Tenochek tabs #28

Tenochek user manual

You can buy Tenochek here

Composition

1 tablet contains active substances:
Atenolol 50 mg, Amlodipine 5 mg
Excipients:
Corn starch, dibasic calcium phosphate, microcrystalline cellulose, povidon-30, sodium starch glycolate, purified talcum, magnesium stearate, silicon colloidal dioxide, isopropyl alcohol, purified water.
Description: Tablets of white or almost white color, round, flat, with beveled edges and embossed TC on one side and dividing the risk on the other side.
Pharmacotherapeutic group: Hypotensive combined agent (beta-blocker and blocker of “slow” calcium channels).
ATX Code: C02

Pharmacodynamics

Combined antihypertensive drug. The effect is caused by the action of two components - beta1-adrenergic blocker (atenolol) and the blocker of “slow” calcium channels, (amlodipine).
A fixed combination of Atenolol and Amlodipine is considered the most effective combination when considered from the standpoint of the metabolic and hemodynamic interaction of drugs. Reception of Amlodipine leads to dilation of arterioles, which is expressed by reflex tachycardia. This is one of the main side effects of Amlodipine. An increase in heart rate leads to an increase in myocardial oxygen demand, which is undesirable for patients with coronary heart disease. Being a selective β1-adrenergic receptor blocker, Atenolol levels the reflex tachycardia caused by Amlodipine. Clinical studies in recent years have demonstrated the beneficial effect of the therapy of blockers of “slow” calcium channels on the lipid spectrum of blood, which helps reduce the risk of cardiovascular outcomes. The complementary mechanism of action of Amlodipine, which reduces the total peripheral vascular resistance and Atenolol, which reduces cardiac output, leads to a more pronounced hypotensive effect and better tolerability compared to monotherapy with Amlodipine and Atenolol, improving the effectiveness / side effects ratio.
Atenolol: has antianginal, hypotensive and antiarrhythmic effects. Does not possess membrane stabilizing and internal sympathomimetic activity. Reduces catecholamine stimulation and the formation of cAMP and ATP, reduces the intracellular current of Ca2 +. In the first 24 hours after oral administration, on the background of a decrease in cardiac output, a reactive increase in the total peripheral vascular resistance is noted, the severity of which gradually decreases within 1-3 days. The antihypertensive effect is associated with a decrease in cardiac output, a decrease in the activity of the renin-angiotensin system, the sensitivity of barotransporters and an effect on the central nervous system. The hypotensive effect is manifested by a decrease in systolic and diastolic blood pressure, a decrease in stroke and minute volumes. In moderate therapeutic doses, it has no effect on the tone of peripheral arteries. The antihypertensive effect lasts for 24 hours, with regular use it stabilizes by the end of 2 weeks of treatment.
The antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (diastole lengthening and improvement in myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation. It reduces the heart rate at rest and during physical exertion. By increasing the tension of the muscle fibers of the ventricles and the end-diastolic pressure in the left ventricle can increase the oxygen demand of the myocardium, especially in patients with chronic insufficiency. The antiarrhythmic effect is manifested by the suppression of sinus tachycardia and is associated with the elimination of arrhythmogenic sympathetic influences on the cardiac conduction system, inhibition of heterogeneous automatism, a decrease in the rate of propagation of excitation through the shinoauricular site and an elongation of the refractory period. Inhibits conduction of impulses in the antegrade and, to a lesser extent, in the retrograde directions through the atrioventricular node and along additional paths.
Increases the survival of patients with myocardial infarction (reduces the frequency of ventricular arrhythmias and seizures of wallcardia).
At therapeutic concentrations, it does not affect beta-2 adrenoreceptors, in contrast to non-selective beta-adrenoborcators, it has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries and on lipid metabolism. Slightly reduces the vital capacity of the lungs, practically does not weaken the bronchodilatory effect of isoproterenol. When taken more than 100 mg per day can have a beta-2-adrenergic blocking effect. The negative chronotropic effect appears 1 hour after administration, reaches a maximum after 2-4 hours and lasts up to 24 hours. Amlodipine: a dihydropyridine derivative. It has an antihypertensive, anti-anginal, antispasmodic and vasodilator action. It blocks the entry of calcium ions through the cell membranes into the smooth muscle cells of the myocardium and blood vessels.
The mechanism of the hypotensive action is due to a direct relaxing effect on vascular smooth muscle.
The anti-anginal effect of Tenochek is due, firstly, to its ability to expand peripheral arterioles, which leads to a decrease in total peripheral vascular resistance. Reducing the load on the heart leads to a decrease in myocardial oxygen demand. Secondly, under the action of Tenochek, due to the expansion of the coronary arteries increases the flow of oxygen into the myocardium (especially with vasospastic angina). Amlodipine does not adversely affect metabolism and blood plasma lipids, has anti-atherosclerotic, antithrombotic activity, increases glomerular filtration rate, has a weak natriuretic effect. In diabetic nephropathy does not increase the severity of microalbuminuria.

Pharmacokinetics

Atenolol: After ingestion, Tenochek is rapidly absorbed from the gastrointestinal tract - approximately 50% of the oral dose. Fat solubility is poor, bioavailability is 40-50%, the time to reach the maximum plasma concentration after ingestion is 2-4 hours. It penetrates the blood-brain barrier poorly, passes in small quantities through the placental barrier and into breast milk. Communication with plasma proteins - 6-16%.
Practically not metabolized in the liver. The elimination half-life is 6–9 hours (it increases in elderly patients). Excreted by the kidneys by glomerular filtration (85-100% unchanged). Impaired renal function is accompanied by an elongation of T & frac; and cumulation, with creatinine clearance below 35 mg / min / 1.73 m2, T & amp; makes 16-27 hours, at clearance below 15 mg / min - more than 27 hours (reduction of doses is necessary). Excreted during hemodialysis.
Amlodipine: after oral administration, amlodipine is rapidly absorbed from the gastrointestinal tract 90%, the maximum concentration of Tenochek in the blood is observed after 6-12 hours. The equilibrium concentration of the drug in the blood plasma is reached after 7-8 days after its continuous use. The drug has a high volume of distribution - about 20 l / kg; bioavailability is 60-65%, communication with plasma proteins is high - more than 95%. T½ of Tenochek is 35-45 hours. Metabolized mainly in the liver to form inactive metabolites. Less than 10% of the ingested dose is excreted unchanged, about 60% is excreted by the kidneys as inactive metabolites; 20-25% is excreted in the form of metabolites with bile and through the intestines, as well as with breast milk. It penetrates the blood-brain barrier.

Indications for use

    arterial hypertension;
    prevention of angina attacks

Contraindications

    Hypersensitivity to Tenochek.
    Severe arterial hypotension Atrioventricular block II and III degree,
    sick sinus syndrome,
    sinoauricular block,
    acute heart failure
    chronic heart failure II B - stage III decompensated,
    severe bradycardia,
    metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease,
    Prinzmetal angina,
    cardiomegaly without signs of heart failure,
    simultaneous use with MAO inhibitors,
    age up to 18 years (efficacy and safety have not been established).

Use with caution when

    Atrioventricular block I degree.
    Liver dysfunction.
    When stenosis of the mouth of the aorta.
    Chronic heart failure (in the stage of compensation).
    Chronic renal failure.
    Pheochromocytoma.
    Diabetes.
    Hypoglycemia.
    Tereotoksikoz.
    Obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome).
    Myasthenia gravis
    Depression (including in history).
    Psoriasis.
    Elderly age.

Pregnancy and lactation period

Pregnant women should be prescribed Tenochek only in cases where the benefit to the mother outweighs the potential risk to the fetus.
Tenochek is excreted in breast milk, so during the feeding period it should be taken only in exceptional cases with great care.

Method of use and dose

Inside, drinking down the necessary amount of fluid.
In 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 of 2 tablets.

Side effects of Tenochek

Usually the drug is well tolerated by patients, however, in some cases the following side effects may occur:
    cardiovascular system: symptoms of heart failure, impaired atrioventricular conduction, bradycardia, marked reduction in blood pressure, feeling cold and paresthesia in the extremities, palpitations, shortness of breath, blood rushes to the skin of the face;
    digestive tract: 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, asthenia, blurred vision, paresthesia;
    musculoskeletal system: muscle cramps, myalgia;
    respiratory system: dyspnea, bronchospasm, apnea;
    hematological reactions: thrombocytopenic purpura, anemia (aplastic), thrombosis;
    endocrine system: gynecomastia, reduced potency, decreased libido, gynecomastia;
    metabolic reactions: hyperlipidemia, hypoglycemia;
    skin reactions: urticaria, dermatitis, pruritus, photosensitivity, rarely - exudative erythema multiforme;
    other: increased urination, peripheral edema, gingival hyperplasia.

Overdose with Tenochek

Symptoms: severe bradycardia, atrioventricular block II-III degree, increased symptoms of heart failure, marked reduction in blood pressure, bronchospasm, hypoglycemia.
Treatment: for severe bradycardia, intravenous administration of 1 ml of 0.1% atropine sulfate solution is indicated. With AV blockade II and III degree, it is possible to prescribe isoprenaline 5 mg tablets under the tongue (if necessary, a second dose in 2-4 hours) or intravenous drip or slow jet injection of Tenochek in a dose of 0.5-1 mg. If bronchospasm occurs, beta2-adrenomimetics are shown. To restore vascular tone - the use of vasoconstrictor drugs (in the absence of contraindications to their use); to eliminate the effects of calcium channel blockade, intravenous administration of calcium gluconate.

Interaction with other drugs

With simultaneous use of atenolol and insulin (or other oral hypoglycemic agents) masks the symptoms of hypoglycemia. When combined with antihypertensive drugs of other groups, there is an increase in the hypotensive effect. The antihypertensive effect is weakened by estrogens (sodium retention).
With simultaneous use of atenolol and cardiac glycosides increases the risk of developing bradycardia and impaired atrioventricular conductivity. With the simultaneous appointment of atenolol with reserpine, methyldopa, clonidine, verapamil, the occurrence of severe bradycardia is possible. Patients taking simultaneously atenolol and clonidine, clonidine is canceled only after several days after stopping treatment with atenolol. While taking atenolol with ergotamine derivatives, xanthine - its effectiveness decreases.
Simultaneous use with lidocaine can reduce its elimination and increase the risk of its toxic action.
Use in conjunction with phenothiazine derivatives, helps to increase the concentration of each of the drugs in serum.
Phenytoin with a / in the introduction, means for general anesthesia increase the severity of the cardiodepressive action of atenolol. Not recommended simultaneous use with MAO inhibitors. Allergens used for immunotherapy or allergen extracts for skin tests and iodine radiopaque substances for IV administration increase the risk of severe systemic allergic reactions or anaphylaxis.
Means for general inhalation anesthesia (hydrocarbon derivatives) increase the risk of inhibition of myocardial function and a pronounced decrease in blood pressure. Amiodarone increases the risk of developing bradycardia and inhibits AV conduction. Cimetidine increases the concentration of atenolol in the blood plasma (inhibits metabolism).
Prolongs the action of non-depolarizing muscle relaxants, anti-coagulation effect of coumarins.

special instructions

Patient monitoring should include monitoring of heart rate and blood pressure (at the beginning of treatment - daily, then once every 3-4 months), monitoring of blood glucose concentration in patients with diabetes mellitus (1 time in 4-5 months). In elderly patients, it is recommended to monitor renal function (once every 4-5 months).
The patient should be trained in the method of counting heart rate and instructed on the need for medical consultation with heart rate less than 50 / min. With thyrotoxicosis, Tenochek may mask certain clinical signs of hyperthyroidism (for example, tachycardia). Abrupt cancellation in patients with thyrotoxicosis is contraindicated, as it can strengthen the symptoms. Unlike non-selective beta-adrenergic blockers, the insulin-induced hypoglycemia practically does not increase and does not delay the restoration of glucose concentration in the blood to normal levels.
In patients with coronary heart disease (CHD), abrupt withdrawal of the drug can cause an increase in the frequency or severity of angina attacks, so stopping treatment for CHD patients should be carried out gradually. Particular attention also requires the selection of doses in patients with decompensated heart failure (compensated).
Special care is needed in cases where surgery is required under general anesthesia. Tenochek should be discontinued 48 hours before surgery. As an anesthetic one should choose a prepasat with a possible minimal negative inotropic effect. With simultaneous use with clonidine, Tenochek is discontinued a few days earlier than clonidine in order to avoid the "cancellation" syndrome of the latter.
Perhaps an increase in the severity of the allergic reaction and the lack of effect from the usual doses of epinephrine on the background of the burdened allergic history. Drugs that reduce the supply of catecholamines (for example, reserpine) can enhance the action of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect pronounced decrease in blood pressure or bradycardia. In the case of elderly patients with severe bradycardia (less than 50 beats / min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg, AV blockade, bronchospasm, ventricular arrhythmias, severe liver function impairment and kidney damage, or discontinue treatment. With the development of depression caused by taking the drug - it is recommended to stop therapy.
If intravenous verapamil is needed, this should be done no less than 48 hours after taking Tenochek.
With the use of atenolol, it is possible to reduce the production of tear fluid, which is important for patients using contact lenses. You can not abruptly interrupt treatment because of the risk of developing severe arrhythmias and myocardial infarction. Cancellation is carried out gradually, reducing the dose for 2 weeks or more (reduce the dose by 25% in 3-4 days).
It is necessary to discontinue Tenochek before the study of the concentration in the blood and urine of catecholamines, vanillyl almond acid; antinuclear antibody titers. In smokers, the effectiveness of beta-blockers below.
You should not abruptly cancel Tenochek in patients suffering from coronary heart disease.

Influence on ability to drive the car and to work with equipment

Tenochek should be carefully assigned to drivers of vehicles and persons working with mechanisms, because of the possible reduction of attention.

Release form

Primary: 10 or 14 tablets in Al / Al strips or Al / PVC blisters.
Secondary: For 2, 3, 4, 5 or 10 strips or blisters together with instructions for use are placed in a cardboard box.

Storage conditions

List B.
In a dry, dark place, at a temperature not higher than 25 ° C. Keep out of the reach of children.
Shelf life - 4 year. Do not use later than the date indicated on the package.

Terms of sell

You don't need a prescription to buy Tenochek.