Telsartan pills 80mg, 30pcs

Composition

1 tablet of 80 mg contains: Active ingredient: Telmisartan 80.00 mgsupport Substances: Meglumine 24.00 mg Sodium Hydroxide 6.70 mg Povidone-K 30 24.00 Mgpolysorbate-80 3.00 mg Mannitol 432.10 mg Magnesium stearate 10.20 mg

Pharmacological action

Pharmacodynamicatelmisartan is a specific angiotensin II (ARA) receptor antagonist, 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 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. Reduces the concentration of aldosterone in the blood, does not inhibit renin in the blood plasma and does not block ion channels. Telmisartan does not inhibit the angiotensin-converting enzyme (kininase II), which also destroys bradykinin. Therefore, an increase in the side effects caused by bradykinin is not expected. In patients with arterial 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 oral 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 4 weeks after regular use of the drug. In patients with 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. Pharmacokinetics of absorption When taken orally, it is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 50%. When taken simultaneously with food, the area under the concentration-time pharmacokinetic curve (AUC) varies 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 food intake. Distribution due to plasma proteins – 99.5% (mainly with albumin and alpha-1 glycoprotein). The average apparent volume of distribution at equilibrium concentration is 500 liters. Metabolismmetabolized by conjugation with glucuronic acid. The metabolites are pharmacologically inactive. Elimination Half-life (T1 / 2) – more than 20 hours. It is excreted through the intestines in unchanged form, excretion 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 special patient groups Gender differencesdifference in plasma concentrations of telmisartan in men and women is observed. The maximum plasma concentration (Cmax) is approximately 3-fold and the AUC is approximately 2-fold higher in women compared to men with no significant effect on efficacy. No dose adjustment is required. Elderly patientsthe pharmacokinetics of telmisartan in elderly patients do not differ from the pharmacokinetics in young patients. No dose adjustment is required. Patients with impaired renal function In patients with mild to moderate renal impairment, no dose adjustment of telmisartan is required. 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. Patients with hepatic impairment pharmacokinetic studies in patients with hepatic insufficiency have shown an increase in the absolute bioavailability of telmisartan to almost 100%. With hepatic insufficiency, T 1/2 does not change. 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

• Arterial hypertension.

• Reduction of cardiovascular morbidity and mortality in patients aged 55 years and older with a high risk of cardiovascular diseases.

Use during pregnancy and lactation

Pregnancy Drugs that directly affect the RAAS can cause serious damage and death to the developing fetus, so when planning or establishing the fact of pregnancy, the drug should be immediately discontinued and, if necessary, an alternative antihypertensive therapy should be prescribed that has an established safety profile for use during pregnancy. The use of the drug during pregnancy is contraindicated. In preclinical studies of telmisartan, no teratogenic effects were detected, but fetotoxicity was established. It is known that exposure to angiotensin II receptor antagonists during the second and third trimesters of pregnancy causes fetotoxicity in humans (decreased renal function, oligohydramnios, slowing of cranial ossification), as well as neonatal toxicity (renal failure, hypotension, hyperkalemia). Patients planning pregnancy should be prescribed alternative therapy. If treatment with angiotensin II receptor antagonists occurred during the second trimester of pregnancy, ultrasound examination of the fetal kidney function and cranial condition is recommended. Newborns whose mothers have received angiotensin II receptor antagonists should be carefully monitored for hypotension. Breast-feeding is contraindicated during telmisartan therapy. Fertility Studies of the effect on human fertility have not been conducted.

Recommendations for use

Telmisartan tablets are intended for daily oral use and are taken with liquid, with or without food. Treatment of essential hypertension: The recommended adult dose is 40 mg once daily. In cases where the desired blood pressure is not achieved, the dose of Telsartan can be increased to a maximum of 80 mg once a day. When increasing the dose, it should be taken into account that the maximum antihypertensive effect is usually achieved within four to eight weeks after the start of treatment. Telsartan can be used in combination with thiazide diuretics, for example, hydrochlorothiazide, which in combination with telmisartan has an additional antihypertensive effect. In patients with severe hypertension, the dose of telmisartan 160 mg / day (two tablets of Telsartan 80 mg) and in combination with hydrochlorothiazide 12.5-25 mg/day was well tolerated and effective. Prevention of cardiovascular morbidity and mortality: The recommended dose is 80 mg once daily. It is not clear whether doses below 80 mg are effective in reducing cardiovascular morbidity and mortality. At the initial stage of using Telsartan® for the prevention of cardiovascular morbidity and mortality, it is recommended to monitor blood pressure( BP), and it may also be necessary to correct blood pressure with drugs that reduce blood pressure. Telsartan can be taken regardless of food intake. Renal insufficiency: No dose adjustment is required in patients with renal insufficiency, including patients on hemodialysis. There is limited experience in treating patients with severe renal insufficiency and hemodialysis. For such patients, it is recommended to start with a lower dose of 20 mg. Telsartan is not removed from the blood during hemofiltration. Liver failure: In patients with mild to moderate hepatic impairment, the daily dose of the drug should not exceed 40 mg once a day. Elderly patients: No dose adjustment is required.

Contraindications

• Hypersensitivity to the Active ingredient or auxiliary components of the drug.

• Pregnancy and 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 angiotensin converting enzyme inhibitors in patients with diabetic nephropathy.

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

With caution:

• Bilateral renal artery stenosis or stenosis of the artery of a single kidney (see the section “Special instructions”).

• Mild to moderate hepatic and/or renal impairment (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.

• Aortic and mitral valve stenosis.

• Idiopathic hypertrophic subaortic stenosis (hypertrophic obstructive cardiomyopathy).

• Primary hyperaldosteronism.

Side effects

Overall, the incidence of adverse reactions reported for telmisartan is comparable to that reported for placebo. The observed cases of side effects did not correlate with the gender, age, or race of the patients. Classification of the frequency of adverse reactions of the World Health Organization( WHO): very common (>1/10); common (>>1/100 to >><1/10); infrequent (>1/1000 to <1/10); infrequent (><1/100); rare (>1/10 000 to <1/100); rare (><1/1000); very rare (from Infectious and parasitic diseases Often-upper respiratory tract infections, including pharyngitis and sinusitis, urinary tract infections (including cystitis); frequency unknown – sepsis, including sepsis with fatal outcome. Blood and lymphatic system disorders: often-anemia; rarely-thrombocytopenia; frequency unknown-eosinophilia. Mental disorders: often – depression; rarely-anxiety. Nervous system disorders: often – insomnia, syncope, vertigo; rarely-syncope. Visual disturbances are sometimes referred to as visual disturbances. Disorders of the heart are frequent-bradycardia; rarely-tachycardia. Vasoconstriction disorders frequently – marked decrease in blood pressure*, orthostatic hypotension; * – often observed in patients with controlled blood pressure who were treated with telmisartan to reduce the risk of cardiovascular mortality in addition to standard treatment. Respiratory, thoracic, and mediastinal disorders often – shortness of breath, cough. Gastrointestinal disorders: Often – abdominal pain, diarrhea, dyspepsia, flatulence, vomiting; rarely-upset stomach, discomfort, dry oral mucosa, liver function disorders/liver diseases. Immune system disorders Rarely – hypersensitivity, angioedema (including fatal ones); frequency unknown – anaphylactic reactions. Skin and subcutaneous tissue disorders Often – hyperhidrosis, pruritus, rash; rarely-erythema, drug rash, toxic skin rash, eczema, frequency unknown-urticaria. Musculoskeletal and connective tissue disorders: myalgia, back pain (for example, sciatica), muscle spasms; rarely-arthralgia, pain in the extremities; frequency unknown-pain in the tendon area (tendinitis-like symptoms). Renal and urinary tract disorders: Frequent renal failure, including acute renal failure. Metabolic and nutritional disorders often include hyperkalemia. Common disorders: often-chest pain, asthenia (weakness); rarely-flu-like condition. Laboratory and instrumental dataonce – increasing the concentration of creatinine in the blood; rarely-increased concentration of uric acid in the blood, “liver” enzymes, serum creatine phosphokinase activity, decreased hemoglobin, hypoglycemia (in patients with diabetes mellitus).

Interaction

Telsartan may increase the antihypertensive effect of other antihypertensive agents. No other clinically significant interactions were identified. Co-use of telmisartan with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin, and amlodipine did not result in a clinically significant interaction. When used concomitantly with digoxin, an increase in the average minimum concentration of digoxin in blood plasma was observed by 20% (in a single case by 39%), so it is necessary to monitor the level of digoxin in blood plasma. With simultaneous use of telmisartan and ramipril, an increase in AUC0-24 and Cmax of ramipril and ramiprilat by 2.5 times was observed. The clinical significance of this phenomenon has not been established. Reversible increases in serum lithium concentrations and toxicity have been reported when lithium is co-administered with angiotensin II receptor antagonists, including telmisartan. In this case, it is recommended to monitor the level of lithium in the blood plasma, and patients should be under strict medical supervision. Concomitant treatment with non-steroidal anti-inflammatory drugs (NSAIDs), including acetylsalicylic acid, cyclooxygenase-2 [COX-2] inhibitors, and non-selective NSAIDs, is associated with the risk of acute renal failure in patients with dehydration. Drugs acting on the renin-angiotensin system may have a synergistic effect. Patients receiving concomitant NSAIDs and telmisartan should be adequately compensated for water loss and renal function monitored at the beginning of treatment. Some reduction in the antihypertensive effect of telmisartan has been reported when co-administered with NSAIDs. Concomitant treatment of telmisartan with corticosteroids reduces the antihypertensive effect

How to take, course of use and dosage

Inside, regardless of food intake, washed down with water. Arterial hypertension The initial recommended dose of Telsartan® is 1 tablet 40 mg once daily. For some patients, a dose of 20 mg per day (1/2 tablet of 40 mg) may be effective. In cases where the therapeutic effect is not achieved, the maximum recommended dose of Telsartan® can be increased to 80 mg (1 tablet of 80 mg or 2 tablets of 40 mg) once a day. When deciding whether to increase the dose, it should be taken into account that the maximum antihypertensive effect is usually achieved within 4-8 weeks after the start of treatment. Reduction of cardiovascular morbidity and mortality The recommended dose of Telsartan® is 1 tablet 80 mg once daily. In the initial period of treatment, additional blood pressure correction may be required. Renal impairment There is limited experience with the use of telmisartan in patients with severe renal impairment or on hemodialysis. Such patients require a low initial dose of 20 mg. No dose adjustment is required in patients with mild to moderate renal impairment. Hepatic impairment In patients with mild to moderate hepatic impairment, the daily dose of Telsartan® should not exceed 40 mg. Use in severe hepatic impairment is contraindicated (see section “Contraindications”). Elderly patients The dosage regimen does not require changes.

Overdose

Data on overdose in humans are very limited. Symptoms: the most likely signs of overdose may be hypotension and tachycardia, the development of bradycardia is also not excluded. Treatment: The recommended treatment is symptomatic. Telmisartan is not removed from the blood by hemodialysis.

Special instructions

Impaired liver function The use of telmisartan is contraindicated in patients with cholestasis, biliary tract obstruction, or severe hepatic impairment (Child-Pugh Class C), as telmisartan is primarily excreted in bile. In such patients, a decrease in drug excretion is expected. Telmisartan should be used with caution in patients with mild to moderate hepatic impairment (Child-Pugh Class A or B). Vasorenal arterial hypertension Patients with bilateral renal artery stenosis or stenosis of a single functioning kidney have an increased risk of developing severe hypotension and renal failure when using drugs that affect the RAAS. Impaired renal function When using telmisartan in patients with renal insufficiency, it is recommended to monitor the serum potassium content and creatinine concentration. Experience of use after a recent kidney transplant is not described. Hypovolemia Patients with hypovolemia and/or hyponatremia due to intensive diuretic therapy, salt restriction, diarrhea or vomiting may develop symptomatic hypotension, especially after taking the first dose of telmisartan. Before starting therapy, violations of the water-electrolyte balance should be corrected. Double blockade of the RAAS Simultaneous use of ACE inhibitors, ARA II or aliskiren increases the risk of hypotension, hyperkalemia and impaired renal function (including acute renal failure), so the use of a combination of these drugs is considered a double blockade of the RAAS. Concomitant use of ARA II 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 m%^%2 of body surface area) and is not recommended in other patients. If absolutely necessary, therapy with double blockade of the RAAS should be carried out under strict medical supervision and careful monitoring of renal function, electrolytes and blood pressure. Other conditions associated with RAAS activation patients whose vascular tone and renal function are determined by RAAS activity (patients with chronic heart failure or kidney diseases, including stenosis of two renal arteries or stenosis of the artery of a single kidney), the use of drugs that affect RAAS may be accompanied by the development of arterial hypotension, hyperazotemia, oliguria and, in rare cases, acute renal failure. Primary hyperaldosteronismpatients with primary hyperaldosteronism are resistant to antihypertensive drugs that affect the RAAS, so the use of telmisartan is not recommended for such patients. Aortic and/or mitral valve stenosis, hypertrophic obstructive cardiomyopathy (HOCMP)Telmisartan should be used with caution in patients with hemodynamically significant aortic and/or mitral valve stenosis or with HOCMP. Patients with diabetes mellitus receiving insulin or hypoglycemic agents for internal use When using telmisartan, such patients may develop hypoglycemia.It is recommended to regularly monitor the concentration of blood glucose and, if necessary, adjust the dose of hypoglycemic agents. Hyperkalemia The use of drugs that affect the RAAS may cause hyperkalemia. Before concomitant use of such drugs, the benefit/risk ratio should be evaluated. Risk factors for hyperkalemia:- kidney failure, age over 70 years, diabetes mellitus;- concomitant use of drugs that affect the RAAS (ACE inhibitors, ARA II) and/or potassium-sparing diuretics (spironolactone, eplerenone, triamterene, amiloride), potassium preparations or potassium – containing salt substitutes, NSAIDs (including COX-2 selective ones), heparin, immunosuppressive drugs (cyclosporine or tacrolimus), as well as trimethoprim; – concomitant conditions, such as dehydration, acute decompensated heart failure, metabolic acidosis, impaired renal function, sudden progression of kidney disease (infectious diseases), conditions accompanied by tissue necrosis (acute limb ischemia, rhabdomyolysis, extensive trauma). Patients at risk should be carefully monitored for serum potassium concentrations. Ethical Specificities ACE and ARA II inhibitors (including telmisartan) may have a less pronounced antihypertensive effect in black patients. This may be due to a decrease in the level of renin in arterial hypertension in such patients compared to representatives of other races. As with any antihypertensive treatment, excessive lowering of blood pressure in patients with CHD or ischemic cardiomyopathy can lead to myocardial infarction or stroke. No specific clinical studies have been conducted to assess the effect of the drug on the ability to drive a car and mechanisms. However, when driving vehicles and engaging in dangerous activities, the possibility of dizziness and drowsiness should be taken into account, which requires caution.

Storage conditions

At a temperature not exceeding 25 °C. Keep out of reach of children!

Shelf life

2 years

Active ingredient

Telmisartan

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension