TELSARTAN PILLS 40MG

International non-proprietary name

Telmisartan

Dosage Form

Tablets 40 mg, 80 mg

Composition

One pill contains

active substance - telmisartan 40 or 80 mg, respectively,

Excipients: meglumine, sodium hydroxide, povidone (PVP K 30), mannitol, Magnesium stearate, water

Description

Tablets 40 mg - pills from white to grayish-white, capsule-shaped with “T” and “L” engraving and painted on one side and “40” on the other side

Tablets 80 mg - pills from white to grayish-white, capsule-shaped with “T” and “L” engraving and painted on one side and “80” on the other side.

Pharmacotherapeutic group

Drugs that affect the system renin-angiotensin. Angiotensin II antagonists. Telmisartan.

Pharmacological properties

Pharmacokinetics

Telmisartan is rapidly absorbed, the amount absorbed varies. Bioavailability of telmisartan is approximately 50%.

When taking telmisartan 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 administration, plasma concentration levels out, regardless of the meal. A slight decrease in AUC does not reduce the therapeutic effect.

There is a difference in plasma concentrations in men and women. Cmax (maximum concentration) and AUC were approximately 3 and 2 times, respectively, higher in women compared to men without a significant effect on efficacy.

Communication with plasma proteins is more than 99.5%, mainly with albumin and alpha-1 glycoprotein. The volume of distribution is approximately 500 liters.

Telmisartan is metabolized by conjugating the parent substance with the glucuronide. Pharmacological activity of the conjugate was not detected.

Telmisartan has a biexponential pharmacokinetics with a terminal half-life of> 20 hours. Cmax and - to a lesser extent - AUC increase disproportionately with the dose. Clinically significant cumulation of telmisartan was not detected.

After oral administration, Telmisartan is almost completely excreted through the intestine in unchanged form. The total excretion in the urine is less than 2% of the dose.The overall plasma clearance is high (approximately 900 ml / min) compared with the “hepatic” blood flow (approximately 1500 ml / min).

Elderly patients:

The pharmacokinetics of telmisartan in elderly patients does not change.

Patients with renal failure:

Patients with renal failure on hemodialysis have lower plasma concentrations. In individuals with renal insufficiency, telmisartan binds more to plasma proteins and is not eliminated during dialysis. In renal failure, the half-life does not change.

Patients with liver failure:

In patients with hepatic insufficiency, the absolute bioavailability of telmisartan increases to 100%. The half-life for liver failure does not change.

Children

The pharmacokinetics of two administrations of telmisartan were evaluated in patients with hypertension (n = 57) aged 6 to 18 years after taking telmisartan at doses of 1 mg / kg or 2 mg / kg during the four-week treatment period. The results of the study confirmed that the pharmacokinetics of telmisartan in children under the age of 12 years correspond to those in adults and, in particular, the nonlinear nature of Cmax was confirmed.

Pharmacodynamics

Telsartan® is an effective and specific (selective) antagonist of angiotensin II receptors (type AT1) for oral administration. Telmisartan with a very high affinity displaces angiotensin II from its binding sites in the AT1 receptor subtype, which are responsible for the known action of angiotensin II. Telmisartan does not have an agonist action on the AT1 receptor. Telmisartan binds selectively to AT1 receptors. Communication is long lasting. Telmisartan does not show affinity for other receptors, including the AT2 receptor and other less studied AT 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 plasma aldosterone, does not block renin in human plasma and ion channels.

Telmisartan does not inhibit the angiotensin-converting enzyme (kinase II), which destroys bradykinin. Therefore, there is no increase in side effects associated with the action of bradykinin.

In humans, the 80 mg dose of telmisartan almost completely inhibits angiotensin II-induced increase in blood pressure (BP). The inhibitory effect is maintained for more than 24 hours and is determined after 48 hours.

Treatment of essential arterial hypertension

After taking the first dose of telmisartan, blood pressure decreases after 3 hours. The maximum decrease in blood pressure is gradually achieved 4 weeks after the start of treatment and is maintained for long-term treatment.

The hypotensive effect lasts for 24 hours after taking the drug, including 4 hours before taking the next dose, which is confirmed by outpatient blood pressure measurements, as well as stable (above 80%) ratios of the minimum and maximum concentrations of the drug after taking 40 and 80 mg of Telsartan® in controlled clinical trials.

In patients with hypertension, Telsartan® decreases both systolic and diastolic pressure without changing the heart rate.

The antihypertensive effect of telmisartan was compared with representatives of other classes of antihypertensive drugs, such as Amlodipine, Atenolol, Enalapril, hydrochlorothiazide, Losartan, lisinopril, Ramipril and valsartan.

In the case of abrupt cancellation of telmisartan, blood pressure gradually returns to the values ​​before treatment for several days without signs of rapid renewal of arterial hypertension (no ricochet syndrome).

Clinical studies have shown that telmisartan use is associated with a statistically significant decrease in left ventricular mass and left ventricular mass index in patients with arterial hypertension and left ventricular hypertrophy.

Patients with hypertension and diabetic nephropathy treated with Telsartan® have a statistically significant decrease in proteinuria (including microalbuminuria and macroalbuminuria).

In multicenter international clinical studies, it was proved that the cases of dry cough in patients taking telmisartan were significantly lower than in patients treated with angiotensin-converting enzyme inhibitors (ACE inhibitors).

Prevention of cardiovascular morbidity and mortality

In patients 55 years and older with a history of coronary artery disease, stroke, peripheral vascular disease or diabetes mellitus with target organs (retinopathy, left ventricular hypertrophy,macro and microalbuminuria) use of the drug Telsartan® allows to reduce the incidence of myocardial infarction, stroke, hospitalization for congestive heart failure and reduce mortality from cardiovascular diseases.

Children

The antihypertensive effect of telmisartan was evaluated in patients with hypertension aged 6 to 18 years (n = 76) after taking telmisartan at a dose of 1 mg / kg (n = 30 treated) or 2 mg / kg (n = 31 treated) .

The systolic blood pressure (MAP) decreased on average from the initial value by 8.5 mm Hg and 3.6 mm Hg. in the telmisartan groups, 2 mg / kg and 1 mg / kg, respectively. The diastolic blood pressure (DBP) on average decreased from the initial value by 4.5 mm Hg. and 4.8 mm Hg. in the telmisartan groups, 1 mg / kg and 2 mg / kg, respectively.

The changes were dose-dependent.

The safety profile was comparable to that of adult patients.

Indications for use

- treatment of essential arterial hypertension

- prevention (reduction) of cardiovascular morbidity and mortality in patients over 55 years old with a high risk of developing cardiovascular diseases

Dosage and administration

Telmisartan pills are intended for daily oral administration and are taken with liquid, with or without food.

Treatment of essential arterial hypertension

The recommended dose for adults is 40 mg once a day.

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.

If you increase the dose, you should take 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 hypotensive effect.

In patients with severe arterial hypertension, a dose of telmisartan is 160 mg / day (two pills of Telsartan® 80 mg) and in combination with hydrochlorothiazide 12.5-25 mg / day was well tolerated and was effective.

Prevention of cardiovascular morbidity and mortality

The recommended dose is 80 mg once a day.

It is not clear whether doses below 80 mg are effective for reducing cardiovascular morbidity and mortality.

At the initial stage of the use of the drug Telsartan® for the prevention of cardiovascular morbidity and mortality, blood pressure control (BP) is recommended, and it may also be necessary to correct blood pressure with drugs that lower blood pressure.

Telsartan® can be taken regardless of the meal.

Renal failure

Changing the dose in patients with renal insufficiency is not required, including patients on hemodialysis. There is limited experience in treating patients with severe renal failure and hemodialysis. For these 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 and moderate hepatic impairment, the daily dose of the drug should not exceed 40 mg once a day.

Elderly patients:

Dose adjustment is not required.

Side effects

In placebo-controlled trials in patients with arterial hypertension, the total number of side effects reported when taking telmisartan (41.4%) is usually comparable to the number of side effects that occur when taking placebo (43.9%). This number of side effects was not dose-dependent, was not related to gender, age or race of patients.

The safety profile of telmisartan in patients taking the drug for the prevention of cardiovascular diseases and mortality corresponded to the safety profile for patients with arterial hypertension.

The side effects listed below were obtained from controlled clinical trials involving patients with hypertension, as well as post-marketing studies. In addition, serious side effects and side effects were included that resulted in discontinuation of the drug, which was reported in three long-term clinical trials involving 21,642 patients taking telmisartan to prevent cardiovascular morbidity and mortality for six years.

Adverse events are listed below using the following classification: often ≥1 / 100 to <1/10, infrequently ≥1 / 1000 to <1/100, rarely ≥1 / 10,000 to <1/1000, very rarely <10,000.

Infections and invasions:

Infrequently:

- urinary tract infections (including cystitis), upper respiratory tract infections

Seldom:

- sepsis (including fatal cases)

Violations of the circulatory and lymphatic systems:

Infrequently:

- anemia

Seldom: