BETALOK
Active material: Metoprolol
When ATH: C07AB02
CCF: Beta1-adrenoblokator
ICD-10 codes (testimony): i20, I21, I47.1
When CSF: 01.01.01.02
Manufacturer: ASTRAZENECA AB (Sweden)
DOSAGE FORM, COMPOSITION AND PACKAGING
The solution for the on / in the clear, colorless.
| 1 ml | 1 amp. | |
| metoprolol tartrate | 1 mg | 5 mg |
Excipients: sodium chloride, water d / and.
5 ml – colorless glass vials (5) – trays, plastic (1) – packs cardboard.
Pharmacological action
Cardioselective beta1-blocker without intrinsic sympathomimetic activity. Has a little membrane stabilizing effect and does not appear to be a partial agonist.
Metoprolol suppresses or inhibits the catalytic activity, the impact of Catecholamines on cardiac activity, from nervous and physical stress. It means, that metoprolol has the ability to prevent an increase in HEART RATE, minute volume and myocardial contractility, as well as raising HELL, due to the dramatic release of Catecholamines.
Patients with symptoms of obstructive lung disease you can optionally assign metoprolol combined with beta2-adrenomimetikami. When coupled with the use of beta2-adrainomimetikami Betalok® in therapeutic doses to a lesser extent affects caused by their bronchial dilatation test, than selective beta-adrenoblokatora.
Metoprolol to a lesser extent, than selective beta-adrenoblokatora, affects the production of insulin and carbohydrate metabolism. The influence of the drug Betalok® the reaction of the cardiovascular system in conditions of hypoglycemia is much less pronounced compared with unselective beta-adrenoblokatorami.
In patients with myocardial infarction with on/in the introduction metoprolol reduced chest pain and reduced risk and trepetania predserdy. In/in the introduction of metoprolol at the first sign (during 24 h after the onset of the first symptoms) reduces the risk of myocardial infarction. Early treatment improves further metoprolol forecast flow of myocardial infarction.
Improving the quality of life when treated with Betalok® observed in patients after myocardial infarction.
In paroxizmalna tachycardia and atrial (fluttering) Atria Betalok® 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.
Deduction
Average T1/2 metoprolol from blood plasma is about 3-5 no. About 5% from the dose appears in the urine in an unmodified form.
Testimony
— najeludochkovaya tachycardia;
-Prevention and treatment of myocardial ischemia, tachycardia and pain in myocardial infarct or suspected.
Dosage regimen
At supraventricular tachycardia the drug is injected in/in a dose of 5 mg (5 ml) with speed 1-2 mg / min. You can repeat the introduction with an interval 5 mines until a therapeutic effect. Usually the total dose is 10-15 mg (10-15 ml). The recommended maximum dose in the on/in the introduction is 20 mg (20 ml).
With the aim of Prevention and treatment of myocardial ischemia, tachycardia and pain in myocardial infarct or suspected preparation is administered in / dose 5 mg (5 ml). You can repeat the introduction with an interval 2 m. The maximum dose – 15 mg (15 ml). Through 15 minutes after the last injection prescribed metoprolol (Betalok® ZOCH) for the reception inside in the dose 50 mg every 6 h for 48 no.
In patients impaired renal function dose adjustment is not required.
In patients with impaired liver function usually due to low binding to plasma proteins, dose adjustment is not required. But, at serious violation of the liver (in patients with portokavalnymi anastomosis) You may need to reduce the dose of the drug.
In elderly patients dose adjustment is not required.
Side effect
To assess the incidence, the following criteria were used: Often – >10%, often – 1-9.9%, sometimes – 0.1-0.9%, rarely – 0.01-0.09%, rarely – < 0.01%.
Cardio-vascular system: often – bradycardia, postural hypotension (very rarely accompanied by fainting), cold extremities, palpitations; sometimes – temporary increased symptoms of heart failure, AV block I degrees, cardiogenic shock in patients with acute myocardial infarction; rarely – other violations conductivity, Arrhythmia; rarely – gangrene in patients with previous severe violations of peripheral blood circulation.
From the central and peripheral nervous system: Often – fatigue; often – dizziness, headache; sometimes – paresthesia, convulsions, depression, decreased ability to concentrate, drowsiness or insomnia, nightmares; rarely – increased nervous irritability, anxiety; rarely – impaired memory/amnesia, oppression, hallucinations.
From the digestive system: often – nausea, abdominal pains, diarrhea, constipation; sometimes – vomiting; rarely – dry mouth, abnormal liver function.
From the hematopoietic system: rarely – thrombocytopenia.
The respiratory system: often – shortness of breath on exertion; sometimes – bronchospasm in patients with bronchial asthma; rarely – rhinitis.
On the part of the musculoskeletal system: rarely – arthralgia.
From the senses: rarely – blurred vision, dryness and/or eye irritation, conjunctivitis; rarely – tinnitus, dysgeusia.
Dermatological reactions: sometimes – rash (in the form of urticaria), increased sweating; rarely – hair loss; rarely – photosensitivity, exacerbation of psoriasis.
Other: rarely – impotence/sexual dysfunction; sometimes – weight gain.
Betalok® characterized by good tolerance, side effects are mostly mild and reversible. In many cases the causal link with the use of the drug has not been installed.
Contraindications
— AV-blockade II and III degrees;
- Heart failure decompensation;
-clinically significant sinusova aetiology;
- SSS;
- Cardiogenic shock;
— expressed by human peripheral blood circulation (incl. with the threat of gangrene);
- Hypotension;
-patients with acute myocardial infarction at a heart rate less than 45 u. / min, PQ interval more 0.24 with or systolic HELL less 100 mmHg.;
— When treating najeludockova tachycardia in patients with systolic HELL less 110 mmHg.;
- Patients, receiving beta-adrenoblokatora, contraindicated in/with the introduction of calcium channel blockers (incl. verapamil);
- Childhood and adolescence up 18 years (the efficacy and safety of the drug is not installed);
-hypersensitivity to the drug or to other beta-adrenoblokatoram.
FROM caution apply when AV blockade degree I, Prinzmetal angina, in COPD (emphysema, chronic obstructive bronchitis, bronchial asthma), for patients with diabetes, severe renal insufficiency.
Pregnancy and lactation
Like most drugs, Betalok® should not be administered during pregnancy and lactation (breast-feeding), except, When the expected benefits to the mother outweighs the potential risk to the fetus.
Like other antihypertensives, Beta-adrenoblokatora may cause side effects, eg, Fetal bradycardia, infants or children, breastfed, so you want to take special care when prescribing beta blockers in the third trimester of pregnancy and childbirth.
When taken by the mother during the lactation period the number of therapeutic doses of metoprolol metoprolol, striking with breast milk, and beta blocking action in a child, breastfed, are minor.
Cautions
Patients, suffering from bronchial asthma or obstructive lung disease, You should assign the accompanying bronhodilatirujushhuju therapy. If necessary, increase the dose of beta2-adrenomimetika.
When applying the beta1-adrenoblokatorov risk their impact on carbohydrate metabolism, or the ability to mask Hypoglycemia is significantly less, than nonselective beta-adrenoblokatorov.
In patients with chronic heart failure at decompensation stage of compensation must be made as to, and during drug treatment.
Patients, suffering from angina Prinzmetala, not recommended to appoint selective beta-adrenoblokatora.
Very rarely in patients with impaired AV conduction can occur the deterioration (possible outcome – AV блокада). If a treatment developed bradycardia, dose Betaloka® It is necessary to reduce.
Metoprolol may worsen the symptoms of human peripheral blood circulation mainly because of lower HELL.
Caution should be prescribed to patients, suffering from severe kidney failure, When metabolic azidoze, at the same time with cardiac glycosides.
