Egilok Retard

The drug Egilok retard based on metoprolol is a selective β-adrenoreceptor blocker. The drug is actively used in diseases of the cardiovascular system.

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Indications Egilok Retard

The drug Egilok retard is prescribed in the following situations:

• with high blood pressure;
• to eliminate and relieve angina;
• in stable symptomatic chronic course of cardiac failure with systolic left ventricular disorder;
• to prevent cardiac arrest and recurrent infarction after the acute period of myocardial infarction;
• in case of cardiac arrhythmia, including supraventricular tachycardia, deterioration of ventricular function in atrial fibrillation and ventricular extrasystoles;
• to correct functional disorders of cardiac activity that occur against the background of a noticeable heartbeat;
• to prevent migraine attacks.

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Release form

The medical preparation Egilok retard is produced in the form of white oblong-convex tablets, film-coated, with a double-sided notch for dosing. The tablets have a prolonged effect.

One tablet of Egilok retard may contain 50 or 100 mg of the active ingredient metoprolol.

The cardboard box contains three blister plates with the drug, 10 tablets in one blister. Instructions for use of the drug are also included.

Pharmacodynamics

The active ingredient Egilok retard belongs to the group of β-adrenoblockers. The main effects of the drug are analgesic, antiarrhythmic and antihypertensive.

Metoprolol blocks the effect of the active sympathetic system on cardiac activity, normalizing the heart rate and the quality of cardiac output.

When blood pressure increases, the drug is able to lower its indicators. The long-term antihypertensive effect is explained by a decrease in total peripheral resistance.

With a single dose of the drug, the activity of plasma renin slows down. This may be due to the fact that β¹-receptors of the kidneys are suppressed, which, in turn, provokes a decrease in renin production and a decrease in vasoconstriction.

With increased blood pressure, long-term use of Egilok retard can lead to a clinically significant decrease in the weight of the left ventricle. Just like other drugs in this group, Egilok retard reduces the need for oxygen in the heart muscle by lowering systemic blood pressure and heart rate. At the same time, blood circulation and oxygen supply to the affected myocardial areas are improved. These properties reduce the likelihood of heart attacks and improve the performance of patients.

Compared with non-selective β-blockers, Egilok retard has a lesser effect on insulin production and carbohydrate metabolism processes. The drug does not significantly affect the reaction of the heart and blood vessels in response to hypoglycemic conditions and does not prolong the periods of hypoglycemic attacks.

Pharmacokinetics

The active ingredient of Egilok retard is largely (~95%) absorbed by the digestive system. However, after absorption, a significant portion of metabolic processes occurs in the liver. The bioavailability of the drug can be about 35%.

The drug is slowly distributed. Within 5 hours after taking Egilok retard, the slow absorption is transformed into a 6-hour plateau, and only after that the slow elimination stage begins. Usually, the half-life can be from 6 to 12 hours: the real half-life of the active component is about 3 hours. This difference is explained by the slow absorption of the drug.

The plasma level of the drug may fluctuate depending on individual characteristics.

Plasma protein binding can reach 10%.

The drug is excreted mainly by the kidneys (~95%). About 10% of the active ingredient is excreted unchanged.

The end products of metabolism do not play a clinically significant role and are excreted in the feces.

Dosing and administration

Egilok retard is usually taken in the morning, once a day, regardless of the time of food intake. In all cases, the amount of the drug taken is selected individually, with a gradual increase in dosage if necessary.

• In case of high blood pressure, the initial dosage is 50 mg/day, with a possible further increase to 100-200 mg. The maximum daily dose of the drug is 200 mg.
• For the treatment of angina, it is recommended to take 50 mg of the drug daily. If the therapeutic effect is insufficient, the dosage can be increased to 100-200 mg, or Egilok retard can be taken in combination with another similar drug.
• As a secondary preventive measure to prevent myocardial infarction, it is recommended to take 200 mg of the drug daily.
• In compensated cardiac insufficiency, treatment begins with 25 mg of Egilok retard daily. After 14 days, the dosage is increased to 50 mg, after another 14 days - to 100 mg, and again after 14 days - to 200 mg.
• For the treatment of arrhythmia, the dosage is determined individually, from 50 to 200 mg daily, in one dose.
• For hyperthyroidism, the standard dose also ranges from 50-200 mg daily.
• To prevent migraine attacks, Egilok retard is taken in quantities of 100 to 200 mg per day.

There is no need to adjust the dosage for elderly patients, patients with insufficient renal function, or persons undergoing hemodialysis.

In severe cases of liver failure, the daily dose of the drug should be reduced depending on the patient's condition.

Egilok retard tablets are taken whole, without crushing or chewing, with a sufficient amount of liquid. It is permissible to divide the tablet into two equal parts.

Use Egilok Retard during pregnancy

Unfortunately, no high-quality studies have been conducted on the use of Egilok retard by pregnant and lactating women. Due to the lack of reliable information on the safety of this drug, it is not recommended to take it during pregnancy and breastfeeding. Presumably, β-blockers can lead to a slowdown in the heart rate of the fetus and the child born.

If it is not possible to refuse taking Egilok retard, then treatment should be carried out under constant monitoring of the condition of the fetus, and then the newborn baby, since at birth such undesirable symptoms as respiratory depression, hypotension and hypoglycemia may develop.

The drug entering breast milk may not always provoke the development of undesirable manifestations in the infant. However, when prescribing Egilok retard to a nursing mother, it is necessary to exercise caution and monitor the baby in order to promptly respond to the possible development of unfavorable symptoms.

Contraindications

The antihypertensive drug Egilok retard is not used:

• if the patient is in a state of cardiogenic shock;
• in case of hypersensitivity to the composition of the drug;
• in case of atrioventricular block of the second or third degree;
• if the patient suffers from decompensated heart failure;
• in case of symptomatic bradycardia or significant decrease in blood pressure;
• in case of sinus node dysfunction syndrome;
• in disorders of peripheral circulation, mainly in arterial vessels;
• if the patient is suspected of having acute myocardial infarction and the heart rate is less than 45 beats/min, or the systolic pressure is less than 100 mmHg;
• with metabolic acidosis;
• if the patient is diagnosed with untreated pheochromocytoma;
• if the patient is undergoing concomitant treatment with MAO-A inhibitor drugs;
• in complicated cases of bronchial asthma or pulmonary obstruction;
• if the patient is receiving intravenous infusions of calcium antagonists (verapamil, diltiazem) or other antiarrhythmic drugs (disopyramide).

Side effects Egilok Retard

In most patients, taking Egilok retard does not cause side effects. However, in some cases, the following undesirable symptoms may occur:

• slowing of the heart, cold extremities, relapse of Raynaud's syndrome, signs of first-degree atrioventricular block, swelling, pain in the heart, abnormal heart rhythms, decreased blood pressure, orthostatic drop in pressure with impaired consciousness;
• decreased levels of platelets and leukocytes in the blood;
• feeling of fatigue, headache, dizziness, numbness of the limbs, cramps;
• blurred vision, redness and irritation of the eyes, impaired hearing, taste changes, conjunctivitis;
• shortness of breath, bronchospasm;
• nausea, epigastric pain, dyspepsia, flatulence, thirst;
• allergies, skin rash, increased sweating, relapse of psoriasis, skin dystrophy, alopecia;
• myasthenia;
• weight gain, lipid metabolism disorder, manifestation of latent diabetes mellitus;
• hepatitis, deterioration of liver function;
• depressive states, hallucinations, sleep disorders, libido disorders, memory disorders.

There are isolated reports of cases of impotence and second- and third-degree atrioventricular block, as well as the appearance of antinuclear antibodies (which does not indicate the presence of systemic lupus erythematosus).

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Overdose

Signs of an overdose include:

• significant decrease in blood pressure;
• severe sinus bradycardia;
• attacks of nausea and vomiting;
• dizziness, fainting;
• heart rhythm disturbances;
• bronchospasm phenomena;
• cardiogenic shock, comatose state, atrioventricular block, heart pain.

As a rule, the first signs of excess Egilok retard in the body are observed within 20-120 minutes after taking the tablets.

The above symptoms may be aggravated by the use of alcoholic beverages, sleeping pills, antihypertensive drugs, and quinidine.

Treatment of this condition is carried out sequentially and in stages:

• intensive care measures;
• control over blood circulation, respiratory function, the functioning of the urinary system, the quality of electrolyte metabolism and the glucose content in the blood.

In case of a sharp or significant decrease in blood pressure, the patient is placed in a lying position at an angle of 45° with the pelvis raised relative to the head. In a critical situation - with a slowing heart rate and an increased risk of cardiac insufficiency - the patient is given β-adrenergic stimulants at intervals of 2 to 5 minutes, or 0.5 to 2 mg of atropine sulfate is administered intravenously. If the desired effect is absent, then norepinephrine, dopamine or dobutamine are administered, followed by glucagon (1-10 mg) and the installation of an intravenous infusion set.

Bronchospasm is eliminated by intravenous injections of β²-adrenergic receptor stimulating drugs.

It is important to know that the active ingredient of the drug Egilok retard – metoprolol – is poorly amenable to hemodialysis.

Interactions with other drugs

Egilok retard can be successfully combined with other antihypertensive medications. In order to prevent severe hypotension due to such a combination, patients' blood pressure should be constantly monitored.

Egilok retard should not be combined with the following medications:

• calcium channel blockers, verapamil;
• MAO inhibitor drugs.

The following combinations of Egilok retard are prescribed with caution:

• with antiarrhythmic drugs for internal use, parasympathomimetics;
• with digitalis preparations - due to the risk of cardiac conduction disturbances;
• with nitrates – due to the possibility of developing hypotension and bradycardia;
• with sleeping pills, tranquilizers, antidepressants, neuroleptics - due to the risk of lowering blood pressure;
• with narcotic drugs - due to the risk of suppression of cardiac function;
• with sympathomimetics - due to the increased risk of cardiac arrest;
• with clonidine – due to the risk of developing a hypertensive crisis;
• with ergotamine – due to increased vasoconstrictor effect;
• with β²-sympathomimetics (are antagonists);
• with NSAIDs and estrogens – due to a decrease in the antihypertensive effect;
• with insulin and antidiabetic agents - due to possible increased hypoglycemic effect;
• with curare-like muscle relaxants - due to increased muscle-nerve blockade;
• with enzyme inhibitors and inducers – due to the possible enhancement or, conversely, decrease in the effect of metoprolol.

Storage conditions

Egilok retard is stored at normal temperature, with a maximum permissible temperature of +30°C. Children's access to storage areas for medical preparations should be restricted.

Shelf life

Egilok retard can be stored for up to 5 years.