Telmisartan - Instructions For Use, Price, Reviews, Tablet Analogs

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

Telmisartan

Telmisartan: 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: Telmisartan

ATX code: C09CA07

Active ingredient: Telmisartan (Telmisartan)

Manufacturer: Ozone LLC (Russia)

Description and photo update: 2019-10-07

Prices in pharmacies: from 145 rubles.

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Telmisartan is an angiotensin II receptor antagonist.

Release form and composition

Dosage form - tablets: round, flat-cylindrical, with a line and a chamfer, white or white-yellowish color (5, 7, 10 and 20 pcs. In blister contour packs, in a cardboard box 1, 2, 3, 4, 5, 8 or 10 packs; 10, 20, 28, 30, 40, 50 and 100 pcs. in cans, sealed with pull-off lids with first opening control or screw lids with a “push-turn” system or with first opening control, in a cardboard box 1 bank. Each pack also contains instructions for the use of Telmisartan).

Composition of 1 tablet:

• active ingredient: telmisartan - 40 or 80 mg;
• excipients (40/80 mg tablets): croscarmellose sodium 12/24 mg, sodium hydroxide 3.35 / 6.7 mg, povidone-K25 12/24 mg, lactose monohydrate (milk sugar) 296.85 / 474.9 mg, magnesium stearate - 3.80 / 6.4 mg, meglumine - 12/24 mg.

Pharmacological properties

Pharmacodynamics

Telmisartan is a specific angiotensin II receptor (ARA II) antagonist (type AT ₁). It is characterized by a high affinity for the AT ₁ subtype of angiotensin II receptors (AT II), through which the action of AT II is realized.

The drug displaces AT II from the connection with the receptor, while it does not exhibit the properties of an antagonist in relation to it. The association with the AT ₁ receptor subtype is long-term.

Telmisartan does not bind to other subtypes of AT II receptors, has no affinity for other receptors, including AT ₂ receptors and other less studied AT receptors. Their functional significance, as well as the effect of possible excessive stimulation of these receptors by angiotensin II, the concentration of which increases under the influence of telmisartan, have not been studied.

The drug reduces the plasma concentration of aldosterone. Does not affect the activity of renin in blood plasma. Does not block ion channels. Does not inhibit the angiotensin-converting enzyme (ACE, kininase II), which also accelerates the degradation of bradykinin, so it does not cause side effects due to the influence of bradykinin (for example, dry cough).

Arterial hypertension

The use of telmisartan at a dose of 80 mg completely blocks the hypertensive effect of AT II. The antihypertensive effect develops within about 3 hours after taking the first dose, persists for 24 hours and remains significant up to 48 hours. A pronounced therapeutic effect usually develops after 4-8 weeks of regular administration of the drug.

In hypertension, telmisartan lowers systolic and diastolic blood pressure (BP) without affecting the heart rate (HR).

After an abrupt discontinuation of the drug, the blood pressure level returns to its original value within several days. Withdrawal syndrome does not develop.

According to comparative clinical studies, the hypotensive effect of telmisartan is comparable to that of drugs of other classes (for example, atenolol, hydrochlorothiazide, enalapril, lisinopril, amlodipine). At the same time, dry cough in patients treated with telmisartan occurred much less frequently than in patients taking ACE inhibitors.

Prevention of cardiovascular diseases

In patients 55 years of age and older with a transient ischemic attack, stroke, coronary artery disease (CAD), peripheral arterial lesions and complications of type 2 diabetes mellitus (such as left ventricular hypertrophy, micro- or macroalbuminuria, retinopathy) in the history of to the risk group for cardiovascular complications, telmisartan had an effect similar to that of ramipril in reducing the primary combined endpoint: hospitalization due to chronic heart failure, nonfatal stroke, nonfatal myocardial infarction, cardiovascular mortality.

Telmisartan, similar to ramipril, has also been shown to be effective in reducing the frequency of secondary points: non-fatal stroke, non-fatal myocardial infarction, cardiovascular mortality.

The efficacy of telmisartan at doses less than 80 mg for reducing the risk of cardiovascular mortality has not been studied.

Unlike ramipril, telmisartan was less likely to cause side effects such as dry cough and angioedema. However, against the background of its administration, arterial hypotension occurred more often.

Pharmacokinetics

When administered orally, the drug is rapidly absorbed in the gastrointestinal tract. The bioavailability of telmisartan is approximately 50%. Simultaneous food intake reduces the AUC (area under the pharmacological curve) by 6-19%, depending on the dose (40-160 mg). After 3 hours after using the drug, the plasma concentration levels out regardless of the time of the meal.

It is assumed that a small decrease in AUC cannot cause a decrease in the therapeutic effect. There is no linear dependence of the plasma concentration of telmisartan on the dose taken. When using the drug in doses of more than 40 mg AUC and especially the maximum plasma concentration (C _max) increase disproportionately.

Telmisartan is characterized by a high binding to plasma proteins (more than 99.5%), mainly with alpha-1 acid glycoprotein and albumin. At equilibrium, the average apparent volume of distribution (V _d) is approximately 500 liters.

Telmisartan is metabolized by conjugation with glucuronide. The conjugate has no pharmacological activity.

The drug is characterized by the pharmacokinetics of biexponential disintegration with a terminal half-life (T _1/2) of more than 20 hours. AUC and especially C _max disproportionately increase with dose. There are no data to support the clinical significance of telmisartan accumulation when taken in therapeutic doses.

After oral and intravenous administration, telmisartan is excreted mainly through the intestines, mainly unchanged. No more than 1% is excreted by the kidneys.

Total plasma clearance is about 1000 ml / min, hepatic blood flow is about 1500 ml / min.

Pharmacokinetics in special cases:

• gender: in women, the C _max and AUC of telmisartan are higher than in men, approximately 3 and 2 times, respectively, however, no differences in the effectiveness of the drug were identified;
• advanced age: in patients aged less than and more than 65 years, the pharmacokinetics of the drug does not differ significantly;
• renal function: patients with renal insufficiency, including those receiving hemodialysis, are advised to start treatment with a lower dose (20 mg), no adjustment to the usual therapeutic dose is required. Telmisartan is highly bound to plasma proteins and is not excreted during dialysis;
• liver function: in patients with hepatic insufficiency, according to pharmacokinetic studies, the bioavailability of telmisartan reaches almost 100%. T _1/2 does not change.

Indications for use

• treatment of arterial hypertension;
• reduction of cardiovascular morbidity and mortality in the presence of their high risk in patients aged 55 years and older.

Contraindications

Absolute:

• severe functional disorders of the liver (class C according to the Child-Pugh classification);
• obstructive diseases of the biliary tract;
• lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
• pregnancy;
• lactation;
• age up to 18 years;
• concomitant administration of ACE inhibitors to patients with diabetic nephropathy;
• joint use in patients with diabetes mellitus and / or moderate / severe renal impairment [glomerular filtration rate (GFR) <60 ml / min / 1.73 m ² body surface area] aliskiren or preparations containing it;
• hypersensitivity to any component of the drug.

Relative (Telmisartan tablets should be used with caution):

• hypertrophic obstructive cardiomyopathy;
• stenosis of the aortic and / or mitral valve;
• chronic heart failure;
• hyperkalemia;
• hyponatremia;
• bilateral stenosis of the renal arteries or stenosis of an artery of a solitary kidney;
• condition after kidney transplantation;
• mild to moderate renal and / or liver dysfunction;
• primary hyperaldosteronism;
• a decrease in circulating blood volume (BCC) due to restriction of sodium chloride intake, previous diuretic therapy, diarrhea or vomiting;
• belonging to the Negroid race.

Telmisartan, instructions for use: method and dosage

Telmisartan tablets should be taken orally, regardless of the time of meals.

For arterial hypertension, the initial dose is 40 mg once a day. For some patients, a dose of 20 mg (½ 40 mg tablet) is sufficient. If the desired therapeutic effect is not achieved, the dose is increased to 80 mg once a day, or a thiazide diuretic (eg, hydrochlorothiazide) is prescribed in addition. When increasing the dose, it is important to take into account that the maximum antihypertensive effect develops within 4-8 weeks after starting telmisartan.

To reduce cardiovascular morbidity and mortality, the recommended dose is 80 mg once a day. Treatment is carried out under the control of blood pressure and, if necessary, reduce the dose of antihypertensive drugs.

Patients with severe renal failure and patients receiving hemodialysis are recommended to start treatment with a daily dose of 20 mg.

Patients with mild to moderate hepatic impairment should not exceed a daily dose of 40 mg.

Side effects

The incidence of side effects with telmisartan is generally comparable to that of placebo (41.4% and 43.9%, respectively), it does not depend on the dose and does not correlate with the patient's gender, age and race.

The following adverse reactions are classified as follows: very often - ≥ 1/10, often - from ≥ 1/100 to <1/10, infrequently - from ≥ 1/1000 to <1/100, rarely - from ≥ 1/10 000 to <1/1000, very rarely - <1/10 000, unknown frequency - insufficient data available to estimate frequency:

• infections and invasions: infrequently - infections of the urinary tract (including cystitis) and upper respiratory tract (including sinusitis and pharyngitis); unknown frequency - sepsis, up to death;
• nervous system and psyche: infrequently - insomnia, syncope (fainting), depression; rarely - anxiety;
• cardiovascular system: infrequently - a marked decrease in blood pressure (most often occurs in patients with controlled blood pressure when using telmisartan to reduce the risk of cardiovascular mortality in addition to standard treatment), orthostatic hypotension, bradycardia; rarely - tachycardia;
• immune system: rarely - hypersensitivity reactions; unknown frequency - anaphylactic reactions;
• blood and lymphatic system: infrequently - anemia; rarely, thrombocytopenia; unknown frequency - eosinophilia;
• nutrition and metabolism: infrequently - hyperkalemia;
• digestive system: infrequently - flatulence, abdominal pain, vomiting, dyspepsia, diarrhea; rarely - dysgeusia, dryness of the oral mucosa, discomfort, indigestion;
• respiratory system: infrequently - shortness of breath; very rarely - interstitial lung disease (noted in a post-marketing study; a causal relationship with the use of telmisartan has not been established);
• urinary system: infrequently - renal failure (including acute);
• hepatobiliary system: rarely - functional liver disorder or liver disease (noted in a post-marketing study, mainly in residents of Japan);
• musculoskeletal system and connective tissue: infrequently - muscle cramps, back pain (for example, sciatica), myalgia; rarely - pain in the limbs, arthralgia; unknown frequency - pain in the tendon area (tendinitis-like symptoms);
• organs of sight, hearing and balance: infrequently - vertigo; rarely - visual impairment;
• skin, subcutaneous tissue: infrequently - itching, skin rashes, hyperhidrosis; rarely - eczema, drug rash, erythema, toxic skin rash, angioedema (including fatal); unknown frequency - urticaria;
• laboratory indicators: infrequently - an increase in blood creatinine levels; rarely - hypoglycemia (in patients with diabetes mellitus), a decrease in hemoglobin, an increase in the concentration of uric acid in the blood, the activity of liver enzymes and creatine phosphokinase in the blood serum;
• others: infrequently - weakness, chest pain; rarely, flu-like condition.

Overdose

There are no reports of cases of overdose of telmisartan. A pronounced decrease in blood pressure and the development of tachycardia are assumed, an increase in serum creatinine concentration, dizziness, bradycardia, acute renal failure is also possible.

In case of taking an excessive dose of the drug, the patient should be provided with careful medical supervision, including the control of plasma creatinine and electrolyte levels. Hemodialysis is not effective. Treatment is supportive and symptomatic. Therapeutic methods are determined depending on the time elapsed since telmisartan was taken and the severity of symptoms. If a little time has passed since the moment when the patient took a high dose of the drug, it is recommended to induce vomiting and / or gastric lavage and take activated charcoal. In the case of a pronounced decrease in blood pressure, the patient needs to lay down and raise his legs, and replenishment of the volume of circulating blood and electrolytes is also required.

special instructions

Before prescribing Telmisartan and regularly during its use, blood pressure, serum potassium levels, and renal function should be monitored. The development of transient arterial hypotension is not a contraindication to further taking the drug, provided that blood pressure is stabilized. If severe arterial hypotension develops repeatedly, it is necessary to reduce the dose or discontinue therapy.

Before the appointment of Telmisartan, the deficiency of fluid and / or sodium should be eliminated, since in this case the likelihood of developing symptomatic arterial hypotension is high, especially after taking the first dose of the drug. A decrease in BCC and sodium content is often noted due to diarrhea, vomiting, or restriction of sodium chloride intake during diuretic therapy.

Treatment of patients with impaired renal function and renal insufficiency should be accompanied by monitoring of serum creatinine concentration and potassium content. There is no experience with telmisartan in renal transplant patients.

Medicines that affect the renin-angiotensin-aldosterone system (RAAS) increase the risk of severe arterial hypotension and renal failure in patients with bilateral renal artery stenosis or stenosis of a solitary kidney artery.

Avoid the use of Telmisartan in patients with severe liver dysfunction, biliary obstruction and cholestasis, since the drug is excreted from the body mainly with bile. In such patients, a decrease in the hepatic clearance of the drug is expected. Mild to moderate hepatic impairment requires special care.

In predisposed patients, due to inhibition of the RAAS, especially in the case of the simultaneous use of drugs that also affect this system, adverse reactions such as arterial hypotension, hyperkalemia, fainting, impaired renal function (including acute renal failure) were noted. Double blockade of RAAS (for example, adding an ACE inhibitor to ARA II) is not recommended for patients with already controlled blood pressure. It is possible in exceptional cases, and requires enhanced monitoring of renal function, including periodic determination of the level of potassium and creatinine in the blood plasma.

In patients in whom renal function and vascular tone depend mainly on the activity of the RAAS (for example, patients with kidney disease, including renal artery stenosis, or chronic heart failure), the use of drugs that affect the RAAS, including Telmisartan, is associated with the development of complications such as oliguria, hyperazotemia, acute arterial hypotension, in rare cases - acute renal failure.

Antihypertensive drugs that inhibit the RAAS, as a rule, are ineffective in patients with primary hyperaldosteronism, therefore, the appointment of Telmisartan to them is not recommended.

RAAS inhibitors can cause hyperkalemia, which is fatal in elderly patients, patients with arterial hypertension, coronary heart disease, diabetes mellitus, renal failure or other concomitant diseases, as well as in people receiving drugs that can increase potassium levels. In this regard, before the appointment of Telmisartan, the balance of benefits and risks should be carefully evaluated.

The main risk factors to be considered are:

• age over 70;
• renal failure;
• diabetes;
• intercurrent diseases, especially metabolic acidosis, dehydration, a sharp deterioration in the condition of the kidneys (for example, with an infectious disease), impaired renal function, acute heart failure, cytolysis syndrome (for example, severe trauma, acute limb ischemia, rhabdomyolysis);
• the simultaneous use of one or more drugs that affect the RAAS, and / or an increase in the level of potassium in the blood serum. Potassium-containing salt substitutes, potassium-sparing diuretics, ARA II, ACE inhibitors, non-steroidal anti-inflammatory drugs (including selective COX-2 inhibitors), trimethoprim, heparin, immunosuppressants (tacrolimus, cyclosporine) can cause hyperkalemia.

In patients at risk, it is recommended to periodically check the serum potassium content.

In the presence of additional cardiovascular risks (for example, coronary heart disease) in diabetic patients, antihypertensive drugs such as ARA II and ACE inhibitors can increase the risk of sudden cardiovascular death and fatal myocardial infarction. It should be borne in mind that IHD can be asymptomatic, that is, not be diagnosed. In this regard, in diabetes mellitus, prior to the appointment of Telmisartan, appropriate diagnostic studies are required, including an exercise test.

Like other ARAs II, telmisartan is less effective in lowering blood pressure in black patients than in other populations. This is probably due to their greater predisposition to a decrease in renin activity.

An excessive decrease in blood pressure in patients with coronary artery disease and ischemic cardiomyopathy can lead to stroke or myocardial infarction.

Influence on the ability to drive vehicles and complex mechanisms

Special clinical studies on the effect of telmisartan on human psychomotor functions have not been conducted. Given the likelihood of developing some side effects (such as drowsiness and dizziness), patients are advised to be careful when driving and working with complex equipment.

Application during pregnancy and lactation

There is no experience of using telmisartan in pregnant women. Animal studies have shown reproductive toxicity. In this regard, the drug is contraindicated during pregnancy. If pregnancy occurs during therapy, telmisartan should be discontinued immediately and an alternative antihypertensive agent belonging to the classes of substances that does not have embryotoxic and teratogenic effects should be prescribed, if necessary.

According to clinical observations, angiotensin II receptor antagonists used in the II and III trimesters of pregnancy have a toxic effect, which is manifested by oligohydramnios, deterioration of renal function and delayed ossification of the skull in the fetus, arterial hypotension, hyperkalemia and renal failure in the newborn. When using ARA II during the second trimester of pregnancy, it is recommended to conduct an ultrasound examination of the kidneys and fetal skull.

Newborns whose mothers took ARA II during pregnancy should be monitored for the development of arterial hypotension.

It is not known whether telmisartan is excreted in breast milk. In animal studies, it was found that the drug penetrates into the milk of lactating females. In this regard, during lactation, the appointment of telmisartan is contraindicated, or the woman may be advised to transfer the child to artificial feeding.

Pediatric use

Telmisartan is contraindicated in children and adolescents under 18 years of age due to the lack of data on its safety and efficacy in this category of patients.

With impaired renal function

Relative contraindications to the appointment of Telmisartan are bilateral stenosis of the renal arteries, stenosis of the artery of a single kidney and the condition after kidney transplantation.

No dose adjustment is required in patients with mild to moderate renal impairment. In the case of severe renal impairment, the recommended starting daily dose is 20 mg.

For violations of liver function

Caution should be exercised in case of mild and moderate liver dysfunctions (class A and B according to the Child-Pugh classification), the daily dose should not exceed 40 mg.

Telmisartan is contraindicated in patients with severely impaired liver function (class C according to the Child-Pugh classification).

Use in the elderly

Elderly patients do not need to change the dose of the drug.

Drug interactions

• other antihypertensive drugs: there is an increase in the antihypertensive effect;
• antidepressants, barbiturates, drugs, ethanol: orthostatic hypotension may increase;
• systemic corticosteroids: the hypotensive effect of telmisartan is weakened;
• lithium preparations: a reversible increase in the plasma concentration of lithium and the development of its toxicity is possible (it is necessary to carefully monitor the lithium content in the blood);
• ramipril: the C _max and AUC of ramipril and its metabolite ramiprilat increase 2.5 times, however, the clinical significance of this phenomenon has not been established;
• loop diuretics (for example, furosemide) and thiazide diuretics (for example, hydrochlorothiazide): when used in high doses, hypovolemia and arterial hypotension may develop at the beginning of treatment with telmisartan;
• digoxin: its maximum concentration increases by an average of 49%, the minimum concentration - by 20% (it is required to carefully monitor the plasma level of digoxin at the beginning of treatment, in case of any dose change and in the process of discontinuation of therapy; if necessary, adjust the dose);
• drugs that can cause hyperkalemia, such as potassium-sparing diuretics (eplerenone, spironolactone, amiloride, triamterene), potassium-containing salt substitutes, potassium-containing dietary supplements, ARA II, ACE inhibitors, non-steroidal anti-inflammatory drugs (including 2-cyclooxygenase inhibitors) immunosuppressants (cyclosporine, tacrolimus), trimethoprim, heparin: the risk of developing hyperkalemia increases (precautions and periodic monitoring of the level of potassium in the blood plasma are required);
• nonsteroidal anti-inflammatory drugs (NSAIDs), including COX-2 inhibitors, acetylsalicylic acid in daily doses of 3000 mg and non-selective NSAIDs: the hypotensive effect of telmisartan may be weakened. In some cases, with impaired renal function (for example, in elderly patients or those with dehydration), the combined use of ARA II and COX-2 inhibitors can cause further deterioration of renal function, up to acute renal failure (usually reversible). The use of such combinations should be done with caution, especially in the elderly. Ensure adequate fluid intake and monitor renal function;
• ACE inhibitors, aliskiren: double blockade of the RAAS develops, which is associated with an increased incidence of side effects such as hyperkalemia, arterial hypotension, and functional renal impairment (up to acute renal failure). The simultaneous use of telmisartan and aliskiren is not recommended for all patients, it is strictly contraindicated in patients with renal insufficiency (GFR <60 ml / min / 1.73 m ²) and diabetes mellitus. The combined use of telmisartan and ACE inhibitors is contraindicated in diabetic nephropathy.

Analogs

Telmisartan analogs are Angiakand, Aprovel, Artinova, Atakand, Bloktran, Valaar, Vazotenz, Valsartan, Valz, Giposart, Diovan, Irbesartan, Kanarb, Kandesartan, Kozaar, Lozap, Lorista, Mikardis, Nortivan, Ordenyse, Prezardartan, Edarbi et al.

Terms and conditions of storage

Store at a temperature not exceeding 25 ° C out of reach of children.

The shelf life is 3 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Telmisartan

According to doctors, Telmisartan is an effective antihypertensive agent. Its important advantage is the absence of an effect on the heart rate, which allows prescribing the drug to patients with concomitant cardiovascular diseases.

Patients also leave positive reviews about Telmisartan: the drug normalizes blood pressure, is well tolerated, and has an affordable cost. There are practically no reports of side effects, in rare cases dizziness and blurred vision are mentioned.

The price of Telmisartan in pharmacies

The price of Telmisartan depends on the dosage, the number of tablets in the package, the pharmacy network and the region of sale. The approximate cost of 40 mg tablets (14 pieces in a package) is 428 rubles, 80 mg each (28 pieces in a package) is 310–325 rubles.

Telmisartan: prices in online pharmacies

Drug name Price Pharmacy

Telmisartan 40 mg tablets 14 pcs. RUB 145 Buy

Telmisartan 80 mg tablets 28 pcs. 254 r Buy

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!