Mikardis tablets: instructions for use, price, reviews, analogues

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Telmisartan is a selective angiotensin II . It has a high affinity for AT1 angiotensin II receptors . Competes with angiotensin II at specific receptors, without having the same effect. The binding is long lasting.

Does not have tropism for other receptor subtypes. Reduces the content of aldosterone in the blood, does not suppress renin in plasma and ion channels in cells.

The onset of the hypotensive effect is observed within the first three hours after taking telmisartan . The effect lasts for a day or more. A pronounced effect develops a month after continuous use.

In persons with arterial hypertension , telmisartan reduces systolic and diastolic pressure, but does not change the number of heart contractions.

Does not cause withdrawal syndrome.

Pharmacokinetics

When taken orally, it is quickly absorbed from the intestine. Bioavailability approaches 50%. After three hours, the plasma concentration reaches its maximum. 99.5% of the active substance binds to blood proteins. Metabolized by reaction with glucuronic acid . Metabolites of the drug are inactive. The half-life is more than 20 hours. Excreted through the digestive tract, excretion in urine is less than 2%.

Mikardis

Trade name: Micardis International name: Telmisartan

Country of origin: Germany

Manufacturer: Boehringer Ingelheim (registered from Boehringer Ingelheim Pharma GmbH & Co.KG)

Release forms: tablets 40, 80 mg (blisters)

Composition: telmisartan 40/80 mg

Pharmacological group: angiotensin II receptor antagonist

Pharmacological group according to ATK: C09CA07 Telmisartan

Pharmacological action: vasodilating, hypotensive, diuretic

Drug registration number: P No. 015387/01

Dates of registration, re-registration: 01.12.2003

RF HS codes: 3004 90 190 9

Pharmacodynamics: Angiotensin II (type AT1) receptor blocker. It has a vasodilating and hypotensive effect. It does not exhibit angiotensin receptor agonist properties and does not affect the state of ion channels involved in the regulation of the activity of the cardiovascular system. Does not inhibit ACE. Reduces both systolic and diastolic blood pressure without affecting heart rate. The onset of the hypotensive effect is 3 hours, a stable decrease in blood pressure is 4 weeks after the start of treatment. The duration of the hypotensive effect after a single dose is 24 hours.

Pharmacokinetics: When taken orally, it is rapidly absorbed from the gastrointestinal tract. Bioavailability - 50%. When taken simultaneously with food, the reduction in AUC ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). 3 hours after administration, the plasma concentration levels off, regardless of whether it is taken with food or on an empty stomach. Bonding with plasma proteins is 99.5%. The average apparent volume of distribution at the equilibrium stage is 500 l. Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive. T1/2 - more than 20 hours. Excreted through the intestines unchanged. Cumulative renal excretion is less than 1%. Total plasma clearance is 1 l/min (renal blood flow is 1.5 l/min).

Indications: Arterial hypertension.

Dosage regimen: Orally, 20-40 mg 1 time per day, if necessary - 80 mg/day. For liver failure, the maximum dose is 40 mg/day.

Side effects: From the nervous system: headache, dizziness, increased fatigue, insomnia, anxiety, depression, convulsions. From the respiratory system: upper respiratory tract infections (including pharyngitis, sinusitis, bronchitis), cough. From the cardiovascular system: marked decrease in blood pressure, palpitations, chest pain. From the digestive system: nausea, dyspepsia, diarrhea, abdominal pain, increased activity of “liver” transaminases. From the musculoskeletal system: myalgia, arthralgia, lower back pain. From the urinary system: peripheral edema, urinary tract infections, hypercreatininemia. Allergic reactions: skin rash, etc. Laboratory indicators: hyperkalemia, anemia, hyperuricemia. Other: influenza-like syndrome.

Overdose. Symptoms: marked decrease in blood pressure. Treatment: symptomatic. Hemodialysis is ineffective.

Contraindications: Hypersensitivity, pregnancy, lactation, biliary obstruction, childhood and adolescence.

Interaction: Increases the concentration of Li+ salts and digoxin in the blood serum by 20%. Diuretics and other antihypertensive drugs increase the risk of developing arterial hypotension. Potassium-sparing diuretics and K+ preparations increase the risk of hyperkalemia.

Special instructions: Before and during treatment, monitoring of blood pressure, renal function, and plasma K+ concentration is necessary. Drugs that affect the renin-angiotensin-aldosterone system can increase the concentration of urea in the blood and creatinine in the serum in patients with stenosis of the bilateral renal artery or artery of a separate kidney. In patients with reduced blood volume (as a result of diuretic therapy), with limited salt intake, dialysis, diarrhea and vomiting, symptomatic hypotension may develop. Transient hypotension is not a contraindication for further treatment with the drug after stabilization of blood pressure. If severe hypotension reoccurs, the dose should be reduced or the drug discontinued. In the presence of renal failure, treatment is carried out with caution under the control of plasma creatinine concentration.

Carefully. Bilateral renal artery stenosis, renal artery stenosis of a solitary kidney, liver and/or renal failure.

Side effects

From the central nervous system: depression , dizziness, headache , fatigue, anxiety, insomnia , convulsions .
From the respiratory system: diseases of the upper respiratory tract ( sinusitis , pharyngitis , bronchitis ), cough.
From the circulatory system: marked decrease in pressure , tachycardia , bradycardia , chest pain.
From the digestive system: nausea, diarrhea , dyspepsia , increased concentration of liver enzymes.
From the musculoskeletal system: myalgia , lower back pain, arthralgia .
From the genitourinary system: edema, infections of the genitourinary system, hypercreatininemia .
Hypersensitivity reactions: skin rash, angioedema , urticaria .
Laboratory indicators: anemia , hyperkalemia .
Other: erythema , itching, dyspnea .

Side effects of Micardis

The overall incidence of adverse events with telmisartan (41.4%) is generally comparable to placebo (43.9%) in placebo-controlled studies. The incidence of side effects does not depend on the dose and gender, age or race of patients. The adverse reactions listed below were identified in clinical trials involving 5,788 patients taking telmisartan. Infections and infestations : urinary tract infections (including cystitis), upper respiratory tract infections. Mental disorders: anxiety. On the part of the organ of vision: impaired accommodation (blurred vision). Vestibular disorders: dizziness. Gastrointestinal: abdominal pain, diarrhea, dry mouth, dyspepsia, flatulence, impaired stomach function. From the skin or subcutaneous tissue: eczema, increased sweating. Musculoskeletal and connective tissue disorders: arthralgia, back pain, calf cramps or leg pain, myalgia, tendinitis-like symptoms. General disorders: chest pain, flu-like symptoms. In addition, cases of erythema, pruritus, syncope/loss of consciousness, insomnia, depression, vomiting, hypotension (including orthostatic hypotension), bradycardia, tachycardia, hepatic dysfunction, renal dysfunction, including acute renal failure have been reported from post-marketing surveillance (see PRECAUTIONS). USE), hyperkalemia, dyspnea, anemia, eosinophilia, thrombocytopenia, weakness and lack of effectiveness. The incidence of these effects is not known. As with other angiotensin II antagonists, isolated cases of angioedema, urticaria and other similar reactions have been reported. Laboratory tests: rarely noted a decrease in hemoglobin levels or an increase in uric acid levels; also reported cases of increases in creatinine or liver enzymes, but the incidence was similar or lower compared with placebo. In addition, according to the results of post-marketing surveillance, cases of increased serum CPK levels were reported.

Mikardis, instructions for use

According to the instructions for use of Micardis, the drug is taken orally. For adults, the recommended dose is 40 mg once daily. In a number of patients, a therapeutic effect is observed even with a dose of 20 mg per day. If a decrease in pressure to the desired level is not observed, then the dose can be increased to 80 mg per day.

The maximum effect of the drug is achieved five weeks after the start of therapy.

In patients with severe forms of arterial hypertension, 160 mg of the drug per day can be used

Micardis®

In some patients, due to suppression of the RAAS, especially when using a combination of drugs acting on this system, renal function is impaired (including acute renal failure). Therefore, therapy accompanied by such dual blockade of the RAAS (for example, when adding an ACE inhibitor or a direct renin inhibitor, aliskiren to angiotensin II receptor antagonist blockers) should be carried out strictly individually and with careful monitoring of renal function (including periodic monitoring of serum potassium and creatinine concentrations ).

In cases where vascular tone and renal function depend primarily on the activity of the RAAS (for example, in patients with chronic heart failure or kidney disease, including bilateral renal artery stenosis, or stenosis of the artery of a single kidney), prescribing drugs that affect this system , may be accompanied by the development of acute arterial hypotension, hyperazotemia, oliguria, and, in rare cases, acute renal failure.

Based on the experience of using other drugs that affect the RAAS, when concomitantly prescribing MIKARDIS® and potassium-sparing diuretics, potassium-containing supplements, potassium-containing table salt, and other drugs that increase potassium levels in the blood (for example, heparin), this indicator should be monitored in patients.

In patients with diabetes mellitus and additional cardiovascular risk, for example, in patients with diabetes mellitus and coronary artery disease (CAD), when using drugs that lower blood pressure, such as angiotensin II receptor antagonists (ARAs) or ACE inhibitors, may increase the risk of fatal myocardial infarction and sudden cardiovascular death.

In patients with diabetes mellitus, CAD may be asymptomatic and therefore may be undiagnosed. In patients with diabetes mellitus, before starting the use of MIKARDIS®, appropriate diagnostic tests, including exercise testing, should be carried out to identify and treat coronary heart disease.

Alternatively, MIKARDIS® can be used in combination with thiazide diuretics, such as hydrochlorothiazide, which additionally have a hypotensive effect (for example, MIKARDIS-PLUS 40 mg/12.5 mg, 80 mg/12.5 mg).

