Espiro – composition, action, dosage, contraindications, precautions

Espiro is a drug indicated for the treatment of heart failure after a heart attack. Read on how to dose Espiro, what are the contraindications to its use and what side effects it can cause.

Espiro – characteristics and indications

Espiro belongs to a group of medicines called selective aldosterone antagonists. These drugs block the action of aldosterone, a substance produced by the body that controls blood pressure and heart function. High levels of aldosterone can cause changes in your body, leading to heart failure.

Espiro is a medicine used to treat heart failure to prevent worsening of the disease and reduce the number of hospitalizations in the case of:

  1. a history of a heart attack – in combination with other drugs used in heart failure,
  2. persistent mild symptoms despite the treatment you have been receiving so far. 

Espiro is available in two forms:

  1. 25 mg – each film-coated tablet contains 25 mg of eplerenone,
  2. 50 mg – each film-coated tablet contains 50 mg of eplerenone.

See: A heart attack attacks younger and younger people

Espiro – the mechanism of action

Eplerenone exhibits relative specificity in binding to recombinant human mineralocorticoid receptors compared to that of recombinant human glucocorticoid, progesterone and androgen receptors. Eplerenone prevents the binding of aldosterone, a key hormone in the renin-angiotensin-aldosterone system (RAA) that is involved in the regulation of blood pressure and the pathophysiology of cardiovascular disease.

Eplerenone has been shown to persistently increase plasma renin activity and serum aldosterone levels, associated with a reduction in the inhibitory effect of aldosterone on renin secretion (negative feedback regulation). The resulting increased plasma renin activity and the increased circulating aldosterone levels do not reduce the effect of eplerenone.

Read: Noisy work increases the risk of a heart attack

Espiro – dosage

Forms containing 25 mg and 50 mg of the active ingredient are available to allow for individual titration of the dose. The maximum dose is 50 mg daily.

Dosage of Espiro in people with heart failure after a heart attack:

  1. the recommended maintenance dose of eplerenone is 50 mg once daily. Treatment should be started at a dose of 25 mg once daily and gradually increased, preferably over a 4 week period with monitoring of serum potassium, to a target dose of 50 mg once daily. Treatment with eplerenone should usually be started within 3-14 days of the diagnosis of acute myocardial infarction.

Dosage of Espiro in people with (chronic) heart failure (NYHA class II):

  1. in patients with chronic heart failure (NYHA class II), treatment should be initiated at a dose of 25 mg once a day and then gradually increased, preferably over 4 weeks, with monitoring of serum potassium, to a target dose of 50 mg once a day.

Dosage of Espiro in people with kidney problems:

  1. in people with mild kidney disease, treatment is started with the usual starting dose. If you have moderate kidney disease, the starting dose is one 25 mg tablet every other day. Your doctor may adjust the dose according to the amount of potassium in your blood. Espiro is contraindicated in people with severe kidney disease.

Dosage of Espiro in people with liver disease:

  1. in people with mild or moderate liver disease, no adjustment of the starting dose is necessary.

Dosage of Espiro in the elderly:

  1. it is not necessary to adjust the starting dose of the drug.

The editorial board recommends: Even slightly elevated cholesterol can cause a heart attack

Espiro – contraindications

Espiro should not be used if:

  1. you are allergic to eplerenone or any of the other ingredients of this medicine,
  2. if you have high levels of potassium in your blood (hyperkalaemia),
  3. if you are taking medicines to help you to excrete excess fluid from your body (potassium-sparing diuretics),
  4. if you have severe kidney problems
  5. if you have severely impaired liver function,
  6. if you are taking medicines for fungal infections (ketoconazole or
  7. itraconazole),
  8. if you are taking medicines used against HIV (nelfinavir or ritonavir).

See: Breast milk can destroy HIV

Espiro – precautions

Talk to your doctor before taking Espiro if:

  1. have kidney or liver problems
  2. you are taking lithium salts (usually used in a manic-depressive disorder called bipolar disorder),
  3. you are taking tacrolimus or cyclosporin (used to treat skin disorders such as psoriasis or eczema and to prevent organ rejection). 

I spiro to hyperkalaemia

Due to the mechanism of action of eplerenone, hyperkalaemia may occur with its use. Serum potassium levels should be monitored in all subjects at the start of treatment and after dose adjustments. During continued treatment, periodic monitoring of potassium levels is especially recommended in people at risk of developing hyperkalaemia, such as the elderly, people with renal failure and diabetes.

Read: Adolescents with depression are more likely to develop heart disease

Espiro – interactions with other drugs

You must not take Espiro with the following medicines:

  1. itraconazole or ketoconazole (used to treat fungal infections), ritonavir, nelfinavir (antiviral drugs for HIV), clarithromycin, telithromycin (used to treat bacterial infections) and nefazodone (used to treat depression) as these drugs may reduce the metabolism of the drug and thus prolong its action in the body,
  2. potassium-sparing diuretics (medicines that help you to remove excess fluid from your body) and potassium supplements. These drugs increase the amount of potassium in your blood
  3. medicines used to treat certain heart conditions or high blood pressure (called angiotensin converting enzyme (ACE) inhibitors together with Angiotensin II Receptor Antagonists (AIIRAs), used to treat high blood pressure, heart disease and some kidney diseases) as they can increase the amount of potassium in your blood blood.

Also, tell your doctor if you are taking the following medications:

  1. lithium (usually used to treat manic depression, also known as bipolar disorder). The use of lithium concomitantly with diuretics and angiotensin converting enzyme (ACE) inhibitors (used to treat high blood pressure and heart disease) increased the level of lithium in the blood, which could cause side effects such as loss of appetite, visual disturbances, fatigue, muscle weakness muscle tremors
  2. cyclosporin or tacrolimus (used to treat skin disorders such as psoriasis or eczema and to prevent organ rejection). These drugs can cause kidney problems and thus increase the amount of potassium in your blood.
  3. non-steroidal anti-inflammatory drugs (NSAIDs – painkillers such as ibuprofen, used to relieve pain, stiffness and inflammation). These drugs can lead to kidney problems and thus increase the amount of potassium in your blood.
  4. trimethoprim (used to treat bacterial infections) may increase the amount of potassium in the blood
  5. alpha-1-blockers such as prazosin or alfuzosin (used to treat high blood pressure and some diseases of the prostate gland). They may cause your blood pressure to drop rapidly and make you feel dizzy when standing up,
  6. tricyclic antidepressants such as amitriptyline or amoxapine (used to treat depression), antipsychotics (also known as neuroleptics) such as chlorpromazine or haloperidol (used to treat mental disorders), amifostine (used in cancer chemotherapy) and baclofen (used in increased muscle tone). These drugs can cause a drop in blood pressure and dizziness when standing up,
  7. glucocorticosteroids such as hydrocortisone or prednisone (used to treat inflammation and certain skin conditions) and tetracosactide (mainly used in the diagnosis and treatment of disorders of the adrenal cortex). They may reduce the blood pressure lowering effect of eplerenone,
  8. digoxin (used to treat heart problems); Concomitant use with eplerenone may increase the concentration of digoxin in the blood,
  9. warfarin (an anti-clotting drug): caution is warranted when taking warfarin as high levels of warfarin in the blood may alter the effects of eplerenone in the body.
  10. Erythromycin (used to treat bacterial infections), saquinavir (an antiviral medicine to treat HIV infection), fluconazole (used to treat fungal infections), amiodarone, diltiazem and verapamil (used to treat heart disease and high blood pressure) increase the half-life of eplerenone. thus prolonging its effect on the body,
  11. St. John’s wort (a herbal medicinal product), rifampicin (a medicine to treat bacterial infections), carbamazepine, phenytoin and phenobarbital (used, inter alia, to treat epilepsy) may shorten the half-life of eplerenone and thus reduce its effect. 

Espiro – side effects

Espiro can cause certain side effects. Seek medical attention immediately if you experience any of the following symptoms:

  1. swelling of the face, tongue or throat
  2. difficulty swallowing
  3. hives and difficulty breathing.

These are symptoms of angioedema, an uncommon side effect (affecting less than 1 in 100 patients).

Other common side effects (occurring in less than 1 in 10 people) include:

  1. increased levels of potassium in the blood (symptoms include muscle cramps, diarrhea, nausea, dizziness or headache)
  2. dizziness,
  3. Headache,
  4. swoon,
  5. increase in blood cholesterol,
  6. insomnia (difficulty falling asleep)
  7. cough,
  8. constipation,
  9. low blood pressure
  10. heart problems such as uneven heart beat and heart failure
  11. diarrhea,
  12. nausea,
  13. vomiting,
  14. kidney problems. 

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