Telmisartan INN and trade name. Telmisartan-sz - instructions for use. Pharmacokinetics in special clinical situations

Telmista: instructions for use and reviews

Telmista is an antihypertensive drug.

Release form and composition

Dosage form Telmista - tablets: almost white or white; at a dose of 20 mg - round, 40 mg - biconvex, oval, 80 mg - biconvex, capsule-shaped (in a blister of combined material 7 pcs., in a cardboard box 2, 4, 8, 12 or 14 blisters; in a blister 10 pcs., in a cardboard box 3, 6 or 9 blisters).

Composition of one tablet:

active substance: telmisartan – 20, 40 or 80 mg;
excipients: sodium hydroxide, lactose monohydrate, magnesium stearate, meglumine, povidone K30, sorbitol (E420).

Pharmacological properties

Pharmacodynamics

Telmisartan, the active substance of Telmista, has antihypertensive properties, being an angiotensin II receptor antagonist (AT 1 receptor blocker). By displacing angiotensin II from its connection with the receptor, it does not have an agonist effect on this receptor. Telmisartan can selectively and for a long time bind only to angiotensin II receptors of the AT 1 subtype. It has no affinity for other angiotensin receptors, the functional significance of which and the result of the excessive (due to the use of telmisartan) influence of angiotensin II on them have not been studied.

Telmisartan reduces the content of aldosterone in the blood plasma, does not affect the concentration of renin and does not block ion channels. The active substance does not suppress ACE (angiotensin-converting enzyme), which also destroys bradykinin, so there are no adverse reactions caused by bradykinin.

Telmisartan, taken at a dose of 80 mg, completely blocks the hypertensive effect of angiotensin II. After the first dose of the drug, the onset of the hypotensive effect is noted within 3 hours, the effect persists for 24 hours and remains significant for up to two days. A stable hypotensive effect usually develops 4–8 weeks from the start of treatment with regular use of telmisartan.

For arterial hypertension, the drug helps reduce systolic and diastolic blood pressure (BP). Telmisartan has no effect on heart rate (heart rate).

In patients who abruptly discontinue telmisartan, blood pressure gradually returns to its original value; no withdrawal syndrome is observed.

Pharmacokinetics

absorption: when taken orally, it is quickly absorbed from the gastrointestinal tract. Bioavailability is 50%. When taken concomitantly with food, the reduction in AUC (area under the pharmacokinetic curve) ranges from 6% to 19% at a dose of 40 and 160 mg, respectively. 3 hours after taking telmisartan, its concentration in the blood plasma levels off (does not depend on the time of food intake). AUC and maximum concentration of the substance in blood plasma (Cmax) in women are approximately 2 and 3 times higher, respectively, than in men. No significant effect on efficiency was noted;
distribution and metabolism: 99.5% of the substance is bound to plasma proteins (mainly alpha-1 glycoprotein and albumin). The apparent volume of distribution at equilibrium concentration is on average 500 l. Metabolism occurs by conjugation with glucuronic acid to form pharmacologically inactive metabolites;
excretion: T 1/2 (half-life) – more than 20 hours. The substance is predominantly excreted unchanged through the intestines, with urine - less than 2%. The total plasma clearance is quite high compared to the hepatic blood flow (approximately 1500 ml/min) and is about 900 ml/min.

The main pharmacokinetic parameters of telmisartan when used in children and adolescents aged 6 to 18 years for 4 weeks at a dose of 1 or 2 mg/kg are generally comparable to those in adult patients and confirm the nonlinearity of the pharmacokinetics of the active substance, especially in relation to C max.

Indications for use

arterial hypertension;
high risk of cardiovascular diseases in patients over 55 years of age - to reduce cardiovascular morbidity and mortality.

Contraindications

Absolute:

severe forms of liver dysfunction (according to the Child-Pugh classification - class C);
obstruction of the biliary tract;
combined use with aliskiren in patients with severe or moderate renal failure (glomerular filtration rate less than 60 ml/min/1.73 m2) or with diabetes mellitus;
lactase/sucrase/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption;
pregnancy and lactation period;
age under 18 years;
individual hypersensitivity to telmisartan or any of the auxiliary components of the drug.

Relative (diseases/conditions in which the use of Telmista requires caution):

impaired renal and/or liver function;
bilateral renal artery stenosis or stenosis of the artery of a single kidney;
conditions after kidney transplantation (due to lack of experience in use);
hyperkalemia;
hyponatremia;
chronic heart failure;
narrowing of the mitral and/or aortic valve;
HOCM (hypertrophic obstructive cardiomyopathy);
a decrease in BCC (circulating blood volume) due to previous treatment with diuretics, limited intake of table salt, vomiting or diarrhea;
primary hyperaldosteronism (safety and effectiveness have not been established).

Instructions for use Telmista: method and dosage

Telmista tablets are taken orally regardless of meal time.

For arterial hypertension, it is recommended to start taking 20 or 40 mg of the drug once a day. In some patients, it is possible to achieve a hypotensive effect at a dose of 20 mg/day. In case of insufficient therapeutic effect, the dose can be increased to the maximum daily dose of 80 mg. When increasing the dose, it must be taken into account that the maximum hypotensive effect of Telmista is usually achieved 4–8 weeks from the start of therapy.

To reduce cardiovascular morbidity and mortality, it is recommended to take 80 mg of the drug once a day.

At the initial stage of treatment, additional methods of normalizing blood pressure may be required.

No dosage adjustment is required for patients with renal failure, including those on hemodialysis.

For liver dysfunction of mild or moderate severity (according to the Child-Pugh classification - class A and B), the maximum daily dose of Telmista is 40 mg.

In elderly patients, the pharmacokinetics of telmisartan does not change, so there is no need to adjust the dose of the drug for them.

Side effects

When using Telmista, the following adverse reactions from systems and organs are possible:

heart: tachycardia, bradycardia;
blood vessels: orthostatic hypotension, significant decrease in blood pressure;
digestive system: diarrhea, abdominal pain, dyspepsia, stomach discomfort, flatulence, vomiting, dysgeusia (taste distortion), dry oral mucosa, liver dysfunction/liver disease;
blood and lymphatic system: thrombocytopenia, eosinophilia, anemia, sepsis (including fatal sepsis);
nervous system: insomnia, anxiety, depression, vertigo, fainting;
immune system: hypersensitivity (urticaria, erythema, angioedema), anaphylactic reactions, itching, eczema, skin rash (including drug rash), hyperhidrosis, angioedema (even death), toxic skin rash;
organ of vision: visual disorders;
respiratory system, chest organs and mediastinum: cough, shortness of breath, upper respiratory tract infections, interstitial lung diseases (a cause-and-effect relationship with the use of telmisartan has not been established);
musculoskeletal and connective tissue: back pain, arthralgia, muscle spasms (calf muscle cramps), myalgia, leg pain, tendon pain (symptoms similar to manifestations of inflammation and degeneration of tendon tissue);
kidneys and urinary tract: renal dysfunction (including acute renal failure), urinary tract infections (including cystitis);
body as a whole: general weakness, flu-like syndrome, chest pain;
instrumental and laboratory tests: increased levels of uric acid, creatinine in the blood plasma, decreased hemoglobin levels, increased activity of liver transaminases, CPK (creatine phosphokinase) in the blood plasma, hypoglycemia (in patients with diabetes), hyperkalemia.

The relationship between the severity of side effects and the age, gender or race of patients has not been established.

Overdose

In case of an overdose of Telmista, the following symptoms may appear: tachycardia, bradycardia, significant decrease in blood pressure.

Special instructions

The simultaneous use of Telmista and ACE inhibitors or a direct renin inhibitor, aliskiren, due to its dual effect on the RAAS (renin-angiotensin-aldosterone system), worsens renal function (including can lead to acute renal failure), and also increases the risk of developing arterial hypotension and hyperkalemia . If such concomitant therapy is absolutely necessary, it should be carried out under close medical supervision, and renal function, blood pressure levels and plasma electrolytes should be regularly checked.

In patients with diabetic nephropathy, it is not recommended to use telmisartan and ACE inhibitors simultaneously.

In cases where vascular tone and renal function depend primarily on the activity of the RAAS (for example, in patients with kidney disease, including bilateral renal artery stenosis or stenosis of the artery of a solitary kidney, or with chronic heart failure), the use of drugs affecting the RAAS can lead to the development hyperazotemia, acute arterial hypotension, oliguria and acute renal failure (in rare cases).

When using potassium-sparing diuretics, potassium-containing salt substitutes, additives and other agents that increase the concentration of potassium in the blood plasma (for example, heparin) together with Telmista, it is necessary to monitor the level of potassium in the blood.

Since telmisartan is excreted mainly in the bile, in case of obstructive diseases of the biliary tract or impaired liver function, the clearance of the drug may be reduced.

In diabetes mellitus and additional cardiovascular risk, for example, coronary artery disease (CHD), the use of Telmista can cause fatal myocardial infarction and sudden cardiovascular death. In patients with diabetes mellitus, coronary artery disease may not be diagnosed, since its symptoms in this case do not always appear. Therefore, before starting drug therapy, it is necessary to conduct appropriate diagnostic examinations, including an exercise test.

In patients with diabetes mellitus who are treated with insulin or oral hypoglycemic drugs, hypoglycemia may develop during therapy with Telmista. Such patients need to monitor the concentration of glucose in the blood, since depending on this indicator it is necessary to adjust the dose of insulin or hypoglycemic drugs.

In primary hyperaldosteronism, the use of antihypertensive drugs - RAAS inhibitors - is usually not effective. Such patients are not recommended to take Telmista.

The use of the drug is possible in combination with thiazide diuretics, since such a combination provides an additional reduction in blood pressure.

Studies have shown that Telmista is less effective in patients of the Negroid race. Liver dysfunction with the use of telmisartan was observed in most cases in Japanese residents.

Impact on the ability to drive vehicles and complex mechanisms

When driving vehicles and performing all types of activities that require a quick mental, motor reaction and increased attention, it is necessary to take into account the likelihood of drowsiness and dizziness during treatment with the drug and exercise caution.

Use during pregnancy and lactation

According to the instructions, Telmista is contraindicated during pregnancy. If pregnancy is diagnosed, the drug should be stopped immediately. If necessary, antihypertensive drugs of other classes approved for use during pregnancy should be prescribed. Women planning pregnancy are also advised to use alternative therapy.

Preclinical studies of the drug did not reveal any teratogenic effects. But it has been established that the use of angiotensin II receptor antagonists in the second and third trimesters of pregnancy causes fetotoxicity (oligohydramnios, decreased renal function, delayed ossification of fetal skull bones) and neonatal toxicity (arterial hypotension, renal failure, hyperkalemia).

Newborns whose mothers took Telmista during pregnancy require medical supervision due to the possible development of arterial hypotension.

Since there is no information on the penetration of telmisartan into breast milk, the drug is contraindicated during breastfeeding.

Use in childhood

The safety and effectiveness of telmisartan in pediatrics have not been established, therefore Telmista 40 mg, 80 mg and 20 mg tablets are prohibited for use in children and adolescents under 18 years of age.

For impaired renal function

In patients with impaired renal function, the use of the drug requires caution.

In severe or moderate renal failure (glomerular filtration rate less than 60 ml/min/1.73 m2), the co-administration of Telmista and aliskiren is contraindicated.

For liver dysfunction

It is not recommended to take the drug in patients with severe liver dysfunction (Child-Pugh class C).

In case of mild to moderate liver failure (according to the Child-Pugh classification - class A and B), the use of Telmista requires caution. The maximum daily dose of the drug in this case should not exceed 40 mg.

Use in old age

There is no need to adjust the dose of Telmista for elderly patients.

Drug interactions

The use of telmisartan simultaneously with certain drugs can lead to the development of the following effects:

