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{{drugbox
__NOTOC__
| IUPAC_name = 3,5-diamino-6-chloro-N- (diaminomethylidene)pyrazine-2-carboxamide
{{Amiloride}}
| image = Amiloride structure_svg.png
{{CMG}}; {{AE}} {{SS}}
| width=250px
| CAS_number = 2016-88-8
| ATC_prefix = C03
| ATC_suffix = DB01
| ATC_supplemental =
| PubChem = 16231
| DrugBank = APRD00790
| C=6 | H=8 | Cl=1 | N=7 | O=1
| molecular_weight = 229.627 g/mol
| bioavailability = Readily absorbed
| protein_bound =
| metabolism = none
| elimination_half-life = 6 to 9 hours
| excretion = unchanged in urine
| pregnancy_category =
| legal_status =
| routes_of_administration = oral
}}
{{SI}}
{{CMG}}


'''''For patient information about Amiloride, click [[Amiloride (patient information)|here]].'''''


{{SB}} MIDAMOR<sup>®</sup>
==Overview==


'''Amiloride''' is a [[potassium-sparing diuretics|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''' is a [[potassium-sparing diuretics|potassium-sparing diuretic]], first approved for use in 1967 (then known as MK 870), used in the management of [[hypertension]] and [[congestive heart failure]].  
==Category==
Potassium-sparing diuretics;Aminopyrazines;Guanidines;World Health Organization essential medicines;Cardiovascular Drugs
==FDA Package Insert==
====MIDAMOR (amiloride hydrochloride) tablet ====


==Structure==
'''  [[Amiloride indications and usage|Indications and Usage]]'''
Amiloride is a [[guanidine|guanidinium]] group containing [[pyrazine]] [[derivative (chemistry)|derivative]].
'''| [[Amiloride dosage and administration|Dosage and Administration]]'''
'''| [[Amiloride dosage forms and strengths|Dosage Forms and Strengths]]'''
'''| [[Amiloride contraindications|Contraindications]]'''
'''| [[Amiloride warnings and precautions|Warnings and Precautions]]'''
'''| [[Amiloride adverse reactions|Adverse Reactions]]'''
'''| [[Amiloride drug interactions|Drug Interactions]]'''
'''| [[Amiloride use in specific populations|Use in Specific Populations]]'''
'''| [[Amiloride overdosage|Overdosage]]'''
'''| [[Amiloride description|Description]]'''
'''| [[Amiloride clinical pharmacology|Clinical Pharmacology]]'''
'''| [[Amiloride nonclinical toxicology|Nonclinical Toxicology]]'''
'''| [[Amiloride clinical studies|Clinical Studies]]'''
'''| [[Amiloride how supplied storage and handling|How Supplied/Storage and Handling]]'''
'''| [[Amiloride patient counseling information|Patient Counseling Information]]'''
'''| [[Amiloride labels and packages|Labels and Packages]]'''
==Mechanism of Action==


==Mode of action==
Amiloride works by directly blocking the [[epithelial sodium channel]] (ENaC) thereby inhibiting [[sodium]] reabsorption in the late [[distal convoluted tubule]]s, connecting tubules, and collecting ducts in the [[kidney]]s (this mechanism is the same for [[triamterene]]).<ref>{{cite journal | author = Loffing, Johannes and Kaissling, Brigitte | title = Sodium and calcium transport pathways along the mammalian distal nephron: from rabbit to human | journal = Am J Physiol Renal Physiol | pages = F628–F643| year = 2003 | pmid = 12620920 | volume = 284 | doi=10.1152/ajprenal.00217.2002 | issue=4}}</ref> 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 diuretic]]s (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 inhibitor]]s or [[spironolactone]]. Patients are also advised not to use potassium-containing salt replacements.<ref>LoSalt [http://www.losalt.com/docs/lo_salt_web_advice.pdf Advisory Statement] (PDF)</ref> Amiloride also carries the risk of developing an [[acidosis]].
Amiloride works by directly blocking the [[epithelial sodium channel]] (ENaC) thereby inhibiting [[sodium]] reabsorption in the [[distal convoluted tubule]]s and collecting ducts in the [[kidney]]s (this mechanism is the same for [[triamterene]]). 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 diuretic]]s (e.g. [[co-amilofruse]]). Due to its potassium-sparing capacities, [[hyperkalemia]] (high blood potassium levels) are occasionally observed in patients taking amiloride. The risk is high in concurrent use of [[ACE inhibitor]]s or [[spironolactone]]. Patients are also advised not to use potassium-containing salt replacements.<ref>LoSalt [http://www.losalt.com/docs/lo_salt_web_advice.pdf Advisory Statement] (PDF)</ref>


A fraction of the effects of amiloride is inhibition of [[cyclic GMP-gated cation channel]]s in the [[inner medullary collecting duct]].<ref name=boron875> {{cite book |author=Walter F., PhD. Boron |title=Medical Physiology: A Cellular And Molecular Approaoch |publisher=Elsevier/Saunders |location= |year= |pages= |isbn=1-4160-2328-3 |oclc= |doi=}} page 875 </ref>


==References==
==References==
<references/>
{{reflist|2}}
 


{{Antihypertensives and diuretics}}
{{Sodium channel blockers}}
{{Diuretics}}


[[Category:Potassium-sparing diuretics]]
[[Category:Potassium-sparing diuretics]]
[[Category:Pyrazines]]
[[Category:Aminopyrazines]]
[[Category:Guanidines]]
[[Category:Guanidines]]
[[Category:World Health Organization essential medicines]]
[[Category:Cardiovascular Drugs]]
[[Category:Drugs]]
[[Category:Drugs]]
[[de:Amilorid]]
[[fr:Amiloride]]
[[hr:Amilorid]]
[[hu:Amilorid]]
[[ja:アミロライド]]
[[pt:Amilorida]]
[[th:อะมิโลไรด์]]
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Revision as of 03:57, 26 February 2014

Amiloride
MIDAMOR® FDA Package Insert
Indications and Usage
Dosage and Administration
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
How Supplied/Storage and Handling
Clinical Trials on Amiloride
ClinicalTrials.gov

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Sheng Shi, M.D. [2]

For patient information about Amiloride, click here.

Synonyms / Brand Names: MIDAMOR®

Overview

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.

Category

Potassium-sparing diuretics;Aminopyrazines;Guanidines;World Health Organization essential medicines;Cardiovascular Drugs

FDA Package Insert

MIDAMOR (amiloride hydrochloride) tablet

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

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).[1] 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.[2] Amiloride also carries the risk of developing an acidosis.


References

  1. 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 (4): F628–F643. doi:10.1152/ajprenal.00217.2002. PMID 12620920.
  2. LoSalt Advisory Statement (PDF)

Template:Sodium channel blockers Template:Diuretics