Telzap tabs 80mg #90

Telzap instruction

You can buy Telzap here

COMPOSITION

Each 40 mg tablet contains:
active ingredient: telmisartan - 40,000 mg; auxiliary
substances: meglumine - 12,000 mg, sorbitol - 162,200 mg, sodium hydroxide -3,400 mg, povidone 25-20,000 mg, magnesium stearate - 2,400 mg.
Each 80 mg tablet contains: active ingredient: Telmisartan - 80,000 mg;
excipients: meglumine - 24,000 mg, sorbitol - 324,400 mg, sodium hydroxide - 6,800 mg, povidone 25 - 40,000 mg, magnesium stearate - 4,800 mg.

DESCRIPTION

Tablets 40 mg: oblong, biconvex tablets from almost white to yellowish color on both sides.
Tablets of 80 mg: oblong, biconvex tablets from almost white to yellowish color with an engraving "80" on one side.
PHARMACOTHERAPY GROUP
Angiotensin II receptor antagonist.
ATX code: C09SA07.

Pharmacodynamics

Telmisartan is a specific angiotensin II receptor antagonist (ARAP) (type ATi) that is effective for ingestion. Telmisartan has a very high affinity for AT | -receptors, through which the action of angiotensin II is realized. It displaces angiotensin II from its association with the receptor, not having the action of an agonist on this receptor. Telmisartan binds only to the AT subtype of angiotensin II. Communication is sustainable. Telmisartan 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 over-stimulation with angiotensin II, the concentration of which increases with the administration of telmisartan, has 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 angiotensin-converting enzyme (ACE) (kininase II), which also catalyzes the breakdown of bradykinin. This avoids the side effects associated with the action of bradykinin (for example, a dry cough).

Essential Hypertension

In patients with telmisartan in a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. The onset of the antihypertensive effect is noted within 3 hours after the first dose of telmisartan. The effect of Telzap lasts for 24 hours and remains clinically significant up to 48 hours. A pronounced antihypertensive effect usually develops 4-8 weeks after regular use.
In patients with arterial hypertension, telmisartan reduces systolic and diastolic blood pressure (BP), without affecting the heart rate (HR).
In the case of abrupt cessation of taking telmisartan blood pressure over several days, it gradually returns to its original level without the development of the "cancellation" 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 compared with the use of telmisartan, in contrast to ACE inhibitors.

Prevention of cardiovascular diseases

Patients aged 55 years and older with ischemic heart disease, stroke, transient ischemic attack, peripheral artery disease, or complications of type 2 diabetes (for example, retinopathy, left ventricular hypertrophy, macro- or microalbuminuria) with a history of heart disease. -vascular events, telmisartan had an effect similar to the effect of ramipril on reducing the combined end point: cardiovascular mortality from non-fatal myocardial infarction, stroke without death or hospitalization due to chronic heart failure.
Telmisartan was as effective as ramipril in reducing the frequency of secondary points: cardiovascular mortality, non-fatal myocardial infarction, or non-fatal stroke. Dry cough and angioedema were less frequently described in patients receiving telmisartan as opposed to ramipril, while arterial hypotension occurred more frequently in patients receiving telmisartan.

Patients of childhood and adolescence

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

Pharmacokinetics

Suction

When ingested, Telmisartan is rapidly absorbed from the gastrointestinal tract. Bioavailability - 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). After 3 hours after administration, the plasma concentration levels out, independently, whether telmisartan was taken at the same time as a meal or not. There is a difference in plasma concentrations in men and women. Stax (maximum concentration) and AUC were approximately 3 and 2 times, respectively, higher in women compared to men without a significant effect on efficacy.
There is no linear relationship between the dose of the drug and its plasma concentration. Stah and, to a lesser extent, AUC increase disproportionately with increasing doses when using doses higher than 40 mg per day.

Distribution

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

Metabolism

Metabolized by conjugation with glucuronic acid. Conjugate does not possess pharmacological activity.

Removal

The half-life (T. / 2) is more than 20 hours. Excreted through the intestine in unchanged form, the excretion by the kidneys - less than 1%. The total plasma clearance is high (about 1000 ml / min) compared with the “hepatic” blood flow (about 1500 ml / min).

Elderly patients

The pharmacokinetics of telmisartan in elderly patients over 65 years of age does not differ from younger patients. Dose adjustment is not required. Patients with impaired renal function
In patients with mild and moderate renal impairment, a dose adjustment of telmisartan is not required. Patients with severe renal insufficiency and patients on hemodialysis are recommended to have a lower initial dose of 20 mg per day (see section "Special Instructions").
Telmisartan is not excreted by hemodialysis.

Patients with impaired liver function

In patients with mild and moderate hepatic impairment (Child-Pugh class A and B), the daily dose of Telzap should not exceed 40 mg.

INDICATIONS FOR USE

• essential hypertension;
• reducing mortality and cardiovascular disease in adult patients:
- with cardiovascular diseases of atherothrombotic genesis (ischemic heart disease, stroke, or a history of peripheral artery disease);
- with type 2 diabetes mellitus with target organ damage.

CONTRAINDICATIONS

• hypersensitivity to the active substance or any excipients of the drug;
• pregnancy and breastfeeding period;
• obstructive diseases of the biliary tract;
• severe liver dysfunction (Child-Pugh class C);
• combined use with aliskiren in patients with diabetes mellitus or severe impaired renal function (glomerular filtration rate [GFR] less than 60 ml / min / 1.73 m2 of body surface area) (see the sections “Interaction with other drugs” and “Special instructions ");
• hereditary intolerance to fructose (due to the presence of sorbitol in the composition of the tablet);
• simultaneous use with inhibitors of angiotensin-converting enzyme (ACE inhibitors) in patients with diabetic nephropathy (see sections "Interaction with other drugs" and "Special instructions");
• age up to 18 years (efficacy and safety have not been established).

CAREFULLY

Telzap should be prescribed with caution in the following conditions / diseases:
• bilateral renal artery stenosis or arterial stenosis of a single functioning kidney;
• impaired renal function;
• mild and moderate liver dysfunction;
• a decrease in circulating blood volume (BCC) against the background of previous diuretic intake, restriction of salt, diarrhea or vomiting;
• hyponatremia;
• hyperkalemia;
• condition after kidney transplantation (no experience);
• severe chronic heart failure;
• stenosis of the aortic and mitral valve;
• hypertrophic obstructive cardiomyopathy;
• primary hyperaldosteronism (efficacy and safety have not been established);
• use in patients of the Negroid race.

USE IN PREGNANCY AND DURING BREASTFEEDING

Pregnancy

Currently, reliable information on the safety of telmisartan in pregnant women is not available. In animal studies, the reproductive toxicity of Telzap was identified. Use of the drug Telzap is contraindicated during pregnancy (see section "Contraindications").
If you need long-term treatment with Telzap, patients planning a pregnancy should choose an alternative antihypertensive drug with a proven safety profile during pregnancy. After the establishment of the fact of pregnancy, treatment with Telzap should be stopped immediately and, if necessary, alternative treatment can be started.
The results of clinical observations showed that the use of ARAP during the second and third trimesters of pregnancy has a toxic effect on the fetus (deterioration of renal function, oligohydramnios, delayed ossification of the skull) and the newborn (renal insufficiency, hypotension and hyperkalemia). When applying ARAN during the second trimester of pregnancy, an ultrasound of the kidneys and the fetal skull is recommended.
Children whose mothers took ARAP during pregnancy should be carefully monitored for hypotension.

Breastfeeding period

Information on the use of telmisartan during breastfeeding is not available. Taking Telzap during breastfeeding is contraindicated (see section “Contraindications”); an alternative antihypertensive drug with a more favorable safety profile should be used, especially when feeding a newborn or premature baby.

METHOD OF ADMINISTRATION AND DOSES

Telzap is taken orally once a day with a liquid, regardless of the meal.

Arterial hypertension

The initial recommended dose of Telzap is 1 tablet (40 mg) once a day. Some patients may be effective in taking 20 mg per day. A dose of 20 mg can be obtained by dividing a 40 mg tablet in half over the risk. In cases where the therapeutic effect is not achieved, the recommended dose of Telzap may be increased to a maximum of 80 mg once a day. Alternatively, Telzap can be taken in combination with thiazide diuretics, for example, hydrochlorothia azide, which, when used together, had an additional antihypertensive effect. When deciding whether to increase the dose should be taken into account that the maximum antihypertensive effect is usually achieved within 4-8 weeks after the start of treatment.
Reducing mortality and the frequency of cardiovascular diseases The recommended dose of Telzap is 80 mg 1 time per day.
In the initial period of treatment, it is recommended to monitor the level of blood pressure (BP), may require correction of antihypertensive therapy.

