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Release form and composition

The dosage form of Espiro is film-coated tablets: round, biconvex, shell color - yellow, core color - from almost white to white; 50 mg - on one side with a score (in a cardboard pack there are 3 or 9 blisters of 10 tablets each).

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; yellow iron oxide dye – 0.09/0.18 mg) – 4/8 mg.

Pharmacological properties

Pharmacodynamics

The active substance of Espiro, eplerenone, has high selectivity for mineralocorticoid receptors in humans, in contrast to glucocorticoid, androgen and progesterone receptors. It prevents the binding of mineralocorticoid receptors to aldosterone, which is a key PAAC (renin-angiotensin system) hormone 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, renin secretion is suppressed by aldosterone (via a feedback mechanism). However, an increase in renin activity or the concentration of circulating aldosterone does not affect 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 eplerenone, its absolute bioavailability is 69%. The time to reach Cmax (maximum concentration of the substance) in the blood plasma is approximately 2 hours. Cmax and AUC (area under the concentration-time curve) are linearly dependent on the dose in the range of 10–100 mg; at a dose of more than 100 mg, a nonlinear relationship is observed. Css (stationary concentration of the substance in the blood) is achieved in 2 days. Eating does not affect absorption.

The substance binds to plasma proteins by approximately 50%, mainly with the alpha1-acid group of glycoproteins. The calculated Vd (volume of distribution) at equilibrium is approximately 50 ± 7 l. Eplerenone does not bind to red blood cells.

The metabolism of eplerenone occurs primarily under the influence of CYP3A4. Active metabolites of the substance are not determined in blood plasma.

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. T1/2 (half-life) is approximately 3–5 hours, plasma clearance is approximately 10 l/h.

In elderly patients (over 65 years of age), at steady state, Cmax and AUC were 22% and 45% higher, respectively, than in younger patients (from 18 to 45 years of age).

In severe renal failure, an increase in steady-state AUC and Cmax is observed by 38% and 24%, respectively; in patients on hemodialysis, a decrease is observed by 26% and 3%, respectively. There was no correlation between the clearance of eplerenone from blood plasma and creatinine clearance. Hemodialysis does not remove the substance.

In severe liver failure, pharmacokinetic processes have not been studied, therefore the use of Espiro in this group of patients is contraindicated. With moderate disturbances (on the Child-Pugh scale from 7 to 9 points), equilibrium Cmax and AUC increase by 3.6% and 42%, respectively.

In patients with heart failure (NYHA functional class II–IV), steady-state AUC and Cmax are higher by 38% and 30%, respectively, compared to healthy volunteers matched by weight, age and gender. In heart failure, the clearance of eplerenone does not differ significantly from that in healthy elderly people.

Indications for use

chronic heart failure - prescribed as an additional treatment to standard therapy to reduce cardiovascular mortality and morbidity in patients with chronic heart failure of functional class II according to the NYHA classification against the background of reduced left ventricular ejection fraction (<35%);
myocardial infarction - prescribed as an adjunct to standard therapy to reduce the likelihood of cardiovascular mortality and morbidity in patients with stable left ventricular dysfunction (with ejection fraction 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 functional class II according to the NYHA classification;
severe liver failure (Child-Pugh score more than 9 points);
lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
combination therapy with potassium-sparing diuretics, potassium supplements 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 under 18 years;
individual intolerance to the components of the drug.

Relative (Espiro is prescribed under medical supervision):

functional renal impairment (with CC < 50 ml/min);
microalbuminuria;
diabetes mellitus type 2;
combination therapy with angiotensin-converting enzyme inhibitors or angiotensin II receptor antagonists, lithium-containing drugs, cyclosporine or tacrolimus, digoxin and warfarin in doses that are close to the maximum therapeutic;
pregnancy;
elderly age.

Analogs

If there are contraindications or individual intolerance to the components of the drug, Espiro cannot be used. In this case, doctors recommend replacing it with another drug.

Structural

Among analogues similar in composition, the most popular are:

Decrease. The drug is available only with a doctor's prescription, as it has many side effects. Used for arterial hypertension as part of complex therapy.
Insp. The drug has a fairly high cost. The price for one package, depending on the dosage of the active ingredient, ranges from 1980 to 2530 rubles. The drug is also used in complex therapy for myocardial infarction and heart failure. Requires specialist supervision throughout the treatment period
Epplepres. The drug is available in tablet form. The medicine has many contraindications and requires specialist supervision.

