Amlodipine, Atenolol

Pharmacological properties

Tenochka - a hypotensive combined drug, which includes amlodipine - a calcium channel blocker and atenolol - a β1-adrenergic receptor blocker.

Amlodipine. The antianginal and antihypertensive effects of amlodipine are due to a direct effect on the smooth muscles of blood vessels, which reduces OPSS and lowers blood pressure. In this regard, there is a decrease in myocardial oxygen demand and energy consumption by the heart muscle. On the other hand, amlodipine probably dilates large-sized coronary arteries and coronary arterioles of both intact and ischemic myocardial sites. This ensures the supply of oxygen to the myocardium during spasm of the coronary arteries.

Atenolol acts primarily on β₁-adrenoreceptors of the heart. It does not have an internal sympathomimetic and membrane stabilizing effect, exhibits antihypertensive properties.

Antianginal and antihypertensive effects are associated with a decrease in heart rate (lengthening diastole and improving myocardial perfusion) and a decrease in myocardial contractility, which results in a decrease in myocardial oxygen demand, which reduces the number of angina attacks.

The combination of atenolol and amlodipine has a more pronounced hypotensive effect than monotherapy with the use of each individual component.

Pharmacokinetics Not studied.

Indications

Ag, chronic coronary heart disease (stable angina).

Application

Applied inside, prescribed only to adults. tablets are taken without chewing, washed down with water, before meals, preferably at the same time. the dose of the drug and the duration of treatment are determined by the doctor individually, depending on the therapeutic effect obtained. Do not change the dosage or stop treatment without the advice of a doctor. with a sudden cessation of the drug, withdrawal syndrome may develop. therefore, dose reduction and drug withdrawal should occur slowly and gradually.

With hypertension - 1 tablet per day. Depending on the individual reaction of the patient, the dose can be increased to a maximum daily dose of 2 tablets.

With angina pectoris - 1 tablet per day.

In patients with significant impaired renal function, the dose depends on creatinine clearance: at 10-30 ml / min, the dose is reduced by 2 times, if clearance is 10 ml / min, the dose is reduced by 4 times compared to the usual one.

Contraindications

Hypersensitivity to the components of the drug, arterial hypotension (systolic hell 90 mm Hg), acute heart failure, av-block II – III degree, sinoatrial block, sick sinus syndrome, myocardial infarction with arterial hypotension, sinus bradycardia (HR 50 beats / min), cardiogenic shock, late stages of peripheral circulation disturbance, metabolic acidosis; severe liver and kidney diseases, Raynauds syndrome, allergic reactions, psoriasis, diabetes mellitus, BA, simultaneous use of MAO inhibitors (with the exception of MAO-B inhibitors). During pregnancy and breastfeeding. children under 18 years old.

Side effects

Usually the drug is well tolerated, but sometimes these side effects are noted:

from the cardiovascular system: bradycardia, arterial hypotension, impaired AV conduction and the appearance of symptoms of heart failure, a feeling of cold and paresthesia in the limbs. In some cases, in patients with angina pectoris, an increase in the severity of seizures cannot be ruled out;

from the gastrointestinal tract: at the beginning of treatment, nausea, vomiting, changes in taste, constipation, diarrhea, dry mouth, pancreatitis, increased concentration of liver enzymes and / or bilirubin in the blood serum, hepatitis, jaundice are possible;

from the nervous system: at the beginning of treatment, fatigue, dizziness, depression, headache, sleep disturbance, nightmares, tinnitus, a feeling of cold and paresthesia in the extremities, hallucinations, mood changes, asthenia, peripheral neuropathy are possible;

endocrine system: decreased potency, decreased glucose tolerance in patients with diabetes mellitus, gynecomastia, hyperglycemia, impotence;

from the respiratory system: in patients predisposed to bronchospasm, bronchial obstruction, shortness of breath are possible;

allergic reactions: itching, skin rash, edema, erythema multiforme;

on the part of the blood system: thrombocytopenia, the formation of antinuclear antibodies, the occurrence of thrombocytopenic or non-thrombocytopenic purpura;

others: increased sweating, redness of the skin, reverse alopecia, visual impairment, decreased secretion of lacrimal fluid, photosensitivity, conjunctivitis, exacerbation of psoriasis, short-term muscle weakness, calf muscle cramps, arthralgia, gingival hyperplasia, myalgia, back pain, increased urination, urination .

Sometimes lipid metabolism disorder may be noted: at a normal level of cholesterol, the level of HDL decreases and the level of TG in the blood plasma rises.

special instructions

Caution is prescribed for patients with severe aortic stenosis, heart failure, impaired liver and kidney function.

Patients with diabetes mellitus and hyperthyroidism should be prescribed with caution, since it can mask tachycardia caused by hypoglycemia or thyrotoxicosis.

In the case of elderly patients with increasing bradycardia (heart rate of 50 beats / min), arterial hypotension (systolic blood pressure of 100 mm Hg), AV blockade, bronchospasm, ventricular arrhythmia, severe liver and kidney function impairment, it is necessary to reduce the dose or cancel the drug. Therapy should be discontinued gradually, reducing the dose within 10-14 days. Patients with coronary heart disease during the period of drug withdrawal should be under medical supervision.

During therapy, alcohol is not recommended.

Particular attention is necessary in the case of surgery using general anesthesia for patients taking Tenochek. With caution, the drug is prescribed for patients with psoriasis, pheochromocytoma, hyperthyroidism and severe myasthenia, with Raynauds disease and other obliterating diseases of the peripheral arteries, in patients with severe impaired renal excretory function. While taking the drug, a decrease in the production of tear fluid is possible, which is important for patients using contact lenses.

Special security measures. In the treatment with the drug, calcium channel blockers such as verapamil and diltiazem or other antiarrhythmic drugs (for example, disopyramide) should not be used iv. The exception is patients who are in intensive care units.

In all these cases, the doctor must carefully weigh the risk / benefit ratio when prescribing the drug.

The drug is contraindicated during pregnancy and lactation.

Children. The drug is contraindicated in children under the age of 18 years.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. With caution is prescribed when driving vehicles or working with other mechanisms.

Interactions

Atenolol

Antiarrhythmic drugs and drugs for anesthesia enhance the cardiodepressive effect of atenolol (the risk of developing bradycardia, arrhythmia, hypotension, heart failure). Reserpine, methyldopa, clonidine, guanfacine, cardiac glycosides potentiate the negative chrono-, dromo- and batmotropic effect of atenolol.When combined, insulin and other antidiabetic agents can cause the development of hypoglycemia. NSAIDs, estrogens, sympathomimetics, xanthines weaken the hypotensive effect; sympatholytics, nitroglycerin, hydralazine enhance; antacids slow down its absorption. Atenolol prolongs the effect of coumarins. Cimetidine inhibits the metabolism of atenolol; co-administration of atenolol with tricyclic antidepressants, antipsychotics, sedatives, hypnotics and alcohol potentiates CNS depression. Incompatible with MAO inhibitors.

Amlodipine

Compatible with major groups of antihypertensive drugs (diuretics, ACE inhibitors, β-adrenergic receptor blockers), nitrates and hypoglycemic drugs. Means for inhalation anesthesia, amiodarone, quinidine and calcium antagonists can potentiate the effect of amlodipine. NSAIDs also do not significantly reduce the hypotensive effect of amlodipine.

Overdose

The main clinical symptoms of an overdose are bradycardia, irregular heartbeat, vomiting, impaired consciousness, bronchospasm, dizziness, cyanosis of the upper and lower extremities may be noted; very rarely - generalized convulsive attacks. an overdose can also lead to excessive peripheral vasodilation and likely reflex tachycardia. Cases of prolonged systemic hypotension, including fatal shock, have been described.

Treatment. In case of an overdose or with a threatening decrease in heart rate and / or blood pressure, drug treatment is stopped. With clinically significant arterial hypotension caused by an overdose, it is necessary to carry out active measures aimed at maintaining the function of the cardiovascular system, including monitoring of indicators of the heart and lungs, careful monitoring of vital signs, monitoring of BCC and urine output. In order to eliminate the effects of blockade of calcium channels, intravenous administration of calcium gluconate is necessary.

If necessary, appoint:

• atropine (0.5–2 ml w / o bolus);

• glucagon: the initial dose is 1–10 mg iv (jet), then 2–2.5 mg / h in the form of a continuous infusion;

• sympathomimetics depending on body weight and effect (dopamine, dobutamine, isoprenaline, oxyprenaline or epinephrine).

If refractoriness to therapy for bradycardia is detected, temporary pacemaking is possible.

With bronchospasm, β is prescribed₂- sympathomimetics in the form of an aerosol (in case of insufficient effect also in / in) or aminophylline in / in.

With generalized seizures, a slow intravenous administration of diazepam is prescribed. There is no specific antidote.

Storage conditions

In a dry, dark place at a temperature of no higher than 25 ° C.