Telmisartan-SZ pills 40mg, 30pcs

Composition

1 tablet contains:

Active ingredient: telmisartan-40 mg

excipients: sodium hydroxide-3.4 mg; povidone K 30 (polyvinylpyrrolidone medium molecular weight) -12.0 mg; meglumine -12.0 mg; mannitol -165.2 mg; magnesium stearate-2.4 mg; talc-5.0 mg

Pharmacological action

Pharmacodynamics

Telmisartan is a specific angiotensin II receptor antagonist (type AT, ) that is effective when taken orally. It has a high affinity for the At subtype of angiotensin II receptors, through which the action of angiotensin II is realized. Displaces angiotensin II from binding to the receptor, without having an agonist effect on this receptor.

Telmisartan binds only to the AT subtype of angiotensin II receptors. The relationship is long-term. It has no affinity for other receptors, including the AT2 receptor and other less well-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. Telmisartan does not inhibit the angiotensin-converting enzyme (kininase II) (an enzyme that also breaks down bradykinin). Therefore, an increase in bradykinin-induced side effects is not expected.

In patients, telmisartan 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 for up to 48 hours. A pronounced antihypertensive effect usually develops 4-8 weeks after regular oral use.

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 its original level without the development of “withdrawal”syndrome.

Pharmacokinetics

When taken 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). After 3 hours after ingestion, the concentration in the blood plasma is leveled, regardless of the time of food intake. There is a difference in plasma concentrations in men and women. Maxax (maximum concentration) and AUC were approximately 3 and 2 times higher in women compared to men, respectively, with no significant effect on efficacy.

The relationship with plasma proteins is 99.5%, mainly with albumin and alpha-1 glycoprotein. The average apparent volume of distribution at equilibrium concentration is 500 liters. It is metabolized by conjugation with glucuronic acid. The metabolites are pharmacologically inactive. The half-life is more than 20 hours. It is excreted unchanged through the intestines, excretion by the kidneys is less than 2% of the dose taken, the total plasma clearance is high (900 ml / min) compared to the “hepatic” blood flow (about 1500 ml / min).

Elderly patients

The pharmacokinetics of telmisartan in elderly patients do not differ from young patients. No dose adjustment is required.

Patients with renal insufficiency

No dose adjustment is required in patients with renal insufficiency, including patients on hemodialysis Telmisartan is not removed by hemodialysis.

Patients with hepatic insufficiency

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

Application in pediatrics

The main indicators of telmisartan pharmacokinetics in children 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 C_

Indications

-Arterial hypertension.

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

Contraindications

-Hypersensitivity to the Active ingredient or auxiliary components

of the drug-Pregnancy

-Breast

-feeding period-Obstructive biliary tract diseases

-Severe liver function disorders (Child-Pugh class C)

– Concomitant use of Telmisartan-SZ with aliskiren in patients with diabetes mellitus or renal insufficiency (glomerular filtration rate (GFR)

– Age up to 18 years (efficacy and safety have not been established)

WITH CAUTION

-Bilateral renal artery stenosis or stenosis of the artery of a single kidney

-Impaired liver and/or kidney function (see section “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)

– Chronic heart failure

– Aortic and mitral valve stenosis

-Hypertrophic obstructive cardiomyopathy

-Primary aldosteronism (efficacy and safety have not been established)

– Hemodialysis

USE DURING PREGNANCY AND LACTATION

The use of Telmisartan-SZ is contraindicated during pregnancy. The use of angiotensin II receptor antagonists during the first trimester of pregnancy is not recommended, and these drugs should not be prescribed during pregnancy. If pregnancy is diagnosed, the drug should be stopped immediately. If necessary, alternative therapy (other classes of antihypertensive drugs approved for use during pregnancy) should be prescribed.

The use of angiotensin II receptor antagonists during the second and third trimesters of pregnancy is contraindicated.

In preclinical studies of telmisartan, no teratogenic effects were detected, but fetotoxicity was established. It is known that exposure to angiotensin II receptor antagonists during the second and third trimesters of pregnancy causes fetotoxicity in humans (decreased renal function, oligohydroamnion, slowing of cranial ossification), as well as neonatal toxicity (renal failure, hypotension, hyperkalemia). Patients planning pregnancy should be given alternative therapy. If treatment with angiotensin II receptor antagonists occurred during the second trimester of pregnancy, ultrasound evaluation of renal function and the condition of the fetal skull is recommended.

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

Telmisartan-SZ therapy is contraindicated during breastfeeding

Studies on the effect on fertility have not been conducted.

Side effects

The observed cases of side effects did not correlate with the gender, age, or race of the patients.

World Health Organization (WHO) classification of side effects: very common >1/10>

common >1/100 to ><1/10

uncommon >1/1000 to ><1/100

rare >1/10000 to ><1/1000

very rare < 1/10000

frequency unknown cannot be estimated based on available data.

Infections:

Infrequently: urinary tract infections (including cystitis), upper respiratory tract infections;

Rare: thrombocytopenia;

Frequency unknown: eosinophilia.

From the central nervous system:

Infrequently: insomnia, drowsiness, depression, vertigo;

Rare: fainting, anxiety.

From the side of the visual organ:

Rare: visual disorders.

From the cardiovascular system:

Infrequently: bradycardia, marked decrease in blood pressure, orthostatic hypotension;

Rare: tachycardia.

Respiratory system disorders:

Infrequently: shortness of breath, cough.

From the digestive system:

Infrequently: abdominal pain, diarrhea, dyspepsia, flatulence, vomiting;

Rare: dry mouth, stomach discomfort, liver function disorders/liver diseases’ (*according to the results of post-marketing observations, in most cases, liver function disorders/ liver diseases were detected in patients in Japan).

Allergic reactions:

Infrequently: skin pruritus, rash, hyperhidrosis;

Rare: hypersensitivity (erythema, angioedema), eczema, angioedema (fatal), drug rash, toxic rash;

Frequency unknown: anaphylactic reactions, urticaria.

From the musculoskeletal system:

Infrequently: myalgia, back pain, muscle spasms (calf muscle spasms); Rarely: arthralgia, lower limb pain;

Frequency unknown: tendon pain (symptoms similar to tendinitis).

From the side of the kidneys and urinary tract:

Infrequently:  impaired renal function, including acute renal

failure.

Common:

Infrequently: chest pain, general weakness;

Rare: flu-like syndrome.

Laboratory parameters:

Infrequently: hyperkalemia, increased blood creatinine concentration; Rarely: increased blood uric acid concentration, increased activity of “liver” enzymes, increased activity of creatine phosphokinase (CPK), decreased hemoglobin, hypoglycemia (in patients with diabetes mellitus);

In the post-marketing period of telmisatran use, the following cases were noted::

Very rare: interstitial lung disease (no causal relationship established).

Interaction

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

Concomitant use with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin and amlodipine does not lead to 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.

When telmisartan and ramipril were coadministered, an increase in AUC0 24 and Ct1 was observed)! ramipril and ramiprilate increased by 2.5 times. The clinical significance of this phenomenon has not been established.

With simultaneous use of angiotensin converting enzyme (ACE) inhibitors and lithium preparations, a reversible increase in the concentration of lithium in the blood was observed, accompanied by a toxic effect. In rare cases, such changes have been reported with the appointment of angiotensin II receptor antagonists. With simultaneous use 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 as an anti-inflammatory agent (more than 3 g/day), cyclooxygenase-2 (COX-2) inhibitors, and non-selective NSAIDs, may 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, BCC should be compensated and renal function monitored at the beginning of treatment.

A reduction in the effect of antihypertensive agents, such as telmisartan, by inhibiting the vasodilating effect of prostaglandins was observed when co-treated with NSAIDs. Concomitant use with aliskiren is contraindicated in patients with diabetes mellitus or moderate to severe renal insufficiency (GFR

The use of ACE inhibitors and ARA II inhibitors in patients with diabetic nephropathy is contraindicated.

When used concomitantly with ACE inhibitors, potassium-sparing diuretics (spironolactone, eplerenone, triamterene or amiloride), immunosuppressants (cyclosporine or tacrolimus), trimethoprim and other drugs that can increase the content of potassium in the blood serum, as well as potassium-containing dietary supplements, especially in patients with renal insufficiency, the risk of hyperkalemia increases. Regular monitoring of the potassium content in the blood serum is necessary. Joint use is not recommended.

How to take, course of use and dosage

Inside, regardless of the meal time.

Arterial hypertension

The initial recommended dose of Telmisartan-SZ is 1 tablet (40 mg) once a day. In cases where the therapeutic effect is not achieved, the maximum recommended dose of Telmisartan-SZ 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 Telmisartan-SZ 80 mg, once a day. In the initial period of treatment, additional blood pressure correction may be required.

Impaired renal function

In patients with renal insufficiency, including patients undergoing hemodialysis, no dosage adjustment is required. In patients with severe renal insufficiency and undergoing hemodialysis, limited experience with the drug is recommended to start therapy with an initial dose of 20 mg (1/2 tablet of 40 mg). Impaired liver function

In patients with mild to moderate hepatic impairment (Child-Pugh class A and B, respectively), the daily dose of Telmisartan-SZ should not exceed 40 mg Elderly patients

The dosage regimen does not require any changes.

Overdose

No cases of overdose have been identified.

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

Treatment: symptomatic therapy, hemodialysis is ineffective.

Description

Tablets are white or almost white in color, round, flat-cylindrical with a chamfer and risk.

Special instructions

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

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 diseases, including bilateral 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 RAAS, when using Telmisartan-SZ together with potassium-sparing diuretics, potassium-containing supplements, potassium-containing food salt, and other drugs that increase the content 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 coronary heart disease (CHD), the use of drugs that reduce blood pressure, such as angiotensin II receptor antagonists (ARA II) 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. In patients with diabetes mellitus, appropriate diagnostic tests, including a physical activity test, should be performed before starting the use of Telmisartan-SZ to detect and treat CHD.

Alternatively, Telmisartan-SZ can be used in combination with thiazide diuretics, such as hydrochlorothiazide, which additionally have an antihypertensive effect.

In patients with primary aldosteronism, antihypertensive drugs, whose mechanism of action consists in inhibiting the renin-angiotensin-aldosterone system, are usually ineffective. Caution should be exercised when using Telmisartan-SZ (as well as other vasodilators) in patients with aortic and mitral stenosis, or with 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 arterial hypertension, the dose of telmisartan 160 mg / day and in combination with hydrochlorothiazide 12.5-25 mg was well tolerated and effective.

Hepatic dysfunction in the use of telmisartan in most cases was observed in residents of Japan.

Patients with reduced BCC and/or sodium levels due to previous diuretic therapy, restriction of salt intake, diarrhea or vomiting may experience symptomatic hypotension, especially after the first use of Telmisartan-SZ. Such conditions should be eliminated before taking it.Fluid and/or sodium deficiencies should be corrected before starting Telmisartan-SZ.

Telmisartan-SZ is less effective in black patients.

Storage conditions

Keep out of the reach of children in a dark place, at a temperature not exceeding 25 °C.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Telmisartan

Conditions of release from pharmacies

By prescription

Dosage form

Tablets