Instructions for Egilok (Metoprolol) pills
Features
Minimum age from. 18 years
Method of use Oral
Pack quantity 30 pcs
Minimum storage temperature allowed, °C 15 °C
Maximum storage temperature allowed, °C 25 °C
Best before date 36M
Storage Conditions In a dry place
Release form Pill
Country of manufacture Hungary
Active substance Metoprolol
Scope Cardiology
Pharmacological group C07AB Selective beta1-adrenoblocators
Course duration 30 days
Registered as Medicinal agent
Application instructions:
Description
25 mg tablets: White or almost white, round, double-convex tablets with a cross-shaped dividing line and a double bevel (double snow shape) on one side and engraved with E 435 on the other, odorless.
Active substances
Metoprolol
Release form
Tablets
Composition
Each tablet contains 25 mg, 50 mg or 100 mg of the active substance methoprolol tartrate. The auxiliary substances: cellulose microcrystalline 41.5/83/166 mg, sodium carboxymethyl starch (type a) 7.5/15/30 mg, silicon dioxide colloidal anhydrous 2/4/8 mg, povidone (k-90) 2/4/8 mg, magnesium stearate 2/4/8 mg.
Pharmacological effect:
Antacid, neutralizes free hydrochloric acid in the stomach. Calcium is a macronutrient involved in the formation of bone tissue, In the process of blood clotting, it is necessary to maintain stable cardiac activity, the implementation of processes and the transmission of nerve impulses.
Pharmacokinetics:
The active ingredient Metoprolol is quickly and completely absorbed in the gastrointestinal tract.
The drug Egilok is characterized by linear pharmacokinetics in the therapeutic dose range.
The maximum concentration in the blood plasma is reached 1.5-2 hours after ingestion.
After suction, methoprolol is largely exposed to the metabolism of the initial passage through the liver. The bioavailability of methoprolol is about 50% at a single dose and about 70% at regular intake.
Taking tablets simultaneously with food can increase the bioavailability of metoprolol by thirty to forty%.
Methoprolol binds only slightly (~5-10%) to blood plasma proteins.
The distribution volume is 5.6 l/kg.
The active ingredient Metoprolol is metabolized in the liver by cytochrome R-450 isoenzymes. Metabolites do not have pharmacological activity.
The half-life (t1/2) averages 3.5 hours (1 to 9 hours). Total clearance is approximately 1 l/min.
Approximately 95% of the administered dose is excreted by the kidneys, 5% in the form of unchanged methoprolol. In some cases, this value can be as high as 30%.
No significant changes in the pharmacokinetics of methoprolol have been identified in older patients.
Kidney failure does not affect systemic bioavailability or the elimination of methoprolol. However, in these cases, there is a decrease in metabolite excretion. In severe renal failure (clubular filtration rate less than 5 ml/min), there is a significant accumulation of metabolites. However, this accumulation of metabolites does not increase the degree of beta-adrenergic blockade.
Liver dysfunction does not significantly affect the pharmacokinetics of methoprolol. However, under severe liver cirrhosis and after application of portocaval shunt, bioavailability may increase and general clearance from the body may decrease. After portocaval bypass treatment, the total clearance of the drug Egilok from the body is approximately 0.3 l/min, and the area under the concentration-time curve increases about 6 times compared to that of healthy volunteers.
Testimony:
- Arterial hypertension (in monotherapy or (if necessary) in combination with other hypotensive drugs Egilok), functional disorders of cardiac activity accompanied by tachycardia.
- Coronary heart disease: Myocardial infarction (secondary prevention - complex therapy), prevention of angina attacks.
- Disorders of the heart rhythm (najeludochkovaya tachykardia, gastric extracistolia).
- Hyperthyroidism (complex therapy).
- Prevention of migraine attacks.
Contraindications Egilok:
Increased sensitivity to Metoprolol or any other component of the drug Egilok, as well as other beta-adrenolocators, atrioventricular blockade (AV) II or III degree, synoatrial blockade, sinus bradycardia (CSU less than 50/min), sinus node weakness syndrome, cardiogenic shock, severe peripheral blood circulation disorders, heart failure in the stage of discompensation, age up to 18 years (due to lack of sufficient clinical data), simultaneous in/out administration of verapamil, severe form of bronchial asthma and pheochromocytoma without simultaneous application alpha-adrenoblators.
Due to insufficient clinical data, Egilok® is contraindicated in acute myocardial infarction, accompanied by a heart rate below 45 bpm, with a PQ interval above 240 ms, and systolic blood pressure below 100 mmHg.
Precautions:
Diabetes mellitus, metabolic acidosis, bronchial asthma, chronic obstructive pulmonary disease (COPD), renal/liver failure, myasthenia gravis, pheochromocytoma (when simultaneously used with alpha-adrenolocators), thyrotoxicosis, AV blockade I degree, depression (including anamnesis), psoriasis, obliterating diseases of peripheral vessels ("dislocating" chromosome, Reino syndrome), pregnancy, lactation period, old age, in patients with aggravated allergies mnezom (may decrease response when using adrenaline).
Use in pregnancy and breastfeeding
Use of the drug Egilok is not recommended during pregnancy. Use of the drug is possible only when the benefit to the mother exceeds the potential risk to the fetus. If the drug Egilok is necessary, care should be taken for the foetus and then for the newborn for several days (48 - 72 h) after delivery, as it is possible to develop bradycardia, respiratory depression, blood pressure reduction and hypoglycemia.
Method of administration, course and dosage of the drug:
individual.
For adults, use as an antacid a single dose of 0.5-1 g. For the prevention of osteoporosis daily dose of 0.6-1.2 g.
In children, for the prevention and treatment of rickets and caries, they are used in a daily dose of 300-600 mg.
Special patient groups:
If the kidney function is impaired, no change in the dosage regime is required.
In liver cirrhosis, a dose change is usually not required due to low binding of Metoprolol to blood plasma proteins (5-10%). In case of severe liver failure (e.g. after a portocaval bypass surgery), it may be necessary to reduce the dose of Egilok®.
In older patients, no dose correction is required.
Side Effects:
usually weak and reversible. The following side effects are reported in clinical trials and in the therapeutic use of methoprolol. In some cases, the link between the undesirable phenomenon and the use of the drug Egilok has not been reliably established.
Nosology (ICD codes)
E55.0
Rickets active
K02
Tooth decay
M80.0
Postmenopausal osteoporosis with pathological fracture
M80.1
Osteoporosis with pathological fracture after ovarian removal
M80.2
Osteoporosis with pathological fracture caused by immobility
M80.4
Drug osteoporosis with pathological fracture
M80.5
Idiopathic osteoporosis with pathological fracture
M80.8
Another osteoporosis with a pathological fracture
M81.0
Postmenopausal osteoporosis
M81.1
Osteoporosis after ovarian removal
M81.2
Osteoporosis caused by immobility
M81.4
Drug osteoporosis
M81.5
Idiopathic osteoporosis
M81.8
Other osteoporosis (senile osteopause)
M82
Osteoporosis in diseases classified in other rubrics
R10.1
Pains localized to upper abdomen
R12
Izzhoga
