Amiloride (Midamor)

Generic Name: Amiloride

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 C6H8ClN7O † HCl † 2H2O and its structural formula is:


amilor

MIDAMOR (Amiloride HCl) is available for oral use as tablets containing 5 mg of anhydrous amiloride HCl. Each tablet contains the following inactive ingredients: calcium phosphate, D&C Yellow 10, iron oxide, lactose, magnesium stearate and starch.

No health feed found.

Amiloride works by inhibiting sodium reabsorption in the distal convoluted tubules and collecting ducts in the kidneys by binding to the amiloride-sensitive sodium channels. This promotes the loss of sodium and water from the body, but without depleting potassium. Amiloride exerts its potassium sparing effect through the inhibition of sodium reabsorption at the distal convoluted tubule, cortical collecting tubule and collecting duct; this decreases the net negative potential of the tubular lumen and reduces both potassium and hydrogen secretion and their subsequent excretion. Amiloride is not an aldosterone antagonist and its effects are seen even in the absence of aldosterone.

Amiloride can be used as a monotherapy (single-drug therapy) or an adjunctive therapy alongside other diuretics (e.g. hydrochlorothiazide, furosemide) for the treatment of ascites and edema (swelling) due to cirrhosis of the liver. The 2012 clinical practice guidelines by the American Association for the Study of Liver Diseases (AASLD) states that amiloride can be used to treat ascites in place of spironolactone if it isn't tolerated (e.g. due to the side effect of gynecomastia), though amiloride isn't a preferred drug due to cost and lack of efficacy.

As an adjunct to other diuretics, amiloride can be use to reduce edema due to heart failure or high blood pressure in people that have low blood potassium (hypokalemia) or in people for which maintaining a normal level of potassium is critically important for their health. For example, people that are taking Digitalis (i.e. digoxin) are at higher risk for changes in heart rhythm if their potassium levels get too high. The 2017 clinical practice guidelines of the American College of Cardiology/American Heart Association Task Force on Clinical Practice Guidelines list amiloride as a "secondary" oral antihypertensive, with minimal efficacy. For people with resistant hypertension, already taking a thiazide diuretic, an angiotensin converting enzyme inhibitor (ACE-i) or an angiotensin II receptor blocker (ARB), and a calcium channel blocker, the addition of amiloride (or spironolactone) was better at reducing blood pressure than adding a beta-blocker (bisoprolol) or an alpha-1 blocker (doxazosin). When combined with hydrochlorothiazide, the addition of amiloride had positive effects on blood pressure and blood sugar tolerance. Amiloride may therefore be useful for preventing the metabolic side effects of thiazide diuretics, allowing for the use of higher thiazide doses (in line with how they were originally studied).

Amiloride is also used in the treatment of Liddle syndrome, a rare genetic disorder that causes mutations in the genes that encode for the ENaC channel (where amiloride acts). Because Liddle syndrome usually involves an upregulation of ENaC channels, leading to hypokalemia, amiloride is a useful as an ENaC channel inhibitor due to its potassium-sparing effects, restoring potassium to normal levels.

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

  • Abdominal pain
  • confusion
  • difficulty with breathing
  • irregular heartbeat
  • nausea or vomiting
  • nervousness
  • numbness or tingling in the hands, feet, or lips
  • shortness of breath
  • weakness or heaviness of the legs

Less common

  • Agitation
  • back pain
  • blurred vision
  • coma
  • dizziness
  • drowsiness
  • fever
  • hallucinations (seeing things that aren't there)
  • headache
  • irritability
  • labored breathing
  • mood or mental changes
  • seizures (convulsions)
  • stiff neck
  • tightness in the chest
  • unusual tiredness or weakness
  • vomiting
  • wheezing

Rare

  • Arm or jaw pain
  • bloody or black, tarry stools
  • burning while urinating
  • burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings
  • change in vision
  • chest pain, discomfort, or heaviness
  • chills
  • clay-colored stools
  • cold sweats
  • constipation
  • dark urine
  • difficult or painful urination
  • dizziness, faintness, or lightheadedness when getting up from a lying or sitting position suddenly
  • fainting
  • fast, pounding, racing, or slow heartbeat or pulse
  • itching
  • light-colored stools
  • loss of appetite
  • loss of vision
  • rash
  • shakiness in the legs, arms, hands, or feet
  • stomach pain, severe
  • sweating
  • trembling or shaking of the hands or feet
  • unpleasant breath odor
  • vomiting of blood or material that looks like coffee grounds
  • yellow eyes or skin

Incidence not known

  • Continuing stomach pain
  • cough
  • lower back or side pain
  • pale skin
  • sore throat
  • sores, ulcers, or white spots on the lips or in the mouth
  • swollen or painful glands
  • unusual bleeding or bruising

Get emergency help immediately if any of the following symptoms of overdose occur:

Symptoms of overdose

  • Decreased urination
  • dry mouth
  • increase in heart rate
  • lightheadedness
  • muscle cramps or pain
  • pain or weakness in the hands or feet
  • rapid breathing
  • sunken eyes
  • thirst
  • wrinkled skin

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

  • Diarrhea
  • weight loss

Less common

  • Changes in appetite
  • decreased interest in sexual intercourse
  • inability to have or keep an erection
  • loss in sexual ability, desire, drive, or performance

Rare

  • Acid or sour stomach
  • belching
  • continuing ringing or buzzing or other unexplained noise in the ears
  • discouragement
  • disturbed color perception
  • double vision
  • excess air or gas in the stomach or intestines
  • feeling of constant movement of self or surroundings
  • feeling sad or empty
  • frequent urination
  • full or bloated feeling
  • hair loss or thinning of hair
  • hearing loss
  • increased need to urinate
  • increased volume of pale, dilute urine
  • indigestion
  • joint pain
  • leg ache or pain
  • loss of interest or pleasure
  • neck or shoulder ache
  • night blindness
  • overbright appearance of lights
  • pain in the chest below the breastbone
  • passing of gas
  • passing urine more often
  • pressure in the stomach
  • seeing halos around lights
  • sensation of spinning
  • sleepiness or unusual drowsiness
  • sleeplessness
  • stomach fullness, discomfort, or upset
  • stuffy nose
  • swelling of abdominal or stomach area
  • swelling of the breasts or breast soreness in both females and males
  • trouble concentrating
  • trouble sleeping
  • tunnel vision
  • unable to sleep

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (tablets):
    • For hypertension or edema:
      • Adults—5 milligrams (mg) once a day. Your doctor may increase your dose if needed.
      • Children—Use and dose must be determined by your doctor .

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

  • Eplerenone
  • Triamterene

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Aceclofenac
  • Acemetacin
  • Alacepril
  • Amtolmetin Guacil
  • Arginine
  • Arsenic Trioxide
  • Aspirin
  • Benazepril
  • Bromfenac
  • Bufexamac
  • Bupropion
  • Captopril
  • Celecoxib
  • Choline Salicylate
  • Cilazapril
  • Clonixin
  • Delapril
  • Dexibuprofen
  • Dexketoprofen
  • Diclofenac
  • Diflunisal
  • Dipyrone
  • Dofetilide
  • Droperidol
  • Droxicam
  • Enalaprilat
  • Enalapril Maleate
  • Etodolac
  • Etofenamate
  • Etoricoxib
  • Felbinac
  • Fenoprofen
  • Fepradinol
  • Feprazone
  • Floctafenine
  • Flufenamic Acid
  • Flurbiprofen
  • Fosinopril
  • Ibuprofen
  • Imidapril
  • Indomethacin
  • Ketoprofen
  • Ketorolac
  • Levomethadyl
  • Lisinopril
  • Lornoxicam
  • Loxoprofen
  • Lumiracoxib
  • Meclofenamate
  • Mefenamic Acid
  • Meloxicam
  • Moexipril
  • Morniflumate
  • Nabumetone
  • Naproxen
  • Nepafenac
  • Niflumic Acid
  • Nimesulide
  • Nimesulide Beta Cyclodextrin
  • Oxaprozin
  • Oxyphenbutazone
  • Parecoxib
  • Pentopril
  • Perindopril
  • Phenylbutazone
  • Piketoprofen
  • Piroxicam
  • Potassium
  • Pranoprofen
  • Proglumetacin
  • Propyphenazone
  • Proquazone
  • Quinapril
  • Ramipril
  • Rofecoxib
  • Salicylic Acid
  • Salsalate
  • Sodium Salicylate
  • Sotalol
  • Spirapril
  • Sulindac
  • Temocapril
  • Tenoxicam
  • Tiaprofenic Acid
  • Tolfenamic Acid
  • Tolmetin
  • Trandolapril
  • Trimethoprim
  • Valdecoxib
  • Zofenopril

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

  • Carbenoxolone
  • Gossypol
  • Licorice
  • Quinidine

Other Interactions

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following may cause an increased risk of certain side effects but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

  • Potassium Containing Food

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

  • Diabetes or
  • Hyperkalemia (high potassium in the blood) or
  • Kidney disease (e.g., anuria or diabetic nephropathy)—Should not be used in patients with these conditions .
  • Heart disease or
  • Liver disease, severe (e.g., cirrhosis or hepatic encephalopathy) or
  • Lung disease—Use with caution. May increase the chance of side effects .

Many patients who have high blood pressure will not notice any signs of the problem. In fact, many may feel normal. It is very important that you take your medicine exactly as directed and that you keep your appointments with your doctor even if you feel well .

Remember that this medicine will not cure your high blood pressure, but it does help control it. You must continue to take it as directed if you expect to lower your blood pressure and keep it down. You may have to take high blood pressure medicine for the rest of your life. If high blood pressure is not treated, it can cause serious problems such as heart failure, blood vessel disease, stroke, or kidney disease .

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of amiloride in the pediatric population. Safety and efficacy have not been established .

Geriatric

Appropriate studies performed to date have not demonstrated geriatrics-specific problems that would limit the usefulness of amiloride in the elderly. However, elderly patients are more likely to have age-related liver, kidney, or heart problems, which may require an adjustment in the dose for patients receiving amiloride .

Pregnancy

Animal studies have revealed no evidence of harm to the fetus, however, there are no adequate studies in pregnant women OR animal studies have shown an adverse effect, but adequate studies in pregnant women have failed to demonstrate a risk to the fetus.

Breastfeeding

Studies suggest that this medication may alter milk production or composition. If an alternative to this medication is not prescribed, you should monitor the infant for side effects and adequate milk intake.

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