Telzap - instructions for use, reviews, analogs and formulations (tablets 40 mg, 80 mg, plus 80 mg + 12.5 mg with diuretic hydrochlorothiazide) drugs for the treatment of hypertension and pressure reduction in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Tespaz. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of physicians specialists on the use of Telzap in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Telzap in the presence of existing structural analogues. Use to treat essential hypertension and reduce blood pressure in adults, children, as well as in pregnancy and lactation. Composition of the preparation.

Tespaz antihypertensive drug.

Telmisartan (the active substance of the preparation Telzap) is a specific antagonist of angiotensin 2 receptors (type AT1), effective for oral administration. Has a very high affinity for the AT1 receptor subtype, through which the action of angiotensin 2 is realized. Telmisartan displaces angiotensin 2 from its binding to the receptor without having an agonist action against this receptor; binds only to the subtype of AT1 receptors of angiotensin 2. Binding is stable. Telmisartan does not have an affinity for other receptors, incl. to AT2-receptors and other less studied angiotensin receptors. The functional significance of these receptors, as well as their possible effect of excessive stimulation by angiotensin 2, the concentration of which increases with 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 ACE (kininase 2), which also catalyzes the destruction of bradykinin. This avoids the side effects associated with the action of bradykinin (eg, dry cough).

Essential hypertension

Telzap at a dose of 80 mg completely blocks the hypertensive effect of angiotensin 2. The onset of antihypertensive action is noted within 3 hours after the first administration of telmisartan. The effect of the drug persists for 24 hours and remains clinically significant until 48 hours. The pronounced antihypertensive effect usually develops 4-8 weeks after regular administration.

In patients with arterial hypertension, telmisartan reduces systolic and diastolic blood pressure without affecting the heart rate.

In the event of a sudden discontinuation of Telzap AD, for several days, it gradually returns to the baseline without the 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 with telmisartan compared with ACE inhibitors.

Prevention of cardiovascular diseases

Patients aged 55 years and older with coronary artery disease, stroke, transient ischemic attack, peripheral arterial disease, or type 2 diabetes complications (eg, retinopathy, left ventricular hypertrophy, macro- or microalbuminuria) who have a history of cardiovascular disease events, Telzap had an effect similar to the effect of Ramipril on reducing the combined endpoint: cardiovascular mortality from a myocardial infarction without a fatal outcome, a non-fatal stroke and a state nourishment in connection with chronic heart failure.

Telmisartan was also effective, as did ramipril for reducing the incidence of secondary points: cardiovascular mortality, myocardial infarction without fatal outcome, or a stroke without fatal outcome.

Dry cough and angioedema were less often described in the background of the use of telmisartan in contrast to ramipril, with arterial hypotension more likely to occur with telmisartan.

Hydrochlorothiazide

Hydrochlorothiazide in the composition of the drug Telzap Plus is a thiazide diuretic.Thiazides affect the reabsorption of electrolytes in the renal tubules, thereby increasing the excretion of sodium and chloride ions in approximately equivalent amounts. The diuretic effect of hydrochlorothiazide leads to a decrease in bcc, increased plasma renin activity, increased production of aldosterone, followed by an increase in potassium and bicarbonate in the urine and a decrease in potassium in the blood plasma. The simultaneous use of telmisartan reduces the loss of potassium caused by this diuretic, probably due to the blockade of the RAAS. After taking hydrochlorothiazide, diuresis is intensified after 2 hours, the maximum effect develops after about 4 hours, the action 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.

Composition

Telmisartan + auxiliary substances.

Telmisartan + Hydrochlorothiazide + excipients (Tepzap Plus).

Pharmacokinetics

Telmisartan

When ingested Tepzap quickly absorbed from the digestive tract. Bioavailability - 50%.Telmisartan binds strongly to blood plasma proteins, mainly with albumin and alpha-1 acid glycoprotein. Metabolized by conjugation with glucuronic acid. The conjugate does not have pharmacological activity. Output through the intestine in an unchanged form, excretion by the kidneys - less than 1%.

Hydrochlorothiazide

Hydrochlorothiazide is not metabolized in humans. It is excreted almost completely unchanged in the urine. About 60% of the dose taken internally is excreted unchanged for 48 hours. Renal clearance is 250-300 ml / min.

