Telzap pills 40mg №90

pharmachologic effect

Antihypertensive drug.

Pharmacodynamics

Telmisartan is a specific angiotensin II receptor antagonist (type AT₁), effective when taken orally. Possesses very high affinity for the AT subtype₁-receptors through which the action of angiotensin II is realized. Telmisartan displaces angiotensin II from its association with the receptor, not having the action of an agonist on this receptor; binds only to the AT subtype₁receptor angiotensin II. Binding is sustainable. Telmisartan has no affinity for other receptors, incl. to AT₂-receptors and other less studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible over-stimulation with angiotensin II, the concentration of which increases with the administration of telmisartan, has not been studied. Telmisartan reduces the concentration of aldosterone in the blood plasma, does not reduce the activity of renin and does not block the ion channels. Telmisartan does not inhibit ACE (kininase II), which also catalyzes the destruction of bradykinin. This avoids the side effects associated with the action of bradykinin (for example, dry cough).

Essential hypertension

Telmisartan in a dose of 80 mg completely blocks the hypertensive effect of angiotensin II.The onset of the antihypertensive effect is noted within 3 hours after the first dose of telmisartan. The effect of the drug lasts 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 cessation of taking telmisartan, blood pressure over several days gradually returns to its original level without developing withdrawal syndrome.

As shown by the results of comparative clinical studies, the antihypertensive effect of telmisartan is comparable to the antihypertensive effect of drugs of other classes (amlodipine, Atenolol, Enalapril, hydrochlorothiazide, and lisinopril).

The incidence of dry cough was significantly lower during the use of telmisartan, in contrast to ACE inhibitors.

Prevention of cardiovascular diseases

In patients aged 55 and older with coronary artery disease, stroke, transient ischemic attack, peripheral artery disease, or complications of type 2 diabetes (for example, retinopathy, left ventricular hypertrophy, macro- or microalbuminuria) with a history of cardiovascular disease. events, telmisartan had a ramipril-like effect on reducing the combined endpoint: cardiovascular mortality from myocardial infarction without fataloutcome, stroke without death and hospitalization due to chronic heart failure.

Telmisartan was as effective as 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 described with telmisartan as opposed to ramipril, while hypotension occurred more frequently with telmisartan.

Patients of childhood and adolescence

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

Suction

When ingested 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 administration, the plasma concentration levels out, regardless of whether telmisartan was taken simultaneously with food or not. There was no linear relationship between the dose of the drug and its plasma concentration. C_max and, to a lesser extent, AUCs increase disproportionately with increasing doses when used in doses above 40 mg / day.

Distribution

Telmisartan binds strongly to plasma proteins (> 99.5%), mainly albumin and alpha-1 acid glycoprotein. Average apparent volume of distribution (V_dss) in the equilibrium state is approximately 500 l.

Metabolism

Metabolized by conjugation with glucuronic acid. Conjugate does not possess pharmacological activity.

Removal

T_1/2 is more than 20 hours. Excreted through the intestine in unchanged form, the excretion by the kidneys - less than 1%. Total plasma clearance is high (about 1000 ml / min) compared with hepatic blood flow (about 1500 ml / min).

Pharmacokinetics in Special Patient Groups

There is a difference in the plasma concentrations of telmisartan in men and women. WITH_max and AUC were approximately 3 and 2 times, respectively, higher in women compared to men without significant effect on efficacy.

The pharmacokinetics of telmisartan in elderly patients over 65 years of age does not differ from younger patients. Dose adjustment is not required.

In patients with mild and moderate renal impairment, a dose adjustment of telmisartan is not required. For patients with severe renal insufficiency and patients on hemodialysis, a lower initial dose of 20 mg / day is recommended. Telmisartan is not excreted by hemodialysis.

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

- essential hypertension;

- reduction of mortality and frequency of cardiovascular diseases in adult patients with cardiovascular diseases of atherothrombotic genesis (coronary artery disease, stroke or peripheral arterial disease in history) and diabetes mellitus type 2 with target organ damage.

The drug is taken orally, 1 time / day, regardless of the meal; pills should be washed down with liquid.

Arterial hypertension

Initial recommended dose of Telzap^® makes 40 mg (1 tab.) 1 time / day. In some patients, it may be effective to take the drug at a dose of 20 mg / day. A dose of 20 mg can be obtained by dividing a 40 mg pill in half over the risk. In cases where the therapeutic effect is not achieved, the recommended dose of Telzap^® may 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 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 cardiovascular disease

The recommended dose of Telzap^® - 80 mg 1 time / day. In the initial period of treatment, monitoring of the level of blood pressure is recommended; correction of antihypertensive therapy may be required.

Experience with telmisartan patients with severe renal failure or hemodialysis patientslimited These patients recommended a lower initial dose of 20 mg / day. For patients with mild to moderate renal dysfunction dose adjustment is not required.

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

The simultaneous use of the drug Telzap^® ACE inhibitors are contraindicated in patients with diabetic nephropathy.

Patients with mild and moderate hepatic insufficiency (class A and B according to Child-Pugh classification) the drug should be prescribed with caution, the dose should not exceed 40 mg 1 time / day. Drug Telzap^® contraindicated patients with severe liver failure (Child-Pugh class C).

Have elderly patients no dose adjustment required.

Use of the drug Telzap^® at children and adolescents under the age of 18 contraindicated due to lack of safety and efficacy data.

According to the WHO, undesirable effects are classified according to the frequency of their development as follows: very often (≥1 / 10), often (from ≥1 / 100 to <1/10), infrequently (from ≥1 / 1000 to <1/100 ), rarely (from ≥1 / 10 000 to <1/1000), very rarely (<1/10 000); frequency is unknown - according to the available data it was not possible to establish the frequency of occurrence.

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

Infectious and parasitic diseases: infrequently, urinary tract infections, including cystitis, upper respiratory tract infections, including pharyngitis and sinusitis; rarely - sepsis, incl. with a fatal outcome.

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

On the part of the immune system: rarely - an anaphylactic reaction, hypersensitivity.

Metabolism: infrequently - hyperkalemia; rarely - hypoglycemia (in patients with diabetes).

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

From the nervous system: infrequently - fainting; rarely - drowsiness.

On the part of the organ of vision: rarely - visual disturbances.

On the part of the organ of hearing and labyrinth disorders: infrequently - vertigo.

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

On the part of the respiratory system: infrequently - shortness of breath, cough; very rarely - interstitial lung disease.

From the digestive tract: infrequently - abdominal pain, diarrhea, dyspepsia, flatulence, vomiting; rarely - dry mouth, discomfort in the stomach, a violation of taste.

Liver and biliary tract: rarely, liver dysfunction / liver damage.

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

From the musculoskeletal system: infrequently - sciatica, muscle spasms, myalgia; rarely - arthralgia, pain in the extremities, tendente-like syndrome.

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

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

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

- obstructive diseases of the biliary tract;

- severe liver dysfunction (Child-Pugh class C);

- combined use with aliskiren in patients with diabetes mellitus or severe renal dysfunction (GFR less than 60 ml / min / 1.73 m² surface area of ​​the body);

- simultaneous use with ACE inhibitors in patients with diabetic nephropathy;

- hereditary intolerance to fructose (due to the presence of sorbitol in the composition of the drug);

- pregnancy;

- breastfeeding period;

- age up to 18 years (efficacy and safety have not been established);

- hypersensitivity to the active substance or any excipients of the drug.

WITH caution the drug should be administered in case of bilateral stenosis of the renal arteries or stenosis of the artery of the only functioning kidney; renal dysfunction; mild and moderate liver dysfunction; lower bcc on the background of previous diuretic intake, restriction of salt, diarrhea or vomiting; hyponatremia; hyperkalemia; condition afterkidney transplantation (no experience); severe chronic heart failure; stenosis of the aortic and mitral valve; hypertrophic obstructive cardiomyopathy; primary hyperaldosteronism (efficacy and safety have not been established); Negroid patients.

Currently, there is no reliable information about the safety of telmisartan in pregnant women. In animal studies revealed reproductive toxicity of the drug. Use of the drug Telzap^® contraindicated during pregnancy.

If necessary, long-term treatment with Telzap^® Patients planning pregnancy should choose an alternative antihypertensive drug with a proven safety profile during pregnancy. After establishing the fact of pregnancy with Telzap^® should stop immediately and, if necessary, start alternative treatment.

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 of the newborn (renal failure, arterial hypotension and hyperkalemia). When using angiotensin II receptor antagonists in the second trimester of pregnancy, an ultrasound scan of the kidney and fetal skull is recommended.Children whose mothers took angiotensin II receptor antagonists during pregnancy should be carefully monitored to detect hypotension.

Information on the use of telmisartan during breastfeeding is not available. Use of the drug 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.

Contraindicated use of the drug for obstructive diseases of the biliary tract; severe liver dysfunction (Child-Pugh class C).

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