"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 physician, 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 beta1-adrenergic receptors, blocking them, which leads to a series of changes in the functioning of organs and blood vessels. The medicinal substance metoprolol tartrate helps lower blood pressure, dilates the blood vessels of the heart, providing 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 heartthe muscle needs less oxygen. Consequently, in patients with angina pectoris, the ability to carry out a large load is increased and the frequency of angina attacks is reduced.
During stressful situations and physical activity 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 rhythm disturbances and tachycardia accompanying hyperthyroidism, the drug brings the frequency back to normal.
Influence on the sinus node leads to the restoration of rhythm and slowing down the conduction of the impulse 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 sugar, fatty acids and high-density lipoproteins.
Absorption and excretion
The drug undergoes the main series of chemical transformations with the help of liver enzymes, according to the instructions for use of Metoprolol. According to reviews of specialists who monitor patients who suffer from serious liver problems (severe cirrhosis), after taking the drug, its bioavailability may change towards an increase and an increase in the number of side effects.
Maximum concentration, almost completely absorbed from the digestive system, the drug reaches in two hours. The drug has a good ability to distribute and accumulate in tissues. It disappears from the plasma in an average of 3.5 hours, excreted by the kidneys. In severe diseases of these organs, secondary metabolic products accumulate in the body, which does not lead to an increase in the effect of the drug.
Diseases for which the drug is taken
What is Metoprolol for:
- Arterial hypertension of all degrees in monotherapy and as part of complex treatment.
- Angina, 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 recurrent conditions and reduce mortality from it.
- Chronic heart failure in a stable phase in combination with other cardiological agents.
- Irregular heart rhythm (supraventricular tachycardia, ventricular premature beats, atrial fibrillation).
- Functional tachycardia.
- Prophylactic use as an anti-migraine agent.
- Suppression of tachycardia in hyperthyroidism.
Metoprolol should be used according to the instructions and according to the appointment of a specialist.
Dosing regimen
Doctors should use an individual approach to prescribing the drug, which depends on the disease. According to the reviews on the instructions for Metoprolol, patients would like a more detailed dosing regimen for this drug.
In case of 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. Dosage may be increased to 100 mg twice (200 mg total) or an additional blood pressure lowering agent may be used.
For the treatment of angina, take 25-50 mg up to three times a day under the control of the frequency of ventricular contraction. The dose may be increased to 200 mg during the day, or an additional drug for the treatment of angina pectoris is added.
For the prevention of a recurrent heart attack, up to one hundred milligrams are prescribed during the day in two doses.
In arrhythmic pathologies, the drug is indicated at a dose of 25-50 mg up to three times a day. If it is not effective enough, there is the possibility of increasing to 200 mg per day or adding another antiarrhythmic agent.
For functional tachycardia, take 50 to 100 mg per day.
For the prevention of migraine attacks, take 50 mg twice a day. Dose may be increased 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 (400mg per day).
Instructions for "Metoprolol" stipulate taking the medicine during or after a meal with enough water. Patients should be taught to count the minute number of heartbeats, which should not be less than 60 beats. The duration of admission is individual and should be monitored by a doctor. Withdrawal of the drug should be carried out very slowly to avoid a jump in blood pressure.
Contraindications to the use of "Metoprolol"
You can not prescribe the drug in cases of previously known cases of individual sensitivity to this group of substances, metoprolol tartrate itself or auxiliary components of the drug, including lactase deficiency.
Violations of the conduction of the heart in the form of atrioventricular blockade of the second and third degree do not allow the use of "Metoprolol" in the treatment. Other contraindications are sick sinus syndrome and bradycardia with a slow heart rate of less than 50 beats per minute.
Decompensated heart failure, accompanied by pulmonary edema, low blood pressure and impaired peripheral circulation, makes it impossible to take this medicine.
Prinzmetal's Angina is a contraindication to Metoprolol due to possible prolongation of its attacks.
It is undesirable to take the drug in the presence of systolic blood pressure below 90 mm Hg. st.
Metabolic acidosis, accompanied by a decrease in blood pH, -contraindication to taking medication.
Severe bronchial asthma and obstructive bronchitis are conditions in which Metoprolol is contraindicated.
Do not take with MAO inhibitors (except MAO-B).
Peripheral circulatory disorders complicated by gangrenous lesions or the threat of its development.
Not tested in persons under 18 years of age, therefore not suitable for children.
Contraindicated in the establishment or suspicion of an acute stage of myocardial infarction with severe bradycardia (up to 45 beats per minute), low blood pressure and prolongation of the P-Q interval.
Cardioselective beta1-blockers are a serious group of medicines widely used in medical practice. Therefore, contraindications must be taken into account before prescribing the drug.
Use of medication 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, getting through the placenta, as it impairs its blood supply. This can lead to growth and developmental delay, premature birth or fetal death.
Three days before the date of delivery, the use of the medication must be stopped, as there is a risk of bradycardia, a drop in pressure and blood sugar, an increase in bilirubin, and also a cessation of respiratory activity in the child. For newborns whose mothers took"Metoprolol" during gestation, should be closely monitored for three days after birth.
