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pharmachologic effect

Telzap® Plus is a combination of telmisartan (angiotensin II receptor antagonist (APA II)) and hydrochlorothiazide (thiazide diuretic). The combination of these components provides a more pronounced antihypertensive effect, while the level of blood pressure decreases more than against the background of monotherapy with these components.

The drug, used 1 time / day in therapeutic doses, effectively and gradually reduces blood pressure.

Telmisartan

Telmisartan is a specific angiotensin II receptor antagonist (subtype AT1), effective when taken orally. Telmisartan has a high affinity for the AT subtype1-receptors of angiotensin II, through which the action of angiotensin II is realized. Telmisartan displaces angiotensin II from binding to the receptor, not showing the properties of an AT agonist1-receptor. Telmisartan selectively and firmly associated with AT1-receptor Telmisartan does not have affinity for other receptors, including AT2 and other less studied at-receptors. The functional role of these receptors, as well as the effect of their possible increased stimulation with angiotensin II, the concentration of which increases under the action of telmisartan, has not been studied. Telmisartan reduces the concentration of aldosterone in the blood plasma, does not inhibit renin and does not block ion channels. Telmisartan does not inhibit ACE (Kininase II), which also destroys bradykinin. This avoids the side effects associated with the action of bradykinin.

In healthy people, telmisartan at a dose of 80 mg almost completely blocks the hypertensive effect of angiotensin II. The overwhelming effect lasts more than 24 hours and lasts up to 48 hours.

The onset of the antihypertensive effect is observed within the first 3 hours after ingestion of telmisartan inside. The duration of the therapeutic effect of the drug is more than 24 hours and includes the last 4 hours before taking the next dose according to the daily monitoring of blood pressure. This is confirmed by measurements made at the time of maximum effect and immediately before taking the next dose (the ratio of the residual effect to the maximum above 80% for dosages of 40 and 80 mg of telmisartan in placebo-controlled studies).The maximum antihypertensive effect develops after 4-8 weeks of regular intake of telmisartan and persists during long-term therapy.

In patients with arterial hypertension, telmisartan reduces both systolic and diastolic pressure without affecting heart rate. According to the results of clinical studies, the effectiveness of the antihypertensive effect of telmisartan is comparable to the therapeutic effect of other classes of drugs, such as Amlodipine, Atenolol, Enalapril, hydrochlorothiazide, and lisinopril. In the case of abrupt cessation of treatment with telmisartan, the blood pressure gradually returns to baseline, without the development of the "withdrawal" syndrome.

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

Hydrochlorothiazide

Hydrochlorothiazide is a thiazide diuretic. Thiazides affect the reabsorption of electrolytes in the renal tubules, thereby increasing the excretion of sodium ions and chlorides in approximately equivalent amounts. The diuretic effect of hydrochlorothiazide leads to a decrease in BCC, an increase in plasma renin activity, an increase in aldosterone production, followed by an increase in potassium and bicarbonate levels in the urine and a decrease in the potassium content in blood plasma. The simultaneous use of telmisartan helps to reduce the loss of potassium caused by this diuretic, probably due to the blockade of the RAAS. After taking hydrochlorothiazide diuresis increases after 2 hours, the maximum effect develops after about 4 hours, the effect lasts about 6-12 hours.

In epidemiological studies, it has been established that prolonged therapy with hydrochlorothiazide reduces the risk of cardiovascular morbidity and mortality.

Patients of childhood and adolescence

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

Pharmacokinetics

In healthy people, the simultaneous use of hydrochlorothiazide and telmisartan does not affect the pharmacokinetics of each of the components of the drug.

Telmisartan

Suction

After oral administration, Telmisartan is rapidly absorbed. WITHmax telmisartan after ingestion is achieved in 0.5-1.5 h. The absolute bioavailability when taking 40 and 160 mg is 42% and 58%, respectively.Meal slightly reduces the bioavailability of telmisartan, a decrease in the AUC value ranges from 6% (dose 40 mg) to 19% (dose 160 mg). After 3 hours after administration, the plasma concentration levels out regardless of whether the drug was taken with food or on an empty stomach. A slight decrease in AUC does not cause a decrease in the therapeutic efficacy of the drug.

The pharmacokinetics of telmisartan after oral administration is not linear. After repeated use, there was no significant accumulation of telmisartan in the blood plasma.

Distribution

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

Metabolism

Telmisartan metabolism occurs by conjugation with glucuronic acid and the formation of a pharmacologically inactive metabolite acylglucuronide. After a single dose of telmisartan, labeled14C, acylglucuronide made up approximately 11% of the total amount of radioactive substance in the blood plasma. The cytochrome P450 isoenzymes do not participate in the metabolism of telmisartan.

Removal

After ingestion or in / in the introduction14C-tagged telmisartan most of the dose (> 97%) is excreted through the intestine with bile; a small amount of the substance is excreted by the kidneys (less than 2%). The total plasma clearance of telmisartan after oral administration is> 1500 ml / min. T1/2 telmisartan is more than 20 h.

Pharmacokinetics in Special Patient Groups

Plasma concentration of telmisartan in women is 2-3 times higher than in men, while in women there is no increase in the antihypertensive effect. There is no need for dose adjustment.

The pharmacokinetics of telmisartan in elderly patients (over 70 years old) is not different from younger patients.

Excretion of telmisartan occurs with little or no kidney involvement (less than 2%). Given the experience of using the drug for the treatment of patients with mild to moderate renal insufficiency (CK 30-60 ml / min, on average - about 50 ml / min), there is no need for dose adjustment in patients with impaired renal function. Telmisartan is not displayed during hemodialysis.

Pharmacokinetic studies in patients with impaired liver function showed an increase in absolute bioavailability up to 100%.In patients with hepatic insufficiency T1/2 did not change.

Hydrochlorothiazide

Suction

After ingestion Cmax Hydrochlorothiazide in plasma is reached after approximately 1–3 hours. With cumulative renal excretion of hydrochlorothiazide, the absolute bioavailability is about 60%.

Distribution

About 68% of hydrochlorothiazide binds to plasma proteins, its Vdssis 0.83-1.14 l / kg.

Metabolism and excretion

Hydrochlorothiazide is not metabolized in humans.

Hydrochlorothiazide is excreted almost completely unchanged in the urine. About 60% of the dose taken orally is excreted unchanged within 48 hours. Renal clearance is 250-300 ml / min. T1/2 hydrochlorothiazide is 10-15 hours.

Pharmacokinetics in Special Patient Groups

Women have a tendency to higher plasma concentrations of hydrochlorothiazide, this finding is not clinically significant.

In patients with renal insufficiency, the rate of elimination of hydrochlorothiazide is reduced. Patients with remote or single kidney T1/2 is about 34 h.

Indications

- arterial hypertension (in the absence of the effectiveness of monotherapy with telmisartan or hydrochlorothiazide).

Dosing regimen

The drug is taken orally 1 time / day, squeezed liquid, regardless of the meal.

Patients whose blood pressure cannot be adequately controlled with monotherapy with telmisartan or hydrochlorothiazide should be given Telzap® A plus. Before switching to a fixed dose combination, an individual dose titration of each component is recommended. In some clinical situations, a direct transition from monotherapy to treatment with a fixed-dose combination can be considered.

Drug Telzap® Plus, 80 mg + 12.5 mg, can be used 1 time / day in patients whose blood pressure can not be properly controlled while taking telmisartan in a dose of 80 mg / day.

Dose adjustment inpatients with impaired renal function of mild or moderate severity (CC more than 30 ml / min) not required. Recommended periodic monitoring of indicators of renal function.

Concomitant use of telmisartan with aliskiren is contraindicated in patients with renal insufficiency (GFR less than 60 ml / min / 1.73 m2).

Drug Telzap® Plus is contraindicatedpatients with impaired liver function.

Forelderly patients (over 70 years old) dose adjustment is not required.

Drug Telzap® Plus is contraindicated for use inchildren and adolescents under the age of 18 due to lack of safety and efficacy data.

Side effect

The most commonly reported adverse events were dizziness. Severe angioedema occurred rarely (≥1 / 10,000, <1/1000).

Telzap Plus 80 mg + 12.5 mg: the overall incidence of adverse reactions was comparable to that on the background of telmisartan monotherapy. The dependence of the development of adverse reactions on the dose of the drug has not been established, there was no correlation with gender, age or race of patients.

Adverse reactions are divided into system-organ classes according to MedDRA. The frequency of side effects was determined in accordance with the WHO classification: very often (≥1 / 10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10,000, <1/1000), very rarely (<1/10 000), including individual messages; the frequency is unknown (according to the available data it is not possible to determine the frequency of occurrence of a side effect).

Infectious and parasitic diseases: rarely - bronchitis, pharyngitis, sinusitis.

On the part of the immune system: rarely, an increase in symptoms or an exacerbation of systemic lupus erythematosus (during post-registration observation).

Metabolism and nutrition: infrequently - hypokalemia; rarely - hyperuricemia, hyponatremia.

Mental disorders: infrequently - anxiety; rarely - depression.

From the nervous system: often - dizziness; infrequently - fainting, paresthesias; rarely - insomnia, sleep disturbance.

On the part of the organ of vision: rarely - visual impairment, transient visual impairment.

From the organ of hearing: infrequently - vertigo.

Since the cardiovascular system: infrequently - tachycardia, arrhythmia, arterial hypotension, orthostatic hypotension.

On the part of the respiratory system: infrequently - shortness of breath; rarely, respiratory distress syndrome (including pneumonitis and pulmonary edema).

From the digestive system: infrequently - diarrhea, dry mouth, flatulence; rarely - abdominal pain, constipation, dyspepsia, vomiting, gastritis.

Liver and biliary tract: rarely - liver dysfunction, liver disease.

Skin and Subcutaneous Tissues: rarely - angioedema (also fatal), erythema, pruritus, skin rash, increased sweating, urticaria.

From the musculoskeletal system and connective tissue: infrequently - back pain, muscle spasms, myalgia; rarely - pain in the joints, muscle spasms, pain in the limbs.

From the genital and breast organs: infrequently - erectile dysfunction.

General disorders and disorders at the site of administration: infrequently - chest pain; rarely - flu-like syndrome, pain.

From the laboratory and instrumental studies: rarely, an increase in the concentration of creatinine in the blood plasma, an increase in the activity of CPK, and an increase in the activity of hepatic transaminases.

Additional information about individual components

The side effects noted when using one of the components, the development of which can be expected when using a combination of telmisartan and hydrochlorothiazide.

Telmisartan

The incidence of adverse reactions with telmisartan, registered in controlled clinical trials, was comparable to the incidence of adverse reactions noted in the placebo group (41.4% and 43.9%, respectively). The following adverse reactions were reported during a clinical trial of telmisartan, including a high-risk cardiovascular patient group over the age of 50 years.

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

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

On the part of the immune system: rarely - hypersensitivity reactions, Anaphylactic reactions.

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

From the nervous system: rarely - drowsiness.