Telmista tabs 80mg #84

Telmista user manual

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Telmista is an antihypertensive drug.

Release form and composition

Dosage form - tablets: almost white or white; at a dose of 20 mg - round, 40 mg - biconvex, oval, 80 mg - biconvex, capsule-shaped (in a blister made of a combined material 7 pcs., in a cardboard box 2, 4, 8, 12 or 14 blisters; in a blister 10 pcs., in a cardboard box 3, 6 or 9 blisters).
Composition of one tablet:
    active substance: telmisartan - 20, 40 or 80 mg;
    excipients: sodium hydroxide, lactose monohydrate, magnesium stearate, meglumine, povidone K30, sorbitol (E420).

Pharmacodynamics

Telmisartan, the active substance of Telmista, has antihypertensive properties, being an angiotensin II receptor antagonist (AT1 receptor blocker). By displacing angiotensin II from the binding to the receptor, it does not have an agonist effect on this receptor. Telmisartan selectively and for a long time can bind only to angiotensin II subtype AT1 receptors. It has no affinity for other angiotensin receptors, the functional significance of which and the result of the excessive (due to the use of telmisartan) the effect of angiotensin II on them has not been studied.
Telmisartan reduces the content of aldosterone in the blood plasma, does not affect the concentration of renin and does not block ion channels. The active substance does not suppress ACE (angiotensin converting enzyme), which also destroys bradykinin, therefore, there are no side reactions caused by bradykinin.
Telmisartan, taken at a dose of 80 mg, completely blocks the hypertensive effect of angiotensin II. After the first intake of the drug within 3 hours, the onset of the hypotensive effect is noted, the effect persists for a day and remains significant for up to two days. A stable hypotensive effect usually develops within 4–8 weeks from the start of treatment with regular telmisartan administration.
With arterial hypertension, the drug helps to reduce systolic and diastolic blood pressure (BP). Telmisartan has no effect on heart rate (heart rate).
In patients with a sharp cancellation of telmisartan, blood pressure gradually returns to its original value, there is no withdrawal syndrome.

Pharmacokinetics

    absorption: when taken orally, it is rapidly absorbed in the gastrointestinal tract. Bioavailability is 50%. When taken simultaneously with food, the decrease in AUC (area under the pharmacokinetic curve) is in the range from 6% to 19% at a dose of 40 and 160 mg, respectively. 3 hours after taking telmisartan, its concentration in the blood plasma levels off (does not depend on the time of the meal). AUC and maximum concentration of a substance in blood plasma (Cmax) in women is approximately 2 and 3 times higher, respectively, than in men. At the same time, no significant effect on efficiency was noted;
    distribution and metabolism: 99.5% of the substance binds to plasma proteins (mainly with alpha-1 glycoprotein and albumin). The apparent volume of distribution in equilibrium concentration is on average 500 liters. Metabolism occurs by conjugation with glucuronic acid to form pharmacologically inactive metabolites;
    Excretion: T1 / 2 (half-life) - more than 20 hours. The substance is mainly excreted unchanged through the intestines, with urine - less than 2%. The total plasma clearance is quite high compared to the hepatic blood flow (approximately 1500 ml / min) and is about 900 ml / min.
The main pharmacokinetic parameters of telmisartan when used in children and adolescents aged 6 to 18 years for 4 weeks at a dose of 1 or 2 mg / kg are generally comparable to those in adult patients and confirm the nonlinearity of the pharmacokinetics of the active substance, especially in relation to Cmax ...

Indications for use

    arterial hypertension;
    high risk of cardiovascular diseases in patients over 55 years of age - to reduce cardiovascular morbidity and mortality.

Contraindications

Absolute:
    severe forms of liver dysfunction (according to the Child-Pugh classification - class C);
    obstruction of the biliary tract;
    combined use with aliskiren in patients with severe or moderate renal failure (glomerular filtration rate less than 60 ml / min / 1.73 m2) or with diabetes mellitus;
    lactase / sucrase / isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption;
    pregnancy and lactation period;
    age under 18;
    individual hypersensitivity to telmisartan or any of the auxiliary components of the drug.
Relative (diseases / conditions in which the use of Telmista requires caution):
    impaired renal and / or liver function;
    bilateral stenosis of the renal arteries or stenosis of an artery of a solitary kidney;
    conditions after kidney transplantation (due to lack of experience in use);
    hyperkalemia;
    hyponatremia;
    chronic heart failure;
    narrowing of the mitral and / or aortic valve;
    GOKMP (hypertrophic obstructive cardiomyopathy);
    decrease in BCC (circulating blood volume) due to previous treatment with diuretics, limited intake of table salt, vomiting or diarrhea;
    primary hyperaldosteronism (safety and efficacy have not been established).

