Inpler

Inpler - Dosage | Interactions | Side effects

Inpler is a drug that contains eplerenone as an active substance. It belongs to a group of drugs called aldosterone antagonists. Aldosterone is a mineralocorticosteroid hormone whose main purpose is to regulate blood pressure. Aldosterone secretion disorders cause various cardiovascular diseases. Inpler selectively binds to aldosterone receptors, prevents binding of aldosterone to its receptors and thus blocks its effects.

Double-blind clinical trial was conducted on 6632 patients who had an acute myocardial infarction, left ventricular dysfunction and clinical signs of heart failure, and it is shown that Inpler reduces the risk of death by 15%. It has also been confirmed that this drug improves symptoms of heart failure.

Thus, Inpler is indicated in the treatment of recent myocardial infarction, heart failure and left ventricular dysfunction as well as to improve the rate of survival. It is also used to treat hypertension.

Precautions and warnings

Inpler should not be used in patients with a known hypersensitivity reaction to an active substance - eplerenone or other similar drugs.

Its use is also contraindicated in patients with high potassium levels in the blood, so-called hyperkalemia (serum potassium level higher than 5.5 mEq / L). High potassium levels may lead to muscle weakness, bradycardia, rapid breathing, heart rhythm disturbances, and sudden death! Therefore, hyperkalemia is considered the most serious side effect of Inpler. The risk of hyperkalemia is higher in patients who:

  • Have moderate or severe kidney damage (creatinine clearance less-than 50 ml / min).
  • Are taking potassium preparations or a large amount of potassium-rich foods (dry plums, tomatoes, beans, yoghurt, milk, bananas, and fish).
  • Are taking potassium-sparing diuretics, such as: amiloride, spironolactone (Aldactone) and triamterene.
  • Are taking drugs used in the treatment of HIV infections, such as: ritonavir, atazanavir, amprenavir, cobicistat, atazanavir-cobicistat, lopinavir, combination of lopinavir and ritonavir (known as Aluvia), nelfinavir, saquinavir and others.
  • Are taking trimethoprim (one of the active ingredients of a medicine called Bactrim), belonging to the antibiotics.
  • Are taking antifungal drugs, such as: ketoconazole, itraconazole, voriconazole, posaconazole, and fluconazole.
  • Are taking antibiotics, such as: clarithromycin and telithromycin.
  • Are taking medicine called tizanidine.
  • Have type 2 diabetes with microalbuminuria.
  • Are taking drugs called angiotensin converting enzyme inhibitors, such as: quinapril, ramipril (Ampril, Tritace), enalapril (Renitec), lisinopril, captopril, fosinopril (Monopril), quinapril, perindopril (Prexanil) and zofenopril (Zofecard).
  • Are taking medications called AR blockers, such as: valsartan, losartan (Lorista) and olmesartan (Menartan).

Patients with severe hepatic impairment should apply this medicine with extra precaution because of the lack of experience on the use of this drug in patients with impaired hepatic function.

Inpler, Pregnancy and Lactation

Animal studies did not reveal embryonic, fetal toxicity or teratogenicity. However, till now, no adequate, and placebo-controlled, double-blind clinical studies in humans have been performed, so the safety of Inpler's use in human pregnancy has not be established yet. It can be used during pregnancy only if the benefits to the mother outweigh the risk to the fetus.

Studies in rats have shown that Inpler is excreted in rat's milk, but there is no evidence that it is excreted in the milk of a lactating woman. Because the effects of this medicine on nursing infants is not known, your doctor should decide whether to stop breastfeeding or stop taking Inpler.

Dosage

The usual starting dose for congestive heart failure is 25 mg once daily. The dose may be increased gradually to 50 mg once daily, in accordance with the serum potassium levels.

The usual dose for hypertension is 50 mg once daily. The maximum dose is 50 mg twice daily.

Potassium monitoring is recommended:

  • Prior initiating therapy
  • Seven days after the start of therapy
  • One month after the start of therapy
  • Two months after the start of therapy
  • Three months after the start of therapy and every 1-3 months thereafter

The doctor may decide to monitor the potassium level even more frequently if necessary, especially at the beginning of therapy, because clinical studies have shown that hyperkalemia mostly occurs during the first three months of therapy.

Use in patients under the age of 18 and above the age of 75 should be avoided.

No dose adjustment is required in patients with mild kidney or liver damage, but serum potassium levels should be monitored more frequently.

Interactions

In addition to the medicines listed in the section Precautions and Warnings, Inpler should not be used at the same time with any of the following drugs:

  • Non-steroidal anti-inflammatory drugs, such as: Simultaneous administration with these medicines can lead to acute renal failure.
  • Alpha-1 antagonists, such as: terazosin (Hytrin), doxazosin (Cardura) and prazosin (Minipress). Simultaneous administration with these medicines can cause hypotension.
  • Glucocorticoids, such as: dexamethasone, prednisolone, prednisone, triamcinolone, hydrocortisone, and methylprednisolone. Simultaneous administration of any of these medicines with Inpler reduces the antihypertensive effects of Inpler.
  • Tricyclic antidepressants.

Side effects

Possible side effects of Inpler include:

  • Hyperkalemia (muscle weakness, slow heart rate - bradycardia, arrhythmias, heart failure and bradypnea)
  • Upper urinary tract infection (pyelonephritis)
  • Low blood sodium
  • High number of eosinophils (a type of white blood cells)
  • Low blood pressure
  • Heart attack
  • High cholesterol and triglyceride levels
  • The appearance of the enlarged glandular breast tissue in men
  • Asthenia
  • Nausea
  • Vomiting
  • Diarrhea
  • Flatulence
  • Coughing
  • Flu-like symptoms
  • Allergic reactions, including angioneurotic edema

References

  1. PIL
  2. FDA