Egilok Retard

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

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Indications Egilok Retard

The drug Egilok retard is assigned in the following situations:

• with high blood pressure;
• to eliminate and relieve angina pectoris;
• with a stable symptomatic chronic course of cardiac insufficiency with systolic left ventricular dysfunction;
• to prevent cardiac arrest and recurrent infarct after an acute period of myocardial infarction;
• with cardiac rhythm failures, including supraventricular tachycardia, worsening of ventricular function in atrial fibrillation and ventricular extrasystoles;
• for the correction of functional disorders of cardiac activity, which occur against a background of palpable palpitation;
• 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 covered with a filmy membrane, with a double-sided incision for dosing. Tablets have a prolonged effect.

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

The cardboard box contains three blister plates with a preparation, 10 pieces each. Tablets in one blister. In addition, an instruction on the use of the drug is attached.

Pharmacodynamics

The active ingredient of retard EGs 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.

With increasing blood pressure, the drug is able to lower its indices. The prolonged antihypertensive effect is explained by the decrease in the total peripheral resistance.

With a single admission, the activity of plasma renin is slowed down. This may be due to the fact that there is an inhibition of β1-receptors of the kidneys, which, in turn, provokes a decrease in the production of renin and a decrease in vasoconstriction.

With increasing blood pressure, a prolonged use of retard Egiloc 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 cardiac muscle in oxygen, by lowering systemic blood pressure and heart rate. At the same time, blood circulation and oxygen supply to the affected myocardial areas improve. These properties can reduce the likelihood of developing heart attacks and improve the performance of patients.

Compared with non-selective β-blockers, Egilok retard has less effect on insulin production and the processes of carbohydrate metabolism. The drug has no significant effect on the response 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 the Egilok retard preparation is absorbed to a large degree (~ 95%) by the digestive system. However, after absorption, a significant proportion of metabolic processes occur in the liver. Biological availability of drug substance can be about 35%.

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

The level of the drug in the plasma can fluctuate, which depends on the individual characteristics.

The connection with plasma proteins can reach 10%.

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

The final products of metabolism do not play a clinically significant role and are excreted with caloric masses.

Dosing and administration

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

• With an increase in blood pressure, the initial dosage is 50 mg / day, with a possible further increase to 100-200 mg. The maximum daily amount of the drug is 200 mg.
• For the treatment of angina pectoris, it is recommended to take 50 mg of the drug daily. If the treatment effect is insufficient, the dosage can be increased to 100-200 mg, or take Egilok retard in combination with another similar drug.
• As a secondary prophylactic for the prevention of myocardial infarction, it is recommended to take 200 mg of the drug daily.
• With compensated cardiac failure, treatment starts with 25 mg of Egilok retard daily. After 14 days, the dosage is increased to 50 mg, after 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, at one time.
• With increased thyroid function, the standard dose also varies between 50-200 mg daily.
• To prevent migraine attacks Egilok retard taken in an amount of 100 to 200 mg per day.

Elderly patients, patients with insufficient renal function, those who are on hemodialysis adjust the dosage is not necessary.

In severe hepatic insufficiency, the daily amount of the drug should be reduced depending on the patient's condition.

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

Use Egilok Retard during pregnancy

Unfortunately, qualitative studies on the use of Egilok retard with pregnant and lactating women were not carried out. Because of 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 slowing of the heart rhythm in the fetus and the child born.

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

Entering the drug in breast milk can not always provoke the development of unwanted manifestations in an infant. However, appointing Egilok retard nursing mother, you must be careful and monitor the baby, in a timely manner to respond to the possible development of adverse symptoms.

Contraindications

Antihypertensive drug Egilok retard not used:

• if the patient is in a state of cardiogenic shock;
• with hypersensitivity to the composition of the drug;
• with atrioventricular blockade of the second or third degree;
• if the patient suffers from decompensated heart failure;
• with symptomatic bradycardia or significant lowering of blood pressure;
• with syndrome of sinus node dysfunction;
• in disorders of peripheral circulation, mainly in arterial vessels;
• if the patient is suspected of acute myocardial infarction, and the heart rate is less than 45 bpm, or a systolic pressure less than 100 mm Hg. P.
• metabolic acidosis;
• if the patient has an untreated pheochromocytoma;
• if the patient undergoes simultaneous treatment with MAO-A inhibitor drugs;
• with complicated course of bronchial asthma, or with obstruction of the lungs;
• if the patient is given an intravenous infusion of calcium antagonist drugs (verapamil, diltiazem) or other antiarrhythmic drugs (disopyramide).

Side effects Egilok Retard

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

• slowing of cardiac activity, cooling of extremities, relapse of Raynaud's syndrome, signs of atrioventricular blockade of the first degree, puffiness, heart pain, heart rhythm disturbances, lowering of blood pressure, orthostatic pressure drop with violation of consciousness;
• reduction of platelets and white blood cells in the blood;
• sensation of fatigue, pain in the head, dizziness, numbness of the limbs, convulsions;
• visual impairment, redness and irritation of the eyes, deterioration of hearing, taste change, conjunctivitis;
• shortness of breath, bronchospasm;
• nausea, epigastric pain, indigestion, flatulence, thirst;
• allergy, skin rash, increased sweating, relapse of psoriasis, skin dystrophy, allopecia;
• myasthenia gravis;
• weight gain, lipid metabolism disorder, manifestation of latent diabetes mellitus;
• hepatitis, worsening of hepatic function;
• Depressive conditions, hallucinations, sleep disturbances, violation of libido, memory disorders.

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

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Overdose

The signs of overdose are:

• significant lowering of blood pressure;
• sinus bradycardia with severe course;
• attacks of nausea and vomiting;
• dizziness, fainting;
• heart rhythm disturbances;
• phenomena of bronchospasm;
• cardiogenic shock, coma, AV blockade, pain in the heart.

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

The above signs can worsen after drinking alcoholic drugs, hypnotics and antihypertensive drugs, quinidine.

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

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

With a sharp or significant decrease in blood pressure, the patient is transferred to a reclining position at an angle of 45 ° with a basin raised in relation to the head. In a critical situation - with a slowing of the heart rate and an increased risk of cardiac insufficiency - the patient is administered β-adrenostimulants with an interval of 2 to 5 minutes, or intravenously from 0.5 to 2 mg of atropine sulfate. If the desired effect is absent, then resort to the introduction of noradrenaline, dopamine or dobutamine, followed by the appointment of glucagon (1-10 mg) and the installation of IV.

Bronchospasm is eliminated by intravenous injections of β2-adrenoreceptor stimulant preparations.

It is important to know that the active ingredient of the drug Egilok retard - metoprolol - does not lend itself to hemodialysis.

Interactions with other drugs

Egilok retard can be successfully combined with other antihypertensive medications. In order to prevent severe hypotension due to this combination, you should constantly monitor the patient's blood pressure.

 Egilok retard is inadmissible to combine with such medicines:

• calcium channel blockers, verapamil;
• drugs-MAO inhibitors.

 With caution appoint such combinations of Egilok retard:

• with antiarrhythmic drugs of internal use, parasympathomimetics;
• with foxglove preparations - because of the risk of cardiac conduction disorder;
• with nitrates - because of the possibility of developing hypotension and bradycardia;
• with hypnotics, tranquilizers, antidepressants, neuroleptics - because of the risk of lowering blood pressure;
• with narcotic drugs - because of the risk of oppression of cardiac function;
• with sympathomimetics - because of increased probability of cardiac arrest;
• with clonidine - because of the danger of developing a hypertensive crisis;
• with ergotamine - due to increased vasoconstrictor action;
• with β²-sympathomimetics (are antagonists);
• with NSAIDs and estrogens - due to lowering of antihypertensive action;
• with insulin and antidiabetics - because of the possible increase in hypoglycemic effects;
• with curare-like muscle relaxants - due to increased musculoskeletal blockade;
• with inhibitors and inducers of enzymes - because of the possible amplification or, conversely, a decrease in the action of metoprolol. 

Storage conditions

Egilok retard is stored at ordinary temperature, with an allowable maximum value of + 30 ° C. Children should be restricted to the storage of medicinal products.

Shelf life

Egilok retard can be stored for up to 5 years.