KORDIL [Metoprolol tartrate] 25 mg Tablets
KORDIL
instructions for medical use of the medicinal product
Tradename
Kordil, Kordil
International non-proprietary name
Metoprolol, Metoprolol
Composition
Each film-coated tablet contains:
active substance: metoprolol tartrate 25 mg
excipients: starch, dextrin, microcrystalline cellulose, hypromellose, talc, magnesium stearate
Dosage form
Tablets.
Pharmacotherapeutic group
Beta blockers. Selective beta-blockers.
Pharmacological properties
Pharmacodynamics
Metoprolol tartrate is a cardioselective β -adrenergic blocker without intrinsic sympathomimetic activity and membrane stabilizing action. It mainly affects the β 1-adrenergic receptors of the heart, has antianginal, hypotensive and antiarrhythmic effects. In patients who have had myocardial infarction, it reduces the risk of recurrent myocardial infarction, and in patients with hypertension, it also reduces the risk of cardiovascular complications (stroke). Its anti-ischemic effect has been proven in the case of painless myocardial ischemia and a decrease in left ventricular hypertrophy in patients with hypertension. The antianginal effect is due to a decrease in heart rate, myocardial contractility, systemic blood pressure, which leads to a decrease in myocardial oxygen demand. Due to the lengthening of diastole (due to the negative chronotropic effect), myocardial perfusion improves. Unlike non-selective β -adrenergic blockers , metoprolol tartrate, when used in medium therapeutic doses, has a less pronounced effect on the smooth muscles of the bronchi and peripheral arteries, insulin release, carbohydrate and lipid metabolism.
Pharmacokinetics
Metoprolol tartrate undergoes oxidative metabolism in the liver to form three major metabolites, none of which has a clinically significant β -blocking effect. About 5% of the dose taken is excreted in the urine unchanged. The mean plasma half-life is about 3-5 hours.
Indications for use
- arterial hypertension: lowering blood pressure and reducing the risk of cardiovascular and coronary death (including sudden death),
- angina,
- cardiac arrhythmias, including supraventricular tachycardia,
- after myocardial infarction (in complex therapy),
- functional disorders of cardiac activity, accompanied by tachycardia,
- prevention of migraine attacks,
- hyperthyroidism (complex therapy).
Contraindications
- atrioventricular block II and III degree,
- heart failure in the stage of decompensation,
- clinically significant sinus bradycardia,
- sick sinus syndrome
- cardiogenic shock
- severe disorders of peripheral circulation,
- arterial hypotension,
- patients with acute myocardial infarction with a heart rate of less than 45 beats per minute, a PQ interval of more than 0.24 seconds or a systolic blood pressure of less than 100 mm Hg,
- with serious peripheral vascular diseases with the threat of gangrene,
- patients receiving long-term or intermittent therapy with inotropic agents acting on β -adrenergic receptors ,
- age up to 18 years (efficacy and safety have not been established),
- known hypersensitivity to metoprolol tartrate and its components or to other β -blockers.
Dosage and administration
inside, both with food and on an empty stomach.
Arterial hypertension. 100–200 mg of the drug once in the morning or in 2 divided doses; morning and evening. If necessary, the dose can be increased or another antihypertensive agent added.
Angina. 100-200 mg / day in 2 divided doses; morning and evening. If necessary, another antianginal drug may be added to therapy.
Heart rhythm disorders. 100-200 mg / day in 2 divided doses; morning and evening. If necessary, another antiarrhythmic drug may be added to therapy.
Maintenance therapy after myocardial infarction. The maintenance dose is 200 mg / day in 2 divided doses; morning and evening.
Functional disorders of cardiac activity, accompanied by tachycardia. 100 mg of the drug 1 time per day, it is recommended to take a tablet in the morning. If necessary, the dose may be increased.
Prevention of migraine attacks. 100-200 mg / day in 2 divided doses; morning and evening.
Hyperthyroidism. 150-200 mg / day in 3-4 doses.
Impaired kidney function. There is no need to adjust the dose in patients with impaired renal function.
Impaired liver function. Usually, due to the low degree of binding to plasma proteins, dose adjustment is not required. However, in severe hepatic impairment, a dose reduction may be required.
Elderly age. There is no need to adjust the dose in elderly patients.
Children. Experience with the drug in children is limited.
Special instructions and precautions
Patients taking β -blockers should not be given intravenous slow calcium channel blockers such as verapamil.
When using β 1-blockers, the risk of their effect on carbohydrate metabolism or the possibility of masking hypoglycemia is much less than when using non-selective β -blockers.
In patients with chronic heart failure in the stage of decompensation, it is necessary to achieve a stage of compensation both before and during treatment with the drug.
Patients suffering from Prinzmetal's angina are not recommended to prescribe non-selective β -blockers.
Very rarely, patients with impaired atrioventricular conduction may worsen (possible outcome - AV block). If bradycardia develops during treatment, the dose should be reduced.
Cordil may worsen the symptoms of peripheral arterial circulatory disorders, mainly due to a decrease in HELL. Caution should be exercised when prescribing the drug to patients suffering from severe renal insufficiency, with metabolic acidosis, co-administration with cardiac glycosides.
Patients suffering from pheochromocytoma, in parallel with Cordil an α -blocker should be prescribed.
In the case of surgery, the anesthesiologist should be informed that the patient is taking a β -blocker.
In patients taking β -blockers, anaphylactic shock is more severe.
Patients suffering from obstructive pulmonary disease are not recommended to prescribe β-blockers. In case of poor tolerance of other antihypertensive drugs or their ineffectiveness, Cordil can be prescribed, since it is a selective drug. It is necessary to prescribe the minimum effective dose, if necessary, it is possible to prescribe a β 2 -agonist.
In patients with cirrhosis of the liver, the bioavailability of metoprolol tartrate is increased.
Abrupt discontinuation of the drug should be avoided. If it is necessary to cancel the drug, the cancellation should be carried out gradually. In most patients, the drug can be discontinued within 14 days. The dose of the drug is reduced gradually, in several doses, until the final dose of 25 mg is reached 1 time per day. Patients with coronary artery disease should be under close medical supervision during drug withdrawal.
Influence on the ability to drive vehicles and mechanisms
Use during pregnancy and during breastfeeding
It should not be used during pregnancy and lactation, unless the expected benefit to the mother outweighs the potential risk to the fetus.
Interaction with other drugs
With simultaneous use with antihypertensive drugs, diuretics, antiarrhythmic drugs, nitrates, there is a risk of developing severe arterial hypotension, bradycardia, AV blockade.
With simultaneous use with barbiturates, the metabolism of metoprolol tartrate is accelerated, which leads to a decrease in its effectiveness.
With simultaneous use with hypoglycemic agents, it is possible to enhance the effect of hypoglycemic agents.
With simultaneous use with NSAIDs, it is possible to reduce the hypotensive effect of metoprolol tartrate.
With simultaneous use with opioid analgesics, the cardiodepressive effect is mutually enhanced.
With simultaneous use with peripheral muscle relaxants, it is possible to increase the neuromuscular blockade.
With simultaneous use with means for inhalation anesthesia, the risk of inhibition of myocardial function and the development of arterial hypotension increases.
With simultaneous use with oral contraceptives, hydralazine, ranitidine, cimetidine, the concentration of metoprolol tartrate in the blood plasma increases.
With simultaneous use with amiodarone, arterial hypotension, bradycardia, ventricular fibrillation, asystole are possible.
With simultaneous use with verapamil, Cmax in blood plasma and AUC of metoprolol taratrata increase. The minute and stroke volume of the heart, pulse rate, and arterial hypotension decrease. Perhaps the development of heart failure, dyspnea and blockade of the sinus node, and the threat of cardiac arrest.
With simultaneous use, it is possible to increase bradycardia caused by digitalis glycosides.
With simultaneous use with dextropropoxyphene, the bioavailability of metoprolol tartrate increases.
With simultaneous use with diazepam, a decrease in clearance and an increase in the AUC of diazepam are possible, which can lead to an increase in its effects and a decrease in the speed of psychomotor reactions.
With simultaneous use with lidocaine, a violation of the excretion of lidocaine is possible.
With simultaneous use with mibefradil in patients with low activity of the CYP2D6 isoenzyme, it is possible to increase the concentration of metoprolol tartrate in the blood plasma and increase the risk of developing toxic effects.
With simultaneous use with norepinephrine, epinephrine, other adreno- and sympathomimetics (including in the form of eye drops or as part of antitussives), some increase in blood pressure is possible.
With simultaneous use with reserpine, guanfacine, methyldopa, clonidine, severe bradycardia may develop.
With simultaneous use with rifampicin, the concentration of metoprolol in the blood plasma decreases.
Metoprolol tartrate may cause a slight decrease in the clearance of theophylline in smoking patients.
There are reports of a decrease in the clearance of metoprolol tartrate from the body when used simultaneously with ciprofloxacin.
With simultaneous use with ergotamine, it is possible to increase peripheral circulatory disorders.
With simultaneous use with estrogens, the antihypertensive effect of metoprolol tartrate decreases.
Side effect
The following criteria were used to assess the incidence of cases: very often (> 10%), often (1–9.9%), infrequently (0.1–0.9%), rarely (0.01–0.09%), and very rarely (<0.01%).
From the side of the cardiovascular system : often - bradycardia, postural disturbances (very rarely accompanied by fainting), cold extremities, palpitations; infrequently - temporary increase in symptoms of heart failure, cardiogenic shock in patients with acute myocardial infarction, AV blockade of the first degree; rarely - other disorders of cardiac conduction, arrhythmias; very rarely - gangrene in patients with previous severe disorders of the peripheral circulation.
From the side of the central nervous system : Often - increased fatigue; often - dizziness, headache; infrequently - paresthesia, convulsions, depression, weakening of attention, drowsiness or insomnia, nightmares; rarely - increased nervous excitability, anxiety, impotence / sexual dysfunction; very rarely - amnesia / memory impairment, depression, hallucinations.
From the gastrointestinal tract: often - nausea, pain in the abdomen, diarrhea, constipation; infrequently - vomit; rarely - dry mouth.
From the side of the skin: infrequently - rash (in the form of urticaria), excessive sweating; rarely - hair loss; very rarely - photosensitivity, exacerbation of psoriasis.
From the side of the liver: rarely - Liver dysfunction.
From the side of the respiratory system: often - shortness of breath with physical effort; infrequently - bronchospasm in patients with bronchial asthma; rarely - rhinitis.
From the sense organs: rarely - visual disturbances, dryness and / or irritation of the eyes, conjunctivitis; very rarely - ringing in the ears, taste disturbances.
From the side of metabolism: infrequently - increase in body weight.
From the musculoskeletal system: very rarely - arthralgia.
From the blood system: very rarely - thrombocytopenia.
If any of the side effects listed in the instructions get worse, or if you notice any other side effects not listed in the instructions, tell your doctor.
Overdose
Symptoms: pronounced decrease BP, sinus bradycardia, AV block, heart failure, cardiogenic shock, cardiac arrest, bronchospasm, impaired consciousness/coma, nausea, vomiting, and cyanosis.
The first signs of an overdose may occur within 20 minutes to 2 hours after taking the drug.
Treatment: administration of activated charcoal, if necessary - gastric lavage, symptomatic treatment.
Storage conditions
Store in a cool and dry place, at a temperature not exceeding 30 0 C.
Keep out of the reach of children.
Best before date
3 years. Do not use after the expiry date stated on the packaging.
Holiday conditions
Released by prescription.
Release form
10 tablets in an aluminum foil blister. 3 blisters with instructions for use in a cardboard box.