Patients, taking beta-blockers, anaphylactic shock is leaking into a more severe form.
Patients, suffering feohromotsytoma, in parallel with the preparation Betalok® You must assign the alpha-blocker.
In the case of surgery should inform the anesthesiologist about how, that the patient takes a selective beta.
You should not assign a repeated dose (second or third) at a heart rate less than 40 u. / min, When the interval PQ more 0.26 with and sistolicheskom the HELL is less 90 mmrt calendar.
Use in Pediatrics
Experience of applying Betaloka® children have limited. Use of the drug in this category is contraindicated in patients.
Overdose
Metoprolol dose 7.5 g adult caused fatal intoxication. The child 5 years, accepting 100 mg metoprolol, after gastric lavage were observed signs of intoxication. Reception 450 mg metoprolol teenager 12 years resulted in moderate intoxication. Reception 1.4 and g 2.5 g metoprolol adults caused moderate and severe intoxication, respectively. Reception 7.5 g for adults has led to extremely severe intoxication.
Symptoms: the most serious are symptoms of cardiovascular system, Sometimes, however,, especially in children and adolescents, may prevail symptoms of the central nervous system and the Suppression of lung function, bradycardia, AV blockade III extent, asistolija, marked reduction in blood pressure, poor peripheral perfusion, heart failure, cardiogenic shock, inhibition of lung function, apnea, increased fatigue, the disruption and loss of consciousness, tremor, convulsions, increased perspiration, paresthesia, bronchospasm, nausea, vomiting, possible jezofagealnyj spasm, gipoglikemiâ (especially in children) or hyperglycemia, hyperkalemia; effect on kidneys; tranzitornyi miasteniceski syndrome.
The accompanying admission alcohol, antihypertensive agents, hinidina or barbiturates can worsen the condition of the patient. The first signs of an overdose can occur through 20 – 120 minutes after administration.
Treatment: in the case of the reception of the drug inside – appointment of activated carbon, if necessary – gastric lavage.
Atropyn (0.25-0.5 mg in/in for adults and 10-20 µg/kg for children) You should assign to gastric lavage (because of the risk of stimulating the vagus nerve).
If necessary, – airway support (Intubation) and the holding of the IVL. For cupping the bronchoconstriction injection or inhalation terbutaline can be applied.
You must fill in the BCC, hold the infusion of glucose. Atropyn 1.0-2.0 mg / in, If necessary, repeat the introduction (especially when vagusnyh symptoms). ECG Monitoring.
In the case of explicit oppression contractile function of myocardium shows or dobutamine infusion of dopamine. You can also use glucagon 50-150 mcg/kg/in every 1 m. In some cases, can be effectively adding to the therapy of epinephrine.
When arrhythmias and increase ventricular complex (QRS) infuzionno injected sodium solutions (chloride or bicarbonate). It is possible to install artificial driver rhythm.
When cardiac arrest due to an overdose may need resuscitation for several hours.
Symptomatic treatment.
Drug Interactions
Metoprolol is a substrate of CYP2D6, in this connection, preparations, inhibiting CYP2D6, (quinidine, terʙinafin, paroxetine, fluoxetine, sertraline, celecoxib, propafepon and diphenhydramine) may affect plasma concentration metoprolola.
Combinations, which should be avoided
Barbituric acid derivatives: barbiturates increase metabolism of metoprolol, as a result of the induction of enzymes (the study was conducted with phenobarbital).
Propafenone: When assigning propafenon 4 patients, receiving metoprolol, There was an increase in concentration metoprolola plasma 2-5 time, at the same time 2 patients experienced side effects, characteristic of metoprolol. This interaction has been confirmed in the course of research on the 8 Volunteers. Probably, interaction is due to inhibition of propafenonom, like hinidinu, metabolism of metoprolol through izofermenta CYP2D6. Taking into account the fact, that propafenone has the properties of beta-adrenoblocker, the joint appointment of metoprolol and propafenon did not seem appropriate.
Verapamil: the combination of beta-adrenoblokatorov (atenolola, propranolol and pindolola) and verapamil can cause bradycardia and lead to lower HELL. Verapamil and beta-adrenoblokatora have complementary ingibiruty effect on AV conductivity and sinus node function.
Combinations, in the application that may require correction doses of the drug Betalok®
Class I antiarrhythmics: in combination with beta-adrenoblokatorami possibly summation of negative effect inotropnogo, as a consequence, develop severe haemodynamic side effects in patients with impaired left ventricular function. Such combinations should also be avoided in patients with SSSU and violation of AV conduction. Interaction described in example dizopiramida.
Amiodarone: joint application with metoprolol may lead to pronounced sinus bradycardia. Taking into consideration the extremely long T1/2 amiodarona (50 days), should take into account possible interaction after long time after the cancellation of amiodarone.
Diltiazem: diltiazem and beta-adrenoblokatora reinforce ingibirutee to AV conductivity and sinus node function. In combination with metoprolol diltiazem cases of bradycardia.
NSAIDs: Npvs weaken antihypertensive action of beta-adrenoblokatorov. This interaction is registered in combination with indomethacin and were observed in combination with sulindakom. In studies with diclofenac this effect not noted.
Difengidramin: Diphenhydramine decreases biotransformatia metoprolol to α–gidroksimetoprolola in 2.5 times. At the same time there has been a strengthening of metoprolol.
Epinephrine (adrenaline): reported on 10 cases expressed arterial hypertension and bradycardia in patients, taking selective beta-adrenoblokatora (including pindolol and propranolol) and treated with epinephrine. Interaction observed in a group of healthy volunteers and. Expected, that such reactions can also occur when applying of epinephrine with local anaesthetics in the event of accidental ingestion in vascular track. Apparently, This risk is far lower when applying cardioselective beta blockers.
Phenylpropanolamine:phenylpropanolamine (norephedrine) single dose 50 mg may improve diastolic HELL to pathological values in healthy volunteers. Propranolol basically lets raise HELL, calling fenilpropanolaminom. However, beta-adrenoblokatora may cause reactions ironic hypertension patients, receiving high doses of phenylpropanolamine. It was reported on several cases development gipertoniceski kriza against the backdrop of the admission of phenylpropanolamine.
Quinidine: quinidine inhibits the metabolism of metoprolol from a specific group of patients with rapid gidroksilirovaniem (in Sweden, about 90% the population), calling, mainly, a significant increase in plasma concentration of metoprolol and increased β-adrenoceptor blockade. It is believed, that such interaction is characteristic for other beta-adrenoblokatorov, in the metabolism of CYP2D6 CYP.
Klonidin: hypertensive reactions in an abrupt cancellation of clonidine may be aggravated while receiving beta-adrenoblokatorov. In a joint application, in case of necessity to cancel clonidine, stopping beta-adrenoblokatorov should begin a few days before the lifting of clonidine.
Rifampicin: rifampin may increase metabolism of metoprolol, decreasing its concentration in blood plasma.
May increase concentration metoprolola plasma when combined with the application of cimetidine, gidralazinom, selective serotonin reuptake inhibitors, such as paroxetine, Fluoxetine and sertraline.
Patients, at the same time taking metoprolol and other beta-adrenoblokatora (eye drops) or MAO inhibitors, should be under close supervision.
In the face of the reception beta-adrenoblokatorov 73.21 anaesthetics increase cardiodepressivne effect.
In the face of the reception beta-adrenoblokatorov patients, receiving oral gipoglikemicakie means, may require dose adjustment the past.
Heart glycosides in a joint application with beta-adrenoblokatorami can increase time AV conductivity and cause bradycardia.
Conditions of supply of pharmacies
The drug is released under the prescription.
Conditions and terms
The drug should be stored out of reach of children, the dark place at a temperature below 25° c. Shelf life – 5 years.
