Guy rohlorotyazyd, Telmysartan | Telpres Plus tablets 80 mg + 25 mg 98 pcs.

Pharmacological action

Pharmacotherapeutic group: Combined antihypertensive agent (angiotensin II receptor antagonist + diuretic)

ATX:

C.09.DA07 Telmisartan in combination with

diuretics Pharmacodynamics:

Telpres Plus is a combination of telmisartan (an angiotensin II receptor antagonist) and hydrochlorothiazide - a thiazide diuretic. The simultaneous use of these components leads to a more pronounced antihypertensive effect than the use of each of them separately.

Taking Telpres Plus once a day leads to a significant gradual decrease in blood pressure (BP).

Telmisartan

Telmisartan is a specific angiotensin II receptor antagonist (type AT1) that is effective when taken orally. It has a high affinity for the AT 1 subtype of angiotensin II receptors, through which the action of angiotensin II is realized. Displaces angiotensin II from the connection with the receptor, not possessing the action of an agonist in relation to this receptor. Telmisartan binds only to the AT1 subtype of angiotensin II receptors. Communication is long lasting. It has no affinity for other receptors, including the AT2 receptor and other less studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible excessive stimulation with angiotensin II, the concentration of which increases with the appointment of telmisartan, has not been studied. It reduces the concentration of aldosterone in the blood, does not inhibit renin in blood plasma and does not block ion channels. Telmisartan does not inhibit the angiotensin converting enzyme (kininase II) (an enzyme that also breaks down bradykinin). Therefore, amplification of 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 administration of telmisartan. The effect of the drug persists for 24 hours and remains significant up to 48 hours. A pronounced antihypertensive effect usually develops 4 weeks after regular use of the drug.

In patients with arterial hypertension, telmisartan lowers systolic and diastolic blood pressure (BP) without affecting heart rate (HR).

In the case of abrupt cancellation of telmisartan, blood pressure gradually returns to its original level without the development of withdrawal syndrome.

Hydrochlorothiazide

Hydrochlorothiazide is a thiazide diuretic. Thiazide diuretics affect the reabsorption of electrolytes in the renal tubules, directly increasing the excretion of sodium and chlorides (approximately in equivalent amounts). The diuretic effect of hydrochlorothiazide leads to a decrease in the volume of circulating blood (BCC), an increase in plasma renin activity, an increase in the secretion of aldosterone, followed by an increase in urine potassium and hydrogen carbonates and, as a result, a decrease in potassium in blood plasma. With simultaneous administration with telmisartan, there is a tendency to stop the loss of potassium caused by these diuretics, presumably due to the blockade of the renin-angiotensin-aldosterone system (RAAS). After oral administration, diuresis increases after 2 hours, and the maximum effect is observed after about 4 hours. The diuretic effect of the drug persists for approximately 6-12 hours.

Long-term use of hydrochlorothiazide reduces the risk of complications of cardiovascular disease and mortality from them.

The maximum antihypertensive effect of Telpres Plus is usually achieved after 4-8 weeksl after starting treatment.

Pharmacokinetics:

The combined use of telmisartan and hydrochlorothiazide does not affect the pharmacokinetics of each of the components of the drug.

Telmisartan:

Absorption

When taken orally, it is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 50%. When taken simultaneously with food, the decrease in AUC (the area under the concentration-time curve) ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). 3 hours after ingestion, the concentration in the blood plasma is leveled regardless of the meal.

Distribution of

Communication with plasma proteins - 99.5%, mainly with albumin and alpha-1 glycoprotein. The average value of the apparent volume of distribution in equilibrium concentration is 500 l.

Metabolism

Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive.

Withdrawal

Elimination half-life (T1 / 2) - more than 20 hours. It is excreted through the intestine unchanged, excretion by the kidneys - less than 2% of the dose taken. The total plasma clearance is high (900 ml / min) compared with hepatic blood flow (about 1500 ml / min).

Pharmacokinetics in special patient groups

Gender differences

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 with men without a significant effect on effectiveness. Dose adjustment is not required.

Elderly patients

The pharmacokinetics of telmisartan in elderly patients are not different from younger patients. Dose adjustment is not required.

Patients with impaired renal function

In patients with mild to moderate impaired renal function, dose adjustment of telmisartan is not required.

Patients with severe renal impairment and those on hemodialysis are recommended a lower initial dose of 20 mg per day. Telmisartan is not excreted by hemodialysis.

Patients with impaired liver function

Pharmacokinetics studies in patients with hepatic impairment showed an increase in the absolute bioavailability of telmisartan to almost 100%. With liver failure, T1 / 2 does not change. In patients with mild to moderate impaired liver function (class A and B on the Child-Pugh scale), the daily dose should not exceed 40 mg.

Hydrochlorothiazide:

After oral administration of Telpres Plus, the maximum plasma concentrations of hydrochlorothiazide are reached within 1-3 hours. Absolute bioavailability based on total kidney excretion is about 60%. It is bound by blood plasma proteins to 64% hydrochlorothiazide, and the distribution volume is 0.8 В± 0.3 l / kg. Hydrochlorothiazide is not metabolized in the body and excreted by the kidneys almost unchanged. About 60% of the dose taken orally is eliminated within 48 hours. Renal clearance of about 250-300 ml / min. T1L hydrochlorothiazide - 10 - 15 hours. There is a difference in plasma concentrations in men and women. In women, the concentration of telmisartan in plasma is 2-3 times higher than in men, and women have a tendency to increase the concentration of hydrochlorothiazide in the blood plasma is clinically insignificant.

Patients with impaired renal function

In patients with impaired renal function, the rate of elimination of hydrochlorothiazide is reduced.

Studies in patients with creatinine clearance (CC) of 90 ml / min showed that T1 / 2 of hydrochlorothiazide is increased. In patients with impaired T1 / 2 renal function, about 34 hours.

Indications

Arterial hypertension (in the case of inefficiency of telmisartan or hydrochlorothiazide in monotherapy).

Contraindications

- Hypersensitivity to the active substances or auxiliary components of the drug or other sulfonamide derivatives

- Pregnancy

- Breastfeeding period

- Obstructive biliary tract disease

- Severe class) Severe dysfunction impaired renal function (CC less than 30 ml / min)

- Refractory hypokalemia, hypercalcemia

- Concomitant use with aliskiren in patients with diabetes mellitus and / or usheniem renal function (glomerular filtration rate of less than 60 ml / min / 1.73 m2)

- Simultaneous use of ACE in patients with diabetic nephropathy

inhibitors - lactase deficiency, lactose intolerance,

glucose-galactose malabsorption syndrome - Age under 18 years (efficacy and safety not established).

Caution:

- Bilateral renal artery stenosis or stenosis of a single kidney artery (see Special instructions)

- Hepatic function impairment (Class A and B according to the Child-Pugh classification) (see Special instructions)

- Decreased BCC due to previous diuretic therapy, restrictions on the intake of salt, diarrhea or vomiting

- Hyperkalemia

- Condition after kidney transplantation (no experience with application)

- Chronic heart failure III-IV functional class (FC) according to the classification of the New York Cardiology Association

- Hypercalcemia

- Hypercholesterolemia - Hypercholesterolemia heart

- Progressive liver disease (risk of hepatic coma)

- Aortic and mitral valve stenosis

- Idiopathic hypertrophic subaortic stenosis (hypertrophic Skye obstructive cardiomyopathy)

- Diabetes

- Primary aldosteronism

- Gout hyperuricemia

- Systemic lupus erythematosus

- Secondary angle-closure glaucoma (due to the presence of hydrochlorothiazide)

- Use in patients of the Negroid race

- Limited experience in patients with impaired kidney (CC more than 30 ml / min) side effects from the kidneys and dose adjustment are not required

- Concomitant use with ACE inhibitors or aliskiren

- Concomitant use with potassium preparations, potassium-sparing diuretics.

Composition

Each tablet 25 mg + 80 mg contains:

active ingredients: hydrochlorothiazide - 25.00 mg, telmisartan - 80.00 mg excipients: mannitol - 327.70 mg, povidone-K25 - 21.60 mg, crospovidone - 20.0 mg, magnesium stearate - 9.00 mg, meglumine - 24.00 mg, sodium hydroxide - 6.70 mg, lactose monohydrate - 99.67 mg, microcrystalline cellulose - 64.00 mg, hypromellose - 6.00 mg, sodium carboxymethyl starch, type A - 4.00 mg, yellow iron oxide (E 172) - 0.33 mg.

Dosage and administration

Inside, regardless of the time of meal.

The drug Telpres Plus must be taken once a day.

- Telpres Plus 12.5 / 40 mg may be prescribed to patients in whom the use of telmisartan preparations in a dosage of 40 mg or hydrochlorothiazide does not lead to adequate control of blood pressure.

- Telpres Plus 12.5 / 80 mg may be prescribed to patients in whom the use of telmisartan preparations in a dosage of 80 mg or Telpres Plus 12, 5/40 mg does not lead to adequate control of blood pressure.

- Telpres Plus 25/80 mg can be prescribed to patients in whom the use of telmisartan preparations in a dosage of 80 mg or Telpres Plus 12.5 / 80 mg drug does not lead to adequate control of blood pressure, or to patients whose condition has previously been stabilized by telmisartan or hydrochlorothiazide with separate application.

In patients with severe arterial hypertension, the maximum daily dose of telmisartan is 160 mg in combination with hydrochlorothiazide in a daily dose of 12.5-25 mg.

Impaired renal function

Limited experience with Telpres Plus in patients with mild to moderate renal impairment does not require dose changes in these cases. In such patients, renal function should be monitored (with CC less than 30 ml / min, see section Contraindications).

Impaired liver function

In patients with mild to moderate impaired liver function (Child-Pugh Class A and B), the daily dose of Telpres Plus should not exceed 12.5 / 40 mg per day (see Pharmacokinetics section).

Elderly patients

Dosage regimen does not require changes.

Side effects of

1) expected based on experience with telmisartan

2) expected based on experience with hydrochlorothiazide

3) side effects that were not observed in clinical trials with telmisartan and hydrochlorothiazide, but are expected during use Disorders of the respiratory system:

respiratory distress syndrome (including pneumonia and non-cardiogenic pulmonary edema) 3), dyspnea 3).

Disturbances from the heart:

arrhythmias3), tachycardia3), bradycardia1).

Vascular disorders:

marked decrease in blood pressure (including orthostatic hypotension) 3).

Disorders of the nervous system:

syncope / fainting 3), paresthesia 3), sleep disturbance 3), insomnia 3), dizziness 3), increased irritability 2), headache 2).

Mental disorders:

anxiety3), depression3).

Disorders of the gastrointestinal tract:

Diarrhea3), dry mucous membranes of the oral cavity3), flatulence3), abdominal pain3), constipation3), vomiting3), gastritis3), decreased appetite2), anorexia2), hyperglycemia2), hypercholesterol2) pancreatitis2), dyspepsia1), 2), 3).

Violations of the liver and biliary tract:

impaired liver function 3), jaundice (hepatocellular or cholestatic) 2). srd

marked decrease in blood pressure (including orthostatic hypotension) 3).

Disorders of the nervous system:

syncope / fainting 3), paresthesia 3), sleep disturbance 3), insomnia 3), dizziness 3), increased irritability 2), headache 2).

Mental disorders:

anxiety3), depression3).

Disorders of the gastrointestinal tract:

Diarrhea3), dry mucous membranes of the oral cavity3), flatulence3), abdominal pain3), constipation3), vomiting3), gastritis3), decreased appetite2), anorexia2), hyperglycemia2), hypercholesterol2) pancreatitis2), dyspepsia1), 2), 3).

Violations of the liver and biliary tract:

impaired liver function 3), jaundice (hepatocellular or cholestatic) 2). srd

marked decrease in blood pressure (including orthostatic hypotension) 3).

Disorders of the nervous system:

syncope / fainting 3), paresthesia 3), sleep disturbance 3), insomnia 3), dizziness 3), increased irritability 2), headache 2).

Mental disorders:

anxiety3), depression3).

Disorders of the gastrointestinal tract:

Diarrhea3), dry mucous membranes of the oral cavity3), flatulence3), abdominal pain3), constipation3), vomiting3), gastritis3), decreased appetite2), anorexia2), hyperglycemia2), hypercholesterol2) pancreatitis2), dyspepsia1), 2), 3).

Violations of the liver and biliary tract:

impaired liver function 3), jaundice (hepatocellular or cholestatic) 2). srd sleep disturbances3), insomnia3), dizziness3), increased irritability2), headache2).

Mental disorders:

anxiety3), depression3).

Disorders of the gastrointestinal tract:

Diarrhea3), dry mucous membranes of the oral cavity3), flatulence3), abdominal pain3), constipation3), vomiting3), gastritis3), decreased appetite2), anorexia2), hyperglycemia2), hypercholesterol2) pancreatitis2), dyspepsia1), 2), 3).

Violations of the liver and biliary tract:

impaired liver function 3), jaundice (hepatocellular or cholestatic) 2). srd sleep disturbances3), insomnia3), dizziness3), increased irritability2), headache2).