Patients with impaired renal function

Experience with telmisartan in patients with severe renal failure or patients on hemodialysis is limited. A lower initial dose of 20 mg per day is recommended for these patients (see section “Special services”). For patients with mild and moderate renal impairment, dose adjustment is not required.
Concomitant use of Telzap with aliskiren is contraindicated in patients with renal insufficiency (GFR less than 60 ml / min / 1.73 m2 of body surface area) (see section “Contraindications”).
The simultaneous use of the drug Telzap with an ACE inhibitor is contraindicated in patients with diabetic nephropathy (see section “Contraindications”). Patients with impaired liver function
Telzap is contraindicated in patients with severe hepatic insufficiency (Child-Pugh class C) (see the “Contraindications” section). In patients with mild and moderate hepatic insufficiency (class A and B according to Child-Pugh classification, respectively), Telzap is administered with caution, the dose should not exceed 40 mg once a day (see section “With caution”).

Elderly patients

Elderly patients do not require dose adjustment.

Children and adolescents

The use of Telzap in children and adolescents under 18 years of age is contraindicated due to the lack of data on safety and efficacy (see section “Contraindications”).

Side effects of Telzap

According to the World Health Organization (WHO), undesirable 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 / 1,000 to <1/100), rarely (from> 1 / 10,000 to <1 / 1,000), very rarely (<1 / 10,000); frequency is unknown - according to the available data it was not possible to establish the frequency of occurrence.
Within each group, according to the frequency of occurrence, undesirable reactions are presented in order of decreasing severity.
Infectious and parasitic diseases
uncommon: urinary tract infections, including cystitis, upper respiratory tract infections, including pharyngitis and sinusitis; •
rarely: sepsis, including fatal.
Violations of the blood and lymphatic system
infrequently: anemia; rarely: eosinophilia, thrombocytopenia.
Immune system disorders
seldom: anaphylactic reaction, hypersensitivity.
Metabolic and nutritional disorders
infrequently: hyperkalemia; rarely: hypoglycemia (in patients with diabetes).
Mental disorders:
infrequently: insomnia, depression; rarely: anxiety.
Nervous system disorders
infrequently: fainting; rarely: drowsiness.
Violations by the organ of vision
rarely: visual disturbances.
Disturbances from an organ of hearing and labyrinth disturbances
infrequently: vertigo.
Cardiac disorders rarely: bradycardia; seldom: tachycardia.
Vascular disorders
infrequently: pronounced decrease in blood pressure, orthostatic hypotension.
Disorders of the respiratory system, chest and mediastinum
infrequently: shortness of breath, cough; very rare: interstitial lung disease. Disorders of the gastrointestinal tract
infrequently: abdominal pain, diarrhea, dyspepsia, flatulence, vomiting; rarely: dry mouth, discomfort in the stomach, a violation of taste. Disorders of the liver and biliary tract
rarely: liver dysfunction / liver damage.
Violations of the skin and subcutaneous tissues
infrequently: pruritus, hyperhidrosis, rash; rarely: angioedema (also fatal), eczema, erythema, urticaria, drug rash, toxic skin rash.
Disorders of the musculoskeletal and connective tissue
infrequently: back pain (ischialgia), muscle spasms, myalgia;
rarely: arthralgia, pain in the limbs, pain in the tendons
(tendenta-like syndrome).
Kidney and urinary tract disorders
infrequently: impaired renal function, including acute renal
failure.
General disorders and disorders at the site of administration
infrequently: chest pain, asthenia (weakness); seldom: flu-like syndrome. Impact on the results of laboratory and instrumental studies
infrequently: increased plasma creatinine concentration; rarely: a decrease in the hemoglobin content, an increase in the uric acid content in the blood plasma, an increase in the activity of “liver” enzymes and creatine phosphokinase (CPK).

OVERDOSE

Symptoms: The most pronounced manifestations of overdose were a pronounced decrease in blood pressure and tachycardia, also reported bradycardia, dizziness, increased serum creatinine concentration and acute renal failure.
Treatment: Telmisartan is not excreted by hemodialysis. Patients should be carefully monitored and symptomatic as well as supportive treatment should be carried out. The approach to treatment depends on the time elapsed after taking the drug, and the severity of symptoms. Recommended interventions include provoking vomiting and / or gastric lavage, it is advisable to receive activated charcoal. It should regularly monitor the content of electrolytes and creatinine in the blood plasma. When a pronounced decrease in blood pressure occurs, the patient should take a horizontal position with the legs elevated, and it is necessary to quickly fill in the volume of the BCC and electrolytes.

INTERACTION WITH OTHER MEDICINES

Dual Blokadarenin-angiotensin-aldosterone system (RAAS) The concomitant use of telmisartan with aliskiren is contraindicated in patients with diabetes or renal failure (GFR less than 60 ml / min / 1.73 m2 of body surface area) and is not recommended for other patients.
Simultaneous use of telmisartan and ACE inhibitors is contraindicated in patients with diabetic nephropathy (see section "Contraindications").
Data from clinical studies have shown that double blockade of RAAS due to the combined use of ACE inhibitors, ARAP or aliskiren is associated with an increased incidence of adverse events, such as arterial hypotension, hyperkalemia and renal impairment (including acute renal failure) in comparison with the use of only one drug, acting on the RAAS.
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), non-steroidal anti-inflammatory drugs (NSAIDs, including selective inhibitors cyclooxygenase-2 (COX-2)), heparin, immunosuppressants (cyclosporin or tacrolimus), and trimethoprim). If necessary, against the background of documented hypokalemia, the combined use of drugs should be carried out with caution and regularly monitor the content of potassium in the blood plasma.

Digoxin

When co-administration of telmisartan with digoxin, the average increase in Stax digoxin in plasma was noted by 49% and the minimum concentration by 20%. At the beginning of treatment, when selecting a dose and stopping treatment with telmisartan, the concentration of digoxin in the blood plasma should be carefully controlled to maintain it within the therapeutic range.
Potassium-sparing diuretics or potassium-containing dietary supplements Angiotensin II receptor antagonists, such as telmisartan, reduce potassium-induced diuretic loss. Potassium-sparing diuretics, for example, spironolactone, eplerenone, triamterene or amiloride, potassium-containing dietary supplements or salt substitutes can lead to a significant increase in plasma potassium. If concomitant use is indicated, since there is documented hypokalemia, they should be used with caution and against the background of regular monitoring of potassium in the blood plasma.

Lithium preparations

When lithium preparations were taken together with ACE inhibitors and ARAP, including telmisartan, there was a reversible increase in plasma concentrations of lithium and its toxic effect. If necessary, the use of this combination of drugs is recommended to carefully monitor the concentration of lithium in the blood plasma.

Nonsteroidal anti-inflammatory drugs (NSAIDs)

NSAIDs (ie, acetylsalicylic acid in doses used for anti-inflammatory treatment, COX-2 inhibitors and non-selective NSAIDs) can weaken the antihypertensive effect of ARAP. In some patients with impaired renal function (for example, patients with dehydration, elderly patients with impaired renal function), the combined use of ARAP and drugs that inhibit cyclooxygenase -2 can lead to further deterioration of renal function, including the development of acute renal failure, which, as a rule is reversible. Therefore, the joint use of drugs should be carried out with caution, especially in elderly patients. Adequate fluid intake should be ensured, in addition, at the beginning of the joint application and periodically in the future, indicators of renal function should be monitored.

Diuretics (thiazide or "loop")

Previous treatment with high doses of diuretics, such as furosemide (“loopback” diuretic) and hydrochlorothiazide (thiazide diuretic), can lead to hypovolemia and the risk of developing hypotension at the beginning of treatment with telmisartan.

Other antihypertensive drugs

The effect of telmisartan may be enhanced by the combined 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 drugs, including telmisartan. In addition, orthostatic hypotension may increase with alcohol intake, barbiturates, narcotic drugs or antidepressants.

Corticosteroids (for systemic use)

Corticosteroids weaken the effect of telmisartan.

SPECIAL INSTRUCTIONS

Liver dysfunction

The use of Telzap is contraindicated in patients with cholestasis, obstruction of the biliary tract, or severe liver dysfunction (Child-Pugh class C) (see section “Contraindications”), since telmisartan is mainly excreted in the bile. It is believed that in such patients the hepatic clearance of telmisartan is reduced. In patients with mild or moderate liver function abnormalities (class A and B according to Child-Pugh classification), Telzap should be used with caution (see section “With caution”.

Renovascular hypertension

When treating drugs acting on the RAAS, in patients with bilateral renal artery stenosis or arterial stenosis of a single functioning kidney, the risk of severe arterial hypotension and renal failure increases.

Impaired renal function and kidney transplantation

When using the drug Telzap in patients with impaired renal function, periodic monitoring of the content of potassium and creatinine in blood plasma is recommended. There is no experience with the clinical use of Telzap in patients who have recently had a kidney transplant.