Russian drugs with similar effects

Russian analogues of the drug, which are also not inferior in effectiveness to Espiro, but are based on a different active component, are:

Spironolactone. A drug based on the substance of the same name. It is one of the inexpensive means, similar in its action to Espiro. The cost of packaging varies between 40-75 rubles, depending on the dosage of the active ingredient and the number of tablets.
Used for edema due to heart failure, arterial hypertension and premenstrual syndrome. Side effects most often include skin itching, drowsiness, dizziness and headache.
Vero-Spironolactone. The active ingredient is spironolactone. Prescribed in the presence of edema that occurs against the background of heart failure, hypertension and cirrhosis of the liver. Before use, you must carefully study the instructions for use, as there are many contraindications and side effects.
Verospilactone. The cost of one package is 70-250 rubles, depending on the dosage of the active substance and the number of tablets. Can be used to treat children aged three years and older.

These medications should be used only after consulting a specialist, since improper use or increased dosage can cause side effects and signs of overdose.

Instructions for use of Espiro: method and dosage

Espiro is taken orally; food intake does not affect the effectiveness of therapy.

Reception begins with Espiro 25 mg 1 time per day. After 28 days, the single dose is increased by 2 times, taking into account the serum concentration of potassium in the blood. The recommended maintenance dose is 50 mg once a day.

When the serum potassium concentration in the blood is <5 mmol/l, an increase in dose from 25 mg once every two days to 25 mg once a day, or from 25 to 50 mg once a day is indicated. 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 days before temporary discontinuation of the drug. In cases where the level is ≥ 6 mmol/l, Espiro is discontinued. Resumption of therapy at a dose of 25 mg once every two days is possible if the serum potassium concentration in the blood decreases to <5 mmol/l.

The maximum daily dose is 50 mg.

Potassium concentrations should be determined before prescribing 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 indicated.

In chronic heart failure of functional class II according to the NYHA classification against the background of moderate renal dysfunction (with creatinine clearance 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 conducting combination therapy with drugs that have a weak/moderate inhibitory effect on the CYP3A4 isoenzyme (erythromycin, saquinavir, diltiazem, amiodarone, fluconazole and verapamil), Espiro is prescribed at a dose of 25 mg 1 time per day without further increase.

Comparison of the effectiveness of Espir and Inspra

The effectiveness of Espira is quite similar to Inspra - this means that the ability of the drug substance to provide the maximum possible effect is similar. For example, if the therapeutic effect of Espira is more pronounced, then using Inspra even in large doses will not achieve this effect. Also, the speed of therapy is an indicator The speed of therapeutic action of Espira and Inspra is approximately the same. And bioavailability, that is, the amount of a drug reaching its site of action in the body, is similar. The higher the bioavailability, the less it will be lost during absorption and use by the body.

Side effects

Possible adverse reactions (> 10% - very common; > 1% and < 10% - often; > 0.1% and < 1% - uncommon; > 0.01% and < 0.1% - rare; < 0. 01%, including individual messages - very rarely):

endocrine system: infrequently – hypothyroidism;
lymphatic system: uncommon – eosinophilia;
cardiovascular system: often – marked decrease in blood pressure, myocardial infarction; uncommon – left ventricular failure, atrial fibrillation, orthostatic hypotension, thrombosis of the arteries of the lower extremities, tachycardia;
nervous system: often – fainting, dizziness; uncommon – hypoesthesia, headache;
digestive system: often – nausea, diarrhea, constipation; infrequently – vomiting, flatulence;
respiratory system: often – cough; uncommon – pharyngitis;
skin and subcutaneous tissues: often – itching; uncommon – increased sweating;
biliary tract/liver: uncommon – cholecystitis;
urinary tract/kidneys: often - impaired renal function;
musculoskeletal system: often – musculoskeletal pain, cramps of the calf muscles; infrequently – back pain;
infectious diseases: infrequently – pyelonephritis;
psyche: infrequently – insomnia;
metabolism: often - dehydration, hyperkalemia, hypertriglyceridemia, hypercholesterolemia; uncommon – hyponatremia;
allergic reactions: infrequently – skin rash; with an unknown frequency - angioedema;
instrumental/laboratory data: infrequently - decreased expression of the epidermal growth factor receptor, increased serum concentration of glucose in the blood, concentration of residual urea nitrogen, creatinine;
general disorders: uncommon – malaise, asthenia, gynecomastia.

special instructions

All patients are advised to monitor the serum potassium concentration in the blood at the beginning of treatment and when adjusting the dosage regimen. During treatment, monitoring should be carried out in cases where there is an increased risk of developing hyperkalemia, in particular in elderly patients, with renal failure and diabetes mellitus. Combination therapy with potassium supplements is not recommended. When the dose of Espiro is reduced, a decrease in the concentration of potassium in the blood serum is observed. One study found that the addition of hydrochlorothiazide to therapy prevented an increase in serum potassium concentrations.

As kidney function decreases, the likelihood of developing hyperkalemia increases.

For mild/moderate hepatic dysfunction, monitoring of electrolyte levels is indicated.

Combination therapy with strong CYP3A4 inducers is not recommended. During treatment, the simultaneous use of cyclosporine, tacrolimus, and lithium-containing drugs should be avoided.

Impact on the ability to drive vehicles and complex mechanisms

During the period of taking Espiro, you must be careful when driving vehicles, which is associated with the likelihood of dizziness and fainting.

Comparison of side effects of Espir and Inspra

Side effects or adverse events are any adverse medical event that occurs in a subject after administration of the drug. Espir's adverse event status is almost the same as Inspra's. They both have few side effects. This implies that the frequency of their occurrence is low, that is, the indicator of how many cases of an undesirable effect of treatment are possible and registered is low. The undesirable effect on the body, the strength of influence and the toxic effect of Espira are similar to Inspra: how quickly the body recovers after taking it and whether it recovers at all.

Drug interactions

Possible interactions:

preparations containing lithium: the combination has not been studied; there is information about increased concentration and intoxication of lithium when used simultaneously with diuretics and angiotensin-converting enzyme inhibitors; if combination 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;
neuroleptics, tricyclic antidepressants, baclofen, amifostine: the antihypertensive effect may be enhanced, the likelihood of orthostatic hypotension may increase;
non-steroidal anti-inflammatory drugs: the risk of developing acute renal failure increases (due to direct suppression of glomerular filtration), this especially applies to patients at risk - elderly patients or patients with dehydration; if combined use is necessary before/during therapy, renal function should be monitored and adequate fluid intake should be ensured;
alpha1-blockers (prazosin, alfuzosin): the antihypertensive effect may be enhanced, the likelihood of orthostatic hypotension may increase; when changing body position, it is recommended to monitor blood pressure;
tacrolimus, cyclosporine: renal dysfunction may develop and the likelihood of hyperkalemia may increase; combinations are recommended to be avoided; if combination 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 in patients with impaired renal function, including elderly patients; regular monitoring of serum potassium concentration is required; 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 in cases of 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, caution is required;
inducers of CYP3A4 (rifampicin, carbamazepine, phenytoin, phenobarbital, preparations containing St. John's wort): eplerenone AUC is significantly reduced; combination therapy is not recommended;
weak and moderate inhibitors of CYP3A4: eplerenone AUC increases; when combined with fluconazole, diltiazem, erythromycin, amiodarone, saquinavir, verapamil, the dose of eplerenone should not exceed 25 mg;
strong CYP3A4 inhibitors: eplerenone AUC increases significantly; Combination therapy with itraconazole, ketoconazole, ritonavir, clarithromycin, nelfinavir, nefazodone, telithromycin is contraindicated.

Comparison of safety of Espir and Inspra

The safety of the drug includes many factors. At the same time, with Espira it is quite similar to Inspra

It is important where the drug is metabolized: drugs are excreted from the body either unchanged or in the form of products of their biochemical transformations. Metabolism occurs spontaneously, but most often involves major organs such as the liver, kidneys, lungs, skin, brain and others

When assessing metabolism in Espira, as well as in Inspra, we look at which organ is the metabolizing organ and how critical the effect on it is. The risk-to-benefit ratio is when the prescription of a drug is undesirable, but justified under certain conditions and circumstances, with the obligatory observance of caution in use . At the same time, Espira does not have any risks when used, just like Inspra. Also, when calculating safety, it is taken into account whether only allergic reactions occur or possible dysfunction of the main organs

In other matters, as well as the reversibility of the consequences of using Espira and Inspra.

Espiro, 30 pcs., 50 mg, film-coated tablets