Aldactone

Follow your doctor's directions for your meals, including advice for a reduced-salt (sodium) diet and daily exercise program. Avoid potassium-containing salt substitutes while you are taking this medication. Talk with your doctor about the amount of potassium-rich foods (e.g., bananas, prunes, raisins, and orange juice) that you may have in your diet.

Yes

Dosage Forms & Strengths

tablet

• 25mg
• 50mg
• 100mg

PO suspension (CaroSpir)

• 5mg/mL

Primary Hyperaldosteronism

Tablet only

Diagnostic agent

• Long test: 400 mg PO qDay for 3-4 weeks
• Short test: 400 mg PO qDay for 4 days

Short-term perioperative treatment for adrenalectomy

• 100-400 mg PO qDay in preparation for surgery initially
• Maintain lowest effective dose individualized for patient

Edematous Conditions

Cirrhosis of the liver with edema and/or ascites; nephrotic syndrome

Tablet

• 100 mg qDay or divided q12hr for 5 days initially; then adjust does based on patient response; if no clinical response, add second diuretic with more specific mechanism of action
• Range: 25-200 mg PO qDay or divided q12hr

PO suspension

• 75 mg PO qDay or divided doses initially; if sole therapy, administer for ≥5 days before increasing dose to obtain effect

Essential Hypertension

Adjunctive therapy for hypertension, to lower blood pressure

Tablet: 25-100mg PO qDay or divided q12hr initially; may adjust dosage to patient response q2weeks

PO suspension

• 20-75 mg PO qDay or divided doses initially; may adjust dosage to patient response q2weeks
• See Dosing Considerations

Congestive Heart Failure

Indicated for NYHA class II/IV heart failure (provided CrCl >30 mL/min and serum K <5 mEq/dL)

ACC/AHA guidelines recommend aldosterone antagonist to be added to an ACE inhibitor or ARB, plus a beta-blocker; patient conditions may also require additional medications (eg, loop diuretics, hydralazine, nitrates, digoxin)

Tablet

• 12.5-25 mg PO qDay initially
• Range: 25mg/day PO initially if serum potassium ≤5 mEq/L and serum creatinine ≤2.5 mg/dL; if tolerated, may increase to 50 mg/day as clinically indicated; if 25 mg/day not tolerated, reduce frequency to every other day

PO suspension

• 20 mg PO qDay; if initial 20 mg dose is tolerated, dosage can be increased to 37.5 mg as clinically indicated

Hypokalemia

Range: 25-100 mg PO qDay

Hirsutism (Off-label)

Women with hirsutism

50-200 mg PO qDay or divided q12hr

Acne (Off-label)

Females with hormonal acne

50-200 mg PO qDay or divided q12hr

Dosing Modifications

Renal impairment

• PO suspension for treatment of patients who develop hyperkalemia on 20 mg PO qDay may reduce dose to 20 mg qOD
• PO suspension for treatment of CHF
  • CrCl 30-50 mL/min/1.73m²: 10 mg PO qDay initially owing to risk of hyperkalemia
• tablet
  • CrCl ≥50 mL/min/1.73 m²: 12.5-25 mg qDay; use maintenance dose of 25 mg qDay or q12hr after 4 weeks of treatment with potassium ≤5 mEq/L
  • CrCl 30-49 mL/min/1.73 m²: 12.5 mg qDay or every other day; use maintenance dose of 12.5-25 mg qDay after 4 weeks of treatment with potassium ≤5 mEq/L
  • CrCl <30 mL/min/1.73 m²: Avoid use

Overdose Management

May use normal saline for volume replacement

May use dopamine or norepinephrine to treat hypotension

Treat hyperkalemia with IV glucose (dextrose 25% in water), concurrently with rapid-acting insulin and IV sodium bicarbonate; oral/rectal solutions of Kayexalate in sorbitol can be used if needed

If dysrhythmia due to decreased K+ or Mg+ suspected, replace aggressively

Discontinue treatment if no symptoms after 6 hr

Dosing Considerations

Oral formulation

• PO suspension formulation is not therapeutically equivalent to tablet
• If PO suspension requires a dose titration >100 mg, use tablet
• For hypertension: Doses >75 mg/day may not provide additional reductions in blood pressure

Dosage Forms & Strengths

tablet

• 25mg
• 50mg
• 100mg

Edema (Off-label)

CHF, cirrhosis, ascites, and nephrotic syndrome

1-3.3 mg/kg/day PO or divided q12hr; not to exceed 3.3 mg/kg/day or up to 100 mg/day 

Hypertension (Off-label)

Among therapeutic options recommended by the National High Blood Pressure Education Program Working Group on High Blood Pressure in Children and Adolescents

1-3.3 mg/kg/day PO or divided q12hr; not to exceed 3.3 mg/kg/day or 100 mg/day 

Hyperaldosteronism (Orphan)

Orphan designation for primary hyperaldosteronism

Sponsor

• CMP Pharma, Inc; PO Box 147, 8026 US Highway 264A; Farmville, NC 27828

Diuresis

12.5 mg PO qDay in 1-2 divided doses; increase by 25-50 mg q5Days PRN; adjust for renal impairment

Hyperaldosteronism

Initial: 400 mg/day PO, THEN

100-300 mg/day

Congestive heart failure

Indicated for NYHA class II/IV heart failure (provided CrCl >30 mL/min and serum K <5 mEq/dL)

25 mg PO qDay initially if serum potassium ≤5 mEq/L and serum creatinine ≤2.5 mg/dL

If initial dose is tolerated, may increase to 50 mg/day as clinically indicated; if not tolerated, reduce frequency to 25 mg qOD

ACC/AHA guidelines recommend aldosterone antagonist to be added to an ACE inhibitor or ARB, plus a beta-blocker; patient conditions may also require additional medications (eg, loop diuretics, hydralazine, nitrates, digoxin)

Dosing considerations

Caution with heart failure and avoid with CrCl <30 mL/min (Beers criteria)

In heart failure, the risk of hyperkalemia is higher in older adults, especially if taking >25 mg/day or with concomitant NSAID, ACE inhibitor, ARB, or potassium supplement

ALDACTONE 25 mg tablets are round, light yellow, film-coated, with SEARLE and 1001 debossed on one side and ALDACTONE and 25 on the other side, supplied as:

ALDACTONE 50 mg tablets are oval, light orange, scored, film-coated, with SEARLE and 1041 debossed on the scored side and ALDACTONE and 50 on the other side, supplied as:

ALDACTONE 100 mg tablets are round, peach-colored, scored, film-coated, with SEARLE and 1031 debossed on the scored side and ALDACTONE and 100 on the other side, supplied as:

Store below 77°F (25°C).

Distributed by: G.D. Searle LLC, Division of Pfizer Inc, NY, NY 10017. Revised: Oct 2016

Potassium Supplementation

Potassium supplementation, either in the form of medication or as a diet rich in potassium, should not ordinarily be given in association with ALDACTONE therapy. Excessive potassium intake may cause hyperkalemia in patients receiving ALDACTONE (see PRECAUTIONS: General).

Concomitant administration of ALDACTONE with the following drugs or potassium sources may lead to severe hyperkalemia:

• other potassium-sparing diuretics
• ACE inhibitors
• angiotensin II antagonists
• aldosterone blockers
• non-steroidal anti-inflammatory drugs (NSAIDs), e.g., indomethacin
• heparin and low molecular weight heparin
• other drugs or conditions known to cause hyperkalemia
• potassium supplements
• diet rich in potassium
• salt substitutes containing potassium

ALDACTONE should not be administered concurrently with other potassium-sparing diuretics. ALDACTONE, when used with ACE inhibitors or indomethacin, even in the presence of a diuretic, has been associated with severe hyperkalemia. Extreme caution should be exercised when ALDACTONE is given concomitantly with these drugs.

Hyperkalemia In Patients With Severe Heart Failure

Hyperkalemia may be fatal. It is critical to monitor and manage serum potassium in patients with severe heart failure receiving ALDACTONE. Avoid using other potassium-sparing diuretics. Avoid using oral potassium supplements in patients with serum potassium > 3.5 mEq/L. RALES excluded patients with a serum creatinine > 2.5 mg/dL or a recent increase in serum creatinine > 25%. The recommended monitoring for potassium and creatinine is one week after initiation or increase in dose of ALDACTONE, monthly for the first 3 months, then quarterly for a year, and then every 6 months.

Discontinue or interrupt treatment for serum potassium > 5 mEq/L or for serum creatinine > 4 mg/dL. (See Clinical Studies: Severe heart failure, and DOSAGE AND ADMINISTRATION: Severe heart failure.) ALDACTONE should be used with caution in patients with impaired hepatic function because minor alterations of fluid and electrolyte balance may precipitate hepatic coma.

Lithium generally should not be given with diuretics (see DRUG INTERACTIONS).

Serious side effects may occur. See "Drug Precautions" section.

Common side effects include:

• diarrhea
• cramping
• nausea
• vomiting
• impotence
• irregular menstruation
• bleeding after menopause
• fever
• rash
• confusion
• headache
• drowsiness
• tiredness

This is not a complete list of Aldactone side effects. Ask your doctor or pharmacist for more information.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Serious side effects can occur including:

• electrolyte imbalance. This medication may affect electrolytes including sodium and potassium. Your doctor will check these levels using a blood test. Warning signs of electrolyte imbalance include:
  • dry mouth
  • thirst
  • weakness
  • lack of energy
  • drowsiness
  • restlessness
  • muscle pains or cramps
  • muscle fatigue
  • low blood pressure
  • decreased urination
  • fast heart rate
  • nausea and vomiting
• worsening of kidney disease
• breast enlargement in men

This medication may cause drowsiness or dizziness. Do not drive or operate heavy machinery until you know how it affects you.

Do not take Aldactone if you:

• are allergic to Aldactone or any other ingredients in Aldactone 
• are not able to produce urine
• have severe kidney disease
• have high potassium levels

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

The active metabolite of Aldactone has been detected in human breast milk. Because of the possibility for adverse reactions in nursing infants from Aldactone, a choice should be made whether to stop nursing or to stop use of Aldactone. The importance of the drug to the mother should be considered.

• Take Aldactone exactly as prescribed.
• This medication comes in tablet form and is usually taken once or twice daily.
• Aldactone can be taken with or without food.
• Because Aldactone increases urination, it is best taken in the morning to avoid having to get up in the night to urinate. If you take it more than once a day, take your last dose by late afternoon.
• If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

General

Hypertension

• Carefully monitor BP during initial titration or subsequent upward dosage adjustment.500 501

• Goal is to achieve and maintain optimal control of BP; individualize specific target BP based on consideration of multiple factors, including patient age and comorbidities, and currently available evidence from clinical studies.500 501

Administration

Administer orally.256 265

Oral Administration

Administer as single or divided doses; 2 doses daily may be adequate.265

For administration in children†, tablets may be pulverized and administered as an oral suspension in cherry syrup.a

When used with a thiazide diuretic in edema associated with cirrhosis of the liver, administer spironolactone for 2–3 days prior to the thiazide diuretic in order to prevent potassium depletion and precipitation of hepatic coma.a

Dosage

Pediatric Patients

3.3 mg/kg (up to 100 mg) daily as a single dose or in divided doses.a

Alternatively, initial dosage of 60 mg/m2 daily in divided doses.a

Initially, 1 mg/kg daily as a single dose or in 2 divided doses.269 Increase dosage as necessary up to a maximum of 3.3 mg/kg (up to 100 mg) daily as a single dose or in 2 divided doses.269

125–375 mg/m2 in divided doses over 24 hours.a

If serum potassium concentration increases during therapy but decreases when the drug is discontinued, a presumptive diagnosis of primary hyperaldosteronism should be considered.265

Adults

Initially, 100 mg daily in single or divided doses.265 Range: 25–200 mg daily.265

