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antacid (trade name Prevacid) that suppresses acid secretion in the stomach (同)Prevacid

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/07/26 12:16:55」(JST)

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Lansoprazole (/lænˈsoʊprəzoʊl/ lan-SOH-prə-zohl; INN) is a proton-pump inhibitor (PPI) which inhibits the stomach's production of gastric acids. It is manufactured by a number of companies worldwide under several brand names. In the United States, it was first approved by the Food and Drug Administration (FDA) in 1995.^[1] Prevacid patent protection expired on November 10, 2009.^[2]^[3] Since 2009, lansoprazole has been available over the counter (OTC) in the U.S. in a 15-mg dose marketed by Novartis as Prevacid 24HR.^[4]^[5]^[6] In Australia, it is marketed by Pfizer as Zoton.

Lansoprazole is a proton-pump inhibitor (PPI) in the same pharmacologic class as omeprazole. Lansoprazole has been marketed for many years and is one of several PPIs available.^[7] It is a racemic 1:1 mixture of the enantiomers dexlansoprazole (Dexilant, formerly named Kapidex) and levolansoprazole.^[8] Dexlansoprazole is an enantiomerically pure active ingredient of a commercial drug as a result of the 'enantiomeric shift'.

Lansoprazole's plasma elimination half-life (1.5 h) is not proportional to the duration of the drug's effects to the person (i.e. gastric acid suppression).^[9] and the effects of the drug last for over 24 hours after it has been used for a day or more.^[5] Lansoprazole, 30-mg administered nasogastrically, effectively controls intragastric pH and is an alternative to intravenous pantoprazole in patients who are unable to swallow solid-dose formulations.^[10]

Indications

Lansoprazole is indicated for treatment of:

Ulcers of the stomach and duodenum, and NSAID-induced ulcers
Helicobacter pylori infection, alongside antibiotics (adjunctive treatment), treatment to kill H. pylori causing ulcers or other problems involves using two other drugs besides lansoprazole known as "triple therapy", and involves taking twice daily for 10 or 14 days lansoprazole 30-mg, amoxicillin 1,000-mg, and clarithromycin 500-mg
Gastroesophageal reflux disease
Zollinger-Ellison syndrome^[5]

Drug interactions

Lansoprazole interacts with several other drugs, either due to its own nature or as a PPI.^[11]

PPIs reduce absorption of antifungals (itraconazole and ketoconazole) ^[12] and possibly increase digoxin in plasma
Increases plasma concentrations of cilostazol (risk of toxicity)

Lansoprazole possibly interacts with, amongst other drugs:

sucralfate
ampicillin
bisacodyl
clopidogrel
delavirdine
fluvoxamine
iron salts
voriconazole
aminophylline and theophylline
astemizole

Side effects

Side effects of PPIs in general^[13] and lansoprazole in particular^[14] may include:

Infrequent: dry mouth, insomnia, drowsiness, blurred vision, rash, pruritus
Rarely and very rarely: taste disturbance, liver dysfunction, peripheral oedema, hypersensitivity reactions (including bronchospasm, urinary, angioedema, anaphylaxis), photosensitivity, fever, sweating, depression, interstitial nephritis, blood disorders (including leukopenia, leukocytosis, pancytopenia, thrombocytopenia), arthralgia, myalgia, skin reactions^[15] including (erythroderma^[16] Stevens–Johnson syndrome, toxic epidermal necrolysis, bullous eruption)
Severe: Gastrointestinal disturbances (such as nausea 1.3%, abdominal pain 2.1%, diarrhea 3.8%)^[9]

PPIs may be associated with a greater risk of hip fractures and Clostridium difficile-associated diarrhea.^[5]^:22

Availability

Prevacid 30 mg

The lansoprazole molecule is off-patent and so generic drugs are available under many brand names in many countries;^[17] there are patents covering some formulations in effect as of 2015.^[18]