Mental disorders:

anxiety3), depression3).

Disorders of the gastrointestinal tract:

Diarrhea3), dry mucous membranes of the oral cavity3), flatulence3), abdominal pain3), constipation3), vomiting3), gastritis3), decreased appetite2), anorexia2), hyperglycemia2), hypercholesterol2) pancreatitis2), dyspepsia1), 2), 3).

Violations of the liver and biliary tract:

impaired liver function 3), jaundice (hepatocellular or cholestatic) 2). srd flatulence3), abdominal pain3), constipation3), vomiting3), gastritis3), decreased appetite2), anorexia2), hyperglycemia2), hypercholesterolemia2), pancreatitis2), dyspepsia1), 2), 3).

Violations of the liver and biliary tract:

impaired liver function 3), jaundice (hepatocellular or cholestatic) 2). srd flatulence3), abdominal pain3), constipation3), vomiting3), gastritis3), decreased appetite2), anorexia2), hyperglycemia2), hypercholesterolemia2), pancreatitis2), dyspepsia1), 2), 3).

Violations of the liver and biliary tract:

impaired liver function 3), jaundice (hepatocellular or cholestatic) 2).

Disorders of the skin and subcutaneous tissues: Ecdema

1), drug rash1), 2), toxic epidermal necrosis1), 2), erythema3), skin itching3), rash3), increased sweating3), photosensitivity reaction2).

Musculoskeletal and connective tissue disorders:

back pain3), muscle spasms3), myalgia3), arthralgia3), calf muscle cramps3), arthrosis1), tendonitis-like symptoms1), chest pain3).

Disorders of the blood and lymphatic system:

iron deficiency anemia1), aplastic anemia2), hemolytic anemia2), thrombocytopenia1), eosinophilia1), leukopenia2), neutropenia / agranulocytosis2), thrombocytopenia2).

Disorders of the kidneys and urinary tract:

renal failure1), 2), including acute renal failure1), interstitial nephritis2), glucosuria 2).

Disorders of the organ of vision:

impaired vision3), transient blurred vision3), xanthopsia2), acute angle-closure glaucoma2), acute myopia2).

Disorders of the genitals and mammary gland:

Impotence 3).

Infectious and parasitic diseases:

sepsis, including fatal cases1), upper respiratory tract infections (bronchitis, pharyngitis, sinusitis) 1), 3), urinary tract infections (including cystitis) 1), salivary gland inflammation 2).

Influence on the results of laboratory and instrumental studies:

increased plasma creatinine concentration 3), increased activity of liver enzymes 3), increased activity of creatine phosphokinase 3), increased activity of blood uric acid concentration 3), hypertriglyceridemia 2), hypokalemia 2), 3), hypomagnesemia2), hyperkalemia1), hyponatremia2), 3), hyperuricemia3), a decrease in BCC2), hypoglycemia (in patients with diabetes mellitus) 1), impaired glucose tolerance2), a decrease in hemoglobin in the blood1).

Immune system disorders:

angioedema (including fatal cases) 3), anaphylactic reactions1), 2), lupus-like reactions2), exacerbation or worsening of symptoms of systemic lupus erythematosus3), necrotic vasculitis2), systemic vasculitis2), lupus erythematosus 2), vasculitis 2).

General disorders and disorders at the injection site:

flu-like syndrome 3), fever 2), weakness 1), 2).

Overdose

Information on overdose is limited. Possible symptoms of an overdose are composed of symptoms from the individual components of the drug. Telmisartan - the most significant - a marked decrease in blood pressure and tachycardia, bradycardia, dizziness, increased serum creatinine concentration and acute renal failure can also be observed.

Hydrochlorothiazide - a violation of the water-electrolyte balance of the blood (hypokalemia, hypochloremia), a decrease in BCC, which can lead to muscle spasms and / or increase disorders of the cardiovascular system: arrhythmias caused by the simultaneous use of cardiac glycosides or some antiarrhythmic drugs.

Treatment: symptomatic therapy, hemodialysis is ineffective. The degree of removal of hydrochlorothiazide during hemodialysis has not been established. Regular monitoring of serum electrolytes and creatinine is required. Hemodialysis is not effective.

Storage conditions

At a temperature not exceeding 25 РC, in the original packaging.

Keep out of the reach of children!

Expiration

2 years

Terms and conditions

prescription

dosage form

tab adolescents