Edarbi tabs 40mg #28

Instruction for Edarbi

You can buy Edarbi on this page

Edarbi is a drug with an antihypertensive effect.

Release form and composition

Dosage form Edarbi - tablets: from almost white to white, round biconvex, engraved on one side "20", "40" or "80" (depending on the dosage), on the other - "ASL" (in a cardboard box 1– 4 or 7 aluminum blisters, 14 tablets each).
Composition of 1 tablet:
    active substance: medoxomil azilsartan - 20, 40 or 80 mg (medoxomil potassium azilsartan - 21.34; 42.68 or 85.36 mg);
    auxiliary components (20/40/80 mg): magnesium stearate - 0.9 / 1.8 / 3.6 mg; mannitol - 47.815 / 95.63 / 191.26 mg; hyprolosis - 2.7 / 5.4 / 10.8 mg; fumaric acid - 1/2/4 mg; sodium hydroxide - 0.345 / 0.69 / 1.38 mg; microcrystalline cellulose - 9/18/36 mg; croscarmellose sodium - 6.9 / 13.8 / 27.6 mg.

Pharmacodynamics

Edarbi is a specific angiotensin II type 1 (AT1) receptor antagonist. Azilsartan medoxomil is a prodrug that quickly converts into the active molecule of azilsartan, which selectively prevents the development of the effects of angiotensin II, which is ensured by blocking its binding to AT1 receptors in different tissues.
Angiotensin II is the primary vasoactive hormone of the RAAS (renin-angiotensin system) with effects that include vasoconstriction, stimulation of aldosterone synthesis / release, cardiac stimulation, and, as a consequence, renal sodium reabsorption.
Due to the blockade of AT1 receptors, the negative regulatory response of angiotensin II to renin secretion is inhibited, however, the resulting increase in plasma renin activity and the level of circulating angiotensin II does not suppress the antihypertensive effect of azilsartan.
The antihypertensive effect of medoxomil azilsartan develops in the first two weeks of therapy, the maximum therapeutic effect is achieved after four weeks. A decrease in blood pressure (blood pressure) after ingestion of a single dose of Edarbi is usually observed within a few hours and persists for 24 hours.
After a sudden cessation of long-term therapy (within 6 months), the development of a withdrawal syndrome is not observed.
The safety / efficacy of Edarbi does not depend on the age of patients, however, a greater sensitivity to a decrease in blood pressure in some elderly patients cannot be ruled out. As with the use of other angiotensin II receptor antagonists and ACE (angiotensin converting enzyme) inhibitors, the antihypertensive effect in black patients is less pronounced.
The simultaneous use of Edarbi 40 mg or 80 mg with dihydropyridine blockers of slow calcium channels (amlodipine) or thiazide diuretics (chlorthalidone) contributes to an additional decrease in blood pressure in comparison with their use as monotherapy.

Pharmacokinetics

The estimated absolute bioavailability of medoxomil azilsartan when taken orally is approximately 60% (based on the plasma concentration profile in the blood). Food intake has no effect on this indicator. The time to reach Cmax (maximum concentration of the substance) of azilsartan in blood plasma averages 1.5–3 hours.
Pharmacokinetic parameters of medoxomil azilsartan are proportional to the dosage in the dose range of 20-320 mg after single / multiple oral administration.
The Vd (volume of distribution) of azilsartan is approximately 16 liters. Binds to blood plasma proteins (more than 99%), mainly albumin. This relationship remains constant when the plasma concentration of azilsartan in the blood significantly exceeds the range that is achieved when taken in recommended doses. Css (stationary concentration of the substance) of azilsartan is achieved in 5 days, with daily use once a day, its cumulation in blood plasma does not occur.
During research, it was found that azilsartan crosses the blood-brain barrier in a minimal amount.
After oral administration during absorption from the gastrointestinal tract, medoxomil azilsartan under the action of the enzyme carboxymethylene butenolidase in the liver and intestines is converted into a pharmacologically active metabolite azilsartan. Metabolized to two primary metabolites, mainly in the liver. The main metabolite in blood plasma, M-II, is formed by O-dealkylation, the minor one, M-I, is formed by decarboxylation. The AUC values ​​(area under the concentration-time curve) for these metabolites compared to azilsartan are 50% and <1%, respectively. The metabolites M-I and M-II have no effect on the pharmacological activity of Edarbi. The main enzyme that provides the metabolism of azilsartan is the CYP2C9 isoenzyme.
The substance and its metabolites are excreted from the body by the kidneys and through the intestines. After oral administration of medoxomil azilsartan, approximately 55% of the dose (mainly in the form of M-I) is found in the feces, approximately 42% (in the form of azilsartan - 15%, in the form of the metabolite M-II - 19%) - in the urine. T1 / 2 (half-life) of azilsartan is about 11 hours, renal clearance is about 2.3 ml / min.
AUC for mild, moderate and severe renal failure increases by 30%, 25% and 95%, respectively. There is no increase in AUC in hemodialysis patients with end-stage renal failure. Azilsartan is not excreted from the systemic circulation through hemodialysis.
With mild and moderate renal failure, there is an increase in AUC by 1.3 and 1.6 times, respectively. The pharmacokinetic parameters of Edarbi in severe hepatic failure have not been studied.

