Espiro
Espiro: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Espiro
ATX code: C03DA04
Active ingredient: eplerenone (eplerenone)
Manufacturer: Pharmaceutical Works POLPHARMA, SA (Poland)
Description and photo updated: 2018-23-11
Prices in pharmacies: from 640 rubles.
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Espiro is a drug with a diuretic effect.
Release form and composition
Dosage form Espiro - film-coated tablets: round biconvex, shell color - yellow, core color - from almost white to white; 50 mg - on one side with a line (in a cardboard box 3 or 9 blisters of 10 tablets).
Composition of 1 tablet:
- active substance: eplerenone - 25 or 50 mg;
- auxiliary components (25/50 mg): croscarmellose sodium - 3/6 mg; lactose monohydrate - 38.67 / 77.34 mg; sodium lauryl sulfate - 0.85 / 1.7 mg; microcrystalline cellulose - 15.38 / 30.76 mg; hypromellose-15cP - 1.25 / 2.5 mg; magnesium stearate - 0.85 / 1.7 mg;
- shell (25/50 mg): Opadry II 33G32578 yellow (triacetin - 0.24 / 0.48 mg; hypromellose-6cP - 1.6 / 3.2 mg; titanium dioxide - 0.91 / 1.82 mg; macrogol -3350 - 0.32 / 0.64 mg; lactose monohydrate - 0.84 / 1.68 mg; dye iron oxide yellow - 0.09 / 0.18 mg) - 4/8 mg.
Pharmacological properties
Pharmacodynamics
The active substance of Espiro - eplerenone, has a high selectivity in relation to mineralocorticoid receptors in humans, in contrast to glucocorticoid, androgenic and progesterone receptors. It interferes with the binding of mineralocorticoid receptors to aldosterone, which is a key PAAC hormone (renin-angiotensin system) involved in the regulation of blood pressure (blood pressure) and the pathogenesis of cardiovascular diseases.
The use of eplerenone leads to a persistent increase in the activity of aldosterone in the blood serum and renin in the blood plasma. Subsequently, the secretion of renin is suppressed by aldosterone (using a feedback mechanism). At the same time, an increase in the activity of renin or the concentration of circulating aldosterone has no effect on the effectiveness of eplerenone.
The substance does not significantly affect the heart rate (heart rate) and the duration of the QRS, QT or PR intervals.
Pharmacokinetics
After oral administration of 100 mg of eplerenone, its absolute bioavailability is 69%. The time to reach C max (maximum concentration of the substance) in blood plasma is approximately 2 hours. C max and AUC (area under the concentration-time curve) are linearly dependent on the dose in the range of 10–100 mg, with a dose of more than 100 mg there is a non-linear relationship. C ss (stationary concentration of a substance in the blood) is reached in 2 days. Food intake does not affect absorption.
The substance binds to blood plasma proteins by about 50%, mainly with the alpha1-acid group of glycoproteins. The calculated V d (volume of distribution) at equilibrium is approximately 50 ± 7 liters. Eplerenone does not bind to erythrocytes.
Eplerenone is metabolized primarily by CYP3A4. Active metabolites of a substance in blood plasma are not determined.
Less than 5% of the dose of unchanged eplerenone is excreted through the intestines and kidneys. After a single oral dose of labeled eplerenone, approximately 67% of the dose was excreted through the kidneys and 32% through the intestines. T 1/2 (half-life) - approximately 3-5 hours, clearance from blood plasma is approximately 10 l / h.
In elderly patients (over 65 years old) in an equilibrium state, C max and AUC were, respectively, 22% and 45% higher than in young patients (from 18 to 45 years old).
In severe renal failure, there is an increase in equilibrium AUC and C max by 38% and 24%, respectively, in patients on hemodialysis, their decrease by 26% and 3%, respectively. No correlation was found between plasma clearance of eplerenone and creatinine clearance. The substance is not removed during hemodialysis.
In severe hepatic insufficiency, pharmacokinetic processes have not been studied, therefore, the use of Espiro in this group of patients is contraindicated. In moderate impairments (on the Child-Pugh scale from 7 to 9 points), the equilibrium C max and AUC increase by 3.6% and 42%, respectively.
In patients with heart failure (NYHA classification II – IV functional class), the equilibrium AUC and C max are higher by 38% and 30%, respectively, in comparison with healthy volunteers matched by weight, age and sex. In heart failure, the clearance of eplerenone is not significantly different from that in healthy older adults.
Indications for use
- chronic heart failure - prescribed as an adjunct to standard therapy to reduce cardiovascular mortality and morbidity in patients with chronic heart failure of functional class II according to NYHA classification against the background of a reduced left ventricular ejection fraction (<35%);
- myocardial infarction - is prescribed as an adjunct to standard therapy to reduce the likelihood of cardiovascular mortality and morbidity in patients with stable left ventricular dysfunction (with an ejection fraction of less than 40%) and the presence of clinical signs of heart failure after myocardial infarction.
