Amiloride

Name: Amiloride

What should I do if I forget a dose?

Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.

Amiloride Interactions

Do not use salt substitutes or low-sodium milk products that contain potassium. These products could cause your potassium levels to get too high while you are taking amiloride.

Avoid a diet high in salt. Too much salt will cause your body to retain water and can make this medication less effective.

Drinking alcohol with this medicine can cause side effects.

Avoid becoming overheated or dehydrated during exercise, in hot weather, or by not drinking enough fluids. Follow your doctor's instructions about the type and amount of liquids you should drink. In some cases, drinking too much liquid can be as unsafe as not drinking enough.

Tell your doctor about all your current medicines and any you start or stop using, especially:

  • lithium;
  • medicine to prevent organ transplant rejection--cyclosporine, tacrolimus;
  • an ACE inhibitor (angiotensin converting enzyme)--benazepril, captopril, enalapril, fosinipril, lisinopril, moexipril, perindopril, quinapril, ramipril, or trandolapril;
  • heart or blood pressure medication--azilsartan, candesartan, eprosartan, irbesartan, losartan, olmesartan, telmisartan, valsartan; or
  • NSAIDs (nonsteroidal anti-inflammatory drugs)--aspirin, ibuprofen (Advil, Motrin), naproxen (Aleve), celecoxib, diclofenac, indomethacin, meloxicam, and others.

This list is not complete. Other drugs may interact with amiloride, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

Amiloride Interactions

Tell your doctor about all the medicines you take including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

  • ACE inhibitors such as benazepril (Lotensin), captopril (Capoten), enalapril (Vasotec), fosinopril (Monopril), lisinopril (Prinivil, Zestril), quinapril (Accupril), ramipril (Altace) and others
  • angiotensin II receptor blockers (ARBs) such as azilsartan (Edarbi), candesartan (Atacand), eprosartan (Teveten), irbesartan (Avapro), losartan (Cozaar), olmesartan (Benicar), telmisartan (Micardis) and valsartan (Diovan)
  • cyclosporine (Gengraf, Neoral, Sandimmune)
  • tacrolimus (Prograf)
  • other medications for high blood pressure
  • nonsteroidal anti-inflammatory medications such as ibuprofen (Motrin, Nuprin) or naproxen (Aleve), and others
  • lithium (Eskalith, Lithobid)
  • potassium products including potassium chloride (K-Dur, Klor-Con, Micro-K), potassium citrate (Urocit-K, Polycitra-K), potassium gluconate, potassium phosphate (Neutra-Phos-K, K-Phos)
  • salt substitutes that contain potassium
  • digoxin
  • spironolactone (Aldactone)
  • triamterene 

This is not a complete list of amiloride drug interactions. Ask your doctor or pharmacist for more information.

Amiloride and Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if amiloride crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using amiloride.

 

What should I discuss with my healthcare provider before taking amiloride?

You should not use amiloride if you are allergic to it, or if:

  • you have kidney disease or are unable to urinate;

  • you have problems with your kidneys caused by diabetes;

  • you have high potassium levels (hyperkalemia);

  • you take a potassium supplement; or

  • you take another potassium-sparing diuretic such Moduretic, spironolactone, or triamterene.

To make sure amiloride is safe for you, tell your doctor if you have:

  • diabetes;

  • heart disease;

  • breathing problems;

  • cirrhosis or other liver disease;

  • if you are on a low-salt diet; or

  • if you are severely ill or debilitated.

Amiloride is not expected to be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while using this medicine.

It is not known whether amiloride passes into breast milk or if it could harm a nursing baby. You should not breast-feed while using this medicine.

What are some other side effects of Amiloride?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

  • Loose stools (diarrhea).
  • Headache.
  • Not hungry.
  • Upset stomach or throwing up.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

Consumer Information Use and Disclaimer

  • If your symptoms or health problems do not get better or if they become worse, call your doctor.
  • Do not share your drugs with others and do not take anyone else's drugs.
  • Keep a list of all your drugs (prescription, natural products, vitamins, OTC) with you. Give this list to your doctor.
  • Talk with the doctor before starting any new drug, including prescription or OTC, natural products, or vitamins.
  • Some drugs may have another patient information leaflet. Check with your pharmacist. If you have any questions about this medicine, please talk with your doctor, nurse, pharmacist, or other health care provider.
  • If you think there has been an overdose, call your poison control center or get medical care right away. Be ready to tell or show what was taken, how much, and when it happened.

This information should not be used to decide whether or not to take amiloride or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to amiloride. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.

Review Date: October 4, 2017

Amiloride Description

Amiloride HCl, an antikaliuretic-diuretic agent, is a pyrazine-carbonyl-guanidine that is unrelated chemically to other known antikaliuretic or diuretic agents. It is the salt of a moderately strong base (pKa 8.7). It is designated chemically as 3,5-diamino-6-chloro-N-(diaminomethylene) pyrazinecarboxamide monohydrochloride, dihydrate and has a molecular weight of 302.12. Its empirical formula is C 6H8CIN7O•HCl•2H2O and its structural formula is:


Each tablet for oral administration contains 5 mg of Amiloride HCI, calculated on the anhydrous basis. Each tablet contains the following inactive ingredients: corn starch, crospovidone, lactose, magnesium stearate, microcrystalline cellulose and povidone.

Contraindications

Hyperkalemia

Amiloride HCl tablets should not be used in the presence of elevated serum potassium levels (greater than 5.5 mEq per liter).

Antikaliuretic Therapy or Potassium Supplementation

Amiloride HCl tablets should not be given to patients receiving other potassium-conserving agents, such as spironolactone or triamterene. Potassium supplementation in the form of medication, potassium-containing salt substitutes or a potassium-rich diet should not be used with Amiloride HCl tablets except in severe and/or refractory cases of hypokalemia. Such concomitant therapy can be associated with rapid increases in serum potassium levels. If potassium supplementation is used, careful monitoring of the serum potassium level is necessary.

Impaired Renal Function

Anuria, acute or chronic renal insufficiency, and evidence of diabetic nephropathy are contraindications to the use of Amiloride HCl tablets. Patients with evidence of renal functional impairment (blood urea nitrogen [BUN] levels over 30 mg per 100 mL or serum creatinine levels over 1.5 mg per 100 mL) or diabetes mellitus should not receive the drug without careful, frequent and continuing monitoring of serum electrolytes, creatinine, and BUN levels. Potassium retention associated with the use of an antikaliuretic agent is accentuated in the presence of renal impairment and may result in the rapid development of hyperkalemia.

Hypersensitivity

Amiloride HCl tablets are contraindicated in patients who are hypersensitive to this product.



WARNINGS

Hyperkalemia

Like other potassium-conserving agents, Amiloride may cause hyperkalemia (serum potassium levels greater than 5.5 mEq per liter) which, if uncorrected, is potentially fatal. Hyperkalemia occurs commonly (about 10%) when Amiloride is used without a kaliuretic diuretic. This incidence is greater in patients with renal impairment, diabetes mellitus (with or without recognized renal insufficiency), and in the elderly. When Amiloride is used concomitantly with a thiazide diuretic in patients without these complications, the risk of hyperkalemia is reduced to about 1-2%. It is thus essential to monitor serum potassium levels carefully in any patient receiving Amiloride, particularly when it is first introduced, at the time of diuretic dosage adjustments, and during any illness that could affect renal function.

The risk of hyperkalemia may be increased when potassium-conserving agents, including Amiloride HCl, are administered concomitantly with an angiotensin-converting enzyme inhibitor, an angiotensin II receptor antagonist, cyclosporine or tacrolimus. (See PRECAUTIONS, Drug Interactions.) Warning signs or symptoms of hyperkalemia include paresthesias, muscular weakness, fatigue, flaccid paralysis of the extremities, bradycardia, shock, and ECG abnormalities. Monitoring of the serum potassium level is essential because mild hyperkalemia is not usually associated with an abnormal ECG.

When abnormal, the ECG in hyperkalemia is characterized primarily by tall, peaked T waves or elevations from previous tracings. There may also be lowering of the R wave and increased depth of the S wave, widening and even disappearance of the P wave, progressive widening of the QRS complex, prolongation of the PR interval, and ST depression.

Treatment of hyperkalemia:If hyperkalemia occurs in patients taking Amiloride HCl, the drug should be discontinued immediately. If the serum potassium level exceeds 6.5 mEq per liter, active measures should be taken to reduce it. Such measures include the intravenous administration of sodium bicarbonate solution or oral or parenteral glucose with a rapid-acting insulin preparation. If needed, a cation exchange resin such as sodium polystyrene sulfonate may be given orally or by enema. Patients with persistent hyperkalemia may require dialysis.

Diabetes Mellitus

In diabetic patients, hyperkalemia has been reported with the use of all potassium-conserving diuretics, including Amiloride HCl, even in patients without evidence of diabetic nephropathy. Therefore, Amiloride HCl should be avoided, if possible, in diabetic patients and, if it is used, serum electrolytes and renal function must be monitored frequently.

Amiloride HCl should be discontinued at least 3 days before glucose tolerance testing.

Metabolic or Respiratory Acidosis

Antikaliuretic therapy should be instituted only with caution in severely ill patients in whom respiratory or metabolic acidosis may occur, such as patients with cardiopulmonary disease or poorly controlled diabetes. If Amiloride HCl is given to these patients, frequent monitoring of acid-base balance is necessary. Shifts in acid-base balance alter the ratio of extracellular/intracellular potassium, and the development of acidosis may be associated with rapid increases in serum potassium levels.

Overdosage

No data are available in regard to overdosage in humans.

The oral LD 50 of Amiloride HCl (calculated as the base) is 56 mg/kg in mice and 36 to 85 mg/kg in rats, depending on the strain.

It is not known whether the drug is dialyzable.

The most likely signs and symptoms to be expected with overdosage are dehydration and electrolyte imbalance. These can be treated by established procedures. Therapy with Amiloride HCl should be discontinued and the patient observed closely. There is no specific antidote.Emesis should be induced or gastric lavage performed.Treatment is symptomatic and supportive. If hyperkalemia occurs, active measures should be taken to reduce the serum potassium levels.

Package label principal display

NDC 50268-071-15
Amiloride Hydrochloride Tablets, USP
5mg
Rx Only
50 Tablets (5 X 10) Unit Dose

5026807115

NDC 50268-071-15
Amiloride Hydrochloride Tablets, USP
5mg
Rx Only
50 Tablets (5 X 10) Unit Dose

5026807115

Each tablet contains:
Amiloride HCl, USP.........5 mg*
*(anhydrous equivalent)

Usual Dosage:
Read Accompanying Literature.

Store at 20o - 25oC (68o - 77oF) [see USP Controlled Room Temperature].

KEEP THIS AND ALL MEDICATIONS OUT OF THE REACH OF CHILDREN.

Manufactured for:
AvKARE, Inc.
Pulaski, TN 38478

AvPAK
A PRODUCT OF AvKARE

Mfg. Rev. 02/09  AV Rev. 09/16 (P)

Amiloride HYDROCHLORIDE  
Amiloride hydrochloride tablet
Product Information
Product Type HUMAN PRESCRIPTION DRUG LABEL Item Code (Source) NDC:50268-071(NDC:64980-151)
Route of Administration ORAL DEA Schedule     
Active Ingredient/Active Moiety
Ingredient Name Basis of Strength Strength
Amiloride HYDROCHLORIDE (Amiloride) Amiloride Hydrochloride 5 mg
Inactive Ingredients
Ingredient Name Strength
STARCH, CORN  
CROSPOVIDONE  
LACTOSE  
MAGNESIUM STEARATE  
CELLULOSE, MICROCRYSTALLINE  
POVIDONE  
Product Characteristics
Color yellow Score no score
Shape ROUND Size 8mm
Flavor Imprint Code 5
Contains     
Packaging
# Item Code Package Description
1 NDC:50268-071-15 50 BLISTER PACK in 1 BOX, UNIT-DOSE
1 NDC:50268-071-11 1 TABLET in 1 BLISTER PACK
Marketing Information
Marketing Category Application Number or Monograph Citation Marketing Start Date Marketing End Date
ANDA ANDA079133 01/28/2013
Labeler - AvPAK (832926666)
Revised: 09/2016   AvPAK

Contraindications

Hypersensitivity to amiloride or any component of the formulation; presence of elevated serum potassium levels (>5.5 mEq/L); if patient is receiving other potassium-conserving agents (eg, spironolactone, triamterene) or potassium supplementation (medicine, potassium-containing salt substitutes, potassium-rich diet) except in severe and/or refractory cases of hypokalemia; anuria; acute or chronic renal insufficiency; evidence of diabetic nephropathy. Patients with evidence of renal impairment (blood urea nitrogen [BUN] >30 mg/dL or serum creatinine >1.5 mg/dL) or diabetes mellitus should not receive amiloride without close, frequent monitoring of serum electrolytes and renal function.

Dosing Renal Impairment

Manufacturer's labeling: Use of amiloride in patients with diabetes mellitus, SCr >1.5 mg/dL, or BUN >30 mg/dL should be done with caution and careful monitoring; use is contraindicated in patients with anuria, acute or chronic renal insufficiency, or evidence of diabetic nephropathy.

Alternate recommendations:

CrCl 10 to 50 mL/minute: Administer at 50% of normal dose (Aronoff 2007). The Beers Criteria recommends avoiding use in older adults ≥65 years of age with a CrCl <30 mL/minute due to the risk of hyperkalemia and hyponatremia (Beers Criteria [AGS 2015]).

CrCl <10 mL/minute: Avoid use (Aronoff 2007).

Extemporaneously Prepared

A 1 mg/mL oral suspension may be made with tablets. Crush ten 5 mg tablets in a mortar and reduce to a fine powder. Add small proportions up to 20 mL of Glycerin BP or Glycerin, USP and mix to uniform paste; mix while adding sterile water in incremental proportions to almost 50 mL; transfer to a calibrated bottle, rinse mortar with sterile water, and add quantity of sterile water sufficient to make 50 mL. Label “shake well” and “refrigerate”. Stable for 21 days.

Nahata MC, Pai VB, and Hipple TF, Pediatric Drug Formulations, 5th ed, Cincinnati, OH: Harvey Whitney Books Co, 2004.

Usual Adult Dose for Edema

Initial dose: 5 mg orally once a day.
Maintenance dose: 5-10 mg once a day.

Liver Dose Adjustments

Data not available

Dialysis

Data not available

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