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

Excipients: sodium hydroxide - 1.70 mg, povidone-K25 - 5.40 mg, meglumine - 6.00 mg, mannitol - 81.90 mg, magnesium stearate - 2.00 mg, crospovidone - 3.00 mg.

Each 40 mg tablet contains: active substance: telmisartan - 40.00 mg;

Excipients: sodium hydroxide - 3.40 mg, povidone-K25 - 10.80 mg, meglumine - 12.00 mg, mannitol - 163,80 mg, magnesium stearate - 4,00 mg, crospovidone - 6.00 mg

Each 80 mg tablet contains: active substance: telmisartan - 80.00 mg;

Excipients: sodium hydroxide - 6.70 mg, povidone-K25 - 21.60 mg, meglumine - 24.00 mg, mannitol - 327.70 mg, magnesium stearate - 8.00 mg, crospovidone - 12,00 mg.

Description:

Tablets 20 mg

Round tablets with bevel, white, engraved "LC" on one side of the tablet.

Tablets 40 mg

Oblong biconvex tablets, white, engraved "LC" on one side of the tablet.

Tablets 80 mg

Oblong biconvex tablets, white, engraved "LC" on one side of the tablet.

Pharmacotherapeutic group:Angiotensin II receptor antagonist

ATX: & nbsp

C.09.C.A.07 Telmisartan

Pharmacodynamics:

Telmisartan is a specific angiotensin receptor antagonist II (a type AT1), effective at ingestion. Has a high affinity for the subtype AT1 receptors of angiotensin II, through which the action of angiotensin is realized II. Releases angiotensin II from binding to a receptor, without the action of an agonist for this receptor. Telmisartan binds only to a subtype AT1 receptors of angiotensin II. Communication is of a lasting nature. Has no affinity for other receptors, including the 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, the concentration of which increases with the appointment of telmisartan, have not been studied.Reduces the concentration of aldosterone in the blood, does not inhibit renin in the blood plasma and does not block the ion channels. Telmisartan does not inhibit the angiotensin converting enzyme (kininaza II) (an enzyme that also destroys bradykinin). Therefore, the gain side effects of bradykinin, 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 intake of telmisartan inside. The drug remains 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.

Pharmacokinetics:

Suction

When ingested quickly absorbed from the gastrointestinal tract.Bioavailability is about 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 administration, the concentration in the blood plasma levels out regardless of the intake of food.

Distribution

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.

Metabolism

Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive.

Excretion

The half-life (T1/2) - 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 "hepatic blood flow" (about 1500 ml / min).

Pharmacokinetics the special patient groups

Gender differences

There is a difference in plasma concentrations in men and women. FROMmax (maximum concentration) and AUC were approximately 3 and 2 times, respectively, higher in women than in men without significant effect on efficacy. Dose correction is not required.

Elderly patients

The pharmacokinetics of telmisartan in elderly patients does not differ from pharmacokinetics in young patients. Dose correction is not required.

Patients with impaired renal function

In patients with mild to moderate renal dysfunction, dosage adjustment for telmisartan is not required.

Patients with severe renal failure and patients on hemodialysis are recommended a lower initial dose of 20 mg per day.

Telmisartan is not excreted by hemodialysis.

Patients with impaired hepatic function

Studies of pharmacokinetics in patients with hepatic insufficiency showed an increase in the absolute bioavailability of telmisartan to almost 100%.

With hepatic insufficiency T1/2 does not change. In patients with mild and moderate impairment of liver function (class A and B on the Child scale-Pdaily 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.

Contraindications:

- Hypersensitivity to the active ingredient or auxiliarycomponents 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 use of Telpres with aliskiren in patients with diabetes mellitus and / or renal dysfunction (glomerular filtration rate less than 60 ml / min / 1.73 m²);

- Simultaneous use of ACE inhibitors in patients with diabetic nephropathy;

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

Carefully:

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

- Violations of the liver and / or kidney function (see section "Special instructions");

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

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

- Hyponatremia;

- Hyperkalemia;

- Chronic heart failure;

- Cardiac ischemia;

- Stenosis of the aortic and mitral valve;

- Idiopathic hypertrophic subaortal stenosis (hypertrophic obstructive cardiomyopathy);

- Primary aldosteronism (efficacy and safety not established);

- Simultaneous use with ACE inhibitors or aliskiren;

- Simultaneous use with potassium preparations, potassium-sparing diuretics;

- Diabetes.

