Telzap pills 40mg, 90pcs

Composition

Each 40 mg tablet contains: Active ingredient: telmisartan-40,000 mg; excipients: meglumine – 12,000 mg, sorbitol-162,200 mg, sodium hydroxide-3,400 mg, povidone 25-20,000 mg, magnesium stearate-2,400 mg. Each 80 mg tablet contains: Active ingredient: telmisartan-80,000 mg; excipients: meglumine – 24,000 mg, sorbitol-324,400 mg, sodium hydroxide-6,800 mg, povidone 25-40,000 mg, magnesium stearate-4,800 mg

Pharmacological action

Pharmacodynamics Telmisartan is a specific angiotensin II receptor antagonist (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 disease 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 (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 of: cardio – vascular resistance. 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 (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 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. Elimination 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.

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 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. Reduction of mortality and frequency 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. In 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 diseases of the biliary tract;- Severe hepatic impairment (Child-Pugh Class C);- co-use with aliskiren in patients with diabetes mellitus or severe renal impairment (GFR less than 60 ml / min/1.73 m2 of body surface area);- concomImpaired renal function and kidney transplantationwhen 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. Reduction of BCC Symptomatic hypotension, especially after the first use of Telzap, may occur in patients with reduced BCC and / or blood sodium content on 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. 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 have received insulin or oral hypoglycemic agents While receiving Telzap, hypoglycemia may occur in these patients. 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. Medications or therapeutic classes of medications that may cause hyperkalemia include salt substitutes containing potassium, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, NSAIDs (including selective COX – 2 inhibitors), heparin, immunosuppressants (cyclosporine or tacrolimus) and trimethoprim; – intercurrent diseases, especially dehydration, acute heart failure metabolic acidosis, impaired renal function, cytolysis syndrome (for example, 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 be less effective in lowering blood pressure 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 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. Effect on the ability to drive motor vehicles and manage mechanismspecial 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.

Storage conditions

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

Shelf life

2 years

Active ingredient

Telmisartan

Conditions of release from pharmacies

By prescription

Purpose

For adults as directed by your doctor

Indications

Hypertension