Pharmacodynamics and pharmacokinetics
Pharmacodynamics
Telmisartan is a selective angiotensin II . It has a high affinity for AT1 angiotensin II receptors . Competes with angiotensin II at specific receptors, without having the same effect. The binding is long lasting.
Does not have tropism for other receptor subtypes. Reduces the content of aldosterone in the blood, does not suppress renin in plasma and ion channels in cells.
The onset of the hypotensive effect is observed within the first three hours after taking telmisartan . The effect lasts for a day or more. A pronounced effect develops a month after continuous use.
In persons with arterial hypertension , telmisartan reduces systolic and diastolic pressure, but does not change the number of heart contractions.
Does not cause withdrawal syndrome.
Pharmacokinetics
When taken orally, it is quickly absorbed from the intestine. Bioavailability approaches 50%. After three hours, the plasma concentration reaches its maximum. 99.5% of the active substance binds to blood proteins. Metabolized by reaction with glucuronic acid . Metabolites of the drug are inactive. The half-life is more than 20 hours. Excreted through the digestive tract, excretion in urine is less than 2%.
Pharmacokinetics
When taken orally, it is quickly absorbed from the gastrointestinal tract. Bioavailability - 50%. When taken concomitantly with food, the reduction in AUC ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). 3 hours after administration, the plasma concentration levels off regardless of taking the drug on an empty stomach or with food. Cmax and AUC are 3 and 2 times higher, respectively, in women compared to men, without a significant effect on concentration. Plasma protein binding is 99.5%, mainly with albumin and alpha1 glycoprotein. The average value of the apparent volume of distribution at the equilibrium stage is 500 l. Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive. T1/2 - more than 20 hours. Total plasma Cl is high (900 ml/min) compared to hepatic blood flow (about 1500 ml/min). Excreted through the intestines unchanged, excretion by the kidneys is less than 2%.
Side effects
- From the central nervous system: depression , dizziness, headache , fatigue, anxiety, insomnia , convulsions .
- From the respiratory system: diseases of the upper respiratory tract ( sinusitis , pharyngitis , bronchitis ), cough.
- From the circulatory system: marked decrease in pressure , tachycardia , bradycardia , chest pain.
- From the digestive system: nausea, diarrhea , dyspepsia , increased concentration of liver enzymes.
- From the musculoskeletal system: myalgia , lower back pain, arthralgia .
- From the genitourinary system: edema, infections of the genitourinary system, hypercreatininemia .
- Hypersensitivity reactions: skin rash, angioedema , urticaria .
- Laboratory indicators: anemia , hyperkalemia .
- Other: erythema , itching, dyspnea .
Mikardis, instructions for use
According to the instructions for use of Micardis, the drug is taken orally. For adults, the recommended dose is 40 mg once daily. In a number of patients, a therapeutic effect is observed even with a dose of 20 mg per day. If a decrease in pressure to the desired level is not observed, then the dose can be increased to 80 mg per day.
The maximum effect of the drug is achieved five weeks after the start of therapy.
In patients with severe forms of arterial hypertension, 160 mg of the drug per day can be used
Instructions for use MICARDIS
In patients with bilateral renal artery stenosis or renal artery stenosis of a single functioning kidney, the use of Micardis increases the risk of severe arterial hypotension and renal failure. Therefore, caution should be exercised in prescribing the drug to this category of patients.
There is no experience with the use of Micardis in patients after kidney transplantation. Since there is little experience with the use of Micardis in patients with mild to moderate renal impairment, in such cases periodic determination of serum potassium and creatinine levels is recommended.
In patients with reduced blood volume and/or hyponatremia resulting from diuretic therapy, restriction of salt intake, diarrhea or vomiting, clinically significant arterial hypotension may develop, especially after taking the first dose of the drug. Before starting to use Micardis, correction of these disorders is necessary.
In cases where vascular tone and renal function are largely dependent on the activity of the renin-angiotensin-aldosterone system (for example, in patients with severe chronic heart failure or concomitant kidney diseases, including renal artery stenosis), the use of drugs which affect the state of this system may be accompanied by the development of acute arterial hypotension, hyperazotemia, oliguria or, in rare cases, acute renal failure. Therefore, caution should be exercised in prescribing the drug to this category of patients.