Contraindications
Absolute:
- clinically significant hyperkalemia;
- serum potassium concentration in the blood at the beginning of therapy> 5 mmol / l;
- moderate / severe renal failure with CC (creatinine clearance) <30 ml / min in patients with chronic heart failure of II functional class according to the NYHA classification;
- severe liver failure (on the Child-Pugh scale more than 9 points);
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
- combination therapy with potassium-sparing diuretics, potassium preparations, or potent CYP3A4 inhibitors (clarithromycin, itraconazole, ritonavir, ketoconazole, nelfinavir, nefazodone and telithromycin);
- plasma creatinine concentration> 1.8 mg / dL (or> 159 mmol / L) in women,> 2 mg / dL (or> 177 mmol / L) in men;
- lactation period;
- age up to 18 years;
- individual intolerance to the components of the drug.
Relative (Espiro is prescribed under medical supervision):
- functional disorders of the kidneys (with CC <50 ml / min);
- microalbuminuria;
- type 2 diabetes mellitus;
- combination therapy with angiotensin-converting enzyme inhibitors or angiotensin II receptor antagonists, lithium-containing drugs, cyclosporin or tacrolimus, digoxin and warfarin in doses that are close to the maximum therapeutic;
- pregnancy;
- elderly age.
Instructions for the use of Espiro: method and dosage
Espiro is taken orally, food intake has no effect on the effectiveness of therapy.
Reception begins with Espiro 25 mg once a day. After 28 days, a single dose is doubled, taking into account the serum potassium concentration in the blood. The recommended maintenance dose is 50 mg once a day.
With a serum potassium concentration in the blood <5 mmol / l, an increase in dose is shown from 25 mg once every two days to 25 mg once a day, or from 25 to 50 mg once a day. If the indicator is in the range of 5–5.4 mmol / l, the dose is not changed. At 5.5-5.9 mmol / L, the dose should be reduced from 50 to 25 mg once a day, or from 25 mg once a day to 25 mg once every two days, or from 25 mg once every two days before the temporary discontinuation of the drug. In cases where the indicator is ≥ 6 mmol / l, Espiro is canceled. Resumption of therapy at a dose of 25 mg once every two days is possible with a decrease in serum potassium concentration in the blood <5 mmol / L.
The maximum daily dose is 50 mg.
The potassium concentration should be determined before the appointment of Espiro, during the first week of therapy and 30 days after starting the drug or in cases of dose adjustment. In the future, periodic monitoring of this indicator is also shown.
In chronic heart failure of the II functional class according to the NYHA classification against the background of moderate renal dysfunction (with CC from 30 to 60 ml / min), therapy should be started with a dose of 25 mg every other day. In the future, the dose can be adjusted taking into account the serum potassium concentration in the blood.
When carrying out combination therapy with drugs that have a weak / moderately pronounced inhibitory effect on the CYP3A4 isoenzyme (erythromycin, saquinavir, diltiazem, amiodarone, fluconazole and verapamil), Espiro is prescribed at a dose of 25 mg once a day without further increase.
Side effects
Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01%, including isolated messages - very rare):
- endocrine system: infrequently - hypothyroidism;
- lymphatic system: infrequently - eosinophilia;
- cardiovascular system: often - a marked decrease in blood pressure, myocardial infarction; infrequently - left ventricular failure, atrial fibrillation, orthostatic hypotension, thrombosis of the arteries of the lower extremities, tachycardia;
- nervous system: often - fainting, dizziness; infrequently - hypesthesia, headache;
- digestive system: often - nausea, diarrhea, constipation; infrequently - vomiting, flatulence;
- respiratory system: often - cough; infrequently - pharyngitis;
- skin and subcutaneous tissue: often - itchy skin; infrequently - increased sweating;
- biliary tract / liver: infrequently - cholecystitis;
- urinary tract / kidney: often - impaired renal function;
- musculoskeletal system: often - musculoskeletal pain, calf muscle cramps; infrequently - back pain;
- infectious diseases: infrequently - pyelonephritis;
- psyche: infrequently - insomnia;
- metabolism: often - dehydration, hyperkalemia, hypertriglyceridemia, hypercholesterolemia; infrequently - hyponatremia;
- allergic reactions: infrequently - skin rash; with an unknown frequency - angioedema;
- instrumental / laboratory data: infrequently - a decrease in the expression of the epidermal growth factor receptor, an increase in the serum concentration of glucose in the blood, the concentration of residual urea nitrogen, creatinine;
- general disorders: infrequently - malaise, asthenia, gynecomastia.
Overdose
Overdose cases are not described.
Possible symptoms: hyperkalemia, excessive decrease in blood pressure.
Therapy:
- hyperkalemia: standard measures;
- excessive lowering of blood pressure: supportive treatment.
There is evidence that eplerenone actively binds to activated carbon. The substance is not removed during hemodialysis.
special instructions
All patients at the beginning of treatment and when adjusting the dosage regimen is shown to monitor the serum potassium concentration in the blood. During treatment, monitoring should be carried out in cases of increased risk of hyperkalemia, in particular in elderly patients, with renal failure and diabetes mellitus. Combination therapy with potassium supplements is not recommended. With a decrease in the dose of Espiro, a decrease in the concentration of potassium in the blood serum is observed. As a result of one study, it was found that the addition of hydrochlorothiazide to therapy prevents an increase in the concentration of potassium in the blood serum.
