Espler

Espler - Dosage | Interactions | Side effects

Espler contains active substance called eplerenone and belongs to the group of selective blockers of aldosterone. It is used as add-on therapy to beta-2 blockers in order to reduce the risk of cardiovascular diseases and death in stable patients with systolic left ventricular dysfunction.

Espler is also used in the treatment of hypertension (alone or combined with other drugs) as well as for the improvement of survival in patients with congestive heart failure.

Contraindications

Espler is contraindicated in the following conditions:

  • In patients with potassium levels greater than 5 mmol / L or 5.5 mEq / L. Espler blocks aldosterone (aldosterone is a hormone that increases the excretion of potassium through urine), and blocking aldosterone causes a significant increase in blood potassium levels. For this reason, regular monitoring of potassium levels in the blood during therapy is necessary. Elevated blood potassium levels can cause serious cardiac arrhythmias.
  • In patients with creatinine clearance less than 50 ml / min (which is a sign of impaired renal function).
  • In patients with severe hepatic impairment (Child-Pugh class C). Espler has a similar chemical structure as a diuretic called spironolactone, which is rarely associated with acute hepatic insufficiency. For this reason, it is assumed that Espler may also cause acute liver damage, although clinical studies have not confirmed this assumption.
  • In patients taking potassium preparations.
  • In patients taking potassium-sparing water pills (spironolactone, triamterene and amyloride). Simultaneous administration increases the risk of hyperkalemia.
  • In patients taking antifungal drugs, such as: itraconazole, ketoconazole, voriconazole, and fluconazole. These drugs enhance the effects of Espler, therefore increase the risk of hyperkalemia.
  • In patients taking antibiotics, such as: clarithromycin, telithromycin, erythromycin, and azithromycin. These drugs inhibit an enzyme that metabolizes Espler, therefore increase plasma concentrations of Espler and risk of hyperkalemia.
  • In patients taking antidepressants, such as: nefazodone.
  • In patients taking HIV protease inhibitors, such as: ritonavir, nelfinavir, indinavir, and others. These drugs enhance the effects of Espler, and increase the risk of hyperkalemia.
  • In patients who suffer from type 2 diabetes mellitus, accompanied by proteinuria. These patients are at higher risk of developing hyperkalemia.
  • In patients with a serum creatinine levels greater than 1.8 mg / dL in women and 2 mg / dL in men, respectively.

Espler, pregnancy and lactation

There are not enough randomized, double-blind and well-controlled clinical trials to confirm the safety of this drug in pregnant women.

Studies in animals that investigated the use of doses that are 30 times greater than those used in humans, have not shown adverse effects on the embryonic, fetal and postnatal development. Therefore, Espler should be used in pregnancy only if the benefit to the mother is greater than the risk to the fetus.

Your doctor will decide whether to discontinue breastfeeding or Espler during the breastfeeding period, after a comprehensive benefit / risk assessment.

Dosage instructions

The usual starting dose is 25 mg once a day. The dose may be gradually increased to 50 mg once daily.

The therapy should begin 3-14 days after a heart attack.

The dosage should be adjusted based on the blood potassium levels.

Interactions

Espler should not be administered concurrently with the following medicines:

  • Tacrolimus and cyclosporin - immunosuppressive drugs. Simultaneous administration with these medicines increases the risk of high blood potassium levels.
  • Medicines used for the treatment of mild and moderate pain, such as: Simultaneous administration with these medicines increases the risk of acute renal failure.
  • Sulfamethoxazole / trimethoprim (also known as Bactrim). Simultaneous administration with this medicine increases the risk of high blood potassium levels.
  • ACE inhibitors, such as: Simultaneous administration with these medicines increases the risk of hyperkalemia.
  • Angiotensin-receptor blockers, such as: olmesartan, valsartan, and losartan. Simultaneous administration with these medicines increases the risk of hyperkalemia.
  • Alpha antagonists, such as: alfuzosin (Xatral SR), terazosin and prazosin. Simultaneous administration with these medicines increases the risk of hypotension.
  • Tricyclic antidepressants (amitriptyline, nortriptyline, and imipramine). Simultaneous administration with these medicines increases the risk of low blood pressure.

Note: Certain interactions are listed in the Contraindications section.

Side effects

Espler may cause the following side effects:

  • Pyelonephritis
  • High blood potassium levels
  • High blood cholesterol levels
  • High blood triglyceride levels
  • Low blood sodium levels
  • Low blood pressure
  • Increased numbers of eosinophilic granulocytes
  • Flatulence
  • Angioneurotic edema
  • Asthenia
  • Gynecomastia
  • Inflammation of the pharynx
  • Heart attack

References

  1. accessdata
  2. PIL