Pregnancy and lactation:

Medicines that directly affect RAAS can cause serious damage and death of the developing fetus, so when planning or establishing the fact of pregnancy, the drug should be immediately withdrawn and, if necessary, an alternative antihypertensive therapy with an established safety profile for use during pregnancy is prescribed. The use of the drug during 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 receptor antagonists II During the second and third trimester of pregnancy, a person causes fetotoxicity (decreased kidney function, oligohydramnion, slowing ossification of the skull), as well as neonatal toxicity (kidney failure, hypotension, hyperkalemia).Patients planning pregnancy should be prescribed alternative therapy. If treatment with angiotensin receptor antagonists II occurred during the second trimester of pregnancy, it is recommended that ultrasound be checked for kidney function and skull conditions in the fetus.

Newborns whose mothers received angiotensin receptor antagonists II, should be carefully observed in relation to hypotension.

Therapy with Telpres is contraindicated in the period of breastfeeding. Studies of the impact on human fertility have not been conducted.

Dosing and Administration:

Inside, regardless of food intake.

Arterial hypertension

The initial recommended dose of the drug Telpres is 1 tab. (40 mg) once a day. In cases where the therapeutic effect is not achieved, the maximum recommended dose of Telpres may be increased to 80 mg once daily. 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 Telpres 80 mg once a day.

In the initial period of treatment, it is recommended to monitor the level of blood pressure (BP), correction of antihypertensive therapy may be required.

Impaired renal function

In patients with severe impairment of kidney function and patients on hemodialysis, experience is limited. In such patients, the recommended starting dose is 20 mg per day. In patients with mild and moderate impairment of renal function, dose adjustment is not required.

Impaired liver function

In patients with mild and moderate impairment of liver function (class A and B on the Child-Pugh scale, respectively), the daily dose of Telpres should not exceed 40 mg.

Elderly patients

Older patients do not need a dose adjustment.

Side effects:

In general, the incidence of adverse reactions noted for telmisartan is comparable to that of placebo. The observed side effects were not correlated with the sex, age or race of the patients. Classification of the frequency of adverse reactions of the World Health Organization (WHO): veryoften (> 1/10); often (from> 1/100 to <1/10); infrequently (from> 1/1000 to <1/100); rarely (from> 1/10 000 to <1/1000); very rarely (from <1/10 000); frequency is unknown (according to available data, it is not possible to establish the frequency of occurrence).

Infectious and parasitic diseases:

infrequently: infections of the upper respiratory tract, including pharyngitis and sinusitis, urinary tract infections (including cystitis);

unknown frequency: sepsis, including sepsis with fatal outcome.

Violations from the blood and lymphatic system:

infrequently: anemia;

rarely: thrombocytopenia;

unknown frequency: eosinophilia.

Disorders from the psyche:

infrequently: depression; rarely: anxiety.

Impaired nervous system:

infrequently: insomnia, syncope, vertigo; rarely: faint.

Disorders from the side of the organ of vision:

rarely: impaired vision.

Heart Disease:

infrequently: aetiology; rarely: tachycardia.

Vascular disorders:

infrequent: marked decrease in blood pressure, orthostatic hypotension;

* was often observed in patients with controlled BP who received telmisartan treatment to reduce the risk of cardiovascular mortality in addition to standard treatment.

Disturbances from the respiratory system, chest and mediastinal organs:

infrequently: shortness of breath, cough.

Disorders from the gastrointestinal tract:

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

rarely: indigestion, discomfort, dryness of the oral mucosa, impaired liver function / liver disease.

Immune system disorders:

rarely: hypersensitivity, angioedema (including fatal); unknown frequency: anaphylactic reactions.

Disturbances from the skin and subcutaneous tissues

infrequently: a hyperhidrosis, a skin itch, a rash;

rarely: erythema, drug rash, toxic skin rash, eczema, unknown frequency: urticaria.

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 kidneys and urinary tract:

infrequently: renal failure, including acute renal failure.

Disorders from nutrition and metabolism:

infrequently: hyperkalemia.

General disorders:

infrequently: chest pain, asthenia (weakness);

rarely: influenza-like condition.

Influence on the results of laboratory indicators and instrumental studies:

infrequently: increased concentration of creatinine in the blood;

rarely: increased concentration of uric acid in the blood, "liver" enzymes, activity of serum creatinophosphinase, a decrease in 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, bradycardia, dizziness, increased serum creatinine concentration and acute renal failure may also occur.