Instructions for use: method and dosage

Telmista tablets are taken orally, regardless of the time of the meal.
With arterial hypertension, it is recommended to start taking with 20 or 40 mg of the drug once a day. In some patients, it is possible to achieve a hypotensive effect at a dose of 20 mg / day. In case of insufficient therapeutic effect, the dose can be increased to a maximum daily dose of 80 mg. When increasing the dose, it should be borne in mind that the maximum hypotensive effect of Telmista is usually achieved after 4-8 weeks from the start of therapy.
To reduce cardiovascular morbidity and mortality, it is recommended to take 80 mg of the drug once a day.
At the initial stage of treatment, additional methods of blood pressure normalization may be required.
It is not required to adjust the dosage regimen for patients with renal insufficiency, including those on hemodialysis.
In case of liver dysfunctions of mild or moderate severity (according to the Child-Pugh classification - class A and B), the maximum daily dose of Telmista is 40 mg.
In elderly patients, the pharmacokinetics of telmisartan does not change, so there is no need to adjust the dose of the drug for them.

Side effects

When using Telmista, the following side reactions from systems and organs are possible:
    heart: tachycardia, bradycardia;
    vessels: orthostatic hypotension, significant decrease in blood pressure;
    digestive system: diarrhea, abdominal pain, dyspepsia, stomach discomfort, flatulence, vomiting, dysgeusia (taste perversion), dry oral mucosa, liver dysfunction / liver disease;
    blood and lymphatic system: thrombocytopenia, eosinophilia, anemia, sepsis (including fatal sepsis);
    nervous system: insomnia, anxiety, depression, vertigo, fainting;
    immune system: hypersensitivity (urticaria, erythema, angioedema), anaphylactic reactions, pruritus, eczema, skin rash (including drug), hyperhidrosis, angioedema (even fatal), toxic skin rash;
    organ of vision: visual disturbances;
    respiratory system, chest and mediastinal organs: cough, shortness of breath, upper respiratory tract infections, interstitial lung diseases (a causal relationship with the use of telmisartan has not been established);
    musculoskeletal and connective tissue: back pain, arthralgia, muscle spasms (calf muscle cramps), myalgia, leg pain, tendon pain (symptoms similar to inflammation and degeneration of tendon tissue);
    kidneys and urinary tract: impaired renal function (including acute renal failure), urinary tract infections (including cystitis);
    the body as a whole: general weakness, flu-like syndrome, chest pain;
    instrumental and laboratory studies: an increase in the content of uric acid, creatinine in the blood plasma, a decrease in the level of hemoglobin, an increase in the activity of hepatic transaminases, CPK (creatine phosphokinase) in the blood plasma, hypoglycemia (in patients with diabetes mellitus), hyperkalemia.
The relationship between the degree of manifestation of side effects with age, gender or race of patients has not been established.

Overdose

In case of an overdose of Telmista, the following symptoms may appear: tachycardia, bradycardia, a significant decrease in blood pressure.
Symptomatic treatment is recommended. Hemodialysis is not effective for the elimination of telmisartan.

Special instructions

The simultaneous use of Telmista and ACE inhibitors or a direct renin inhibitor, aliskiren, due to the double effect on the RAAS (renin-angiotensin-aldosterone system) impairs renal function (including may lead to acute renal failure), and also increases the risk of arterial hypotension and hyperkalemia ... If such joint therapy is absolutely necessary, it should be carried out under close medical supervision, as well as regularly check kidney function, blood pressure and electrolytes in the blood plasma.
In patients with diabetic nephropathy, it is not recommended to use telmisartan and ACE inhibitors simultaneously.
In cases where vascular tone and renal function depend mainly on the activity of the RAAS (for example, in patients with kidney diseases, including bilateral renal artery stenosis or stenosis of a single kidney artery, or with chronic heart failure), the use of drugs affecting the RAAS can lead to the development of hyperazotemia, acute arterial hypotension, oliguria and acute renal failure (in rare cases).
When used together with Telmista potassium-sparing diuretics, potassium-containing salt substitutes, supplements and other drugs that increase the concentration of potassium in the blood plasma (for example, heparin), it is necessary to control the level of potassium in the blood.
Since telmisartan is excreted mainly in the bile, with obstructive diseases of the biliary tract or impaired liver function, a decrease in the clearance of the drug is possible.
With diabetes mellitus and additional cardiovascular risk, for example, coronary artery disease (coronary artery disease), Telmista can cause fatal myocardial infarction and sudden cardiovascular death. In patients with diabetes mellitus, IHD may not be diagnosed, since its symptoms in this case do not always appear. Therefore, before starting drug therapy, it is necessary to conduct appropriate diagnostic examinations, including an exercise test.
In patients with diabetes mellitus receiving treatment with insulin or oral hypoglycemic drugs, hypoglycemia may develop during therapy with Telmista. Such patients need to control the concentration of glucose in the blood, since, depending on this indicator, the dose of insulin or hypoglycemic drugs must be adjusted.
In primary hyperaldosteronism, the use of antihypertensive drugs - RAAS inhibitors - is usually not effective. It is not recommended for such patients to take Telmista.
The use of the drug is possible in combination with thiazide diuretics, since such a combination provides an additional decrease in blood pressure.
Studies have shown that Telmista is less effective in patients of the Negroid race. Liver dysfunctions with telmisartan have been observed in most cases in Japan.

Influence on the ability to drive vehicles and complex mechanisms

When driving vehicles and performing all types of activities requiring a quick mental, motor reaction and increased attention, it is necessary to take into account the likelihood of drowsiness and dizziness during drug treatment and be careful.

Application during pregnancy and lactation

According to the instructions, Telmista is contraindicated during pregnancy. If pregnancy is diagnosed, the drug should be stopped immediately. If necessary, antihypertensive drugs of other classes, approved for use during pregnancy, should be prescribed. Alternative therapy is also recommended for women planning a pregnancy.
In preclinical studies of the drug, teratogenic effects were not revealed. But it was found that the use of angiotensin II receptor antagonists in the second and third trimesters of pregnancy causes fetotoxicity (oligohydramnios, decreased renal function, slowing of ossification of the fetal skull bones) and neonatal toxicity (arterial hypotension, renal failure, hyperkalemia).
Newborns whose mothers took Telmista during pregnancy require medical supervision due to the possible development of arterial hypotension.
Since there is no information on the penetration of telmisartan into breast milk, the drug is contraindicated to be taken during breastfeeding.

Childhood use

The safety and efficacy of telmisartan in pediatrics has not been established, therefore, Telmista tablets 40 mg, 80 mg and 20 mg are prohibited for prescribing to children and adolescents under 18 years of age.

With impaired renal function

In patients with impaired renal function, the use of the drug requires caution.
In severe or moderate renal failure (glomerular filtration rate less than 60 ml / min / 1.73 m2), the joint appointment of Telmista and aliskiren is contraindicated.

For violations of liver function

It is not recommended to take the drug in patients with severely impaired liver function (according to the Child-Pugh classification - class C).
In case of mild to moderate hepatic insufficiency (according to the Child-Pugh classification - class A and B), the use of Telmista requires caution. The maximum daily dose of the drug in this case should not exceed 40 mg.

Use in the elderly

There is no need to adjust the dose of Telmista for elderly patients.

Drug interactions

The use of telmisartan concurrently with certain drugs can lead to the development of the following effects:
    antihypertensive drugs: increased antihypertensive effect;
    warfarin, digoxin, ibuprofen, glibenclamide, hydrochlorothiazide, paracetamol, amlodipine and simvastatin: no clinically significant interaction was observed. In some cases, it is possible to increase the content of digoxin in the blood plasma by an average of 20%. When used together with digoxin, it is recommended to periodically monitor its plasma concentration;
    potassium-sparing diuretics (for example, spironolactone, amiloride, triamterene, eplerenone), potassium-containing substitutes, ACE inhibitors, angiotensin II receptor antagonists, NSAIDs (non-steroidal anti-inflammatory drugs), including selective inhibitors of cyclooxygenase, or tacoxygenase-inhibitors and trimethoprim: increased risk of hyperkalemia (due to synergistic effect);
    ramipril: 2.5-fold increase in Cmax and AUC0-24 ramipril and ramiprilat;
    lithium preparations: a reversible increase in the concentration of lithium in the blood plasma (have been reported in rare cases) with an accompanying toxic effect. It is recommended to periodically check the plasma lithium level;
    NSAIDs (including acetylsalicylic acid, nonselective NSAIDs and cyclooxygenase-2 inhibitors): a decrease in the hypotensive effect of telmisartan, an increased risk of developing acute renal failure with dehydration. At the beginning of combination therapy with telmisartan and NSAIDs, it is necessary to compensate for the BCC and check renal function;
    amifostine, baclofen: potentiation of the hypotensive effect of telmisartan;
    barbiturates, alcohol, antidepressants and drugs: worsening orthostatic hypotension.

Terms and conditions of storage

Store at a temperature not exceeding 25 ° C, out of the reach of children.
Shelf life is 3 years.

Reviews

In a few reviews of Telmista, users note that the drug does a good job with its main task - it quite effectively lowers blood pressure. But there is an unwanted side effect on the functioning of the kidneys and liver.

Terms of sell

A prescription is not required to buy Telmista.