Telpres pills 40mg, 56pcs

Composition

Each 40 mg tablet contains:  

Active ingredient:  telmisartan – 40.00 mg;

excipients:  

sodium hydroxide-3.40 mg,

povidone-K 25-10.80 mg,

meglumine-12.00 mg,

mannitol-163.80 mg,

magnesium stearate-4.00 mg,

crospovidone – 6.00 mg

Pharmacological action

Telmisartan is a specific angiotensin II receptor antagonist (type AT1) effective when taken orally. It has a high affinity for the AT1 subtype of angiotensin II receptors through which the action of angiotensin II is realized.

Displaces angiotensin II from binding to the receptor without having an agonist effect on this receptor. Telmisartan binds only to the AT1 subtype of angiotensin II receptors. The relationship is long-term. It has no affinity for other receptors, including the AT2 receptor and other less well-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 when telmisartan is prescribed, have not been studied. Reduces the concentration of aldosterone in the blood does not inhibit renin in the 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, an increase in 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 use of telmisartan. The effect of the drug persists for 24 hours and remains significant for up to 48 hours. A pronounced antihypertensive effect usually develops 4 weeks after regular use of the drug.

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

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

Pharmacokinetics:

Suction

When taken orally, it is rapidly absorbed from the gastrointestinal tract. Bioavailability is about 50%. When taken simultaneously with food, the decrease in AUC (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 equalized regardless of food intake.

Distribution

The relationship with plasma proteins is 995%, mainly with albumin and alpha-1 glycoprotein. The average apparent volume of distribution at equilibrium concentration is 500 liters.

Metabolism

It is metabolized by conjugation with glucuronic acid. The metabolites are pharmacologically inactive.

Deduction

The half-life (T 1/2) is more than 20 hours. Excreted through the intestines in unchanged form, excretion by the kidneys is less than 2% of the dose taken. Total plasma clearance is high (900 ml / min) compared to “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 higher, respectively, in women compared to men, with no significant effect on efficacy. No dose adjustment is required.

Elderly patients

The pharmacokinetics of telmisartan in elderly patients do not differ from the pharmacokinetics in young patients. No dose adjustment is required.

Patients with impaired renal function

No dose adjustment of telmisartan is required in patients with mild to moderate renal impairment.

A lower initial dose of 20 mg / day is recommended for patients with severe renal insufficiency and patients undergoing hemodialysis.

Telmisartan is not eliminated by hemodialysis.

Patients with impaired liver function

Pharmacokinetic studies in patients with hepatic insufficiency have shown an increase in the absolute bioavailability of telmisartan to almost 100%.

With hepatic insufficiency, T 1/2 does not change. In patients with mild to moderate hepatic impairment (Child-Pugh class A and B), the daily dose of the drug should not exceed 40 mg.

Indications

-Arterial hypertension;

– Reduction of cardiovascular morbidity and mortality in patients aged 55 years and older with a high risk of cardiovascular diseases.

Use during pregnancy and lactation

Drugs that directly affect the RAAS can cause serious damage and death to the developing fetus so when planning or establishing the fact of pregnancy, the drug should be immediately discontinued and, if necessary, an alternative antihypertensive therapy should be prescribed that has an established safety profile for use during pregnancy.

The use of the drug during pregnancy is contraindicated.

In preclinical studies of telmisartan, no teratogenic effects were detected, but fetotoxicity was established.

It is known that exposure to angiotensin II receptor antagonists during the second and third trimesters of pregnancy causes fetotoxicity in humans (decreased renal function, oligohydramnios, slowing of cranial ossification) and neonatal toxicity (renal failure, hypotension, hyperkalemia).

Patients planning pregnancy should be prescribed alternative therapy. If treatment with angiotensin II receptor antagonists occurred during the second trimester of pregnancy, ultrasound examination of the fetal kidney function and skull condition is recommended.

Newborns whose mothers have received angiotensin II receptor antagonists should be carefully monitored for hypotension.

Telpres therapy is contraindicated during breastfeeding. Studies of the effect on human fertility have not been conducted.

Contraindications

– Hypersensitivity to the Active ingredient or auxiliary components of the drug;

– Pregnancy;

– the Period of breastfeeding;

– Obstructive disease of the biliary tract;

Severe disturbances of liver function (class C child-Pugh);

– Simultaneous use of the drug Telpas with aliskiren in patients with diabetes mellitus and/or impaired renal function (glomerular filtration rate less than 60 ml/min/173 m 2);

– Simultaneous use of ACE inhibitors in patients with diabetic nephropathy;

– Age up to 18 years (efficacy and safety not established).

With caution:

– Bilateral renal artery stenosis or stenosis of the artery to a solitary kidney;

– Disorders of liver function and/or kidney (see “Special instructions”);

– Condition after kidney transplantation (experience of missing);

– Reduced volume of circulating blood (BCC) as a result of prior diuretic therapy, restriction of salt diarrhea or vomiting;

– Hyponatremia;

– Hyperkalemia;

– Chronic heart failure;

Ischemic heart disease;

– stenosis of the aortic and mitral valve;

– Idiopathic hypertrophic subaortic stenosis (hypertrophic obstructive cardiomyopathy);

– Primary aldosteronism (efficacy and safety not established);

– the Simultaneous use of ACE inhibitors or aliskiren;

– Simultaneous use with potassium supplements and potassium-sparing diuretics;

– diabetes.

Side effects

In general, the incidence of adverse reactions reported for telmisartan is comparable to that for placebo. The observed cases of side effects did not correlate with the gender, age, or race of the patients. Classification of the frequency of adverse reactions of the World Health Organization( WHO): very common (>1/10); common (>>1/100 to >><1/10); infrequent (>1/1000 to <1/10); infrequent (><1/100); rare (>1/10 000 to <1/100); rare (><1/1000); very rare (from

Infectious and parasitic diseases:

infrequently: upper respiratory tract infections, including pharyngitis and sinusitis urinary tract infections (including cystitis);

unknown frequency: sepsis, including sepsis with fatal outcome.

Disorders of the blood and lymphatic system:

infrequently: anemia;

rarely: thrombocytopenia;

unknown frequency: eosinophilia.

Mental disorders:

infrequently: depression; rarely: anxiety.

Nervous system disorders:

infrequently: insomnia syncope vertigo; rarely: syncope.

Visual disturbances:

rare: visual impairment.

Cardiac disorders:

infrequently: bradycardia; rarely: tachycardia.

Vascular disorders:

infrequently: marked reduction in blood pressure * orthostatic hypotension;

* often observed in patients with controlled blood pressure who received treatment with telmisartan to reduce the risk of cardiovascular mortality in addition to standard treatment.

Respiratory, thoracic and mediastinal disorders:

infrequently: shortness of breath, cough.

Disorders of the gastrointestinal tract:

infrequently: abdominal pain diarrhea dyspepsia flatulence vomiting;

rarely: upset stomach discomfort dry oral mucosa liver function disorders/liver diseases.

Immune system disorders:

rare: hypersensitivity angioedema (including fatal cases); unknown frequency: anaphylactic reactions.

Skin and subcutaneous tissue disorders

uncommon: hyperhidrosis pruritus skin rash;

rare: erythema drug rash toxic skin rash eczema of unknown frequency: urticaria.

Musculoskeletal and connective tissue disorders: infrequently: myalgia back pain (such as sciatica) muscle spasms;

rarely: arthralgia pain in the extremities;

unknown frequency: pain in the tendon area (tendinitis-like symptoms).

Kidney and urinary tract disorders:

infrequently: renal failure including acute renal failure.

Nutritional and metabolic disorders:

infrequently: hyperkalemia.

Common disorders:

infrequently: chest pain asthenia (weakness);

rarely: flu-like condition.

Influence on the results of laboratory parameters and instrumental studies:

infrequently: increased blood creatinine concentration;

rarely: increased blood uric acid concentration “liver” enzymes serum creatine phosphokinase activity decreased hemoglobin hypoglycemia (in patients with diabetes mellitus).

Interaction

Telmisartan may increase the antihypertensive effect of other antihypertensive agents. Other types of interactions of clinical significance have not been identified. Couse with digoxin warfarin hydrochlorothiazide glibenclamide ibuprofen paracetamol simvastatin and amlodipine did not result in a clinically significant interaction.

Double blockade of the renin-angiotensin-aldosterone system (RAAS).

Concomitant use of telmisartan with aliskiren is contraindicated in patients with diabetes mellitus or renal insufficiency (GFR less than 60 ml / min/173 m2 of body surface area) and is not recommended for other patients. Concomitant use of telmisartan and HT1F inhibitors is contraindicated in patients with diabetic nephropathy.

The clinical trial data has shown that dual blockade of RAAS due to the combined use of ACE inhibitors or ARA II aliskiren associated with increased frequency of adverse events such as hypotension hyperkalemia and impaired renal function (including acute renal failure) compared to using only one drug acting on the RAAS.

The risk of hyperkalemia may increase when used together with other medications can cause hyperkalemia (potassium-containing dietary supplements and salt substitutes containing potassium and potassium-sparing diuretics (spironolactone, eplerenone triamterene or amiloride) nonsteroidal anti-inflammatory drugs (NSAIDs including selective cyclooxygenase-2 inhibitors (COX)) heparin immunosuppressants (cyclosporine tacrolimus trimethoprim)).

If necessary, against the background of documented hypokalemia, the combined use of drugs should be carried out with caution and the content of potassium in blood plasma should be regularly monitored.

Digoxin

When telmisartan was co-administered with digoxin, an increase in the average Cmax of digoxin in blood plasma by 49% and the minimum concentration by 20% was noted. At the beginning of treatment, when selecting the dose and stopping treatment with telmisartan, the concentration of digoxin in the blood plasma should be carefully monitored to maintain it within the therapeutic range.

Potassium-sparing diuretics or potassium-containing dietary supplements

Angiotensin II receptor antagonists such as telmisartan reduce diuretic-induced potassium loss. Potassium-sparing diuretics such as spironolactone eplerenone triamterene or amiloride potassium-containing dietary supplements or salt substitutes can lead to a significant increase in the potassium content in blood plasma. If concomitant use is indicated because 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 co-administered with ACE and ARAII inhibitors, including telmisartan, a reversible increase in the concentration of lithium in 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.

Nonsteroidal anti-inflammatory drugs (NSAIDs)

NSAIDs (including acetylsalicylic acid in the doses used for anti-inflammatory treatment, COX-2 inhibitors and non-selective NSAIDs) may weaken the antihypertensive effect of ARAII.

In some patients with impaired renal function (for example, patients with dehydration, elderly patients with impaired renal function), the combined use of ARAII and drugs that inhibit cyclooxygenase-2 may lead to further deterioration of renal function, including the development of acute renal failure, which is usually reversible.

Therefore, the combined use of drugs should be carried out with caution, especially in elderly patients. Proper fluid intake should be ensured in addition, renal function indicators should be monitored at the beginning of co-use and periodically thereafter.

Diuretics (thiazide or loop diuretics)

Previous treatment with high-dose diuretics such as furosemide (loop diuretic) and hydrochlorothiazide (thiazide diuretic) may lead to hypovolemia and the risk of hypotension at the start of telmisartan treatment.

Other antihypertensive agents

The effect of telmisartan may be enhanced with 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 barbiturates narcotic drugs or antidepressants.

Corticosteroids (for systemic use)

Corticosteroids weaken the effect of telmisartan.

How to take, course of use and dosage

Inside, regardless of food intake.

Arterial hypertension

The initial recommended dose of Telpres is 1 tablet. (40 mg) once a day. In cases where the therapeutic effect is not achieved, the maximum recommended dose of Telpres can be increased to 80 mg once a day. 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 cardiovascular morbidity and mortality

The recommended dose is 1 tablet of Telpres 80 mg once a day.

During the initial period of treatment, monitoring of blood pressure (BP) is recommended. It may be necessary to adjust antihypertensive therapy.

Impaired renal function

In patients with severe renal impairment and patients undergoing hemodialysis, experience with the drug is limited. In such patients, the recommended starting dose is 20 mg per day. No dose adjustment is required in patients with mild to moderate renal impairment.

Impaired liver function

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

Elderly patients

No dose adjustment is required in elderly patients.

Overdose

Information regarding overdose is limited.

Symptoms: the most significant – a marked decrease in blood pressure and tachycardia may also occur bradycardia dizziness increased serum creatinine concentration and acute renal failure.

Treatment: symptomatic and supportive. Suggested measures include: inducing vomiting and / or gastric lavage taking activated charcoal replenishing the lack of fluids and salts. Constant monitoring of the content of electrolytes and creatinine in the blood serum. Hemodialysis is not effective.

Special instructions

Liver function disorders

The use of Telpres is contraindicated in patients with cholestasis, biliary tract obstruction or severe hepatic impairment (Child-Pugh Class C) (see section “Contraindications”), since telmisartan is mainly excreted in the bile. It is assumed that the hepatic clearance of telmisartan is reduced in such patients.

In patients with mild or moderate hepatic impairment (Child-Pugh Class A and B), Telpres should be used with caution (see section “With caution”).

Renovascular hypertension

Patients with bilateral arterial stenosis or stenosis of the artery of a single functioning kidney are at increased risk of severe hypotension and renal failure when treated with drugs acting on the RAAS.

Impaired kidney function and kidney transplantation

When using Telpres in patients with impaired renal function, periodic monitoring of the content of potassium and creatinine in blood plasma is recommended. There is no experience of clinical use of Telpres in patients who have recently undergone kidney transplantation.

Reduced circulating blood volume

Symptomatic hypotension, especially after the first use of Telpres, may occur in patients with reduced BCC and / or plasma sodium levels, with previous treatment with diuretics, restriction of salt intake, diarrhea or vomiting. Such conditions (fluid and/or sodium deficiency) should be corrected before starting Telpres.

Double blockade of the renin-angiotensin-aldosterone system

Concomitant use of telmisartan with aliskiren is contraindicated in patients with diabetes mellitus or renal insufficiency (glomerular filtration rate less than 60 ml / min/173 m2) (see section “Contraindications”).

Concomitant use of telmisartan and ACE inhibitors is contraindicated in patients with diabetic nephropathy (see section “Contraindications”).

Hypotension syncope hyperkalemia and impaired renal function (including acute renal failure) have been reported as a result of RAAS inhibition in predisposed patients, especially when several medications also act on this system are used together. Therefore, double blockade of RAAS (for example, while taking telmisartan with other RAAS antagonists) is not recommended.

In cases of dependence of vascular tone and renal function mainly on the activity of the RAAS (for example, in patients with chronic heart failure or kidney diseases, including renal artery stenosis or stenosis of the artery of a single kidney), the appointment of drugs that affect this system may be accompanied by the development of acute arterial hypotension hyperazotemia oliguria and in rare cases acute renal failure.

Primary aldosteronism

In patients with primary aldosteronism, treatment with antihypertensive drugs that act by inhibiting the RAAS is usually ineffective.

Aortic and mitral valve stenosis hypertrophic obstructive cardiomyopathy

Caution should be exercised when using Telpres (as well as other vasodilators) in patients with aortic or mitral stenosis and hypertrophic obstructive cardiomyopathy.

Hyperkalemia

Taking medications that act on the RAAS can cause hyperkalemia. In elderly patients patients with renal insufficiency or diabetes mellitus patients also taking medications that increase the content of potassium in the blood plasma and/or patients with concomitant diseases, hyperkalemia can lead to death.

When deciding on the concomitant use of drugs acting on the RAAS, it is necessary to assess the risk-benefit ratio.

The main risk factors for 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 dietary supplements. Medicinal products or therapeutic classes of drugs that can cause hyperkalemia are salt substitutes containing potassium, potassium-sparing diuretics ACE inhibitors and receptor antagonists of angiotensin II nonsteroidal anti-inflammatory drugs (NSAIDs including selective COX-2 inhibitors) heparin immunosuppressants (cyclosporine or tacrolimus) and trimethoprim;

– intercurrent disease in particular dehydration, acute cardiac failure, metabolic acidosis, the kidney dysfunction syndrome cytolysis (e. g. acute limb ischemia, rhabdomyolysis extensive injury).

Patients at risk are recommended to carefully monitor the potassium content in the blood plasma (see the section “Interaction with other drugs”).

Ethnic differences

ACE inhibitors telmisartan and other ARAII appear to reduce blood pressure less effectively in black patients than in other races, possibly due to a greater predisposition to a decrease in renin activity in the population of these patients.

Other things

As with other antihypertensive agents, excessive lowering of blood pressure in patients suffering from ischemic cardiomyopathy or coronary heart disease can lead to the development of myocardial infarction or stroke.

Influence on the ability to drive vehicles and mechanisms:

Special clinical studies of the effect of the drug on the ability to drive a car and mechanisms have not been conducted. When driving a car and working with mechanisms that require increased concentration of attention, care should be taken as dizziness and drowsiness may rarely occur while taking telmisartan.

Storage conditions

At a temperature not exceeding 25 °C.

Keep out of reach of children!

Shelf

life is 2 years.

Active ingredient

Telmisartan

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension