2010/12/17

Betaloc

Release form, composition and packing Betaloc 
 
Solution for injection in a clear, colorless. 1 ml 1 amp. metoprolol tartrate 1 mg 5 mg. Excipients: sodium chloride, water, d / and.

Clinico-pharmacological group: Beta1-blocker.

Pharmacological action

Cardioselective beta1-blocker without intrinsic sympathomimetic activity. Has little membrane-stabilizing action and does not exhibit partial agonist activity. Metoprolol suppresses or inhibits the stimulatory effect exerted by catecholamines on cardiac activity resulting from the nervous and physical stress.

This means that metoprolol has the ability to prevent an increase in heart rate, cardiac output and myocardial contractility, and increased blood pressure caused a sharp release of catecholamines. Patients with symptoms of obstructive lung disease and if you want to assign metoprolol in combination with beta2-adrenomimetikami.

In a joint application with the beta2-adrenomimetikami Betaloc in therapeutic doses, to a lesser extent affects they cause bronchodilation than nonselective beta-blockers. Metoprolol to a lesser extent than nonselective beta-blockers, affects the production of insulin and carbohydrate metabolism. The influence of the drug Betaloc on the reaction of the cardiovascular system in conditions of hypoglycemia is much less pronounced compared with nonselective beta-blockers.

In patients with myocardial infarction at high / vvvedenii metoprolol reduced chest pain, and reduced risk of developing atrial and atrial flutter. In the intravenous metoprolol at the first sign (within 24 hours after symptom onset) reduces the risk of myocardial infarction. Early treatment with metoprolol leads to further improvement of prognosis of myocardial infarction.

Improving quality of life in the treatment of drug Betaloc observed in patients after myocardial infarction. In paroxysmal tachycardia and atrial flutter () atrial Betaloc reduces heart rate.

Pharmacokinetics

Metabolism

Metoprolol undergoes oxidative metabolism in the liver with the formation of three major metabolites, none of which has no clinically significant beta-blocking effect.

Breeding

The average T1 / 2 of metoprolol from plasma is about 3-5 hours about 5% of the administered dose excreted in the urine in unchanged form.

Statement
supraventricular tachycardia;
Prevention and treatment of myocardial ischemia, tachycardia, and pain in myocardial infarction or suspected it.

Dosing regimen

When supraventricular tachycardia drug is administered IV at an initial dose of 5 mg (5 ml) at 1 - 2 mg / min. You can repeat administration with an interval of 5 min to achieve a therapeutic effect. Usually the total dose of 10-15 mg (10-15 ml). The recommended maximum dose of iv administration of 20 mg (20 ml). With a view to preventing and treating myocardial ischemia, tachycardia, and pain in myocardial infarction or suspected drug he administered iv at a dose of 5 mg (5 ml).

You can repeat administration with an interval of 2 min. The maximum dose - 15 mg (15 ml). 15 min after the last injection prescribed metoprolol (Betaloc ZOK) oral dose of 50 mg every 6 h for 48 h. In patients with impaired renal function, dosage adjustment is required.

Patients with impaired liver function is usually due to a low degree of binding to plasma proteins, dosage adjustment is required.

However, in severe liver dysfunction (patients with portokavalnymi anastomosis) may require a reduction in dose. Elderly patients dosage adjustment is required.

Side effect

To estimate the incidence used the following criteria: very common -> 10%, often - 1-9.9%, sometimes - 0.1-0.9%, rare - 0.01-0.09%, very rare - 0.01%.
With the cardiovascular system: often - bradycardia, postural hypotension (very rarely accompanied by fainting), cold extremities, a feeling the heartbeat, and sometimes - a temporary boost in heart failure symptoms, AV-block I degree, cardiogenic shock in patients with acute myocardial infarction; rarely - other conduction abnormalities, arrhythmias, very rarely - gangrene in patients with previous severe disorders of peripheral circulation.
CNS and peripheral nervous system: Very common - fatigue, often - dizziness, headache, and sometimes - paresthesia, cramps, depression, decreased ability to concentrate, drowsiness or insomnia, nightmares, rarely - increased nervous irritability, anxiety; very rare - impaired memory / amnesia, depression, hallucinations.
From the digestive system: frequent - nausea, abdominal pain, diarrhea, constipation, and sometimes - vomiting, rarely - dry mouth, liver function abnormalities.
From the hematopoietic system: very rarely - thrombocytopenia.
Part of the respiratory system: often - shortness of breath on exertion, and sometimes - bronchospasm in patients with asthma, rarely - rhinitis.
From the musculoskeletal system: very rarely - arthralgia.
From the sensory organs: rarely - blurred vision, dryness and / or eye irritation, conjunctivitis, is very rare - tinnitus, disorders of taste sensations.

