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Aldosterone Blockers
July 16, 2009 | Leave a Comment
Type of Drug
Aldosterone Blockers (al-DOH-stir-own)
Brand Names
Generic Ingredient: Eplerenone Inspra
Generic Ingredient. Spironolactone Aldactone
Combination Product
Generic Ingredients: Hydrochlorothiazide + Spironolactone Aldactazide
Prescribed For
High blood pressure, cirrhosis, and congestive heart failure (CHF); also used for people with low blood potassium who require a diuretic.
General Information
Aldosterone blockers limit the access of aldosterone—a hormone that helps to regulate several different body functions—from its receptor. Too much aldosterone results in high sodium levels, which can lead to water retention and potassium loss; it can also affect the size, shape, and function of the heart. Aldosterone blockers are generally combined with other medicines in the management of disease. These drugs are useful in removing excess body fluids in conditions associated with high aldosterone levels.
One in every ten people with high blood pressure has excess aldosterone in their systems. In people with congestive heart failure (CHF), aldosterone levels can be 20 times higher than normal, which can worsen their condition, making the use of aldosterone blockers an important part of their treatment. Aldosterone block-ers also help the heart return to normal size, shape, and function in people with heart failure. Eplerenone is broken down in the liver, primarily by an enzyme system known as CYP3A4.
Cautions and Warnings
Do not take aldosterone blockers if you are allergic or sensitive to any of their ingredients.
Do not use aldosterone blockers if you have kidney failure or high blood potassium.
People with liver disease should be cautious about using a!- dosterone blockers.
People taking an aldosterone blocker should have their potassium levels checked periodically.
People with diabetes who have albumin in their urine should not take aldosterone blockers.
Possible Side Effects
Eplerenone
✓ Less common: dizziness, diarrhea, fatigue, flu-like symptoms, coughing, abdominal pain, elevation of blood cholesterol and/or triglyceride levels, elevation of blood potassium levels, and albumin in the urine.
✓ Rare: enlargement of the breasts in males, irregular menstrual cycles in women, and painful breasts. Contact your doctor if you experience any side effect not listed above.
Spironolactone
✓ Less common: drowsiness, lethargy, headache, gastrointestinal upset, cramps and diarrhea, rash, mental confusion, fever, feeling unwell, enlargement of the breasts in males, impotence, and irregular menstrual cycles or deepening of the voice in women.
Drug Interactions
• Do not combine eplerenone with itraconazole or ketoconazole. These drugs can cause the amount of eplerenone in the blood to increase by up to 500% and may cause fatal increases in blood potassium.
• Mixing eplerenone with erythromycin, fluconazole, saquinavir, or verapamil increases the amount of eplerenone in the blood. People taking this combination must watch for signs of high blood potassium (see “Special Information”) and have their blood potassium levels checked regularly.
• Combining a potassium supplement and an aldosterone blocker can lead to dangerously high blood levels of potassium. Do not use a salt-substitute or take any extra potassium unless prescribed by your doctor.
• Combining an aldosterone blocker with an ACE inhibitor or an angiotensin H receptor blocker (ARB) may significantly raise blood potassium. Be sure your doctor monitors your potassium levels if you combine these drugs.
• Spironolactone may interfere with anticoagulant (blood-thinning) drugs and mitotane (an anticancer drug).
• Aspirin can interfere with the diuretic effect of spironolactone but does not alter its effect on high blood pressure or CHF.
• Combining spironolactone with alcohol, barbiturates, or narcotics can lead to dizziness or fainting when rising suddenly from a sitting or lying position.
• Combining spironolactone and a corticosteroid can lead to very low blood potassium.
• Spironolactone may alter your response to drugs used during general anesthesia.
• Lithium generally should not be combined with any diuretic.
• Combining nonsteroidal anti-inflammatory drugs (NSAIDs) with aldosterone blockers can lead to severe elevations of blood potassium and reduce the blood-pressure-lowering effect of the diuretic.
• Spironolactone may raise digoxin blood levels and increase the risk of severe digoxin side effects. Your doctor may have to adjust your digoxin dosage.
• St. John’s wort (a CYP3A4 inducer) may decrease eplerenone levels by about 30%.
Food Interactions
Food appears to increase the amount of spironolactone absorbed into the blood. Take this drug with food at the same time every day. Eplerenone may be taken without regard to food or meals. Taking this drug with grapefruit juice increases the amount of drug absorbed into your body.
Usual Dose
Eplerenone
Adult 50-100 mg a day. Child: not recommended.
Spironolactone
Adult: Starting dosage is 50-100 mg a day in divided doses for high blood pressure; 25-200 mg a day in divided doses for high fluid levels related to other diseases; and 25-100 mg a day for low potassium levels related to diuretic use.
Child: 1-2 mg per lb. of body weight a day.
Spironolactone + Hydrochlorothiazide Adult: 1-4 tablets daily.
Overdosage
Eplerencne overdose may lead to low blood pressure and high blood potassium. Spironolactone overdose may lead to drowsiness. confusion, rash, nausea, vomiting, dizziness, and diarrhea. Rarely. coma may occur in people with severe liver disease. High blood potassium may also occur, especially in people with kidney zsease. Call your local poison control center or a hospital emercency room for more information. If you seek treatment, ALWAYS oring the prescription bottle or container.
Special Information
<e a c!osterone blockers exactly as they are prescribed.
High blood levels of potassium associated with aldosterone blockers may cause weakness, lethargy, drowsiness, muscle pain or cramps, and muscular fatigue. Use caution while doing anything that requires intense concentration, like driving or operating machinery.
Do not use a salt substitute or take anything else that is a source of extra potassium, including many multivitamin or supplement products.
People with high blood pressure should not self-medicate with over-the-counter cough, cold, or allergy remedies containing stimulants. These drugs can raise blood pressure effectiveness and have an adverse effect on the heart.
!f you forget a dose, take it as soon as you remember. If it is almost time for your next dose, skip the one you forgot and continue with your regular schedule. Do not take a double dose.
Special Populations
Pregnancy/Breast-feeding: Animal studies with eplerenone showed no effects on a developing fetus. Spironolactone crosses into the fetal circulation. When your doctor considers either of these drugs crucial, their potential benefits must be carefully weighed against their risks.