Telsartan - instructions for use, dose, side effects, contraindications

Excipients: meglumine 12.00 mg, sodium hydroxide 3.35 mg, povidone-K30 12.0 mg, polysorbate-80 1.50 mg, mannitol 216.05 mg, magnesium stearate 5.10 mg.

1 tablet of 80 mg contains:

Active substance: telmisartan 80.00 mg;

Excipients: meglumine 24.00 mg, sodium hydroxide 6.70 mg, povidone-K30 24.0 mg, polysorbate-80 3.00 mg, mannitol 432.10 mg, magnesium stearate 10.20 mg.

Description:

Tablets 40 mg

The tablet is capsular-shaped, biconvex, white or almost white in color, on one side is the dividing risk and the "T" and "L"on different sides of it, on the other side stamping" 40 ".

Tablets 80 mg

The tablet is capsular, biconvex, white or almost white,on one side the dividing risk and embossing "T" and "L"On different sides of it, on the other side is embossed" 80 ".

Pharmacotherapeutic group:Angiotensin II receptor antagonist

ATX: & nbsp

C.09.C.A.07 Telmisartan

Pharmacodynamics:

Telmisartan is a specific angiotensin receptor antagonist (APA) II, effective when ingested. 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 without exhibiting the properties of an agonist for this receptor. Telmisartan binds only to a subtype AT₁receptors of angiotensin II. Communication is of a lasting nature. Has no affinity for other receptors, including AT₂-receptor and other less studied angiotensin receptors. 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. Telmisartan reduces the concentration of aldosterone in the blood plasma, 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), which also catalyzes the degradation of bradykinin. Therefore, the enhancement of bradykinin-induced side effects is not expected.

In patients with hypertension 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 reception of telmisartan inside. The effect of the drug persists for 24 hours and remains significant up to 48 hours. The pronounced antihypertensive effect usually develops 4 weeks after regular intake of the drug.

In patients suffering from 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.

The telmisartan study evaluated cardiovascular mortality, non-fatal myocardial infarction, nonfatal stroke, or hospitalization due to congestive heart failure.Cardiovascular morbidity and mortality in patients with high cardiovascular risk (coronary artery disease, stroke, peripheral arterial disease, or diabetes mellitus with concomitant lesion of target organs such as retinopathy, left ventricular hypertrophy, macro- or microalbuminuria in anamnesis) over the age of 55 years.

Pharmacokinetics:

When ingested quickly absorbed from the gastrointestinal tract. Bioavailability is 50%. When taken simultaneously with food, a decrease in the area under the pharmacokinetic curve "concentration-time" (AUC) ranges from 6% (when taking a dose of 40 mg) to 19% (with a dose of 160 mg). After 3 hours after ingestion, the concentration in the blood plasma levels out regardless of food intake. There is a difference in the concentrations of telmisartan in the blood plasma in men and women. The maximum concentration in the blood plasma (C_mOh) approximately 3 times and AUC approximately 2 times higher in women than in men without a significant effect on efficacy.

Communication with plasma proteins is 99.5% (mainly with albumin and alpha-1-glycoprotein). The volume of distribution is approximately 500 liters.

Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive. The half-life (T_1/2) 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 (about 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 change in the dose of telmisartan 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 according to the Child-Pugh classification), the daily dose of the drug should not exceed 40 mg.

Indications:

- Arterial hypertension.

- Reduction of cardiovascular morbidity and mortality in patients aged 55 years and older with a high risk of cardiovascular disease,including history of atherothrombotic events such as coronary heart disease (CHD), stroke or atherosclerosis of peripheral arteries, or history of type II diabetes mellitus with documented affection of target organs.

Contraindications:

- Hypersensitivity to the active ingredient or auxiliary components of the drug.

- Pregnancy and the period of breastfeeding.

- Obstructive diseases of the biliary tract.

- Severe liver dysfunction (Child-Pugh class C).

- Simultaneous use with aliskiren and preparations containing aliskiren, in patients with diabetes mellitus and / or moderate or severe renal dysfunction (glomerular filtration rate (GFR) of less than 60 ml / min / 1.73 m²surface area of the body).

- Simultaneous use with angiotensin-converting enzyme inhibitors in patients with diabetic nephropathy.

- Age to 18 years (effectiveness and safety not established).

Carefully:

- Two-sided stenosis of the renal arteries or stenosis of the artery of a single kidney (see section "Special instructions").

- Mild and moderate impairment of liver and / or kidney function (see section "Special instructions").

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

- Hyponatremia.

- Hyperkalemia.

- Conditions after kidney transplantation (no experience of application).

- Chronic heart failure.

- Stenosis of the aortic and mitral valve.

- Idiopathic hypertrophic subaortic stenosis (hypertrophic obstructive cardiomyopathy).

- Primary hyperaldosteronism.

Pregnancy and lactation:

The use of the drug during pregnancy and during breastfeeding is contraindicated.

Pregnancy

There is no adequate data on the use of telmisartan in pregnant women. Studies in animals have shown the presence of reproductive toxicity.

Patients planning a pregnancy should be prescribed an alternative therapy with established safety profile regarding pregnancy.

When establishing the fact of pregnancy, taking the drug should be stopped immediately and consider alternative therapy options.

The use of ARA II in the II and III trimesters of pregnancy in humans is manifested by fetotoxic effects (decreased kidney function, oligohydramnion, delayed ossification of the skull) and neonatal toxicity (renal failure, arterial hypotension, hyperkalemia).

If ARA II was used in the second trimester of pregnancy or later, it is recommended to perform ultrasound examination of the kidneys and bones of the fetal skull.

Newborns, whose mothers received ARA II, should be carefully monitored for arterial hypotension.

Breastfeeding period

Breastfeeding is not recommended during telmisartan therapy, as there is no available data on experience with telmisartan during this period. It is recommended to use alternative therapy with established safety profile regarding breastfeeding, especially in the period of newborns and in nursing preterm infants.

Fertility

There was no effect of telmisartan on the fertility of males and females in pre-clinical studies.

Dosing and Administration:

Inside, regardless of food intake, washing down with water.

Arterial hypertension

The initial recommended dose of Telsartan® is 1 tablet of 40 mg once a day. Some patients may benefit from a dose of 20 mg per day (1/2 tablet 40 mg). In cases where a therapeutic effect is not achieved, the maximum recommended dose of Telsartan® can be increased to 80 mg (1 80 mg tablet or 2 40 mg tablets) 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 of Telsartan^® - 1 tablet of 80 mg once a day.

In the initial period of treatment, an additional correction of blood pressure may be required.

Impaired renal function

There is limited experience with telmisartan in patients with severe renal dysfunction or who are on hemodialysis. Such patients require a low initial dose of 20 mg.

Patients with mild or moderate renal dysfunction are not required to adjust the dose.

Dysfunction of the liver

In patients with mild and moderate impairment of liver function, the daily dose of Telsartan® should not exceed 40 mg.

Application for severe violations of the liver is contraindicated (see section "Contraindications").

Elderly patients

Dosing regimen does not require any changes.

Side effects:

The total incidence of side effects of telmisartan in patients with hypertension in controlled trials is usually comparable to placebo (41.4% versus 43.9%). The observed side effects were not correlated with the sex, age or race of the patients. The safety profile of the drug in patients who received telmisartan for the prevention of cardiovascular morbidity and mortality corresponds to data obtained in patients with arterial hypertension.

The frequency of undesirable effects is as follows: very often (≥1 / 10 appointments); often (1/10 - 1/100 of appointments); infrequently (1/100 - 1/1000 appointments); rarely (1/1000 - 1/10 000); very rarely (<1/10 000 appointments).

Infectious and parasitic diseases

Infrequent infections of the upper respiratory tract (including pharyngitis and sinusitis), urinary tract infections (including cystitis); rarely - sepsis, including cases with a fatal outcome (the mechanism of occurrence is unknown).

Violations of the blood and lymphatic system

Infrequent anemia; rarely - eosinophilia.thrombocytopenia.

Immune system disorders

Rarely - anaphylactic reactions, hypersensitivity.

Disorders from the metabolism and nutrition

Infrequent - hyperkalemia; rarely - hypoglycemia (in patients with diabetes mellitus).

Disorders of the psyche

Infrequently - depression, insomnia; rarely - anxiety.

Disturbances from the nervous system

Infrequent - fainting; rarely - drowsiness.

Disturbances on the part of the organ of sight

Rarely - visual disorders.

Hearing disorders and labyrinthine disorders

Infrequently - vertigo.

Heart Disease

Infrequent bradycardia; rarely - tachycardia.

Vascular disorders

Infrequently, orthostatic hypotension, a decrease in blood pressure (the effect was noted in patients with controlled BP who used telmisartan with the aim of reducing cardiovascular morbidity and mortality against the background of standard therapy).

Disturbances from the respiratory system, chest and mediastinal organs

Infrequent - shortness of breath, cough; very rarely - interstitial lung disease (post-marketing data, cause-and-effect relationship not established).

Disorders from the gastrointestinal tract

Infrequent - pain in the abdomen, diarrhea, indigestion, flatulence, vomiting; rarely - discomfort in the stomach, dry mouth, dysgeusia.

Disturbances from the liver and bile ducts

Rarely - a violation of liver function / liver disease (in most cases have been identified in patients in Japan).

Disturbances from the skin and subcutaneous tissues

Infrequently - a hyperhidrosis, a skin itch, a skin rash; rarely - angioedema (fatal), eczema, erythema, urticaria, drug and toxic rash.

Disturbances from musculoskeletal and connective tissue

Infrequently - myalgia, back pain, muscle spasms; rarely - arthralgia, pain in the extremities, pain in the tendons (symptoms similar to the manifestation of tendinitis).

Disorders from the kidneys and urinary tract

Infringement of function of kidneys, including acute renal failure is infrequent.

General disorders and disorders at the site of administration

Infrequent pain in the chest, general weakness; rarely - flu-like syndrome.

Laboratory and instrumental data

Infrequent - increase in the level of creatinine in the blood; rarely - increasing the concentration of uric acid, increasing the activity of "liver" enzymes, increasing the activity of creatine phosphokinase,decrease in serum hemoglobin level.

Overdose:

Cases of overdose have not been identified.

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

Treatment: symptomatic therapy, hemodialysis is ineffective.

Interaction:

Receiving telmisartan. as well as other drugs acting on the system of renin-angiotensin-aldosterone (RAAS), is capable of provoking hyperkalemia. The risk of hyperkalemia may increase with simultaneous administration with potassium-containing salt substitutes; potassium-sparing diuretics; ACE inhibitors; ARA II; non-steroidal anti-inflammatory drugs (NSAIDs), including selective to cyclooxygenase (COX) type 2; heparin; immunosuppressive drugs (cyclosporine or tacrolimus) and trimethoprim.

The frequency of development of hyperkalemia depends on the presence of risk factors. With the simultaneous use of potassium-sparing diuretics and potassium-containing salt substitutes, the risk of developing hyperkalemia is particularly high. Simultaneous use with ACE inhibitors or NSAIDs is associated with a lower risk of hyperkalemia. Careful observance of precautionary measures.

Double blockade of the renin-angiotensin-aldosterone system

As shown by clinical studies, double blockade of RAAS with the use of ACE inhibitors, ARA II or aliskiren in comparison with monotherapy is associated with an increased risk of arterial hypotension, hyperkalemia and impaired renal function (including acute renal failure).

Digoxin

With the simultaneous administration of telmisartan and digoxin, there is a median increase in peak and residual concentrations of digoxin in blood plasma (49% and 20%, respectively). At the beginning, when correcting and stopping the intake of telmisartan, it is necessary to monitor the concentration of digoxin in the blood serum in order to maintain it within the therapeutic range.

Potassium-sparing diuretics and salt substitutes, containing potassium

ARA II, such as telmisartan, reduce the loss of potassium caused by diuretics. Potassium-sparing diuretics, such as spironolactone. eplerenone, triamterene or amiloride, potassium preparations or potassium-containing salt substitutes, can cause a significant increase in serum potassium content.If their simultaneous use is necessary in connection with the presence of proven hypokalemia, treatment should be conducted with caution under frequent monitoring of potassium content in the blood serum.

Lithium

With simultaneous administration of lithium preparations with ACE inhibitors and ARA II, including telmisartan, there was a reversible increase in the concentration of lithium in the blood plasma, accompanied by a toxic effect. If it is necessary to simultaneously use these drugs, it is recommended to monitor the content of lithium salts in the blood serum.

Nonsteroidal anti-inflammatory drugs

Acetylsalicylic acid in doses of 3 g per day or more, inhibitors of COX-2 and nonselective NSAIDs can reduce the antihypertensive effect of ARA II. In patients with impaired renal function (with dehydration or elderly age), simultaneous administration of ARA II and COX inhibitors can lead to reversible impairment of renal function. Therefore, the drugs in this combination are administered with caution, especially in elderly patients. Before using telmisartan, it is recommended to evaluate the function of the kidneys, as well as correct the violations of the water-electrolyte balance; in the future, it is advisable to monitor kidney function.

Ramipril

Simultaneous application with ramipril leads to an increase in AUC_0-24and C_mOh ramipril and ramiprilata 2.5 times. The clinical significance of this effect is not established.

Loop and thiazide diuretics

Prior therapy with diuretics in high doses, including furosemide (loop diuretic) and hydrochlorothiazide (thiazide diuretic), can lead to a decrease in the volume of circulating blood and an increased risk of arterial hypotension at the beginning of telmisartan therapy.

Other antihypertensives

The ability of telmisartan to reduce blood pressure can be enhanced by the simultaneous use of other antihypertensive agents. Given the pharmacological properties may increase the effect of antihypertensive drugs including telmisartan with simultaneous administration with baclofen or amifostine.

Ethanol, barbiturates, anesthetics and antidepressants can contribute to the development of orthostatic hypotension.

Systemic corticosteroids

Glucocorticosteroids reduce the antihypertensive effect of telmisartan.

Special instructions:

Impaired liver function

Telmisartan should not be given to patients with cholestasis, bile duct obstruction, or severe liver dysfunction (Child-Pugh class C), since telmisartan is excreted mainly with bile. In such patients, the excretion of the drug is expected to decrease. Telmisartan Caution should be used with caution in patients with mild or moderate hepatic impairment (Child-Pugh class A or B).

Vasorenal arterial hypertension

When using drugs that affect RAAS in patients with bilateral renal artery stenosis or stenosis of a single functioning kidney, the risk of developing severe arterial hypotension and renal failure is increased.

Impaired renal function

When using telmisartan in patients with renal insufficiency, it is recommended to monitor serum potassium content and creatinine concentration. The experience of application after the recently transferred kidney transplantation is not described.

Hypovolemia

In patients with hypovolemia and / or hyponatremia due to intensive diuretic therapy, limiting salt intake, diarrhea, or vomiting, symptomatic arterial hypotension may develop, especially after taking the first dose of telmisartan. Before the beginning of therapy it is necessary to correct violations of water electrolyte balance.

Double blockade of RAAS

Simultaneous administration of ACE inhibitors, APA II or aliskiren increases the risk of hypotension, hyperkalemia and renal dysfunction (including acute renal failure), therefore the use of a combination of these drugs is regarded as a double blockade of RAAS and is not recommended for prescribing to patients. If absolutely necessary, therapy using double blockade of RAAS should be performed under strict medical supervision and careful monitoring of kidney function, electrolytes and blood pressure.

ACE inhibitors and ARA II should not be used simultaneously in patients with diabetic nephropathy.

Other conditions accompanied by activation of RAAS

In patients whose vascular tone and renal function is determined by the activity of RAAS (patients with chronic heart failure or kidney disease, including stenosis of the two renal arteries or stenosis of the single kidney artery), the use of drugs that affect RAAS can be accompanied by the development of arterial hypotension, hyperaemia, oliguria and, in rare cases, acute renal failure.

Primary hyperaldosteronism

Patients with primary hyperaldosteronism resistant to antihypertensive drugs affecting RAAS therefore such patients use of telmisartan is not recommended.

Stenosis of the aortic and / or mitral valve, hypertrophic obstructive cardiomyopathy (GOKMP)

Telmisartan must be used with caution in patients with hemodynamically significant stenosis of the aortic and / or mitral valves or GOKMP.

Patients with diabetes who are receiving insulin or hypoglycemic agents for ingestion

When using telmisartan in these patients, hypoglycemia may develop. It is recommended to regularly monitor the concentration of blood glucose and, if necessary, to correct the dose of hypoglycemic agents.

Hyperkalemia

The use of drugs that affect RAAS can cause hyperkalemia. Before the simultaneous use of such drugs should evaluate the benefit / risk ratio.

Risk factors for hyperkalemia:

- kidney failure, age over 70 years, diabetes mellitus;

- simultaneous use of drugs that affect RAAS (ACE inhibitors, APA II) and / or potassium-sparing diuretics (spironolactone, eplerenone, triamterene, amiloride), potassium or potassium-containing food salt substitutes, NSAIDs (including COX-2 selective), heparin, immunosuppressive drugs (ciclosporin or tacrolimus), as well as trimethoprim;

- concomitant conditions such as dehydration, acute heart failure in the stage of decompensation, metabolic acidosis, impaired renal function, sudden progression of kidney disease (infectious diseases), conditions accompanied by tissue necrosis (acute limb ischemia, rhabdomyolysis, extensive trauma).

Patients at risk should carefully monitor the serum potassium concentration.

Ethnic Features

ACE inhibitors and ARA II (including telmisartan) may have a less pronounced antihypertensive effect in patients of the Negroid race.

Perhaps this is due to a decrease in the level of renin in hypertension in such patients compared with representatives of other races.

Other

As with any antihypertensive treatment, excessive BP reduction in patients with ischemic heart disease or ischemic cardiomyopathy can lead to myocardial infarction or stroke.

Effect on the ability to drive transp. cf. and fur:

Special clinical studies to assess the effect of the drug on the ability to drive and machinery have not been carried out. However, when driving and dealing with hazardous activities, it 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 7 tablets in a blister of (PVC / Al / PA) foil / aluminum foil. For 2 or 4 blisters together with instructions for use in a pack of cardboard.

For 10 tablets in a blister of (PVC / Al / PA) foil / aluminum foil. For 3 blisters together with instructions for use in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

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

Terms of leave from pharmacies:On prescription

Registration number:LP-004161

Date of registration:28.02.2017

Expiration Date:28.02.2022

The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India

Manufacturer: & nbsp

DR. REDDY`S LABORATORIES, LTD. India

Representation: & nbspDr. Reddy`c Laboratoris Ltd.Dr. Reddy`c Laboratoris Ltd.

Information update date: & nbsp30.03.2017

Illustrated instructions

Instructions

Telsartan® (Telsartan®)