Pharmacokinetics in specific patient groups

There is a difference in plasma concentrations of telmisartan in men and women. Cmax and AUC were approximately 3 and 2 times higher in women than in men, without significant effect on efficacy.

Women tend to have higher concentrations of hydrochlorothiazide in the blood plasma, this is not clinically significant.

The pharmacokinetics of telmisartan in elderly patients over the age of 65 do not differ from young patients. Correction of the dose is not required.

In patients with mild to moderate renal dysfunction, correction of the dose of telmisartan is not required.Patients with severe renal failure and patients on hemodialysis are recommended a lower initial dose of 20 mg per day. Telmisartan is not excreted by hemodialysis.

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

Indications

• essential hypertension;
• reduction in mortality and the incidence of cardiovascular diseases in adult patients with cardiovascular diseases of atherothrombotic origin (IHD, stroke or peripheral arterial lesions in the anamnesis) and type 2 diabetes mellitus with target organ damage.

Forms of release

Tablets of 40 mg and 80 mg.

Tablets 80 mg + 12.5 mg (Telzap Plus).

Instructions for use and dosage

Tespaz

The drug is taken orally, once a day, regardless of food intake; tablets should be washed down with liquid.

Arterial hypertension

The initial recommended dose of the preparation is 40 mg (1 tablet) once a day. Some patients may be effective in taking the drug at a dose of 20 mg per day. A dose of 20 mg can be obtained by dividing the tablet 40 mg in half by the risk.In cases where the therapeutic effect is not achieved, the recommended dose of Tepzap can be increased to a maximum of 80 mg once a day.

As an alternative, Telpos can be taken in combination with thiazide diuretics, for example, hydrochlorothiazide, which, when combined, 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 incidence of cardiovascular diseases

The recommended dose of Tepzap is 80 mg once a day. In the initial period of treatment, monitoring of blood pressure level is recommended, correction of hypotensive therapy may be required.

The experience with telmisartan in patients with severe renal failure or patients on hemodialysis is limited. These patients are recommended a lower initial dose of 20 mg per day. For patients with mild to moderate renal dysfunction, dose adjustment is not required.

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

Simultaneous application of the preparation of Tepaz with ACE inhibitors is contraindicated in patients with diabetic nephropathy.

Patients with mild to moderate hepatic insufficiency (class A and B according to Child-Pugh classification) should be administered with caution, the dose should not exceed 40 mg once a day. The drug Telzaz is contraindicated in patients with severe hepatic insufficiency (class C according to the Child-Pugh classification).

Older patients do not need a dose adjustment.

Telzap Plus

Inside, once a day, washed down with liquid, regardless of the meal.

Patients whose blood pressure can not be adequately controlled by monotherapy with telmisartan or hydrochlorothiazide should take the drug, Telzap Plus. Before switching to a combination with fixed doses, individual titration of the dose of each component is recommended. In some clinical situations, a direct transition from monotherapy to treatment with a fixed dose combination can be considered.

The drug Telzap Plus, can be applied once a day to patients whose blood pressure can not be properly controlled when taking telmisartan at a dose of 80 mg per day.

Side effect

• urinary tract infections, including cystitis;
• upper respiratory tract infections, including pharyngitis and sinusitis;
• sepsis, incl. with lethal outcome;
• Anemia, eosinophilia, thrombocytopenia;
• anaphylactic reaction;
• hypersensitivity;
• hyperkalemia;
• hypoglycemia (in patients with diabetes mellitus);
• insomnia;
• depression;
• anxiety;
• fainting;
• drowsiness;
• visual disorders;
• vertigo;
• bradycardia;
• excessive decrease in blood pressure;
• orthostatic hypotension;
• tachycardia;
• dyspnea;
• cough;
• interstitial lung disease;
• abdominal pain;
• diarrhea;
• dyspepsia;
• flatulence;
• vomiting;
• dry mouth;
• discomfort in the stomach;
• a violation of taste sensations;
• impaired liver function / liver damage;
• itching;
• hyperhidrosis;
• rash;
• angioedema (also fatal);
• eczema;
• erythema;
• hives;
• drug rash;
• toxic skin rash;
• ischialgia;
• muscle spasms;
• myalgia;
• arthralgia;
• pain in the limbs;
• tendenitis-like syndrome;
• impaired kidney function, including acute renal failure;
• increase in the concentration of creatinine in the blood plasma;
• reduction of hemoglobin;
• an increase in the content of uric acid in the blood plasma;
• increased activity of hepatic enzymes and CK;
• chest pain;
• asthenia;
• influenza-like syndrome.

