Pharmacodynamics and pharmacokinetics
The active ingredient Betaloc reduces or eliminates the stimulating effect of catecholamines during stress and exercise, reduces myocardial and cardiac output, reduces high blood pressure and heart rate. In addition, metoprolol reduces myocardial oxygen demand and prolongs diastole .
The drug may slightly increase TG levels and also slightly reduce HDL fractions and free fatty acid levels in the blood plasma.
The tablets are characterized by a delayed release of the active substance, so the concentration of the drug in the blood plasma remains unchanged, which ensures a stable clinical effect for a day or more. The drug is better tolerated than its analogues, and the risk of developing unwanted side effects is significantly reduced.
Betaloc ZOK is completely absorbed. Absorption does not depend on the timing of meals. The degree of connection with blood plasma proteins is 5-10%. The active substance is metabolized in the liver to form three metabolites without beta-blocking activity .
About 95% of the drug is excreted in the urine, the remaining amount remains unchanged. The half-life averages 3-4 hours.
Composition and release form
The drug for the treatment of cardiac pathologies is available in tablet form. They have a white shell and an oval shape. Betalok Zok tablets are convex on both sides, have a notch and engraving. As a rule, the medicine is sold in cardboard packages or plastic bottles. One pill of the drug contains the active ingredient metoprolol succinate in the amount of 23.75 mg, 47.5 mg or 95 mg, which is equal to 25, 50 or 100 mg of metoprolol tartrate. Additional auxiliary elements:
- paraffin;
- hyprolose;
- sodium stearyl fumarate;
- titanium dioxide;
- hypromellose;
- ethylcellulose;
- silica;
- macrogol;
- microcrystalline cellulose.
Indications for use
What are Betaloc ZOK tablets for? First of all, they are prescribed to patients with:
- arterial hypertension;
- heart rhythm disturbance;
- angina pectoris;
- functional disorders of the heart, which are accompanied by tachycardia .
As an element of therapy, the drug is used for chronic heart failure . In addition, Betaloc ZOK is used to reduce mortality and the likelihood of recurrent infarction after the acute phase of myocardial infarction , as well as as a prophylactic against migraine .
Can I take the drug during pregnancy?
Pregnancy and breastfeeding are contraindications for taking Betaloc tablets.
Neglecting this prescription may cause a slow heart rate in the fetus or breastfed child.
However, in some clinical cases the use of the drug is still allowed. In such situations, the benefits to the mother's health are many times greater than the harm that the fetus or newborn may receive.
To use tablets during pregnancy and lactation, consultation and supervision of a doctor is required. Otherwise, irreparable harm to the fetus or child may occur.
Contraindications
This drug is contraindicated in cases of atrioventricular block II-III degree, therapy with inotropic agents to activate beta-adrenergic receptors , sick sinus , peripheral arterial circulation , heart failure in the decompensation phase, clinically significant sinus bradycardia , cardiogenic shock , as well as hypersensitivity to beta-adrenergic and any component of the drug.
In addition, Betaloc ZOK is not suitable for patients with acute myocardial infarction with a heart rate less than 45 per minute, systolic blood pressure less than 100 mm Hg. Art. or the duration of the P-Q interval on the ECG is more than 0.24 s.
Side effects
As a rule, when used correctly, the medicine is well tolerated by patients to whom it is prescribed. Side effects are minor or easily reversible.
Cardiovascular system: bradycardia , coldness of the extremities, increased manifestations of heart failure , orthostatic hypotension , cardiogenic shock , edema , pain in the heart, fainting, palpitations, first degree atrioventricular block arrhythmia .
Gastrointestinal tract: nausea , diarrhea , vomiting , abdominal pain, constipation .
Skin: rash, increased sweating.
Metabolism: increased body fat.
CNS: increased fatigue, headache , convulsions, problems concentrating, insomnia , dizziness , paresthesia , depression , drowsiness , nightmares.
Respiratory organs: shortness of breath , bronchospasm .
In rare cases, when taking the drug, the following are possible:
- gangrene;
- increased nervous excitability;
- memory impairment;
- hallucinations;
- anxiety;
- depression;
- dryness of the oral mucosa;
- hepatitis;
- hair loss;
- exacerbation of psoriasis ;
- liver dysfunction;
- photosensitivity;
- rhinitis;
- visual impairment;
- conjunctivitis;
- taste disturbances;
- irritation and/or dry eyes;
- tinnitus;
- arthralgia;
- thrombocytopenia;
- impotence , sexual dysfunction .
Legal status
In the UK, metoprolol is classified as a prescription-only drug in the beta-blocker class and is regulated by the Medicines and Healthcare Products Regulatory Agency (MHRA). The MHRA is a government body created in 2003 that is responsible for regulating medicines, medical devices and equipment used in healthcare. The MHRA recognizes that no product is completely risk-free, but takes into account research and evidence to ensure that any associated risks are minimal.
The use of beta blockers such as metoprolol was approved in the US by the US Food and Drug Administration in 1967. The FDA has approved beta blockers to treat cardiac arrhythmias, hypertension, migraines, and others. Prescribers may prescribe beta blockers for other treatments if there is only a reason, even if it is not FDA approved. Drug manufacturers, however, cannot advertise beta blockers for other uses that have not been approved by the FDA. Because the FDA does not regulate the practice of medicine after a drug has been approved, it is legal to prescribe beta blockers for other treatments such as performance anxiety.
Legislation
The MHRA granted Intas Pharmaceuticals Limited a marketing authorization (license) for metoprolol tartrate (50 and 100 mg tablets) for prescribing only on 23 September 2011; this was after it was determined that there were no new or unexpected safety issues and that the benefits of metoprolol tartrate were greater than the risks. Metoprolol tartrate is a generic version of Lopressor that was licensed and approved on June 6, 1997 by Novartis Pharmaceuticals. [34]
In sports
Metoprolol is a beta blocker and is banned by the World Anti-Doping Agency in some sports. Beta blockers can be used to lower the heart rate and minimize tremors, which can improve performance in sports such as archery. All beta blockers are prohibited during and outside of archery and shooting competitions. Some sports, such as billiards, darts and golf, only prohibit beta blockers during competition. Additionally, any collegiate athletic association prohibits any form of beta blocker in shooting competitions.
To determine whether beta blockers have been used, a person's trace urine is analyzed. Uncharged drugs and/or metabolites of beta blockers can be analyzed using gas chromatography-mass spectrometry in selected ion monitoring (GC-MS-SIM). However, nowadays it is becoming increasingly difficult to detect the presence of beta blockers used for sports doping purposes. A disadvantage of using GC-MS-SIM is that prior knowledge of the molecular structure of the target drugs/metabolites is required. Modern times have shown differences in structures and hence new beta blockers may go unnoticed.
Litigation
In 2012, a US$11 million settlement was reached with Toprol XL (a sustained-release version of metoprolol) and its generic equivalent metoprolol. The lawsuit involved pharmaceutical companies AstraZeneca AB, AstraZeneca LP, AstraZeneca Pharmaceuticals LP and Aktiebolaget Hassle. The lawsuit says the manufacturers violated antitrust and consumer protection laws by alleging that cheaper generic versions of Toprol XL were deliberately withdrawn from the market to increase profits. This claim was subsequently rejected by the defendants.
Instructions for use of Betaloc ZOK (Method and dosage)
Instructions for use of Betaloc ZOK include taking the drug once daily, regardless of meals (preferably in the morning). Tablets should not be crushed or chewed. During dosage selection, heart rate should be monitored.
Arterial hypertension : 50 mg per day (if the therapeutic effect is not achieved, the dose can be gradually increased to 100-200 mg per day, while Betaloc ZOK tablets, instructions for use, can be combined with other antihypertensive drugs).
Stable chronic heart failure of functional class III-IV: to begin with, the dosage is prescribed - 12.5 mg per day (1/2 tablet of 25 mg). If necessary, the dose is gradually increased, but this must be done strictly under the supervision of a doctor. After 14 days, the initial dosage is increased to 25 mg per day; after another 2 weeks, 50 mg per day can be prescribed. Thus, every 14 days the dose can be doubled until a maximum dosage of 200 mg is reached. However, the dose should not be increased until there is clear evidence that the patient is stable. Kidney function needs to be monitored.
Stable chronic heart failure of functional class II: at the beginning, a dose of 25 mg is prescribed. After the first 2 weeks, it can be increased to 50 mg per day, and then doubled every 14 days until a therapeutic effect is achieved. The maximum dosage is 200 mg per day.
Migraine prevention : 100–200 mg per day is prescribed.