Reduction in circulating blood volume (BCC)

Symptomatic arterial hypotension, especially after the first dose of TE3EOR, may occur in patients with reduced BCC and / or sodium in the blood plasma on the background of previous treatment with diuretics, limitation of salt, diarrhea or vomiting.
Similar conditions (lack of liquid and / or sodium) should be eliminated before taking Telzap.
Double blockade of the renin-angiotensin-aldosterone system The concomitant use of telmisartan with aliskiren is contraindicated in patients with diabetes or renal failure (GFR less than 60 ml / min / 1.73 m2 of body surface area) (see the section "Contraindications").
Simultaneous use of telmisartan and ACE inhibitors is contraindicated in patients with diabetic nephropathy (see section "Contraindications").
As a result of inhibition of the RAAS, arterial hypotension, syncope, hyperkalemia and impaired renal function (including acute renal failure) in susceptible patients were noted, especially when several drugs were used together, also acting on this system. Therefore, a double blockade of the RAAS (for example, against the background of taking telmisartan with other RAAS antagonists) is not recommended.
In cases of dependence of the vascular tone and kidney function, mainly on the activity of the RAAS (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 affecting this system can accompanied by the development of acute arterial hypotension, hyperasotemia, oliguria, and in rare cases, acute renal failure.

Primary hyperadosteronism

In patients with primary hyperaldosteronism, treatment with antihypertensive drugs, which are mediated by inhibition of the RAAS, is usually ineffective. In this regard, the use of the drug Telzap is not recommended.
Stenosis of the aortic and mitral valves, hypertrophic obstruction of the cardiovascular system and myopathy
As with other vasodilators, patients with aortic or mitral stenosis, as well as hypertrophic obstructive cardiomyopathy, when using TEZESG should be especially careful.

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

During treatment with Telzap, hypoglycemia may occur in these patients. In such patients, glycemia control should be enhanced, as it may be necessary to adjust the dose of insulin or hypoglycemic agent.

Hypercalcium

Taking medicines acting on the RAAS can cause hyperkalemia. In elderly patients, patients with renal insufficiency or diabetes mellitus, patients also taking medications that increase the plasma content of potassium, and / or patients with concomitant diseases, hyperkalemia can be fatal.
When deciding on the concomitant use of drugs acting on the RAAS, it is necessary to evaluate the risk-benefit ratio. The main risk factors for the development of hyperkalemia that should be considered are:
• diabetes mellitus, renal failure, age (patients older than 70 years);
• combination with one or more drugs acting on the RAAS, and / or potassium-containing food additives. Drugs or therapeutic classes of drugs that can cause hyperkalemia are salt substitutes containing potassium, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, non-steroidal anti-inflammatory drugs (NSAIDs, including selective COX-2 inhibitors, heparin, IOC,), heparin, IOC,), heparin, IOC,), heparin, IOC,), heparin, IOC,), heparin, IOC,), heparin, IOC, I, I, I, I, I, I, I, II, I, I, I, II, I, I, I, I, I, I, I, I, I,… (cyclosporine or tacrolimus) and trimethoprim;
• intercurrent diseases, especially dehydration, acute heart failure, metabolic acidosis, impaired renal function, cytolysis syndrome (for example, acute limb ischemia, rhabdomyolysis, extensive trauma).
Patients at risk are advised to carefully monitor their potassium in the blood plasma (see the section "Interaction with other drugs").

Sorbitol

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

Ethnic differences

As noted for ACE inhibitors, telmisartan and other ARAP seem to be less effective in lowering blood pressure in patients of the Negroid race than in other races, possibly due to a greater propensity to decrease renin activity in the population of these patients.

Other

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

INFLUENCE ON THE ABILITY TO MANAGE THE VEHICLES, MECHANISMS

Special clinical studies on the effect of the drug on the ability to drive and mechanisms were not conducted. When driving and working with mechanisms that require increased concentration of attention, caution should be exercised, since dizziness and drowsiness can rarely occur while taking Telzap.

FORM OF ISSUE

Tablets, 40 mg, 80 mg.
On 10 tablets in the blister from OPA / Alyu / PVC / Alyu. 3, 6 or 9 blisters are placed in a cardboard box along with instructions for use.

STORAGE CONDITIONS

Store at a temperature not higher than 25 ° С.
Keep out of the reach of children.
Shelf life - 2 years.
Do not use after the expiration date printed on the package.

Terms of sell

You can buy Telzap without a prescription.