The drug can pass into breast milk, therefore, when using this drug, you should refrain from feeding or change the drug. If the mother continues to breastfeed while taking this medication, the baby should be monitored for bradycardia, low blood pressure, and low blood sugar.
Side effects
Having studied the contraindications, the side effects of Metoprolol also need to be paid attention to:
- Cardiovascular adverse effects: slow heart rate less than 60 beats per minute, increase - more than 90 beats, lower blood pressure (more than 10%); exacerbation of heart failure, atrioventricular blockade of the first degree, pain in the projection of the heart, the development of a shock state in the acute period of a heart attack, coldness of the distal extremities (1-9, 99%); functional disturbances of rhythm and conduction of the heart (0.1-0.99%), necrotic injuries of the limbs (up to 0.0099%).
- The nervous system and sense organs may respond to the drug with fatigue (more than 10%); dizziness, imbalance, headache (1-9, 99%); paresthesias on the skin, depressive symptoms, sleep disturbance or hypersomnia, nightmares (0.1-0.99%); visual impairment, inflammation of the conjunctiva, dry eyes, nervous strain (0.099-0.0099%); memory impairment, 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 mucous membranes (0.099-0.0099%).
- Effects on the part of the digestive system and liver: nausea, abdominal pain, stool disorders (1-9, 99%); vomiting (0.1-0.99%); dryness of the mucous membranes of the 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 react with a decrease in 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, photosensitivity, psoriasis (up to 0.0099%).
- Endocrine side effects: weight gain (0.1-0.99%); exacerbation of previously hidden diabetes (0.099-0.0099%).
- Kidneys and 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 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.
Used with caution in asthmatics due to the negative effect of this group of substances on bronchial tissue.
Patients with diabetes mellitus should have their blood glucose monitored more frequently due to possible lowering bydrug.
In persons suffering from psoriasis, the course of the disease may worsen, since Metoprolol can lead to increased formation of epidermal scales.
For adrenal tumors, the drug should be combined with an alpha-adrenergic agent.
Before administering anesthesia, you should tell your doctor about taking the medicine to avoid the risk of a pronounced decrease in blood pressure.
In the elderly, the drug should be started at low dosages, with caution and under the supervision of a specialist.
Contact lens wearers should be aware of the potential for dry eyes from this drug.
Interactions with other drugs
The drug is capable of serious drug interactions, so taking some other drugs is a contraindication. Metoprolol should not be taken together:
- With barbiturates, so they increase its effect on the liver.
- "Verapamil", as the risk of hypotension and bradycardia is significantly increased, as well as a high probability of sick sinus syndrome.
- "Propafenone", since the action of "Metoprolol" in this combination can increase five times, which leads to a significant risk of side effects.
Dose adjustment often needed when co-administered:
- With Amiodarone (due to severe bradycardia).
- First-class antiarrhythmics that can reduce myocardial contractility.
- Non-steroidal anti-inflammatory drugs, as they can weaken the action of Metoprolol in lowering blood pressure.
- "Diltiazem" (due to the possibility of a blockade).
- "Diphenhydramine" (due to the increased action of "Metoprolol").
- "Epinephrine" (due to increased blood pressure and severe bradycardia).
- There is a risk of increased heart pressure with norephedrine.
- "Quinidine", which can enhance the blocking ability of "Metoprolol".
- "Clonidine" (due to severe withdrawal reactions associated with increased blood pressure).
- "Rifampicin", which is able to reduce the concentration of "Metoprolol" in plasma.
- Cardiac glycosides, which can cause bradycardia.
- Drugs that reduce the concentration of the substance CYP2D6 (metoprolol substrate), as they can reduce its amount in the blood (Terbinafine, Paroxetine, Sertraline, Fluoxetine, Celecoxib).
Analogues and prices
Analogues of "Metoprolol" (the instructions should always be studied before using any drugs) can only be prescribed by a doctor.
Analogues of the drug are:
- "Betaloc" company AB "AstraZeneca", made in Sweden. The cost of the medicine is from 122 to 973 rubles.
- Betaloc Zok by the Swedish manufacturer AB AstraZeneca worth from 122 to 491 rubles.
- "Egilok" produced at the pharmaceutical plant of CJSC "Egis", in Hungary, costing from 67 to 343 rubles per pack.
- "Egilok Retard" of the plant CJSC "Egis", price - from 81 to 230rubles.
- "Metoprolol-Akri" produced in the Russian Federation, plant JSC "Akrikhin HPC". 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" of the 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 get the opinions of specialists and patients who were prescribed the drug.
"Metoprolol" and analogues reviews from doctors are mostly positive because of the effectiveness and broad profile. However, one must be very careful not to harm patients, considering contraindications and drug interactions.
Patients who used "Metoprolol" according to the instructions for use, reviews of this drug can leave objective. A positive opinion about him was, according to statistics, from 82 to 100 percent of people. 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 drug prescribed by a doctor.
Now you know all the information about the drug "Metoprolol": indications for use,contraindications, composition and dosage.
