Reducing the load on the heart leads to a decrease in myocardial oxygen demand. Secondly, under the action of the drug, due to expansion of the coronary arteries increasing the oxygen supply to the myocardium (especially with vasospastic angina). Amlodipine does not adversely affect the metabolism of lipids and blood plasma, has antiatherosclerotic, antithrombotic proviron steroid activity, increases the glomerular filtration rate, has a weak natriuretic effect. In diabetic nephropathy does not increase the severity of microalbuminuria. The pharmacokinetics of atenolol: after ingestion of the drug is rapidly absorbed from the gastrointestinal tract – approximately 50% of the dose ingested. Poor solubility in fats, bioavailability – 40-50%, time to reach maximum concentration in plasma after ingestion – 2.4 hours. Poorly penetrates the blood-brain barrier, held in neznachitelnbyh amounts through the placenta and breast milk. Contact with blood plasma proteins -. 6-16% Practically not metabolized in the liver. The half-life of 6-9 hours (increases in elderly patients). Excreted by the kidneys by glomerular filtration (85-100% unchanged). Renal dysfunction is accompanied by elongation of the T & frac; and cumulation with creatinine clearance less than 35 mg / min / 1.73 m 2 , the T & frac; is 16-27 hours, with clearance of less than 15 mg / min – over 27 hours (necessary to decrease the dose ). Output during hemodialysis. Amlodipine: after ingestion of amlodipine is rapidly absorbed from the gastrointestinal tract of 90%, the maximum concentration of drug in the blood observed after 6-12 hours. The equilibrium concentration of drug in blood plasma achieved after 7-8 days of its continuous use. The drug has a high volume of distribution – about 20 l / kg; bioavailability is 60-65%, the connection to plasma proteins . It is metabolized primarily in the liver to inactive metabolites. Less than 10% of an oral dose is excreted unchanged in, about 60% is excreted by the kidneys as inactive metabolites; 20-25% is excreted as metabolites in the bile and through the intestines, and in breast milk. It penetrates through the blood-brain barrier.
- arterial hypertension;
- prevention of angina attacks
- Hypersensitivity to the drug.
- Severe hypotension atrioventricular block II and III degree,
- sick sinus syndrome,
- sinoauricular block,
- acute heart failure,
- Chronic heart failurestage of asthma,
- metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease,
- Prinzmetal angina,
- cardiomegaly without signs of heart failure,
- concomitant use with proviron steroid inhibitors,
- age of 18 years (effectiveness and safety have been established).
Be wary appoint:
- Atrioventricular block of I degree.
- Abnormal liver function.
- When aortic stenosis.
- Chronic heart failure (in the stage of compensation).
- Chronic renal failure.
- Occlusive peripheral vascular disease ( “intermittent” claudication, Raynaud’s syndrome).
- Myasthenia gravis.
- Dipressiya (including history).
- Elderly age.
Pregnancy and lactation
Pregnant women should appoint Tenochek only in cases where the benefit to the mother outweighs the potential risk to the fetus.
Tenochek excreted in breast milk, so the feeding period it should be taken only in exceptional cases with great care.
Dosing and Administration
Inside, squeezed the required amount of liquid.
When hypertension and angina, the dose is 1 tablet per day.
If necessary, the daily dose may be increased to 2 tablets per day.
The maximum daily dose is 2 tablets.
Usually the drug is well tolerated, however, the following side effects may occur in some cases:
- cardiovascular system: the proviron steroid emergence of symptoms of heart failure, violation of atrioventricular conduction, bradycardia, marked reduction in blood pressure, feeling cold and paresthesias in extremities, palpitations, shortness of breath, rush of blood to the face;
- digestive system: dry mouth, nausea, vomiting, diarrhea, abdominal pain, constipation, rarely: increased activity of “liver” transaminases and jaundice (caused by cholestasis), dyspepsia;
- central nervous system: dizziness, insomnia, decreased ability to concentrate, drowsiness, depression, hallucinations, lethargy, fatigue, headache, rarely – mood changes, fatigue, blurred vision, paresthesia;
- musculoskeletal system: muscle cramps, myalgia;
- respiratory system: dyspnea, bronchospasm, apnea;
- Hematologic reactions: thrombocytopenic purpura, anemia (aplastic), thrombosis;
- Endocrine System: gynecomastia, reduced potency, decreased libido, gynecomastia;
- metabolic reactions: hyperlipidemia, hypoglycemia;
- Skin reactions: rash, dermatitis, pruritus, photosensitivity, rarely – exudative erythema multiforme;
- Other: frequent urination, peripheral edema, gingival hyperplasia.
Overdose Symptoms: bradycardia, atrioventricular block degree II-III, an increase of symptoms of heart failure, marked reduction in blood pressure, bronchospasm, hypoglycemia. Treatment: in severe bradycardia shown intravenous administration of 1 ml of 0.1% solution of atropine sulfate. When AV blockade II and III extent possible appointment of isoprenaline in tablets of 5 mg under the tongue (if necessary -povtorny reception 2-4 hours) or intravenous drip or slow bolus of the drug at a dose of 0.5-1 mg. In the event of bronchospasm shown proviron steroid. To restore vascular tone -Application vasoconstrictor drugs (in the absence of contraindications to their use); to eliminate the effects of calcium channel blockade -vnutrivennoe administration of calcium gluconate.