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medicalmeds.eu Medicines Angiotensin II of receptors blocker. Микардис®

Микардис®

Препарат Микардис®. Boehringer Ingelheim Pharma  (Берингер Ингельхайм Фарма) Германия


Producer: Boehringer Ingelheim Pharma (Beringer Ingelkhaym Pharma) Germany

Code of automatic telephone exchange: C09CA07

Release form: Firm dosage forms. Tablets.

Indications to use: Arterial hypertension.


General characteristics. Structure:

Active ingredient: 20 mg, 40 mg or 80 mg of a telmisartan.

Excipients: povidone, меглумин, sodium hydroxide, sorbitol, magnesium stearate.

Anti-hypertensive drug.




Pharmacological properties:

Pharmacodynamics.  Telmisartan is the specific antagonist of receptors of angiotensin II (AT1 type), effective at intake. Has high affinity to the AT1 subtype of receptors of angiotensin II through which effect of angiotensin II is implemented. Forces out angiotensin I from communication with a receptor, without possessing action of an agonist concerning this receptor.

Telmisartan contacts only the AT1 subtype of receptors of angiotensin II. Communication has long character. Has no affinity to other receptors, including to AT2 to a receptor and another, less studied angiotensin receptors. Functional value of these receptors, and also effect of their possible excess stimulation by angiotensin II which concentration increases at purpose of a telmisartan, are not studied. Reduces concentration of Aldosteronum in blood, does not inhibit a renin in a blood plasma and does not block ion channels. Telmisartan does not inhibit an angiotensin-converting enzyme (a kininaz of II) (enzyme which is also destroyed by bradikinin). Therefore strengthening of the side effects caused by bradikinin is not expected.

At patients телмисартан in a dose of 80 mg completely blocks hypertensive effect of angiotensin II. The beginning of hypotensive action is noted within 3 hours after the first reception of a telmisartan. Effect of drug remains within 24 hours and remains significant till 48 o'clock. The expressed hypotensive effect usually develops in 4-8 weeks after regular reception.

At the patients having arterial hypertension телмисартан reduces the systolic and diastolic arterial pressure (AP), without exerting impacts on the heart rate (HR).

In case of sharp cancellation of a telmisartan of the ABP gradually is returned to initial level without development of a syndrome of "cancellation".

Pharmacokinetics. At intake it is quickly soaked up from digestive tract. Bioavailability - 50%. At reception along with food decrease in AUC (the area under a curve "concentration time") fluctuates from 6% (at a dose of 40 mg) to 19% (at a dose of 160 mg). 3 hours later after reception concentration in a blood plasma is leveled, irrespective of meal. The difference in plasma concentration at men and women is observed. Cmax (the maximum concentration) and AUC were approximately in 3 and 2 times, respectively, is higher at women in comparison with men without significant influence on efficiency.

Communication with proteins of a blood plasma - 99,5%, generally with albumine and alfa-1 a glycoprotein. Average value of visible volume of distribution in equilibrium concentration - 500 l. It is metabolized by a konjyugirovaniye with glucuronic acid. Metabolites pharmacological are inactive. An elimination half-life (Т½) - more 20th hour. Removal by kidneys - less than 2% is removed through intestines in an invariable look. The general plasma clearance high (900 ml/min.) in comparison with a "hepatic" blood-groove (about 1500 ml/min.).

Elderly patients. The pharmacokinetics of a telmisartan at patients of advanced age does not differ from young patients. Correction of doses is not required.
Patients with a renal failure
 Change of a dose with a renal failure is not required from patients, including the patients who are on a hemodialysis.
Telmisartan does not leave by means of a hemodialysis.
Patients with a liver failure
 At patients with easy and moderate abnormal liver functions (a class A and B on a scale of Chayld-Pyyu) the daily dose of drug should not exceed 40 mg.
At children
 The main indicators of pharmacokinetics of a telmisartan at children aged from 6 up to 18 years, in general, are comparable to the data obtained at treatment of adults and confirm nonlinearity of pharmacokinetics of a telmisartan, especially concerning Cmax.


Indications to use:

Arterial hypertension.
• Decrease in cardiovascular incidence and mortality at patients at the age of 55 years is also more senior with high risk of cardiovascular diseases.


Route of administration and doses:

Inside, regardless of meal.

Arterial hypertension. The initial recommended dose of the drug Mikardis® makes 1 таб. (40 mg) once a day. In cases when the therapeutic effect is not reached, the maximum recommended dose of the drug Mikardis® can be increased to 80 mg once a day. At the solution of a question of increase in a dose it is necessary to take into account that the maximum anti-hypertensive effect is usually reached within 4-8 weeks after an initiation of treatment.

Decrease in cardiovascular incidence and mortality. The recommended dose - 1 tablet of the drug Микардис® 80 of mg, 1 times a day. During an initial stage of treatment additional correction of the ABP can be required.

Renal failure. With a renal failure, including at the patients who are on a hemodialysis, correction of the mode of dosing is not required from patients.

Abnormal liver function. At patients with easy and moderate abnormal liver functions (a class A and B on a scale of Chayld-Pyyu, respectively) the daily dose of the drug Mikardis® should not exceed 40 mg.

Elderly patients. The mode of dosing does not demand changes.


Features of use:

At some patients, owing to suppression of RAAS, especially when using a combination of the means operating on this system function of kidneys is broken (including an acute renal failure). Therefore the therapy which is followed by similar double blockade of RAAS has to be carried out strictly individually and at careful control of function of kidneys (including periodic monitoring of potassium concentration and creatinine in serum).

In cases of dependence of a vascular tone and function of kidneys preferential from activity of RAAS (for example, at patients with chronic heart failure, or diseases of kidneys, including, at a stenosis of renal arteries, or a stenosis of an artery of the only kidney), purpose of the drugs influencing this system can be followed by development of acute arterial hypotension, a hyperazotemia, oliguria, and, in rare instances, an acute renal failure.

Based on experience of use of other means influencing RAAS at joint purpose of the drug Mikardis® and kaliysberegayushchy diuretics, kaliysoderzhashchy additives, kaliysoderzhashchy edible salt, other means increasing potassium concentration in blood (for example, heparin), it is necessary to control this indicator at patients.

As an alternative the drug Mikardis® can be used in a combination with thiazide diuretics, such as a hydrochlorothiazide which in addition render hypotensive effect (for example, the mg drug МикардисПлюс® 40 / 12,5 in mg, 80 mg/) 2,5 mg).

Patients with heavy degree of arterial hypertension have a dose of a telmisartan of 160 mg/days and in a combination with Hydrochlorthiazidum of 12,5-25 mg was well transferable and effective. Микардис® is less effective at patients of negroid race.

Influence on ability to drive the car and to work with mechanisms. Special clinical trials of influence of drug on ability to drive the car and mechanisms it was not carried out. However during the driving and work with mechanisms it is necessary to take a possibility of development of dizziness and drowsiness into account that demands respect for care.


Side effects:

Observed cases of side effects did not correlate with a sex, age or race of patients.

Infections: sepsis, including sepsis with a lethal outcome, infections of urinary tract (including cystitis), upper respiratory tract infections.

From circulatory and lymphatic system: anemia, eosinophilia, thrombocytopenia.

From the central nervous system: uneasiness, sleeplessness, depression, faint.

From organs of sight and hearing: visual frustration, dizziness.

From cardiovascular system: bradycardia, tachycardia, the expressed decrease in the ABP, orthostatic hypotension.

From respiratory system: asthma.

From the alimentary system: an abdominal pain, diarrhea, dryness in a mouth, dyspepsia, a meteorism, discomfort in a stomach, vomiting, an abnormal liver function.

Allergic reactions: anaphylactic reactions, hypersensitivity to active agent or auxiliary components of drug, a Quincke's disease (from the death), eczema, an erythema, a skin itch, rash (including, medicinal), a hyperhidrosis, urticaria, toxic rash.

From a musculoskeletal system: arthralgia, dorsodynia, spasms of muscles (spasm of gastrocnemius muscles), lower extremity pain, mialgiya, sinew pain (symptoms similar to manifestation of a tendinitis).

From kidneys and urinary tract: a renal failure, including an acute renal failure.

The general: thorax pain, a grippopodobny syndrome, an adynamy (weakness), a hyperpotassemia, a hypoglycemia (at patients with a diabetes mellitus).

Laboratory indicators: decrease in concentration of hemoglobin, increase in concentration of uric acid, creatinine in blood, increase in activity of "hepatic" enzymes, increase in concentration of a kreatinfosfokinaza (KFK).


Interaction with other medicines:

Telmisartan can increase hypotensive effect of other anti-hypertensive means. Other types of interactions having the clinical importance are not revealed. The combined use with digoxin, warfarin, a hydrochlorothiazide, Glibenclamidum, an ibuprofen, paracetamol, simvastatiny and amlodipiny does not lead to clinically significant interaction. Increase in average concentration of digoxin in a blood plasma on average for 20% is noted (in one case for 39%). At co-administration of a telmisartan and digoxin reasonablly periodic definition of concentration of digoxin in blood.

At simultaneous use of a telmisartan and ramipril increase in AUC0-24 and Cmax of a ramipril and ramiprilat by 2,5 times was observed. The clinical importance of this phenomenon is not established.

At co-administration of inhibitors of an angiotensin-converting enzyme (APF) and drugs of lithium the reversible increase in concentration of lithium in blood which is followed by toxic action was noted. In rare instances similar changes are registered at purpose of angiotensin II of receptors of antagonists. At co-administration of drugs of lithium and angiotensin II of receptors of antagonists it is recommended to carry out definition of concentration of lithium to blood.

Treatment by non-steroidal anti-inflammatory drugs (NPVP), including acetylsalicylic acid, inhibitors of cyclooxygenase-2 (TsOG-2) and non-selective NPVP, can cause development of an acute renal failure in the dehydrated patients. The drugs operating on the renin-angiotensin-aldosteronovuyu system (RAAS) can have synergy effect. At the patients receiving NPVP and телмисартан in an initiation of treatment OTsK has to be compensated and control of function of kidneys is carried out.

Decrease in effect of anti-hypertensive means, such as телмисартан, by means of inhibition of vasodilating effect of prostaglandins it was noted at joint treatment with NPVP.


Contraindications:

• Hypersensitivity to active agent or auxiliary components of drug
• Pregnancy
• Feeding period breast
• Obstructive diseases of biliary tract
• The expressed abnormal liver functions (a class C on a scale of Chayld-Pyyu)
• Hereditary intolerance of fructose (contains sorbitol)
• Age up to 18 years (efficiency and safety are not established)

With care:

• Bilateral stenosis of renal arteries or stenosis of an artery of the only kidney,
• Abnormal liver functions and/or kidneys (see also Special instructions),
• Decrease in the volume of the circulating blood (VCB) owing to the previous diuretic therapy, restriction of reception of table salt, diarrhea or vomiting
Hyponatremia,
Hyperpotassemia,
• States after transplantation of a kidney (experience of use is absent),
Chronic heart failure,
• Stenosis of the aortal and mitral valve,
Idiopathic hypertrophic subaortal stenosis,
• Primary aldosteronism (efficiency and safety are not established)


Overdose:

Overdose cases at people are not revealed. Symptoms: the expressed lowering of arterial pressure.

Treatment: in case of development of the expressed lowering of arterial pressure it is necessary to carry out symptomatic therapy. The hemodialysis is not effective.


Storage conditions:

List B. To store at a temperature not above 30 °C in the place protected from moisture. To store in the place, unavailable to children! Period of validity 4 years. Not to apply after expiry date.


Issue conditions:

According to the recipe


Packaging:

Mg tablets 20, 40 and 80. On 7 tablets in the blister from polyamide/aluminium/PVC. On 2, 4, 8 or 14 blisters together with the application instruction in a cardboard box.



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