Dermatological reactions: sometimes - a rash (in the form of hives), increased sweating, rarely - hair loss, very rarely - photosensitivity, exacerbation of psoriasis.

Other: rarely - impotence / sexual dysfunction, and sometimes - an increase of body weight. Betaloc is well tolerated, side effects are mostly mild and reversible.

In many cases, a causal relationship with the drug has not been established.

Contraindications
AV-block grade II and III;
heart failure in the stage of decompensation;
clinically significant sinus bradycardia;
SSS;
cardiogenic shock;
expressed by peripheral blood circulation disorders (including the threat of gangrene);
hypotension;
patients with acute myocardial infarction with heart rate below 45 beats / min, an interval of more than 0.24 with PQ or systolic blood pressure less than 100 mm Hg;
in the treatment of supraventricular tachycardia in patients with systolic blood pressure less than 110 mm Hg;
patients receiving beta-blockers were contraindicated in intravenous calcium channel blockers (including verapamil);
childhood and adolescence to 18 years (the effectiveness and safety of the drug not established);
hypersensitivity to the drug or other beta-blockers.

Be wary of a drug at AV-blockade of I degree, Prinzmetal angina, COPD (emphysema, chronic obstructive bronchitis, bronchial asthma), diabetes, kidney failure, severe.

Pregnancy and lactation

Like most medicines, Betaloc should not be administered during pregnancy and lactation (breastfeeding), except in cases where the expected benefit duration the mother outweighs the potential risk to the fetus. Like other antihypertensive drugs, beta-blockers can cause side effects such as bradycardia in the fetus, infants or children who are breastfed, and therefore require special care in the appointment of beta-blockers in the III trimester of pregnancy and immediately before delivery. When you receive the mother during lactation metoprolol in therapeutic doses of metoprolol, is excreted in breast milk, and beta-blocking effect of a child who is breastfed, are negligible. Use in hepatic dysfunction in patients with impaired liver function is usually due to a low degree of binding to plasma proteins, dosage adjustment is required.

However, in severe liver dysfunction (patients with portokavalnymi anastomosis) may require a reduction in dose.

Use in renal impairment

Patients with impaired renal function, dosage adjustment is required.

Cautions

Patients suffering from bronchial asthma or obstructive lung disease, should appoint a concomitant bronchodilatory therapy. If necessary, increase the dose of beta 2-adrenomimetic.

In applying the beta1-adrenergic blockers the risk of their influence on carbohydrate metabolism or the possibility of masking of hypoglycemia is much less than the nonselective beta-blockers. In patients with chronic heart failure in decompensated need to get the compensation stage, both before and during drug treatment.

Patients suffering from angina, Prinzmetal, not advisable to appoint non-selective beta-blockers. It is very rare in patients with impaired AV-conduction can occur impairment (a possible outcome - AV-block). If during treatment developed bradycardia, a dose of Betaloc should be reduced. Metoprolol can worsen the symptoms of disorders of the peripheral arterial circulation is mainly due to the reduction of blood pressure. Should be prescribed with care to patients suffering from severe renal insufficiency, metabolic acidosis, together with cardiac glycosides.

Patients taking beta-blockers, anaphylactic shock occurs in a more severe form. Patients suffering from pheochromocytoma, in parallel with the drug Betaloc should appoint an alpha-blocker. In the case of surgical intervention should inform the doctor-anesthesiologist that the patient takes a beta-blocker. Should not appoint a second dose of the drug (second or third) in heart rate below 40 beats / min, with a PQ interval of 0.26 s and systolic blood pressure less than 90 mm Hg