Telsartan - Instructions For Use, 40 And 80 Mg, Price, Analogues, Reviews

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Telsartan

Telsartan: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Use in the elderly
14. 14. Drug interactions
15. 15. Analogs
16. 16. Terms and conditions of storage
17. 17. Terms of dispensing from pharmacies
18. 18. Reviews
19. 19. Price in pharmacies

Latin name: Telsartan

ATX code: C09CA07

Active ingredient: Telmisartan (Telmisartan)

Manufacturer: Dr. Reddy's Laboratories, Ltd. (Dr. Reddy`s Laboratories, Ltd.) (India)

Description and photo update: 2020-05-02

Prices in pharmacies: from 252 rubles.

Buy

Telsartan is an antihypertensive drug, an angiotensin II receptor antagonist, an AT ₁ receptor blocker.

Release form and composition

Dosage form - tablets: capsule-shaped, biconvex, from almost white to white, embossed on one of the sides on the sides of the dividing line T | L, on the other side - the number corresponding to the dosage, "40" or "80" (in a blister 7 tablets, in a cardboard box 2 or 4 blisters; in a blister 10 tablets, in a cardboard box 3 blisters; in each pack together with blisters is placed instructions for the use of Telsartan).

Composition for 1 tablet:

• active ingredient: telmisartan - 40 or 80 mg;
• excipients: meglumine, povidone-K30, sodium hydroxide, polysorbate-80, magnesium stearate, mannitol.

Pharmacological properties

Pharmacodynamics

The active ingredient in Telsartan - telmisartan, is a specific antagonist of angiotensin receptors (ARA) II, effective when taken orally. It shows a high affinity for the receptors of angiotensin II subtype AT ₁, through which the effect of angiotensin II is realized. Telmisartan displaces angiotensin II from the connection with the receptor, while not showing agonism in relation to this receptor; binds exclusively to the receptors of angiotensin II subtype AT ₁. This relationship is long-term. Affinity for other receptors, including AT ₂- and other less studied angiotensin receptors, telmisartan does not. The functional potential of these receptors and the effect of their possible overstimulation by angiotensin II, the content of which increases with the administration of Telsartan, have not been studied. The drug lowers the plasma level of aldosterone in the blood, does not block the ion channels of the cell membrane. It does not inhibit renin, as well as ACE (angiotensin converting enzyme) (kininase II), which is a catalyst for the degradation of bradykinin. This pharmacological action of the substance makes it unlikely that the side effects caused by bradykinin will increase.

With arterial hypertension, a dose of Telsartan 80 mg completely blocks the increase in blood pressure (blood pressure) under the influence of angiotensin II. The drug begins to act within 3 hours after oral administration, stabilizes blood pressure within 24 hours, exerting a clinically significant effect up to 48 hours. A pronounced antihypertensive effect, as a rule, develops by the end of the 4th week of regular pill intake.

In arterial hypertension, telmisartan lowers systolic and diastolic blood pressure, but does not affect heart rate (heart rate).

A sudden discontinuation of Telsartan does not cause the development of a withdrawal syndrome, blood pressure returns to its initial level gradually.

When evaluating the efficacy of telmisartan in a study of patients aged 55 years and older with high cardiovascular risk (stroke, peripheral / coronary artery disease, diabetes mellitus, aggravated by such target organ lesions as retinopathy or left ventricular hypertrophy, macro- or microalbuminuria history) has been shown to reduce cardiovascular morbidity and mortality.

Pharmacokinetics

The main pharmacokinetic characteristics of telmisartan:

• absorption: after oral administration, the substance from the gastrointestinal tract (gastrointestinal tract) is rapidly absorbed. Its bioavailability is approximately 50%. Simultaneous administration of the drug with food reduces the AUC (area under the pharmacokinetic curve "concentration - time"). The decrease in the indicator depends on the dose taken: for 40 mg it is from 6%, for 160 mg - up to 19%. After 3 hours, the plasma level of the drug in the blood, regardless of food intake, stabilizes. The gender of the patient affects the plasma concentration of telmisartan. So the value of C _max (maximum concentration) in plasma in women is approximately 3 times higher than in men. AUC in women is approximately 2 times higher. But such a difference does not significantly affect the effectiveness of the drug;
• distribution: V _d (volume of distribution) is about 500 liters. Telmisartan binds to plasma proteins (mainly albumin and α-1-glycoprotein) at the level of 99.5%;
• metabolism: the process of biotransformation occurs by conjugation with glucuronic acid to form pharmacologically inactive metabolites;
• excretion: telmisartan is excreted unchanged, mainly through the intestines; renal elimination is subject to less than 2% of the dose taken. The cleansing factor (total plasma clearance) is high and is about 900 ml / min, with hepatic blood flow - about 1500 ml / min. T _1/2 (half-life) exceeds 20 hours.

Pharmacokinetics of telmisartan in special patient groups:

• old age: the effect of the drug on elderly patients does not differ from that on younger patients;
• renal failure: impaired renal function does not affect the effectiveness of Telsartan, telmisartan is not excreted from the body through hemodialysis;
• hepatic failure: in case of mild to moderate hepatic dysfunction, classes A and B according to the Child-Pugh classification, the daily dose should not exceed 40 mg.

Indications for use

Telsartan is used to lower blood pressure in hypertension.

The drug is also prescribed to patients over 55 years of age in order to reduce the number of episodes of cardiovascular morbidity and mortality at high risks of cardiovascular pathologies, including anamnestic data on such consequences of atherothrombosis as stroke, coronary artery disease (coronary artery disease), peripheral atherosclerosis. arteries, or a history of type 2 diabetes mellitus with documented target organ damage.

Contraindications

Absolute:

• severe hepatic dysfunction related to class C according to the Child-Pugh classification;
• obstruction of the bile ducts;
• combined use with aliskiren and / or aliskiren-containing drugs for diabetes mellitus and moderate or severe renal dysfunction, GFR (glomerular filtration rate) <60 ml / min / 1.73 m ² body surface area;
• combined use with ACE inhibitors for diabetic nephropathy;
• the entire period of pregnancy;
• period of breastfeeding;
• children and adolescents up to 18 years old;
• individual hypersensitivity to the active substance and / or auxiliary components of the drug.

With caution, Telsartan is prescribed for bilateral renal artery stenosis or artery stenosis of a single functioning kidney; mild to moderate impairment of liver / kidney function; a decrease in the BCC (volume of circulating blood) as a result of previous therapy with diuretic drugs, restriction of the use of table salt, vomiting or diarrhea; hyperkalemia; hyponatremia; chronic heart failure; condition after kidney transplant (due to lack of experience in use); stenosis of the aortic and mitral valves; idiopathic hypertrophic subaortic stenosis (hypertrophic obstructive cardiomyopathy); primary hyperaldosteronism.

Telsartan, instructions for use: method and dosage

Telsartan tablets are taken orally, regardless of the diet, with water. The frequency of taking the drug is once a day.

In the treatment of arterial hypertension, the drug is recommended to be used in an initial daily dose of 40 mg (1 tablet). For some patients, a dose of 20 mg (1/2 Telsartan 40 mg tablet) may be effective. If it is not possible to achieve a therapeutic effect, the maximum daily dose of Telsartan is prescribed - 80 mg (2 tablets of 40 mg or 1 tablet of 80 mg). The decision to increase the dose is made taking into account the fact that usually the maximum hypotensive effect is achieved within 4-8 weeks from the start of therapy.

In order to reduce cardiovascular morbidity and mortality, the drug is recommended to be taken in a daily dose of 80 mg (2 tablets of Telsartan 40 mg or 1 tablet of 80 mg).

At the beginning of treatment, additional correction of blood pressure may be required.

Side effects

In the treatment of arterial hypertension, the overall incidence of adverse side effects of telmisartan in controlled studies is usually comparable to that in the placebo group (41.4% and 43.9%, respectively). Correlation of side effects with patients' age, gender or race was not found. When telmisartan was used for the prevention of cardiovascular morbidity and mortality, the safety profile corresponded to that obtained during the treatment of arterial hypertension.

Negative side effects from systems and organs registered while taking Telsartan [using the following observation frequency scale: very often (≥ 0.1%); often (0.1–0.01%); infrequently (0.01–0.001%); rarely (0.001–0.0001%); very rare (<0.0001%)]:

• infections and invasions: infrequently - infectious lesions of the upper respiratory tract (including pharyngitis and sinusitis), infectious lesions of the urinary tract (including cystitis); rarely - sepsis, up to cases of death with an unexplained mechanism of occurrence;
• circulatory and lymphatic systems: infrequently - anemia; rarely - thrombocytopenia, eosinophilia;
• immune system: rarely - anaphylactic reactions, hypersensitivity;
• metabolism and nutrition: infrequently - hyperkalemia; rarely (in patients with diabetes mellitus) - hypoglycemia;
• mental disorders: infrequently - insomnia, depression; rarely - anxiety;
• nervous system: infrequently - syncope; rarely - drowsiness;
• organ of vision: rarely - impaired visual perception;
• organ of hearing and labyrinthine disorders: infrequently - vertigo;
• myocardium: infrequently - bradycardia; rarely - tachycardia;
• vascular pathologies: infrequently - orthostatic (postural) hypotension, a decrease in blood pressure (observed in patients with controlled blood pressure taking telmisartan against the background of standard therapy to reduce cardiovascular morbidity and mortality);
• respiratory system, chest and mediastinal organs: infrequently - cough, shortness of breath; very rarely - interstitial lung diseases (observed in post-marketing use, it was not possible to establish a causal relationship with telmisartan intake);
• digestive tract: infrequently - diarrhea, abdominal pain, dyspepsia, vomiting, flatulence; rarely - dry mouth, discomfort in the stomach, dysgeusia;
• hepatobiliary system: rarely - impaired hepatic function / liver disease (mainly observed in patients in Japan);
• skin and subcutaneous fat: infrequently - itching, hyperhidrosis, skin rash; rarely - drug / toxic rash, urticaria, angioedema (possibly fatal), erythema, eczema;
• musculoskeletal and connective tissue: infrequently - back pain, myalgia, muscle spasms; rarely - pain in the extremities, arthralgia, pain in the tendons (symptoms are similar to the manifestation of tendonitis);
• kidneys and urinary tract: infrequently - impaired renal function, including acute renal failure;
• general disorders: infrequently - general weakness, chest pain; rarely - flu-like syndrome;
• data from laboratory and instrumental studies: infrequently - an increase in the content of creatinine in the blood; rarely - an increase in the concentration of uric acid, an increase in the activity of liver enzymes and creatine phosphokinase, a decrease in the serum hemoglobin level in the blood.

Overdose

No cases of telmisartan overdose have been identified.

Possible symptoms of intoxication: tachycardia, marked decrease in blood pressure, bradycardia.

Hemodialysis is ineffective, symptomatic therapy is recommended.

special instructions

Since telmisartan is excreted mainly in the bile, with cholestasis, obstruction of the biliary tract, severe liver dysfunction, class C according to the Child-Pugh classification, a decrease in the excretion of the drug is expected. It is contraindicated to take Telsartan to patients with these diseases. The drug is prescribed with caution in case of mild or moderate liver dysfunction, class A or B according to the Child-Pugh classification.

When treating vasorenal (secondary) hypertension with the use of drugs that affect the RAAS (renin-angiotensin-aldosterone system), in patients with bilateral renal artery stenosis or stenosis of an artery of a single kidney, the likelihood of developing renal failure and severe arterial hypotension is significantly increased. The use of Telsartan in patients with impaired renal function is recommended under the control of serum potassium and creatinine concentrations. There is no experience in the treatment of patients who have recently undergone kidney transplantation.

As a result of salt restriction, intensive diuretic therapy, diarrhea or vomiting, patients with hyponatremia and / or hypovolemia are more likely to develop symptomatic arterial hypotension, especially after the first dose of telmisartan. Given this, before starting treatment, it is necessary to ensure the restoration of the water and electrolyte balance.

With the simultaneous use of aliskiren-containing drugs, ACE inhibitors or ARA II, the risk of developing hyperkalemia, hypotension and impaired renal function (including acute renal failure) increases. As a result, the combined use of these drugs is not recommended for prescription, since it qualifies as a double blockade of the RAAS. In case of clinical necessity of using a double blockade of the RAAS, the patient needs to ensure strict medical supervision and careful monitoring of renal function, electrolyte concentration and blood pressure.

In diabetic nephropathy, the simultaneous use of ACE inhibitors and ARA II is prohibited.

In patients whose renal function and vascular tone determines the activity of the RAAS (with chronic heart failure or kidney disease, including stenosis of two renal arteries or stenosis of an artery of the only functioning kidney), due to the use of drugs that affect the RAAS, the development of arterial hypotension, oliguria, hyperazotemia and, in some cases, acute renal failure.

With primary hyperaldosteronism, resistance to antihypertensive drugs that affect the RAAS develops, and therefore telmisartan is not prescribed to patients with this diagnosis.

Patients with hemodynamically significant stenosis of the aortic and / or mitral valves or HOCMP (hypertrophic obstructive cardiomyopathy) Telsartan should be taken with caution.

In the case of using telmisartan for the treatment of patients with diabetes mellitus receiving insulin or oral hypoglycemic agents, hypoglycemia may develop. Patients are advised to regularly monitor the concentration of glucose in the blood and, if necessary, adjust the dose of hypoglycemic agents.

Drugs affecting the RAAS can cause hyperkalemia; before they are used simultaneously with telmisartan, the doctor assesses the balance of benefits and risks.

Factors contributing to an increased risk of developing hyperkalemia:

• diabetes mellitus, renal dysfunction, advanced age (over 70 years);
• combined use with drugs that affect the RAAS (ACE inhibitors, ARA II), and / or potassium-sparing diuretics (for example, amiloride, spironolactone, triamterene, eplerenone), NSAIDs [including those selectively acting in relation to cyclooxygenase-2 (COX -2)], preparations of potassium or potassium-containing substitutes for table salt, heparin, immunosuppressive drugs (cyclosporine or tacrolimus), as well as trimethoprim;
• concomitant pathological conditions, such as acute decompensated heart failure, dehydration, metabolic acidosis, renal failure, sudden progression of kidney disease (infectious lesions), conditions accompanied by tissue necrosis (for example, rhabdomyolysis, acute limb ischemia, extensive trauma).

The presence of one or more factors that increase the likelihood of developing hyperkalemia indicates the need for careful regular monitoring of the serum potassium content.

An ethnic feature of the Negroid race is a possible decrease in the level of renin in patients with arterial hypertension in comparison with representatives of other races. In this regard, ACE inhibitors and ARA II (including telmisartan) may have a less pronounced hypotensive effect on them.

As in the case of therapy with other antihypertensive drugs, a strong drop in blood pressure in patients with ischemic cardiomyopathy or coronary artery disease due to taking Telsartan can cause myocardial infarction or stroke.

Influence on the ability to drive vehicles and complex mechanisms

Special clinical studies to assess the effect of telmisartan on human psychomotor functions have not been conducted. Nevertheless, when performing potentially hazardous types of work, the possibility of developing such adverse reactions as dizziness and drowsiness should be considered. This requires caution when engaging in hazardous activities, including driving.

Application during pregnancy and lactation

The use of Telsartan is contraindicated for pregnant and breastfeeding women.

There are no adequate data on the use of telmisartan during pregnancy in women, but its reproductive toxicity has been identified in animal studies. Patients planning pregnancy are prescribed an alternative therapy with an established safety profile for use during gestation. If pregnancy is confirmed, Telsartan should be stopped immediately. The attending physician should consider alternative antihypertensive therapy options.

When using ARA II in women in the II – III trimesters of pregnancy, a fetotoxic effect on the fetus was noted, expressed by a decrease in renal function, a slowdown in ossification of the skull, a decrease in the amount of amniotic fluid, as well as neonatal toxicity (arterial hypotension, renal failure, hyperkalemia). In the case of using ARA II in the second trimester of pregnancy and later, it is necessary to carry out an ultrasound (ultrasound) examination of the bones of the skull and kidneys of the fetus. Newborns whose mothers received ARA II should be closely monitored for arterial hypotension.

There is insufficient data on the experience of using telmisartan during the lactation period, and therefore breastfeeding during therapy with Telsartan is not recommended. The doctor is obliged to prescribe alternative drugs with an established safety profile for use during breastfeeding, especially when feeding newborns and premature babies.

In the course of preclinical studies, the effect of telmisartan on the fertility of female and male animals was not observed.

Pediatric use

In pediatric practice, it is contraindicated to use Telsartan for the treatment of children and adolescents under the age of 18, because the effectiveness and safety of the drug for this age group have not been established.

With impaired renal function

Telsartan is prescribed with caution for the treatment of patients with bilateral renal artery stenosis or artery stenosis of a single functioning kidney, as well as for mild to moderate renal impairment. No dose adjustment is necessary.

Due to the fact that there is no experience with telmisartan in severe renal dysfunction and in patients on hemodialysis, it is recommended that such patients begin therapy with a dose of 20 mg / day.

For violations of liver function

It is contraindicated to use Telsartan for severe hepatic dysfunction, belonging to class C according to the Child-Pugh classification.

In case of mild and moderate hepatic insufficiency, classes A and B according to the Child-Pugh classification, the daily dose of Telsartan should not exceed 40 mg.

Use in the elderly

Since the effect of telmisartan on gerontological patients does not differ from that on younger patients, no dosage adjustment is required for them.

Drug interactions

Telmisartan, like other substances acting on the RAAS, increases the risk of hyperkalemia, which can be increased by concurrently used potassium-containing salt substitutes, potassium-sparing diuretics, ACE inhibitors, ARA II, NSAIDs (including those selective for COX type 2), heparin, immunosuppressive drugs (cyclosporine or tacrolimus), trimethoprim.

The presence of additional risk factors determines the incidence of hyperkalemia. It is especially likely to occur with the simultaneous use of Telsartan with potassium-sparing diuretics and potassium-containing salt substitutes. In the case of the combined use of the drug with ACE inhibitors or NSAIDs, a significant increase in serum potassium concentration (above 5.5 mEq / l) is unlikely, especially if safety measures are strictly followed.

When using telmisartan with other drugs / drugs, the following types of pharmacological interactions are likely:

• ACE inhibitors, ARA II or drugs containing aliskiren (double blockade of RAAS): increase the risk of developing hyperkalemia, arterial hypotension and renal dysfunction (including acute renal failure);
• digoxin: telmisartan increases the average value of the peak and residual levels of digoxin in the blood plasma (by 49 and 20%, respectively), which at the beginning of Telsartan administration, when adjusting its dose and in case of discontinuation of treatment, requires monitoring the serum digoxin concentration to maintain it within the therapeutic range;
• potassium preparations, potassium-sparing diuretics (for example, amiloride, spironolactone, triamterene, eplerenone), potassium-containing salt substitutes: these agents can cause a clinically significant increase in serum potassium levels; ARA II, including telmisartan, reduce diuretic-induced potassium loss; if the simultaneous use of the listed drugs with Telsartan is necessary, taking into account the proven hypokalemia, such treatment should be carried out with caution, constantly monitoring the potassium content in the blood serum;
• lithium preparations: telmisartan promotes a reversible increase in the lithium content in the blood plasma, accompanied by a toxic effect; if the simultaneous use of these drugs is necessary, treatment is required under the control of the serum concentration of lithium salts;
• non-selective NSAIDs, acetylsalicylic acid in a daily dose of 3 g or more, COX-2 inhibitors: these drugs can reduce the antihypertensive effect of ARA II; in patients with renal failure (due to old age or dehydration), ARA II and COX inhibitors, when used simultaneously with telmisartan, can cause a reversible deterioration in renal function. Therefore, the specified combination of drugs is used with caution, especially when treating elderly patients. Before taking them together with Telsartan, the patient's renal function is assessed, the water-electrolyte balance is corrected, and renal function is further monitored;
• ramipril: when combined with telmisartan, the AUC _0-24 and C _{max of} ramipril and its active metabolite, ramiprilat, increase 2.5 times; the clinical significance of this interaction has not been clarified;
• diuretic drugs (loop and thiazide): prior to taking telmisartan, high-dose diuretic treatment, including the loop diuretic furosemide and thiazide - hydrochlorothiazide, at the beginning of telsartan therapy can cause a decrease in circulating blood volume and increase the risk of arterial hypotension;
• other antihypertensive drugs (for example, baclofen or amifostine): potentiate the hypotensive properties of telmisartan, promoting a more pronounced decrease in blood pressure;
• barbiturates, ethanol, anesthetics, antidepressants: may contribute to the development of postural hypotension;
• corticosteroids for systemic use: inhibit the antihypertensive effect of Telsartan.

Analogs

The analogues of Telsartan are Mikardis, Teseo, Telminorm, Telmisartan Stada, Telmisartan-Richter, Telmisartan-SZ, Telmista, Telpres, etc.

Terms and conditions of storage

Store at temperatures up to 25 ° C. Keep out of the reach of children.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Telsartan

All patient reviews about Telsartan are positive. The drug, subject to regular intake once a day for a long time, stably stabilizes blood pressure. No negative adverse reactions have been reported. A pleasant bonus for hypertensive patients is the reduction in the risk of death from cardiovascular diseases when taken regularly over the age of 55.

There are no complaints about the cost, but to reduce the cost of therapy, if it is necessary to take a daily dose of 40 mg, it is recommended to purchase the agent at a dosage of 80 mg and divide the pill in half, which makes it easy to make a dividing risk.

The price of Telsartan in pharmacies

The approximate price for Telsartan, depending on the dosage and the number of tablets in the package, is:

• tablets 40 mg: 14 pcs. - 329 rubles; 30 pcs. - 226-268 rubles;
• tablets 80 mg: 14 pcs. - 364 rubles; 30 pcs. - 294–325 rubles.

Telsartan: prices in online pharmacies

Drug name Price Pharmacy

Telsartan 40 mg film-coated tablets 30 pcs. 252 RUB Buy

Telsartan 40mg tablets 30 pcs. 265 RUB Buy

Telsartan N 12.5 mg + 40 mg tablets 28 pcs. 289 r Buy

Telsartan 80 mg film-coated tablets 30 pcs. 299 r Buy

Telsartan tablets 80mg 30 pcs. 304 RUB Buy

Telsartan N tablets 12.5mg + 40mg 28 pcs. RUB 319 Buy

Telsartan AM 5 mg + 40 mg film-coated tablets 28 pcs. 329 r Buy

Telsartan AM tablets 5mg + 40mg 28 pcs. 347 r Buy

Telsartan AM 5 mg + 80 mg tablets 28 pcs. 363 r Buy

Telsartan N 12.5 mg + 80 mg tablets 28 pcs. 369 r Buy

Telsartan AM 10 mg + 40 mg film-coated tablets 28 pcs. 389 r Buy

Telsartan N tablets 12.5mg + 80mg 28 pcs. 398 RUB Buy

Telsartan AM tablets 10mg + 40mg 28 pcs. RUB 400 Buy

Telsartan AM tablets 5mg + 80mg 28 pcs. 419 RUB Buy

Telsartan AM 10 mg + 80 mg tablets 28 pcs. 489 r Buy

See all offers from pharmacies

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!