Telmista pills 80mg, 84pcs

Composition

1 tablet 40 mg / 80 mg contains:

Active ingredient:

Telmisartan 40.00 mg/80.00 mg

Auxiliary substances:

Meglumine, Sodium hydroxide, Povidone-K 30, lactose monohydrate, Sorbitol (E420), Magnesium stearate

Pharmacological action

of Angiotensin II receptor antagonist (ARA II)

Clinical Pharmacology

Pharmacodynamics

Telmisartan-specific ARA II (type AT₁), effective when taken orally. It has a high affinity for the AT1 subtype of angiotensin II receptors, through which the action of angiotensin II is realized. Displaces angiotensin II from binding to the receptor, without having an agonist effect on this receptor. Telmisartan binds only to the AT1 subtype of angiotensin II receptors. The relationship is long-term. It has no affinity for other receptors, including AT₂ receptors and other less well-studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible overstimulation with angiotensin II, the concentration of which increases with the use of telmisartan, have not been studied. Reduces the concentration of aldosterone in the blood plasma, does not inhibit renin in the blood plasma and does not block ion channels. Telmisartan does not inhibit the angiotensin-converting enzyme (ACE) (kininase II) (an enzyme that also breaks down bradykinin). This allows you to avoid side effects associated with the action of bradykinin (for example, dry cough).

Essential hypertension

In patients, telmisartan 80 mg completely blocks the hypertensive effect of angiotensin II. The onset of antihypertensive action is noted within 3 hours after the first use of telmisartan. The effect of the drug persists for 24 hours and remains significant for up to 48 hours. A pronounced antihypertensive effect usually develops after 4-8 weeks of regular use of telmisartan.

In patients with arterial hypertension, telmisartan reduces systolic and diastolic blood pressure( BP) without affecting the heart rate (HR).

In the case of abrupt withdrawal of telmisartan, blood pressure gradually returns to its original level without the development of “withdrawal”syndrome.

The results of comparative clinical studies have shown that the antihypertensive effect of telmisartan is comparable to the antihypertensive effect of other classes of drugs (amlodipine, atenolol, enalapril, hydrochlorothiazide and lisinopril).

The incidence of dry cough was significantly lower with telmisartan compared to ACE inhibitors.

Prevention of cardiovascular diseases

In patients aged 55 years and older with a history of coronary heart disease (CHD), stroke, transient ischemic attack, peripheral artery disease, or complications of type 2 diabetes mellitus (such as retinopathy, left ventricular hypertrophy, macro – or microalbuminuria) who are at risk of cardiovascular events, telmisartan had an effect similar to that of ramipril in reducing the combined end point: cardiovascular mortality, heart failure, and heart failure. from non-fatal myocardial infarction, non-fatal stroke, and hospitalization for chronic heart failure(CHF).

Telmisartan was also effective, as was ramipril, in reducing the frequency of secondary points: cardiovascular mortality, non-fatal myocardial infarction.

Dry cough and angioedema were less frequently reported with telmisartan compared to ramipril, while hypotension was more likely to occur with telmisartan.

Children’s and adolescent patients

The safety and efficacy of telmisartan in children and adolescents under 18 years of age have not been established.

Pharmacokinetics

When taken orally, it is rapidly absorbed from the gastrointestinal tract (GIT). Bioavailability – 50%. The decrease in the area under the concentration-time curve (AUC) with simultaneous use of telmisartan with food intake ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). After 3 hours after ingestion, the concentration in the blood plasma is leveled, regardless of the time of food intake. There is a difference in plasma concentrations in men and women. The maximum concentration (cmax) in blood plasma and AUC in women compared to men were approximately 3 and 2 times higher, respectively (without significant effect on efficacy).

The relationship with plasma proteins is 99.5%, mainly with albumin and alpha-1 glycoprotein.

The average apparent volume of distribution at equilibrium concentration is 500 liters. It is metabolized by conjugation with glucuronic acid. The metabolites are pharmacologically inactive. The half-life (_half-life) is more than 20 hours. It is excreted mainly through the intestines in unchanged form and by the kidneys – less than 2% of the dose taken. Total plasma clearance is high (900 ml / min) compared to “hepatic” blood flow (about 1500 ml / min).

Pharmacokinetics in selected groups of patients

Elderly patients

The pharmacokinetics of telmisartan in elderly patients do not differ from the pharmacokinetics in young patients. No dose adjustment is required.

Patients with renal insufficiency

No dose adjustment is required in patients with renal insufficiency, including patients on hemodialysis.

Telmisartan is not removed by hemodialysis.

Patients with hepatic insufficiency

In patients with mild to moderate hepatic impairment (Child-Pugh class A and B), the daily dose of the drug should not exceed 40 mg.

Application in pediatrics

The main indicators of telmisartan pharmacokinetics in children aged 6-18 years after taking telmisartan at a dose of 1 mg / kg or 2 mg/kg for 4 weeks are generally comparable with those obtained in the treatment of adult patients, and confirm the non-linearity of telmisartan pharmacokinetics, especially with respect to_max.

Indications

Essential hypertension.

Reduction of mortality and incidence of cardiovascular diseases in adult patients:

– with cardiovascular diseases of atherothrombotic origin (ischemic heart disease, stroke or peripheral artery disease in the anamnesis);

– with type 2 diabetes mellitus with damage to target organs.

Use during pregnancy and lactation

Pregnancy

The useof Telmista® is contraindicated during pregnancy. The use of ARA II in the first trimester of pregnancy is not recommended, these drugs should not be used during pregnancy. If pregnancy is diagnosed, Telmista® should be discontinued immediately. If necessary, alternative antihypertensive therapy (other classes of antihypertensive drugs approved for use during pregnancy) should be prescribed.

The use of ARA II in the second-third trimesters of pregnancy is contraindicated.

In preclinical studies of telmisartan, no teratogenic effects were detected, but fetotoxicity was established. It is known that the use of ARA II in the second-third trimesters of pregnancy causes fetotoxicity in humans (decreased renal function, oligohydramnios, slowing ossification of the fetal skull bones), as well as neonatal toxicity (renal failure, hypotension, hyperkalemia). Alternative therapy should be used in patients planning pregnancy. If you still used ARA II in the second or third trimesters of pregnancy, then it is necessary to conduct an ultrasound examination of the kidneys and skull bones of the fetus.

Newborns whose mothers took ARA II during pregnancy should be monitored, as hypotension may develop in the newborn.

Breast-feeding period

Information on the use of telmisartan during breastfeeding is not available. The use of Telmista® during breastfeeding is contraindicated (see the section “Contraindications”), an alternative antihypertensive drug with a more favorable safety profile should be used, especially when feeding a newborn or premature baby.

Studies on the effect on human fertility have not been conducted.

Contraindications

Hypersensitivity to the Active ingredient or excipients of the drug.

Pregnancy.

Breast-feeding period.

Obstructive diseases of the biliary tract.

Severe hepatic impairment (Child-Pugh class C).

Concomitant use with aliskiren and drugs containing aliskiren in patients with diabetes mellitus and/or moderate to severe renal impairment (glomerular filtration rate [GFR] less than 60 ml/min/1.73 m2 of body surface area).

Concomitant use with ACE inhibitors in patients with diabetic nephropathy.

Fructose or lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome (Telmista® contains lactose and sorbitol [E 420]).

Age up to 18 years (efficacy and safety have not been established).

Side effects

According to the World Health Organization (WHO), undesirable effects are classified according to their frequency as follows: very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥1/1,000 to < 1/100), rare (≥1/10,000 to < 1/1,000), very rare (

Within each group, according to the frequency of occurrence, adverse reactions are presented in descending order of severity.

Infectious and parasitic diseases

infrequently: urinary tract infections, including cystitis, upper respiratory tract infections, including pharyngitis and sinusitis;

rarely: sepsis, including fatal outcome.

Disorders of the blood and lymphatic system

infrequently: anemia;

rarely: eosinophilia, thrombocytopenia.

Immune system disorders

are rare: anaphylactic reaction, hypersensitivity.

Metabolic and nutritional

disorders infrequently: hyperkalemia;

rarely: hypoglycemia (in patients with diabetes mellitus).

Mental disorders

infrequently: insomnia, depression;

rarely: anxiety.

Nervous system disorders

infrequently: syncope;

rarely: drowsiness.

Visual disturbances

are rare: visual disturbances.

Hearing disorders and labyrinth disorders

infrequently: vertigo.

Cardiac disorders

infrequently: bradycardia;

rarely: tachycardia.

Vascular disorders

infrequently: marked decrease in blood pressure, orthostatic hypotension.

Respiratory, thoracic and mediastinal

disorders uncommon: shortness of breath, cough;

very rare: interstitial lung disease.

Disorders of the gastrointestinal tract

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

rarely: dryness of the oral mucosa, stomach discomfort, impaired taste sensations.

Liver and biliary tract

disorders rare: impaired liver function/liver damage.