antihypertensive drugs: increased antihypertensive effect;
warfarin, digoxin, ibuprofen, glibenclamide, hydrochlorothiazide, paracetamol, amlodipine and simvastatin: no clinically significant interaction is observed. In some cases, it is possible to increase the digoxin content in the blood plasma by an average of 20%. When used together with digoxin, it is recommended to periodically monitor its plasma concentration;
potassium-sparing diuretics (eg, spironolactone, amiloride, triamterene, eplerenone), potassium substitutes, ACE inhibitors, angiotensin II receptor antagonists, NSAIDs (non-steroidal anti-inflammatory drugs), including selective cyclooxygenase-2 inhibitors, heparin, immunosuppressants (tacrolimus or cyclosporine) and trimethoprim: increased risk of hyperkalemia (due to a synergistic effect);
ramipril: 2.5-fold increase in Cmax and AUC 0-24 of ramipril and ramiprilat;
Lithium preparations: a reversible increase in the concentration of lithium in the blood plasma (has been reported in rare cases) with an accompanying toxic effect. It is recommended to periodically check plasma lithium levels;
NSAIDs (including acetylsalicylic acid, non-selective NSAIDs and cyclooxygenase-2 inhibitors): decreased hypotensive effect of telmisartan, increased risk of acute renal failure due to dehydration. At the beginning of combination therapy with telmisartan and NSAIDs, it is necessary to compensate for volumetric volume and check renal function;
amifostine, baclofen: potentiation of the hypotensive effect of telmisartan;
Barbiturates, alcohol, antidepressants and narcotic drugs: worsening orthostatic hypotension.

Analogs

Analogues of Telmista are: Mikardis, Teseo, Telmisartan-Richter, Telmisartan-SZ, Telpres, Telsartan and others.

Terms and conditions of storage

Store at a temperature not exceeding 25 °C out of the reach of children.

Shelf life – 3 years.

film-coated tablets

Owner/Registrar

NORTH STAR, JSC

International Classification of Diseases (ICD-10)

I10 Essential [primary] hypertension

Pharmacological group

Angiotensin II receptor antagonist

Pharmacological action

Antihypertensive agent, angiotensin II receptor antagonist (AT1 type). It has a very high affinity for this receptor subtype. By selectively and long-term binding to receptors, telmisartan displaces angiotensin II from its connection with AT1 receptors. Does not show affinity for other AT receptor subtypes. The functional significance of other receptor subtypes and the effect of increased (as a result of the administration of telmisartan) levels of angiotensin II on them is not known. Telmisartan reduces the level of aldosterone in the blood plasma, does not inhibit plasma renin, does not block ion channels, and does not inhibit ACE (kinase II), which also destroys bradykinin. Therefore, there are no side effects associated with bradykinin.

Pharmacokinetics

When taken orally, it is quickly absorbed from the gastrointestinal tract. Bioavailability is 50%. When taken simultaneously with food, the reduction in AUC ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). 3 hours after administration, the plasma concentration levels off, regardless of whether it is taken with food or on an empty stomach. Plasma protein binding is 99.5%. The average values of apparent Vd at the equilibrium stage are 500 l. Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive.

T1/2 – more than 20 hours. Excreted through the intestines unchanged. Cumulative renal excretion is less than 1%. Total plasma clearance is 1000 ml/min (renal blood flow is 1500 ml/min).

Arterial hypertension.

Obstruction of the biliary tract, severe dysfunction of the liver and kidneys, pregnancy, lactation (breastfeeding), hypersensitivity to telmisartan.

From the side of the central nervous system: headache, dizziness, fatigue, insomnia, anxiety, depression, convulsions.

From the digestive system: abdominal pain, dyspepsia, nausea, diarrhea, increased activity of liver transaminases.

From the respiratory system: cough, pharyngitis, upper respiratory tract infections.

From the hematopoietic system: decrease in hemoglobin level.

Allergic reactions: rash; in a single case - angioedema.

From the urinary system: peripheral edema, urinary tract infections, increased uric acid levels, hypercreatininemia.

From the cardiovascular system: marked decrease in blood pressure, palpitations, chest pain.

From the musculoskeletal system: lower back pain, myalgia, arthralgia.

From the laboratory parameters: hyperkalemia, anemia, hyperuricemia.

Others: flu-like syndrome.

Special instructions

Telmisartan is used with caution in cases of liver dysfunction, gastric and duodenal ulcers in the acute stage, other gastrointestinal diseases, aortic and mitral valve stenosis, obstructive hypertrophic cardiomyopathy, coronary artery disease, and heart failure.

In patients with bilateral renal artery stenosis or renal artery stenosis of a single functioning kidney, the use of telmisartan increases the risk of severe arterial hypotension and renal failure. Therefore, telmisartan should be used with caution in this category of patients.

During the period of use of telmisartan in patients with impaired renal function, it is necessary to monitor the content of potassium and creatinine in the blood plasma.

There are currently no data on the use of telmisartan in patients with recent kidney transplantation.

In patients with reduced blood volume and/or hyponatremia, symptomatic arterial hypotension may occur, especially after taking the first dose of telmisartan. Therefore, before carrying out therapy, correction of such conditions is necessary.

The use of telmisartan is possible in combination with thiazide diuretics, because This combination provides an additional reduction in blood pressure.

When considering the possibility of increasing the dose of telmisartan, it should be remembered that the maximum hypotensive effect is usually achieved 4-8 weeks after the start of treatment.

Use in pediatrics

There are no data on the safety and effectiveness of telmisartan in children and adolescents.

Impact on the ability to drive vehicles and operate machinery

The question of the possibility of engaging in potentially hazardous activities that require increased attention and rapid psychomotor reactions should be decided only after assessing the individual response to telmisartan.

For renal failure

Contraindicated in severe renal impairment.

In case of liver dysfunction

Contraindicated in severe liver dysfunction.

Elderly

Elderly patients do not require dose adjustment.

Use during pregnancy and breastfeeding

Telmisartan is contraindicated for use during pregnancy and lactation (breastfeeding).

Drug interactions

When used simultaneously with antihypertensive drugs, the antihypertensive effect may be enhanced.

When used simultaneously with potassium-sparing diuretics, heparin, dietary supplements, salt substitutes containing potassium, hyperkalemia may develop.

When used simultaneously with lithium preparations, an increase in the concentration of lithium in the blood plasma is possible.

With simultaneous use, it is possible to increase the concentration of digoxin in the blood plasma.

For adults, the daily dose is 20-40 mg (1 time/day). In some patients, a hypotensive effect can be achieved with a dose of 20 mg/day. If necessary, the dose can be increased to 80 mg/day.

Patients with impaired renal function, as well as elderly patients, do not require dose adjustment.

For patients with impaired liver function, the daily dose is 40 mg.

Gross formula

C 33 H 30 N 4 O 2

Pharmacological group of the substance Telmisartan

Nosological classification (ICD-10)

CAS Code

144701-48-4

Characteristics of the substance Telmisartan

White or colorless crystalline powder, odorless, practically insoluble in water and at pH from 3 to 9, partially soluble in strong acids (except hydrochloric acid), soluble in strong alkalis.

Pharmacology

Pharmacological action- antihypertensive.

Blocks angiotensin II receptors (AT subtype 1). Dose-dependently inhibits the pressor effect of angiotensin II, lowers plasma aldosterone levels, increases diuresis, sodium and chloride excretion. Has a nephroprotective effect, reduces the level of albuminuria. Reduces renal blood flow by 10% without impairing glomerular filtration. In high doses, it reduces the severity of myocardial hypertrophy. In patients with arterial hypertension, it lowers both SBP and DBP without changing heart rate.

Well absorbed from the gastrointestinal tract. Absolute bioavailability is 40-60% (due to the “first pass” effect through the liver). After taking a single dose of 80 mg, Cmax is achieved within 1 hour. Intensively binds to plasma proteins, mainly albumin and acidic alpha 1-glycoprotein. Relatively evenly distributed in the body (highly lipophilic and easily penetrates tissues), the volume of distribution is 500 liters. Metabolized in the liver by conjugation with glucuronic acid, forming a stable inactive acyl glucuronide, which is rapidly excreted in bile: about 85% of unchanged telmisartan and 11% of glucuronide are found in feces; renal excretion does not exceed 2%. It is excreted slowly, T1/2 is about 21 hours in men and 31 hours in women. Hypotension develops 3 hours after oral administration, persists for more than 24 hours and stabilizes during a 4-8 week course of use. When you stop taking blood pressure, it gradually (over several days) returns to its original values without the development of “rebound” hypertension.

Use of the substance Telmisartan

Arterial hypertension.

Contraindications

Hypersensitivity, biliary tract obstruction, severe liver and kidney dysfunction, pregnancy, breastfeeding.

Restrictions on use

Children and adolescents (safety and effectiveness of use in children and adolescents have not been determined).

Use during pregnancy and breastfeeding

Contraindicated during pregnancy. Before a planned pregnancy, it is recommended to replace the drug with another antihypertensive drug in advance.

Breastfeeding should be stopped during treatment.

Side effects of Telmisartan

From the nervous system and sensory organs:≥ 1% - headache, dizziness.

From the gastrointestinal tract:≥ 1% - nausea, dyspepsia, abdominal pain, diarrhea.

From the respiratory system:≥ 1% - cough, pharyngitis, flu-like symptoms, decreased tolerance to upper respiratory tract infections.

Others:≥ 1% - chest and lower back pain, myalgia, urinary tract infections, decreased hemoglobin, increased uric acid levels.

Interaction

Hydrochlorothiazide enhances the (mutually) hypotensive effect. With the simultaneous administration of ACE inhibitors, potassium-sparing diuretics and other drugs that can increase plasma potassium levels, as well as potassium-containing nutritional supplements, especially in patients with renal failure, the risk of developing hyperkalemia increases. Increases the concentration of lithium and digoxin in the blood.

Overdose

Symptoms: hypotension.

Treatment: symptomatic and supportive therapy. Hemodialysis is ineffective.

Routes of administration

Inside.

Precautions for the substance Telmisartan

Prescribe with caution to patients with symptomatic renovascular hypertension caused by bilateral renal artery stenosis or renal artery stenosis of a single functioning kidney (the risk of severe hypotension and renal failure increases). In patients with moderate renal impairment, regular monitoring of plasma creatinine and electrolyte (potassium) levels is necessary. Caution should be exercised when prescribing to patients with low blood volume and/or sodium deficiency (during treatment with diuretics, limited salt intake, diarrhea, vomiting), aortic and mitral valve stenosis, obstructive hypertrophic cardiomyopathy, moderate liver dysfunction, severe heart failure (requires constant monitoring the level of potassium and creatinine in the blood serum), with ischemic heart disease (the development of acute coronary syndrome and myocardial infarction is possible), gastric or duodenal ulcers in the acute stage or other diseases of the gastrointestinal tract (gastrointestinal bleeding is likely to occur). It is not recommended for use in cases of primary aldosteronism, congenital fructose intolerance (1 tablet of 80 mg contains 338 mg of sorbitol). Drivers of vehicles and people whose profession involves increased concentration of attention should be careful. When taking digoxin or lithium drugs simultaneously, monitoring their content in the blood serum is necessary.

Interactions with other active ingredients

Trade names

Name	The value of the Vyshkowski Index ®
	0.0329

Telmisartan

Composition and release form of the drug

Pills white or white with a yellowish tint, round, flat-cylindrical, with a chamfer and a notch.

Excipients: lactose monohydrate (milk sugar) - 474.9 mg, croscarmellose sodium - 24 mg, K25 - 24 mg, meglumine - 24 mg, sodium hydroxide - 6.7 mg, magnesium stearate - 6.4 mg.

5 pcs. - contour cellular packaging (1) - cardboard packs.
5 pcs. - contour cellular packaging (2) - cardboard packs.
5 pcs. - contour cellular packaging (3) - cardboard packs.
5 pcs. - contour cellular packaging (4) - cardboard packs.
5 pcs. - contour cellular packaging (5) - cardboard packs.
5 pcs. - contour cellular packaging (8) - cardboard packs.
5 pcs. - contour cellular packaging (10) - cardboard packs.
7 pcs. - contour cellular packaging (1) - cardboard packs.
7 pcs. - contour cellular packaging (2) - cardboard packs.
7 pcs. - contour cellular packaging (3) - cardboard packs.
7 pcs. - contour cellular packaging (4) - cardboard packs.
7 pcs. - contour cellular packaging (5) - cardboard packs.
7 pcs. - contour cellular packaging (8) - cardboard packs.
7 pcs. - contour cellular packaging (10) - cardboard packs.
10 pcs. - contour cellular packaging (1) - cardboard packs.
10 pcs. - contour cellular packaging (2) - cardboard packs.
10 pcs. - contour cellular packaging (3) - cardboard packs.
10 pcs. - contour cellular packaging (4) - cardboard packs.
10 pcs. - contour cellular packaging (5) - cardboard packs.
10 pcs. - contour cellular packaging (8) - cardboard packs.
10 pcs. - contour cellular packaging (10) - cardboard packs.
20 pcs. - contour cellular packaging (1) - cardboard packs.
20 pcs. - contour cellular packaging (2) - cardboard packs.
20 pcs. - contour cellular packaging (3) - cardboard packs.
20 pcs. - contour cellular packaging (4) - cardboard packs.
20 pcs. - contour cellular packaging (5) - cardboard packs.
20 pcs. - contour cellular packaging (8) - cardboard packs.
20 pcs. - contour cellular packaging (10) - cardboard packs.
10 pcs. - cans made of polyethylene terephthalate (1) - cardboard packs.
20 pcs. - cans made of polyethylene terephthalate (1) - cardboard packs.
28 pcs. - cans made of polyethylene terephthalate (1) - cardboard packs.
30 pcs. - cans made of polyethylene terephthalate (1) - cardboard packs.
40 pcs. - cans made of polyethylene terephthalate (1) - cardboard packs.
50 pcs. - cans made of polyethylene terephthalate (1) - cardboard packs.
100 pcs. - cans made of polyethylene terephthalate (1) - cardboard packs.

Pharmacological action

Antihypertensive agent, angiotensin II receptor antagonist (AT1 type). It has a very high affinity for this receptor subtype. By selectively and long-term binding to receptors, telmisartan displaces angiotensin II from its connection with AT1 receptors. Does not show affinity for other AT receptor subtypes. The functional significance of other receptor subtypes and the effect of increased (as a result of the administration of telmisartan) levels of angiotensin II on them is not known. Telmisartan reduces the level of aldosterone in the blood, does not inhibit plasma renin, does not block ion channels, and does not inhibit ACE (kinase II), which also destroys bradykinin. Therefore, there are no side effects associated with bradykinin.

Pharmacokinetics

T1/2 – more than 20 hours. Excreted through the intestines unchanged. Cumulative renal excretion is less than 1%. Total plasma clearance is 1000 ml/min (renal blood flow is 1500 ml/min).

Indications

Contraindications

Obstruction of the biliary tract, severe dysfunction of the liver and kidneys, pregnancy, lactation (breastfeeding), hypersensitivity to telmisartan.

Dosage

For adults, the daily dose is 20-40 mg (1 time/day). In some patients, a hypotensive effect can be achieved with a dose of 20 mg/day. If necessary, the dose can be increased to 80 mg/day.

Patients with impaired renal function, as well as elderly patients, do not require dose adjustment.

For patients with impaired liver function, the daily dose is 40 mg.

Side effects

From the side of the central nervous system: headache, dizziness, fatigue, insomnia, anxiety, depression, convulsions.

From the digestive system:, dyspepsia, nausea, diarrhea, increased activity of liver transaminases.

From the respiratory system: cough, pharyngitis, upper respiratory tract infections.

From the hematopoietic system: decrease in hemoglobin level.

Allergic reactions: rash; in a single case - angioedema.

From the urinary system: peripheral edema, urinary tract infections, increased uric acid levels, hypercreatininemia.

From the cardiovascular system: marked decrease in blood pressure, palpitations, chest pain.

From the musculoskeletal system: lower back pain, myalgia, arthralgia.

From the laboratory parameters: hyperkalemia, anemia, hyperuricemia.

Others: flu-like syndrome.

Drug interactions

When used simultaneously, the antihypertensive effect may be enhanced.

When used simultaneously with potassium-sparing diuretics, heparin, dietary supplements, salt substitutes containing potassium, hyperkalemia may develop.

When used simultaneously with lithium preparations, an increase in the concentration of lithium in the blood plasma is possible.

With simultaneous use, it is possible to increase the concentration of digoxin in the blood plasma.

Special instructions

In patients with bilateral renal artery stenosis or renal artery stenosis of a single functioning kidney, the use of telmisartan increases the risk of severe arterial hypotension and. Therefore, telmisartan should be used with caution in this category of patients.

During the period of use of telmisartan in patients with impaired renal function, it is necessary to monitor the content of potassium and creatinine in the blood plasma.

There are currently no data on the use of telmisartan in patients with recent kidney transplantation.

The use of telmisartan is possible in combination with thiazide diuretics, because This combination provides an additional reduction in blood pressure.

When considering the possibility of increasing the dose of telmisartan, it should be remembered that the maximum hypotensive effect is usually achieved 4-8 weeks after the start of treatment.

Use in pediatrics

Impact on the ability to drive vehicles and operate machinery