Tablets 40 mg
White or almost white oblong tablets, engraved “51H” on one side, and the company symbol on the other side.
Tablets 80 mg
White or almost white oblong tablets, engraved “52H” on one side, and the company symbol on the other side.
Pharmacotherapeutic group:angiotensin II receptor antagonist. ATX:C.09.C.A.07 Telmisartan
Pharmacodynamics:Telmisartan is a specific angiotensin II receptor antagonist (type
AT1), effective when taken orally. Has a high affinity for the subtype AT1 angiotensin II receptors, through which the action of angiotensin II is realized. Displaces angiotensinIIfrom binding to a receptor without having an agonist effect on that receptor. binds only to the AT subtype angiotensin II receptors. Communication islong lasting character. It has no affinity for other receptors, including the AT 2 receptor and other, less studied angiotensin receptors. The functional significance of these receptors, as well as the effect of their possible excessive stimulation by angiotensin II, the concentration of which increases with the administration of telmisartan, have not been studied. Reduces the concentration of aldosterone in the blood, does not inhibit renin in the blood plasma and does not block ion channels. does not inhibit angiotensin-converting enzyme (kininase II) (an enzyme that also destroys bradykinin). Therefore, the enhancement of bradykinin-induced side effects not expected.In patients, a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. Start hypotensive effect observed within 3 hours after the first dose of telmisartan. The effect of the drug lasts for 24 hours and remains significant for up to 48 hours. Expressed hypotensive effect usually develops 4-8 weeks after regular use.
In patients suffering from arterial hypertension, it reduces systolic and diastolic blood pressure (BP) without affecting heart rate (HR).
In case of abrupt withdrawal of telmisartan, blood pressure gradually returns to original level without the development of withdrawal syndrome.
Pharmacokinetics:When taken orally, it is rapidly absorbed from gastrointestinal tract. Bioavailability - 50%. When taken simultaneously with food, a decreaseAUC(area under the concentration-time curve) ranges from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). 3 hours after administration, the concentration in the blood plasma levels off, regardless of the time of meal. There is a difference in plasma concentrations between men and women. C max ( maximum concentration) AndAUCwere approximately 3 and 2 times higher, respectively, in women compared to men, without a significant effect on effectiveness.Connection with blood plasma proteins - 99.5%, in mainly with albumin and alpha-1 glycoprotein. The average apparent volume of distribution at equilibrium concentration is 500 l.
Metabolized by conjugation with glucuronic acid. Metabolites are pharmacologically inactive. The half-life (T 1/2) is more than 20 hours. It is excreted unchanged through the intestines, excretion by the kidneys is less than 2% of the dose taken. Total plasma clearancehigh (900 ml/min.) compared to the “hepatic” blood flow (about 1500 ml/min.).
Elderly patients
The pharmacokinetics of telmisartan in elderly patients does not differ from young patients. No dose adjustment is required.
Patients with kidney failure
No dose adjustment is required in patients with renal impairment, including patients on hemodialysis. cannot be removed by hemodialysis.
Patients with hepaticinsufficiency
In patients with mild to moderate liver dysfunction (Child-Pugh class A and B) daily dose the drug should not exceed 40 mg.
Use in pediatrics
The main pharmacokinetics of telmisartan in children aged 6 to 18 years, after taking telmisartan at a dose of 1 mg/kg or 2 mg/kg for 4 weeks, are generally comparable to the data obtained in the treatment of adults, and confirm the non-linearity of the pharmacokinetics of telmisartan , especially in relation to C max.
Indications:- Arterial hypertension.
- Reduced cardiovascular morbidity and mortality in patients aged 55 years and older with high risk cardiovascular diseases.
Contraindications:fetotoxicity (decreased renal function, oligohydroamnion, delayed ossification of the skull), as well as neonatal toxicity (renal failure, hypotension, hyperkalemia). Patients planning pregnancy should be prescribed alternative therapy. If treatment with angiotensin II receptor antagonists occurred during the second trimester of pregnancy, ultrasound testing of the renal function and condition of the skull in the fetus is recommended.
Neonates whose mothers received angiotensin II receptor antagonists should be closely monitored for hypotension.
Therapy with MICARDIS is contraindicated during breastfeeding.
No studies have been conducted on the effect on human fertility. Directions for use and dosage:Inside, regardless of food intake.
Arterial hypertension
The initial recommended dose of Micardis® is 1 tablet. (40 mg) once daily. In cases where therapeutic effect is not achieved, the maximum recommended dose of Micardis® 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.
Reducing cardiovascular morbidity and mortality
During the initial period of treatment, additional blood pressure correction may be required.
Renal dysfunction
In patients with renal failure, including patients on hemodialysis, no dosage adjustment is required.
Liver dysfunction
In patients with mild to moderate liver dysfunction (class A and B on the Child-Pugh scale, respectively), the daily dose of Micardis should not exceed 40 mg.
Elderly patients
The dosage regimen does not require changes.
Side effects:Observed cases of side effects
did not correlate with gender, age orrace of patients.Infections:
sepsis, including fatal sepsis
outcome, urinary tract infections(including cystitis), infections of the upper respiratory tract.From the hematopoietic andlymphatic system:
anemia, eosinophilia, thrombocytopenia.
From the central nervoussystems:
anxiety, insomnia, depression,fainting, vertigo.