Skin and subcutaneous tissue disorders

infrequently: pruritus, hyperhidrosis, skin rash;

rarely: angioedema (also fatal), eczema, erythema, urticaria, drug rash, toxic skin rash.

Musculoskeletal and connective tissue

disorders infrequently: back pain (sciatica), muscle spasms, myalgia;

rarely: arthralgia, limb pain, tendon pain (tendinitis-like syndrome).

Renal and urinary tract

disorders infrequently: impaired renal function, including acute renal failure.

General disorders and disorders at the injection

site infrequently: chest pain, asthenia (weakness);

rarely: flu-like syndrome.

Laboratory and instrumental studies

are infrequent: increased concentration of creatinine in the blood plasma;

rarely: decreased hemoglobin, increased concentration of uric acid in the blood plasma, increased activity of “liver” enzymes and creatine phosphokinase (CK) in the blood plasma.

Interaction

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

Concomitant use of telmisartan with drugs containing aliskiren is contraindicated in patients with diabetes mellitus and/or moderate or severe renal insufficiency (GFR less than 60 ml/min / 1.73 m2 of body surface area) and is not recommended in other patients.

Concomitant use of telmisartan and ACE inhibitors is contraindicated in patients with diabetic nephropathy (see section “Contraindications”) and is not recommended in other patients.

The clinical trial data has shown that dual blockade of RAAS due to the combined use of ACE inhibitors, APA II or aliskiren associated with increased frequency of adverse events such as hypotension, hyperkalemia, and impaired renal function (including acute renal failure) compared to using only one drug acting on the RAAS.

The risk of hyperkalemia may be increased when concomitant use with other drugs that can cause hyperkalemia (potassium-containing dietary supplements and salt substitutes containing potassium, potassium-sparing diuretics [e. g., spironolactone, eplerenone, triamterene or amiloride], nonsteroidal anti-inflammatory drugs [NSAIDs], including selective cyclooxygenase-2 inhibitors (COX-2), heparin, immunosuppressants [cyclosporine or tacrolimus], and trimethoprim). If necessary, against the background of documented hypokalemia, concomitant use of drugs should be carried out with caution and regularly monitor the content of potassium in the blood plasma.

Digoxin

When telmisartan was co-administered with digoxin, there was an average increase_{in cmax} of digoxin in blood plasma by 49% and a minimum concentration by 20%. At the beginning of treatment, when selecting the dose and stopping treatment with telmisartan, the concentration of digoxin in the blood plasma should be carefully monitored to maintain it within the therapeutic range.

Potassium-sparing diuretics or potassium

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

Lithium preparations

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

NSAIDs

NSAIDs (i. e. acetylsalicylic acid in doses used for anti-inflammatory treatment, COX-2 inhibitors and non-selective NSAIDs) may weaken the antihypertensive effect of APA II. In some patients with impaired renal function (for example, in patients with dehydration, elderly patients with impaired renal function), the simultaneous use of APA II and drugs that inhibit COX-2 may lead to further deterioration of renal function, including the development of acute renal failure, which is usually reversible. Therefore, concomitant use of drugs should be carried out with caution, especially in elderly patients. Proper fluid intake should be ensured, in addition, at the beginning of simultaneous use and periodically thereafter, renal function indicators should be monitored.

Diuretics (thiazide or loop)

Previous treatment with high-dose diuretics, such as furosemide (loop diuretic) and hydrochlorothiazide (thiazide diuretic), may lead to hypovolemia and the risk of hypotension at the start of telmisartan treatment.

Other antihypertensive agents

The effect of telmisartan may be enhanced with the simultaneous 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 alcohol, barbiturates, narcotic drugs or antidepressants.

Corticosteroids (for systemic use)

Corticosteroids weaken the effect of telmisartan.

How to take, course of use and dosage

Inside, once a day, washed down with liquid, regardless of the time of meal.

To ensure the following dosage regimen, in particular, to ensure the initial doses of the drug in certain groups of patients, it is necessary to use telmisartan tablets with a dosage option of 20 mg (for example,20 mg tablets or 40 mg tablets with a risk).

Essential hypertension

The initial recommended dose of Telmista® is 40 mg (1 tablet of 40 mg) once a day. In some patients,20 mg per day may be effective. In cases where the therapeutic effect is not achieved, the maximum recommended dose of Telmista® can be increased to 80 mg once a day. Alternatively, Telmista® can be taken in combination with thiazide diuretics, for example, hydrochlorothiazide, which, when used simultaneously, had an additional antihypertensive effect. 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.

Reduced mortality and incidence of cardiovascular diseases

The recommended dose is 1 tabletof Telmista ® 80 mg once a day.

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

Special patient populations

Impaired renal function

There is limited experience with telmisartan in patients with severe renal insufficiency or patients undergoing hemodialysis.

A lower initial dose of 20 mg per day is recommended for these patients (see section “Special instructions”). No dose adjustment is required for patients with mild to moderate renal impairment.

Concomitant use of Telmista® with aliskiren-containing drugs in patients with diabetes mellitus and/or moderate to severe renal impairment (GFR less than 60 ml/min / 1.73 m2 of body surface area) is contraindicated (see section “Contraindications”).

Concomitant use ofTelmista with ACE inhibitors is contraindicated in patients with diabetic nephropathy (see section “Contraindications”).

Impaired liver function

Telmista® is contraindicated in patients with severe hepatic insufficiency (Child-Pugh Class C) (see section “Contraindications”). In patients with mild to moderate hepatic insufficiency (Child-Pugh class A and B, respectively), Telmista® should be prescribed with caution, the dose should not exceed 40 mg once a day (see the section “With caution”).

Elderly patients

No dose adjustment is required for elderly patients.

Childhood and adolescence

The use of the drug in children and adolescents under 18 years of age is contraindicated due to the lack of data on safety and efficacy (see the section “Contraindications”).

Overdose

Symptoms: The most pronounced manifestations of overdose were a marked decrease in blood pressure and tachycardia, and bradycardia, dizziness, increased serum creatinine concentrations, and acute renal failure were also reported.

Treatment: telmisartan is not eliminated by hemodialysis. Patients ‘ condition should be carefully monitored and symptomatic as well as supportive treatment should be provided. The approach to treatment depends on the time elapsed after taking the drug, and the severity of symptoms. Recommended measures include provoking vomiting and / or gastric lavage, and taking activated charcoal is advisable. Electrolyte levels and plasma creatinine levels should be monitored regularly. If there is a marked decrease in blood pressure, the patient should take a horizontal position with raised legs, while it is necessary to quickly replenish the volume of BCC and the content of electrolytes.

Description

Tablets 40 mg: oval, biconvex tablets of white or almost white color.

Tablets 80 mg: capsule-shaped, biconvex tablets of white or almost white color.

Special instructions

Bilateral renal artery stenosis or single kidney artery stenosis.

Impaired liver and/or kidney function (see section “Special instructions”).

Decreased 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 use).

Chronic heart failure (CHF).

Aortic and/or mitral valve stenosis.

Hypertrophic obstructive cardiomyopathy (HOCMP).

Primary hyperaldosteronism (efficacy and safety have not been established).

Use in patients of the black race.

The use of the drug in children and adolescents under 18 years of age is contraindicated due to the lack of data on safety and efficacy.

Impaired renal function

There is limited experience with telmisartan in patients with severe renal insufficiency or patients undergoing hemodialysis.

A lower initial dose of 20 mg per day is recommended for these patients (see section “Special instructions”). No dose adjustment is required for patients with mild to moderate renal impairment.

Concomitant use of Telmista® with aliskiren-containing drugs in patients with diabetes mellitus and/or moderate to severe renal impairment (GFR less than 60 ml/min / 1.73 m2 of body surface area) is contraindicated (see section “Contraindications”).

Concomitant use ofTelmista with ACE inhibitors is contraindicated in patients with diabetic nephropathy (see section “Contraindications”).

Impaired liver function

Telmista® is contraindicated in patients with severe hepatic insufficiency (Child-Pugh Class C) (see section “Contraindications”). In patients with mild to moderate hepatic insufficiency (Child-Pugh class A and B, respectively), Telmista® should be prescribed with caution, the dose should not exceed 40 mg once a day (see the section “With caution”).

Elderly patients

No dose adjustment is required for elderly patients.

Impaired liver function

The use of Telmista® is contraindicated in patients with cholestasis, biliary tract obstruction, or severe hepatic impairment (Child-Pugh Class C) (see section “Contraindications”), since telmisartan is mainly excreted in the bile. It is assumed that the hepatic clearance of telmisartan is reduced in such patients. In patients with mild to moderate hepatic impairment (Child-Pugh Class A and B), Telmista® should be used with caution (see section “With caution”).

Renovascular hypertension

Patients with bilateral renal artery stenosis or stenosis of the artery to a single functioning kidney are at an increased risk of developing severe hypotension and renal failure when treated with drugs acting on the RAAS.

Impaired renal function and kidney transplantation

When using Telmista® in patients with impaired renal function, periodic monitoring of the potassium content and creatinine concentration in blood plasma is recommended. There is no experience of clinical use of telmisartan in patients who have recently undergone kidney transplantation.