Indications for use

According to the instructions, Edarbi is prescribed for the treatment of essential hypertension.

Contraindications

Absolute:
    severe impairment of hepatic function (> 9 points on the Child-Pugh scale);
    combined use with aliskiren in patients with diabetes mellitus;
    pregnancy and lactation;
    age under 18;
    individual intolerance of the components that make up the drug.
Relative (Edarbi is prescribed under medical supervision):
    hypertrophic obstructive cardiomyopathy;
    severe chronic heart failure (NYHA functional class IV);
    bilateral renal artery stenosis and arterial stenosis of a single functioning kidney;
    severe renal impairment (creatinine clearance <30 ml / min);
    ischemic cerebrovascular disease;
    ischemic cardiomyopathy;
    conditions that are accompanied by a decrease in the volume of circulating blood;
    conditions after kidney transplantation;
    simultaneous use with high doses of diuretics;
    stenosis of the aortic / mitral valves;
    hyperkalemia;
    primary hyperaldosteronism;
    age from 75 years.

Instructions for use: method and dosage

Edarbi is taken orally 1 time a day, regardless of food intake.
The drug must be taken daily, without interruption. In case of termination of treatment, it is necessary to notify the doctor about it.
At the beginning of therapy, it is recommended to take Edarbi 40 mg. In patients with insufficient therapeutic effect, the dose may be increased to a maximum of 80 mg.
With inadequate blood pressure control, Edarbi can be used in combination with other antihypertensive drugs, including diuretics (hydrochlorothiazide, chlorthalidone) and dihydropyridine slow calcium channel blockers (amlodipine).
If you skip taking a single dose, you should not double the next one or change the usual time for taking Edarbi.
For patients over 75 years old, the drug is prescribed at an initial dose of 20 mg, which is associated with the risk of arterial hypotension.
In severe renal impairment and end-stage renal failure, Edarbi should be used with caution.
With mild to moderate severity of hepatic dysfunction, Edarbi therapy should be started with 20 mg per day. Treatment should be carried out under close medical supervision. Also, in a reduced initial dose and under conditions of strict medical control, the drug is prescribed with a reduced volume of circulating blood and / or hyponatremia (for example, with prolonged vomiting, diarrhea, or with the use of large doses of diuretics).
In severe chronic heart failure (NYHA functional class IV), therapy should be carried out with caution.
For adequate control of blood pressure in patients of the Negroid race, an increase in the dose of Edarbi may be required.

Side effects

Possible adverse reactions (> 10% - very often;> 1% and <10% - often;> 0.1% and <1% - infrequently;> 0.01% and <0.1% - rarely; <0, 01% - very rare):
    laboratory / instrumental studies: often - an increase in the activity of creatine phosphokinase; infrequently - hyperuricemia, increased creatinine concentration;
    cardiovascular system: infrequently - a marked decrease in blood pressure;
    nervous system: often - dizziness;
    digestive system: often - diarrhea; infrequently - nausea;
    musculoskeletal system: infrequently - muscle spasms;
    skin and subcutaneous tissues: infrequently - itching, rash; rarely - angioedema;
    others: infrequently - peripheral edema, increased fatigue.
With the combined use of Edarbi with other drugs with antihypertensive action / diuretics, the incidence of some adverse reactions may vary.

Overdose

Usually the drug is well tolerated.
The main symptoms of overdose are dizziness and a marked decrease in blood pressure.
Therapy: with a pronounced decrease in blood pressure, the patient must be transferred to a horizontal position with a low headboard; measures aimed at increasing the volume of circulating blood are recommended, symptomatic treatment is indicated. Due to ineffectiveness, hemodialysis is not prescribed.

Special instructions

The likelihood of oliguria, azotemia, acute arterial hypotension or, in rare cases, acute renal failure during therapy is higher in patients in whom renal function and vascular tone depend to a large extent on RAAS activity (in severe chronic heart failure of functional class IV according to the classification NYHA, severe renal failure or renal artery stenosis).
Against the background of a sharp decrease in blood pressure in patients with ischemic cardiomyopathy / ischemic cerebrovascular diseases, stroke or myocardial infarction may develop.
After the initiation of therapy, patients with a reduced circulating blood volume and / or with hyponatremia (due to diarrhea, vomiting, taking high doses of diuretics, or adhering to a diet with limited salt intake) may develop clinically significant arterial hypotension. Before starting treatment, hypovolemia must be corrected, you need to start taking Edarbi with 20 mg per day.
Patients with primary hyperaldosteronism in most cases are resistant to therapy with antihypertensive drugs that affect the RAAS, so it is not recommended to prescribe Edarbi to them.
In patients with arterial hypertension, Edarbi's combination therapy with potassium-sparing diuretics, potassium preparations or salt substitutes containing potassium or other drugs that can increase the potassium content in the blood (in particular, heparin) can lead to hyperkalemia. In elderly patients, as well as in renal failure, diabetes mellitus and / or other concomitant diseases, the risk of developing hyperkalemia, including fatal, increases. In this group of patients, it is recommended to monitor the serum potassium content.
It is not recommended to use Edarbi in combination with lithium preparations.

Influence on the ability to drive vehicles and complex mechanisms

Edarbi does not significantly affect the ability to drive vehicles, however, patients should take into account the likelihood of developing increased fatigue and dizziness.

Application during pregnancy and lactation

Edarbi is not prescribed during pregnancy / lactation. The safety profile has not been studied, and therefore women are recommended therapy with drugs approved for use during this period. Also, the transition to these drugs is indicated in the case of planning pregnancy.
In newborns whose mothers took Edarbi, it is possible to develop arterial hypotension, therefore, careful medical supervision should be established for the condition of the newborns.

Childhood use

Edarbi therapy is contraindicated in patients under 18 years of age (safety profile has not been studied).

With impaired renal function

Severe renal impairment and end-stage renal failure: therapy should be carried out with caution due to lack of clinical experience.

For violations of liver function

Hepatic dysfunction:
    mild / moderate severity: therapy should be carried out under close supervision at a reduced initial dose;
    severe degree: taking Edarbi is contraindicated, due to the lack of clinical experience with the drug.

Use in the elderly

Edarbi for patients over 75 years old is prescribed in an initial dose of 20 mg (due to the increased risk of arterial hypotension).

Drug interactions

Possible interactions:
    lithium preparations: the combination is not recommended, which is associated with an increase in serum lithium concentration in the blood and manifestations of toxicity; if combined therapy is necessary, regular monitoring of serum lithium levels is required;
    non-steroidal anti-inflammatory drugs: the antihypertensive effect may weaken, in addition, the likelihood of impaired renal function and serum potassium in the blood may increase; at the beginning of therapy, regular intake of fluid in sufficient quantities and monitoring of renal function are recommended;
    potassium-sparing diuretics, potassium preparations, salt substitutes containing potassium and some other drugs (for example, heparin): the serum potassium content in the blood increases, during the period of therapy this indicator must be monitored;
    aliskiren: the likelihood of arterial hypotension, hyperkalemia and impaired renal function (including acute renal failure) increases;
    other antihypertensive drugs, including diuretics (hydrochlorothiazide, chlorthalidone), dihydropyridine blockers of slow calcium channels (amlodipine): the antihypertensive effect is enhanced.

Terms and conditions of storage

Store at temperatures up to 25 ° C in a place protected from light and moisture. Keep out of the reach of children.
Shelf life is 3 years.

Reviews

According to reviews, Edarbi effectively reduces blood pressure in hypertension. A convenient dosage regimen is noted that provides an effect throughout the day. Among the shortcomings, they point to the high cost of the drug and the likelihood of a significant decrease in blood pressure, especially in elderly patients.

Terms of sell

You can buy Edarbi without a prescription from a doctor.