From the side of the organ of vision:
visual disturbances.
Cardiovascularsystems:
bradycardia, tachycardia, severedecreased blood pressure, orthostatic hypotension.
From the respiratory system:
dyspnea.
From the digestive system:
abdominal pain, diarrhea, dry mouth,dyspepsia, flatulence, discomfort in stomach area, vomiting, liver dysfunction/liver disease* (*based on post-marketing surveillance, most cases of liver dysfunction/liver disease were identified in Japanese patients).
Allergic reactions:
anaphylactic reactions, increasedsensitivity (erythema, urticaria, angioedema), eczema, itchy skin, rash (including drug rash), angioedema (fatal), hyperhidrosis, toxic rash.
From the musculoskeletal sidedevice:
arthralgia, back pain, muscle spasms(calf muscle cramps), pain in lower extremities, myalgia, tendon pain (symptoms similar to tendonitis).
From the kidneys and urinary tract:
impaired renal function, including acute renal failure.
General:
chest pain, flu-like syndrome, general weakness, hyperkalemia, hypoglycemia (in patients with diabetes).
Laboratory indicators:decrease in hemoglobin concentration, increase in concentration uric acid, creatinine in the blood, increased activity of liver enzymes, increased concentration of creatine phosphokinase (CPK).
Overdose:No cases of overdose have been identified.
Symptoms
: marked decrease in blood pressure, tachycardia, bradycardia.Treatment : symptomatic therapy, hemodialysis is not effective.
Interaction:Telmisartan may increase the hypotensive effect of other antihypertensive agents. Other types of interactions of clinical significance have not been identified.
Combination use with digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin and amlodipine does not lead to clinically significant interactions. There was an increase in the average concentration of digoxin in the blood plasma by an average of 20% (in one case by 39%). When telmisartan and digoxin are administered simultaneously, it is advisable to periodically determine the concentration of digoxin in the blood.
With simultaneous use of telmisartan and ramipril, an increase in AU Co was observed -24 and Cmax of ramipril and ramiprilat by 2.5 times. The clinical significance of this phenomenon has not been established.
With the simultaneous administration of angiotensin-converting enzyme (ACE) inhibitors and lithium preparations, a reversible increase in the concentration of lithium in the blood was observed, accompanied by toxic effect. In rare cases, such changes have been reported with the administration of angiotensin II receptor antagonists. When prescribing lithium and angiotensin II receptor antagonists simultaneously, it is recommended to determine the concentration of lithium in the blood.
Treatment with non-steroidal anti-inflammatory drugs (NSAIDs), including acetylsalicylic acid, cyclooxygenase-2 (COX-2) inhibitors and non-selective NSAIDs, may cause the development of acute renal failure in dehydrated patients. Drugs acting on the renin-angiotensin-aldosterone system (RAAS) may have a synergistic effect. In patients receiving NSAIDs, blood volume should be compensated and renal function monitored at the beginning of treatment.
A decrease in the effect of antihypertensive drugs, such as, by inhibiting the vasodilatory effect of prostaglandins, was observed when combined with NSAIDs.
Special instructions: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 double blockade of the RAAS (for example, by adding an ACE inhibitor or direct inhibitor renin, 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 MICARDIS 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, e.g. coronary disease heart disease (CHD), the risk of fatal myocardial infarction and sudden cardiovascular death may be increased with the use of drugs that lower blood pressure, such as angiotensin II receptor antagonists (ARAs) or ACE inhibitors. In patients with diabetes mellitus, CAD may be asymptomatic and therefore may be undiagnosed. In patients with diabetes mellitus, before starting the use of MICARDIS, to identify and treatment of ischemic heart disease appropriate diagnostic studies, including a test with physical activity.
Alternatively, MIKARDIS can be used in combination with thiazide diuretics, such as thiazide diuretics, 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 MICARDIS (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 diseases biliary tract or liver failure a decrease in drug clearance 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.
Impact on the ability to drive vehicles. Wed and fur.:Special clinical trials The effect of the drug on the ability to drive a car and operate machinery was not assessed. However, when driving and operating machinery, the possibility of dizziness and drowsiness should be taken into account, which requires caution.
Release form/dosage:Tablets 40 mg and 80 mg.
Package: 7 tablets per blister made of polyamide/aluminum/PVC. 2 or 4 blisters with instructions for use in a cardboard box (for a dosage of 40 mg). 2, 4 or 8 blisters with instructions for use in a cardboard box (for a dosage of 80 mg). Storage conditions:Store at a temperature not exceeding 30 °C, in the original packaging.
Keep out of the reach of children!
Best before date: 4 years. Do not use after expiration date. Conditions for dispensing from pharmacies: By prescription Registration number: P N015387/01 Registration date: 22.10.2008 / 29.09.2014 Expiration date: Indefinite Owner of the Registration Certificate:Boehringer Ingelheim International GmbH Germany Manufacturer: Representative office: Boehringer Ingelheim, LLC Information update date: 24.04.2018 Illustrated instructionsMicardis is a drug prescribed to patients to reduce arterial hypertension.
The medicine has a persistent hypotensive effect; the dosage of the drug is selected in each case strictly individually. The main active ingredient of the drug is Telmisartan. One tablet may contain 80, 40 or 20 mg.
When taken orally, it is quickly absorbed from the intestine. Bioavailability approaches 50%. After three hours, the plasma concentration reaches its maximum. 99.5% active substance binds to blood proteins. Metabolized by reaction with glucuronic acid.
Angiotensin II receptor antagonist.
Dispensed with a doctor's prescription.
How much does Mikardis cost? The average price in pharmacies is 1,000 rubles.
The medicine is pills white, oblong in shape, with “51H” engraved on one edge and the company logo on the other edge.
Seven such tablets with a dosage of 40 mg in a blister, 2 or 4 such blisters in a cardboard box. Either 7 such tablets with a dosage of 80 mg in a blister, 2, 4 or 8 such blisters in a cardboard box
The maximum effect develops 3 hours after a single dose. The hypotensive effect lasts more than 24 hours, including the last 4 hours before taking the next dose. A stable clinical result is achieved after 4–8 weeks of course use and is maintained for a long time. If you abruptly stop taking blood pressure, it gradually (over several days) returns to initial values without the manifestation of “rebound” hypertension.
The drug is also used to reduce cardiovascular morbidity and, accordingly, mortality in people over 55 years of age with a high risk of developing diseases cardiovascular system.
As stated in the instructions for Micardis, this drug is contraindicated:
The drug is prescribed, but with extreme caution and under medical supervision to patients with:
Caution should be exercised when treating with Micardis for people in the period after kidney transplantation, as well as for patients who have a decrease in circulating blood volume as a result of previous diuretic therapy, vomiting or diarrhea, or limiting the intake of table salt.
Prohibited for use by pregnant and lactating women.
The instructions for use indicate that Micardis is prescribed orally, regardless of food intake.
Patients with renal failure (including those on hemodialysis) do not require dose adjustment.
In patients with impaired liver function, mild and medium degree(class A and B on the Child-Pugh scale), the daily dose of the drug should not exceed 40 mg.
The dosage regimen in elderly patients does not require changes.
The following side effects have been reported during therapy with Micardis:
Cases of drug overdose have not been registered.
If symptoms such as a marked decrease in blood pressure, tachycardia, bradycardia appear, a symptomatic therapy. Hemodialysis is ineffective.
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 renal artery stenosis or stenosis of the artery of a single kidney), the prescription of drugs that affect this system may be accompanied by the development of acute arterial hypotension, hyperazotemia, oliguria and, in rare cases, acute renal failure.
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 a double blockade of the RAAS (for example, by adding ACE inhibitors 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 patients with diabetes mellitus and additional cardiovascular risk, such as patients with diabetes mellitus and coronary artery disease, the risk of fatal myocardial infarction and sudden cardiac death may be increased when taking blood pressure-lowering drugs such as angiotensin II receptor antagonists or ACE inhibitors. vascular death. In patients with diabetes mellitus, CAD may be asymptomatic and therefore may be undiagnosed. Before starting to use the drug Micardis for the detection and treatment of coronary artery disease, appropriate diagnostic studies should be carried out, incl. exercise test.
Based on the experience of using other drugs that affect the RAAS, with the simultaneous administration of Micardis and potassium-sparing diuretics, potassium-containing supplements, potassium-containing table salt, and other drugs that increase the concentration of potassium in the blood (for example, heparin), this indicator should be monitored in patients.
In patients with primary aldosteronism, antihypertensive drugs whose mechanism of action is to inhibit the RAAS are usually not effective.
Alternatively, Micardis can be used in combination with thiazide diuretics, such as hydrochlorothiazide, which additionally have a hypotensive effect (for example, Micardis Plus 40 mg/12.5 mg, 80 mg/12.5 mg).
Caution must be exercised when using Micardis (as well as other vasodilators) in patients with aortic or mitral stenosis and hypertrophic obstructive cardiomyopathy.
In patients with severe arterial hypertension, a dose of telmisartan 160 mg/day in combination with hydrochlorothiazide 12.5-25 mg was effective and well tolerated.
Telmisartan is excreted mainly in bile. In patients with obstructive biliary disease or hepatic insufficiency, reduced clearance of the drug can be expected.
Liver dysfunction when prescribed telmisartan was observed in most cases in Japanese residents.
Micardis is less effective in black patients.
When using the drug, it is necessary to take into account interactions with other medications:
(Hydrochlorothiazide) :
(If factory combinations are unavailable, a similar effect will be achieved by the combined use of the drugs included in the combination in the same doses.)
Antihypertensive drug
Antihypertensive drug. It is a combination of telmisartan (angiotensin II receptor antagonist) and hydrochlorothiazide (thiazide diuretic). The simultaneous use of these components leads to a greater antihypertensive effect than the use of each of them separately. Taking MicardisPlus® 1 time leads to a significant gradual decrease in blood pressure.
Telmisartan is a specific angiotensin II receptor antagonist. It has a high affinity for the AT1 receptor subtype of angiotensin II, through which the action of angiotensin II is realized. Telmisartan displaces angiotensin II from binding to the receptor without having an agonist effect on this receptor. Telmisartan binds only to the AT1 receptor subtype of angiotensin II. The binding is long lasting. Telmisartan has no affinity for other receptors (including AT2 receptors) of angiotensin. The functional significance of these receptors, as well as the effect of their possible excessive stimulation by angiotensin II, the concentration of which increases with the administration of telmisartan, have not been studied. Telmisartan leads to a decrease in aldosterone levels in the blood. Telmisartan does not block renin in the blood and ion channels, does not block ACE, and does not inactivate bradykinin.
In patients with arterial hypertension, telmisartan reduces systolic and diastolic blood pressure without affecting heart rate.
Telmisartan at a dose of 80 mg completely blocks the hypertensive effect of angiotensin II. Its effect lasts more than 24 hours, including the last 4 hours before taking the next dose. The onset of the hypotensive effect is observed within 3 hours after the first dose of telmisartan. In case of abrupt withdrawal of telmisartan, blood pressure gradually returns to its original level without the development of withdrawal syndrome.
Hydrochlorothiazide is a thiazide diuretic. Thiazide diuretics affect the reabsorption of electrolytes in the renal tubules, directly increasing the excretion of sodium and chloride (in approximately equivalent amounts). The diuretic effect of hydrochlorothiazide leads to a decrease in blood volume, an increase in plasma renin activity, an increase in the secretion of aldosterone and is accompanied by an increase in the content of potassium and bicarbonates in the urine, as well as hypokalemia. With simultaneous administration of telmisartan, there is a tendency to stop the loss of potassium caused by these diuretics, presumably due to blockade of the RAAS.
Long-term use of hydrochlorothiazide reduces the risk of complications of cardiovascular diseases and mortality from them.
After taking hydrochlorothiazide, diuresis increases after 2 hours, and the maximum effect is observed after approximately 4 hours. The diuretic effect of the drug lasts for approximately 6-12 hours.
The maximum antihypertensive effect of MicardisPlus® is usually achieved 4 weeks after the start of treatment.
The combined use of hydrochlorothiazide and telmisartan does not affect the pharmacokinetics of each of the components of the drug.
Telmisartan
Suction
When taken orally, the Cmax of telmisartan is achieved within 0.5-1.5 hours after administration. The absolute bioavailability of telmisartan in doses from 40 to 160 mg was 42% and 58%, respectively. When taken simultaneously with food, the bioavailability of telmisartan is slightly reduced with a decrease in the AUC value by 6% at a dose of 40 mg and about 19% at a dose of 160 mg. 3 hours after oral administration, the concentration in the blood plasma levels off, regardless of whether the drug was taken with food or on an empty stomach. The pharmacokinetics of telmisartan when administered orally is nonlinear at doses of 20-160 mg, with a more than proportional increase in plasma concentrations (Cmax and AUC) with increasing doses.
Distribution
Binding to plasma proteins is significant (more than 99.5%), mainly to albumin and α1-glycoprotein. Vd for telmisartan is approximately 500 l.
Penetrates the placental barrier and is detected in the umbilical cord blood.
Metabolism
Telmisartan is metabolized by conjugation with glucuronic acid. The metabolite (acyl glucuronide) is pharmacologically inactive. Glucuronide is the main metabolite that is detected only in humans.
Removal
Most of the administered dose (more than 97%) is excreted in bile and then in feces. Telmisartan is excreted in the urine in small quantities. The total plasma clearance is more than 1500 ml/min. T1/2 is more than 20 hours.
In women, the plasma concentration of telmisartan is 2-3 times higher than in men. However, an increase in the hypotensive effect is not observed in women.
The pharmacokinetic parameters of telmisartan do not differ significantly between young and elderly patients.
Renal excretion does not affect the clearance of telmisartan. Based on the level of excretion in patients with mild to moderate renal impairment (creatinine clearance 30 to 60 ml/min), no dosage adjustment is required. Telmisartan is not removed by dialysis.
Pharmacokinetic studies in patients with liver failure showed an increase in absolute bioavailability to almost 100%. In liver failure, T1/2 does not change.
Hydrochlorothiazide
Suction
After oral administration of MicardisPlus® Cmax of hydrochlorothiazide is achieved within 1-3 hours. Absolute bioavailability is assessed by the cumulative renal excretion of hydrochlorothiazide and is about 60%.
Distribution
Binds to plasma proteins by 64%. Vd - 0.8±0.3 l/kg.
Metabolism and excretion
It is not metabolized in the human body and is excreted in urine almost unchanged. About 60% of the dose taken orally is eliminated within 48 hours. Renal clearance is about 250 - 300 ml/min. T1/2 - 10-15 hours.
Pharmacokinetics in special clinical situations
In women there is a tendency to increase plasma concentrations of hydrochlorothiazide. However, an increase in the hypotensive effect is not observed in women.
In patients with impaired renal function, the rate of elimination of hydrochlorothiazide is reduced. T1/2 of hydrochlorothiazide with CC 90 ml/min increases and is about 34 hours.
MicardisPlus® should be taken orally once a day, regardless of meals.
MicardisPlus® 40/12.5 mg can be prescribed to patients in whom the use of Micardis® at a dose of 40 mg or hydrochlorothiazide does not lead to adequate blood pressure control.
MicardisPlus® 80/12.5 mg can be prescribed to patients in whom the use of Micardis® at a dose of 80 mg or MicardisPlus® 40/12.5 mg does not lead to adequate blood pressure control.
In patients with mild or moderate liver dysfunction, MicardisPlus® should not be used in a daily dose of more than 40/12.5 mg.
No changes to the dosage regimen are required in elderly patients.
1) - side effects expected based on experience with telmisartan.
2) - side effects expected based on experience with hydrochlorothiazide.
From the respiratory system: upper respiratory tract infections (including bronchitis, pharyngitis, sinusitis), shortness of breath1), dyspnea, respiratory distress syndrome (including pneumonia and pulmonary edema)2).
From the cardiovascular system: bradycardia1), tachycardia1), arrhythmias2), marked decrease in blood pressure1), orthostatic hypotension2), necrotizing angiitis (vasculitis)2), chest pain1).
From the side of the central nervous system: excitability, fear, depression1)2), anxiety2), dizziness, fainting1), insomnia1), staggering when walking2), paresthesia2).
From the digestive system: abdominal pain, diarrhea, dyspepsia, gastritis, anorexia2), loss of appetite2), sialadenitis2), dry mouth1), flatulence1), vomiting1), constipation2), pancreatitis2), impaired liver function1), jaundice (hepatocellular or cholestatic)2).
From the endocrine system: loss of control of hypoglycemia during diabetes mellitus.
Metabolic disorders: hypercholesterolemia, hyperuricemia, hypokalemia, hyperkalemia, hyponatremia2), decrease in blood volume2), disturbance of electrolyte metabolism2), hyperglycemia2), hypercalcemia1).
From the hematopoietic system: eosinophilia1), anemia (including aplastic anemia2), hemolytic anemia2), inhibition of bone marrow hematopoiesis2), leukopenia2), neutropenia/agranulocytosis2), thrombocytopenia1)2).
From the urinary system: urinary system infections, interstitial nephritis2), impaired renal function2), acute renal failure1), glycosuria2).
From the musculoskeletal system: arthralgia, arthrosis, back pain, pain in the legs, myalgia, convulsive twitching of the calf muscles (cramps)1), symptoms similar to tendinitis1), weakness1)2), muscle spasm2).
Allergic reactions: anaphylactic reactions2), eczema, erythema1), itching1), cutaneous lupus-like reactions2), cutaneous vasculitis2), photosensitivity reactions2), rash2), reactivation of cutaneous lupus erythematosus2), toxic epidermal necrolysis2), angioedema, urticaria and other similar reactions (as is the case with the use of other angiotensin II antagonists).
From the senses: impaired visual acuity1), transient blurred vision2), xanthopsia2), vertigo.
From the reproductive system: decreased potency.
Laboratory indicators: decrease in hemoglobin1), increase in uric acid1), creatinine1), liver enzymes1), blood CPK1), triglycerides2).
Other: flu-like symptoms, fever2), increased sweating1).
The use of thiazide diuretics may impair glucose tolerance.
The drug should be prescribed with caution in case of impaired liver function or progressive liver diseases; bilateral renal artery stenosis or stenosis of the artery of a single kidney; renal dysfunction; condition after kidney transplantation; a decrease in blood volume due to previous diuretic therapy, restriction of salt intake, diarrhea or vomiting; for chronic heart failure; stenosis of the aortic and mitral valve; obstructive hypertrophic cardiomyopathy; diabetes mellitus; IHD; systemic lupus erythematosus; gout
Telmisartan does not have a teratogenic effect, but has a fetotoxic effect. Therefore, MicardisPlus® should not be used in the first trimester of pregnancy. In case of planned pregnancy, MicardisPlus® should be replaced with drugs approved for use during pregnancy. If pregnancy is established, you should immediately stop taking the drug.
In the second and third trimesters, the use of the drug can cause electrolyte disturbances in the fetus, as well as possibly other disturbances that are known in adults. The development of neonatal thrombocytopenia and jaundice (in the fetus or newborn) has been reported when the mother took thiazide diuretics (including hydrochlorothiazide). Therefore, the drug is contraindicated in the second and third trimesters of pregnancy.
While it is not known whether telmisartan passes into breast milk, hydrochlorothiazide passes into breast milk and may inhibit lactation. Therefore, MicardisPlus® is contraindicated for use during lactation.
Contraindicated in cases of severe liver dysfunction. The drug should be prescribed with caution in cases of impaired liver function or progressive liver diseases. In patients with mild or moderate liver dysfunction, MicardisPlus® should not be used in a daily dose of more than 40/12.5 mg.
Contraindicated in cases of severe renal impairment (creatinine clearance less than 30 ml/min). The drug should be prescribed with caution in case of bilateral renal artery stenosis or stenosis of the artery of a single kidney, impaired renal function, or the condition after kidney transplantation.
For mild or moderate renal impairment, no dose changes are required. In such patients, renal function should be monitored.
In patients with impaired liver function or progressive liver disease, MicardisPlus® should be used with caution, since even slight changes in water and electrolyte balance may contribute to the development of hepatic coma.
In patients with bilateral renal artery stenosis or arterial stenosis of a single functioning kidney, the risk of severe arterial hypotension and renal failure increases when using telmisartan.
There is no experience with the use of MikardisPlus® in patients with severely impaired renal function or in patients after kidney transplantation. Since there is little experience with the use of MicardisPlus® in patients with mild to moderate renal impairment, in such cases it is recommended to periodically determine the levels of potassium and creatinine in the blood serum. The use of hydrochlorothiazide in patients with impaired renal function may lead to azotemia. Periodic monitoring of renal function is recommended.
In patients with reduced blood volume and/or hyponatremia resulting from massive 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 MicardisPlus®, correction of these disorders is necessary.
In cases where vascular tone and renal function are largely dependent on the activity of the RAAS (for example, in patients with severe chronic heart failure or concomitant kidney diseases, including renal artery stenosis), the use of drugs that 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.
In patients with primary aldosteronism, antihypertensive drugs whose mechanism of action is to inhibit the activity of the RAAS are usually ineffective. In such cases, the use of MicardisPlus® is not recommended.
In patients with aortic or mitral stenosis or obstructive hypertrophic cardiomyopathy, the use of MicardisPlus® (as well as other vasodilators) requires special caution.
In patients with diabetes mellitus, changes in the dosage of insulin or oral hypoglycemic agents may be required. During therapy with hydrochlorothiazide, a latent form of diabetes mellitus may manifest.
In some cases, when using hydrochlorothiazide, hyperuricemia and gout may develop.
When using MicardisPlus®, periodic determination of the level of electrolytes in the blood serum is necessary.
Thiazide diuretics, incl. hydrochlorothiazide can cause electrolyte imbalance and acid-correcting reactions (hypokalemia, hyponatremia and hypochloremic alkalosis). Symptoms of these disorders are dry mouth, thirst, general weakness, lethargy, drowsiness, anxiety, myalgia or convulsive twitching of the calf muscles, muscle weakness, hypotension, oliguria, tachycardia, nausea or vomiting.
When using hydrochlorothiazide, hypokalemia may develop, but concomitantly used telmisartan can reduce this disorder. The risk of hypokalemia is greatest in patients with liver cirrhosis, with increased diuresis, with inadequate oral replacement of electrolytes, and in the case of simultaneous use of corticosteroids or ACTH. Telmisartan, which is part of MicardisPlus®, on the contrary, can lead to hyperkalemia due to antagonism of angiotensin II receptors. Although clinically significant hyperkalemia has not been reported with the use of MicardisPlus®, it should be taken into account that risk factors for its development include renal and/or heart failure and diabetes mellitus.
There is no evidence that MicardisPlus® can reduce or prevent diuretic-induced hyponatremia. Chloride deficiency is usually minor and does not require treatment.
Hydrochlorothiazide may reduce calcium excretion and cause (in the absence of known metabolic disorders of this ion) a transient and small increase in serum calcium levels. More significant hypercalcemia may be a sign of hidden hyperparathyroidism. Before determining parathyroid function, thiazide diuretics should be discontinued.
Hydrochlorothiazide has been shown to increase urinary excretion of magnesium, which may lead to hypomagnesemia.
In patients with ischemic cardiopathy or coronary artery disease, any antihypertensive drug, if the blood pressure is reduced excessively, can lead to myocardial infarction or stroke.
Hypersensitivity reactions to hydrochlorothiazide may occur, especially in patients with a history of allergies or bronchial asthma.
MicardisPlus® can, if necessary, be used in conjunction with another antihypertensive drug.
When used together with MicardisPlus® potassium-containing diuretics, laxatives, corticosteroids, ACTH, amphotericin, carbenoxolone, penicillin G (sodium salt), salicylic acid and its derivatives, regular monitoring of potassium levels in the blood plasma is recommended.
When using MicardisPlus® together with potassium-sparing diuretics, potassium preparations, other drugs that can increase the potassium level in the blood serum (for example, sodium heparin), or when replacing table salt with potassium salts, regular monitoring of the level of potassium in the blood plasma is recommended.
If you need to use calcium supplements, you should regularly monitor the concentration of calcium in the blood and, if necessary, change the dose of these drugs.
The effectiveness and safety of MicardisPlus® in children and adolescents under 18 years of age have not been established.
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 a car and working with machinery, you should be aware of the possibility of developing dizziness and drowsiness when using the drug MicardisPlus®.
Symptoms of telmisartan overdose: marked decrease in blood pressure, tachycardia and/or bradycardia.
An overdose of hydrochlorothiazide is accompanied by loss of electrolytes (hypokalemia, hypochloremia) and dehydration resulting from massive diuresis. The most common signs and symptoms of hydrochlorothiazide overdose are nausea and drowsiness. Hypokalemia may lead to muscle spasms and/or worsen cardiac arrhythmias caused by concomitant use of cardiac glycosides or certain antiarrhythmic drugs.
Treatment: symptomatic and supportive therapy, the nature of which depends on the time elapsed since taking the drug and the severity of the symptoms. It is recommended to induce vomiting and/or perform gastric lavage and prescribe activated charcoal. Frequent monitoring of electrolytes and serum creatinine is necessary. If arterial hypotension develops, the patient should be placed on his back and quickly undergo therapy aimed at replacing electrolytes and blood volume. Telmisartan is not removed by hemodialysis. The extent to which hydrochlorothiazide is removed during hemodialysis has not been established.
With the simultaneous use of lithium and angiotensin II receptor antagonists (including telmisartan), in rare cases, an increase in the concentration of lithium in the blood serum and increased toxic effects were observed. In addition, the use of thiazide diuretics reduces the clearance of lithium. Therefore, the simultaneous use of lithium preparations and MicardisPlus® is allowed only under the condition of careful medical supervision; Monitoring serum lithium levels is recommended.
The hypokalemic effect of hydrochlorothiazide is compensated by the potassium-sparing effect of telmisartan. However, the hypokalemic effect of hydrochlorothiazide may be enhanced by other drugs that lead to potassium excretion and hypokalemia (for example, other diuretics, laxatives, corticosteroids, ACTH, amphotericin, carbenoxolone, penicillin G (sodium salt), salicylic acid and its derivatives).
The simultaneous use of potassium-sparing diuretics, potassium preparations, other drugs that can increase the potassium content in the blood serum (for example, sodium heparin), or the replacement of table salt with potassium salts, can, on the contrary, lead to hyperkalemia.
In cases where MicardisPlus® is used in conjunction with drugs whose effect changes with a decrease in potassium levels in the blood (for example, cardiac glycosides, antiarrhythmic drugs and drugs that can cause cardiac arrhythmias such as "pirouette"), periodic monitoring of plasma potassium levels is recommended blood.
Telmisartan may enhance the hypotensive effect of other antihypertensive drugs.
Drugs such as digoxin, warfarin, hydrochlorothiazide, glibenclamide, ibuprofen, paracetamol, simvastatin and amlodipine have been studied in pharmacokinetic studies. Since an increase in median basal digoxin concentrations of 20% was detected (in one case the increase in concentration reached 39%), it should be taken into account that monitoring of digoxin plasma concentrations may be required.
When hydrochlorothiazide is used concomitantly with ethanol, barbiturates or opioid analgesics, the risk of developing orthostatic hypotension increases; with metformin - the risk of developing lactic acidosis.
With the simultaneous use of hydrochlorothiazide with cholestyramine and colestipol, the absorption of hydrochlorothiazide is impaired.
With the simultaneous use of hydrochlorothiazide with cardiac glycosides, the risk of developing digitalis arrhythmias increases due to hypokalemia or hypomagnesemia caused by hydrochlorothiazide.
With the simultaneous use of hydrochlorothiazide with NSAIDs (including acetylsalicylic acid in a dose of > 0.3 g / day and COX-2 inhibitors), its diuretic, natriuretic and antihypertensive effect is reduced in some patients. Acute renal failure may develop in patients with dehydration. Patients receiving combined therapy with MicardisPlus® and NSAIDs should compensate for dehydration and monitor renal function at the beginning of treatment.
When used simultaneously with hydrochlorothiazide, the effect of pressor amines (for example, norepinephrine) may be weakened.
Hydrochlorothiazide may enhance the effect of non-depolarizing muscle relaxants (including tubocurarine).
Because hydrochlorothiazide may increase serum uric acid levels, changes in the dosage regimen of uricosuric drugs may be necessary. The use of thiazide diuretics may increase the incidence of hypersensitivity reactions to allopurinol.
Hydrochlorothiazide may increase serum calcium levels due to decreased calcium excretion.
Hydrochlorothiazide may potentiate the hyperglycemia caused by beta-blockers and diazoxide. Anticholinergic drugs (for example, atropine, biperidine) can, by reducing gastric and intestinal motility, increase the bioavailability of hydrochlorothiazide.
The drug may increase the risk unwanted effects induced by amantadine, reduce the renal excretion of cytotoxic drugs (for example, cyclophosphamide, methotrexate) and enhance their myelosuppressive effect.
The drug is available with a prescription.
List B. The drug should be stored in a place protected from moisture, out of the reach of children, at a temperature not exceeding 25°C. Shelf life - 3 years.
Photo of the drug
Latin name: Micardis
ATX code: C09CA07
Active ingredient: Telmisartan
Manufacturer: Boehringer Ingelheim Pharma (Germany)
Description is valid on: 27.10.17
Micardis is a medicine used in the treatment of high blood pressure.
Telmisartan.
Available in the form of white or almost white, oblong tablets, of two types. Some have the engraving "51H" on one side and the company symbol on the other side. Other tablets are engraved with "51H" on one side and the company symbol on the other side.
Prescribed for arterial and essential hypertension, as well as to prevent cardiovascular pathologies.
Effective in reducing cardiovascular morbidity and mortality in patients aged 55 years and older with a high risk of cardiovascular disease.
Should be used with caution when:
The tablets are taken orally, regardless of meals.
Application may cause the following side effects:
Cases of drug overdose have not been registered.
When symptoms such as a marked decrease in blood pressure, tachycardia, bradycardia appear, symptomatic therapy is required. Hemodialysis is ineffective.
Analogs by ATX code: Praytor, Teseo, Telzal, Telmisartan-SZ, Telmista.
Do not decide to change the drug on your own; consult your doctor.
Micardis is an antihypertensive drug. The active substance is telmisartan, a specific angiotensin II receptor antagonist. It has a high affinity for the AT 1 receptor subtype of angiotensin II, through which the action of angiotensin II is realized.
Contraindicated during pregnancy and breastfeeding.
Contraindicated in children and adolescence up to 18 years old.
The dosage regimen in elderly patients does not require changes.
Micardis is prescribed to patients to eliminate signs of hypertension. The drug has a persistent hypotensive property, the dosage for each patient is selected individually. Before taking the drug, it is recommended to read the instructions for it, study contraindications, as well as side effects.
The active substance, which is the main component of the drug, is telmisartan. One tablet can contain from 20 to 80 milligrams. Additional components, helping to most quickly absorb the active microelement are:
The first dose of Micardis leads to a gradual normalization of blood pressure. It decreases slowly over several hours. The hypotensive effect is observed a day after taking the drug. This means that to maintain normal blood pressure you need to take one Micardis tablet per day. The greatest decrease in blood pressure can be noticed a month after starting to take the drug. If you abruptly stop taking Micardis, there is no “withdrawal” effect; the initial values return within 2-3 weeks.
All substances included in the drug are absorbed quite quickly from the intestine when taken orally, the maximum concentration active substance reaches almost 50%.
"Micardis" is available in the form of white tablets. The package can contain from two to eight blisters, each containing 7 tablets.
In rare cases, the medicine is prescribed to patients over 55 years of age who are at risk of developing severe heart disease associated with high blood pressure.
In addition to the regular Micardis, the drug Micardis Plus is produced. The latter contains 12.5 milligrams hydrochlorothiazide, which has diuretic properties.
The combination of a diuretic drug with an angiotensin antagonist helps achieve maximum effect. Diuretic effects begin to appear two hours after taking the drug. Micardis Plus is prescribed if it is not possible to achieve a decrease in blood pressure when taking regular Micardis.
Important!
Under no circumstances should you prescribe the drug and dosage yourself, since only the attending doctor must find out all the contraindications and analyze the patient’s tests.
"Mikardis 40" has the same contraindications as drugs with other amounts of active substance. The medicine should not be taken in the following cases:
The instructions for use of Micardis indicate that the drug is not prescribed to patients with:
Preparation "Mikardis" is prescribed with extreme caution for:
Important!
The drug should be taken with extreme caution in case of diabetes mellitus and gout (a disease of the joints and tissues caused by metabolic disorders in the body).
Reviews about "Mikardis" are not always positive. Some patients report feeling unwell, which directly depends on the dosage of the drug, age and the presence of diseases. The most common side effects are:
Clinical studies have proven fetotoxic influence of the drug. Therefore, Micardis should not be taken in all trimesters of pregnancy and lactation. If a woman plans to become a mother, then doctors advise her to switch to more safe drugs. If pregnancy occurs, stop taking the medication.
The drug is prescribed only by a doctor and can be used either alone or with other medications that are aimed at improving the functioning of the cardiovascular system. Russian analogues of Micardis also have the same spectrum of action.
The instructions for use indicate that daily use of the drug should be limited to one 40 milligram tablet. It must be remembered that in patients with mild forms of hypertension, a decrease in blood pressure also occurs when taking a tablet with 20 milligrams of the active substance. The therapeutic dosage is selected over a period of up to four weeks. Actually, that’s how much time is needed for Mikardis to demonstrate all its positive influence on the patient's body.
If during the month of taking Micardis 20 there is no desired result, then the doctor prescribes a drug with a dosage of 80 milligrams, which also must be taken one tablet per day.
In case of severe disease, the doctor may prescribe Micardis in a dosage of 160 milligrams, that is, you will need to take 2 tablets per day, 80 milligrams each.
In rare situations, a sick person is unable to lower blood pressure with a single drug, then such a patient is prescribed Micardis Plus, thanks to which the pressure decreases quickly. In this case, the dosage of the drug is selected based on the development hypertension. Reviews of Mikardis and analogues prove its positive effect in lowering blood pressure.
Important!
Patients with a medical history of impaired renal function do not require an individual dosage. If the information contains records of a moderate pathological abnormality of the liver, then the sick person must take Micardis 40. Do not increase the dose of the drug: this can lead to disturbances in the functioning of the kidneys and liver. For elderly patients, the dosage is not adjusted.
In patients with diabetes mellitus, as well as coronary heart disease or other cardiovascular diseases, the use of the drug Micardis increases the risk of fatal myocardial infarction and sudden death.
Coronary heart disease in diabetes mellitus may occur without symptoms and may not be initially detected. Therefore, before starting therapy with Micardis, you need to pass all necessary tests and undergo diagnostics.
Before a doctor prescribes Micardis to a patient, he must find out what other medications the patient is taking. When taking the following medications, their effect or the effect of Micardis may be enhanced:
The instructions for use indicate that special research on how the active substance (t elmisartan), which is part of the drug and most analogues, affects concentration and the ability to drive a car, have not been carried out. But! It must be remembered that medications containing diuretic components can cause drowsiness and dizziness.
Preparation "Micardis" must be stored in a place that is difficult for children to reach, at a temperature of no more than 30 degrees. Shelf life:
The drug is released strictly according to prescription. "Mikardis" is prohibited for children under 18 years of age.
The price of the medicine depends on the dosage of the active substance. The cost of Mikardis 40 (14 tablets) is from 500 rubles and above. "Mikardis 80" - from 900 to 1000 rubles. The price for Micardis Plus (28 tablets) is from 850 rubles and above.
The instructions for use say that the drug can be taken at any time of the day; eating does not affect the body’s ability to absorb the drug. Total duration Treatment depends on the doctor; after assessing the patient’s health, the doctor may recommend switching to a dose of 20 milligrams. People who take the medication note rapid decline blood pressure and no side effects. But most patients from buying this drug The high price stops it.
Cheaper analogues of Micardis Plus are selected by the doctor; the most well-known medications with a similar effect include:
The price of analogues of the drug "Micardis" depends on the country of manufacture and the composition of the drug. You can buy the following analogues at a reduced cost:
