Concor
Concor: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Concor
ATX code: C07AB07
Active ingredient: bisoprolol (bisoprolol)
Manufacturer: Merck KGaA (Germany)
Description and photo update: 2019-13-08
Prices in pharmacies: from 130 rubles.
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Concor is a selective beta 1 -adrenergic blocker.
Release form and composition
Dosage form Concor - film-coated tablets: light yellow or light orange, have a biconvex heart-shaped shape and a dividing line on both sides (5 mg or 10 mg in blisters: 10 pcs., In cartons 3 or 5 blisters; 25 pcs., in cardboard packs 2 blisters; 30 pcs., in a cardboard box 1 blister; 5 mg each, 30 pcs. in a blister, in a cardboard box 3 blisters).
The active ingredient is bisoprolol hemifumarate (bisoprolol fumarate (2: 1)):
- 1 light yellow tablet - 5 mg;
- 1 light orange tablet - 10 mg.
Auxiliary components: corn starch, anhydrous calcium hydrogen phosphate, anhydrous colloidal silicon dioxide, crospovidone, microcrystalline cellulose, magnesium stearate.
The composition of the film shell: titanium dioxide (E171), hypromellose 2910/15, dimethicone 100, macrogol 400, dye iron oxide yellow (E172).
Additionally, in the composition of the light orange film sheath - iron oxide red dye (E172).
Pharmacological properties
Pharmacodynamics
Concor is a selective beta 1 -adrenergic blocker that does not have its own sympathomimetic activity and membrane-stabilizing effect. Has a slight affinity for beta 2 -adrenergic receptors of smooth muscles of blood vessels, bronchi and beta 2 -adrenergic receptors, which are involved in the regulation of metabolism. The drug has no effect on airway resistance, as well as on metabolic processes that occur with the participation of beta 2 -adrenergic receptors.
The selective effect of bisoprolol on beta 2 -adrenergic receptors is observed outside the therapeutic range.
Bisoprolol has no pronounced negative inotropic effect. After oral administration, the maximum effect is achieved after 3-4 hours. The half-life is 10-12 hours. When using the drug once a day, the therapeutic effect lasts for 24 hours. Most often, the maximum decrease in blood pressure is achieved 2 weeks after the start of therapy.
Bisoprolol blocks beta 2 -adrenergic receptors of the heart and reduces the activity of the sympathoadrenal system.
In ischemic heart disease and in the absence of chronic heart failure, a single oral administration of bisoprolol decreases the heart rate and decreases the stroke volume of the heart, which leads to a decrease in the ejection fraction and a decrease in myocardial demand for incoming oxygen.
With long-term treatment, there is a decrease in the initially increased total peripheral vascular resistance, and the activity of renin in the blood plasma also decreases (this effect is considered one of the components of the hypotensive effect of beta-blockers).
Pharmacokinetics
- absorption: bisoprolol is absorbed from the gastrointestinal tract almost completely (over 90%). Oral bioavailability is about 90%, there is a slight "first pass" effect through the liver, in which about 10% is metabolized. Food intake does not affect bioavailability. The drug demonstrates linear kinetics, its concentration in blood plasma is proportional to the dose of bisoprolol taken in the range of 5–20 mg. The time to reach the maximum concentration in the blood plasma is about 2–3 hours;
- distribution: bisoprolol is widely distributed. The volume of distribution is 3.5 l / kg, the connection with plasma proteins is about 30%;
- metabolism: bisoprolol is metabolized by the oxidative pathway without conjugation. Bisoprolol metabolites are polar (water-soluble), excreted by the kidneys. The main metabolites found in urine and blood plasma lack pharmacological activity. The results of studies of human liver microsomes showed that in vitro bisoprolol is primarily metabolized using the CYP3A4 isoenzyme (approximately 95%), and the role of the CYP2D6 isoenzyme is insignificant;
- excretion: clearance of bisoprolol is due to the balance between excretion unchanged by the kidneys (about half of the dose) and its metabolism in the liver (about half of the dose) to metabolites excreted by the kidneys. The total clearance is 15 l / h, the half-life is 10-12 hours.
There are no data on the pharmacokinetics of Concor in patients with impaired renal or hepatic function and concurrent ischemic heart disease.
Indications for use
- Chronic heart failure;
- Arterial hypertension;
- Stable angina pectoris with ischemic heart disease.
Contraindications
- Acute form of heart failure;
- Decompensated chronic heart failure;
- Cardiogenic shock;
- Atrioventricular (AV) block II and III degree (in the absence of a pacemaker);
- Sick sinus syndrome;
- Severe bradycardia (heart rate (HR) less than 60 beats per minute);
- Severe decrease in blood pressure (BP) (systolic blood pressure below 100 mm Hg);
- Sinoatrial blockade;
- Severe bronchial asthma and chronic obstructive pulmonary disease (COPD), indicated in history;
- Raynaud's disease, severe disorders of peripheral arterial circulation;
- Metabolic acidosis;
- Pheochromocytoma (without a combination with alpha-blockers);
- Age under 18;
- Breastfeeding period;
- Hypersensitivity to drug components.
Concor should be prescribed with caution in patients with severely impaired liver function, Prinzmetal angina pectoris, type 1 diabetes mellitus and diabetes mellitus with significant fluctuations in blood glucose, hyperthyroidism, degree I AV block, psoriasis, severe renal failure (creatinine clearance less than 20 ml / min), congenital heart disease or heart valve disease with severe hemodynamic disturbances, restrictive cardiomyopathy, chronic heart failure against the background of myocardial infarction within the next 3 months, during the period of desensitizing therapy, as well as patients on a strict diet.
The use of Concor during pregnancy is possible if, according to the doctor's definition, the expected therapeutic effect for the mother outweighs the potential risk to the fetus (bisoprolol hemifumarate reduces blood flow in the placenta).
Instructions for the use of Concor: method and dosage
Concor tablets are taken orally, without chewing, with a sufficient amount of liquid. The drug should be taken once a day, in the morning, regardless of food intake.
The doctor prescribes dosage individually, taking into account the patient's condition and clinical indications.
When treating angina pectoris and arterial hypertension, the dose is selected, taking into account the patient's heart rate. It should start with 5 mg per day. If necessary, the dose can be increased to 10 mg; it is not recommended to exceed 20 mg.
Treatment of chronic heart failure is carried out according to the standard scheme, which includes combination therapy, which includes angiotensin-converting enzyme (ACE) inhibitors or angiotensin II receptor antagonists (with intolerance to ACE inhibitors), diuretics, beta-blockers, cardiac glycosides.
Concor is indicated only for stable chronic heart failure without exacerbation symptoms. Special titration phases must be completed according to a specific scheme.
The recommended starting dosage for the treatment of chronic heart failure is 1.25 mg. Further dose adjustment depends on the individual tolerance of bisoprolol and is carried out after a certain adaptation to the previous one.
The dose is increased gradually, once every 2 weeks by 1.25 mg, the maximum dose is 10 mg. The selection of the dose of Concor is carried out under the supervision of a physician and control of heart rate, blood pressure, in case of an exacerbation of the condition against the background of the last titration, the dose should be reduced to the previous one.
A temporary exacerbation of symptoms of the course of the disease, the appearance of arterial hypotension or bradycardia is possible from the first days of using the drug, during titration and treatment. In this case, it is necessary to simultaneously adjust the doses of concomitant therapy and bisoprolol, and in critical situations, cancel it until the patient's condition stabilizes. Treatment can then be continued or titrated again.
The use of Concor for all indications is long-term.
Patients with mild to moderate hepatic or renal dysfunction and elderly patients usually do not need dosage adjustment.
In severely impaired renal and liver function, the recommended daily dose should not exceed 10 mg, and increasing the dose in this category of patients is carried out with extreme caution.
Side effects
With the use of Concor, the following side effects may occur:
- From the side of the cardiovascular system: very often - bradycardia (with chronic heart failure); often - exacerbation of symptoms of chronic heart failure (with chronic heart failure), feeling of numbness or coldness in the extremities, a strong decrease in blood pressure (more often in patients with chronic heart failure); infrequently - bradycardia (with angina pectoris or arterial hypertension), impaired AV conduction, orthostatic hypotension, increased signs of chronic heart failure (with angina pectoris or arterial hypertension);
- From the digestive system: often - vomiting, nausea, diarrhea or constipation; rarely - hepatitis;
- From the nervous system: often - dizziness and headache (more often at the beginning of treatment for arterial hypertension or angina pectoris, is mild and disappears after 1-2 weeks of therapy); rarely - loss of consciousness;
- From the senses: rarely - hearing impairment, decreased lacrimation; very rarely - conjunctivitis;
- From the side of the psyche: infrequently - insomnia, depression; rarely - terrible dreams, hallucinations;
- Reproductive system disorders: rarely - potency disorders;
- From the respiratory system: infrequently - bronchospasm against the background of bronchial asthma or obstructive airway diseases in history;
- From the musculoskeletal system: infrequently - muscle cramps, muscle weakness;
- From the side of the skin: very rarely - alopecia; in patients with psoriasis - exacerbation of the disease or the appearance of a psoriasis-like rash;
- Allergic reactions: rarely - itching, skin rash, hyperemia, allergic rhinitis;
- On the part of laboratory parameters: rarely - an increase in the level of concentration of liver enzymes (alanine aminotransferase and aspartate aminotransferase) in the blood;
- Others: often - asthenia (with chronic heart failure), increased fatigue (more often at the beginning of treatment for arterial hypertension or angina pectoris, is mild and disappears after 1-2 weeks of therapy); infrequently - asthenia (with arterial hypertension or angina pectoris).
Overdose
The most common symptoms: AV block, a marked decrease in blood pressure, severe bradycardia, acute heart failure, hypoglycemia, bronchospasm.
With a single dose of a high dose of bisoprolol, sensitivity varies greatly in individual patients. Sensitivity is probably increased for patients with chronic heart failure.
In case of an overdose, you should stop taking Concor and resort to supportive symptomatic therapy.
With severe bradycardia, intravenous atropine is recommended. If these measures are not enough, a drug with a positive chronotropic effect can be administered with caution. In some cases, an artificial pacemaker is temporarily installed.
In the case of a pronounced decrease in blood pressure, intravenous administration of vasopressor drugs and plasma-substituting solutions is recommended.
In case of AV blockade, constant monitoring of the patient should be ensured and therapy with beta-adrenomimetics (for example, epinephrine) should be prescribed. In some cases, it is advisable to temporarily install an artificial pacemaker.
In case of exacerbation of the course of chronic heart failure, intravenous administration of diuretics, vasodilators and drugs with a positive inotropic effect is recommended.
For bronchospasm, bronchodilators are prescribed, including beta 2 -adrenomimetics and / or aminophylline.
For hypoglycemia, intravenous glucose (dextrose) is recommended.
special instructions
You can not abruptly stop therapy, especially for patients with coronary heart disease, the cancellation of Concor should take place by gradually reducing the dose. Dosage adjustments are made under supervision and on the recommendation of a physician.
For patients with bronchial asthma or COPD, the administration of the drug is indicated only while taking bronchodilators. With an increase in airway resistance, an increase in the dose of beta 2 -adrenomimetics is recommended for patients with bronchial asthma.
Against the background of Concor, an increase in sensitivity to allergens and the severity of anaphylactic reactions is possible, while treatment with adrenaline (epinephrine) may not have a sufficient therapeutic effect.
Before a planned surgical operation using general anesthesia, it is necessary to gradually reduce the dose of the drug and stop taking it 48 hours before the operation. The anesthesiologist should be informed about taking bisoprolol.
With pheochromocytoma, the use of the drug is possible only against the background of alpha-blockers.
The drug can mask the symptoms of hyperthyroidism.
Although Concor does not affect the patient's ability to drive vehicles and mechanisms, given the different individual tolerability of the drug and the possible violation of the condition when changing the dose, it is recommended to be careful, especially at the beginning of treatment and in the case of simultaneous alcohol consumption.
Application during pregnancy and lactation
According to the instructions, Concor is allowed to be used during pregnancy only in cases where the potential risk to the fetus is lower than the intended benefit to the mother.
Under the influence of beta-blockers, blood flow in the placenta decreases, which can affect the development of the fetus. Shows the control of blood flow in the uterus and placenta, as well as monitoring the development of the fetus. In case of diagnostics of adverse events, it is recommended to turn to alternative methods of treatment. The newborn should be examined carefully after delivery. In the first three days of life, symptoms of hypoglycemia and bradycardia may appear.
There are no data on the excretion of bisoprolol in breast milk, therefore, it is not recommended to take Concor during breastfeeding. If the use of the drug is necessary, then breastfeeding should be discontinued.
Pediatric use
It is contraindicated to use Concor for the treatment of patients under the age of 18 years.
With impaired renal function
With severe renal failure (CC up to 20 ml / min) Concor should be used with caution. With mild to moderate renal impairment, there is no need to adjust the dose.
For violations of liver function
In case of severe violations of liver function, Concor should be used with caution. The maximum dose in such patients should not exceed 10 mg. With mild to moderate liver dysfunction, there is no need to adjust the dose.
Use in the elderly
When treating elderly patients, dose adjustment is not required.
Drug interactions
When prescribing Concor, the patient must inform the doctor about all the medicines he is taking. This information will allow the doctor to take into account the possible interaction of drugs and give the patient the necessary recommendations on the rules and sequence of their use.
In the treatment of chronic heart failure, the simultaneous administration of quinidine, lidocaine, disopyramide, phenytoin, propafenone, flecainide and other class I antiarrhythmic drugs is not recommended.
Undesirable combinations for the simultaneous use of Concor:
- Diltiazem, verapamil and other blockers of slow calcium channels can cause a decrease in myocardial contractility and impaired AV conduction;
- Clonidine, moxonidine, methyldopa, rilmenidine and other centrally acting antihypertensive drugs can cause a decrease in cardiac output and heart rate and lead to vasodilation against the background of a decrease in central sympathetic tone. The likelihood of rebound arterial hypertension increases with abrupt withdrawal of the drug before the withdrawal of beta-blockers.
Special care should be taken in the treatment of angina pectoris and hypertension in combination with lidocaine, quinidine, disopyramide, flecainide, phenytoin, propafenone (class I antiarrhythmics), this combination with bisoprolol can reduce myocardial contractility and AV conduction.
Drugs, in combination with which the appointment of Concor requires special care:
- Felodipine, nifedipine, amlodipine and other dihydropyridine derivatives - increase the risk of arterial hypotension; in chronic heart failure, subsequent deterioration of the contractile function of the heart is possible;
- Non-steroidal anti-inflammatory drugs - reduce the hypotensive effect of bisoprolol;
- Amiodarone and other class III antiarrhythmic drugs - can exacerbate AV conduction disturbances;
- Beta-blockers for local use, including eye drops for the treatment of glaucoma - increase the systemic effect of bisoprolol;
- Parasympathomimetics - may increase the risk of developing bradycardia and impaired AV conduction;
- Oral hypoglycemic agents and insulin - increase their clinical effect, symptoms of hypoglycemia (tachycardia) can be suppressed or masked;
- Drugs for general anesthesia - increase the likelihood of cardiodepressant action, which can lead to arterial hypotension;
- Cardiac glycosides - can increase the duration of the impulse and lead to the development of bradycardia;
- Tricyclic antidepressants, phenothiazines, barbiturates and other drugs with an antihypertensive effect - can increase the antihypertensive effect of Concor;
- Mefloquine - increases the likelihood of developing bradycardia;
- Monoamine oxidase (MAO) inhibitors (except MAO B inhibitors) - potentiate the hypotensive effect of the drug and can cause the development of a hypertensive crisis.
The combination of Concor with isoprenaline, dobutamine and other beta-adrenergic agonists leads to a decrease in the clinical effect of both drugs.
Concomitant use of adrenergic agonists with bisoprolol that affect alpha and beta adrenergic receptors (norepinephrine, epinephrine) leads to an increase in blood pressure.
Analogs
Concor's analogues are: Bisoprolol, Bisoprolol Sandoz, Bisoprolol-Richter, Bisoprolol-Maxpharma, Biprol, Bikard, Bisokard, Bisostad, Bisoprofar, Coronal, Cordinorm, Concor Cor, Coronal.
Terms and conditions of storage
Store at temperatures up to 30 ° C. Keep out of the reach of children.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Concor
Reviews of Konkor indicate that this drug effectively lowers blood pressure and reduces heart rate. The main disadvantages of Concor, according to users, are the frequent development of side effects, withdrawal symptoms and the relatively high cost.
Price for Concor in pharmacies
The approximate price for Concor is: 50 tablets of 10 mg - 515 rubles, 30 tablets of 10 mg - 360 rubles, 50 tablets of 5 mg - 350 rubles, 30 tablets of 5 mg - 220 rubles.
Concor: prices in online pharmacies
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!