Mikardis - instructions for use, dose, side effects, contraindications

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 m g

White or almost white oblong-shaped tablets, on one side engraving "51H", on the other side - the symbol of the firm.

Tablets 80 mg

White or almost white oblong pill forms, on one side engraving "52H", on the other side - the symbol of the firm.

Pharmacotherapeutic group:angiotensin II receptor antagonist.

ATX: & nbsp

C.09.C.A.07 Telmisartan

Pharmacodynamics:

Telmisartan is a specific angiotensin II receptor antagonist (type AT1), effective at ingestion. Has a high affinity for the subtype AT1 receptors of angiotensin II, through which the action of angiotensin II is realized. Releases angiotensin II from binding to a receptor, without the action of an agonist for this receptor. Telmisartan binds only to the subtype AT | receptors of angiotensin II. Communication bears lasting character. Has no affinity for other receptors, including AT₂receptor and other, less studied receptors of angiotensin. The functional significance of these receptors, as well as the effect of their possible excessive stimulation with angiotensin II, whose concentration 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 the ion channels. Telmisartan does not inhibit the angiotensin-converting enzyme (kininase II) (an enzyme that also breaks down bradykinin). Therefore, the enhancement of bradykinin-induced side effects is not expected.

Patients telmisartan in 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 administration of telmisartan.The effect of the drug persists for 24 hours and remains significant up to 48 hours. The expressed hypotensive effect usually develops in 4-8 weeks after regular admission.

In patients suffering from hypertension, telmisartan reduces systolic and diastolic blood pressure (BP), without affecting the heart rate (heart rate).

In the case of a sharp cancellation of telmisartan, blood pressure gradually returns to the initial level without the development of the "withdrawal" syndrome.

Pharmacokinetics:When ingested quickly absorbed from the gastrointestinal tract. Bioavailability - 50%. At reception simultaneously with food decrease AUC (the area under the concentration-time curve) ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). After 3 hours after taking the concentration in the blood plasma levels, regardless of the time of eating. There is a difference in plasma concentrations in men and women. FROM_max (maximum concentration) and AUC were approximately 3 and 2 times, respectively, higher in women than in men without significant effect on efficacy.

The connection with blood plasma proteins is 99.5%, in mainly with albumin and alpha-1 glycoprotein. The average value of the apparent volume of distribution in the equilibrium concentration - 500 liters.

Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive. The half-life (T_1/2) - more than 20 hours. Output through the intestine in an unchanged form, excretion by the kidneys - less than 2% of the dose. Total plasma clearance High (900 ml / min) compared with the "hepatic" blood flow (about 1500 ml / min.).

Elderly patients

The pharmacokinetics of telmisartan in elderly patients does not differ from young patients. Dose correction is not required.

Patients with renal insufficiency

A dose change in patients with renal insufficiency is not required, including patients on hemodialysis. Telmisartan not removed by hemodialysis.

Patients from hepatic insufficiency

In patients with mild and moderate impairment of liver function (class A and B on the Child-Pugh scale), the daily dose of the drug should not exceed 40 mg.

Pediatric Use

The main indicators of the pharmacokinetics of telmisartan in children aged 6 to 18 years after receiving telmisartan at a dose of 1 mg / kg or 2 mg / kg for 4 weeks are generally comparable to those obtained in the treatment of adults and confirm the non-linearity of the pharmacokinetics of telmisartan , especially with respect to C_max.

Indications:

- Arterial hypertension.

- Reduction of cardiovascular morbidity and mortality in patients aged 55 years and older with a high risk of cardiovascular disease.

Contraindications:

Hypersensitivity to the active substance or auxiliaries of the drug
Pregnancy
Breastfeeding period
Obstructive diseases of the biliary tract
Severe violations of liver function (class C on the Child-Pugh scale)
The simultaneous use of the drug MICARDAIS with aliskiren in patients with diabetes mellitus or renal insufficiency (glomerular filtration rate (GFR) <60 ml / min / 1.73 m²)
Fructose intolerance and glucose / galactose absorption disorder or sucrose / isomaltase insufficiency
Age to 18 years (efficiency and safety not established)

Carefully:

Two-sided stenosis of the renal arteries or stenosis of the artery of a single kidney
Violations of the liver and / or kidney function (see section Special instructions)
Reduction of the volume of circulating blood (BCC) as a result of previous diuretic therapy, restriction of salt intake, diarrhea or vomiting
Hyponatremia
Hyperkalemia
Conditions after kidney transplantation (no experience of application)
Chronic heart failure
Stenosis of the aortic and mitral valve
Idiopathic hypertrophic subaortic stenosis
Primary aldosteronism (efficacy and safety not established)

Pregnancy and lactation:The use of the drug MICARDI is contraindicated during pregnancy. The use of angiotensin II receptor antagonists during the first trimester of pregnancy is not recommended, these drugs should not be administered during pregnancy. When diagnosing pregnancy, the drug should be stopped immediately. If necessary, alternative therapy should be prescribed (other classes of antihypertensive drugs permitted for use during pregnancy). The use of angiotensin II receptor antagonists during the second and third trimesters of pregnancy is contraindicated. Pre-clinical studies of telmisartan did not reveal teratogenic effects, but fetotoxicity was established. It is known that the effect of angiotensin II receptor antagonists during the second and third trimesters of pregnancy causes a person

fetotoxicity (decreased kidney function, oligohydroamnion, delayed ossification of the skull), as well as neonatal toxicity (kidney failure, hypotension, hyperkalemia). Patients planning pregnancy should be prescribed alternative therapy. If treatment with antagonists of angiotensin II receptors occurred during the second trimester of pregnancy, an ultrasound scan of the kidney function and skull condition in the fetus is recommended.

Newborns whose mothers received angiotensin II receptor antagonists should be carefully monitored for hypotension.

Therapy with the drug MICARDI is contraindicated in the period of breastfeeding.

Studies of the impact on human fertility have not been conducted.

Dosing and Administration:

Inside, regardless of food intake.

Arterial hypertension

The initial recommended dose of the drug Mikardis ® is 1 tab. (40 mg) once a day. In cases where a therapeutic effect is not achieved, the maximum recommended dose of Mikaridis® can be increased to 80 mg once daily. 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 Mikardis ® 80 mg, once a day.

In the initial period of treatment, an additional correction of blood pressure may be required.

Impaired renal function

In patients with renal insufficiency, including in patients on hemodialysis, correction of the dosing regimen is not required.

Impaired liver function

In patients with mild or moderate impairment of liver function (class A and B on the Child-Pugh scale, respectively), the daily dose of Mikardis® should not exceed 40 mg.

Elderly patients

Dosing regimen does not require any changes.

Side effects:

Observed cases of side effects were not correlated with gender, age or race of patients.

Infections:

sepsis, including sepsis with lethal outcome, urinary tract infection (including cystitis), upper respiratory tract infections.

From the hemopoietic and lymphatic system:

anemia, eosinophilia, thrombocytopenia.

From the central nervous system:

anxiety, insomnia, depression, fainting, vertigo.

From the side of the organ of vision:

visual disorders.

From the side of cardiovascular system:

bradycardia, tachycardia, expressed reduction of blood pressure, orthostatic hypotension.

From the respiratory system:

dyspnea.

From the digestive system:

abdominal pain, diarrhea, dry mouth, Dyspepsia, flatulence, discomfort in the stomach, vomiting, abnormal liver / liver disease function * (* as a result of postmarketing observations, in most cases, violations of the liver / liver function disorders have been identified in Japanese patients).

Allergic reactions:

anaphylactic reactions, increased sensitivity (erythema, urticaria, angioedema), eczema, itching, rash (including dosage), angioedema (fatal), rash, toxic rash.

From the side of the locomotor system apparatus:

arthralgia, back pain, muscle spasms (spasms of gastrocnemius muscles), pain in lower extremities, myalgia, pain in the tendons (symptoms similar to the manifestation of tendinitis).

From the side of the kidneys and urinary tract:

impaired kidney function, including acute renal failure.

Are common:

chest pain, flu-like symptoms, fatigue, hyperkalemia, hypoglycemia (in diabetic patients).

Laboratory indicators: a decrease in hemoglobin concentration, an increase in the concentration of uric acid, creatinine in the blood, an increase in the activity of "hepatic" enzymes, an increase in the concentration of creatine phosphokinase (CKF).

Overdose:

Cases of overdose have not been identified.

Symptoms: marked decrease in blood pressure, tachycardia, bradycardia.

Treatment: symptomatic therapy, hemodialysis is not effective.

Interaction:

Telmisartan may increase the antihypertensive effect of other antihypertensive agents. Other types of interactions that have clinical relevance have not been identified.

Combined use with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin and amlodipine does not lead to clinically significant interaction. An increase in the average concentration of digoxin in the blood plasma was observed on average by 20% (in one case by 39%). With the simultaneous administration 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 AUCo-24 and C_max ramipril and ramiprilata 2.5 times. The clinical significance of this phenomenon is not established.

When concomitant administration of angiotensin converting enzyme inhibitors (ACE) and lithium preparations mentioned reversible increase the concentration of lithium in the blood, accompanied by toxic effects. In rare cases, such changes were registered with the appointment of angiotensin II receptor antagonists. When concomitant administration of drugs lithium and angiotensin II receptor antagonists recommended determining the concentration of lithium in the blood.

Treatment of non-steroidal antiinflammatory drugs (NSAIDs), including aspirin, COX-2 inhibitors (COX-2) and non-selective NSAIDs may cause the development of acute renal failure in dehydrated patients. Drugs that act on the renin-angiotensin-aldosterone system (RAAS), may have a synergistic effect. In patients receiving NSAIDs and telmisartan, at the beginning of treatment should be compensated for BCC and kidney function monitoring performed.

Reduction of the effect of antihypertensive agents, such as telmisartan, by inhibiting the vasodilating effect of prostaglandins was noted in the joint treatment with NSAIDs.

Special instructions:

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

In cases of vascular tone and renal function, mainly from RAAS activity (for example, in patients with chronic heart failure or kidney disease, including bilateral renal artery stenosis, or stenosis of the single kidney artery), administration of drugs that affect this system , can be accompanied by the development of acute arterial hypotension, hyperaemia, oliguria, and, in rare cases, acute renal failure.

Based on the experience of using other agents that affect RAAS, with the joint appointment of the drug MICARDI and potassium-sparing diuretics,potassium-containing additives, potassium-containing edible salt, other agents that increase the potassium content in the blood (for example, heparin), this indicator should be monitored in patients.

In patients with diabetes mellitus and an additional cardiovascular risk, for example, in patients with diabetes mellitus and coronary heart disease (CHD), in the case of drugs that lower blood pressure, such as angiotensin II receptor antagonists (ARAPs) or ACE inhibitors, can increase the risk of fatal myocardial infarction and sudden cardiovascular death. In patients with diabetes, IHD can be asymptomatic and therefore can be undiagnosed. In patients with diabetes mellitus, before starting the use of the drug MICARIDIS for the identification and treatment of IHD, appropriate diagnostic tests should be carried out, including a physical exercise test.

Alternatively, MICARIDIS may be used in combination with thiazide diuretics, such as hydrochlorothiazide, which additionally have an antihypertensive effect (for example, the preparation of MICARDI-PLUS 40 mg / 12.5 mg, 80 mg / 12.5 mg).

In patients with primary aldosteronism, antihypertensive drugs, whose mechanism of action is inhibition of the renin-angiotensin-aldosterone system, are generally not effective. Care should be taken when using the drug MICARDI (as well as other vasodilators) in patients with aortic or mitral stenosis, or with hypertrophic obstructive cardiomyopathy.

Telmisartan is excreted mainly with bile. In patients with obstructive diseases of the biliary tract or liver failure, a decrease in the clearance of the drug can be expected.

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. Disorders of liver function in the appointment of telmisartan in most cases were observed in the inhabitants of Japan. Mycardis is less effective in patients of the Negroid race.

Effect on the ability to drive transp. cf. and fur:

Special clinical studies of the effect of the drug on the ability to control the car and mechanisms were not carried out.However, when driving and working with machinery, one should take into account the possibility of developing dizziness and drowsiness, which requires caution.

Form release / dosage:

Tablets of 40 mg and 80 mg.

Packaging:For 7 tablets in a blister of polyamide / aluminum / PVC. For 2 or 4 blisters with instructions for use in a cardboard box (for a dosage of 40 mg). For 2, 4 or 8 blisters with instructions for use in a cardboard pack (for a dosage of 80 mg).

Storage conditions:

Store at temperatures not higher than 30 ° C, in the original packaging.

Keep out of the reach of children!

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

Terms of leave from pharmacies:On prescription

Registration number:П N015387 / 01

Date of registration:22.10.2008 / 29.09.2014

Expiration Date:Unlimited

The owner of the registration certificate:Boehringer Ingelheim International GmbHBoehringer Ingelheim International GmbH Germany

Manufacturer: & nbsp

Boehringer Ingelheim Pharma GmbH & Co. KG

Representation: & nbspBehringer Ingelheim, LLCBehringer Ingelheim, LLC

Information update date: & nbsp24.04.2018

Illustrated instructions

Instructions

Mycardis® (Micardis®)