WordNet

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

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/06/29 11:25:16」(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'

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UpToDate Contents

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1. 利尿剤とカルシウムバランス diuretics and calcium balance
2. 成人における高カリウム血症の原因および評価 causes and evaluation of hyperkalemia in adults
3. 利尿剤の作用機序 mechanism of action of diuretics
4. リチウムの腎毒性 renal toxicity of lithium
5. 腎集合管ナトリウムチャンネルの遺伝的障害：リドル症候群および偽性低アルドステロン症1型 genetic disorders of the collecting tubule sodium channel liddles syndrome and pseudohypoaldosteronism type 1

English Journal

Simultaneous determination of atenolol and amiloride by capillary electrophoresis with capacitively coupled contactless conductivity detection (c(4)d).

Azzam KM, Aboul-Enein HY.SourceSchool of Chemical Sciences, Universiti Sains Malaysia, Penang, Malaysia.
Methods in molecular biology (Clifton, N.J.).Methods Mol Biol.2013;919:67-78.
Capillary electrophoresis coupled with a capacitively coupled contactless conductivity detector (CE-C(4)D) has been employed for the determination of the β-blocker drugs (atenolol and amiloride) in pharmaceutical formulations. 150 mM acetic acid was used as background electrolyte. The influence of
PMID 22976091

Stress response to high osmolarity in Trypanosoma cruzi epimastigotes.

Bonansea S, Usorach M, Gesumaría MC, Santander V, Gimenez AM, Bollo M, Machado EE.SourceQuímica biológica, Facultad de Ciencias Exactas, Físico-Químicas y Naturales, Universidad Nacional de Río Cuarto, 5800 Río Cuarto, Córdoba, Argentina.
Archives of biochemistry and biophysics.Arch Biochem Biophys.2012 Nov 1;527(1):6-15. doi: 10.1016/j.abb.2012.07.014. Epub 2012 Aug 2.
Trypanosoma cruzi undergoes differentiation in the rectum of triatomine, where increased osmolarity is caused mainly by elevated content of NaCl from urine. Early biochemical events in response to high osmolarity in this parasite have not been totally elucidated. In order to clarify the relationship
PMID 22884762

Japanese Journal

SHR-SPの味神経感受性の加齢に伴う低下

長田和実,駒井三千夫,BRYANT Bruce P.,鈴木均,角田健司,古川勇次
The journal of veterinary medical science 65(3), s・vi-s・vii, 313-317, 2003-03-25
ラットの味神経応答が老若群間で差があるかどうかを明らかにするために,鼓索神経(舌の前方3分の2の領域の味情報を伝える)の神経応答を測定した.実験には老若両群のSHR-SP(脳卒中易発症ラット)を用い,味溶液として250mM NH4Cl,100mM NaCl,100mM KCl, 500mM ショ糖,20mM塩酸キニーネ,10mM HCl,10mMグルタミン酸ナトリウム(MSG), 10mMグルタミ …
NAID 110003947926

未熟心筋の虚血再潅流傷害に対するamiloride誘導体(amiloride, 5-(N, N-dimethyl)hydrochloride)の保護効果 : 口述発表 : 第57回日本循環器学会学術集会

小池明,加藤聡,秋田利明,阿部稔雄,児玉逸雄,外山淳治
Japanese circulation journal 57(SupplementI), 175, 1993-03-01
NAID 110002596509

「アミロライド」

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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