Mikardis tablets 40mg, No. 28

• Arterial hypertension.

• Reducing cardiovascular morbidity and mortality in patients aged 55 and over with a high risk of cardiovascular disease.

Inside, regardless of food intake.
Arterial hypertension The
initial recommended dose of MikardisЃ is 1 tab. (40 mg) once a day. In cases where the therapeutic effect is not achieved, the maximum recommended dose of MikardisЃ can be increased to 80 mg once a day. When deciding whether to increase the dose, it should be taken into account that the maximum antihypertensive effect is usually achieved within 4-8 weeks after the start of treatment.
Reduction of cardiovascular morbidity and mortality The
recommended dose is 1 tablet of MikardisЃ 80 mg, i times a day.
In the initial period of treatment, additional correction of blood pressure may be required.
Impaired renal function
In patients with renal failure, including those on hemodialysis, no dosage adjustment is required.
Liver dysfunction
In patients with mild and moderate hepatic dysfunction (class A and B on the Child-Pugh scale, respectively), the daily dose of MikardisЃ should not exceed 40 mg.
Elderly patients
The dosage regimen does not require changes.

1 tablet contains:
Active ingredient : - Telmisartan 40 mg
Excipients : - Sodium hydroxide 3.36 mg, Polyvidone (Kollidon 25) 12 mg, meglumine 12 mg, sorbitol 168.64 mg, magnesium stearate 4 mg.

• Hypersensitivity to the active substance or auxiliary components of the drug

• Pregnancy

• Breastfeeding period

• Obstructive diseases of the biliary tract

• Severe liver dysfunction (class C on the Child-Pugh scale)

• Hereditary fructose intolerance (contains sorbitol)

• Age under 18 years of age (efficacy and safety have not been established)

Carefully

• Bilateral renal artery stenosis or stenosis of an artery of a solitary kidney,

• Dysfunction of the liver and / or kidneys (see also Special instructions),

• Decreased circulating blood volume (BCC) due to previous diuretic therapy, restriction of salt intake, diarrhea, or vomiting

• Hyponatremia

• Hyperkalemia

• Conditions after kidney transplantation (no experience with use),

• Chronic heart failure

• Stenosis of the aortic and mitral valves,

• Idiopathic hypertrophic subaortic stenosis,

• Primary aldosteronism (efficacy and safety not established)

Trade name of the drug : MikardisЃ

International Non-Proprietary Name (INN) : Telmisartan

Dosage form : tablets

Composition : 1 tablet contains:
Active substance : - Telmisartan 40 mg or 80 mg;
Excipients : - sodium hydroxide 3.36 mg / 6.72 mg, polyvidone (Kollidon 25) 12 mg / 24 mg, meglumine 12 mg / 24 mg, sorbitol 168.64 mg / 337.28 mg, magnesium stearate 4 mg / 8 mg.

Description
Tablets 40 mg
White or almost white oblong tablets, engraved on one side '51H', on the other side - the symbol of the company.
Tablets 80 mg
White or almost white oblong tablets, engraved on one side '52H', on the other side - the symbol of the company.

Pharmacotherapeutic group : angiotensin II receptor antagonist.

Pharmacological properties
Pharmacodynamics
Telmisartan is a specific angiotensin II receptor antagonist (type AT1), effective when taken orally. It has a high affinity for the AT1 subtype of angiotensin II receptors, through which the action of angiotensin II is realized. Displaces angiotensin I from the connection with the receptor, without having an agonist effect on this receptor.
Telmisartan binds only to the AT1 subtype of angiotensin II receptors. Communication is long lasting. It has no affinity for other receptors, including the AT2 receptor and other less studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible excessive stimulation with angiotensin II, the concentration of which increases with the appointment of telmisartan, have not been studied. Reduces the concentration of aldosterone in the blood, does not inhibit renin in the blood plasma and does not block ion channels. Telmisartan does not inhibit angiotensin-converting enzyme (kininase II) (an enzyme that also breaks down bradykinin). Therefore, an increase in the side effects caused by bradykinin is not expected.
In patients, telmisartan at a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. The onset of hypotensive action is noted within 3 hours after the first telmisartan administration. The effect of the drug lasts for 24 hours and remains significant up to 48 hours. A pronounced hypotensive effect usually develops 4-8 weeks after regular intake.
In patients with arterial hypertension, telmisartan reduces systolic and diastolic blood pressure (BP) without affecting the heart rate (HR).
In the case of abrupt withdrawal of telmisartan, blood pressure gradually returns to the initial level without the development of a 'withdrawal' syndrome.

Pharmacokinetics
When administered orally, it is rapidly absorbed from the gastrointestinal tract. Bioavailability -50%. When taken simultaneously with food, the decrease in AUC (area under the concentration-time curve) ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). 3 hours after ingestion, the concentration in the blood plasma levels off, regardless of the meal. There is a difference in plasma concentrations in men and women. Cmax (maximum concentration) and AUC were approximately 3 and 2 times, respectively, higher in women compared with men, with no significant effect on efficacy.
The connection with blood plasma proteins is 99.5%, mainly with albumin and alpha-1 glycoprotein.
The average value of the apparent volume of distribution at equilibrium concentration is 500 liters. Metabolized by conjugation with glucuronic acid. The metabolites are pharmacologically inactive. The half-life (T?) Is more than 20 hours. It is excreted through the intestines unchanged, excretion by the kidneys is less than 2%. The total plasma clearance is high (900 ml / min.) In comparison with the 'hepatic' blood flow (about 1500 ml / min.).
Elderly patients The
pharmacokinetics of telmisartan in elderly patients does not differ from young patients. No dose adjustment is required.
Patients with renal insufficiency
Dose adjustment is not required in patients with renal insufficiency, including patients on hemodialysis.
Telmisartan is not removed by hemodialysis.
Patients with hepatic impairment
In patients with mild to moderate liver dysfunction (class A and B on the Child-Pugh scale), the daily dose of the drug should not exceed 40 mg.
In children
The main indicators of the pharmacokinetics of telmisartan in children aged 6 to 18 years are, in general, comparable to those obtained in the treatment of adults, and confirm the nonlinearity of the pharmacokinetics of telmisartan, especially in relation to Cmax.

Indications for use

• Arterial hypertension.

• Reducing cardiovascular morbidity and mortality in patients aged 55 and over with a high risk of cardiovascular disease.

Contraindications

• Hypersensitivity to the active substance or auxiliary components of the drug

• Pregnancy

• Breastfeeding period

• Obstructive diseases of the biliary tract

• Severe liver dysfunction (class C on the Child-Pugh scale)

• Hereditary fructose intolerance (contains sorbitol)

• Age under 18 years of age (efficacy and safety have not been established)

Carefully

• Bilateral renal artery stenosis or stenosis of an artery of a solitary kidney,

• Dysfunction of the liver and / or kidneys (see also Special instructions),

• Decreased circulating blood volume (BCC) due to previous diuretic therapy, restriction of salt intake, diarrhea, or vomiting

• Hyponatremia

• Hyperkalemia

• Conditions after kidney transplantation (no experience with use),

• Chronic heart failure

• Stenosis of the aortic and mitral valves,

• Idiopathic hypertrophic subaortic stenosis,

• Primary aldosteronism (efficacy and safety not established)

Method of administration and dosage
Inside, regardless of food intake.
Arterial hypertension The
initial recommended dose of MikardisЃ is 1 tab. (40 mg) once a day. In cases where the therapeutic effect is not achieved, the maximum recommended dose of MikardisЃ can be increased to 80 mg once a day. When deciding whether to increase the dose, it should be taken into account that the maximum antihypertensive effect is usually achieved within 4-8 weeks after the start of treatment.
Reduction of cardiovascular morbidity and mortality The
recommended dose is 1 tablet of MikardisЃ 80 mg, i times a day.
In the initial period of treatment, additional correction of blood pressure may be required.
Impaired renal function
In patients with renal failure, including those on hemodialysis, no dosage adjustment is required.
Liver dysfunction
In patients with mild and moderate hepatic dysfunction (class A and B on the Child-Pugh scale, respectively), the daily dose of MikardisЃ should not exceed 40 mg.
Elderly patients
The dosage regimen does not require changes.

Side effects The
observed incidence of side effects did not correlate with gender, age or race of patients.
Infections :
Sepsis, including fatal sepsis, urinary tract infections (including cystitis), upper respiratory tract infections.
From the circulatory and lymphatic system :
anemia, eosinophilia, thrombocytopenia.
From the side of the central nervous system :
Anxiety, insomnia, depression, fainting.
From the side of the organs of vision and hearing :
Visual disturbances, dizziness.
From the side of the cardiovascular system :
Bradycardia, tachycardia, marked decrease in blood pressure, orthostatic hypotension
From the respiratory system:
Shortness of breath.
From the digestive system :
Abdominal pain, diarrhea, dry mouth, dyspepsia, flatulence, stomach discomfort, vomiting, liver dysfunction.
Allergic reactions:
Anaphylactic reactions, hypersensitivity to the active substance or auxiliary components of the drug, angioedema (fatal), eczema, erythema, pruritus, rash (including drug), hyperhidrosis, urticaria, toxic rash.
From the musculoskeletal system :
Arthralgia, back pain, muscle spasms (cramps of the calf muscles), pain in the lower extremities, myalgia, pain in the tendons (symptoms similar to tendonitis).
On the part of the kidneys and urinary tract :
Impaired renal function, including acute renal failure.
General :
Chest pain, flu-like syndrome, asthenia (weakness), hyperkalemia, hypoglycemia (in patients with diabetes mellitus).
Laboratory indicators : A
decrease in the concentration of hemoglobin, an increase in the concentration of uric acid, creatinine in the blood, an increase in the activity of 'liver' enzymes, an increase in the concentration of creatine phosphokinase (CPK).

Overdose
No cases of overdose have been identified.
Symptoms : marked decrease in blood pressure, tachycardia, bradycardia.
Treatment : symptomatic therapy, hemodialysis is not effective.

Interaction with other drugs
Telmisartan can increase the hypotensive effect of other antihypertensive drugs. Other types of interactions with clinical significance have not been identified. Combined use with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin and amlodipine does not lead to clinically significant interactions. An increase in the average concentration of digoxin in blood plasma by an average of 20% (in one case by 39%) was noted. With the simultaneous appointment of telmisartan and digoxin, it is advisable to periodically determine the concentration of digoxin in the blood.
With the simultaneous use of telmisartan and ramipril, there was an increase in AUC0-24 and Cmax of ramipril and ramiprilat by 2.5 times. The clinical significance of this phenomenon has not been established.
With the simultaneous administration of angiotensin-converting enzyme (ACE) inhibitors and lithium preparations, a reversible increase in the concentration of lithium in the blood was noted, accompanied by a toxic effect. In rare cases, such changes have been reported with the appointment of angiotensin II receptor antagonists. With the simultaneous appointment of lithium preparations and angiotensin II receptor antagonists, it is recommended to determine the concentration of lithium in the blood.
Treatment with non-steroidal anti-inflammatory drugs (NSAIDs), including acetylsalicylic acid, cyclooxygenase-2 (COX-2) inhibitors, and non-selective NSAIDs, can cause acute renal failure in dehydrated patients. Drugs acting on the renin-angiotensin-aldosterone system (RAAS) may have a synergistic effect. In patients receiving NSAIDs and telmisartan, at the beginning of treatment, BCC should be compensated and renal function monitored.
A decrease in the effect of antihypertensive drugs such as telmisartan, by inhibiting the vasodilating effect of prostaglandins, has been observed with concomitant treatment with NSAIDs.

Special instructions
In some patients, due to the suppression of the RAAS, especially when using a combination of agents acting on this system, renal function is impaired (including acute renal failure). Therefore, therapy, accompanied by a similar double blockade of the RAAS, should be carried out strictly individually and with careful monitoring of renal function (including periodic monitoring of the concentration of potassium and creatinine in serum).
In cases of dependence of vascular tone and renal function mainly on the activity of the RAAS (for example, in patients with chronic heart failure, or kidney disease, including renal artery stenosis, or stenosis of the artery of a single kidney), the appointment of 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, with the joint appointment of MikardisЃ and potassium-sparing diuretics, potassium-containing supplements, potassium-containing food salt, and other drugs that increase the concentration of potassium in the blood (for example, heparin), this indicator should be monitored in patients.
Alternatively, MikardisЃ can be used in combination with thiazide diuretics, such as hydrochlorothiazide, which additionally have an antihypertensive effect (for example, MikardisPlusЃ 40 mg / 12.5 mg, 80 mg /) 2.5 mg).
In patients with severe arterial hypertension, the dose of telmisartan 160 mg / day and in combination with hydrochlorothiazide 12.5-25 mg was well tolerated and effective. MikardisЃ is less effective in black patients.

Influence on the ability to drive a car and work with mechanisms
Special clinical studies of the effect of the drug on the ability to drive a car and mechanisms have not been conducted. However, when driving and operating machinery, the possibility of dizziness and drowsiness should be taken into account, which requires caution.

Release form
Tablets 40 mg and 80 mg.
7 tablets per blister made of polyamide / aluminum / PVC. 2 or 4 blisters with instructions for use in a cardboard box (for a dosage of 40 mg). 2, 4 or 8 blisters with instructions for use in a cardboard box (for a dosage of 80 mg).

Storage conditions
List B.
Store at a temperature not exceeding 30 ? C in a place protected from moisture.
Keep out of the reach of children!

Shelf life is
4 years. Do not use after the expiration date.

Terms of dispensing from pharmacies
Prescription.