Tenochek, pills, 28pcs

Composition

1 tablet contains active substances:

• Active ingredients:
• atenolol 50 mg, aAmlodipine 5 mg.
• Auxiliary substances:
• corn starch,
• calcium phosphate dibasic,
• microcrystalline cellulose,
• povidone-30,
• sodium starch glycolate,
• purified talc,
• magnesium stearate,
• colloidal silicon dioxide,
• isopropyl alcohol,
• purified water.

Pharmacological action

Tenochek is a combined antihypertensive drug.

Pharmacodynamics

The effect is due to the action of two components-a beta-1-adrenoblocker (atenolol) and a blocker of “slow” calcium channels (amlodipine).

The fixed combination of Atenolol and Amlodipine is considered the most effective combination when considered from the standpoint of metabolic and hemodynamic drug interaction. Taking Amlodipine leads to dilation of the 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. As a selective blocker of β1-adrenergic receptors, Atenolol eliminates reflex tachycardia caused by Amlodipine. Recent clinical studies have demonstrated the beneficial effect of therapy with slow calcium channel blockers on the blood lipid spectrum, which helps reduce the risk of cardiovascular outcomes. The complementary mechanism of action of Amlodipine, which reduces 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, antihypertensive and antiarrhythmic effects. It has no membrane-stabilizing and internal sympathomimetic activity. Reduces catecholamine stimulation of cAMP and ATP formation, reduces intracellular Ca2+current. In the first 24 hours after oral use, against the background of a decrease in cardiac output, a reactive increase in total peripheral vascular resistance is noted, the severity of which gradually decreases over 1-3 days. The hypotensive effect is associated with a decrease in cardiac output, a decrease in the activity of the renin-angiotensin system, the sensitivity of barocereptors, 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 medium therapeutic doses, it has no effect on the tone of peripheral arteries. The antihypertensive effect lasts 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 (prolongation of diastole and improvement of myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation. Reduces the heart rate at rest and during exercise. By increasing the tension of the ventricular muscle fibers and the final diastolic pressure in the left ventricle, it can increase the myocardial oxygen demand, 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 sinoauricular node, and prolongation of the refractory period. It inhibits the conduction of impulses in the antegrade and, to a lesser extent, in the retrograde directions through the atrioventricular node and along additional pathways. Increases the survival rate of patients who have had a myocardial infarction (reduces the frequency of ventricular arrhythmias and angina attacks).

In therapeutic concentrations, it does not affect beta-2 adrenergic receptors, in contrast to non-selective beta-adrenergic blockers, 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 bronchodilating effect of isoproterenol. When taken more than 100 mg per day, it can have a beta-2-adrenoblocking effect. The negative chronotropic effect manifests itself 1 hour after use, reaches a maximum after 2-4 hours and lasts up to 24 hours. Amlodipine: a dihydropyridine derivative. It has antihypertensive, atnianginal, antispasmodic and vasodilating effects. Blocks the flow of calcium ions through cell membranes to smooth muscle cells of the myocardium and blood vessels.

The mechanism of antihypertensive action is due to a direct relaxing effect on the smooth muscles of blood vessels. The antianginal effect of the drug is due, firstly, to its ability to dilate peripheral arterioles, which leads to a decrease in total peripheral vascular resistance. Reducing the load on the heart leads to a decrease in the need for oxygen in the myocardium. Secondly, under the influence of the drug, due to the expansion of the coronary arteries, oxygen supply to the myocardium increases (especially in vasospastic angina pectoris). Amlodipine does not adversely affect the metabolism and plasma lipids, has anti-atherosclerotic, antithrombotic activity, increases the glomerular filtration rate, and has a weak natriuretic effect. In diabetic nephropathy, it does not increase the severity of microalbuminuria.

Pharmacokinetics

Atenolol: after oral use, the drug is rapidly absorbed from the gastrointestinal tract-approximately 50% of the oral dose. Fat solubility is poor, bioavailability is 40-50%, and the time to reach the maximum concentration in blood plasma after oral use is 2-4 hours. Poorly penetrates the blood-brain barrier, passes in insignificant amounts through the placental barrier and into breast milk. Binding to plasma proteins is 6-16%.

It is practically not metabolized in the liver. The elimination half-life is 6-9 hours (increased in elderly patients). It is excreted by the kidneys by glomerular filtration (85-100% unchanged). Impaired renal function is accompanied by prolongation of T_-frac and accumulation, with creatinine clearance below 35 mg / min/1.73 m2, T_-frac is 16-27 hours, with clearance below 15 mg / min-more than 27 hours (dose reduction is necessary). It is removed during hemodialysis.

Amlodipine: after oral use, amlodipine is rapidly absorbed from the gastrointestinal tract 90%, the maximum concentration of the drug in the blood is observed after 6-12 hours. The equilibrium concentration of the drug in the blood plasma is reached in 7-8 days after its continuous use.

The drug has a high volume of distribution – about 20 l / kg; bioavailability is 60-65%, the connection with plasma proteins is high-more than 95%. The_half-life of the drug is 35-45 hours. It is mainly metabolized in the liver to form inactive metabolites. Less than 10% of the oral dose is excreted unchanged, about 60% is excreted by the kidneys as inactive metabolites; 20-25% is excreted as metabolites in the bile and through the intestine, as well as in breast milk. Penetrates the blood-brain barrier.

Indications

Arterial hypertension; prevention of angina attacks

Use during pregnancy and lactation

Pregnant women should be prescribed Tenochek only in cases where the benefit to the mother exceeds 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 caution.

Contraindications

• Hypersensitivity to the drug Tenochek.
• Severe hypotension Atrioventricular block II and III degree,
• the syndrome of weakness of the sinus node,
• sinoauricular blockade,
• acute heart failure,
• chronic heart failure II B – III stage of asthma,
• bradycardia,
• metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease,
• Prinzmetal’s angina,
• cardiomegaly without signs of heart failure,
• concurrent use with MAO inhibitors,
• age to 18 years (efficacy and safety not established).

Prescribe with caution when: :

• Grade I atrioventricular block.
• Impaired liver function.
• With stenosis of the aortic mouth.
• Chronic heart failure (at the stage of compensation).
• Chronic renal failure.
• Pheochromocytoma.
• Diabetes mellitus.
• Hypoglycemia.
• Tereotoxicosis.
• Obliterating peripheral vascular diseases (intermittent claudication, Raynaud’s syndrome).
• Myasthenia gravis.
• Depression (including a history of it).
• Psoriasis.
• Advanced age.

Side effects

Usually, the drug is well tolerated by patients, however, in some cases, the following side effects may occur: :

• cardiovascular system: the appearance of symptoms of heart failure, impaired atrioventricular conduction, bradycardia, a pronounced decrease in blood pressure, a feeling of cold and paresthesia in the extremities, palpitations, shortness of breath, flushes of blood to the skin of the face;
• digestive tract: dry mouth, nausea, vomiting, diarrhea, abdominal pain, constipation, rare: increased activity of “liver” transaminases and jaundice (due to cholestasis), dyspepsia;
• Central nervous system: dizziness, sleep disturbance, decreased ability to concentrate, drowsiness, depression, hallucinations, lethargy, fatigue, headache, rarely – changing mood, asthenia, blurred vision, paresthesia;
• musculoskeletal: muscle cramps, myalgia;
• respiratory system: dyspnea, bronchospasm, apnea;
• hematologic reactions: thrombocytopenic purpura, anemia (aplastic), pulmonary;
• endocrine system: gynecomastia, reduced potency, decreased libido, gynecomastia;
• metabolic reactions: hyperlipidemia, hypoglycemia;
• skin reactions: urticaria, dermatitis, pruritus, photosensitivity, rarely – exudative erythema multiforme;
• other: increased frequency of urination, peripheral edema, gingival hyperplasia.

Interaction

Concomitant use of atenolol and insulin (or other oral hypoglycemic agents) masks the symptoms of hypoglycemia. When combined with antihypertensive agents of other groups, the hypotensive effect increases. The hypotensive effect is weakened by estrogens (sodium retention).

Concomitant use of atenolol and cardiac glycosides increases the risk of developing bradycardia and impaired atrioventricular conduction. When atenolol is co-administered with reserpine, methyldopa, clonidine, verapamil, severe bradycardia may occur. Patients taking atenolol and clonidine at the same time should be discontinued only after a few days after discontinuation of atenolol treatment. With simultaneous use of atenolol with derivatives of ergotamine, xanthine-its effectiveness decreases.

Concomitant use with lidocaine may reduce its excretion and increase the risk of its toxic effects.

Application together with phenothiazine derivatives helps to increase the concentration of each of the drugs in the blood serum.

Phenytoin with intravenous use, general anesthesia agents increase the severity of the cardiodepressive effect of atenolol. Concomitant use with MAO inhibitors is not recommended. Allergens used for immunotherapy, or allergen extracts for skin tests and iodine-containing radiopaque substances for intravenous use increase the risk of severe systemic allergic reactions or anaphylaxis.

Inhaled general anesthesia agents (hydrocarbon derivatives) increase the risk of myocardial function depression and a marked 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, anticoagulation effect of coumarins.

How to take, course of use and dosage

Inside, with the required amount of liquid.

With arterial hypertension and angina pectoris, the dose is 1 tablet per day.

If necessary, the daily dose can be increased to 2 tablets per day.

The maximum daily dose is 2 tablets.

Overdose

Symptoms: severe bradycardia, grade II-III atrioventricular block, increased symptoms of heart failure, marked decrease in blood pressure, bronchospasm, hypoglycemia.

Treatment: for severe bradycardia, intravenous use of 1 ml of 0.1% atropine sulfate solution is indicated. With AV blockade of II and III degrees, it is possible to prescribe isoprenaline in tablets of 5 mg under the tongue (if necessary, repeated use after 2-4 hours) or intravenous drip or slow jet use of the drug in a dose of 0.5-1 mg. If bronchospasm occurs, beta-2-adrenomimetics are indicated. To restore vascular tone-the use of vasoconstrictor drugs (in the absence of contraindications to their use); to eliminate the consequences of calcium channel blockade-intravenous use of calcium gluconate.

Special instructions

Monitoring of patients 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 (once every 4-5 months). In elderly patients, it is recommended to monitor renal function (1 time in 4-5 months).

The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50/ min. With thyrotoxicosis, the drug may mask certain clinical signs of hyperthyroidism (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, as it can increase symptoms. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal levels.

In patients with coronary heart disease (CHD), abrupt discontinuation of the drug may cause an increase in the frequency or severity of anginal attacks, so discontinuation in patients with CHD should be carried out gradually. Special attention should also be paid to the selection of doses in patients with decompensated heart failure (compensated).

Special attention should be paid in cases where surgical intervention under general anesthesia is required. The drug should be discontinued 48 hours before surgery. As an anesthetic, you should choose a prepazate with a possible minimal negative inotropic effect. When used concomitantly with clonidine, Tenochek is stopped several days earlier than clonidine in order to avoid the “withdrawal” syndrome of the latter.

It is possible to increase the severity of an allergic reaction and the lack of effect from conventional doses of epinephrine against the background of a burdened allergic history. Drugs that reduce the supply of catecholamines (for example, reserpine) can increase the effect of beta-blockers, so patients taking such combinations of drugs should be constantly monitored by a doctor for a pronounced decrease in blood pressure or bradycardia. If elderly patients develop severe bradycardia (less than 50 beats/min), a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg, AV block, bronchospasm, ventricular arrhythmias, severe liver and kidney function disorders, it is necessary to reduce the dose or discontinue treatment. If you develop depression caused by taking the drug, it is recommended to stop therapy.

If intravenous use of verapamil is necessary, this should be done at least 48 hours after taking Tenochek. When using atenolol, it is possible to reduce the production of tear fluid, which is important for patients using contact lenses. Do not abruptly interrupt treatment due to the risk of developing severe arrhythmias and myocardial infarction. Withdrawal 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 cancel the drug before testing the concentration in the blood and urine of catecholamines, vanillylmindal acid; titers of antinuclear antibodies. In smokers, the effectiveness of beta-blockers is lower.

Do not abruptly cancel Tenochek in patients suffering from coronary heart disease.

Impact on the ability to drive a car and work with machinery

Tenochek should be prescribed with caution to drivers of motor vehicles and people working with mechanisms, because of a possible decrease in attention.

Form of production

Tablets

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years

Active ingredient

Amlodipine, Atenolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension, Angina