With decreased kidney function, the likelihood of developing hyperkalemia increases.
For mild to moderate impairment of hepatic function, electrolyte control is indicated.
Combination therapy with potent CYP3A4 inducers is not recommended. During the treatment period, the simultaneous use of cyclosporine, tacrolimus, lithium-containing preparations should be avoided.
Influence on the ability to drive vehicles and complex mechanisms
During the period of taking Espiro, care must be taken when driving vehicles, which is associated with the likelihood of dizziness and fainting.
Application during pregnancy and lactation
There is no information on the use of Espiro during pregnancy / lactation.
The peculiarity of therapy in this group of patients:
- pregnancy: Espiro can only be prescribed if the expected benefit from the treatment is higher than the possible risk;
- pregnancy period: therapy is contraindicated.
Pediatric use
Espiro therapy is contraindicated in patients under 18 years of age, since the safety profile has not been studied.
With impaired renal function
Application features depend on the QC level:
- <50 ml / min: Espiro is prescribed under medical supervision;
- <30 ml / min: therapy is contraindicated.
With deterioration in renal function, the degree of hyperkalemia increases. Periodic monitoring of serum potassium concentration in the blood is recommended.
For violations of liver function
Espiro therapy is contraindicated in severe hepatic impairment.
Use in the elderly
According to the instructions, Espiro in elderly patients should be used under medical supervision. Periodic monitoring of serum potassium concentration in the blood is shown.
Drug interactions
Possible interactions:
- preparations containing lithium: the combination has not been studied; there is information about an increase in the concentration and intoxication with lithium when used simultaneously with diuretics and angiotensin-converting enzyme inhibitors; if combined therapy is necessary, it is recommended to monitor the plasma concentration of lithium in the blood;
- potassium preparations and potassium-sparing diuretics: the effects of antihypertensive drugs and other diuretics are enhanced; the increased likelihood of hyperkalemia must be taken into account; the combination is not recommended;
- antipsychotics, tricyclic antidepressants, baclofen, amifostine: the antihypertensive effect may increase, the likelihood of orthostatic hypotension may increase;
- nonsteroidal anti-inflammatory drugs: the risk of developing acute renal failure increases (due to direct suppression of glomerular filtration), especially in patients at risk - elderly patients or patients with dehydration; if combined use is necessary before / during therapy, it is necessary to monitor renal function and provide an adequate water regime;
- alpha 1 -adrenergic blockers (prazosin, alfuzosin): the antihypertensive effect may increase, the likelihood of orthostatic hypotension may increase; when changing body position, it is recommended to control blood pressure;
- tacrolimus, cyclosporine: impaired renal function may develop and the likelihood of hyperkalemia may increase; combinations are recommended to be avoided; if combined therapy is necessary, it is recommended to monitor renal function and serum potassium concentration in the blood;
- angiotensin-converting enzyme inhibitors and angiotensin II receptor antagonists: the risk of hyperkalemia increases, especially with impaired renal function, including elderly patients; requires regular monitoring of the concentration of potassium in the blood serum; a triple combination of these drugs is not recommended;
- trimethoprim: the likelihood of hyperkalemia increases; monitoring of serum potassium concentration in the blood and renal function is recommended, especially in elderly patients and with renal failure;
- tetracosactide, glucocorticoids: fluid and sodium retention may occur;
- warfarin: when used in doses close to the maximum therapeutic, caution is required;
- digoxin: its AUC increases; when using digoxin in doses close to the maximum therapeutic dose, caution is required;
- CYP3A4 inducers (rifampicin, carbamazepine, phenytoin, phenobarbital, preparations containing St. John's wort): AUC of eplerenone significantly decreases; combination therapy is not recommended;
- weak to moderate inhibitors of CYP3A4: AUC of eplerenone increases; when combined therapy with fluconazole, diltiazem, erythromycin, amiodarone, saquinavir, verapamil, the dose of eplerenone should not exceed 25 mg;
- potent inhibitors of CYP3A4: eplerenone AUC is significantly increased; combined therapy with itraconazole, ketoconazole, ritonavir, clarithromycin, nelfinavir, nefazodone, telithromycin is contraindicated.
Analogs
Espiro's analogues are Inspra, Eplerenone-Teva.
Terms and conditions of storage
Store at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Espiro
Reviews about Espiro are few. According to doctors, it is one of the effective drugs necessary for the treatment of patients with acute myocardial infarction with signs of heart failure. In severe chronic heart failure, taking Espiro can reduce cardiovascular mortality.
The price of Espiro in pharmacies
The approximate price for Espiro 25 mg is 558-780 rubles. for 30 tablets, 50 mg - 773-1050 rubles. for 30 tablets.
Espiro: prices in online pharmacies
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Drug name Price Pharmacy |
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Espiro 25 mg film-coated tablets 30 pcs. 640 RUB Buy |
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Espiro tablets p.p. 25mg 30 pcs. 738 RUB Buy |
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Espiro 50 mg film-coated tablets 30 pcs. 899 RUB Buy |
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Espiro tablets p.p. 50mg 30 Pcs. 922 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