Treatment: symptomatic and supportive. Proposed measures include: causing vomiting and / or gastric lavage, taking activated charcoal, replenishing lack of fluid and salts. Constant monitoring of the content of electrolytes and creatinine in the blood serum. Hemodialysis is not effective.

Interaction:

Telmisartan may increase the antihypertensive effect of other antihypertensive agents.Other types of interactions that have clinical relevance have not been identified. Combined use with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin and amlodipine does not lead to clinically significant interaction.

Double blockade of the renin-angiotensin-aldosterone system (RAAS).

The concomitant use of telmisartan with aliskiren is contraindicated in patients with diabetes mellitus or renal insufficiency (GFR less than 60 mL / min / 1.73 m²body surface area) and is not recommended for other patients. The simultaneous use of telmisartan and inhibitors of AG1F is contraindicated in patients with diabetic nephropathy.

Clinical studies have shown that the double blockade of RAAS due to the combined use of ACE inhibitors, APA II or aliskiren is associated with an increased incidence of adverse events such as hypotension, hyperkalemia and renal dysfunction (including acute renal failure) compared with the use of only one drug , operating on the RAAS.

The risk of developing hyperkalemia may increase when combined withother drugs that can cause hyperkalemia (potassium-containing dietary supplements and salt substitutes containing potassium and potassium-sparing diuretics (spironolactone, eplerenone, triamterene or amiloride), non-steroidal anti-inflammatory drugs (NSAIDs, including selective inhibitors of cyclooxygenase-2 (COX)), heparin, immunosuppressants (ciclosporin, tacrolimus, trimethoprim)). If necessary, against the background of documented hypokalemia, joint use of drugs should be carried out with caution and regularly monitor the potassium content in the blood plasma.

Digoxin

With the joint administration of telmisartan with digoxin, an increase in the mean Cmof digoxin in the blood plasma by 49% and a minimum concentration of 20%. At the beginning of treatment, when choosing a dose and stopping telmisartan treatment, the concentration of digoxin in the blood plasma should be carefully monitored for its maintenance within the therapeutic range.

Potassium-sparing diuretics or potassium-containing food additives

Angiotensin II receptor antagonists, such as telmisartan, reduce the diuretic-induced loss of potassium.Potassium-sparing diuretics, for example, spironolactone, eplerenone, triamterene or amiloride, potassium-containing dietary supplements or salt substitutes can lead to a significant increase in potassium levels in the blood plasma. If concomitant use is indicated, since there is documented hypokalemia, they should be used with caution and against a background of regular control of potassium in the blood plasma.

Lithium preparations

When co-administration of lithium preparations with ACE inhibitors and APAII, including telmisartan, there was a reversible increase in the concentration of lithium in the blood plasma and its toxic effect. If it is necessary to use this combination of drugs, it is recommended to carefully monitor the concentration of lithium in the blood plasma.

Non-steroidal anti-inflammatory drugs (NSAIDs)

NSAIDs (including acetylsalicylic acid in doses used for anti-inflammatory treatment, COX-2 inhibitors and nonselective NSAIDs) can weaken the antihypertensive effect of APAII. In some patients with impaired renal function (eg, patients with dehydration, elderly patients with impaired renal function), joint application of APAII and drugs depressing cyclooxygenase-2 can lead to further deterioration of renal function, including the development of acute renal failure, which is usually reversible. Therefore, joint use of drugs should be done with caution, especially elderly patients. Proper fluid intake should also be ensured, in addition, at the beginning of the joint application and periodically the kidney function should be monitored periodically thereafter.

Diuretics (thiazide or loop diuretics)

Prior treatment with high doses of diuretics, such as furosemide (loop diuretic) and hydrochlorothiazide (thiazide diuretic), can lead to hypovolemia and the risk of developing arterial hypotension at the beginning of telmisartan treatment.

Other antihypertensive agents

The effect of telmisartan may be enhanced by the joint use of other antihypertensive drugs. Based on the pharmacological properties of baclofen and amifostine, it can be assumed that they will enhance the therapeutic effect of all antihypertensive agents, including telmisartan. In addition, orthostatic hypotension may increase with the use of alcohol, barbiturates, drugs or antidepressants.

Corticosteroids (for systemic use)

Corticosteroids weaken the action of telmisartan.

Special instructions:

Dysfunction of the liver

The use of Telpres is contraindicated in patients with cholestasis, bile duct obstruction, or severe liver dysfunction (class C Child-Pugh classification) (see "Contraindications"), because telmisartan mostly excreted with bile. It is suggested that in these patients the hepatic clearance of telmisartan is reduced. In patients with mild to moderate liver failure (class A and B according to the Child-Pugh classification), Telpres should be used with caution (see "With caution").

