Telsartan, tablets 80 mg 30 pcs

Pharmacodynamics

Telmisartan is a specific angiotensin II receptor antagonist (ARA) type AT1, effective by oral administration. It has high affinity for the AT1 subtype of angiotensin II receptors, through which angiotensin II action is realized. It displaces angiotensin II from binding to the receptor, having no agonist effect against this receptor. Telmisartan binds only to the AT1 subtype of angiotensin II receptor.

The binding is long lasting. It has no affinity for other receptors, including AT2 receptor and other less studied angiotensin receptors. The functional significance of these receptors and the effect of their possible overstimulation by angiotensin II, the concentration of which increases with telmisartan administration, have not been studied. It reduces the blood concentration of aldosterone, does not inhibit plasma renin and does not block ion channels. Telmisartan does not inhibit angiotensin-converting enzyme (kininase II), which also degrades bradykinin. Therefore, an increase in bradykinin-induced side effects is not expected.

In patients with arterial hypertension, telmisartan at a dose of 80 mg completely blocks the hypertensive effects of angiotensin II. Initiation of antihypertensive action is observed within 3 hours after the first oral administration of telmisartan. The action of the drug persists for 24 hours and remains significant up to 48 hours. A pronounced antihypertensive effect usually develops after 4 weeks of regular use.

Indications

Hypertension (high blood pressure)

• Arterial hypertension.

• Reducing cardiovascular morbidity and mortality in patients aged 55 years and older with high risk of cardiovascular disease.

Active ingredient

Telmisartan

Composition

1 tablet 80 mg contains:

The active ingredient:

Telmisartan 80.00 mg

Associates:

Meglumine 24.00 mg

Sodium hydroxide 6.70 mg

Povidone-K30 24.00 mg

How to take, the dosage

Orally, with water and regardless of meals.

Arterial hypertension

The initial recommended dose of Telsartan® is 1 tablet 40 mg once daily. In some patients, a dose of 20 mg per day (1/2 tablet of 40 mg) may be effective. In cases when therapeutic effect is not achieved, the maximum recommended dose of Telsartan® can be increased to 80 mg (1 tablet of 80 mg or 2 tablets of 40 mg) once daily. When deciding on dose increase it should be taken into consideration that maximal antihypertensive effect is usually achieved within 4-8 weeks after the treatment start.

Lower cardiovascular morbidity and mortality

Recommended dose of Telsartan® is 1 tablet of 80 mg once daily.
Additional BP adjustment may be required during initial treatment.

Renal dysfunction

There is limited experience with telmisartan in patients with severe renal dysfunction or those on hemodialysis. Such patients require a low starting dose of 20 mg.
Patients with mild to moderate renal impairment do not require dose adjustment.

Hepatic disorders

In patients with mild to moderate hepatic impairment the daily dose of Telsartan® should not exceed 40 mg.

Use in severe hepatic impairment is contraindicated (see section “Contraindications”).

Patients of advanced age

The dosing regimen does not require changes.

Interaction

Telsartan may increase the hypotensive effect of other antihypertensive agents. Other clinically significant interactions have not been identified. Concomitant use of telmisartan with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin and amlodipine does not lead to clinically significant interaction.

When concomitant use with digoxin an increase in mean minimum plasma concentration of digoxin by 20% (in a single case by 39%) was observed, so it is necessary to monitor plasma levels of digoxin. Simultaneous use of telmisartan and ramipril resulted in 2.5-fold increase in AUC0-24 and Cmax of ramipril and ramiprilat.

The clinical significance of this phenomenon has not been established. Reversible increases in serum lithium concentrations and toxicity have been reported when lithium is coadministered with angiotensin II receptor antagonists, including telmisartan. In this case, it is recommended to monitor plasma lithium levels and patients should be under close medical supervision.

Concurrent treatment with nonsteroidal anti-inflammatory drugs (NSAIDs), including acetylsalicylic acid, cyclooxygenase-2 [COX-2] inhibitors and non-selective NSAIDs, is associated with the risk of acute renal failure in patients with dehydration. Drugs acting on the renin-angiotensin system may have a synergistic effect.

Patients receiving concomitant NSAIDs and telmisartan should adequately replenish water loss and monitor renal function at the start of treatment. Some decrease in antihypertensive effect of telmisartan has been reported with concomitant use of NSAIDs. Concomitant treatment with telmisartan and corticosteroid drugs decreases the antihypertensive effect

Directions for use

Telmisartan tablets are for daily oral administration and are taken with fluid, with or without food. Treatment of essential hypertension: The recommended dose for adults is 40 mg once daily. In cases where the desired BP is not achieved, the dose of Telsartan may be increased to a maximum of 80 mg once daily. When increasing the dose, it should be taken into account that the maximum antihypertensive effect is usually achieved within four to eight weeks after the start of treatment.

Telsartan may be used in combination with thiazide diuretics such as hydrochlorothiazide, which in combination with telmisartan has an additional hypotensive effect. In patients with severe arterial hypertension the dose of telmisartan 160 mg/day (two tablets of drug Telsartan 80 mg) and in combination with hydrochlorothiazide 12.5-25 mg/day was well tolerated and effective.

Prevention of cardiovascular morbidity and mortality: The recommended dose is 80 mg once daily. It is not clear whether doses below 80 mg are effective in reducing cardiovascular morbidity and mortality. Initial use of Telsartan® to prevent cardiovascular morbidity and mortality recommends blood pressure (BP) control and may require BP correction with BP lowering medications.

Telsartan can be taken regardless of food intake. Renal Impairment: No dose modification is required in patients with renal impairment, including patients on hemodialysis. There is limited experience with treatment of patients with severe renal impairment and hemodialysis. For these patients, it is recommended to start with a lower dose of 20 mg.

Telsartan is not eliminated from the blood by hemofiltration. Hepatic impairment: In patients with mild to moderate hepatic impairment, the daily dose of the drug should not exceed 40 mg once daily. Elderly patients: Dose adjustment is not required.

Special Instructions

Hepatic impairment

Telmisartan is contraindicated in patients with cholestasis, biliary obstruction or severe hepatic impairment (Child-Pugh class C), since telmisartan is mainly excreted with bile. Decreased drug excretion is expected in such patients. Telmisartan should be used with caution in patients with mild to moderate hepatic impairment (Child-Pugh class A or B)
.
Vasorenal arterial hypertension

When using drugs that affect the RAAS in patients with bilateral renal artery stenosis or stenosis of the only functioning kidney, the risk of severe arterial hypotension and renal failure is increased.

Kidney function impairment

When using telmisartan in patients with renal impairment it is recommended to monitor serum potassium and creatinine concentration. No experience with use after recent renal transplantation has been described.

Hypovolemia

Patients with hypovolemia and/or hyponatremia due to intensive diuretic therapy, salt restriction, diarrhea or vomiting may develop symptomatic arterial hypotension, especially after the first dose of telmisartan. Water-electrolyte balance abnormalities should be corrected before initiating therapy.

Double RAAS blockade

The simultaneous use of ACE inhibitors, ARA II or aliskiren increases the risk of hypotension, hyperkalemia and renal dysfunction (including acute renal failure), therefore the combination of these drugs is considered as double RAAS blockade.

Simultaneous use of ARA II with drugs containing aliskiren is contraindicated in patients with diabetes and/or with moderate or severe renal insufficiency (FFR less than 60 ml/min/1.73 m2 body surface area) and is not recommended in other patients.

If absolutely necessary, therapy using dual RAAS blockade should be carried out under strict medical supervision and close monitoring of renal function, electrolytes and blood pressure.
Other conditions accompanied with activation of RAAS

In patients whose vascular tone and renal functionin patients with RAAS activity (patients with chronic heart failure or kidney diseases, including stenosis of two renal arteries or stenosis of the artery of the only kidney) the use of medications that affect the RAAS may be accompanied by arterial hypotension, hyperazotemia, oliguria and in rare cases – acute renal failure.

Primary hyperaldosteronism

Patients with primary hyperaldosteronism are resistant to hypotensive drugs affecting the RAAS, so telmisartan is not recommended for these patients.

Aortic and/or mitral valve stenosis, hypertrophic obstructive cardiomyopathy (HCMP)
Telmisartan should be used with caution in patients with hemodynamically significant aortic and/or mitral valve stenosis or HCMP.

Patients with diabetes mellitus receiving insulin or hypoglycemic agents for oral administration
When using telmisartan in such patients hypoglycemia may develop. It is recommended to monitor blood glucose concentration regularly and adjust the dose of hypoglycemic agents if necessary.

Hyperkalemia

The use of drugs affecting the RAAS may cause hyperkalemia. Before the simultaneous use of such drugs the benefit/risk ratio should be evaluated.

Risk factors for hyperkalemia:

– renal failure, age over 70 years, diabetes mellitus;

– concomitant use of drugs that affect the RAAS (ACE inhibitors, ARA II) and/or potassium-saving diuretics (spironolactone, eplerenone, triamterene, amiloride), potassium drugs or potassium-containing salt substitutes, NSAIDs (including COX-2 selective), heparin, immunosuppressive drugs (cyclosporine or tacrolimus), and trimethoprim;

– concomitant conditions such as dehydration, acute heart failure in decompensation, metabolic acidosis, renal dysfunction, sudden progression of renal disease (infectious diseases), conditions accompanied by tissue necrosis (acute limb ischemia, rhabdomyolysis, extensive trauma).

Patients at risk should be closely monitored serum potassium concentration.
Ethics

ACE inhibitors and ARA II (including telmisartan) may have less pronounced antihypertensive effect in patients of non-highland race.
This may be due to decreased renin levels in arterial hypertension in these patients compared with other races.

Other

As with any hypotensive treatment, excessive BP reduction in patients with CHD or ischemic cardiomyopathy may lead to myocardial infarction or stroke.

Special clinical studies to evaluate the effect of the drug on the ability to drive and operate machinery have not been conducted. However, when driving motor transport and engaging in hazardous activities, the possibility of dizziness and somnolence should be taken into account, which requires caution.