Telsartan tab. 80mg 30 pc

Description

Composition
Active substance:
80,00 mg telmisartan
Excipients:
24.00 mg of meglumine, sodium hydroxide, 6.70 mg Povidone K30 24.0 mg Polysorbate 80 3.00 mg Mannitol 432.10 mg 10.20 mg magnesium stearate.
Description:
Kapsulovidnoy tablet form, biconcave, white or nearly white, one side of the separation of risk and embossed “T” and “L” on each side of her. on the other side of the embossed “80”.
Product form:
Tablets of 80 mg.
10 tablets in a blister (PVC / Al / PA) foil / aluminum foil.
3 blisters together with instructions for use in a cardboard pack.
Contraindications
• Hypersensitivity to the active substance or auxiliary ingredients.
• Pregnancy and lactation.
• obstructive biliary tract disease.
• Severe liver problems (class C by Child-Pugh classification).
• simultaneous use of aliskiren and preparations containing aliskiren in patients with diabetes and / or moderate to severe renal function (glomerular filtration rate (GFR) of less than 60 ml / min / 1.73 m2 body surface area).
• simultaneous use of inhibitors of angiotensin converting enzyme in patients with diabetic nephropathy.
• Age 18 years (effectiveness and safety have been established).
Precautions • Bilateral renal artery stenosis or stenosis of the artery to a solitary kidney (see. Section “Special Instructions”).
• mild to moderate hepatic dysfunction and / or kidney problems (see. Section “Special Instructions”).
• Reduction of circulating blood volume (CBV) due to prior diuretic therapy restrictions Hour salt, diarrhea or vomiting.
• Hyponatremia.
• Hyperkalemia.
• The status after kidney transplantation (application no experience).
• Chronic heart failure.
• Stenosis of the aortic and mitral valves.
• Idiopathic hypertrophic subaortic stenosis (hypertrophic obstructive cardiomyopathy).
• Primary aldosteronism.
Dosage
80 mg
Indications
• Arterial hypertension.
• Reduction of cardiovascular morbidity and mortality in patients aged 55 years or older at high risk of cardiovascular disease.
Interaction with other drugs
Receiving telmisartan as well as other drugs acting on the renin-angiotensin-aldosterone system (RAAS) is capable to provoke hyperkalemia. The risk of hyperkalemia can increase with concomitant administration of a potassium-containing salt substitutes; potassium-sparing diuretics; angiotensin converting enzyme (ACE); ARA II; nonsteroidal antiinflammatory drugs (NSAIDs), including selective cyclooxygenase (COX) type 2; heparin; immunosuppressive agents (cyclosporin or tacrolimus), and trimethoprim.
The incidence of hyperkalemia depends on the presence of risk factors. With simultaneous use of potassium-sparing diuretics and potassium-containing salt substitutes the risk of hyperkalemia particularly high. The simultaneous use of ACE inhibitors or NSAIDs is accompanied by a lower risk of hyperkalemia, with careful precautions.
Dual blockade of the renin-angiotensin-aldosterone
The simultaneous use of ACE inhibitors or ARA II Aliskiren increases the risk of hypotension, hyperkalaemia and renal dysfunction (including acute renal failure), so that the combination of these drugs is regarded as a dual blockade of the RAAS.
The simultaneous use of ARA II with preparations containing aliskiren, contraindicated in patients with diabetes and / or with moderate or severe renal failure (GFR of less than 60 ml / min / 1.73 m2 body surface area) and are not recommended for other patients. The simultaneous use of ARA II with ACE inhibitors is contraindicated in patients with diabetic nephropathy, and is not suitable for other patients.
When absolutely necessary therapy with the use of dual blockade of the RAAS should be done under strict medical supervision and careful monitoring of renal function, electrolytes and blood pressure.
Digoxin
When simultaneous administration of telmisartan and digoxin observed median increased peak and residual concentration of digoxin in plasma (49% and 20% respectively). In the beginning, and when adjusting the termination telmisartan is necessary to monitor the concentration of digoxin in serum, to keep it within the therapeutic range.
Potassium-sparing diuretics and substitutes, salts containing potassium
ARA II, such as telmisartan, reduce the loss of potassium caused by diuretics. Potassium-sparing diuretics such as spironolactone, eplerenone, triamterene or amiloride, potassium supplements or kalisodergaszczye salt substitutes, may cause a significant increase in serum potassium. If you want to use them at the same time due to the presence of proven hypokalaemia, treat with caution under the common control of the content of potassium in the blood serum.
Lithium
When concomitant administration of drugs lithium with ACE inhibitors and ARA II, including telmisartan mentioned reversible increase the concentration of lithium in the blood plasma, accompanied by toxic effects. If necessary, the simultaneous use of these drugs is recommended to control the salt content of lithium in blood serum.
Nonsteroidal anti-inflammatory drugs
Acetylsalicylic acid in doses of 3 grams per day or more, COX-2 inhibitors and non-selective NSAIDs might reduce the antihypertensive effect of ARA II. Patients with impaired renal function (compared to dehydration or elderly) co-administration of ARA and COX II inhibitors can lead to reversible renal function deterioration. Therefore, drugs in this combination are assigned with caution, especially in elderly patients. Before use telmisartan recommended to evaluate kidney function and correct altered fluid and electrolyte balance; further advantageous to control the function of the kidneys.
ramipril
The simultaneous use of ramipril increases the AUC0-24 and Cmax of ramipril and ramiprilat 2.5 times. The clinical significance of this effect is not established.
Loop and thiazide diuretics
Prior therapy with diuretics in high doses, including furosemide ( “loop” diuretic) and hydrochlorothiazide (thiazide diuretic) may result in a decrease in blood volume and increase the risk of hypotension at the beginning of therapy with telmisartan.
Other antihypertensives
The ability of telmisartan to lower blood pressure can be enhanced, while the application of other antihypertensives. Given the pharmacological properties may increase the effect of antihypertensives including telmisartan with concomitant administration of baclofen or with amifostine.
Ethanol, barbiturates, means for anesthesia and antidepressants can contribute to the development of orthostatic hypotension.
systemic corticosteroids
Glucocorticosteroids reduce the antihypertensive effect of telmisartan.
Overdose
Information is limited regarding overdose.
Symptoms: The most important – marked reduction in blood pressure and tachycardia may also occur bradycardia, dizziness, increase in serum creatinine concentration in the serum and acute renal failure.
Treatment: symptomatic and supportive. Proposed measures include vomiting and / or gastric lavage, administration of activated charcoal, filling shortage of the liquid and salts. Permanent monitoring of the content of electrolytes and creatinine in serum. Hemodialysis is not effective.
pharmachologic effect
Pharmacological group:
angiotensin II receptor antagonist.
Pharmacodynamics:
Telmisartan – specific antagonist of angiotensin (ARA) receptor II, AT1 type effective when taken orally. It has high affinity for the AT1 subtype angiotensin II receptor, which is realized through the action of angiotensin II. Displaces angiotensin II from binding with the receptor, having no agonist action against this receptor. Telmisartan binds only to the AT1 subtype angiotensin II receptor. Relationship is long-term nature. No affinity for other receptors, including AT2 receptor and other receptors of angiotensin less studied. The functional significance of these receptors, as well as their possible effect of excessive stimulation by angiotensin II, whose concentration increases with telmisartan, have not been studied. Reduces the concentration of aldosterone in the blood, does not inhibit renin in plasma and does not block the ion channels. Telmisartan does not inhibit the angiotensin converting enzyme (kininaza II), which also destroys bradykinin. Therefore, the strengthening of the side effects caused by bradykinin, is not expected.
In patients with hypertension telmisartan 80 mg completely blocks the hypertensive effect of angiotensin II. Starting antihypertensive effects observed for 3 hours after the first reception of telmisartan inside. Effect of the drug lasts for 24 hours and is still significant 48 hours. Antihypertensive effect usually develops within 4 weeks after taking the drug regularly.
In patients suffering from hypertension, telmisartan reduces the systolic and diastolic blood pressure (BP), without affecting the heart rate (HR).
In the case of abrupt withdrawal of telmisartan, blood pressure gradually returned to baseline without the development of the syndrome of “cancellation”.
Pharmacokinetics:
Suction
If ingestion is rapidly absorbed from the gastrointestinal tract. The bioavailability is about 50%. When taken with food simultaneously reducing the area under the curve “concentration-time» (AUC) ranges from 6% (at 40 mg) to 19% (at a dose of 160 mg). After 3 hours after administration, plasma concentration equalized regardless of the meal.
Distribution
Communication with plasma proteins – 99,5% (mainly to albumin and alpha-1 glycoprotein). The mean value of the apparent distribution volume in the equilibrium concentration – 500 liters.
Metabolism
It is metabolized by conjugation with glucuronic acid. The metabolites are pharmacologically inactive.
breeding
The half-life (T1 / 2) – over 20 hours. Is output through the intestine unaltered, renal excretion – less than 2% of the dose. Total plasma clearance is high (900 mL / min) compared with “liver blood flow” (about 1500 ml / min).
Pharmacokinetics in special patient groups
gender differences
There is a difference in plasma concentrations of telmisartan in men and women. The maximum plasma concentration (Cmax) is about 3 times and AUC of about 2 times higher in women compared to men without significant effect on efficiency. Dosage adjustment is not required.
elderly patients
The pharmacokinetics of telmisartan in elderly patients does not differ from the pharmacokinetics in younger patients. Dose adjustment is not required.
Patients with impaired renal function
In patients with mild to moderate renal impairment dose adjustment telmisartan is not required.
For patients with severe renal failure and patients on hemodialysis, a lower recommended initial dose – 20 mg per day.
Telmisartan does not rely on hemodialysis.
Patients with impaired liver function
Pharmacokinetic studies in patients with hepatic impairment showed an increase in absolute bioavailability of telmisartan almost 100%. In hepatic insufficiency T1 / 2 is not changed. Patients with mild to moderate hepatic impairment (class A and B according to the classification Child-Pugh) daily dose should not exceed 40 mg.
Pregnancy and breast-feeding
Pregnancy
Drugs that act directly on the RAAS can cause serious injury and death of the developing fetus, so when planning or establishing the fact of pregnancy, the drug should be discontinued immediately and, if necessary, appoint an alternative antihypertensive treatment, which has established safety profile when used during pregnancy. Use of the drug during pregnancy is contraindicated.
In preclinical studies of telmisartan teratogenic effects have been identified, but is set fetotoxicity. It is known that the effect of angiotensin II receptor antagonists in the second and third trimesters of pregnancy causes human fetotoxicity (decreased renal function, oligohydramnios, skull ossification retardation) and neonatal toxicity (renal failure, hypotension, hyperkalaemia). Patients planning pregnancy should be prescribed an alternative therapy. If treatment of angiotensin II receptor antagonists occurred during the second trimester of pregnancy, it is recommended ultrasonic inspection method renal function and status of the skull of the fetus.
Newborns whose mothers received angiotensin II receptor antagonists should be closely observed for hypotension.
Breastfeeding
Breastfeeding is contraindicated during treatment with telmisartan.
fertility
Studies of the effect on human fertility have not been conducted.
Conditions of supply of pharmacies
Prescription.
side effects
In general, the frequency of occurrence of adverse reactions noted for telmisartan is comparable to a similar placebo. The observed incidence of side effects did not correlate with gender, age or race of patients.
Classification of frequency of adverse reactions to the World Health Organization (WHO): very common (> 1/10); often (by> 1/100 to
special instructions
Abnormal liver function
Use of telmisartan is contraindicated in patients with cholestasis, biliary tract obstruction or severe hepatic impairment (class C Child-Pugh classification), as telmisartan excreted mainly in the bile. In these patients, it is expected to reduce the excretion of the drug. Telmisartan should be used with caution in patients with mild or moderate hepatic impairment (Class A or B on the Child-Pugh classification).
Renovascular hypertension
If the use of drugs that affect the RAAS in patients with bilateral renal artery stenosis or stenosis of the only functioning kidney increased risk of severe hypotension and renal insufficiency.
Renal function
When telmisartan in patients with renal failure patients is recommended to control serum potassium and creatinine concentration. Previous use after recently undergone renal transplantation is not described.
hypovolemia
In patients with hypovolemia and / or hyponatremia due to intensive diuretic therapy, restriction of salt intake, diarrhea or vomiting may develop symptomatic hypotension, especially after the first dose of telmisartan. Before starting therapy should correct the violations of water-electrolyte balance.
Dual blockade of the RAAS
The simultaneous use of ACE inhibitors or ARA II Aliskiren increases the risk of hypotension, hyperkalaemia and renal dysfunction (including acute renal failure), so that the combination of these drugs is regarded as a dual blockade of the RAAS.
The simultaneous use of ARA II with preparations containing aliskiren, contraindicated in patients with diabetes and / or with moderate or severe renal failure (GFR of less than 60 ml / min / 1.73 m2 body surface area) and are not recommended for other patients. The simultaneous use of ARA II with ACE inhibitors is contraindicated in patients with diabetic nephropathy, and is not suitable for other patients.
When absolutely necessary therapy with the use of dual blockade of the RAAS should be done under strict medical supervision and careful monitoring of renal function, electrolytes and blood pressure.
Other conditions associated with activation of the RAAS
Patients vascular tone and renal function is determined RAAS activity (patients with congestive heart failure or renal diseases including stenosis two renal artery stenoses or artery only kidneys), the use of drugs affecting the RAAS may be accompanied by the development of hypotension, hyperasotemia, oliguria, and in rare cases – acute renal failure.
primary aldosteronism
Patients with primary hyperaldosteronism resistant to antihypertensive drugs affecting RAAS therefore such patients use of telmisartan is not recommended.
Stenosis of the aortic and / or mitral valve, hypertrophic obstructive cardiomyopathy (GOKMP)
Telmisartan must be used with caution in patients with hemodynamically significant stenosis of the aortic and / or mitral valves or GOKMP.
Patients with diabetes treated with insulin or hypoglycemic agents for oral administration
With telmisartan in these patients may develop hypoglycaemia. It recommended regularly monitor the concentration of blood glucose and if necessary to carry out a correction dose hypoglycemic agents.
hyperkalemia
Application RAAS affecting drugs can cause hyperkalemia. Before the simultaneous application of such drugs should be evaluated benefit / risk ratio.
Risk factors for the development of hyperkalemia:
– renal insufficiency, age over 70 years, diabetes mellitus;
– simultaneous administration of drugs affecting the RAAS (ACE inhibitors ARA II) and / or potassium-sparing diuretics (spironolactone, eplerenone, triamterene, amiloride), potassium preparations or potassium-based substitutes for edible salt, NSAID (including COX-2 selective), heparin, immunosuppressive drugs (cyclosporine or tacrolimus), and trimethoprim;
– associated conditions such as dehydration, acute heart failure decompensation, metabolic acidosis, renal failure, sudden progression of renal disease (infectious diseases), conditions accompanied by tissue necrosis (acute limb ischemia, rhabdomyolysis, extensive trauma).
risk patients should be closely monitored the concentration of potassium in the blood serum.
ethical features
ACE inhibitors and ARA II (including telmisartan) may have a less pronounced antihypertensive effect in patients blacks.
Perhaps this is due to lower levels of renin in hypertension in these patients as compared to members of other races.
Other
As with any treatment antihypertensives excessive lowering of blood pressure in patients with coronary heart disease or ischemic cardiomyopathy can lead to myocardial infarction or stroke.
Effect on driving ability
Specific clinical studies to assess the impact of the drug on the ability to drive and not carried out mechanisms. However, when motor vehicles and Employment hazardous activities should take into account the possibility of dizziness and drowsiness, which requires compliance with caution.
Storage conditions
At temperatures above 25 ° C.
Keep out of the reach of children!
Dosing and Administration
Inside, regardless of the meal with water.
Arterial hypertension
Starting Telsartan® recommended dose of preparation – 1 tablet of 40 mg once a day. For some patients, the effective dose may be 20 mg per day (40 mg tablets 1/2). In cases where the therapeutic effect is not achieved, the maximum recommended dose Telsartan® drug can be increased to 80 mg (1 tablet of 80 mg or 40 mg 2 tablets) once daily. In deciding whether to increase the dose should be taken into account that the maximum antihypertensive effect is usually achieved within 4-8 weeks after starting treatment.
Reduction in cardiovascular morbidity and mortality
The recommended dose of the drug Telsartan® – 1 tablet of 80 mg once a day.
In the initial period of treatment may require additional correction of blood pressure.
Renal function
Существует ограниченный опыт применения телмисартана у пациентов с тяжёлым нарушением функции почек или находящихся на гемодиализе. Таким пациентам требуется низкая начальная доза 20 мг.
Пациентам с легким или умеренным нарушением функции почек коррекции дозы не требуется.
Liver function abnormalities
У пациентов с легкими и умеренными нарушениями функции печени суточная доза препарата Телсартан® не должна превышать 40 мг.
Применение при тяжелых нарушениях функции печени противопоказано (см. раздел «Противопоказания»).
Elderly patients
The dosage regimen does not require modification.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist