (UK) ℞-only (US)
Routes	Oral
Pharmacokinetic data
Bioavailability	52%
Metabolism	mostly non-enzymatic,; partly hepatic (CYP2C19)
Half-life	1 - 1.5 hours
Excretion	90% renal
Identifiers
CAS number	117976-89-3
ATC code	A02BC04
PubChem	CID 5029
DrugBank	DB01129
ChemSpider	4853
UNII	32828355LL
ChEBI	CHEBI:8768
ChEMBL	CHEMBL1219
Chemical data
Formula	C18H21N3O3S
Mol. mass	359.444 g/mol
	SMILES O=S(c2nc1ccccc1n2)Cc3nccc(OCCCOC)c3C;
	InChI InChI=1S/C18H21N3O3S/c1-13-16(19-9-8-17(13)24-11-5-10-23-2)12-25(22)18-20-14-6-3-4-7-15(14)21-18/h3-4,6-9H,5,10-12H2,1-2H3,(H,20,21) ; Key:YREYEVIYCVEVJK-UHFFFAOYSA-N ;
(what is this?) (verify);

　　[★]

英: proton pump inhibitor PPI
同: プロトン-カリウムATPアーゼ阻害薬 proton-potassium ATPase inhibitor、H＋ポンプ阻害薬

命名法："-azole"
特徴

胃潰瘍の治癒率を向上する (⇔H2受容体拮抗薬)

プロトンポンプ阻害薬

消化性潰瘍治療薬

攻撃因子抑制剤

プロトンポンプ阻害薬

相互作用

　プロトンポンプ　
　　H+/K+ ATPase　・・・これはNa+/K+ ATPaseと60%相同性を持つ
　　　2,4のαサブユニットと同数のβサブユニットを含む。
　　　　αサブユニット10回膜貫通, 120-150kDa, glycoprotein
　　　　αは管腔側、原形質膜まで。細胞内輸送に必要。
　　　　βサブユニットは管腔側に突き出ており、反対側は膜内に埋もれている。

　休止期には小胞体内内腔へのH+,K+,Cl-の移動、分泌期には小胞は管腔の細胞膜と癒合してK+, Cl-を管腔側に排出する一方でH+を排出でしてK+を取り込む。

　PPIは弱塩基性

　PPIはH+と反応してPPIaとなりS-S-活性体となり、H+,K+-ATPaseのSH基と結合して不可逆的に阻害する。

　比較
　　PPI：胃潰瘍の治癒率↑
　　H2R阻害薬：十二指腸潰瘍の治癒率↑

　PPI問題
　　胃潰瘍8
　　十二指腸6
　　逆流性食道炎8
　副作用
　　血中ガストリン↑→ECL cell↑→リバウンドが激しい
　　week end therapy: 週末3日だけ投与後休薬
　　ピレンゼピン(Mi R blocker), PG(プロスタグランジン)　→　ガストリン↑を軽減
　　ラベプラゾール：ガストリン濃度を上げず酸分泌↓
　　　→リバウンドが少ない。

　PPI抵抗性潰瘍：PPIによる酸分泌抑制不十分
　①個人差によるPPIの用量不足
　②胃内でのPPIの不活性化→
　　胃内容の排泄遅延。PPIが不活化、アルカリに晒される。