Telmist® (Telmista®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceTelmisartanTelmisartan
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    • Dosage form: & nbsppills
    Composition:

    For 1 tablet of 20 mg / 40 mg / 80 mg:

    Active substance: telmisartan 20.00 mg / 40.00 mg / 80.00 mg

    Excipients: meglumine, sodium hydroxide, povidone-KZO, lactose monohydrate, sorbitol (E420), magnesium stearate.

    Description:

    Tablets of 20 mg:

    Round tablets are white or almost white in color.

    Tablets 40 mg:

    Oval, biconvex tablets are white or almost white in color.

    Tablets 80 mg:

    Capsule-shaped, biconvex tablets of white or almost white color.
    Pharmacotherapeutic group:Angiotensin II receptor antagonist
    ATX: & nbsp

    C.09.C.A.07   Telmisartan

    Pharmacodynamics:

    Telmisartan is a specific angiotensin II receptor antagonist (ARA II) (type AT1), effective at ingestion. Has a high affinity for the subtype AT1 receptors of angiotensin II, through which the action of angiotensin II is realized.It displaces angiotensin II from the bond to the receptor, not having the action of an agonist for this receptor. Telmisartan binds only to the subtype AT1 receptors of angiotensin II. Communication is of a lasting nature. Has no affinity for other receptors, including AT2 receptors and other, less studied receptors of angiotensin. The functional significance of these receptors, as well as the effect of their possible excessive stimulation with angiotensin II, whose concentration increases with telmisartan, have not been studied. Reduces the concentration of aldosterone in the blood plasma, does not inhibit renin in the blood plasma and ns blocks ion channels. Telmisartan does not inhibit angiotensin-converting enzyme (ACE) (kininase II) (an enzyme that also breaks down bradykinin). Therefore, the enhancement of bradykinin-induced side effects is not expected.

    Patients telmisartan in a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. The onset of antihypertensive action is noted within 3 hours after the first administration of telmisartan. The drug remains for 24 hours and remains significant up to 48 hours.The pronounced antihypertensive effect usually develops after 4-8 weeks of regular intake of telmisartan.

    In patients with hypertension telmisartan reduces systolic and diastolic blood pressure (BP), without affecting the heart rate (heart rate).

    In the case of a sharp cancellation of telmisartan, blood pressure gradually returns to the initial level without the development of the "withdrawal" syndrome.

    Pharmacokinetics:

    When ingested quickly absorbed from the gastrointestinal tract (GIT). Bioavailability - 50%. Decrease AUC (the area under the concentration-time curve) with simultaneous use of telmisartan with food intake ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). After 3 hours after taking the concentration in the blood plasma levels, regardless of the time of eating. There is a difference in plasma concentrations in men and women. The maximum concentration (CmOh) in the blood plasma and AUC women compared with men were about 3 and 2 times higher, respectively (without a significant effect on effectiveness).

    Communication with plasma proteins is 99.5%, mainly with albumin and alpha-1 glycoprotein.

    The average value of the apparent volume of distribution in the equilibrium concentration is 500 liters. Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive. The half-life (T1/2) - more than 20 hours. It is excreted mainly through the intestine in an unchanged form and kidneys - less than 2% of the dose taken. The total plasma clearance is high (900 ml / min) but compared with the "hepatic" blood flow (about 1500 ml / min).

    Elderly patients

    The pharmacokinetics of telmisartan in elderly patients does not differ from pharmacokinetics in patients of young age. Dose correction is not required.

    Patients with renal insufficiency

    A dose change in patients with renal insufficiency is not required, including patients on hemodialysis.

    Telmisartan is not removed by hemodialysis.

    Patients with hepatic insufficiency

    In patients with mild and moderate impairment of liver function (class A and B according to the Child-Pugh classification), the daily dose of the drug should not exceed 40 mg.

    Pediatric Use

    The main indicators of the pharmacokinetics of telmisartan in children aged 6 to 18 years after receiving telmisartan in a dose of 1 mg / kg or 2 mg / kg for 4 weeks, in general, are comparable with the data,obtained in the treatment of adult patients, and confirm the non-linearity of the pharmacokinetics of telmisartan, especially with respect to CmOh.

    Indications:

    - Arterial hypertension.

    - Reduction of cardiovascular morbidity and mortality in patients aged 55 years and older with a high risk of cardiovascular disease.

    Contraindications:

    - Hypersensitivity to the active substance or excipients of the drug.

    - Pregnancy.

    - Breastfeeding period.

    - Obstructive diseases of the biliary tract.

    - Severe liver dysfunction (Child-Pugh class C).

    - Simultaneous use with aliskiren in patients with diabetes mellitus or moderate and severe renal failure (glomerular filtration rate (GFR) <60 ml / min / 1.73 m2).

    - Intolerance to fructose or lactose, deficiency of lactase or sucrose / isomaltase, glucose-galactose malabsorption syndrome.

    - Age to 18 years (effectiveness and safety not established).

    Carefully:

    - Two-sided stenosis of the renal arteries or stenosis of the artery of a single kidney.

    - Violations of the liver and / or kidney function (see section "Special instructions").

    - Reduction of circulating blood volume (BCC) due to previous diuretic therapy, restriction of salt intake, diarrhea or vomiting.

    - Hyponatremia.

    - Hyperkalemia.

    - Conditions after kidney transplantation (no experience of application).

    - Chronic heart failure (CHF).

    - Stenosis of the aortic and / or mitral valve.

    - Hypertrophic obstructive cardiomyopathy (GOKMP).

    - Primary hyperaldosteronism (efficacy and safety not established).

    Pregnancy and lactation:

    The use of Telmist® is contraindicated in pregnancy. The use of ARA II in the first trimester of pregnancy is not recommended, these drugs should not be used during pregnancy. When diagnosing pregnancy, taking Telmist® should be stopped immediately. If necessary, alternative hypotensive therapy should be prescribed (other classes of antihypertensive drugs permitted for use in pregnancy).

    The use of ARA II in the second-third trimesters of pregnancy is contraindicated.

    Pre-clinical studies of telmisartan did not reveal teratogenic effects, but fetotoxicity was established.It is known that the use of APA II in the second and third trimesters of pregnancy causes a person to have fetotoxicity (decreased kidney function, oligohydramnion, slowing ossification of the fetal bones), and neonatal toxicity (renal failure, arterial hypotension, hyperkalemia). Patients planning pregnancy should use alternative therapy. If nevertheless used APA II in the second-third trimesters of pregnancy, it is necessary to perform ultrasound examination of the kidneys and bones of the fetal skull.

    Newborns, whose mothers took ARA II during pregnancy, should be monitored, since the development of arterial hypotension in a newborn is possible.

    There is no information on the release of telmisartan into breast milk. Therapy with Telmist® is contraindicated during breastfeeding.

    Studies to study the effect on human fertility have not been conducted.

    Dosing and Administration:

    Inside, regardless of the time of ingestion.

    Arterial hypertension

    The initial recommended dose of Telmist® is 1 tablet (40 mg) once a day.In cases where the therapeutic effect is not achieved, the maximum The recommended dose of Telmist® can be increased to 80 mg once daily. When deciding whether to increase the dose, it should be taken into account that the maximum antihypertensive effect is usually achieved within 4-8 weeks after the start of treatment.

    Reduction of cardiovascular morbidity and mortality

    The recommended dose is 1 tablet of Telmyst® 80 mg once a day.

    In the initial period of treatment, an additional correction of blood pressure may be required.

    Impaired renal function

    In patients with renal insufficiency, including patients on hemodialysis, correction of the dosing regimen is not required.

    Impaired liver function

    In patients with mild or moderate impairment of liver function (Class A and B but Child-Pugh classification, respectively), the daily dose of Telmist® should not exceed 40 mg. Use in patients with severe impairment of liver function (class C according to the Child-Pugh classification), see "Contraindications".

    Elderly patients

    The dosage regimen does not require correction.

    Side effects:

    The observed side effects were not correlated with the sex, age or race of the patients.

    Infectious and parasitic diseases: sepsis, including fatal sepsis, urinary tract infections (including cystitis), upper respiratory tract infections.

    Violations from the blood and lymphatic system: anemia, eosinophilia, thrombocytopenia.

    Immune system disorders: anaphylactic reactions, hypersensitivity (erythema, urticaria, angioedema), eczema, skin itching, skin rash (including medicinal), angioedema (fatal), hyperhidrosis, toxic skin rash.

    Impaired nervous system: anxiety, insomnia, depression, fainting, vertigo.

    Disorders from the side of the organ of vision: visual disorders.

    Heart Disease: bradycardia, tachycardia.

    Vascular disorders: marked decrease in blood pressure, orthostatic hypotension.

    Disturbances from the respiratory system, chest and mediastinal organs: dyspnea, cough, interstitial lung disease * (* in postmarketing period of use, cases have been described interstitial lung disease, with the presence of a temporary connection with the administration of telmisartan. However, a causal relationship with telmisartan was not established).

    Disorders from the digestive system: abdominal pain, diarrhea, dryness of the oral mucosa, dyspepsia, flatulence, discomfort in the stomach, vomiting, taste distortion (dysgeusia), violations of liver function / liver disease * (* Based on the results postmarketing observations in most cases of liver dysfunction / liver disease have been identified in Japan).

    Disturbances from the musculoskeletal and connective tissue: arthralgia, back pain, muscle spasms (calf muscle cramps), pain in the lower extremities, myalgia, pain in the tendons (symptoms similar to tendonitis).

    Disorders from the kidneys and urinary tract: impaired kidney function, including acute renal failure.

    General disorders and disorders at the site of administration: pain in the chest, flu-like syndrome, general weakness.

    Laboratory and instrumental data: reduction of hemoglobin, increased concentration of uric acid, creatinine in blood plasma, increased activity of "liver" enzymes, creatine phosphokinase (CK) in blood plasma, hyperkalemia, hypoglycemia patients with diabetes mellitus).

    Overdose:

    Cases of overdose have not been identified.

    Symptoms: marked decrease in blood pressure, tachycardia, bradycardia.

    Treatment: symptomatic therapy, hemodialysis is ineffective.

    Interaction:

    Telmisartan may increase the antihypertensive effect of other antihypertensive agents. Other types of interactions that have clinical relevance have not been identified.

    Simultaneous use with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin and amlodipine does not result in a clinically significant interaction. An increase in the average concentration of digoxin in the blood plasma was observed on average by 20% (in one case - by 39%). With the simultaneous use of telmisartan and digoxin, it is advisable to periodically determine the concentration of digoxin in the blood plasma.

    Like other drugs acting on the renin-angiotensin-aldosterone system (RAAS), the use of telmisartan can cause hyperkalemia (see section "Special instructions").The risk may increase in the case of simultaneous use with other drugs, which can also provoke development hyperkalemia (potassium-containing salt substitutes, potassium-sparing diuretics, ACE inhibitors, ARA II, non-steroidal anti-inflammatory drugs [NSAIDs], including selective inhibitors cyclooxygenase-2 | COG-2 |, heparin, immunosuppressants [cyclosporin or tacrolimus] and trimethoprim.

    The development of hyperkalemia depends on the attendant risk factors. Risk increases also in the case of simultaneous application the above combinations. In particular, the risk is particularly high with simultaneous application from potassium-sparing diuretics, and also with potassium-containing salt substitutes. For example, simultaneous application with ACE inhibitors or NSAIDs is a lower risk if strictly followed by precautions. ARA II, such as telmisartan, reduce the loss of potassium on the background of therapy with diuretics. Application of potassium-sparing diuretics, for example, spironolactone, eplerenone, triamterene or amiloride, potassium-containing additives or potassium-containing salt substitutes can lead to a significant increase in potassium content in the serum. Simultaneous use with documented hypokalemia should be used with caution and with regular monitoring of potassium levels in the blood plasma. With the simultaneous use of telmisartan and ramipril, there was an increase in AUC0-24 and CmOh ramipril and ramiprilata 2.5 times. The clinical significance of this phenomenon is not established. With the simultaneous use of ACE inhibitors and lithium preparations, a reversible increase in the lithium content in the blood plasma was observed, accompanied by a toxic effect. In rare cases, such changes were recorded with the use of ARA II and lithium preparations. With simultaneous use of lithium and ARA II preparations, it is recommended to determine the content of lithium in blood plasma. Treatment of NSAIDs, including acetylsalicylic acid, COX-2 and nonselective NSAIDs, can cause development of acute renal failure in dehydrated patients. Drugs acting on RAAS, may have a synergistic effect. In patients receiving NSAIDs and telmisartan, at the beginning of treatment should be compensated for BCC and kidney function monitoring performed. Simultaneous use with aliskiren in patients with diabetes mellitus or moderate and severe renal failure (glomerular filtration rate [GFR] <60 ml / min / 1.73 m2) is contraindicated. Reduction of the effect of antihypertensive drugs, such as telmisartan, by inhibiting vasodilator the effect of prostaglandins was noted with simultaneous application with NSAIDs. Given the pharmacological properties of such drugs as baclofen, amifostine, it is possible to potentiate the antihypertensive effect of all antihypertensive drugs, including telmisartan. Besides Togo, Orthostatic hypotension may be aggravated by simultaneous use of alcohol, barbiturates, narcotic drugs or antidepressants.
    Special instructions:

    In some patients, due to the suppression of RAAS, especially when using a combination of agents acting on this system, renal function (including acute renal failure) is impaired. Therefore, therapy accompanied by a similar double blockade of RAAS (eg, with the addition of ACE inhibitors, or a direct inhibitor of renin, aliskiren to therapy ARA II), should be carried out strictly individually and with regular monitoring of kidney function (including periodic control the content of potassium and the concentration of creatinine in the blood plasma). Simultaneous use of ACE inhibitors, ARA II or aliskiren increases the risk of arterial hypotension, hyperkalemia and reduces kidney function (including the development of acute kidney failure). Therefore, the double blockade of RAAS with simultaneous use of ACE inhibitors, APA II or aliskiren is not recommended (see subsection "Pharmacodynamics").

    If a double blockade is considered absolutely necessary, it should be carried out under the supervision of a doctor, as well as regular monitoring of kidney function, the content of electrolytes in blood plasma and blood pressure.

    Patients with diabetic nephropathy should not simultaneously use ACE inhibitors and ARA II.

    In cases of vascular tone and kidney function, mainly from RAAS activity (for example, in patients with CHF or kidney disease, including bilateral renal artery stenosis or arterial stenosis of a single kidney), the use of drugs that affect this system may be accompanied by the development of acute arterial hypotension, hyperaemia, oliguria, and, in rare cases, acute renal failure.Based on the experience of using other agents that affect RAAS, while using Telmist® and potassium-sparing diuretics, potassium supplements, potassium-containing substitutes salt, other agents that increase the level of potassium in the blood plasma (for example, heparin), this indicator should be monitored in patients.

    In patients with diabetes mellitus and an additional cardiovascular risk, for example, in patients with diabetes mellitus and ischemic heart disease (IHD) in the case of hypotensive drugs such as ARA II or ACE inhibitors may increase the risk of fatal myocardial infarction and sudden cardiovascular death. In patients with diabetes mellitus, IHD can be asymptomatic, and therefore may not be diagnosed. In patients with diabetes mellitus, before starting the use of Telmist®, appropriate diagnostic tests should be performed to identify and treat coronary artery disease, including a physical exercise test.

    Alternatively, Telmist® can be used in combination with thiazide diuretics, such as hydrochlorothiazide, which additionally provide antihypertensive effect.

    In patients with primary hyperaldosteronism, antihypertensive drugs, whose mechanism of action is inhibition of RAAS, are usually not effective. Caution should be exercised when using Telmist® (as well as other vasodilators) in patients with aortic and / or mitral stenosis, or with GOKMP.

    Patients with diabetes mellitus, receiving insulin or hypoglycemic agents for oral administration

    Have These patients may develop hypoglycemia against telmisartan therapy. Therefore, it is necessary to carry out appropriate monitoring of blood glucose concentration, in the presence of indications, it may be necessary to adjust the dose of insulin or hypoglycemic agents.

    Primary hyperaldosteronism

    Have patients with primary hyperaldosteronism, as a rule, there is no positive response to therapy with antihypertensive agents acting by suppressing RAAS. The use of Telmist® is not recommended in this group of patients.

    Telmisartan is excreted mainly with bile.In patients with obstructive biliary tract disease or liver failure, a decrease in clearance of the drug can be expected.

    In patients with severe arterial hypertension hypertension dlight telmisartan - 160 mg / day and in combination with hydrochlorothiazide - 12.5-25 mg / day was well tolerated and effective. Dysfunction of the liver with telmisartan in most of the cases were observed in the inhabitants of Japan. The Telmyst® preparation is less effective in patients of the Negroid race.

    Effect on the ability to drive transp. cf. and fur:Special clinical studies of the influence of telmisartan on the ability to control the car and mechanisms were not carried out. However, when driving vehicles and working with machinery, one should take into account the possibility of developing dizziness and drowsiness, which requires caution.
    Form release / dosage:

    Tablets, 20 mg, 40 mg, 80 mg.

    Packaging:

    For 7 or 10 tablets in a blister of the combined material OPA / Al / PVC - aluminum foil.

    For 2, 4, 8, 12 or 14 blisters (a blister of 7 tablets) or 3, 6 or 9 blisters (a blister of 10 tablets) will be pinched into a cardboard box together with instructions for use.

    Storage conditions:

    At a temperature of no higher than 25 ° C in the original packaging.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use the drug after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003269
    Date of registration:26.10.2015
    Expiration Date:26.10.2020
    The owner of the registration certificate:KRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
    Manufacturer: & nbsp
    KRKA, d.d. Slovenia
    Representation: & nbspKRKA, dd, Novo mesto, AOKRKA, dd, Novo mesto, AO
    Information update date: & nbsp27.02.2017
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