Active substanceTelmisartanTelmisartan
Similar drugsTo uncover
  • Mycardis®
    pills inwards 
  • Theseo®
    pills inwards 
    Zentiva c.s.     Czech Republic
  • Telmisartan
    pills inwards 
    ATOLL, LLC     Russia
  • TELMISARTAN-RICHTER
    pills inwards 
    GEDEON RICHTER, OJSC     Hungary
  • Telmisartan-SZ
    pills inwards 
    NORTH STAR, CJSC     Russia
  • Telmist®
    pills
  • Telpres
    pills inwards 
  • Telsartan®
    pills inwards 
  • Dosage form: & nbsp

    film-coated tablets

    Composition:

    Composition per 1 tablet:

    The dosage of 40 mg

    Active substance: telmisartan 40 mg.

    Excipients: sodium hydroxide 3.35 mg, povidone-K25 12.00 mg,

    meglumine 12.00 mg, lactose monohydrate 217.35 mg, crospovidone 12.00 mg, dye

    iron oxide yellow 0.30 mg, magnesium stearate 3.00 mg.

    Film sheath (opadraj yellow *) 9.00 mg: hypromellose-5cP 5.409 mg, titanium

    dioxide 2.704 mg, macrogol-400 0.541 mg, talc 0.173 mg, an iron oxide dye yellow 0.173 mg.

    Dosage of 80 mg

    Active substance: telmisartan 80 mg.

    Excipients: sodium hydroxide 6.70 mg, POVIDON-K25 24.00 mg,

    meglumine 24.00 mg, lactose monohydrate 434.70 mg, crospovidone 24.00 mg, dye

    iron oxide yellow 0.60 mg, magnesium stearate 6.00 mg.

    Film sheath (opadraj yellow *) 18.00 mg: hypromellose-5cP 10.817 mg,

    titanium dioxide 5,409 mg, macrogol-400 1.082 mg, talc 0.346 mg, iron dye

    oxide yellow 0.346 mg.

    * code 02B82506

    Description:

    The dosage of 40 mg

    The capsule-shaped tablets covered with a film shell of yellow color, with engraving "40" on one side and engraving "T" on the other side.

    Dosage of 80 mg

    The capsule-shaped tablets covered with a film shell of yellow color, with engraving "80" on one side and engraving "T" on the other side.

    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), has a high affinity for the subtype AT1 receptor of angiotensin II, through which the action of angiotensin II is realized. Telmisartan does not show any activity as an agonist AT1 receptor. Telmisartan selectively binds to AT1 receptor. Binding is long-lasting. Telmisartan does not show affinity for other receptors, including the AT2 receptor and other, less studied angiotensin receptors. The functional role of these receptors is unknown,the effect of their possible increased stimulation with angiotensin II, whose level is enhanced by telmisartan, is also unknown. Telmisartan reduces the concentration of aldosterone in the blood plasma, does not reduce the activity of renin in the blood plasma and does not block the ion channels. Telmisartan does not inhibit the angiotensin-converting enzyme (kininase II), which also catalyzes the degradation of bradykinin. This avoids the side effects associated with the action of bradykinin.

    Telmisartan at a dose of 80 mg completely blocks the hypertensive effect of angiotensin I in patients. The effective effect of the drug lasts more than 24 hours and even more after 48 hours.

    After the first reception of telmisartan, the onset of antihypertensive action is observed within three hours. The maximum decrease in blood pressure is usually achieved in 4-8 weeks after the start of treatment and persists with long-term treatment.

    Antihypertensive effect persists for more than 24 hours after taking the drug.

    In patients with hypertension telmisartan reduces both systolic and diastolic blood pressure, without affecting the heart rate.

    In the case of a sharp cancellation of telmisartan, the blood pressure gradually (within a few days) returns to the initial values ​​without the development of the "withdrawal" syndrome.

    In comparative clinical trials, the incidence of "dry" cough was significantly lower in patients who received telmisartan, compared with those who received inhibitors of the angiotensin-converting enzyme.

    The effectiveness of reducing the risk of cardiovascular mortality by telmisartan doses less than 80 mg has not been studied.

    Pharmacokinetics:

    Suction

    After ingestion telmisartan quickly absorbed from the gastrointestinal tract. Bioavailability is about 50%. When taking telmisartan concomitantly with food, a decrease in the area under the concentration-time curve (AUC) for telmisartan varies from 6 % (at a dose of 40 mg) to 19% (with a dose of 160 mg). After 3 hours after taking the drug, telmisartan concentrations in the blood plasma equalize regardless of whether the drug is taken on an empty stomach or with food.

