Betaloc Zoc, 50 mg 30 pcs
€8.52 €7.46
Pharmacotherapeutic group: beta1-adrenoblocker selective
ATX code: C07AB02
Pharmacological properties
Pharmacodynamics
Metoprolol is a b1-adrenoblocker that blocks b1-receptors at doses significantly lower than those required to block b2-receptors.
Metoprolol has little membrane-stabilizing effect and does not exhibit partial agonist activity.
Metoprolol reduces or inhibits the agonist effect that catecholamines, released during nervous and physical stress, have on cardiac activity. This means that metoprolol has the ability to inhibit the increase in heart rate (HR), minute volume and increased
heart contractility, as well as increased blood pressure (BP) caused by the sudden release of catecholamines.
Unlike common tablet forms of selective b1-adrenoblockers (including metoprolol tartrate), during Betaloc® ZOC use constant concentration of the drug in plasma is observed and stable clinical effect (b1-blockade) is provided for more than 24 hours.
Due to the absence of obvious peak plasma concentrations, clinically Betaloc® ZOC is characterized by better b1-selectivity compared to conventional tablet forms of b1-adreno-blockers. In addition, the potential risk of side effects observed at peak plasma concentrations of the drug, such as bradycardia and weakness in the legs when walking, is significantly reduced.
Patients with symptoms of obstructive lung disease may be prescribed Betalok® ZOK in combination with b2-adrenomimetics if necessary. When used in combination with b2-adrenomimetics, Betaloc® ZOC in therapeutic doses has less effect on bronchodilation induced by b2-adrenomimetics than non-selective b-adrenoblockers. Metoprolol affects insulin production and carbohydrate metabolism to a lesser extent than non-selective b-adrenoblockers. Compared with non-selective b-adrenoblockers, the drug effect on cardiovascular system response in hypoglycemic conditions is significantly less pronounced.
Administration of Betaloc® ZOC in arterial hypertension leads to a significant reduction of blood pressure for more than 24 hours both when lying and standing and under load. At the beginning of metoprolol therapy, an increase in vascular resistance is noted. However, with long-term therapy BP may decrease due to decreased vascular resistance with unchanged cardiac output.
In MERIT-HF study (survival in chronic heart failure (NYHA class II-IV) and reduced cardiac output fraction (≤ 0.40), including 3991 patients) Betaloc® ZOC showed increased survival and decreased hospitalization rate. With long-term treatment, patients achieved an overall improvement in symptoms (according to NYHA grades). Also therapy with Betaloc® ZOC showed increased left ventricular ejection fraction, decreased left ventricular end systolic and end diastolic volumes.
Quality of life during treatment with Betaloc® ZOC did not deteriorate or improve. Improved quality of life during treatment with Betaloc® ZOC was observed in patients after myocardial infarction.
Pharmacokinetics
Tablets disintegrate rapidly on contact with liquid, with dispersion of the active substance in the gastrointestinal tract. The rate of release of the active substance depends on the acidity of the environment. The duration of therapeutic effect after using Betaloc® ZOC (sustained release tablets) is more than 24 hours, while a constant rate of active substance release is achieved over 20 hours. The elimination half-life is on average 3.5 hours.
Betaloc® ZOC is completely absorbed after oral administration. Systemic bioavailability after a single oral dose is approximately 30-40%.
Metoprolol undergoes oxidative metabolism in the liver. The three major metabolites of metoprolol showed no clinically significant b-blocking effect. About 5% of the oral dose of the drug is excreted unchanged in the urine, the rest of the drug is excreted as metabolites. Binding to blood plasma proteins is low, approximately 5-10%.
Indications
Active ingredient
Composition
How to take, the dosage
Betaloc® ZOC is intended to be taken once daily and is recommended to be taken in the morning. The Betaloc® ZOC tablet should be swallowed with fluids. Tablets (or tablets divided in half) should not be chewed or crumbled. Food intake does not affect the bioavailability of the drug.
The development of bradycardia should be avoided when adjusting the dose.
Arterial hypertension
50-100 mg once daily. If necessary, the dose may be increased to 200 mg daily or another antihypertensive agent may be added, preferably a diuretic and a dihydropyridine-type slow calcium channel blocker.
Stenocardia
100-200 mg of Betaloc® ZOC once daily. If necessary, another antianginal drug may be added to therapy.
Stable symptomatic chronic heart failure with impaired left ventricular systolic function
Patients must be in stable chronic heart failure without an episode of exacerbation within the past 6 weeks and without changes in underlying therapy within the past 2 weeks.
The therapy of heart failure with β-adrenoblockers may sometimes lead to a temporary worsening of the symptomatic picture. In some cases, continuation of therapy or reduction of the dose may be possible; in some cases it may be necessary to discontinue the drug.
Stable chronic heart failure, functional class II
The recommended starting dose of Betalock® ZOC for the first 2 weeks is 25 mg once daily. After 2 weeks of therapy, the dose may be increased to 50 mg once daily and may be doubled every 2 weeks thereafter.
The maintenance dose for long-term treatment is 200 mg of Betaloc® ZOC once daily.
Stable chronic heart failure, functional class III-IV The recommended starting dose for the first 2 weeks is 12.5 mg of Betaloc® ZOC (half tablet 25 mg) once daily. The dose is adjusted individually. During the period of dose increase the patient should be monitored, because in some patients the symptoms of heart failure may worsen.
After 1 to 2 weeks, the dose may be increased to 25 mg of Betaloc® ZOC once daily. Then, after 2 weeks, the dose may be increased to 50 mg once daily. In patients who tolerate the drug well the dose may be doubled every 2 weeks up to a maximum dose of 200 mg of Betaloc® ZOC once daily.
In cases of arterial hypotension and/or bradycardia, it may be necessary to reduce concomitant therapy or decrease the dose of Betaloc® ZOC. Arterial hypotension at the start of therapy does not necessarily indicate that a given dose of Betaloc® ZOC will not be tolerated with continued long-term treatment. However, the dose should not be increased until the condition has stabilized. Renal function may need to be monitored.
Heart rhythm disorders
100-200 mg of Betaloc® ZOC once daily. Supportive treatment after myocardial infarction 200 mg of Betaloc® ZOC once daily.
Functional cardiac disorders with tachycardia
100 mg of Betaloc® ZOC once daily. If necessary, the dose can be increased to 200 mg daily.
Prevention of migraine attacks
100-200 mg of Betaloc® ZOC once daily.
Renal dysfunction
There is no need to adjust the dose in patients with impaired renal function.
Hepatic dysfunction
Because of the low degree of binding to plasma proteins, no dose adjustment of metoprolol is usually required. However, in severe liver function impairment (in patients with severe cirrhosis or portocaval anastomosis), dose reduction may be required.
Elderly age
There is no need to adjust the dose in elderly patients.
Children
Limited experience with Betaloc® ZOC in children.
Interaction
Special Instructions
Synopsis
Contraindications
Side effects
Betaloc® ZOC is well tolerated by patients; side effects are mostly mild and reversible.
The following criteria were used to assess incidence: very common (>10%), common (1-9.9%), infrequent (0.1-0.9%), rare (0.01-0.09%), and very rare (<0.01%).
Cardiovascular System
Often: bradycardia, orthostatic hypotension (very rarely accompanied by syncope), coldness of extremities, palpitations;
Infrequent: Temporary worsening of heart failure symptoms, grade I AV block; cardiogenic shock in patients with acute myocardial infarction, edema, pain in the heart region;
Rare: other conduction disorders, arrhythmias;
Very rare: gangrene in patients with previous severe peripheral circulatory disturbances.
Central nervous system
Very common: increased fatigue; Frequent: dizziness, headache;
Infrequent: paresthesia, seizures, depression, decreased concentration, drowsiness or insomnia, nightmares;
Rare: increased nervous excitability, anxiety;
Very rare: amnesia/memory disturbances, depression, hallucinations.
Gastrointestinal tract
Often: nausea, abdominal pain, diarrhea, constipation; Infrequent: vomiting;
Rarely: dry oral mucosa.
Liver
Rarely: disorders of liver function; Very rare: hepatitis.
Skin
Infrequent: skin rash (similar to psoriasis-like urticaria), increased sweating;
Rare: Hair loss;
Very rare: photosensitization, exacerbation of psoriasis.
Respiratory organs
Often: shortness of breath on exercise; Infrequent: bronchospasm;
Rarely: rhinitis.
Sensory organs
Rarely: visual disturbances, dry and/or irritated eyes, conjunctivitis; Very rare: ringing in the ears, taste disturbances.
Skeletal and muscular system
Very rare: arthralgia.
Metabolism
Infrequent: weight gain.
blood
Very rare: thrombocytopenia.
Others
Rarely: impotence/sexual dysfunction.
Overdose
Pregnancy use
Similarities
Weight | 0.032 kg |
---|---|
Shelf life | 3 years. Do not use after the expiration date. |
Conditions of storage | Store at a temperature not exceeding 30°C. Keep out of reach of children. |
Manufacturer | AstraZeneca Industries/AstraZeneca AB, Russia |
Medication form | sustained release tablets |
Brand | AstraZeneca Industries/AstraZeneca AB |
Other forms…
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