Renovascular hypertension

When treating with drugs that act on RAAS, patients with bilateral artery stenosis or stenosis of the artery of a single functioning kidney are at increased risk for severe arterial hypotension and renal failure.

Impaired renal function and kidney transplantation

When using the drug Telpres in patients with impaired renal function, periodic monitoring of the potassium and creatinine content in the blood plasma is recommended. The experience of clinical use of Telpres in patients who have recently undergone kidney transplantation is not available.

Decreased circulating blood volume

Symptomatic arterial hypotension, especially after the first administration of Telpres, may occur in patients with reduced BCC and / or sodium content in blood plasma on the background of previous treatment with diuretics, restriction of salt intake, diarrhea, or vomiting. Such conditions (deficiency of fluid and / or sodium) should be eliminated before the start of taking Telpres.

Double blockade of the renin-angiotensin-aldosterone system

The concomitant use of telmisartan with aliskiren is contraindicated in patients with diabetes mellitus or renal insufficiency (glomerular filtration rate is less than 60 ml / min / 1.73 m²) (see the section "Contraindications").

Simultaneous use of telmisartan and ACE inhibitors is contraindicated in patients with diabetic nephropathy (see section "Contraindications").

As a result of the oppression of RAAS, arterial hypotension, syncope, hyperkalemia and impaired renal function (including acute renal failure) were noted in patients who were predisposed to this, especially when several drugs were used together, also acting on this system. Therefore, the double blockade of RAAS (for example, against the background of taking telmisartan with other antagonists of RAAS) is not recommended.

In cases of vascular tone and kidney function, mainly from RAAS activity (for example, in patients with chronic heart failure or kidney diseases, including stenosis of the renal arteries, or stenosis of the artery of a single kidney), the administration of drugs that affect this system may be accompanied by the development of acute arterial hypotension, hyperazotemia, oliguria and, in rare cases, acute renal failure.

Primary aldosteronism

In patients with primary aldosteronism, treatment with antihypertensive drugs, which are effected by inhibition of RAAS, is usually ineffective.

Stenosis of the aortic and mitral valve, hypertrophic obstructive cardiomyopathy

Care should be taken when using Telpres (as well as other vasodilators) in patients with aortic or mitral stenosis, as well as hypertrophic obstructive cardiomyopathy.

Hyperkalemia

Taking medicines acting on RAAS can cause hyperkalemia. In elderly patients, patients with renal insufficiency or diabetes mellitus, patients also taking medications that promote increased levels of potassium in the blood plasma, and / or patients with concomitant diseases, hyperkalemia can be fatal.

When deciding on the concomitant use of drugs acting on RAAS, it is necessary to assess the risk-benefit ratio.

The main risk factors for the development of hyperkalemia, which 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 potassium-containing food additives.Drugs or therapeutic classes of medications 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, cytolysis syndrome (eg, acute limb ischemia, rhabdomyolysis, extensive trauma).

Patients at risk should carefully monitor potassium levels in the blood plasma (see section "Interaction with other drugs").

Ethnic differences

ACE inhibitors, telmisartan and other ARAII, 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 a decrease in renin activity in the population of these patients.

Other

As with the use of other antihypertensive drugs, excessive reduction in blood pressure in patients suffering from ischemic cardiomyopathy or coronary heart disease can lead to the development of myocardial infarction or stroke.

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

Special clinical studies of the effect of the drug on the ability to control the car and mechanisms were not carried out. When driving and working with mechanisms that require increased concentration of attention, care should be taken, as when taking telmisartan seldom there may be dizziness and drowsiness.

Form release / dosage:

Tablets 20 mg, 40 mg, 80 mg.

Packaging:

For 14 tablets in Al / Al blister. For 2 or 7 blisters with instructions for use in a cardboard bundle.

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.

Terms of leave from pharmacies:On prescription

Registration number:LP-004400

Date of registration:02.08.2017

Expiration Date:02.08.2022

The owner of the registration certificate:SiNViTi Pharma Co., Ltd.SiNViTi Pharma Co., Ltd. Cyprus

Manufacturer: & nbsp

Laboratorios LICONSA, S.A. Spain

Representation: & nbspXanter Pharma, LLCXanter Pharma, LLCRussia

Information update date: & nbsp04.09.2017

Illustrated instructions

Instructions

Telpres (Telpres)