Contraindications

• obstructive diseases of the biliary tract;
• severe liver dysfunction (Child-Pugh class C);
• joint application with aliskiren in patients with diabetes mellitus or severe renal dysfunction (GFR <60 ml / min / 1.73 m2 body surface area);
• simultaneous use with ACE inhibitors in patients with diabetic nephropathy;
• hereditary intolerance to fructose (due to the presence of sorbitol in the formulation);
• pregnancy;
• the period of breastfeeding;
• age under 18 years (effectiveness and safety not established);
• hypersensitivity to the active substance or any excipients of the drug.

Application in pregnancy and lactation

At present, there is no reliable information on the safety of telmisartan in pregnant women. In animal studies, the reproductive toxicity of the drug was identified. The use of the drug is contraindicated during pregnancy.

If long-term treatment with Tepzap is necessary, patients planning a pregnancy should choose an alternative antihypertensive drug with a proven safety profile during pregnancy. After establishing the fact of pregnancy, treatment with Tepzap should be stopped immediately and, if necessary, started alternative treatment.

As the results of clinical observations have shown, the use of angiotensin 2 receptor antagonists in the 2nd and 3rd trimester of pregnancy has a toxic effect on the fetus (impairment of renal function, oligohydramnios, ossification of the skull) and newborn (renal failure, arterial hypotension and hyperkalemia). When angiotensin 2 receptor antagonists are used, ultrasound of the kidneys and fetal skull is recommended in the 2nd trimester of pregnancy. Children whose mothers took angiotensin 2 receptor antagonists during pregnancy should be carefully monitored for the detection of arterial hypotension.

Information on the use of telmisartan during breastfeeding is absent. The use of Tzapaz 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.

Use in children

Contraindicated the use of the drug Tamsap under the age of 18 years (efficacy and safety not established).

Application in elderly patients

Older patients do not need a dose adjustment.

special instructions

Impaired liver function

The use of the drug TALZAP is contraindicated in patients with cholestasis, bile duct obstruction or severe liver function disorder (Child-Pugh class C), since telmisartan is mainly excreted with bile. It is suggested that these patients have a reduced hepatic clearance of telmisartan. In patients with mild to moderate liver failure (class A and B according to the Child-Pugh classification), Cauldron should be used with caution.

Renovascular hypertension

In the treatment of drugs acting on RAAS, in patients with bilateral stenosis of the renal arteries or stenosis of the artery of a single functioning kidney, the risk of severe arterialhypotension and renal failure.

Impaired renal function and kidney transplantation

With the use of the preparation, Telzap, in patients with impaired renal function, periodic monitoring of the potassium and creatinine content in the blood plasma is recommended. The experience of clinical use of the drug Telzap in patients who have recently undergone kidney transplantation is absent.

Decrease of BCC

Symptomatic arterial hypotension, especially after the first administration of the drug, can occur in patients with reduced BCC and / or sodium in the blood plasma on the background of previous treatment with diuretics, restriction of salt intake, diarrhea or vomiting. Such conditions (deficiency of fluid and / or sodium) should be eliminated before the beginning of taking the drug Tepzap.

Double blockade of RAAS

The 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 body surface area).

The simultaneous use of Telzap and ACE inhibitors is contraindicated in patients with diabetic nephropathy.

As a result of oppression of RAAS, arterial hypotension, syncope, hyperkalemia and impaired renal function were noted (incl.acute renal failure) in predisposing patients, especially when several drugs are used together, also acting on this system. Therefore, the double blockade of RAAS (for example, against the background of taking telmisartan with other antagonists of RAAS) is not recommended.

In cases of vascular tone and renal function, mainly from RAAS activity (for example, in patients with chronic heart failure or kidney disease, including stenosis of the renal arteries or stenosis of the artery of a single kidney), the administration of drugs that affect this system can accompanied by the development of acute arterial hypotension, hyperaemia, oliguria, and in rare cases acute renal failure.

Primary hyperaldosteronism

In patients with primary hyperaldosteronism, treatment with antihypertensive drugs, which are effected by inhibition of RAAS, is usually ineffective. In this regard, the use of the drug is not recommended.

Stenosis of aortic and mitral valves, hypertrophic obstructive cardiomyopathy

As with other vasodilators, patients with aortic or mitral stenosis, as well as hypertrophic obstructive cardiomyopathy, should be especially careful when using Tepzap.

Patients with diabetes who received insulin or hypoglycemic agents for oral administration

Against the backdrop of treatment with Tepzap, hypoglycemia may occur in such patients. It is necessary to strengthen the control of glycemia, t. it may be necessary to correct the dose of insulin or hypoglycemic agent.

Hyperkalemia

The use of drugs acting on RAAS can cause hyperkalemia. In elderly patients, patients with renal insufficiency or diabetes mellitus, patients taking medications that promote an increase in potassium in the blood plasma, and / or patients with concomitant diseases, hyperkalemia can be fatal.

When deciding on the concomitant use of medicines acting on RAAS, it is necessary to assess the relationship between risk and benefit. The main risk factors for the development of hyperkalemia, which should be considered, are:

• diabetes mellitus, renal failure, age (patients older than 70 years);
• combination with one or more drugs acting on RAAS, and / or potassium-containing food additives. Drugs or therapeutic classes of drugs that can cause hyperkalemia include salt substitutes containing potassium, potassium-sparing diuretics, ACE inhibitors, angiotensin receptor 2 antagonists, non-steroidal anti-inflammatory drugs (NSAIDs) (including selective COX-2 inhibitors), heparin, immunosuppressants (cyclosporin or tacrolimus), and trimethoprim;
• intercurrent diseases, especially dehydration, acute heart failure, metabolic acidosis, impaired renal function, cytolysis syndrome (eg, acute limb ischemia, rhabdomyolysis, extensive trauma).

Patients at risk should carefully monitor potassium levels in the blood plasma.

Sorbitol

The drug Telzap contains sorbitol (E420). Patients with a rare hereditary intolerance to fructose should not take the drug.

Ethnic differences

As noted for ACE inhibitors, telmisartan and other angiotensin 2 receptor antagonists appear to be less effective in lowering blood pressure in patients of the Negroid race than in representatives of other races, possibly due to a greater predisposition to decreased renin activity in the population of these patients.

Other

As with the use of other antihypertensive drugs, excessive reduction in blood pressure in patients with ischemic cardiomyopathy or IHD can lead to the development of myocardial infarction or stroke.

Impact on the ability to drive vehicles and manage mechanisms

Special clinical studies to study the effect of the drug on the ability to drive a car and mechanisms were not conducted. Care should be taken when driving a car and working with mechanisms that require high concentration of attention, because On the background of the use of the drug, Tazap seldom there may be dizziness and drowsiness.

Drug Interactions

Double blockade of RAAS

Concomitant use of Telzap with aliskiren is contraindicated in patients with diabetes mellitus or renal insufficiency (GFR less than 60 mL / min / 1.73 m2 body surface area) and is not recommended for other patients.

The simultaneous use of telmisartan and ACE inhibitors is contraindicated in patients with diabetic nephropathy.

Clinical studies have shown that the double blockade of RAAS due to combined use of ACE inhibitors, angiotensin 2 receptor antagonists or aliskiren is associated with an increased incidence of adverse events such as hypotension, hyperkalemia, and renal dysfunction (including acute renal failure) compared with the use of only one drug acting on the RAAS.

Hyperkalemia

The risk of developing hyperkalemia may increase when combined with other medicines that can cause hyperkalemia (potassium-containing dietary supplements and salt substitutes containing potassium, potassium-sparing diuretics (eg spironolactone, eplerenone, triamterene or amiloride), NSAIDs (including selective COX-2 inhibitors) , heparin, immunosuppressants (cyclosporine or tacrolimus), and trimethoprim). If necessary, against the background of documented hypokalemia, joint use of drugs should be carried out with caution and regularly monitor the potassium content in the blood plasma.

Digoxin

With the combined use of telmisartan with digoxin, an average increase of Cmax Digoxin in blood plasma was observed at 49% and Cmin by 20%. At the beginning of treatment, when choosing a dose and stopping telmisartan treatment, the concentration of digoxin in the blood plasma should be carefully monitored for its maintenance within the therapeutic range.

Potassium-sparing diuretics or potassium-containing food additives

Angiotensin 2 receptor antagonists, such as telmisartan, reduce the diuretic-induced loss of potassium. Potassium-sparing diuretics (eg, spironolactone, eplerenone, triamterene or amiloride), potassium-containing dietary supplements or salt substitutes can lead to a significant increase in potassium levels in the blood plasma. If a concomitant use is indicated, since there is documented hypokalemia, they should be used with caution and against a background of regular monitoring of potassium in the blood plasma.

Lithium preparations

With the combined use of lithium preparations with ACE inhibitors and angiotensin 2 receptor antagonists, including telmisartan, a reversible increase in the concentration of lithium in the blood plasma and its toxic effect occurred.If it is necessary to use this combination of drugs, it is recommended to carefully monitor the concentration of lithium in the blood plasma.

NSAIDs

NSAIDs (ie, Acetylsalicylic acid at doses used for anti-inflammatory treatment, COX-2 inhibitors and nonselective NSAIDs) can attenuate the antihypertensive effect of angiotensin 2 receptor antagonists. In some patients with impaired renal function (eg, patients with dehydration, elderly patients with impaired renal function), the combined use of angiotensin 2 receptor antagonists and drugs that oppress COX-2 can lead to further deterioration of renal function, including the development of acute renal failure tatochnosti, which is usually reversible. Therefore, joint use of drugs should be carried out with caution, especially in elderly patients. Proper fluid intake should also be ensured, in addition, at the beginning of the joint application and periodically the kidney function should be monitored periodically thereafter.

Diuretics (thiazide or "loop")

Prior treatment with diuretics in high doses, such as Furosemide (loop diuretic) and hydrochlorothiazide (thiazide diuretic),can lead to hypovolemia and the risk of developing arterial hypotension at the beginning of telmisartan treatment.

Other antihypertensives

The action of Telzap can be enhanced by the joint use of other antihypertensive drugs.

Based on the pharmacological properties of Baclofen and amifostine, it can be assumed that they will enhance the therapeutic effect of all antihypertensive agents, including telmisartan. In addition, orthostatic hypotension may increase with the use of ethanol (alcohol), barbiturates, narcotics or antidepressants.

Corticosteroids (for systemic use)

Corticosteroids weaken the action of telmisartan.

Analogues of the medicinal product Tzapaz

Structural analogs for the active substance:

• Mycardis;
• MykardisPlus;
• Pritor;
• Tanidol;
• Theseo;
• Telzap Plus;
• Telmisartan;
• Telmist;
• Telpres;
• Telpres Plus;
• Telsartan;
• Telsartan N.

Analogues on the pharmacological group (angiotensin 2 receptor antagonists:

• Aprovask;
• Aprovel;
• Artinova;
• Atacand;
• Bloktran;
• Brozaar;
• Vasotensis;
• Wales;
• Wales H;
• Valsartan;
• Walsakor;
• Vylloset;
• Gisaar;
• Hypoart;
• Diovan;
• Duopress;
• Zisakar;
• Ibertan;
• Irbesartan;
• Irsar;
• Candecor;
• Candesartan;
• Cardomin;
• Cardos;
• Cardosal;
• Cardosten;
• Karzartan;
• Ko-Exforge;
• Co-span;
• Cosaar;
• Ksarten;
• Lozap;
• Lopaz Plus;
• Lozarel;
• Losartan;
• Losartan N;
• Lorist;
• Losakor;
• Mycardis;
• Naviten;
• Nortivan;
• Olimestra;
• Ordiss;
• Pritor;
• Prezartan;
• Renikard;
• Sartavell;
• Tanidol;
• Tareg;
• Twentieth;
• Teveten;
• Telmisartan;
• Telpres;
• Telsartan;
• Firmas;
• Edarby;
• Exforge;
• Exototans;
• Eprosartan mesylate.

Similar medicines:

Other medicines: