Egilok, tablets 100 mg 60 pcs

Pharmgroup:

A beta1-adrenoblocker selective.

Pharmic action:

Egilok is a cardioselective β-adrenoreceptor blocker with no intrinsic sympathomimetic and membrane-stabilizing activity. It has antihypertensive, antianginal and antiarrhythmic action.
Blocking in low doses of cardiac β1-adrenoceptors, reduces catecholamine-stimulated formation of cAMP from ATP, decreases intracellular Ca2+ flow, produces negative chrono-, dromo-, batmo- and inotropic action (decreases HR, inhibits conduction and excitability, reduces myocardial contractility).

The HRPS at the beginning of drug administration (within the first 24 hours after oral administration) increases, after 1-3 days of use it returns to the baseline level, and with further use it decreases.

The antihypertensive effect is caused by the decrease of cardiac output and renin synthesis, inhibition of the activity of renin-angiotensin system and CNS, restoration of sensitivity of aortic arch baroreceptors (there is no increase of their activity in response to a decrease of BP) and as a result, a decrease of peripheral sympathetic effects. Reduces elevated BP at rest, under physical stress and strain.

The BP decreases in 15 min, maximum in 2 h; action lasts for 6 h. Stable decrease is observed after several weeks of regular use.

The antianginal effect is determined by decrease of myocardial oxygen demand as a result of decrease of HR (prolongation of diastole and improvement of myocardial perfusion) and contractility and decrease of myocardial sensitivity to sympathetic innervation. It reduces the frequency and severity of angina attacks and increases exercise tolerance.

The antiarrhythmic effect is caused by the removal of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increase of cAMP, arterial hypertension), decrease of spontaneous excitation rate of sinus and ectopic pacemakers and slowing of AV conduction (mainly in the antegrade and, to a lesser degree, in the retrograde direction through the AV node) and through additional pathways.

In supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart disease and hyperthyroidism, it slows the HR and may even lead to restoration of sinus rhythm.

Prevent the development of migraine.

Long-term use reduces blood cholesterol.

In medium therapeutic doses, it has less effect on the organs containing β2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi, uterus) and on carbohydrate metabolism.

When used in high doses (more than 100 mg/day) it has a blocking effect on both subtypes of β-adrenoreceptors.

Pharmacokinetics:

Absorption

It is rapidly and completely (95%) absorbed from the GI tract. Cmax in plasma is reached 1.5-2 hours after oral administration. Bioavailability is 50%. During treatment the bioavailability increases to 70%. Food intake increases bioavailability by 20-40%.

Distribution
Vd is 5.6 l/kg. Binding with blood plasma proteins is 12%. It penetrates through the HEB and the placental barrier. It is excreted with breast milk in small amounts.

Metabolism
Metoprolol is biotransformed in the liver. Metabolites have no pharmacological activity.

Elimation
T1/2 averages 3.5-7 h. Metoprolol is almost completely excreted in the urine in 72 hours. About 5% of the dose is excreted unchanged.

Pharmacokinetics in special clinical cases

The bioavailability and T1/2 of metoprololol increase with marked hepatic impairment, which may require adjustment of the drug dose.

In impaired renal function, the T1/2 and systemic clearance of metoprololol do not change significantly.

Indications

– Arterial hypertension (in monotherapy or in combination with other antihypertensive agents);
– Chronic heart failure in the compensation stage (in addition to standard therapy with diuretics, ACE inhibitors, cardiac glycosides);
– CHD (secondary prevention of myocardial infarction, prevention of angina attacks);
– hyperkinetic cardiac syndrome;
– hyperthyroidism (as a part of complex therapy);
– prevention of migraine attacks.

Active ingredient

Composition

1 tablet contains metoprolol tartrate 100 mg;

excipients:

MCC;

Sodium carboxymethyl starch;

Colloidal anhydrous silica;

povidone;

Magnesium stearate.

How to take, the dosage

Egilok is prescribed for arterial hypertension in a daily dose of 50-100 mg/day in 1 or 2 doses. In case of insufficient therapeutic effect, the daily dose may be gradually increased to 100-200 mg.

In angina pectoris, supraventricular arrhythmias, for prevention of migraine attacks, the dose of 100-200 mg/day in 2 doses (morning and evening) is prescribed.

In secondary prevention of myocardial infarction the drug is indicated in the average daily dose of 200 mg in two doses (morning and evening).
In functional disorders of cardiac activity with tachycardia the drug is indicated in the daily dose of 100 mg in two doses (morning and evening).

The tablets should be taken orally during or immediately after the meal. The tablets may be divided in half, but not chewed.

Interaction

When concomitant use of Egilok with MAO inhibitors, a significant increase in the hypotensive effect is possible. A break between taking MAO inhibitors and Egilok should be at least 14 days.

Concomitant intravenous administration of verapamil may provoke cardiac arrest, simultaneous administration of nifedipine leads to a significant decrease in BP.

Anesthetic agents (hydrocarbon derivatives) when used simultaneously with Egilok, increase the risk of myocardial contractile depression and development of arterial hypotension.

When used concomitantly, beta-adrenergic stimulants, theophylline, cocaine, estrogens, indomethacin and other NSAIDs reduce the hypotensive effect of Egiloc.

When concomitant use of Egilok and ethanol an increase in CNS depressant effect is noted.

Concomitant use of Egilok with ergot alkaloids increases the risk of peripheral circulatory disorders.
Concomitant use of Egilok increases the effect of oral hypoglycemic drugs and insulin and increases the risk of hypoglycemia.

Concomitant use of Egilok with antihypertensive agents, diuretics, nitrates, calcium channel blockers increases the risk of arterial hypotension.

In concomitant use of Egilok with verapamil, diltiazem, antiarrhythmic agents (amiodarone), reserpine, methyldopa, clonidine, guanfacine, agents for general anesthesia and cardiac glycosides may increase the severity of HR depression and suppression of AV conduction.

Hepatic microsomal enzyme inducers (rifampicin, barbiturates) increase metabolism of metoprolol, which leads to decreased plasma concentrations of metoprolol and decreased effect of Egilok.

Hepatic microsomal enzyme inhibitors (cimetidine, oral contraceptives, phenothiazines) increase the plasma concentration of metoprolol.

Allergens used for immunotherapy or allergen extracts for skin tests, when combined with Egiloc, increase the risk of systemic allergic reactions or anaphylaxis.

Iodine-containing x-ray contrast agents for IV administration increase the risk of anaphylactic reactions when used concomitantly with Egiloc.

Egilok with concomitant use decreases clearance of xanthines, especially in patients with initially increased clearance of theophylline due to smoking.

Concomitant use with Egiloc decreases lidocaine clearance and increases plasma lidocaine concentrations.

Concomitant use of Egilok increases and prolongs the effect of nondepolarizing muscle relaxants; prolongs the effect of indirect anticoagulants.

When co-administered with ethanol, there is an increased risk of marked BP decrease.

Special Instructions

The heart rate and BP should be monitored regularly when prescribing Egilok. The patient should be warned that if the HR is less than 50 bpm, a physician should be consulted.

In patients with diabetes mellitus, blood glucose levels should be monitored regularly and the dose of insulin or oral hypoglycemic drugs should be adjusted if necessary.

Prescribing of Egilok to patients with chronic heart failure is possible only after compensation stage is reached.
Patients taking Egilok may have increased hypersensitivity reactions (with a history of allergy) and no effect from administration of usual doses of epinephrine (adrenaline).

The use of Egilok may aggravate the symptoms of peripheral circulatory disorders.

Egiloc should be withdrawn gradually, gradually reducing the dose over 10 days. Withdrawal syndrome (worsening of angina attacks, increase of BP) may occur if the treatment is stopped abruptly. During drug withdrawal, patients with angina pectoris should be under close medical supervision.

In angina patients with tension angina, the selected dose of the drug should provide an HR at rest within 55-60 bpm, and not more than 110 bpm on exertion.

Patients who wear contact lenses should be aware that treatment with beta-adrenoblockers may decrease lacrimal fluid production.

Methoprolol may mask some clinical manifestations of hyperthyroidism (tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it may exacerbate the symptoms.

In diabetics taking Egilok may mask the symptoms of hypoglycemia (tachycardia, sweating, increased BP).
When metoprolol is administered to patients with bronchial asthma, beta2-adrenomimetics should be used concomitantly.
In patients with pheochromocytoma, Egilok should be used in combination with alpha-adrenoblockers.

Before any surgical intervention, the anesthesiologist should be informed about the therapy with Egilok (choice of general anesthesia drug with minimal negative inotropic effect); cancellation of the drug is not required.