BCC reduction

Symptomatic hypotension, especially after the first use of Telmista®, may occur in patients with low BCC and / or plasma sodium levels due to previous treatment with diuretics, restriction of salt intake, diarrhea or vomiting. These conditions (hypovolemia and hyponatremia) should be resolved before starting Telmista.

Double blockade of the RAAS

Concomitant use of telmisartan with drugs containing aliskiren is contraindicated in patients with diabetes mellitus and/or moderate or severe renal insufficiency (GFR less than 60 ml/min / 1.73 m2 of body surface area) and is not recommended in other patients.

Concomitant use of telmisartan and ACE inhibitors is contraindicated in patients with diabetic nephropathy (see section “Contraindications”) and is not recommended in other patients.

As a result of RAAS suppression, hypotension, syncope, hyperkalemia, and impaired renal function (including acute renal failure) were noted in predisposed patients, especially with the simultaneous use of several medications that also affect this system. Therefore, double blockade of RAAS (for example, while taking telmisartan with other RAAS antagonists) is not recommended.

In cases of dependence of vascular tone and renal function mainly on the activity of the RAAS (for example, in patients with CHF or kidney diseases, including renal artery stenosis or stenosis of the artery of a single kidney), the appointment 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 hyperaldosteronism

In patients with primary hyperaldosteronism, treatment with antihypertensive drugs, the effect of which is carried out by inhibiting the RAAS, is usually ineffective. Therefore, the use of Telmista® is not recommended.

Aortic or mitral valve stenosis, HOCMP

As with other vasodilators, special care should be taken in patients with aortic or mitral stenosis, as well as HOCMP, when using Telmista®.

Patients with diabetes mellitus receiving insulin or hypoglycemic agents for oral use

These patients may develop hypoglycemia during treatment with Telmista®. In such patients, glycemic control should be increased, as it may be necessary to adjust the dose of insulin or hypoglycemic agent.

Hyperkalemia

Taking medications that act on the RAAS can cause hyperkalemia. In elderly patients, patients with renal insufficiency or diabetes mellitus, patients also taking medications that increase the content of potassium in the blood plasma, and/or patients with concomitant diseases, hyperkalemia can lead to death.

When deciding on the concomitant use of drugs acting on the RAAS, it is necessary to assess the risk-benefit ratio. The main risk factors for hyperkalemia that should be considered are::

diabetes mellitus, renal failure, age (patients older than 70 years);

concomitant use with one or more medicinal products acting on the RAAS and / or potassium-containing food additives. Medicinal products or therapeutic classes of drugs that can cause hyperkalemia are salt substitutes containing potassium, potassium-sparing diuretics, ACE inhibitors, ARA II, NSAIDs, including selective COX-2 inhibitors, heparin, immunosuppressants (ciclosporin or tacrolimus) and trimethoprim;

intercurrent disease, in particular dehydration, acute cardiac decompensation, metabolic acidosis, impaired renal function, the cytolysis syndrome (e. g. acute limb ischemia, rhabdomyolysis, extensive trauma).

Patients at risk are recommended to carefully monitor the potassium content in the blood plasma (see the section “Interaction with other drugs”).

Ethnic differences

As noted for ACE inhibitors, telmisartan and other APA II drugs appear to be less effective in lowering blood pressure in black patients than in other races, possibly due to a greater predisposition to reduced renin activity in the population of these patients.

Other things

As with other antihypertensive agents, a marked decrease in blood pressure in patients with ischemic cardiomyopathy or CHD can lead to the development of myocardial infarction or stroke.

Special information on excipients

Telmista® is contraindicated in patients with rare hereditary problems of fructose or lactose intolerance, lactase deficiency, or glucose-galactose malabsorption syndrome, as it contains lactose and sorbitol (E 420).

Special clinical studies on the effect of the drug on the ability to drive a car and mechanisms have not been conducted. Caution should be exercised when driving vehicles and working with mechanisms that require increased concentration of attention, as dizziness and drowsiness may rarely occur while taking Telmista®.

Form of production

Tablets,40 mg,80 mg.

7 or 10 tablets in a blister of combined OPA/Al/PVC material and aluminum foil.

2,4,8,12 or 14 blisters (7 tablets each) or 3,6 or 9 blisters (10 tablets each) are placed in a cardboard pack together with the instructions for use.

Storage conditions

At a temperature not exceeding 25 ° C, in the original packaging.

Keep out of reach of children.

Shelf

life is 3 years.

Do not use the drug after the expiration date.

Active ingredient

Telmisartan

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension