Telzap pills 80mg, 90pcs

Composition

of 1 tab. – telmisartan 80 mg. Auxiliary substances: meglumine – 24 mg, sorbitol-324.4 mg, sodium hydroxide-6.8 mg, povidone 25-40 mg, magnesium stearate-4.8 mg

Pharmacological action

Antihypertensive, blocking ATII receptors. Pharmacodynamicatelmisartan is a specific angiotensin II receptor antagonist (type AT₁), effective when taken orally. It has a very high affinity for the subtype of AT1receptors, through which the action of angiotensin II is realized. Telmisartan displaces angiotensin II from binding to the receptor, without having an agonist effect on this receptor; it binds only to the AT1 subtype_{of angiotensin II}receptors. Binding is stable. Telmisartan has no affinity for other receptors, including AT₂receptors 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 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 Telmisartan at 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 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 arterial hypertension, telmisartan reduces systolic and diastolic blood pressure without affecting heart rate. 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 diseasesin patients aged 55 years and older with CHD, stroke, transient ischemic attack, peripheral artery disease, or a history of complications of type 2 diabetes mellitus (e. g., 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 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 and adolescents The safety and efficacy of telmisartan in children and adolescents under 18 years of age have not been established. Pharmacokinetics of absorption When taken orally, telmisartan is rapidly absorbed from the gastrointestinal tract. Bioavailability – 50%. When taken simultaneously with food, the decrease in AUC ranges from 6% (when taken at a dose of 40 mg) to 19% (when taken 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 food or not. There is a difference in plasma concentrations of telmisartan in men and women. C_max 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 used at doses above 40 mg / day. Distribution Telmisartan binds strongly to plasma proteins (>99.5%), mainly albumin and alpha-1 acid glycoprotein. The average apparent volume of distribution (_vdss) at steady state is approximately 500 liters. Metabolismmetabolized by conjugation with glucuronic acid. The conjugate has no pharmacological activity. Excretionet_1/2 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). Pharmacokinetics in special patient groupsthe pharmacokinetics of telmisartan in elderly patients over 65 years of age do not differ from young patients. No dose adjustment is required. No dose adjustment of telmisartan is required in patients with mild to moderate renal impairment. A lower initial dose of 20 mg / day is recommended for patients with severe renal insufficiency and patients undergoing hemodialysis. Telmisartan is not eliminated by hemodialysis. 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.

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.

Use during pregnancy and lactation

Currently, there is no reliable information on the safety of using telmisartan in pregnant women. In animal studies, reproductive toxicity of the drug was revealed. The use of Telzap® is contraindicated during pregnancy. If long-term treatment with Telzap® is necessary, patients planning pregnancy should choose an alternative antihypertensive drug with a proven safety profile for use during pregnancy. Once pregnancy is established, treatment with Telzap® should be stopped immediately and alternative treatment should be initiated if necessary. The results of clinical observations showed that the use of angiotensin II receptor antagonists in the second and third trimesters of pregnancy has a toxic effect on the fetus (deterioration of renal function, oligohydramnios, delayed ossification of the skull) and the newborn (renal failure, hypotension and hyperkalemia). When using angiotensin II receptor antagonists in the second trimester of pregnancy, ultrasound of the fetal kidneys and skull is recommended. Children whose mothers have taken angiotensin II receptor antagonists during pregnancy should be carefully monitored for hypotension. Information on the use of telmisartan during breastfeeding is not available. The use of Telzap® during breastfeeding is contraindicated. An alternative antihypertensive drug with a more favorable safety profile should be used, especially when feeding a newborn or premature baby.

Recommendations for use

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

Arterial hypertension

Initial recommended dose of Telzap® it is 40 mg (1 tab. ) 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 once a 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 m% ^%2 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.

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, adverse events are classified according to their frequency as follows: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1000 to <1/100), rare (≥1/10,000 to <1/1000), 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 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 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.

Data from clinical studies have shown that double blockade of the RAAS due to the combined use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren is associated with an increased frequency of adverse events, such as hypotension, hyperkalemia and impaired renal function (including acute renal failure), compared with the use of only one drug acting on the RAAS.

Hyperkalemia

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), NSAIDs (including selective COX-2 inhibitors), heparin, immunosuppressants (ciclosporin 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, there was an average increase in C_max of digoxin in blood plasma by 49% and C_min 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 dietary supplements

Angiotensin II receptor antagonists, such as telmisartan, reduce diuretic-induced potassium loss. Potassium-sparing diuretics (such as spironolactone, eplerenone, triamterene, or amiloride), potassium-containing dietary supplements, or salt substitutes may cause a significant increase in blood potassium levels. 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 angiotensin II receptor antagonists, 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 the doses used for anti-inflammatory treatment, COX-2 inhibitors, and non-selective NSAIDs) may weaken the antihypertensive effect of angiotensin II receptor antagonists. In some patients with impaired renal function (for example, patients with dehydration, elderly patients with impaired renal function), the combined use of angiotensin II receptor antagonists 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, 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 the use of ethanol, barbiturates, narcotic drugs or antidepressants.

Corticosteroids (for systemic use)

Corticosteroids weaken the effect of telmisartan.

Overdose

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

Treatment: 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 blood pressure is too low, the patient should take a horizontal position with raised legs, while it is necessary to quickly fill up the BCC and lack of electrolytes.Telmisartan is not eliminated by hemodialysis.

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 a low BCC and / or blood sodium content against the background of 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. Therefore, the use of Telzap®is not recommended.

Aortic and mitral valve stenosis, hypertrophic obstructive cardiomyopathy

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

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

Hypoglycaemia 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. Caution should be exercised when driving a car or working with mechanisms that require increased concentration of attention, as dizziness and drowsiness may rarely occur when using Telzap®.

Form of production

Tablets are almost white to yellowish in color, oblong, biconvex, with the inscription “80” on one side.

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

Active ingredient

Telmisartan

Conditions of release from pharmacies

By prescription

Purpose

For adults as directed by your doctor

Indications

Hypertension