Telzap pills 40mg, 30pcs

Composition

	of 1 tab.
telmisartan	40 mg

Auxiliary substances:

meglumine – 12 mg,

sorbitol-162.2 mg,

sodium hydroxide-3.4 mg,

povidone

25-20 mg, magnesium stearate-2.4 mg

Pharmacological action

Pharmacodynamics

Telmisartan is a specific angiotensin II receptor antagonist (ARAP) (ATi type), effective when taken orally. Telmisartan has a very high affinity for AT|-receptors, through which the action of angiotensin II is realized. It displaces angiotensin II from binding to the receptor without having an agonist effect on this receptor. Telmisartan binds only to the angiotensin II AT|T receptor subtype. The connection is stable.

Telmisartan has no affinity for other receptors, including the AT2 receptor 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 appointment of telmisartan, have not been studied. Telmisartan reduces the concentration of aldosterone in the blood plasma, does not reduce the activity of renin and does not block ion channels. Telmisartan does not inhibit the angiotensin-converting enzyme (ACE) (kininase II), which also catalyzes the breakdown of 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 clinically significant up to 48 hours. A pronounced antihypertensive effect usually develops 4-8 weeks after regular use.

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

In the case of abrupt discontinuation of telmisartan, blood pressure gradually returns to its original level within a few days without the development of a “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, 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 endpoint: cardiovascular mortality from heart attack non-fatal myocardial infarction, non-fatal stroke, and hospitalization for chronic heart failure.

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

Suction

When taken orally, telmisartan is rapidly absorbed from the gastrointestinal tract. Bioavailability – 50%. When taken simultaneously with food, the decrease in AUC (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 ingestion, the concentration in the blood plasma is equalized, regardless of whether telmisartan was taken simultaneously with a meal or not. There is a difference in plasma concentrations in men and women. Maxax (maximum concentration) and AUC were approximately 3 and 2 times higher in women compared to men, respectively, with no significant effect on efficacy.

There was no linear relationship between the dose of the drug and its plasma concentration. Cmax and, to a lesser extent, AUC increase disproportionately to the dose increase when using doses above 40 mg per day.

Distribution

Telmisartan binds strongly to plasma proteins (>99.5%), mainly to albumin and alpha-1 acid glycoprotein. The average apparent volume of distribution (Vdss) at steady state is approximately 500 liters.

Metabolism

It is metabolized by conjugation with glucuronic acid. The conjugate has no pharmacological activity.

Deduction

The elimination half-life (T/2) is more than 20 hours. It is excreted through the intestines in unchanged form, excretion by the kidneys-less than 1%. Total plasma clearance is high (about 1000 ml / min) compared to “hepatic” blood flow (about 1500 ml / min).

Indications

-essential hypertension;

– reduction of mortality and frequency of cardiovascular diseases in adult patients with cardiovascular diseases of atherothrombotic origin (CHD, stroke or peripheral artery disease in the anamnesis) and with type 2 diabetes mellitus with damage to target organs.

Contraindications

— obstructive disease of the biliary tract;

severe disturbances of liver function (class C classification for child-Pugh);

— joint use with aliskiren in patients with diabetes or severe impairment of renal function (EGFR less than 60 ml/min/1.73 m 2 of the body surface area);

— concomitant use with ACE inhibitors in patients with diabetic nephropathy;

— hereditary fructose intolerance (due to the presence of sorbitol in the product);

— pregnancy;

— the period of breastfeeding;

— age up to 18 years (efficacy and safety not established);

— hypersensitivity to the Active ingredient or to any auxiliary substances of the drug.

With caution, the drug should be prescribed for bilateral renal artery stenosis or stenosis of the artery of a single functioning kidney; impaired renal function; mild to moderate liver function disorders; BCC reduction against the background of previous diuretic use, restriction of salt intake, diarrhea or vomiting; hyponatremia; hyperkalemia; condition after kidney transplantation (no experience); severe chronic heart failure; aortic and mitral valve stenosis; hypertrophic obstructive cardiomyopathy; primary hyperaldosteronism (efficacy and safety have not been established); patients of the black race.

Side effects

According to WHO, undesirable effects are classified according to their frequency as follows: very common (≥1/10), common (≥1/100 to

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 outcomes.

From the hematopoietic system:  infrequently-anemia; rarely-eosinophilia, thrombocytopenia.

From the immune system:  rarely – anaphylactic reaction, hypersensitivity.

From the side of metabolism:  infrequently-hyperkalemia; rarely-hypoglycemia (in patients with diabetes mellitus).

Mental disorders:  infrequently – insomnia, depression; rarely-anxiety.

Nervous system disorders:  infrequently-fainting; rarely-drowsiness.

From the side of the visual organ:  rarely-visual disorders.

Hearing disorders and labyrinth disorders:  infrequently – vertigo.

From the cardiovascular system:  infrequently-bradycardia, marked decrease in blood pressure, orthostatic hypotension; rarely-tachycardia.

Respiratory system disorders:  infrequently-shortness of breath, cough; very rarely – interstitial lung disease.

From the gastrointestinal tract:  infrequently-abdominal pain, diarrhea, dyspepsia, flatulence, vomiting; rarely-dry mouth, stomach discomfort, impaired taste sensations.

Liver and biliary tract disorders:  rarely-impaired liver function/liver damage.

Skin and subcutaneous tissue disorders:  infrequently-pruritus, hyperhidrosis, rash; rarely-angioedema (also fatal), eczema, erythema, urticaria, drug rash, toxic skin rash.

Musculoskeletal disorders:  infrequently-sciatica, muscle spasms, myalgia; rarely-arthralgia, pain in the extremities, tendinitis-like syndrome.

From the urinary system:  infrequently-impaired renal function, including acute renal failure.

From the side of laboratory and instrumental studies:  infrequently-an increase in the concentration of creatinine in blood plasma; rarely-a decrease in the content of hemoglobin, an increase in the content of uric acid in blood plasma, an increase in the activity of liver enzymes and CPK.

Other services:  infrequently-chest pain, asthenia; rarely-flu-like syndrome.

Interaction

Double blockade of the renin-angiotensin-aldosterone system (RAAS) Concomitant use of telmisartan with aliskiren is contraindicated in patients with diabetes mellitus or renal insufficiency (GFR less than 60 ml / min/1.73 m2 of body surface area) and is not recommended for other patients.

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

The clinical trial data has shown that dual blockade of RAAS due to the combined use of ACE inhibitors, ARAP 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 increase when used together with other medications 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, the combined use of drugs should be carried out with caution and the content of potassium in blood plasma should be regularly monitored.

Digoxin

When telmisartan was co-administered with digoxin, an average increase in plasma digoxin Cmax by 49% and a minimum concentration by 20% was noted. 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 dietary supplements Angiotensin II receptor antagonists, 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 inhibitors and ARAP, including telmisartan, there was a reversible increase in the concentration of lithium in 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.

Nonsteroidal anti-inflammatory drugs (NSAIDs)

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

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 combined 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

The drug is taken orally,1 time/day, regardless of food intake; tablets should be washed down with liquid.

Arterial hypertension

The initial recommended dose of Telzap is 40 mg (1 tablet) 1 time/day. In some patients, taking the drug at a dose of 20 mg/day may be effective. A 20 mg dose can be obtained by dividing a 40 mg tablet in half according to risk. In cases where the therapeutic effect is not achieved, the recommended dose of Telzap can be increased to a maximum of 80 mg 1 time / day.

Alternatively, Telzap can be taken in combination with thiazide diuretics, for example, hydrochlorothiazide, which, when used together, 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 of Telzap is 80 mg 1 time/day. During the initial period of treatment, monitoring of blood pressure levels is recommended, and correction of antihypertensive therapy may be required.

There is limited experience with telmisartan in patients with severe renal insufficiency or patients undergoing hemodialysis. A lower initial dose of 20 mg/day is recommended for these patients. No dose adjustment is required for patients with mild to moderate renal impairment.

Concomitant use of Telzap with aliskiren is contraindicated in patients with renal insufficiency (GFR less than 60 ml / min/1.73 m2 of body surface area).

Concomitant use of Telzap with ACE inhibitors is contraindicated in patients with diabetic nephropathy.

Patients with mild to moderate hepatic insufficiency (Child-Pugh class A and B) the drug should be administered with caution, the dose should not exceed 40 mg 1 time/day. Telzap is contraindicated in patients with severe hepatic insufficiency (Child-Pugh Class C).

No dose adjustment is required in elderly patients.

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

Overdose

Symptoms: the most pronounced manifestations of overdose were a marked decrease in blood pressure and tachycardia, and bradycardia, dizziness, increased serum creatinine, 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. It is necessary to regularly monitor the content of electrolytes and creatinine in the blood plasma. 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 electrolytes.

Special instructions

Impaired liver function

Telzap is contraindicated in patients with cholestasis, biliary tract obstruction, or severe hepatic impairment (Child-Pugh Class C), as telmisartan is primarily excreted in the bile. It is assumed that the hepatic clearance of telmisartan is reduced in such patients. In patients with mild or moderate hepatic impairment (Child-Pugh class A and B), Telzap should be used 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 Telzap in patients with impaired renal function, periodic monitoring of the content of potassium and creatinine in blood plasma is recommended. There is no experience of clinical use of Telzap in patients who have recently undergone kidney transplantation.

BCC reduction

Symptomatic hypotension, especially after the first use of Telzap, may occur in patients with reduced BCC and / or plasma sodium levels during previous treatment with diuretics, restriction of salt intake, diarrhea or vomiting. Such conditions (fluid and/or sodium deficiency) should be eliminated before starting Telzap.

Double blockade of the RAAS

Concomitant use of telmisartan with aliskiren is contraindicated in patients with diabetes mellitus or renal insufficiency (GFR less than 60 ml / min/1.73 m2 of body surface area).

Concomitant use of telmisartan and ACE inhibitors is contraindicated in patients with diabetic nephropathy.

Hypotension, syncope, hyperkalemia, and impaired renal function (including acute renal failure) have been reported as a result of RAAS inhibition in predisposed patients, especially when several medications that also affect this system are used together. 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 chronic heart failure 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. In this regard, the use of Telzap is not recommended.

Aortic and mitral valve stenosis, hypertrophic obstructive cardiomyopathy

As with other vasodilators, patients with aortic or mitral stenosis, as well as hypertrophic obstructive cardiomyopathy, should take special care when using Telzap.

Patients with diabetes mellitus who received insulin or hypoglycemic agents for oral use

Hypoglycemia may occur in these patients during treatment with Telzap. Glycaemic control should be strengthened, as it may be necessary to adjust the dose of insulin or hypoglycaemic agent.

Hyperkalemia

The use of drugs acting on the RAAS may cause hyperkalemia. In elderly patients, patients with renal insufficiency or diabetes mellitus, patients 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);

– combination with one or more drugs acting on the RAAS, and/or potassium-containing dietary supplements. Medicinal products or therapeutic classes of drugs that can cause hyperkalemia are salt substitutes containing potassium, potassium-sparing diuretics, ACE inhibitors, receptor antagonists of angiotensin 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 advised to carefully monitor the potassium content in the blood plasma.

Sorbitol

Telzap contains sorbitol (E420). Patients with rare hereditary problems of fructose intolerance should not take this medicine.

Ethnic differences

As noted for ACE inhibitors, telmisartan and other angiotensin II receptor antagonists appear to reduce blood pressure less effectively in black patients than in other races, possibly due to a greater predisposition to a decrease in renin activity in the population of these patients.

Other things

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

Influence on the ability to drive motor vehicles and manage mechanisms

Special clinical studies on the effect of the drug on the ability to drive a car and mechanisms have not been conducted. When driving a car and working with mechanisms that require increased concentration of attention, care should be taken, because dizziness and drowsiness may rarely occur against the background of the use of Telzap.

Form of production

Coated tablets.

Storage conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C.

Shelf

life is 2 years.

Active ingredient

Telmisartan

Conditions of release from pharmacies

By prescription

Purpose

For adults as directed by your doctor

Indications

Hypertension