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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/12/24 16:14:33」(JST)

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Amiloride is a potassium-sparing diuretic, first approved for use in 1967 (then known as MK 870), used in the management of hypertension and congestive heart failure. Amiloride was also tested as treatment of cystic fibrosis, but it was revealed inefficient in vivo due to its short time of action, therefore longer-acting ENaC inhibitors may prove more effective, e.g. Benzamil.^[1]

Structure

Amiloride is a guanidinium group containing pyrazine derivative.

Mechanism of action

Amiloride works by directly blocking the epithelial sodium channel (ENaC) thereby inhibiting sodium reabsorption in the late distal convoluted tubules, connecting tubules, and collecting ducts in the kidneys (this mechanism is the same for triamterene).^[2] This promotes the loss of sodium and water from the body, but without depleting potassium. The drug is often used in conjunction with thiazide (e.g. co-amilozide) or loop diuretics (e.g. co-amilofruse). Due to its potassium-sparing capacities, hyperkalemia (high blood potassium levels) is occasionally observed in patients taking amiloride. The risk is high in concurrent use of ACE inhibitors or spironolactone. Patients are also advised not to use potassium-containing salt replacements.^[3] Amiloride also carries the risk of developing an acidosis.

A fraction of the effects of amiloride is inhibition of cyclic GMP-gated cation channels in the inner medullary collecting duct.^[4]

Amiloride has a second action on the heart, blocking Na+/H+ exchangers Sodium-hydrogen antiporter 1 or NHE-1. This minimizes reperfusion injury in ischemic attacks.

Acid-sensing ion channels (ASICs) are also sensitive to inhibition by amiloride. ASICs are involved in nociceptor responses to pH.^[5]

Formulations and trade names

amiloride hydrochloride
- Midamor (U.S.)

co-amilozide (amiloride hydrochloride with hydrochlorothiazide)

References

^ (Review)Pharmacological treatment of the biochemical defect in cystic fibrosis airways, H.C. Rodgers, A.J. Knoxhttp://erj.ersjournals.com/content/17/6/1314.full.pdf+html
^ Loffing, Johannes and Kaissling, Brigitte (2003). "Sodium and calcium transport pathways along the mammalian distal nephron: from rabbit to human". Am J Physiol Renal Physiol 284: F628-F643. PMID 12620920.
^ LoSalt Advisory Statement (PDF)
^ Walter F., PhD. Boron. Medical Physiology: A Cellular And Molecular Approaoch. Elsevier/Saunders. ISBN 1-4160-2328-3. page 875
^ Hunt and Koltzenburg 2005 'The neurobiology of pain'

UpToDate Contents

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3. 低マグネシウム血症の評価および治療 evaluation and treatment of hypomagnesemia
4. 利尿剤とカルシウムバランス diuretics and calcium balance
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English Journal

Alveolar epithelial CNGA1 channels mediate cGMP-stimulated, amiloride-insensitive, lung liquid absorption.

Wilkinson WJ, Benjamin AR, De Proost I, Orogo-Wenn MC, Yamazaki Y, Staub O, Morita T, Adriaensen D, Riccardi D, Walters DV, Kemp PJ.SourceDivision of Pathophysiology and Repair, School of Biosciences, Cardiff University, Museum Avenue, Cardiff, CF10 3AX, UK.
Pflugers Archiv : European journal of physiology.Pflugers Arch.2011 Aug;462(2):267-79. Epub 2011 May 11.
Impairment of lung liquid absorption can lead to severe respiratory symptoms, such as those observed in pulmonary oedema. In the adult lung, liquid absorption is driven by cation transport through two pathways: a well-established amiloride-sensitive Na(+) channel (ENaC) and, more controversially, an
PMID 21559843

Gross intestinal adaptations in relation to broiler performance during chronic aflatoxin exposure.

Yunus AW, Ghareeb K, Abd-El-Fattah AA, Twaruzek M, Bohm J.SourceInstitute of Animal Nutrition, Department for Farm Animal and Veterinary Public Health, University of Veterinary Medicine Vienna, Veterinarplatz 1, A-1210 Vienna, Austria;
Poultry science.Poult Sci.2011 Aug;90(8):1683-9.
The present trial was conducted to study some morphological, digestive, and electrophysiological variables of the small intestine during chronic exposure of broilers to aflatoxin B(1) (AFB(1)). Ross 308 male chicks (7 d old) were randomly allotted to control (no AFB(1)), low AFB(1) (0.07 mg of AFB(1
PMID 21753204

Japanese Journal

P-030 塩味に対する日本人のアミロライド感受性 : 記述検査法による解析(ポスターセッション,2010年度日本味と匂学会第44回大会)

小林哲宏,香山裕喜,鈴木聡恵,宮川博義,井上雅司
日本味と匂学会誌 17(3), 255-258, 2010-12
NAID 110008451329

浸透圧変化によるモルモット気道上皮イオントランスポートの反応性の検討

服部知洋,馬島徹,橋本修
アレルギー 59(8), 974-983, 2010-08-30
… 化による反応性を検討した.【方法】高張食塩水及びマンニトール負荷による影響をopen circuit potential differenceを測定することにより検討した.【結果】0.9-10.8%粘膜側高張食塩水負荷で,diphenylamine-2-carboxylate(DPC),amiloride,disodium cromoglycate(DSCG)はpotential difference(PD)の増加を抑制した.1.8%粘膜側高張食塩水単独負荷でPDの増加を認めたが,585mOsm/kgH_2O粘膜側マンニトール単独負荷では増加を認めず,Cl-free溶液でも同様であった.1.8%粘膜 …
NAID 110007700754

Related Pictures

Amiloride - Wikipedia Amiloride, 5-(N,N-Dimethyl)-, hydrochloride | CAS 1214-79-5 (free base) | SCBT - Santa Amiloride; alphapharm brand of amiloride hydrochloride; amidal; amiduret trom 5-(N-Ethyl-N-isopropyl)-Amiloride | CAS 1154-25-2 | SCBT - Santa Cruz Biotechnology 12.01.2 Diuretics for Hypertension - Pharmacology in one semester Amiloride • HCl | CAS 2016-88-8 | SCBT - Santa Cruz Biotechnology Diuretic Stock Vectors, Images & Vector Art | Shutterstock

★リンクテーブル★

リンク元	「利尿薬」「アミロライド」

「利尿薬」

Amiloride
Systematic (IUPAC) name
	3,5-diamino-6-chloro-N-(diaminomethylene)pyrazine-2-carboxamide
Clinical data
Trade names	Midamor
AHFS/Drugs.com	monograph
Pregnancy cat.	B (US)
Legal status	℞-only (US)
Routes	oral
Pharmacokinetic data
Bioavailability	Readily absorbed
Metabolism	none
Half-life	6 to 9 hours
Excretion	unchanged in urine
Identifiers
CAS number	2016-88-8
ATC code	C03DB01
PubChem	CID 16231
IUPHAR ligand	2421
DrugBank	DB00594
ChemSpider	15403
UNII	7M458Q65S3
KEGG	D07447
ChEBI	CHEBI:2639
ChEMBL	CHEMBL945
Chemical data
Formula	C6H8ClN7O
Mol. mass	229.627 g/mol
	SMILES Clc1nc(C(=O)\N=C(/N)N)c(nc1N)N;
	InChI InChI=1S/C6H8ClN7O/c7-2-4(9)13-3(8)1(12-2)5(15)14-6(10)11/h(H4,8,9,13)(H4,10,11,14,15) ; Key:XSDQTOBWRPYKKA-UHFFFAOYSA-N ;
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