Amiloride
Drug Info:
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Amiloride
Brand names: Midamor®
Chemical formula:
Amiloride Hydrochloride Oral tablet
What is this medicine?
AMILORIDE (a MIL oh ride) is a diuretic. It helps you make more urine and to lose excess water from your body. This medicine is used in combination with other medicines to treat high blood pressure or congestive heart failure.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•diabetes
•high levels of potassium in the blood
•kidney or liver disease
•an unusual or allergic reaction to amiloride, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take with food. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on the advice of your doctor or health care professional.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is less than four hours to your next dose, take only that dose. Do not take double or extra doses.What may interact with this medicine?
Do not take this medicine with any of the following medications:
•eplerenone
•potassium sparing diuretics like spironolactone and triamterene
•quinidine
This medicine may also interact with the following medications:
•antiinflammatory drugs, NSAIDs like ibuprofen
•cyclosporine
•lithium
•medicines for high blood pressure or heart failure
•potassium supplements
•tacrolimus
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular checks on your progress. Check your blood pressure as directed. Ask your doctor what your blood pressure should be, and when you should contact them.
You may need to be on a special diet while taking this medicine. Ask your doctor. Also, ask how many glasses of fluid you need to drink a day. You must not get dehydrated.
You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•chest pain
•confusion
•dark urine
•fast or irregular heartbeat
•nervousness
•numbness, tingling in hands or feet
•trouble passing urine
•unusually weak or tired
•weakness or heaviness of legs
•yellowing of the eyes or skin
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•change in sex drive or performance
•constipation, or diarrhea
•headache
•loss of appetite
•muscle cramps
•nausea, vomiting
•stomach pain
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
Keep out of the reach of children.
Store at room temperature below 30 degrees C (86 degrees F). Protect from moisture, freezing and excessive heat. Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
Related Videos:
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Amiloride
Oxford Dictionary of Biochemistry:
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amiloride
N-amidino-3,5-diamino-6-chloropyrazinecarboxamide; a potent and specific inhibitor of Na+ entry into cells. It inhibits Na+, K+-ATPase at low concentrations. It is used as a potassium-sparing diuretic.
| amidorphin, amidorphin, amidophosphoribosyltransferase | |
| amine, amine oxidase, aminergic |
Wikipedia on Answers.com:
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Amiloride
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| 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 | eMolecules & PubChem |
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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]
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Contents
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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)
See also
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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Oxford Dictionary of Biochemistry
Oxford University Press. Oxford Dictionary of Biochemistry and Molecular Biology © 1997, 2000, 2006 All rights reserved.
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Saunders Veterinary Dictionary
Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.
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