Micardis, pills 40mg, 28pcs

Composition

Tablets are white or almost white in color, oblong, with the inscription “52 H” on one side and the company’s symbol on the other side. 1 tab. telmisartan 40 mgsupportable substances: sodium hydroxide, polyvidone (collidone 25), meglumine, sorbitol, magnesium stearate.

Pharmacological action

Clinical and pharmacological group: Angiotensin II receptor antagonistpharmacotherapy group: Angiotensin II receptor antagonistpharmacological action of an antihypertensive drug. Pharmacodynamics Emisartan is a specific angiotensin II receptor antagonist. It has a high affinity for the AT1 receptor subtype of angiotensin II, through which the action of angiotensin II is realized. Telmisartan displaces angiotensin II from binding to the receptor, without having an agonist effect on this receptor. It binds only to the AT1 receptor subtype of angiotensin II. Binding is long-term. Telmisartan has no affinity for other receptors (including AT2-receptors) and other less studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible overstimulation 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. It does not inhibit ACE (kininase II), an enzyme that also breaks down bradykinin, so an increase in bradykinin-induced side effects is not expected. Telmisartan at a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. The onset of antihypertensive action is noted within 3 hours after the first use of telmisartan. The effect of the drug persists for 24 hours and remains significant up to 48 hours. A pronounced hypotensive effect usually develops after 4-8 weeks of regular use. In patients with arterial hypertension, telmisartan reduces systolic and diastolic blood pressure without affecting heart rate. In the case of abrupt withdrawal of telmisartan, blood pressure gradually returns to its original level without the development of withdrawal syndrome. Pharmacokinetics of absorption When taken orally, telmisartan is rapidly absorbed from the gastrointestinal tract. Bioavailability – 50%. When taken simultaneously with food, the decrease in AUC values ranges from 6% (when used at a dose of 40 mg) to 19% (when used at a dose of 160 mg). After 3 hours after ingestion, the concentration in the blood plasma is equalized regardless of the time of food intake. Distribution Binding to plasma proteins is more than 99.5%, mainly with albumin and α1-glycoprotein. The average apparent Vd at steady state is 500 liters. Metabolismmetabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive. Vydaveniyet1 / 2-more than 20 hours. It is excreted through the intestines in unchanged form, excretion by the kidneys – less than 2% of the dose taken. Total plasma clearance is high (900 ml / min) compared to hepatic blood flow (about 1500 ml / min). Pharmacokinetics in special clinical cases, there is a difference in concentrations in men and women. In women, Cmax and AUC were approximately 3 and 2 times higher, respectively, than in men (with no significant effect on efficacy). The pharmacokinetics of telmisartan in elderly patients do not differ from the pharmacokinetics in young patients. No dose adjustment is required. No dose adjustment is required in patients with renal insufficiency, including patients on hemodialysis. Telmisartan is not removed by hemodialysis. In patients with mild to moderate hepatic impairment (Child-Pugh class A and B), the daily dose of the drug should not exceed 40 mg. The main indicators of telmisartan pharmacokinetics in children and adolescents aged 6-18 years after taking telmisartan at a dose of 1 mg / kg or 2 mg/kg for 4 weeks are generally comparable with those obtained in the treatment of adults, and confirm the non-linearity of telmisartan pharmacokinetics, especially with respect to Cmax.

Indications

-arterial hypertension; – reduction of cardiovascular morbidity and mortality in patients aged 55 years and older with a high risk of cardiovascular diseases.

Contraindications

-obstructive diseases of the biliary tract;- Severe hepatic impairment (Child-Pugh class C);- concomitant use with aliskiren in patients with diabetes mellitus or renal insufficiency (GFR;- age up to 18 years (efficacy and safety have not been established);— pregnancy; – breast-feeding period; – hypersensitivity to the Active ingredient or auxiliary components of the drug. With caution-bilateral renal artery stenosis or stenosis of the artery of a single kidney; – impaired liver and/or kidney function— – decreased BCC due to previous diuretic therapy, restriction of salt intake, diarrhea or vomiting;— hyponatremia; – hyperkalemia— – conditions after kidney transplantation (no experience of use);- chronic heart failure;— aortic and mitral valve stenosis; – idiopathic hypertrophic subaortic stenosis;- primary aldosteronism (efficacy and safety have not been established).

Side effects

The observed cases of side effects did not correlate with the gender, age, or race of the patients. Infections: sepsis, including fatal sepsis, urinary tract infections (including cystitis), upper respiratory tract infections. From the hematopoietic system: anemia, eosinophilia, thrombocytopenia. From the central nervous system: insomnia, anxiety, depression, syncope, vertigo. From the side of the organ of vision: visual disorders. From the cardiovascular system: marked decrease in blood pressure, orthostatic hypotension, bradycardia, tachycardia. Respiratory system disorders: shortness of breath. From the digestive system: abdominal pain, diarrhea, dry mouth, dyspepsia, flatulence, stomach discomfort, vomiting, liver function disorders/liver diseases* (*according to the results of post-marketing observations, most cases of liver function disorders/liver diseases were detected in patients in Japan). Allergic reactions: anaphylactic reactions, hypersensitivity (erythema, urticaria, angioedema), eczema, pruritus, rash (including drug), angioedema (fatal), toxic rash, hyperhidrosis. Musculoskeletal disorders: arthralgia, back pain, muscle spasms (calf cramps), lower limb pain, myalgia, tendon pain (symptoms similar to tendinitis). From the urinary system: impaired renal function (including acute renal failure). From the laboratory parameters: decreased hemoglobin, increased uric acid and creatinine concentrations in the blood, increased activity of liver enzymes, increased CPK activity, hyperkalemia, hypoglycemia (in patients with diabetes mellitus). Others: chest pain, flu-like syndrome, general weakness.

Interaction

Telmisartan may increase the antihypertensive effect of other antihypertensive agents. No other interactions of clinical significance have been identified. Co-use with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin and amlodipine did not result in clinically significant interactions. There was an increase in the average concentration of digoxin in blood plasma by an average of 20% (in one case by 39%). With simultaneous use 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, an increase in AUC0-24 and Cmax of ramipril and ramiprilat by 2.5 times was observed. The clinical significance of this phenomenon has not been established. With simultaneous use of ACE inhibitors and lithium preparations, a reversible increase in the concentration of lithium in the blood was observed, accompanied by toxic effects. In rare cases, such changes have been reported with the appointment of angiotensin II receptor antagonists. When prescribing lithium preparations and angiotensin II receptor antagonists at the same time, it is recommended to determine the concentration of lithium in the blood. Treatment with NSAIDs, including acetylsalicylic acid, COX-2 inhibitors, and non-selective NSAIDs, may cause acute renal failure in patients with dehydration. Drugs acting on the RAAS may have a synergistic effect. In patients receiving NSAIDs and telmisartan, BCC should be compensated at the beginning of treatment and renal function should be evaluated. A reduction in the effect of antihypertensive agents, such as telmisartan, by inhibiting the vasodilating effect of prostaglandins was observed with simultaneous therapy with NSAIDs.

How to take it, course of use and dosage

The drug is prescribed orally, regardless of food intake. In patients with arterial hypertension, the recommended initial dose of Micardis® is 1 tab. (40 mg) 1 time/day. In cases where the therapeutic effect is not achieved, the dose of the drug can be increased to 80 mg 1 time / 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. To reduce cardiovascular morbidity and mortality, the recommended dose is 1 tab. (80 mg) 1 time/day. In the initial period of treatment, additional blood pressure correction may be required. Patients with renal insufficiency (including those on hemodialysis) do not need to adjust the dose of the drug. In patients with mild to moderate hepatic impairment (Child-Pugh class A and B), the daily dose of the drug should not exceed 40 mg. The dosage regimen in elderly patients does not require changes.

Overdose

No cases of overdose have been identified. Symptoms: marked decrease in blood pressure, tachycardia, bradycardia. Treatment: performing symptomatic therapy. Hemodialysis is ineffective.

Special instructions

In some patients, renal function (including acute renal failure) is impaired due to suppression of the RAAS, especially when using a combination of agents acting on this system. Therefore, therapy accompanied by such a double blockade of the RAAS (for example, when adding ACE inhibitors or a direct renin – aliskiren inhibitor 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 renal artery stenosis or stenosis of the artery of a single kidney), the use 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, when Micardis® is prescribed simultaneously with potassium-sparing diuretics, potassium-containing supplements, potassium-containing food salt, or other agents that increase the concentration of potassium 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 CHD, the use of blood pressure-lowering drugs, such as angiotensin II receptor antagonists or ACE inhibitors, may increase the risk of fatal myocardial infarction and sudden cardiovascular death. In patients with diabetes mellitus, CHD may be asymptomatic and therefore may be undiagnosed. Before starting the use of Micardis® for the detection and treatment of CHD, appropriate diagnostic tests should be performed, including a test with physical activity. Alternatively, Micardis® can be used in combination with thiazide diuretics, such as hydrochlorothiazide, which additionally have a hypotensive effect (for example, Micardis® Plus 40 mg/12.5 mg,80 mg/12.5 mg). In patients with primary aldosteronism, antihypertensive drugs, the mechanism of action of which is to inhibit the RAAS, are usually not effective. Caution should be exercised when using Micardis® (as well as other vasodilators) in patients with aortic or mitral stenosis and hypertrophic obstructive cardiomyopathy. Telmisartan is mainly excreted in the bile. In patients with obstructive biliary tract diseases or hepatic insufficiency, a decrease in drug clearance can be expected. In patients with severe hypertension, a dose of telmisartan 160 mg / day in combination with hydrochlorothiazide 12.5-25 mg was effective and well tolerated. Hepatic dysfunction in the use of telmisartan in most cases was observed in residents of Japan. Micardis® is less effective in black patients. Effect on the ability to drive motor vehicles and manage mechanismspecial clinical studies of the effect of the drug on the ability to drive a car and mechanisms have not been conducted. However, when driving a car and working with mechanisms, the possibility of dizziness and drowsiness should be taken into account, which requires caution.

Storage conditions

The drug should be stored out of the reach of children, protected from moisture at a temperature not exceeding 30°C.

Shelf

life is 4 years.

Active ingredient

Telmisartan

Conditions of release from pharmacies

By prescription

Dosage form

Tablets