Universal reference book for medicines
Product name: TELZAP ® (TELZAP)

Active substance: telmisartan

Type: Angiotensin II receptor antagonist

Manufacturer: ZENTIVA (Czech Republic) is produced by ZENTIVA SAGLIK URUNLERI SANAYI VE TICARET (Turkey)
Composition, form of production and packaging

Tablets from almost white to yellowish color, oblong, biconcave, with a risk from both sides.

1 tab.

telmisartan 40 mg

[PRING] meglumine - 12 mg, sorbitol - 162.2 mg, sodium hydroxide - 3.4 mg, povidone 25 - 20 mg, magnesium stearate - 2.4 mg.

10 pieces.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (9) - packs of cardboard.
Tablets from almost white to yellowish color, oblong, biconcave, with engraving "80" on one side.

1 tab.

telmisartan 80 mg

[PRING] meglumine - 24 mg, sorbitol - 324.4 mg, sodium hydroxide - 6.8 mg, povidone 25 - 40 mg, magnesium stearate - 4.8 mg.

10 pieces.
- blisters (3) - packs of cardboard.
10 pieces.
- blisters (9) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2017.

PHARMACHOLOGIC EFFECT

Antihypertensive drug.

Pharmacodynamics

Telmisartan is a specific angiotensin II receptor antagonist (type AT 1 ), effective when ingested.
Has a very high affinity for the subtype of AT 1 -receptors, through which the action of angiotensin II is realized. Telmisartan displaces angiotensin II from its bond to the receptor without the action of an agonist for this receptor; binds only to the subtype of AT 1 -receptor angiotensin II. Binding is stable. Telmisartan does not have an affinity for other receptors, incl. to AT 2 -receptors and other, less studied receptors of angiotensin. The functional significance of these receptors, as well as the effect of their possible excessive stimulation with angiotensin II, whose concentration increases with the appointment of 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 II), which also catalyzes the destruction of bradykinin. This avoids the side effects associated with the action of bradykinin (eg, dry cough).
Essential hypertension

Telmisartan at a dose of 80 mg completely blocks the hypertensive effect of angiotensin II.
The onset of antihypertensive action is observed 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 case of a sharp discontinuation of telmisartan, blood pressure gradually returns to the baseline within a few days without the development of 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 of the events, telmisartan had an effect similar to that of ramipril for reducing the combined endpoint: cardiovascular mortality from a myocardial infarction without a fatal outcome, a stroke without a fatal outcomeand hospitalization due to 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.

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.

PHARMACOKINETICS

Suction

When administered, telmisartan is rapidly absorbed from the digestive tract.
Bioavailability - 50%. When taken concomitantly with food, the decrease in AUC ranges from 6% (when taken in a dose of 40 mg) to 19% (when taken in a dose of 160 mg). After 3 hours after taking the concentration in the blood plasma levels, regardless of whether telmisartan was taken 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, AUC increase disproportionally to a dose increase when administered at doses above 40 mg / day.
Distribution

Telmisartan binds strongly to blood plasma proteins (> 99.5%), mainly with albumin and alpha-1 acidic glycoprotein.
The average apparent volume of distribution (Vdss ) in the equilibrium state is approximately 500 liters.
Metabolism

Metabolized by conjugation with glucuronic acid.
The conjugate does not have pharmacological activity.
Excretion

T 1/2 is more than 20 hours. It is excreted through the intestine in an unchanged form, excretion by the kidneys - less than 1%.
The total plasma clearance is high (about 1000 ml / min) compared with hepatic blood flow (about 1500 ml / min).
Pharmacokinetics in specific patient groups

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

DOSING MODE

The drug is taken orally, 1 time / day, regardless of food intake;
tablets should be washed down with liquid.
Arterial hypertension

The initial recommended dose of the preparation Telzap ® is 40 mg (1 tab.) 1 time / day.
Some patients may be effective in taking the drug at a dose of 20 mg / 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 the preparation can be increased to a maximum of 80 mg once a day.
As an alternative, the preparation of Telzap ® 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 the preparation Telzap ® is 80 mg 1 time / 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 / day. For patients with mild to moderate renal dysfunction, dose adjustment is not required.
Concomitant use of the preparation Telzap ® with aliskiren is contraindicated in patients with renal insufficiency (GFR less than 60 ml / min / 1.73 m 2 body surface area).

Simultaneous use of the preparation of Tazap ® with ACE inhibitors is contraindicated in patients with diabetic nephropathy.

Patients with mild to moderate degree of hepatic insufficiency (class A and B according to Child-Pugh classification) should be administered with caution, the dose should not exceed 40 mg 1 time / day.
The preparation Telzap ® is contraindicated in patients with severe hepatic insufficiency (class C according to the Child-Pugh classification) .
Older patients do not need a dose adjustment.

The use of the preparation of Tazap ® in children and adolescents under the age of 18 is contraindicated because of the lack of safety and efficacy data.

SIDE EFFECT

According to the WHO, unwanted 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 available data, it was not possible to establish the frequency of occurrence.
Within each group according to the incidence of adverse reactions are presented in descending order of severity.

Infectious and parasitic diseases: infrequent - urinary tract infections, including cystitis, upper respiratory tract infections, including pharyngitis and sinusitis;
rarely - sepsis, incl. with a lethal outcome.
From the hemopoietic system: infrequently - anemia;
rarely - eosinophilia, thrombocytopenia.
From the immune system: rarely - anaphylactic reaction, hypersensitivity.

From the side of metabolism: infrequently - hyperkalemia;
rarely - hypoglycemia (in patients with diabetes mellitus).
Mental disturbances: infrequently - insomnia, depression;
rarely - anxiety.
From the nervous system: infrequently - fainting;
rarely - drowsiness.
From the side of the organ of vision: rarely - visual disorders.

From the side of the organ of hearing and labyrinthine disturbances: infrequently - vertigo.

From the side of the cardiovascular system: infrequently - bradycardia, excessive reduction of blood pressure, orthostatic hypotension;
rarely - tachycardia.
From the respiratory system: infrequently - shortness of breath, cough;
very rarely - interstitial lung disease.
From the gastrointestinal tract: infrequently - abdominal pain, diarrhea, dyspepsia, flatulence, vomiting;
rarely - dry mouth, discomfort in the stomach, a violation of taste.
From the liver and biliary tract: rarely - a violation of liver function / liver damage.

From the skin and subcutaneous tissues: infrequently - skin itching, hyperhidrosis, rash;
rarely - angioedema (also fatal), eczema, erythema, urticaria, drug rash, toxic skin rash.
From the musculoskeletal system: infrequently - ischialgia, muscle spasms, myalgia;
rarely - arthralgia, pain in the limbs, tendenitis-like syndrome.
From the urinary system: infrequently - a violation of kidney function, including acute renal failure.

From laboratory and instrumental studies: infrequently - an increase in the concentration of creatinine in the blood plasma;
rarely - reduction of hemoglobin, increased uric acid in the blood plasma, increased activity of hepatic enzymes and CK.
Other: infrequently - chest pain, asthenia;
rarely - flu-like syndrome.
CONTRAINDICATIONS

- Obstructive diseases of the biliary tract;

- severe violations of liver function (class C according to the Child-Pugh classification);

- joint use with aliskiren in patients with diabetes mellitus or severe renal dysfunction (GFR less than 60 ml / min / 1.73 m 2 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.

Caution should be given to the drug in bilateral stenosis of the renal arteries or stenosis of the artery of a single functioning kidney;
impaired renal function; light and moderate violations of liver function; reduction of BCC against the background of previous intake of diuretics, restriction of consumption of table salt, diarrhea or vomiting; hyponatremia; hyperkalemia; condition after kidney transplantation (no experience of application); severe chronic heart failure; stenosis of the aortic and mitral valve; hypertrophic obstructive cardiomyopathy; primary hyperaldosteronism (efficacy and safety not established); patients Negroid race.
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 Tazap ® is contraindicated during pregnancy.
If prolonged treatment with Telzap ® is necessary, the patient planning a pregnancy should choose an alternative antihypertensive drug with a proven safety profile during pregnancy.
After establishing the fact of pregnancy, treatment with Tazap ® should be stopped immediately and, if necessary, started alternative treatment.
As the results of clinical observations have shown, the use of angiotensin II receptor antagonists in the II and III trimesters 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 II receptor antagonists are used, ultrasound of the kidneys and fetal skull is recommended in the second trimester of pregnancy. Children whose mothers took angiotensin II receptor antagonists during pregnancy should be carefully monitored to detect arterial hypotension.
Information on the use of telmisartan during breastfeeding is absent.
The use of the preparation 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.
APPLICATION FOR FUNCTIONS OF THE LIVER

Caution should be given to the drug in bilateral stenosis of the renal arteries or stenosis of the artery of a single functioning kidney;
impaired renal function; condition after kidney transplantation (no experience of application).
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Contraindicated use of the drug in obstructive diseases of the biliary tract;
severe violations of liver function (class C according to the Child-Pugh classification).
With caution should prescribe the drug for light and moderate violations of the liver.

APPLICATION FOR CHILDREN

Contraindicated in the use of drugs 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 preparation Telzap ® 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), the preparation should be used with caution.
Renovascular hypertension

When treating with RAAS-acting drugs, patients with bilateral stenosis of the renal arteries or stenosis of the artery of a single functioning kidney are at increased risk for severe arterial hypotension and renal insufficiency.

Impaired renal function and kidney transplantation

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

Symptomatic arterial hypotension, especially after the first administration of the preparation, can occur in patients with reduced BCC and / or sodium content in 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 preparation of Tazap ® .
Double blockade of RAAS

The concomitant use of telmisartan with aliskiren is contraindicated in patients with diabetes mellitus or renal insufficiency (GFR <60 ml / min / 1.73 m 2 body surface area).

The simultaneous use of telmisartan 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 (including acute renal failure) were noted in patients who were predisposed to this, especially when several drugs were 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 depending vascular tone and renal function preferably from RAAS activity (e.g., patients with chronic heart failure or renal diseases, including renal artery stenosis or artery stenosis single kidney), designation drugs affecting this system may accompanied by the development of acute arterial hypotension, hyperasotemia, oliguria, and in rare cases acute renal failure.
Primary hyperaldosteronism
Patients with primary hyperaldosteronism treatment antihypertensive drugs whose action is effected by inhibition of the RAAS usually inefficient. In connection with this use of the drug Telzap ® not recommended.
Stenosis of the aortic and mitral valves, hypertrophic obstructive cardiomyopathy
As with other vasodilators patients with aortic or mitral stenosis and hypertrophic obstructive cardiomyopathy in applying Telzap preparation ® must be particularly careful.
Patients with diabetes treated with insulin or hypoglycemic agents for oral administration
The treatment drug Telzap ® such patients hypoglycemia can occur. It should enhance glycemic control, as It may be necessary to dose adjustment of insulin or hypoglycemic agents.
hyperkalemia
The use of drugs acting on the RAAS can cause hyperkalemia. Elderly patients, patients with renal insufficiency or diabetes, patients taking medications that enhance the potassium content in the blood plasma, and / or in patients with concomitant diseases hyperkalemia may lead to death.
When deciding on the concomitant use of drugs acting on the RAAS, it is necessary to weigh the risks and benefits. The main risk factors for hyperkalaemia to be considered are:
- Diabetes mellitus, renal impairment, age (patients older than 70 years);
- a combination with one or more drugs acting on the RAAS and / or potassium-containing food additives. Therapeutic drugs or classes of drugs that can cause hyperkalemia are salt substitutes containing potassium, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, NSAIDs (including selective COX-2 inhibitors), heparin, immunosuppressants (cyclosporin or tacrolimus), and trimethoprim;
- intercurrent illness, particularly dehydration, acute heart failure, metabolic acidosis, impaired renal function, cytolysis syndrome (e.g., acute limb ischemia, rhabdomyolysis, extensive trauma).
Patients at risk should carefully monitor the content of potassium in the blood plasma.
Sorbitol
drug Telzap ® contains sorbitol (E420). Patients with rare hereditary fructose intolerance should not take the drug.
Ethnic differences
As noted ACE inhibitors, telmisartan and other antagonists of angiotensin II receptors, apparently less effective in lowering blood pressure in patients blacks than in people of other races, possibly due to the greater susceptibility to reduction renin activity in the population of these patients.
Other

As with other antihypertensives, excessive lowering of blood pressure in patients with ischemic heart disease or ischemic cardiomyopathy can lead to myocardial infarction or stroke.
Impact on the ability to drive vehicles and manage mechanisms

Special clinical studies on the effect of the drug on the ability to drive and not carried out mechanisms. When driving and operating machinery that require high concentration of attention, care must be taken because against the background of the drug Telzap ® may rarely occur dizziness and drowsiness.
OVERDOSE

Symptoms: The most prominent manifestations of overdose were an excessive fall in blood pressure and tachycardia; also reported bradycardia, dizziness, increase in the concentration of serum creatinine, and acute renal failure.
Treatment:Patients should be closely monitored and the condition being symptomatic and supportive treatment. The approach to treatment depends on the elapsed time after drug administration, and the severity of symptoms. Recommended actions include induced vomiting and / or gastric lavage, administration of activated charcoal expedient. Should regularly monitor the content of electrolytes and creatinine in the blood plasma. When excessive decrease in blood pressure, patients should take a horizontal position with raised legs, with the need to quickly fill the BCC and the lack of electrolytes. Telmisartan is not displayed by hemodialysis.
DRUG INTERACTION

Dual blockade of the RAAS
Concomitant use of telmisartan with aliskiren is contraindicated in patients with diabetes or renal failure (GFR of less than 60 ml / min / 1.73 m 2 body surface area) and is not suitable for other patients.
The simultaneous use of telmisartan and ACE inhibitors is contraindicated in patients with diabetic nephropathy.
Data from clinical studies have shown that dual blockade of the RAAS due to the combined use of ACE inhibitors, angiotensin II receptor antagonists or aliskiren is associated with increased incidence of adverse effects, such as hypotension, hyperkalaemia and renal function (including acute renal failure) as compared with the use of only one a drug acting on the RAAS.
hyperkalemia
The risk of hyperkalemia can increase when combined with other drugs capable of causing hyperkalemia (kalisodergaszczye supplements and salt substitutes containing potassium, potassium-sparing diuretics (e.g., spironolactone, eplerenone, triamterene or amiloride), NSAIDs (including selective COX-2) , heparin, immunosuppressants (cyclosporin or tacrolimus), and trimethoprim). If necessary, against the background of documented hypokalemia combined use of drugs should be undertaken with caution and regular monitoring of the content of potassium in the blood plasma.
Digoxin
When combined with digoxin telmisartan average increase was observed C max of digoxin in blood plasma by 49% and C min20%. At the beginning of treatment, at dose selection and termination of treatment with telmisartan should carefully monitor the concentration of digoxin in the blood plasma to maintain it within the therapeutic range.
Potassium-sparing diuretics or kalisodergaszczye supplements
antagonists of angiotensin II receptors, such as telmisartan, reduce the loss of potassium caused by diuretics. Potassium-sparing diuretics (e.g., spironolactone, eplerenone, amiloride or triamterene) kalisodergaszczye supplements or salt substitutes can lead to significant increase of potassium in the blood plasma. If concomitant use is indicated because there is documented hypokalaemia, they should be used with caution and on a background of regular monitoring of potassium in the blood plasma.
of lithium drugs
When the joint application of drugs lithium with ACE inhibitors and angiotensin II receptor antagonists, including telmisartan, arise reversible increases lithium concentration in the blood plasma and its toxic action. If necessary, the application of this combination of drugs is recommended to carefully control the concentration of lithium in the blood plasma.
NSAIDs
NSAIDs (i.e., acetylsalicylic acid at doses used for anti-inflammatory treatment, COX-2 inhibitors and the nonselective NSAIDs) may reduce the antihypertensive effect of angiotensin II receptor antagonists. In some patients with impaired renal function (e.g., patients with dehydration, elderly patients with impaired renal function) combined use of angiotensin II receptor antagonists and drugs which depress the COX-2 may lead to further deterioration of renal function, including the development of acute renal failure, which usually it is reversible. Therefore, the combined use of drugs should be performed with caution, especially in elderly patients. It is necessary to ensure an adequate flow of fluid, in addition,at the beginning of a joint application and periodically thereafter should monitor renal function.
Diuretics (thiazide or "loop")
Previous treatment with diuretics at higher doses, such as furosemide ( "loop" diuretics) and hydrochlorothiazide (thiazide diuretic) may lead to hypovolemia and hypotension risk of early treatment with telmisartan.
Other antihypertensives
effect of telmisartan may be increased by concomitant use of other antihypertensive drugs.
Based on pharmacological properties, baclofen and amifostine can be assumed that they will enhance the therapeutic effect of antihypertensive agents including telmisartan. Furthermore, orthostatic hypotension can be amplified in the background of ethanol, barbiturates, narcotics or antidepressants.
Corticosteroids (for systemic use)
Corticosteroids weaken the effect of telmisartan.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children at a temperature of no higher than 25 ° C.
Shelf life - 2 years.
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