When prescribing the drug in elderly patients, hepatic function should be monitored regularly. Correction of the dosage regimen is required only in case of increasing bradycardia, marked BP decrease, AV-blockade, bronchospasm, ventricular arrhythmias, severe liver function abnormalities in elderly patients. Sometimes it is necessary to stop treatment.

Patients with a history of depressive disorders should be especially monitored. If depression develops, Egiloc should be discontinued.

Pediatric use

The efficacy and safety of Egiloc in children and adolescents under 18 years of age have not been determined.

Impact on driving and operating ability

In patients whose activities require increased attention, the prescription of the drug on an outpatient basis should be decided only after evaluating the patient’s individual response.

Contraindications

– cardiogenic shock;
– II and III degree AV-blockade;
– sinoatrial block;
– CCSU;
– expressed bradycardia (heart rate less than 50 beats/min).
– heart failure in decompensation stage;
– angiospastic angina pectoris (Prinzmetal angina pectoris);
– significant arterial hypotension (systolic BP below 100 mm Hg.Lactation period;
– concurrent use of MAO inhibitors;
– concurrent intravenous administration of verapamil;
– hypersensitivity to metoprolol and other ingredients of the preparation.

. The preparation should be used with caution in diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (pulmonary emphysema, chronic obstructive bronchitis), peripheral vascular obliterating diseases (intermittent claudication, Raynaud’s syndrome), liver failure, chronic renal failure, myasthenia gravis, pheochromocytoma, 1st degree AV-blockade, thyrotoxicosis, depression (including anamnesis).including in anamnesis), psoriasis, as well as in children and teenagers under 18 years old and elderly patients.

Side effects

CNS and peripheral nervous system: increased fatigue, weakness, headache, slowed rate of mental and motor reactions; rarely – paresthesias in the extremities, depression, anxiety, decreased ability to concentrate, drowsiness, insomnia, nightmares, confusion or short-term memory loss, asthenic syndrome, muscle weakness.

Sensory organs: rarely – decreased vision, decreased tear fluid secretion, xerophthalmus, conjunctivitis, tinnitus.

Cardiovascular system disorders: Sinus bradycardia, palpitations, decreased BP, orthostatic hypotension; rarely – reduced myocardial contractility, temporary aggravation of symptoms of chronic heart failure, arrhythmias, increased peripheral circulation disorders (coldness of the lower extremities, Raynaud syndrome), myocardial conduction disorders; in isolated cases – AV-blockade, cardialgia.

Digestive system disorders: nausea, vomiting, abdominal pain, diarrhea, constipation, dry mouth, change in taste; increased activity of liver transaminases; rarely – hyperbilirubinemia.

Dermatological reactions: urticaria, skin itching, rash, exacerbation of psoriasis, psoriasis-like skin changes, skin hyperemia, exanthema, photodermatosis, increased sweating, reversible alopecia.

Respiratory system: nasal congestion, difficulty in exhaling (bronchospasm in high doses or in susceptible patients), shortness of breath.

Endocrine system disorders: hypoglycemia (in patients receiving insulin); rarely – hyperglycemia.

Hematopoietic system: thrombocytopenia, agranulocytosis, leukopenia.

Others: back or joint pain, slight increase in body weight, decreased libido and/or potency.

Overdose

Symptoms: pronounced sinus bradycardia, dizziness, nausea, vomiting, cyanosis, arterial hypotension, arrhythmia, ventricular extrasystole, bronchospasm, syncope; in acute overdose – cardiogenic shock, loss of consciousness, coma, AV-blockade up to development of complete transverse block and cardiac arrest, cardialgia.

The first signs of overdose appear 20 minutes to 2 hours after intake.

Treatment: gastric lavage, prescription of adsorbents, symptomatic therapy: in case of pronounced BP decrease – Trendelenburg position, in case of acute arterial hypotension, bradycardia and threatening heart failure – intravenous (at 2-5 min intervals) injection of beta-adrenostimulants or intravenous injection of 0.5-2 mg of atropine sulfate, in the absence of a positive effect – dopamine, dobutamine or norepinephrine.

As a follow-up, 1-10 mg of glucagon may be administered, and a transvenous intracardiac pacemaker may be placed. In bronchospasm – IV administration of beta2-adrenergic stimulants, in seizures – slow IV administration of diazepam. Metoprolol is poorly excreted by hemodialysis.

Similarities