As monotherapy, administer usual initial dosage for ≥5 days; if response is satisfactory, titrate to optimal dosage.265

For management of fluid retention (e.g., edema) associated with heart failure, some experts recommend initiating spironolactone at a low dosage (e.g., 12.5–25 mg once daily) and increasing dosage until urine output increases and weight decreases, generally by 0.5–1 kg daily.524

If response is not satisfactory after initial 5 days of therapy, add a thiazide or loop diuretic.265 Do not adjust spironolactone dosage during combined diuretic therapy.265

Spironolactone 100 mg daily and hydrochlorothiazide 100 mg daily as a single dose or in divided doses.256 Range: spironolactone 25–200 mg daily and hydrochlorothiazide 25–200 mg daily as a single dose or in divided doses.256

Initial use of fixed-combination preparations is not recommended; adjust by administering each drug separately, then use the fixed combination if the optimum maintenance dosage corresponds to the ratio of drugs in the combination preparation.256 Administer separately for subsequent dosage adjustment.256

Usual initial dosage recommended by manufacturer: 50–100 mg daily as a single dose or in divided doses.265 Full hypotensive response may require 2 weeks.265

Some experts recommend usual dosage of 25–50 mg daily.500

Spironolactone 50–100 mg daily and hydrochlorothiazide 50–100 mg daily as a single dose or in divided doses.256

Initial use of fixed-combination spironolactone/hydrochlorothiazide preparations is not recommended; adjust by administering each drug separately, then use the fixed combination if the optimum maintenance dosage corresponds to the ratio of drugs in the combination preparation.256 Administer separately for subsequent dosage adjustment.256

Initially, 25 mg once daily recommended by manufacturer in patients with serum potassium concentration ≤5 mEq/L and Scr ≤2.5 mg/dL.265 If tolerated, may increase dosage to 50 mg once daily as clinically indicated.265 If 25-mg daily dosage not tolerated, may decrease dosage to 25 mg every other day.265

Alternatively, ACCF/AHA recommend 12.5–25 mg once daily initially in patients with serum potassium concentration ≤5 mEq/L and eGFR ≥50 mL/minute per 1.73 m2.524 May increase dosage to 25 mg once or twice daily after 4 weeks if clinically indicated and if serum potassium concentration ≤5 mEq/L and eGFR ≥50 mL/minute per 1.73 m2.524

Monitor closely for hyperkalemia and renal insufficiency.265 (See Hyperkalemia under Cautions.)

Manufacturer recommends holding or discontinuing spironolactone therapy if serum potassium >5 mEq/L or Scr >4 mg/dL.265

ACCF/AHA recommends holding spironolactone therapy if serum potassium >5.5 mEq/L or renal function worsens; consider resuming therapy at reduced dosage following resolution (for ≥72 hours) of hyperkalemia (serum potassium <5 mEq/L) and renal insufficiency.524

Instruct patients to stop therapy with an aldosterone receptor antagonist if they have diarrhea or are dehydrated or if therapy with a concomitant loop diuretic is interrupted.524

400 mg daily for 3–4 weeks.265 Correction of hypokalemia and hypertension provides presumptive evidence for the diagnosis of primary hyperaldosteronism.265

Alternatively, 400 mg daily for 4 days.265 If serum potassium concentration increases during spironolactone therapy but decreases when the drug is discontinued, consider presumptive diagnosis of primary hyperaldosteronism.265

Patients with a definitive diagnosis: 100–400 mg daily before surgery.265

Initially, 400 mg daily.265

Maintenance dosage: 100–300 mg daily.265 Use lowest effective dosage for long-term maintenance therapy.265

25–100 mg daily.265

50–200 mg daily.210 Regression of hirsutism evident within 2 months, maximal within 6 months, and has been maintained for ≥16 months with continued therapy.210

Prescribing Limits

Pediatric Patients

Maximum 3.3 mg/kg (up to 100 mg) daily.269

Adults

Management of fluid retention in heart failure: ACCF/AHA recommends maximum 50 mg daily; higher dosage may be used with close monitoring.524

ACCF/AHA recommends maximum 50 mg daily.524

Special Populations

Renal Impairment

Manufacturer states that spironolactone is contraindicated in patients with anuria, acute renal insufficiency, or substantial impairment of renal excretory function.265

Heart failure patients with eGFR 30–49 mL/minute per 1.73 m2: Initially, 12.5 mg once daily or every other day recommended by ACCF/AHA; maintenance dosage of 12.5–25 mg once daily (after 4 weeks of therapy and if serum potassium is ≤5 mEq/L).524

Heart failure patients with eGFR <30 mL/minute per 1.73 m2: ACCF/AHA states that use may be harmful because of potentially life-threatening hyperkalemia or renal insufficiency.524

Specific Drugs, Foods, and Laboratory Tests

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 spironolactone in the pediatric population. Safety and efficacy have not been established.

Geriatric

No information is available on the relationship of age to the effects of spironolactone in geriatric patients.

Pregnancy

Breast Feeding

Studies in women suggest that this medication poses minimal risk to the infant when used during breastfeeding.

Interactions with Medicines

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
• Captopril
• Celecoxib
• Choline Salicylate
• Cilazapril
• Clonixin
• Delapril
• Dexibuprofen
• Dexketoprofen
• Diclofenac
• Diflunisal
• Digoxin
• Dipyrone
• Droperidol
• Droxicam
• Enalaprilat
• Enalapril Maleate
• Etodolac
• Etofenamate
• Etoricoxib
• Felbinac
• Fenoprofen
• Fepradinol
• Feprazone
• Floctafenine
• Flufenamic Acid
• Flurbiprofen
• Fosinopril
• Ibuprofen
• Imidapril
• Indomethacin
• Ketoprofen
• Ketorolac
• Levomethadyl
• Lisinopril
• Lithium
• 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.

• Digitoxin
• Gossypol
• Licorice

Interactions with Food/Tobacco/Alcohol

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. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

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:

• Addison's disease (adrenal problem) or
• Anuria (not able to pass urine) or
• Hyperkalemia (high potassium in the blood) or
• Kidney disease, severe—Should not be used in patients with these conditions.

• Electrolyte imbalance (eg, low chloride, magnesium, or sodium in the body) or
• Fluid imbalances (caused by dehydration, vomiting, or diarrhea) or
• Liver disease, severe (eg, cirrhosis)—Use with caution. May make these conditions worse.

In addition to the use of this medicine, treatment for your high blood pressure may include weight control and changes in the types of foods you eat, especially foods high in sodium (salt) and potassium. Your doctor will tell you which of these are most important for you. You should check with your doctor before changing your diet.

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.

Dosing

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 edema:
    • Adults—At first, 100 milligrams (mg) per day, taken in either single or divided doses. Your doctor may adjust your dose if needed.
    • Children—Use and dose must be determined by your doctor.
  • For heart failure:
    • Adults—At first, 25 milligrams (mg) once a day. Your doctor may adjust your dose if needed and tolerated.
    • Children—Use and dose must be determined by your doctor.
  • For high blood pressure:
    • Adults—At first, 50 to 100 milligrams (mg) per day, taken in either single or divided doses. Your doctor may adjust your dose if needed.
    • Children—Use and dose must be determined by your doctor.
  • For low potassium in the blood:
    • Adults—25 to 100 milligrams (mg) per day.
    • Children—Use and dose must be determined by your doctor.
  • For too much aldosterone in the body:
    • Adults—400 milligrams (mg) for 4 days, or 400 mg per day for 3 to 4 weeks to diagnose the condition. Then, 100 to 400 mg per day after the diagnosis is confirmed.
    • 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.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly and to decide if you should continue to take it. Blood and urine tests may be needed to check for unwanted effects.

Do not take this medicine together with eplerenone (Inspra®). Using these medicines together may cause serious unwanted effects.

Do not take other medicines unless they have been discussed with your doctor. This especially includes potassium supplements or salt substitutes containing potassium, certain diuretics (such as amiloride, triamterene (Dyazide®, Dyrenium®, Maxzide®, Midamor®, Moduretic®), or other products containing spironolactone (Aldactazide®).

This medicine may cause dizziness, drowsiness, or lightheadedness. Make sure you know how you react to this medicine before you drive, use machines, or do anything else that could be dangerous until you know how this medicine affects you.

Check with your doctor right away if you become sick while taking this medicine, especially if you have severe or continuing nausea, vomiting, or diarrhea that does not stop. These conditions may cause you to lose too much water or salt and may lead to low blood pressure. You can also lose water by sweating, so drink plenty of water during exercise or in hot weather.

This medicine may cause swelling of the breasts (gynecomastia) and breast pain in some patients. If you have questions about this, talk to your doctor.

NDC 0025-1001-31

100 Tablets
Rx only

Aldactone®
spironolactone
tablets, USP

25 mg

Pfizer
Distributed by
G.D. Searle LLC
Division of Pfizer Inc, NY, NY 10017

NDC 0025-1031-31

100 Tablets
Rx only

Aldactone®
spironolactone
tablets, USP

100 mg

Pfizer
Distributed by
G.D. Searle LLC
Division of Pfizer Inc, NY, NY 10017

You should not use spironolactone if you are allergic to it, or if you have kidney disease, high levels of potassium in your blood, or if you are unable to urinate. Do not use potassium supplements or other diuretics while you are taking spironolactone.

Before using this medication, tell your doctor if you have liver disease, or if you use a steroid or another diuretic.

Drinking alcohol can increase certain side effects of spironolactone.

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

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 spironolactone.

Avoid becoming overheated or dehydrated during exercise and in hot weather. 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.

If you are being treated for high blood pressure, keep using this medication even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.

Drinking alcohol can increase certain side effects of spironolactone.

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 spironolactone.

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

Spironolactone may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

Avoid becoming overheated or dehydrated during exercise and in hot weather. 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.

Taking this medicine with other drugs that make you dizzy or lower your blood pressure can worsen these effects. Ask your doctor before taking Aldactone with a narcotic pain medicine, muscle relaxer, or medicine for anxiety or seizures.

Other drugs may interact with spironolactone, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

A decision should be made to discontinue breastfeeding or discontinue the drug, taking into account the importance of the drug to the mother. Excreted into human milk: Yes (as active metabolite)

According to some authorities, use of this drug appears acceptable during breastfeeding.

Mechanism of Action

Aldosterone antagonist with diuretic and antihypertensive effects; competitive binding of receptors at aldosterone-dependent Na-K exchange site in distal tubules results in increased excretion of Na+, Cl-, and water and retention of K+ and H+

Increases testosterone clearance and estradiol production; blocks conversion of potent androgens to weaker ones in peripheral tissues

Absorption

Bioavailability: 73% (tablet)

Onset: 2-4 hr (tablet)

Duration: 2-3 days (tablet)

Peak serum time: 2.6-4.3 hr (tablet); 0.5-1.5 hr (PO suspension); 2.5-5 hr (PO suspension, active metabolite)

A high fat and high calorie meal (57% of the ~1000 kcal of the meal were from fat) increased the bioavailability of spironolactone (as measured by AUC) by ~90%

Distribution

Protein bound: 90%

Metabolism

Metabolized by the liver and kidneys

Metabolites: Canrenone, 7-alpha-thiomethylspirolactone, 6-beta-hydroxy-7-alpha-thiomethylspirolactone (active)

Elimination

Half-life (tablet): 1.3-1.4 hr (parent drug); 16.5 hr (canrenone); 13.8 hr (7-α-[thiomethyl] spirolactone [TMS]); 15 hr (6-ß-hydroxy-7-α-[thiomethyl] spirolactone [HTMS])

Half-life (PO suspension): 1-2 hr (parent drug); 10-35 hr (canrenone, 7-α-[thiomethyl] spirolactone [TMS], 6-ß-hydroxy-7-α-[thiomethyl] spirolactone [HTMS])

Excretion (tablet): Urine (47-57%); feces (35-41%)

Excretion (PO suspension): Urine