In patients with primary aldosteronism, antihypertensive drugs whose mechanism of action is to inhibit the renin-angiotensin-aldosterone system are usually not effective.

Caution should be exercised when using MIKARDIS® (as well as other vasodilators) in patients with aortic or mitral stenosis, or hypertrophic obstructive cardiomyopathy.

Telmisartan is excreted mainly in bile. In patients with obstructive biliary disease or hepatic insufficiency, reduced clearance of the drug can be expected.

In patients with severe arterial hypertension, a dose of telmisartan 160 mg/day and in combination with hydrochlorothiazide 12.5-25 mg was well tolerated and effective.

Liver dysfunction when prescribed telmisartan was observed in most cases in Japanese residents.

MICARDIS® is less effective in black patients.

Interaction

Telmisartan activates the hypotensive effect of other blood pressure lowering drugs.

When telmisartan and digoxin , it is necessary to periodically determine the concentration of digoxin in the blood, as it may increase.

When taking lithium and ACE inhibitors lithium content in the blood may occur , which manifests itself as a toxic effect.

Treatment with non-steroidal anti-inflammatory drugs together with Micardis in dehydrated patients may lead to the development of acute renal failure.

Interactions of the drug Micardis

Telmisartan may potentiate the hypotensive effect of other antihypertensive agents. Compounds that were studied in pharmacokinetic studies: digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin and amlodipine. Only for digoxin, a 20% (in some cases 39%) increase in its concentration in the blood plasma relative to the average level is noted, so the need to monitor the level of digoxin in the blood plasma should be taken into account. When used simultaneously with lithium salts, it is possible to increase the concentration of lithium in the blood plasma and develop toxic reactions, therefore it is necessary to regularly monitor the level of lithium in the blood plasma. NSAID therapy (including acetylsalicylic acid in doses exceeding 0.3 g per day and COX-2 inhibitors) can lead to the development of acute renal failure in dehydrated patients. Compounds that affect the renin-angiotensin system, such as telmisartan, have a synergistic effect. When initiating combination therapy with NSAIDs and Micardis, patients should be provided with adequate hydration and close monitoring of renal function. During concomitant therapy with NSAIDs, a decreased effect of antihypertensive agents such as telmisartan has been reported due to inhibition of the vasodilatory effect of prostaglandins.

special instructions

For dehydrated patients (restriction of salt intake, treatment with diuretics , diarrhea , vomiting), a reduction in the dose of Micardis is necessary.

Prescribe with caution to persons with stenosis of both renal arteries , stenosis of the mitral valve or aorta, obstructive hypertrophic cardiomyopathy , severe renal, hepatic or heart failure, diseases of the digestive tract.

It is prohibited to use in case of primary aldosteronism and fructose intolerance .

If you are planning a pregnancy, you must find in advance a replacement for Micardis with another antihypertensive drug .

Use with caution when driving vehicles.

When taken simultaneously with lithium , monitoring of lithium levels in the blood is indicated, as a temporary increase in its level is possible.

Micardis analogs

Level 4 ATC code matches:
Telmisartan

Irbesartan

Presartan

Nortivan

Mikardis price

In Russia, a package of the drug 80 mg No. 28 will cost from 830 to 980 rubles. In Ukraine, the price of Mikardis in the same release form is close to 411 hryvnia.

Online pharmacies in RussiaRussia
Online pharmacies in UkraineUkraine
Online pharmacies in KazakhstanKazakhstan

ZdravCity

Mikardis tablets 40 mg 28 pcs. Boehringer Ingelheim Ellas AE
RUB 1,060 order
Micardis Plus tablets 80mg+12.5mg 28 pcs.Boehringer Ingelheim
RUB 1,147 order
Micardis tablets 80 mg 28 pcs. Boehringer Ingelheim Ellas AE
RUB 1,061 order

Pharmacy Dialogue

Micardis (tab. 80 mg No. 28) Boehringer Ingelheim
1104 rub. order
Mikardis (tab. 40 mg No. 28) Boehringer Ingelheim
1101 rub. order
Mikardis plus (tab. 80 mg/12.5 mg No. 28)Boehringer Ingelheim
RUB 1,123 order
Mikardis plus (tab. 80 mg/12.5 mg No. 28)Boehringer Ingelheim
1108 rub. order

Pharmacy24

Mikardis plus 80 mg N28 tablets Boehringer Ingelheim Pharma GmbH & Co. KG/Boehringer Ingelheim Ellas A.E., Nimechina/Greece
807 UAH.order
Mikardis 80 mg N28 tablets Boehringer Ingelheim Pharma GmbH & Co. KG/Boehringer Ingelheim Ellas A.E., Nimecchina/Greece
749 UAH. order

PaniPharmacy

Micardis tablets Micardis tablets. 80 mg No. 28 Germany, Boehringer Ingelheim Pharma
812 UAH order