In patients with primary aldosteronism, antihypertensive drugs whose mechanism of action is to inhibit the activity of the renin-angiotensin-aldosterone system are usually ineffective. In such cases, the use of Micardis is not recommended.
In patients with aortic or mitral stenosis or idiopathic hypertrophic subaortic stenosis, the use of Micardis (as well as other vasodilators) requires special caution.
It should be taken into account that when using antihypertensive drugs in patients with ischemic cardiopathy or coronary artery disease, in the event of an excessive decrease in blood pressure, myocardial infarction or stroke may develop.
It should be borne in mind that when using Micardis, especially in the presence of kidney disease and/or heart failure, as well as simultaneously with potassium-sparing diuretics, salt substitutes containing potassium, and other drugs that increase the concentration of potassium in the blood (heparin), the risk of developing hyperkalemia increases. Therefore, in these cases it is recommended to monitor the level of potassium in the blood.
Micardis should be prescribed with caution to patients with impaired liver function. Telmisartan is excreted mainly in bile. Therefore, in patients with biliary obstruction or severe liver failure, the clearance of the drug may be reduced. Therefore, Micardis should not be used in this category of patients. For mild or moderate liver dysfunction, the drug is used with caution.
The recommended daily dose of Micardis 40 mg or 80 mg contains 169 mg or 338 mg of sorbitol, respectively. Therefore, the drug should not be prescribed to patients with hereditary fructose intolerance.
Micardis is less effective in lowering blood pressure in blacks. This may be due to the higher prevalence of conditions with a decrease in renin levels in arterial hypertension in patients of the Black race.
Use in pediatrics
The drug is not indicated for use in children and adolescents, because There are no data on efficacy and safety in this category of patients.
Impact on the ability to drive vehicles and operate machinery
A special study of the effect of the drug on the ability to drive a car and operate machinery has not been conducted. However, when driving and operating machinery, you should be aware of the possibility of dizziness and drowsiness when using Micardis.
Interaction
Telmisartan activates the hypotensive effect of other blood pressure lowering drugs.
When telmisartan and digoxin , it is necessary to periodically determine the concentration of digoxin in the blood, as it may increase.
When taking lithium and ACE inhibitors lithium content in the blood may occur , which manifests itself as a toxic effect.
Treatment with non-steroidal anti-inflammatory drugs together with Micardis in dehydrated patients may lead to the development of acute renal failure.
Micardis®
In some patients, due to suppression of the RAAS, especially when using a combination of drugs acting on this system, renal function is impaired (including acute renal failure). Therefore, therapy accompanied by such dual blockade of the RAAS (for example, when adding an ACE inhibitor or a direct renin inhibitor, aliskiren to angiotensin II receptor antagonist blockers) should be carried out strictly individually and with careful monitoring of renal function (including periodic monitoring of serum potassium and creatinine concentrations ).
In cases where vascular tone and renal function depend primarily on the activity of the RAAS (for example, in patients with chronic heart failure or kidney disease, including bilateral renal artery stenosis, or stenosis of the artery of a single kidney), prescribing drugs that affect this system , may be accompanied by the development of acute arterial hypotension, hyperazotemia, oliguria, and, in rare cases, acute renal failure.
Based on the experience of using other drugs that affect the RAAS, when concomitantly prescribing MIKARDIS® and potassium-sparing diuretics, potassium-containing supplements, potassium-containing table salt, and other drugs that increase potassium levels in the blood (for example, heparin), this indicator should be monitored in patients.
In patients with diabetes mellitus and additional cardiovascular risk, for example, in patients with diabetes mellitus and coronary artery disease (CAD), when using drugs that lower blood pressure, such as angiotensin II receptor antagonists (ARAs) or ACE inhibitors, may increase the risk of fatal myocardial infarction and sudden cardiovascular death.
In patients with diabetes mellitus, CAD may be asymptomatic and therefore may be undiagnosed. In patients with diabetes mellitus, before starting the use of MIKARDIS®, appropriate diagnostic tests, including exercise testing, should be carried out to identify and treat coronary heart disease.
Alternatively, MIKARDIS® can be used in combination with thiazide diuretics, such as hydrochlorothiazide, which additionally have a hypotensive effect (for example, MIKARDIS-PLUS 40 mg/12.5 mg, 80 mg/12.5 mg).
In patients with primary aldosteronism, antihypertensive drugs whose mechanism of action is to inhibit the renin-angiotensin-aldosterone system are usually not effective.
Caution should be exercised when using MIKARDIS® (as well as other vasodilators) in patients with aortic or mitral stenosis, or hypertrophic obstructive cardiomyopathy.
Telmisartan is excreted mainly in bile. In patients with obstructive biliary disease or hepatic insufficiency, reduced clearance of the drug can be expected.
In patients with severe arterial hypertension, a dose of telmisartan 160 mg/day and in combination with hydrochlorothiazide 12.5-25 mg was well tolerated and effective.
Liver dysfunction when prescribed telmisartan was observed in most cases in Japanese residents.
MICARDIS® is less effective in black patients.
special instructions
For dehydrated patients (restriction of salt intake, treatment with diuretics , diarrhea , vomiting), a reduction in the dose of Micardis is necessary.
Prescribe with caution to persons with stenosis of both renal arteries , stenosis of the mitral valve or aorta, obstructive hypertrophic cardiomyopathy , severe renal, hepatic or heart failure, diseases of the digestive tract.
It is prohibited to use in case of primary aldosteronism and fructose intolerance .
If you are planning a pregnancy, you must find in advance a replacement for Micardis with another antihypertensive drug .
Use with caution when driving vehicles.
When taken simultaneously with lithium , monitoring of lithium levels in the blood is indicated, as a temporary increase in its level is possible.
Directions for use and doses
Inside, regardless of food intake. Adults - 40 mg 1 time per day. In some patients, a therapeutic effect can be achieved using a dose of 20 mg/day. If there is no reduction in blood pressure to the desired level, the dose can be increased to 80 mg 1 time per day. The maximum effectiveness of the antihypertensive effect of the drug is usually observed 4–8 weeks after the start of treatment.
For patients with severe arterial hypertension - up to 160 mg/day or in combination with hydrochlorothiazide 12.5–25 mg/day.
Micardis analogs
Level 4 ATC code matches:
Telmisartan
Irbesartan
Presartan
Nortivan
Candesartan
Kozaar
Aprovel
Teveten
Blocktran
Cardosal
Valsartan
Losartan
Atakand
Diovan
Valsacor
Vazar
Valz
Lorista
Lorista
Lozap
The most accessible analogues of Mikardis are: Praytor , Telmista , Hipotel .
Mikardis price
In Russia, a package of the drug 80 mg No. 28 will cost from 830 to 980 rubles. In Ukraine, the price of Mikardis in the same release form is close to 411 hryvnia.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
- Online pharmacies in KazakhstanKazakhstan
ZdravCity
- Mikardis tablets 40 mg 28 pcs. NOT DEFINED
RUB 1,175 order - Mikardis Plus tablets 80mg+12.5mg 28pcs Boehringer Ingelheim
RUB 1,176 order
- Micardis tablets 80 mg 28 pcs. Boehringer Ingelheim Ellas AE
RUB 1,147 order
Pharmacy Dialogue
- Mikardis plus tablets 80mg/12.5mg No. 28Boehringer Ingelheim
1102 rub. order
- Mikardis tablets 40 mg No. 28 Boehringer Ingelheim
1101 rub. order
- Micardis tablets 80 mg No. 28 Boehringer Ingelheim
1100 rub. order
- Mikardis plus (tab. 80 mg/12.5 mg No. 28)Boehringer Ingelheim
1112 rub. order
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Pharmacy24
- Mikardis plus 80 mg N28 tablets Boehringer Ingelheim Pharma GmbH & Co. KG/Boehringer Ingelheim Ellas A.E., Nimechina/Greece
807 UAH.order - Mikardis 80 mg N28 tablets Boehringer Ingelheim Pharma GmbH & Co. KG/Boehringer Ingelheim Ellas A.E., Nimecchina/Greece
749 UAH. order
PaniPharmacy
- Micardis tablets Micardis tablets. 80 mg No. 28 Germany, Boehringer Ingelheim Pharma
812 UAH order
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