Telmisartan-SZ - instructions for use, doses, side effects, contraindications

Excipients: sodium hydroxide - 3.4 mg; povidone-K30 (medium-molecular weight polyvinylpyrrolidone) - 12.0 mg; meglumine - 12,0 mg; mannitol - 165.2 mg; magnesium stearate - 2.4 mg; talc - 5.0 mg.

dosage: 80 mg

active substance: telmisartan - 80 mg

Excipients: sodium hydroxide - 6.8 mg; povidone-K30 (medium-molecular weight polyvinylpyrrolidone) - 24.0 mg; meglumine - 24,0 mg; Mannitol - 330.4 mg; magnesium stearate - 4.8 mg; talc - 10.0 mg.

Description:

Tablets are white or almost white, round, flat-cylindrical, with a facet and a risk.

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. It displaces angiotensin II from the bond to the receptor, not having the action of an agonist for this receptor.

Telmisartan binds only to the subtype AT₁ receptors of angiotensin II. Communication is of a lasting nature. Has no affinity for other receptors, including AT₂ receptor 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 antihypertensive action is noted within 3 hours after the first administration of telmisartan. The drug remains for 24 hours and remains significant up to 48 hours. The pronounced antihypertensive effect usually develops 4-8 weeks after regular ingestion.

In patients with 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_mOh(maximum concentration) and AUC were approximately 3 and 2 times, respectively, higher in women than in men without significant effect on efficacy.

Communication with plasma proteins is 99.5%, mainly with albumin and alpha-1 glycoprotein. The average value of the apparent volume of distribution in the equilibrium concentration is 500 liters. Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive. Half-life is more than 20 hours. Output through the intestine in an unchanged form, excretion by the kidneys - less than 2% of the dose. The total plasma clearance is 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 with 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 taking 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_mOh.

Indications:

- Arterial hypertension.

- reduction in 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 auxiliary components of the drug;

- pregnancy;

- the period of breastfeeding;

- obstructive diseases of the biliary tract;

- severe violations of liver function (class C on the Child-Pugh scale);

- simultaneous application of the preparation Telmisartan-SZ with aliskiren in patients with diabetes mellitus or renal insufficiency (glomerular filtration rate (GFR) <60 ml / min / 1.73 ml / min / m² surface area of the body);

- age to 18 years (efficacy and safety not established).

Carefully:

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

- impaired liver and / or kidney function (see section "Special instructions");

- decrease in circulating blood volume (BCC) due to previous diuretic therapy, restriction of salt intake, diarrhea or vomiting;

- hyponatremia;

- hyperkalemia;

- condition after kidney transplantation (no experience of application);

- chronic heart failure;

- stenosis of the aortic and mitral valve;

- hypertrophic obstructive cardiomyopathy;

- primary aldosteronism (efficacy and safety not established);

- hemodialysis.

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, 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 fetotoxicity in a person (decreased kidney function, oligohydroamnion, slowing ossification of the skull), and neonatal toxicity (kidney failure, arterial hypotension, hyperkalemia). Patients planning a pregnancy should be prescribed alternative therapy. If treatment with angiotensin II receptor antagonists occurred during the second trimester of pregnancy, an ultrasound evaluation of renal function and skull condition in the fetus is recommended.

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

Therapy with Telmisartan-SZ is contraindicated in the period of breastfeeding.

Investigation of the impact on fertility not conducted.

Dosing and Administration:

Inside, regardless of the time of ingestion.

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 the preparation Telmisartan-SZ 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.

In patients with severe renal failure and on hemodialysis, the experience of using the drug is limited, it 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 or moderate impairment of liver function (class A and B on the Child-Pugh scale, respectively), the daily dose of Telmisartan-SZ should not exceed 40 mg.

Elderly patients

Dosing regimen does not require any changes.

Side effects:

The observed side effects were not correlated with the sex, age or race of the patients.

Classification of the frequency of development of side effects of the World Health Organization (WHO): very often ≥1 / 10, often from ≥1 / 100 to <1/10, infrequently from ≥1 / 1000 to <1/100, rarely from ≥1 / 10000 to <1/1000, very rarely <1/10000, the frequency is unknown - can not be estimated from the available data.

Infections:

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

The frequency is unknown: sepsis, including sepsis with fatal outcome.

From the hematopoietic and lymphatic system:

Infrequently: anemia;

Rarely: thrombocytopenia;

Frequency unknown: eosinophilia.

From the central nervous system:

Infrequently: insomnia, drowsiness, depression, vertigo;

Rarely: faint, anxiety.

From the side of the organ of vision:

Rarely: visual disorders.

From the cardiovascular system:

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

Rarely: tachycardia.

From the respiratory system:

Infrequent: shortness of breath, cough.

From the digestive system:

Infrequent: abdominal pain, diarrhea, indigestion, flatulence, vomiting;

Rarely: dry mouth, discomfort in the stomach, liver dysfunction / liver disease *.

