"Metoprolol" is regularly used by cardiologists and therapists in the practice of treating arterial hypertension and coronary heart disease. The drug successfully fights diseases, but should be taken under the supervision of a doctor, according to the instructions for use. "Metoprolol" and analogues, according to experts and patients, are effective drugs.
Pharmacological action of the drug
"Metoprolol" has the ability to act on beta 1 -adrenoreceptors, blocking them, which leads to a series of changes in the functioning of organs and blood vessels. The medicinal substance metoprolol tartrate helps to lower blood pressure, dilates the blood vessels of the heart, has an antianginal effect, and has an antiarrhythmic effect.
The drug slows down the heart rate and the force of contraction of the heart, which leads to the fact that the heart muscle needs less oxygen. Therefore, in patients with angina pectoris, the ability to perform a large load increases and the frequency of angina attacks decreases.
During stressful situations and physical stress in the blood of people, the amount of adrenal hormones increases, which lead to increased heart rate and increased blood pressure, and Metoprolol (contraindications are described below) reduces this effect on the cardiovascular system. With arrhythmias and tachycardia accompanying hyperthyroidism, the drug brings the frequency back to normal.
The effect on the sinus node leads to a restoration of the rhythm and a slowdown in the conductivity of the pulse between the atria and ventricles. Acting on the vessels of the brain, it fights headaches.
The drug is able to some extent affect carbohydrate and fat metabolism, increasing the number of triglycerides in the bloodstream, reducing the rate of sugar, fatty acids and high density lipoproteins.
Suction and removal
The drug undergoes the main series of chemical transformations using hepatic enzymes, according to the instructions for use of Metoprolol. According to experts who monitor patients who suffer from serious liver problems (severe cirrhosis), after taking the drug, its bioavailability may increase and increase the number of side effects.
The maximum concentration, almost completely absorbed from the digestive system, the drug reaches after two hours. The medicine has a good ability to distribute and accumulate in the tissues. From the plasma, it disappears in an average indicator of 3.5 hours, excreted by the kidneys. In severe diseases of these organs, an accumulation of secondary metabolic products in the body occurs, which does not lead to an increase in the action of the drug.
Diseases in which the drug is taken
What is Metoprolol for?
- Arterial hypertension of all degrees in monotherapy and as part of complex treatment.
- Angina pectoris, characterized by spastic processes in the vessels of the heart, leading to pain and lack of oxygen supply to the heart muscle.
- Condition after myocardial infarction (after the acute phase) to prevent recurrence and reduce mortality from it.
- Chronic heart failure in a stable phase in combination with other cardiological agents.
- Heart rhythm disturbance (supraventricular tachycardia, ventricular extrasystole, atrial fibrillation).
- Functional tachycardia.
- Prophylactic use as an anti-migraine agent.
- Stopping tachycardia with hyperthyroidism.
Metoprolol should be used according to the instructions and according to the appointment of a specialist.
Dosage regimen
Doctors should use an individual approach to the prescription of the drug, which depends on the disease. According to the reviews following the instructions for Metoprolol, patients would like a more detailed dosing schedule for this drug.
With hypertension of the first and second degree (systolic pressure - up to 160 mm Hg. Art.), You should start with 25-50 mg of the drug twice a day with an interval of 12 hours. The dosage can be increased to 100 mg twice (200 mg in total) or use an additional tool to reduce pressure.
For the treatment of angina pectoris, take 25-50 mg up to three times a day under the control of the frequency of ventricular contraction. The dose can be increased to 200 mg during the day, or an additional drug is added to treat angina pectoris.
To prevent re-infarction, up to one hundred milligrams is prescribed during the day in two divided doses.
With arrhythmic pathologies, the drug is indicated in a dose of 25-50 mg up to three times during the day. With insufficient effectiveness, there is the possibility of increasing to 200 mg per day or the addition of another antiarrhythmic agent.
With functional tachycardia take from 50 to 100 mg per day.
To prevent migraine attacks, take 50 mg twice a day. It is possible to increase the dose to 100 mg twice a day.
Patients suffering from tachycardia, with an increased content of thyroid hormones in the blood, are prescribed 50 mg up to four times a day under the control of the frequency of contractions of the heart muscle. Three days after treatment, the dosage can be increased to 100 mg 3-4 times a day, which will be equal to the maximum daily dose of Metoprolol (400 mg per day).
Instructions for “Metoprolol” stipulate medication during or after meals with enough water. Patients should be trained in the calculation of the minute number of heart contractions, which should not be less than 60 beats. The duration of admission is individual and should be monitored by a doctor. Drug withdrawal should be carried out very slowly in order to avoid a jump in blood pressure.
Contraindications to the use of "Metoprolol"
You can not prescribe the drug in previously known cases of individual sensitivity to this group of substances, metoprolol tartrate itself or auxiliary components of the drug, including with lactase deficiency.
Violations of the conduction of the heart in the form of atrioventricular block of the second and third degree do not allow to use Metoprolol in the treatment. Contraindications are also sick sinus syndrome and bradycardia with a slowdown in heart rate of less than 50 beats per minute.
Decompensated heart failure, accompanied by pulmonary edema, decreased blood pressure and impaired peripheral circulation, makes it impossible to take this medication.
Prinzmetal angina is a contraindication to the appointment of "Metoprolol" due to the possible lengthening of its attacks.
It is undesirable to take the drug in the presence of systolic blood pressure below 90 mm Hg. Art.
Metabolic acidosis, accompanied by a decrease in blood pH, is a contraindication to taking the medication.
Severe course of bronchial asthma and obstructive bronchitis are conditions in which Metoprolol is contraindicated.
It cannot be taken together with MAO inhibitors (except for MAO-B).
Peripheral circulatory disorders complicated by gangrenous lesions or a threat to their development.
It has not been tested on persons under 18 years of age, therefore, medicine is not prescribed for children.
Contraindicated in the establishment or suspicion of an acute stage of a heart attack with severe bradycardia (up to 45 beats per minute), low pressure and prolongation of the P – Q interval.
Cardioselective beta 1- blockers are a serious group of drugs widely used in medical practice. Therefore, contraindications must be taken into account before prescribing the drug.
The use of the drug during pregnancy and lactation
Pregnancy is not an absolute contraindication. "Metoprolol" can be prescribed in the case when the positive effect of the drug prevails over the possible negative consequences for the unborn child. The drug can harm the fetus by passing through the placenta, as it impairs its blood supply. This can lead to stunted growth and development, cause premature birth or fetal death.
Three days before the date of birth, the use of the medication must be stopped, since there is a risk of bradycardia, a drop in pressure and blood sugar, an increase in bilirubin, as well as the cessation of respiratory activity in the child. Newborns whose mothers took Metoprolol during gestation should be closely monitored for three days after delivery.
The drug is able to pass into breast milk, so when using this medication, you should refrain from feeding or replace the drug. If the mother continues to feed while taking this medication, the child should be examined for the development of bradycardia, lowering blood pressure and blood sugar.
Side effects
Having studied contraindications, side effects of Metoprolol also need to be paid attention to:
- Undesirable cardiovascular effects: slowing the heart rate of less than 60 per minute, increased frequency - more than 90 strokes, decreased blood pressure (more than 10%); exacerbation of heart failure, atrioventricular block of the first degree, pain in the projection of the heart, the development of a shock state in the acute period of heart attack, cooling of the distal extremities (1-9.99%); functional disorders of the rhythm and conduction of the heart (0.1-0.99%), necrotic damage to the limbs (up to 0.0099%).
- The nervous system and sensory organs may respond to the drug fatigue (more than 10%); dizziness, imbalance, headache (1-9.99%); paresthesias on the skin, depressive symptoms, impaired falling asleep or hypersomnia, nightmares (0.1-0.99%); visual impairment, conjunctival inflammation, dry eyes, nervous strain (0.099-0.0099%); violation of the processes of memorization, hallucinations, mood swings, confusion, hearing loss and tinnitus (up to 0.0099%).
- Respiratory organs can worsen their work due to shortness of breath (1-9.99%); bronchospasm (0.1-0.99%); catarrhal manifestations of the mucous membranes (0.099-0.0099%).
- Effects from the digestive system and liver: nausea, abdominal pain, stool disorders (1-9,99%); vomiting (0.1-0.99%); dry mouth, increased liver enzymes in the blood (0.099-0.0099%); taste disturbance, inflammation of the liver tissue (up to 0.0099%).
- Blood and lymph can respond by lowering white blood cells and platelets (up to 0.0099%).
- Skin, muscles and bones react negatively to the drug in the form of: urticaria, sweating, muscle cramps, edema (0.1-0.99%); alopecia (0.099-0.0099%); joint pain, muscle weakness, photosensitization, scaly lichen (up to 0.0099%).
- Endocrine side effects: weight gain (0.1-0.99%); exacerbation of previously hidden diabetes (0,099-0,0099%).
- The kidneys and the reproductive system suffer in the form of: impotence, Peyronie’s disease — fibrous curvature of the penis (0.099-0.0099%).
special instructions
Given the ability to act on the nervous system and sensory organs of the drug "Metoprolol", the indications and contraindications of which we have already considered, the possibility of driving a car and working in dangerous and harmful conditions should be decided individually in each case.
It is used with caution in asthmatics due to the negative effect of this group of substances on bronchial tissue.
Patients with diabetes should often monitor blood glucose due to its possible decrease under the influence of the drug.
In patients with psoriasis, the course of the disease may worsen, since Metoprolol can lead to increased formation of epidermal flakes.
In adrenal tumors, the drug should be combined with an alpha-adrenolytic substance.
Before conducting anesthesia, the doctor should be informed about taking the medicine to avoid the risk of a marked decrease in blood pressure.
For older people, medication should be started with low dosages, with caution and under the supervision of a specialist.
Persons using contact lenses should be aware of possible dry eyes from this drug.
Interactions with other medicinal substances
A medication is able to enter into serious drug interactions, so taking some other drugs is a contraindication. Metoprolol should not be taken together:
- With barbiturates, so they enhance its effect on the liver.
- “Verapamil”, since the risk of hypotension and bradycardia is significantly increased, and the likelihood of a sick sinus syndrome is also high.
- "Propafenone", since the effect of "Metoprolol" in this combination can be increased by five times, which leads to a significant risk of side effects.
Dose adjustment is often necessary when taken together:
- With Amiodarone (due to severe bradycardia).
- First-class antiarrhythmics, which can reduce myocardial contractility.
- Non-steroidal anti-inflammatory drugs, as they can weaken the effect of Metoprolol in lowering blood pressure.
- "Diltiazem" (due to the possibility of developing a blockade).
- "Diphenhydramine" (due to the increased action of "Metoprolol").
- "Epinephrine" (due to increased blood pressure and severe bradycardia).
- With drugs with norephedrine, there is a risk of increased heart pressure.
- "Quinidine", which can enhance the blocking ability of "Metoprolol."
- “Clonidine” (due to strong withdrawal reactions associated with increased blood pressure).
- "Rifampicin", which is able to reduce the concentration of "Metoprolol" in plasma.
- Cardiac glycosides that can cause bradycardia.
- Drugs that reduce the concentration of the substance CYP2D6 (Metoprolol substrate), since they can reduce its amount in the blood (Terbinafine, Paroxetine, Sertraline, Fluoxetine, Celecoxib).
Analogs and prices
Analogues of Metoprolol (the instructions should always be studied before using any drugs) can only be prescribed by a doctor.
The analogues of the drug are:
- Betalok of the company AB AstraZeneca, manufactured in Sweden. The cost of the medicine is from 122 to 973 rubles.
- Betalok Zok, a Swedish manufacturer of JSB AstraZeneca, costing from 122 to 491 rubles.
- Egilok, manufactured at the pharmaceutical factory of Egis CJSC in Hungary, costing from 67 to 343 rubles per package.
- "Egilok Retard" plant of JSC "Egis", the price is from 81 to 230 rubles.
- "Metoprolol-Acre" produced by the Russian Federation, the plant of JSC "Akrikhin HFK." The price varies from 39 to 853 rubles.
- Metoprolol-Ratiopharm (costs from 28 to 3150 rubles) of the German company Ratiopharm.
- "Metoprolol Zentiva" of the Czech company "Zentiva" for 125 rubles.
- "Metoprolol-Teva" pharmaceutical company "Teva" from Israel. The cost of the drug ranges from 19 to 142 rubles.
Price fluctuations depend on the dosage of the drug (25, 50, 100 mg) and the number of tablets in the package.
Reviews on the use of Metoprolol
In order to objectively evaluate this drug, it is necessary to find out the opinions of specialists and patients who were prescribed the medication.
"Metoprolol" and analogues reviews from doctors are mostly positive because of their effectiveness and wide profile. However, you should be very careful so as not to harm patients, given contraindications and drug interactions.
Patients who have used Metoprolol according to the instructions for use, reviews about this drug may leave objective. According to statistics, 82 to 100 percent of people made up a positive opinion of him. Reviews about "Metoprolol" are not indicated in the instructions. But they should be taken into account by a patient who doubts or is afraid to take this medication prescribed by a doctor.
Now you know all the information about Metoprolol: indications for use, contraindications, composition and dosage.