    Linearity / nonlinearity

    It is not assumed that a small decrease AUC can cause a decrease in therapeutic effectiveness. The linear relationship between dose and concentration of the drug in the blood plasma is absent.At doses of more than 40 mg, the maximum concentration in the blood plasma (Stach) and, to a lesser extent, AUC increase disproportionately.

    Distribution

    Telmisartan actively binds to blood plasma proteins (more than 99.5%), mainly with albumin and alpha-1 acid glycoprotein. The average value of the apparent volume of distribution in the equilibrium stage (Vdss) is approximately 500 liters.

    Metabolism

    Telmisartan is metabolized by conjugation of the starting material with glucuronide. The pharmacological activity of the conjugate was not detected.

    Excretion

    Telmisartan is characterized by the pharmacokinetics of biexponential decay with a finite half-life of more than 20 hours. The maximum concentration in the blood plasma (Cmax) and, to a lesser extent, the area under the concentration-time curve (AUC) increase with dose disproportionately. There is no evidence that the accumulation of telmisartan when taken at recommended doses is of clinical significance. Plasma concentrations were higher in women than in men, but there was no corresponding effect on efficacy.

    After the administration of the drug inside (and intravenously), telmisartan "is excreted practically only through the intestine, mostly unchanged.The total number excreted by the kidneys is less than 1 % of the dose. Total plasma clearance (Cltot) high (about 1000 ml / min) compared with hepatic blood flow (about 1500 ml / min).

    Pharmacokinetics in special groups patients '

    Gender differences

    There were differences in the concentration of blood in the blood of the stems and AUC in women compared to men, they were approximately 3 and 2 times higher, respectively.

    Elderly patients

    The pharmacokinetics of telmisartan in elderly patients and patients younger than 65 years does not differ.

    Patients with renal insufficiency

    A dose change in patients with renal insufficiency is not required, including patients on hemodialysis. Telmisartan actively binds to blood plasma proteins in patients with renal insufficiency and is not excreted in dialysis. The half-life in patients with renal insufficiency does not change.

    Patients with hepatic insufficiency

    Pharmacokinetic studies involving patients with liver failure revealed an increase in absolute bioavailability to almost 100%. The half-life in patients with liver failure does not change.

    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 other components of the drug;

    - Pregnancy and lactation;

    - Obstructive diseases of the biliary tract;

    - Children's age (up to 18 years);

    - Lactase deficiency, lactose intolerance, glucose-galactose malabsorption;

    - Heavy violations of liver function (class C on the Child-Pugh scale (10-15 points));

    - Primary aldosteronism.

    Carefully:

    Bilateral renal artery stenosis, renal artery stenosis, kidney and / or liver function, condition after kidney transplantation (no experience), decreased circulating blood volume as a result of previous diuretic therapy, restriction of salt intake, diarrhea or vomiting, hyponatremia, hyperkalemia, chronic heart failure, stenosis of the aortic and / or mitral valve, hypertrophic obstructive cardiomyopathy, ischemic heart disease.

    Pregnancy and lactation:

    Pregnancy

    Adequate data on the use of telmisartan by pregnant women are absent. Pre-clinical studies showed no teratogenic effects of the drug, but fetotoxic effects (decreased renal function, oligohydramnios, delayed ossification of the skull) and neonatal toxicity (renal failure, arterial hypotension, hyperkalemia) were noted.

    The use of the drug Telmisartan-Richter is contraindicated in pregnancy.

    Lactation period

    There is no information as to whether the telmisartan in breast milk. Telmisartan-Richter is preferably replaced with a drug with a better safety profile, especially when feeding newborns or premature babies.

    Dosing and Administration:

    Inside, regardless of the reception of food.

    Arterial hypertension

    The initial dose is usually 40 mg once a day. If the target values ​​of arterial pressure are not achieved, the dose of the drug can be increased to a maximum (80 mg) once a day. Alternatively, Telmisartan-Richter can be used in combination with thiazide diuretics, such as hydrochlorothiazide, which with simultaneous application demonstrated an additive antihypertensive effect. If it is necessary to increase the dose, it should be taken into account that the maximum antihypertensive effect usually develops 4-8 weeks after the start of treatment (see the section "Pharmacodynamics").

    Reduction of cardiovascular morbidity and mortality The recommended dose is 80 mg once a day.

    It is recommended to regularly monitor blood pressure and, if necessary, adjust the dose of drugs that lower blood pressure.

    Specials populations patients

    Renal insufficiency: patients with mild to moderate renal failure are not required to adjust the dose. The experience of using in patients with severe renal insufficiency or patients in need of hemodialysis is limited.

    Liver failure:

    In patients with mild or moderate hepatic impairment, the daily dose of the drug should not exceed 40 mg (see section "Special instructions").

    Elderly patients

    For elderly patients, dose adjustment is not required.

    Children

    Telmisartan-Richter is not recommended for use in children under 18 years of age due to the lack of sufficient data on safety and efficacy.

    Side effects:

    In general, the incidence of adverse events noted for telmisartan (41.4%) is comparable to that for placebo (43.9%). The incidence of adverse events was not dose-related and did not correlate with gender, age, or race.

    Adverse adverse reactions are presented according to the frequency of occurrence: 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), an unknown frequency (based on the available data it is impossible to assess).

    In each frequency group, adverse side reactions are presented in order of decreasing severity.

    Infections and invasions

    Infrequent: upper respiratory tract infection, including pharyngitis and sinusitis, urinary tract infection, including cystitis;

    Unknown frequency: sepsis, including fatal.

    Violations of the blood and lymphatic system ,

    Infrequently: anemia;

    Rarely: thrombocytopenia;

    Unknown frequency: eosinophilia.

    Immune system disorders Rarely: hypersensitivity;

    Unknown frequency: anaphylactic reactions.

    Disorders of nutrition and metabolism Infrequent: hyperkalemia.

    Mental disorders Infrequently: depression, insomnia;

    Rarely: anxiety.

    Violations from hand nervous system Not often: syncope.

    Disturbances on the part of the organ of sight Rarely: impaired vision.

    Hearing and balance disorders Infrequently: vertigo.

    Disorders from the cardiovascular system

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

    Rarely: tachycardia.

    * - Often observed in patients with controlled arterial pressure who received telmisartan to reduce the risk of cardiovascular mortality in addition to standard treatment.

    Violations from hand respiratory system, chest and mediastinal organs Infrequent: shortness of breath.

    Violations from hand digestive system Infrequent: abdominal pain, diarrhea, indigestion, flatulence, vomiting;

    Rarely: indigestion, discomfort, dryness of the oral mucosa. Disorders from the hepatobiliary system Rarely: a violation of liver function / liver disease.

    Violations from the skin and subcutaneous tissue Infrequently: a hyperhidrosis, a skin itch, a rash;

    Rarely: erythema, angioedema (including fatal), drug rash, toxic skin rash, eczema;

    Unknown frequency: hives.

    Disturbances from the musculoskeletal system and connective tissue Infrequently: myalgia, back pain (eg, sciatica), muscle spasms;

    Rarely: arthralgia, pain in the limbs;

    Unknown frequency: pain in the tendon area (tendinitis-like symptoms).

    Disorders from the urinary system

    Infrequent: renal failure, including acute renal failure.

    Systemic disorders

    Infrequent: chest pain, asthenia (weakness);

    Rarely: influenza-like condition.

    Laboratory indicators

    Infrequent: increased concentration of creatinine in the blood;

    Rarely: an increase in the concentration of uric acid in the blood, "liver" enzymes, the activity of creatine phosphokinase in the blood serum; decreased hemoglobin; hypoglycemia (in patients with diabetes mellitus).

    Overdose:

    Information on overdose is limited.

    Symptoms: the most significant - a marked decrease in blood pressure and tachycardia; also bradycardia, dizziness, increased serum creatinine concentration, and acute renal failure may occur.

    Treatment: treatment should be symptomatic and supportive. Suggested measures include: vomiting and / or gastric lavage, taking activated charcoal, replenishment of lack of fluid and salts. The content of electrolytes and creatinine in the blood serum should be constantly monitored. Hemodialysis is not effective.

    Interaction:

    Angiotensin-converting enzyme inhibitors (APFG potassium-sparing diuretics

    With simultaneous administration of <ACE inhibitors, potassium-sparing diuretics (spironolactone, eplerenone, triamterene or amiloride) and other drugs that can increase the potassium content in blood serum, as well as potassium-containing food supplements, 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.