Angina : 100–200 mg per day is prescribed (can be combined with other drugs for the treatment of angina).
Arrhythmia : 100–200 mg per day is prescribed.
Cardiac disorders with palpitations: 100 mg per day (if necessary, the dosage can be increased to 200 mg).
Price
The cost of a medicine often depends on the form of release, the manufacturer, and the specific place where the drug is sold. The tablets have an affordable price; they can be purchased at almost every pharmacy kiosk in the capital and region, and they can also be bought inexpensively in an online store or ordered from a catalog. Below is a table with the approximate cost of a beta blocker in Moscow and the region.
Name of the medical product | Price in rubles |
Tablets 25 mg | 140-145 |
50 mg tablets | 250-280 |
100 mg pills | 400-420 |
Overdose
There are cases where, at a dosage of 7.5 g, the drug caused severe intoxication with a fatal outcome in an adult. At doses of 1.4 and 2.5 g, respectively, there was moderate and severe intoxication.
An overdose of this drug can lead to respiratory depression, atrioventricular block I–III degrees, decreased blood pressure , heart failure, bradycardia , asystole , poor peripheral perfusion , cardiogenic shock , apnea . In addition, Betaloc ZOK in increased doses can cause impairment of consciousness, tremor , excessive sweating and fatigue, bronchospasm , vomiting, hypoglycemia or hyperglycemia , renal impairment, loss of consciousness, convulsions, paresthesia , nausea, as well as esophageal spasm and hyperkalemia .
Initial signs of a drug overdose will be noticeable 20-120 minutes after administration.
Activated carbon is prescribed as treatment, as well as gastric lavage if necessary.
Depending on the manifestations of overdose, symptomatic treatment is carried out. So, you may need intubation and adequate ventilation , ECG monitoring , blood volume replenishment and glucose infusion . If necessary, atropine intravenously (before gastric lavage) 1-2 mg. For myocardial dobutamine or dopamine is administered . It is possible to use glucagon intravenously at a dosage of 50–150 mcg per 1 kg of weight. In some cases, adrenaline , terbutaline (to relieve bronchospasm ), and an artificial pacemaker help. For arrhythmia and an extensive ventricular complex, a sodium solution is injected. Resuscitation measures may be necessary.
General description of the drug
"Betalok ZOK", the price of which differs depending on the dosage and number of tablets in the package, is classified as one of the types of cardioselective beta-blockers. Externally, these tablets are enteric-coated. "Betalok ZOK", reviews from cardiologists, whose effects are mostly positive, is a long-acting drug. Due to its shell, the medicine has a delayed release. However, it does not have sympathomimetic internal activity.
The main active ingredient of the drug is metoprolol, a substance that has the following effects on the body:
- antihypertensive;
- antianginal;
- antiarrhythmic.
Also, this drug quite effectively reduces the excitability of the myocardium, reducing its need for oxygen.
Interaction
When using the drug Betaloc ZOK and other beta-adrenergic receptor , as well as MAO inhibitors and ganglion blockers , strict medical supervision is required.
The drug should not be combined with Propafenone , Verapamil . When taking Diltiazem and/or antiarrhythmic ino- and chronotropic effect may develop . When using inhalational anesthetics , the cardiodepressive effect is enhanced .
It is possible that inducers or inhibitors of microsomal liver enzymes may influence the content of the active substance Betaloc ZOK in the blood plasma. Its concentration is reduced when combined with rifampicin or increased when taken simultaneously with cimetidine , hydralazine , phenytoin , and serotonin .
When discontinuing clonidine, Betaloc ZOK must be discontinued several days before.
In combination with COX inhibitors, the antihypertensive effect of the drug may be reduced. antidiabetic agents may also be necessary when administered concomitantly.
Pharmacological compatibility
The drug Betaloc is not compatible with the following drugs:
- Quinidine;
- Verampil;
- Reserpine;
- Barbiturates;
- Antihypertensive medications;
- Alcohol-containing preparations.
When used simultaneously with non-steroidal anti-inflammatory drugs, the hypotensive effect of Betaloc tablets is significantly reduced.
Your doctor will tell you about Betalok’s compatibility with other drugs.
Analogues of Betalok ZOK
Level 4 ATC code matches:
Biol
Metocard
Metozok
Nebilet
Nebilong
Betaxolol
Bisogamma
Aritel
Cordinorm
Vasocardin
Corvitol
Bidop
Bisoprolol
Nebivolol
Biprol
Bisoprol
Concor Cor
Lokren
Concor
Niperten
The following analogues of Betalok ZOK are sold in pharmacies:
- Azoprol Retard;
- Vasocardin;
- Corvitol;
- Metocore;
- Metoprolol;
- Metoprolol Zentiva;
- Metoprolol Tartrate;
- Egilok Retard.
Reviews about analogues of Betalok ZOK are quite different. Some of them are almost as good as him, and some are of a fairly low level. So the price of analogs of this product, as well as their manufacturers, deserves special attention. To finally decide which medicine is best for each specific case, you should consult a doctor. In addition, before use, be sure to read the instructions.
What can be substituted for hypertension
The following analogues of Betalok are presented on the pharmaceutical market:
- Metoprolol;
- Vasocardin;
- Metocard;
- Nebilet;
- Anaprilin;
- Sotahexal.
Betaloc for high blood pressure is an effective drug that allows you to stabilize blood pressure and eliminate other signs of hypertension. Considering the fairly wide range of contraindications and side effects, the form of the drug, dosage and duration of therapy should be determined by a specialist individually!
Reviews of Betaloka ZOK
Reviews of Betalok ZOK indicate that quite often after its use undesirable symptoms occur. Thus, patients often report cases of rhinitis . Some also complain of irregular pulse and instability of blood pressure . Because of this, specialists prescribe additional medications that are designed to eliminate these side effects. However, it should be noted that most people still tolerate this medication easily.
In addition, reviews of Betalok ZOK draw attention to the fact that the selection of dosages should be approached with particular care. The patient’s condition must be constantly monitored and the danger of deterioration must be eliminated in a timely manner.
Use in childhood and old age
Elderly patients are not recommended to adjust dosage conditions. The use of tablets for children and adolescents (under 18 years of age) is contraindicated, because at the moment doctors do not have accurate information about the safety and effectiveness of the medicine for this category of patients. In any case, it is necessary to consult a qualified specialist who will suggest the most optimal treatment option.
Betaloka ZOK price, where to buy
The average price of Betaloc ZOK 50 mg is 270 rubles, the price of 25 mg is 160 rubles, and the average cost of 100 mg of the drug is 370 rubles.
- Online pharmacies in RussiaRussia
- Online pharmacies in UkraineUkraine
ZdravCity
- Betaloc ZOK tablets p.p.o.
with deceleration release 50 mg 30 pcs. Astra Zeneca AB/LLC Astra Zeneca Industries 306 rub. order - Betaloc ZOK tablets p.p.o. with deceleration release 100 mg 30 pcs. AstraZeneca AB / Astra Zeneca Industries LLC
RUB 375 order
- Betaloc ZOK tablets p.p.o. with deceleration release 25 mg 14 pcs. AstraZeneca AB / ZiO-Zdorovye / Astra Zeneca Industries LLC
132 RUR order
Pharmacy Dialogue
- Betalok Zok (tablet p/o 100 mg No. 30)Astra Zeneсa/AstraZeneca Industries
403 rub. order
- Betaloc Zok tablets 25 mg No. 14Astra Zenesa/AstraZeneca Industries
RUB 141 order
- Betalok Zok (tablet p/o 25 mg No. 14)Astra Zeneca/ZIO Health
129 RUR order
- Betaloc Zok tablets 50 mg No. 30Astra Zenesa/AstraZeneca Industries
RUB 276 order
- Betalok Zok (tablet p/o 50 mg No. 30)Astra Zeneca/ZIO Health
RUB 278 order
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Pharmacy24
- Betaloc Zok 100 mg N30 Astra Zeneca AB, Sweden
199 UAH order - Betaloc Zok 50 mg N30 tablets Astra Zeneca AB, Sweden
142 UAH order
- Betaloc Zok 25 mg No. 14 tablets Astra Zeneca AB, Sweden
80 UAH order
Average cost of the drug
"Betalok ZOk", the price of which depends on the number of tablets in the package and on the markup of the final seller, costs on average from 130 to 460 rubles. The cheapest are 25 mg tablets, which are packaged in 14 pieces. in a pack. Their price is about 130-150 rubles.
The most expensive is Betalok ZOK with a dosage of 100 mg, which is packaged in 30 pieces. into bottles. It costs about 420–480 rubles.