Micardis
Micardis (Telmisartan)Pharmacological action
The antagonist of receptors of angiotensin II. Micardis (Telmisartan) - the specific antagonist of receptors of angiotensin II. Possesses high affinity to a subtype of AT1-receptors of angiotensin II through which action of angiotensin II is realised. Micardis (Telmisartan) supersedes angiotensin II of communication with a receptor, not possessing action of an agonist concerning this receptor. Micardis (Telmisartan) forms communication only with a subtype of AT1-receptors of angiotensin II. Linkage has long character. Micardis (Telmisartan) does not possess affinity to other receptors (including to AT2-receptors) angiotensin. Functional value of these receptors, and also effect of their possible superfluous stimulation by the angiotensin II which concentration is enlarged at Micardis (Telmisartan) appointment, are not studied. Micardis (Telmisartan) leads to depression of level of Aldosteronum in blood. Micardis (Telmisartan) does not block a renin in bloods and ionic channels, the bradikinin does not inactivate (it allows to avoid the side-effects bound to a bradikinin).
At patients with an arterial hypertensia Micardis (Telmisartan) reduces a systolic and diastolic BP, not rendering influence on the CARDIAC CONTRACTIONS RATE.
Micardis (Telmisartan) in a dose of 80 mg completely block hypertensive effect of angiotensin II. Its action proceeds more than 24 h (including the last 4 h before reception next a dose) and remains through 48 h.
The beginning of hypotensive action becomes perceptible during 3 h after the first Micardis (Telmisartan) reception. The maximum depression of a BP is observed in 4 weeks after the treatment beginning.
In case of sharp Micardis (Telmisartan) cancellation the BP gradually comes back to initial level without withdrawal development.
Micardis (Telmisartan) influence on an indicator of cardiovascular diseases and a mortality is not established.
Indications
- An arterial hypertensia.
Dosage regimen
Prescribe the adult inside in a dose of 1 times/days of 40 mg At some patients hypotensive effect will reach at preparation appointment in a dose of 20 mg/days If necessary a preparation dose it can be possible to enlarge about 80 mg/days Thus it is necessary to consider, that the maximum hypotensive effect develops in 4-8 weeks.
At patients with serious arterial hypertensia Micardis is applied in a daily dose of 160 mg (in the form of monotherapy).
With disturbances of function of kidneys and the patient of advanced age of correction of a dose it is not required to patients.
For patients with easy and moderate disturbances of function of a liver the daily dose makes 40 mg.
Preparation prescribe irrespective of food intake.
Side effect
From party TSNS: a headache, giddiness, fatigability, a sleeplessness, uneasiness, depression, cramps.
From the alimentary system: abdominal pains, a dyspepsia, a nausea, a diarrhoeia, rising of activity of hepatic transaminases.
From respiratory system: tussis, infections of the top departments of respiratory tracts (including a pharyngitis, a bronchitis, a sinusitis).
From cardiovascular system: the expressed depression of a BP, a bradycardia, a tachycardia, a stethalgia.
From hemopoiesis system: seldom - an anaemia, an eosinophilia, a thrombocytopenia.
From osteomuscular system: a back pain, an arthralgia, the symptoms similar to a tendinitis.
Allergic reactions: a dermal eruption, an urticaria, a Quincke's disease; seldom - an erythema, an itch.
The other: seldom - a hyperpotassemia.
Contraindications
- Serious disturbances of function of a liver;
- Serious disturbances of function of kidneys;
- Hereditary intolerance of fructose;
- Pregnancy;
- A lactemia (thoracal feeding);
- A hypersensibility to Micardis and to other components of a preparation.
The preparation is not shown to application for children and teenagers since data about efficiency and safety at this category of patients are absent.
Pregnancy and lactemia
Micardis is contraindicative to application at pregnancy.
At planned pregnancy it is necessary to replace in advance Micardis with other antihypertensive preparation. At an establishment of pregnancy Micardis application should be stopped as soon as possible. Preparation application in II and III trimesters of pregnancy can cause disturbance of development and destruction of a foetus.
Micardis application during thoracal feeding since it is not known is contraindicative, whether the preparation with thoracal milk is allocated.
Special indicatings
At patients with a bilateral stenosis of renal arteries or a renal artery stenosis of a unique functioning kidney Micardis application enlarges risk of development of a serious arterial hypotension and renal insufficiency. Therefore it is necessary to prescribe a preparation of the given category of patients with care.
Experience of Micardis application after kidney transplantation is not available for patients. As experience of Micardis application at patients with small and moderate disturbances of function of kidneys is insignificant, in such cases periodic definition of levels of a potassium, a creatinine in blood serum is recommended
When the tonus of vessels and function of kidneys substantially depend on activity of system a renin-angiotensin-Aldosteronum (for example, at patients with the expressed chronic heart failure or accompanying diseases of kidneys, including a renal artery stenosis), application of preparations which influence a condition of this system, can be accompanied by development of an acute arterial hypotension, a hyperazotemia, an oliguria or, in rare instances, acute renal insufficiency. Therefore it is necessary to prescribe a preparation of the given category of patients with care.
At patients with a primary aldosteronism the antihypertensive preparations, which mechanism of action the renin-angiotensin-Aldosteronum consists in inhibition of activity of system, are usually noneffective. In such cases Micardis appointment is not recommended.
With an aortal either mitral stenosis or an idiopathic hypertrophic subaortal stenosis Micardis application demands extra care from patients.
It is necessary to consider, that at application of antihypertensive preparations for patients with an ischemic cardiopathy or the ischemic heart disease in case of excessive depression of a BP can develop a myocardial infarction or a stroke.
It is necessary to consider, that at Micardis application, especially in the presence of diseases of kidneys and-or a heart failure, and also simultaneously with the substitutes of salt containing a potassium, and other preparations enlarging concentration of a potassium in blood (heparin), the risk of development of a hyperpotassemia is enlarged. Therefore in the given cases it is recommended to supervise potassium level in blood.
With care it is necessary to prescribe Micardis to patients with disturbances of function of a liver. Micardis is deduced basically with bile. Therefore at patients with disturbances of function of a liver retardation of deducing of a preparation is possible.
Recommended daily Micardis dose of 40 mg or 80 mg contains 169 mg. Therefore the preparation is contraindicative to patients with hereditary intolerance of fructose.
Influence on ability to driving of motor transport and to management of mechanisms
Special research of influence of a preparation on ability to a driving and work with mechanisms it was not spent. However at a driving and work with mechanisms it is necessary to remember possibility of development of giddiness and drowsiness at application of Micardis preparation.
Overdosage
Overdosage cases are not taped.
Symptoms: the expressed depression of a BP.
Treatment. At an arterial hypotension prescribe symptomatic therapy. Micardisit is not deduced by a hemodialysis.
Medicinal interaction
At simultaneous Micardis application can strengthen hypotensive action of other antihypertensive preparations.
Conditions and periods of storage
B.Preparat's list should be stored in protected from a moisture, a place inaccessible to children at temperature not above 30 C. The Period of validity - 4 years.
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