    Lithium preparations

    With simultaneous reception of lithium preparations with ACE inhibitors and angiotensin II receptor antagonists, including telmisartan, a reversible increase in the concentration of lithium in serum was noted. It is recommended that the concentration of lithium in the blood serum be closely monitored. Joint application requires caution.

    Digoxin

    Telmisartan increases the digoxin concentration by an average of 20% (in one case - by 39%); it is necessary to determine the concentration of digoxin when used simultaneously.

    Warfarin

    On the background of taking telmisartan, the concentration of warfarin in the blood plasma is reduced (insignificantly).

    Risperidone

    Strengthens the antihypertensive effect of telmisartan.

    Non-steroidal anti-inflammatory drugs (NSAIDs)

    NSAIDs (for example, acetylsalicylic acid in doses that have an anti-inflammatory effect, 4 cyclooxygenase (COX-2) inhibitors and non-selective non-steroidal anti-inflammatory drugs) can reduce the antihypertensive effect of the Telmisartan-Richter preparation. In patients with impaired renal function (eg, patients with reduced circulating blood volume (BCC) or elderly patients with impairedrenal function), the simultaneous administration of the Telmisartan-Richter preparation and cyclooxygenase inhibiting drugs can cause an even greater deterioration in renal function, including possible acute renal failure, which is usually reversible. Care should be taken with simultaneous admission, especially in elderly patients. It should be monitored kidney function after the initiation of combination therapy and periodically thereafter.

    Diuretics (thiazide or "loop" diuretics)

    Preliminary therapy with high doses of diuretics, such as furosemide (looped diuretic) and hydrochlorothiazide (diuretic thiazide type) may lead to a decrease in the volume of fluid in the body and an increased risk of arterial hypotension at the beginning of therapy with the Telmisartan-Richter preparation.

    Other antihypertensives

    The antihypertensive effect of the Telmisartan-Richter preparation can be enhanced when combined with other antihypertensive agents.

    Based on data on pharmacological properties, it can be assumed that the following drugs can enhance the antihypertensive effect of all antihypertensive agents, including telmisartan: baclofen, amifosten.

    Ethanol, barbiturates, narcotics or antidepressants can enhance orthostatic hypotension.

    Corticosteroids (systemic action)

    Reduction of antihypertensive action of telmisartan.

    Special instructions:

    Before and during the treatment with Telmisartan-Richter, blood pressure control, renal function, potassium content in blood serum should be monitored. Transient arterial hypotension is not a contraindication for further treatment with Telmisartan-Richter after stabilization of arterial pressure. In the case of repeated occurrence of severe arterial hypotension, the dose should be reduced or the drug should be withdrawn. In the presence of renal failure, treatment is carried out with caution under the control of serum creatinine concentration.

    Liver failure

    Telmisartan-Richter should not be used in patients with cholestasis, obstruction of the biliary tract or acute liver failure (see "Contraindications"), since telmisartan, mainly, is excreted with bile. It is assumed that these patients reduced the hepatic clearance of telmisartan.Telmisartan-Richter should be used with extreme caution in patients with mild or moderate hepatic impairment.

    Renovascular hypertension

    In the treatment of drugs acting on the renin-angiotensin-aldosterone system (RAAS), in patients with bilateral renal artery stenosis and stenosis of the artery of a single kidney, the risk of severe arterial hypotension and renal failure increases.

    Renal failure and kidney transplantation

    When using the drug Telmisartan-Richter in patients with impaired renal function, periodic monitoring of the potassium and serum levels of creatinine is recommended. The clinical experience of using the preparation Telmisartan-Richter in patients who have recently undergone kidney transplantation is absent.

    Reduction of the volume of circulating blood (OSHO)

    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-Richter.Such conditions should be eliminated before it is received. The deficiency of fluid and / or sodium should be eliminated before the start of taking Telmisartan-Richter.

    Double blockade of the oenine-angiotensin-aldosterone system

    As the effects of inhibition of RAAS were observed: the occurrence of arterial hypotension, syncope, hyperkalemia and impaired renal function (including acute renal failure) in predisposing patients, especially when used in combination with drugs also acting on this system. Double blockade of RAAS, for example, with the addition of an ACE inhibitor (angiotensin converting enzyme) to an angiotensin II receptor antagonist, is not recommended for patients with already controlled blood pressure and should be limited to individual cases with enhanced monitoring of renal function.

    Other diseases characterized by RAAS stimulation

    In patients whose vascular tone and renal function depend primarily on RAAS activity (eg, patients with chronic heart failure or kidney disease, including renal artery stenosis), the use of drugs acting on this system such as telmisartan, was associated with the emergence of acute arterial hypotension, hyperaemia, oliguria, or rarely - with acute renal failure (see section "Side effect").

    Primary aldosteronism

    Patients with primary aldosteronism, as a rule, do not respond to treatment with antihypertensive drugs, the effect of which is manifested by inhibition of RAAS. In this regard, the use of the drug Telmisartan-Richter in these cases is not recommended.

    Stenosis of the aortic and mitral valve, hypertrophic obstructive cardiomyopathy

    As with other vasodilators, special precautions are indicated for patients with aortic and mitral stenosis or hypertrophic obstructive cardiomyopathy.

    Hyperkalemia

    The use of drugs acting on RAAS can cause hyperkalemia.

    For elderly patients, patients with renal insufficiency, patients with diabetes mellitus and also with arterial hypertension and coronary heart disease (CHD), patients receiving concomitant medication therapy that may cause an increase in potassium content,and / or patients with concomitant disease, hyperkalemia can be fatal.

    Before considering the possibility of concomitant use of drugs acting on RAAS, it is necessary to evaluate the benefit-risk relationship.

    The main risk factors that should be considered are:

    - Diabetes mellitus, renal failure, age (patients older than 70 years).

    - Combination with one or more drugs acting on RAAS and / or an increase in serum potassium. Drugs or therapeutic classes of drugs that can cause hyperkalemia include salt substitutes containing potassium, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, non-steroidal anti-inflammatory drugs (NSAIDs, including selective COX-2 inhibitors), heparin, immunosuppressants (ciclosporin or tacrolimus) and trimethoprim.


    - Intercurrent diseases, especially dehydration, acute heart failure, metabolic acidosis, impaired renal function, severe deterioration of the kidneys (eg, infectious diseases), cytolysis syndrome (eg, acute limb ischemia, rhabdomyolysis, severe trauma).

    For patients at risk, regular monitoring of serum potassium is recommended (see section "Interaction with other drugs").

    Lactose

    This preparation contains lactose monohydrate. Patients with rare hereditary diseases, such as galactose intolerance, Lappa lactase deficiency or impaired glucose-galactose absorption, should not take this medication.

    Racial differences

    As noted for angiotensin-converting enzyme (ACE) inhibitors, Telmisartan-Richter and other angiotensin II receptor antagonists appear to be less effective in lowering arterial pressure in patients of the Negroid race than in representatives of other races, possibly due to a greater predisposition to decreased renin activity in the population patients of the Negroid race, patients with diabetes mellitus and also with arterial hypertension and ischemic heart disease.

    Other

    As with the use of other antihypertensive drugs, excessive reduction in blood pressure in patients suffering from ischemic cardiopathy, or patients with sugardiabetes and also with arterial hypertension and coronary artery disease can lead to the development of myocardial infarction or cerebral circulation disorders.

    Effect on the ability to drive transp. cf. and fur:Special studies of the effect of the drug on the ability to drive vehicles and work with machinery were not conducted. Care must be taken when driving vehicles, as well as when working with machinery (risk of dizziness and drowsiness).
    Form release / dosage:

    Tablets, film-coated, 40 mg, 80 mg. 7 tablets per blister of Al / Al foil. For 2.4 or 8 blisters in a cardboard box together with instructions for use. By 10 tablets in a blister from Al / Al foil. For 3 or 9 blisters together in a cardboard box.

    Packaging:(10) - blisters (3) - packs cardboard
    (10) - blisters (9) - packs cardboard
    (7) - blisters (2) - packs cardboard
    (7) - blisters (4) - packs cardboard
    (7) - blisters (8) - packs cardboard
    Storage conditions:

    At a temperature of no higher than 30 ° C.

    Keep out of the reach of children!

    Shelf life:

    3 years.

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

    Terms of leave from pharmacies:On prescription
    Registration number:LP-001746
    Date of registration:02.07.2012
    The owner of the registration certificate:GEDEON RICHTER, OJSC GEDEON RICHTER, OJSC Hungary
    Manufacturer: & nbsp
    Representation: & nbspGEDEON RICHTER OJSC GEDEON RICHTER OJSC Hungary
    Information update date: & nbsp01.09.2015
    Illustrated instructions
      Instructions
      Up