Research

In vitro experiments have shown that lansoprazole binds to the pathogenic form of tau protein.^[19] As of 2015 laboratory studies were underway on analogs of lansoprazole to explore their use as potential PET imaging agents for diagnosing tauopathies including Alzheimer's disease.^[19] Lansoprazole is also a prodrug that targets the cytochrome bc1 complex of Mycobacterium tuberculosis once converted to lansoprazole sulfide in mycobacterial host cells.^[20]

References

^ Mosby's Drug Consult: Lansoprazole
^ Prevacid drug patents
^ Teva to release Prevacid version when patent expires
^ "Novartis launches Prevacid 24HR over-the-counter for full 24-hour frequent heartburn treatment" (PDF) (Press release). November 12, 2009. Retrieved November 13, 2009.
^ ^a ^b ^c ^d "Prevacid 24HR Label" (PDF). May 2010. Retrieved November 15, 2014.
^ "Novartis launches Prevacid 24HR over-the-counter for full 24-hour frequent heartburn treatment" (Press release). November 12, 2009. Retrieved November 13, 2009.
^ http://www.patient.co.uk/showdoc/30002943/
^ "Pharmacy Benefit Update". Retrieved 2 July 2014.
^ ^a ^b "Prevacid Pharmacology, Pharmacokinetics, Studies, Metabolism". RxList.com. 2007. Retrieved April 14, 2007.
^ Effects on 24-Hour Intragastric pHFreston M.D., Ph.D., James; Yi-Lin Chiu, Ph.D., Wei-Jian Pan, Ph.D., Nancy Lukasik, B.S.N., and Jörg Täubel, M.D., A.F.P.M. (2001). "Effects on 24-Hour Intragastric pH: A Comparison of Lansoprazole Administered Nasogastrically in Apple Juice and Pantoprazole Administered Intravenously". American Journal of Gastroenterology 96 (7): 2058–2065. doi:10.1111/j.1572-0241.2001.03939.x. ISSN 0002-9270. OCLC 440925790. PMID 11467632.
^ British National Formulary (Free registration required) Lansoprazole interactions
^ Antimicrob Agents Chemother. 1991 September; 35(9): 1765–1771. Effects of ranitidine and sucralfate on ketoconazole bioavailability. S C Piscitelli, T F Goss, J H Wilton, D T D'Andrea, H Goldstein, and J J Schentag [1]
^ British National Formulary (Free registration required) 1.3.5 Proton pump inhibitors
^ British National Formulary (Free registration required) Lansoprazole
^ K C Singhal & S Z Rahman, Lansoprazole Induced Adverse Effects on the Skin, Indian Medical Gazette, July 2001, Vol. CXXXV. N0. 7: 223-225
^ Sterry W, Assaf C (2007). "Erythroderma". In Bolognia JL. Dermatology. St. Louis: Mosby. p. 154. ISBN 1-4160-2999-0. .
^ drugs.com International availability of lansoprazole Page accessed February 3, 2015
^ drugs.com Generic lansoprazole Page accessed February 3, 2015
^ ^a ^b Villemagne, VL; Fodero-Tavoletti, MT; Masters, CL; Rowe, CC (January 2015). "Tau imaging: early progress and future directions.". The Lancet. Neurology 14 (1): 114–24. PMID 25496902.
^ Rybniker, Jan et al. (July 2015). "Lansoprazole is an antituberculous prodrug targeting cytochrome bc1". Nature communications. doi:10.1038/ncomms8659.

External links

Prevacid official website Takeda Pharmaceuticals North America
Prevacid 24HR official website Novartis Consumer Health
Prevpac official website Takeda Pharmaceuticals North America
U.S. National Library of Medicine: Drug Information Portal - Lansoprazole

UpToDate Contents

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1. 非ステロイド性抗炎症剤（NSAIDs）（アスピリンを含む）：胃十二指腸障害の一次予防 nsaids including aspirin primary prevention of gastroduodenal toxicity
2. 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
3. 小児および思春期における胃食道逆流症のマネージメント management of gastroesophageal reflux disease in children and adolescents
4. 成人における胃食道逆流症の内科的マネージメント medical management of gastroesophageal reflux disease in adults
5. ヘリコバクターピロリ菌の治療レジメン treatment regimens for helicobacter pylori

English Journal

Do the laryngopharyngeal symptoms and signs ameliorate by empiric treatment in patients with suspected laryngopharyngeal reflux?

Naiboglu B, Durmus R, Tek A, Toros SZ, Egeli E.SourceHaydarpa?a Numune Education and Research Hospital, Deparment of Otolaryngology Head and Neck Surgery, Turkey. drbnaib@yahoo.com
Auris, nasus, larynx.Auris Nasus Larynx.2011 Oct;38(5):622-7. Epub 2011 Feb 12.
OBJECTIVES: In clinical practice, antireflux medication is given almost always empirically without pH monitorization. We aimed to evaluate the improving effect of empiric antireflux treatment on layngopharyngeal symptoms and signs in patients with gastroesophageal reflux (GER) and suspected laryngop
PMID 21320761

Effect of fluoxetine on the pharmacokinetics of lansoprazole: a two-treatment period study in healthy male subjects.

Vlase L, Popa A, Neag M, Muntean D, Leucuta SE.SourceDepartment of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, University of Medicine and Pharmacy Iuliu Hatieganu Cluj-Napoca, Cluj, Romania.
Clinical drug investigation.Clin Drug Investig.2011 Oct 1;31(10):727-33. doi: 10.2165/11589010-000000000-00000.
Background: Fluoxetine is an inhibitor of the main metabolizing enzymes of lansoprazole and could influence the pharmacokinetics of lansoprazole. The changes in lansoprazole pharmacokinetics could have clinical significance concerning the safety of the therapy. Objective: The aim of this study was t
PMID 21877765

Japanese Journal

低用量アスピリンの長期投与時にみられる胃・十二指腸潰瘍に対するランソプラゾールの抑制効果 (特集低用量アスピリンによる消化管粘膜傷害研究の進歩)

榊信廣,蘆田潔,溝上裕士 [他]
消化器内科 55(3), 311-316, 2012-09
NAID 40019458748

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

Related Pictures

★リンクテーブル★

リンク元	「プロトンポンプ阻害薬」「ランソプラゾール」

「プロトンポンプ阻害薬」

Lansoprazole
Systematic (IUPAC) name
	(RS)-2-([3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl]methylsulfinyl)-1H-benzo[d]imidazole
Clinical data
Trade names	Prevacid
AHFS/Drugs.com	monograph
MedlinePlus	a695020
Licence data	US FDA:link
Pregnancy; category	AU: B3; US: B (No risk in non-human studies);
Legal status	UK: Prescription-only (POM); US: OTC;
Routes of; administration	Oral, IV
Pharmacokinetic data
Bioavailability	80% or more
Protein binding	97%
Metabolism	Hepatic (CYP3A4- and CYP2C19-mediated)
Biological half-life	1–1.5 hours
Excretion	Renal and fecal
Identifiers
CAS Registry Number	103577-45-3
ATC code	A02BC03
PubChem	CID: 3883
IUPHAR/BPS	7208
DrugBank	DB00448
ChemSpider	3746
UNII	0K5C5T2QPG
KEGG	D00355
ChEBI	CHEBI:6375
ChEMBL	CHEMBL480
Chemical data
Formula	C16H14F3N3O2S
Molecular mass	369.363 g/mol
	SMILES FC(F)(F)COc1c(c(ncc1)CS(=O)c3nc2ccccc2n3)C ;
	InChI InChI=1S/C16H14F3N3O2S/c1-10-13(20-7-6-14(10)24-9-16(17,18)19)8-25(23)15-21-11-4-2-3-5-12(11)22-15/h2-7H,8-9H2,1H3,(H,21,22) ; Key:MJIHNNLFOKEZEW-UHFFFAOYSA-N ;
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　　[★]

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)