(* Based on the results of post-marketing observations, in most cases, violations of liver function / liver disease have been identified in patients in Japan).

Allergic reactions:

Infrequent: itchy skin, rash, hyperhidrosis;

Rarely: hypersensitivity (erythema, angioedema), eczema, angioedema (with fatal outcome), drug rash, toxic rash;

The frequency is unknown: anaphylactic reactions, urticaria.

From the musculoskeletal system:

Infrequently: myalgia, back pain, muscle spasms (calf muscle cramps);

Rarely: arthralgia, pain in the lower limbs;

The frequency is unknown: pain in the tendons (symptoms similar to the manifestation of tendinitis).

From the side of the kidneys and urinary tract:

Infrequent: impaired renal function, including acute renal failure.

Are common:

Infrequent: chest pain, general weakness;

Rarely: flu-like syndrome.

Laboratory indicators:

Infrequent: hyperkalaemia, increased concentration of creatinine in the blood;

Rarely: increased concentration of uric acid in the blood, increased activity of "hepatic" enzymes, increased activity of creatine phosphokinase (CK), decreased hemoglobin, hypoglycemia (in patients with diabetes mellitus);

In the postmarketing period the use of telmisatran was noted:

Very rarely: interstitial lung disease (cause-effect relationship not established).

Overdose:

Cases of overdose have not been identified.

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

Treatment: symptomatic therapy, hemodialysis is ineffective.

Interaction:

Telmisartan may increase the antihypertensive effect of other hypothetical agents.

Other types of interactions that have clinical relevance have not been identified.

Simultaneous 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 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, there was an increase AUC_0-₂₄ and C_mOh ramipril and ramiprilata 2.5 times. The clinical significance of this phenomenon is not established.

With the 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 were registered with the appointment of angiotensin receptor antagonists II. With the 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 drug (more than 3 g / day), cyclooxygenase-2 (COX-2) inhibitors and nonselective NSAIDs, can cause 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 drugs, such as telmisartan, by inhibiting the vasodilating effect of prostaglandins was noted in the joint treatment with NSAIDs.

Contraindicated simultaneous use with aliskiren in patients with diabetes mellitus or moderate and severe renal failure (GFR <60 ml / min / 1.73 ml / min / m² surface area of the body).

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

With simultaneous use with ACE inhibitors, potassium-sparing diuretics (spironolactone, eplerenone, triamterene or amiloride), immunosuppressors (ciclosporin or tacrolimus), trimethoprim and other drugs that can increase the serum potassium content, as well as potassium-containing food additives, especially in patients with renal insufficiency, increases the risk of hyperkalemia. Regular monitoring of the potassium content in serum is required. Joint use is not recommended.

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 accompanied by a similar double blockade of RAAS (eg, with the addition of ACE inhibitors or direct inhibitor of renin-aliskiren to APA II), should be carried out strictly individually and with careful monitoring of kidney function (including periodic monitoring of potassium and creatinine in the blood serum).

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, when combined with Telmisartan-SZ and potassium-sparing diuretics, potassium supplements,potassium-containing dietary 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 (APA II) or ACE inhibitors, may 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 preparation Telmisartan-SZ for the identification and treatment of IHD, appropriate diagnostic tests should be carried out, including a physical exercise test.

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,the mechanism of action of which consists in inhibiting the renin-angiotensin-aldosterone system, as a rule, ineffective.

Care should be taken when using Telmisartan-SZ (as well as other vasodilators) in patients with aortic and 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.

In patients with reduced BCC and / or sodium content due to previous diuretic therapy, restriction of salt intake, diarrhea or vomiting, symptomatic arterial hypotension may occur, especially after the first administration of Telmisartan-SZ. Such conditions must be eliminated before it is received.The deficiency of fluid and / or sodium should be eliminated before the start of taking Telmisartan-SZ.

Telmisartan-SZ 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 preparation Telmisartan-SZ on the ability to drive vehicles and mechanisms were not carried out. However, when driving vehicles and working with machinery, one should take into account the possibility of developing dizziness and drowsiness, which requires caution.

Form release / dosage:

Tablets, 40 mg and 80 mg.

Packaging:

For 10 or 14 tablets in a contour mesh package.

For 30 tablets in a can of polymeric low-density polyethylene with a lid of high-density polyethylene or a bottle of polymer from low-density polyethylene with a lid of high-density polyethylene.

Each jar or bottle, 3, 6 contour packs of 10 tablets or 1, 2 contour packs of 14 tablets together with the instructions for use are placed in a cardboard box.

Storage conditions:

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-003650

Date of registration:26.05.2016

Expiration Date:26.05.2021

The owner of the registration certificate:NORTH STAR, CJSC NORTH STAR, CJSC Russia

Manufacturer: & nbsp

NORTH STAR, CJSC Russia

Representation: & nbspNORTH STAR CJSC NORTH STAR CJSC Russia

Information update date: & nbsp23.07.2016

Illustrated instructions

Instructions

Telmisartan-SZ (Telmesteine-SZ)