Diseases of the heart vascular system definitely needs to be treated. The main medicinal purpose is antihypertensive beta-blockers, but like other medicines, they have contraindications and side effects.
If taken for long courses, they can cause swipe according to the consistency of the reproductive system, the overwhelming effect on the synthesis of testosterone, as the main male hormone. But how does concor behave, does it have side effects for men? Can they lead to a decrease in potency, because the annotation does not say how this drug negatively affects erectile function?
Concor, what kind of medicine?
Concor is a beta-blocker, which contains bisoprolol, as active ingredient. Indications for use:
Active drug
- ischemia of the heart;
- myocardial infarction (secondary);
- arrhythmia;
- tachycardia;
- hypertension;
- heart failure;
- angina.
This is a new generation cardio drug with a small amount side effects unlike other old counterparts. Concor has an antianginal effect, helps to reduce heart rate, supply oxygen to the heart muscle, normalize blood pressure, increase vascular elasticity, and compensate for heart failure. As a result, to the normalization of pressure indicators, the elimination of tachycardia attacks.
If you neglect the doses, then side effects can be taken by surprise:
Weakness and dizziness - weakness;
- numbness of hands, feet;
- headache;
- nausea, vomiting;
- a sharp decline vision;
- increased sweating;
- slowdown heart rate;
- dysfunction of the gastrointestinal tract.
The main contraindications for use:
- heart failure;
- low pressure;
- bronchial asthma.
REFERENCE! Drowsiness and headache are the main side effects after taking Concor. It is undesirable to take the drug if you are concerned about depression, which can also be triggered during treatment. It is better to choose more gentle analogues, consult a specialist. For example, Nebivolol has similar action, but does not lead to such adverse reactions, does not adversely affect erection, reproductive functions men
Side effects
Concor belongs to the group of strong beta-blockers of the new generation. Designed to reduce pressure, but at the same time can lead to the development erectile dysfunction, other complications, side effects and effects.
When using the drug, a direct effect is on the nervous system, which in turn can provoke unpleasant symptoms:
Fatigue and sleepiness - distortion of color perception;
- drowsiness;
- dizziness;
- fear for no reason;
- chronic fatigue;
- headache;
- excessive feeling of anxiety;
- nightmares;
- chronic fatigue.
Persistent manifestations of such symptoms are not in the best way are reflected in the psycho-emotional background of men, in particular the reproductive system, resulting in impotence, disorders of erectile functions. So if at an early stage there is no ejaculation, and ejaculation comes 2-3 hours late at the time of intimacy after excitability, then over time the disease will begin to progress and erection problems may become apparent.
On a note? If there are constant depressions, suicidal tendencies while taking Concor, then it is better to refuse and look for gentle analogues with another chemical composition. If there are signs of an overdose and a toxic effect, then you need to urgently rinse the stomach, take a pill activated carbon visit a therapist, urologist
How does the drug affect potency
It can be assumed that this medication will not have a negative effect on potency, since it is recommended for use even by older men with diabetes. But, the opinion of doctors and patients is ambiguous. The whole thing is in arterial hypertension, the blow at which falls on the organs of the genitourinary system - the kidneys, blood vessels, heart. If the vessels begin to suffer, then the reproductive system will experience a shortage nutrients, and the prostate - oxygen when supplied to the tissue. If there are heart problems, then the physical state and stamina in men will be severely undermined.
The kidneys, as the main urinary organ, in the event of a malfunction, will lead to a water-salt imbalance, and these are problems with urination:
Poor urine output - departure of a sluggish stream.
- urinary retention.
- pain, pain, burning.
- incontinence at first.
Erectile function begins to gradually decline. Besides antihypertensive drugs depressing effect on testosterone synthesis. V male body concentration begins to increase, on the contrary, female hormone- estradiol. It is unlikely that with such an imbalance in hormonal background we can talk about a normal timely erection.
Is it worth looking for a replacement for concor?
A cardiac beta blocker does not have the best effect on genital area men, but proved to be effective in the treatment of vascular and heart diseases. It can become indispensable for patients with diabetes mellitus.
If we compare concor and side effects for men with other analogues, then the number of unpleasant manifestations is minimal.
Use as directed by a doctor in compliance with dosages will prevent the development of complications, severe defects:
- bronchospasm;
- heart failure;
- a sharp decrease in blood pressure;
- bradycardia;
- myocardial infarction.
According to doctors? Not Concor itself renders Negative influence on potency, namely hypertension, which leads to dysfunction of the heart muscle, deterioration of blood flow. So it begins to have a negative impact on potency. Men develop impotence. Needless to say that a healthy erection is possible only with a normal outflow of blood, tides to the cavernous bodies of the penis.
hypertension, like high pressure- enemy men's health. Fear and fear of getting sexual disorders provoke only additional psycho-emotional instability in the stronger sex. It is men after 50 who often experience complete list problems in the genital area and a lot of unpleasant manifestations.
During the clinical research it was found that there is no negative effect of concor on potency. The drug did not have the best effect on intimate life only 5% of men in old age, and those who experienced erectile dysfunction before using Concor. If we talk about the younger generation, then Bisoprolol as an active ingredient can adversely affect potency in isolated cases. This component is harmless, low-toxic.
If hypertension is not treated, then impotence will develop much faster than from taking Concor's medication. The instruction indicates that the drug reduces libido and potency, although the overwhelming effect on reproductive system high pressure can be much stronger.
How to increase potency and stabilize blood pressure
Products for potency For young guys, of course, potency is more important than blood pressure jumps. But if you completely stop taking adreno-blockers prescribed by your doctor, then high blood pressure is fraught with complications - stroke, myocardial infarction. Diseases are clearly life threatening. However, minimize negative impact on potency in men, genitourinary system, everything is possible. After all simple measures prevention, lifestyle has not been canceled.
This:
- Dieting, refusal of products that provoke an increase in pressure. Only proper nutrition prevent an increase in pressure, reduce the dosage of medications taken.
- Elimination of bad habits (alcohol, smoking), because you can reduce the dose of Concor if you refuse to drink alcohol in excess of the norm, while the pressure will not jump to high values.
- Doing active image life, because it is congestion in the pelvic area that provokes a violation of urination, at the same time - a deterioration in erection.
REFERENCE! Alcohol and tobacco lead to poisoning of the body on cellular level. Nicotine deposits in the body reduce elasticity and permeability vascular walls, worsen blood supply, provoke insufficiency of rushes of blood to cavernous bodies. The heart, blood vessels, kidneys, potency begin to suffer. Alcohol contributes to a decrease in sperm motility, a deterioration in the quality of sperm. Endogenous testosterone gradually reduces its production, fertilization and conception for men becomes problematic
Negatively influencing bad habits lead to the development of prostatitis and this is also an enemy of male ability. If the disease is not treated in time, then it is possible to live up to oncology, when there can be no question of viability in sex. If tobacco can be attributed to a fairly weak, harmless drug, then abuse, for example, marijuana can lead to damage to the chromosomes, genetic mutations in men. And this is despite the fact that this herb is of plant origin.
Doctors have a special attitude towards steroids. The effect of the application is the acceleration of protein synthesis and increased endurance, which is important for athletes. But a long, illiterate intake of these drugs is fraught with the development of erectile dysfunction, a sharp decrease in testosterone production.
If you still reconsider your lifestyle, start actively playing sports and walking more. Physical activity promotes potency, activates blood flow, normalizes metabolic processes. If there is a tendency to depression, then it will not be superfluous for men to undergo a course of psychotherapy, reconsider their behavior and outlook on life.
As for Concor, one of the side effects is excessive anxiety, an obsessive feeling of fear. Men tend to sleep, but the fear of seeing nightmares leads to depression, erectile disorders. emotional sphere and potency in men are inextricably linked. If there is a tendency to suicidal acts, then of course, you should consult a doctor. It is better to stop taking Concor and choose another optimal drug. Although in the treatment of cardiac pathologies it is quite effective, new drug unlike other analogues of the old generation with the presence more side effects.
The main thing is to take Concor, according to the instructions, do not neglect the dosages and instructions of the doctors.
Bisoprolol (INN - bisoprololum) is a selective β1-adrenergic blocker. When used in therapeutic doses, it does not have ICA and clinically significant membrane stabilizing properties. Reduces the activity of blood plasma renin, reduces myocardial oxygen demand, reduces heart rate (at rest and during exercise). By blocking β1-adrenergic receptors of the heart in low doses, it reduces the formation of cAMP from ACE stimulated by catecholamines, reduces the intracellular current of calcium ions, has a negative chrono-, dromo- and inotropic effect (inhibits conduction, excitability, slows down AV conduction). The antianginal effect is due to a decrease in myocardial oxygen demand as a result of a decrease in heart rate, a slight decrease in contractility, a prolongation of diastole, and an improvement in myocardial perfusion.
With an increase in the dose above the therapeutic one, it has a β2-adrenergic blocking effect.
Concor Cor has an antihypertensive effect due to the reduction cardiac output, inhibition of renin secretion by the kidneys, as well as the effect on the baroreceptors of the aortic arch and carotid sinus. With AH (arterial hypertension), the effect occurs after 2-5 days, a stable effect after 1-2 months. With prolonged use, bisoprolol reduces elevated OPSS.
When used in medium therapeutic doses, unlike non-selective β-blockers, it has a less pronounced effect on organs containing β2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause retention of sodium ions (Na +) in the body. The severity of the atherogenic action does not differ from the action of propranolol.
After oral administration, bisoprolol is well absorbed from the gastrointestinal tract. Bioavailability is about 90% and does not depend on food intake. The maximum concentration is reached after 1-3 hours. Plasma protein binding is about 30%.
The effect of the primary passage through the liver is expressed slightly (about 10%). About 50% of bisoprolol is biotransformed in the liver to form inactive metabolites. The main metabolites found in blood plasma and urine do not show pharmacological activity. The pharmacokinetics of bisoprolol is linear. Its plasma concentration is proportional to the administered dose in the dose range of 5 to 20 mg. The maximum plasma concentration is reached after 2-3 hours.
Bisoprolol is distributed quite widely. The volume of distribution is 3.5 l/kg. Communication with blood plasma proteins is about 35%.
The total clearance is 15.6 ± 3.2 l / h, and the renal clearance is 9.6 ± 1.6 l / h. The half-life is 10-12 hours. Approximately 98% is excreted from the body in the urine, 50% is unchanged, the rest is in the form of metabolites, approximately 2% of the dose is excreted in the feces.
Dose adjustments for patients with mild hepatic or renal impairment medium degree gravity is not required.
Indications for use of the drug Concor cor
Chronic heart failure.
The use of the drug Concor cor
The tablets should be taken with a small amount of liquid in the morning before, during or after breakfast. Tablets should not be chewed or crushed into powder.
The start of treatment of chronic heart failure with Concor Cor requires a special titration phase and regular medical supervision.
Treatment of chronic heart failure with Concor Cor begins in accordance with the following titration scheme. This may require individual adaptation depending on how well the patient tolerates the prescribed dose, i.e. the dose can be increased only if the previous dose was well tolerated.
* To ensure the above dosing regimen in the subsequent stages of treatment, it is recommended to use the drug Concor.
The maximum recommended dose in the treatment of chronic heart failure is 10 mg of bisoprolol 1 time per day. Patients are advised to take the dose of the drug selected by the doctor if no adverse reactions occur.
After starting treatment with the drug at a dose of 1.25 mg (1/2 t of a tablet of Concor Cor), the patient should be observed for about 4 hours (control of heart rate, blood pressure, conduction disturbances, signs of worsening heart failure).
During the titration phase or after it, a temporary worsening of the symptoms of heart failure, fluid retention in the body, arterial hypotension or bradycardia. In this case, it is recommended, first of all, to pay attention to the selection of the dosage of concomitant basic therapy (to optimize the dose of the diuretic and / or ACE inhibitor) before reducing the dosage of Concor Cor. Treatment with Concor Cor should be interrupted only if absolutely necessary. After stabilization of the patient's condition, re-titration should be carried out, or treatment should be continued.
Dose adjustment for patients with mild to moderate hepatic or renal impairment is usually not required. For patients with severe renal impairment (creatinine clearance less than 20 ml/min) and severe hepatic impairment daily dose should not exceed 10 mg. In any case, the dose is selected individually.
Treatment with Concor Cor is usually long-term. If necessary, treatment can be interrupted and resumed in compliance with certain rules.
Treatment should not be interrupted suddenly, especially in patients with CAD. If it is necessary to stop treatment, then the dosage of the drug should be reduced gradually.
Contraindications to the use of the drug Concor Cor
Hypersensitivity to bisoprolol or any of the components of the drug and other β-adrenergic blockers; shock ( cardiogenic shock), collapse; AV block II-III degree, sick sinus syndrome, severe sinoatrial block, bradycardia (heart rate ≤50 bpm), Prinzmetal's angina; arterial hypotension (systolic blood pressure ≤90 mm Hg), severe forms BA and COPD in history; late stages violations peripheral circulation, Raynaud's disease; simultaneous use of MAO inhibitors (with the exception of MAO inhibitors type B), psoriasis (including family history), pheochromocytoma, pregnancy and lactation.
Side effects of Concor Cor
From the side nervous system:
may be observed (especially at the beginning of therapy) fatigue, dizziness, headache, sleep disturbances, depression, rarely - hallucinations (usually mild and disappear within 1-2 weeks), sometimes - paresthesia.
From the side of the organ of vision: visual impairment, decreased tearing (should be taken into account when wearing contact lenses), conjunctivitis.
From the side of cardio-vascular system:
in some cases - orthostatic hypotension, bradycardia, AV conduction disturbances, decompensation of heart failure with the development of peripheral edema, at the beginning of treatment - worsening of the condition of patients with intermittent claudication or Raynaud's syndrome.
From the side respiratory system:
in isolated cases - shortness of breath (in patients prone to bronchospasm).
From the gastrointestinal tract: in some cases - diarrhea, constipation, nausea, abdominal pain, increased activity of liver enzymes in the blood serum (AST, ALT), hepatitis.
From the musculoskeletal system: in some cases - muscle weakness, convulsions, arthropathy with damage to one or more joints (mono- or polyarthritis).
From the side endocrine system:
decrease in glucose tolerance (with latent diabetes mellitus) and masking of signs of hypoglycemia, in some cases - an increase in the level of TG in the blood, potency disorders.
From the side of the skin: sometimes - itching, flushing of the skin, excessive sweating, rash. In the treatment of β-adrenergic blockers, hair loss, hearing impairment or tinnitus, weight gain, mood changes, short-term memory loss, allergic rhinitis, priapism are observed in some cases.
Special instructions for the use of the drug Concor cor
Concor Cor should not be used during pregnancy and lactation due to the lack of reliable clinical data confirming the safety of the drug. During pregnancy, Concor Cor should be recommended only if the benefit to the mother outweighs the risk of side effects in the fetus. In exceptional cases of the use of bisoprolol during pregnancy, treatment should be discontinued 72 hours before the expected date of delivery due to the possibility of developing bradycardia, hypoglycemia and respiratory depression in the newborn. If drug withdrawal is not possible, then after childbirth the newborn should be under medical supervision. Symptoms of hypoglycemia may occur during the first 3 days.
In some cases, β-adrenergic blockers can cause the development or exacerbation of psoriasis. In patients who take β-adrenergic blockers, anaphylactic reactions may have a more severe course due to weakened adrenergic inverse regulation.
Due to the individual nature of reactions to the drug, the ability to drive vehicles or work with mechanisms may decrease. To a greater extent this concerns initial stage treatment and changes in the dose of the drug, as well as with simultaneous use alcohol.
Clinical data on the efficacy and safety of Concor Cor in children are not available.
Interactions of the drug Concor cor
With the simultaneous use of Concor Cor can enhance the effect of antihypertensive drugs. With the simultaneous use of bisoprolol and reserpine, methyldopa, clonidine or guanfacine, a sharp decrease in heart rate is possible. At joint application Concora Cor and clonidine, digitalis preparations, as well as guanfacine, the development of cardiac conduction disorders is possible.
With the combined use of Concor and verapamil or diltiazem and others antiarrhythmic drugs possible decrease in blood pressure, increased risk of development or exacerbation of bradycardia, AV blockade, cardiac arrest and heart failure, (should be avoided in / in the introduction of blockers calcium channels and antiarrhythmic drugs against the background of Concor Cor therapy). Nifedipine can lead to a significant decrease in blood pressure.
Phenytoin for intravenous administration, drugs for inhalation general anesthesia(derivatives of hydrocarbons) increase the severity of the cardiodepressive effect and the likelihood of a decrease in blood pressure when they are used while taking bisoprolol.
Efficacy of insulin and oral hypoglycemic agents medicines may change during the treatment of Concor Cor (masks the symptoms of developing hypoglycemia: tachycardia, increased blood pressure).
Clearance of lidocaine and xanthines may decrease due to possible increase their plasma concentrations, especially in patients with initially increased clearance of theophylline under the influence of smoking.
NSAIDs, corticosteroids and estrogens weaken the hypotensive effect of bisoprolol (Na + retention, blockade of prostaglandin synthesis by the kidneys).
With the simultaneous use of Concor Cor and sympathomimetics (including in cough medicines, in eye drops and drops in the nose) the effect of bisoprolol may be weakened.
Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure.
The action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins during treatment with bisoprolol may be prolonged.
Tri- and tetracyclic antidepressants, antipsychotics(neuroleptics), ethanol, sedative and hypnotic drugs increase CNS depression. Simultaneous use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect. A break in treatment between taking MAO inhibitors and bisoprolol should be at least 14 days. Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.
Ergotamine increases the risk of developing peripheral circulatory disorders; sulfasalazine increases the concentration of bisoprolol in the blood plasma; rifampicin shortens the half-life. With the simultaneous use of ergotamine derivatives (including ergotamine-containing drugs for migraine) and Concor Cor, an increase in the severity of peripheral circulatory disorders is possible.
With the simultaneous use of Concor Cor and rifampicin, the half-life of bisoprolol may slightly decrease (an increase in the dose of Concor is usually not required).
Overdose of the drug Concor cor, symptoms and treatment
Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, AV blockade, marked decrease in blood pressure, acute heart failure, hypoglycemia, acrocyanosis, shortness of breath, bronchospasm, dizziness, fainting, convulsions.
Treatment: gastric lavage and the appointment of adsorbing drugs; symptomatic therapy: with developed AV blockade, in / in the introduction of 1-2 mg of atropine, epinephrine or setting a temporary pacemaker; at ventricular extrasystole- lidocaine (class IA drugs are not used); with a pronounced decrease in blood pressure - the patient should be in a position with a raised foot end of the bed; if there are no signs of pulmonary edema, intravenous plasma-substituting solutions; if ineffective, administration of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and eliminate a pronounced decrease in blood pressure); in heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - in / in diazepam; with bronchospasm - β 2-adrenergic stimulants by inhalation.
Storage conditions of the drug Concor cor
At room temperature not higher than 25 °C. Shelf life - 3 years.
List of pharmacies where you can buy Concor core:
- Saint Petersburg
The number of people suffering from cardiovascular diseases is steadily increasing every year in the world. For the treatment of these ailments, different medicines, for example, concor indications for the use of this drug just relate to this profile of diseases. The drug belongs to the group of cardioselective beta-blockers. Concor has been successfully used in cardiology since the early 1960s. It occupies one of the leading places by appointment among the medicines used for therapy. cardiovascular diseases.
Composition and mechanism of action of the drug
The basic component of Concor is bisoprolol, a beta-blocker. The action of the drug begins 1-3 hours after ingestion and lasts about 24 hours. Concor has a hypothetical effect by reducing cardiac output. By reducing the diastolic pressure of myocardial oxygen supply, Concor has an antianginal effect. With the systematic use of the drug, the well-being of patients improves significantly.
Indications for the use of Concor tablets
A drug with this name is prescribed for the main cardiac syndromes: arterial hypertension, coronary and heart failure, heart rhythm disturbances. The use of a coronary is advisable in the treatment of patients with left ventricular hypertrophy, symptoms of coronary disease, primarily angina pectoris, in patients who have had a myocardial infarction.
The results of clinical and pharmacological studies have proven the effectiveness of Concor in the treatment of arterial hypertension, coronary insufficiency, prevention of cardiac arrhythmias, circulatory failure. Medicine has a sufficient amount of data indicating the ability of the drug to improve the prognosis of the life of patients arterial hypertension.
Instructions for use and dosage
The medicine is available in the form of coated tablets. An annotation is enclosed in the package, which describes in detail how to take the drug. Chewing the medicine is not recommended. Concor is taken orally in the morning, on an empty stomach. The dose of the drug is prescribed individually in each hotel case, based on the patient's condition andconcomitant diseases. General recommendations for use:
- For the treatment of angina, a single daily dose of 5 mg is recommended - 1 tablet of Concor 5 mg. If necessary, the rate is increased to 10 mg.
- In the treatment of chronic heart failure, the medication is prescribed according to the scheme: 1 week - 1.25 mg of Concor, 2 - 2.5 mg, 3 - 3.75 mg, from 4 to 7 - 5 mg, from 8 to 11 - 7.5 mg, starting with 12 - 10 mg.
- Patients with arterial hypertension, cardiac arrhythmias, circulatory failure are prescribed 2.5 mg per day. Maximum dose- 20 mg.
Side effects and contraindications
Unwanted Effects, developing as a result of taking concor, are extremely a rare thing observed in 1% of patients. In other people, subject to the recommended dosage, the treatment is positive, without side effects. If during therapy with Concor you identify in yourself anxiety symptoms or feel discomfort, immediately seek advice from your doctor. He evaluates the feasibility further treatment with this drug. Side effects:
- fatigue, dizziness, headaches, sleep disturbance, depression, nightmares, rare cases- hallucinations;
- violation of lacrimation, non-infectious conjunctivitis;
- bradycardia, orthostatic hypotension;
- shortness of breath, apnea, difficulty breathing;
- diarrhea, constipation, nausea, vomiting, colic;
- impotence;
- feeling cold, numbness of the extremities;
- hearing loss;
- allergic rhinitis;
- skin redness, itching, peeling;
- muscle weakness cramps;
- hepatitis.
Systematic and long-term therapy Concor significantly improves the course of diseases, reduces the likelihood of complications, and prolongs the life of people. The drug is contraindicated in pregnant women, nursing mothers, patients with state of shock, under anesthesia, during a strict diet. The drug is prescribed with caution to patients suffering from:
- diabetes mellitus;
- Prinzmetal's angina;
- violation of peripheral circulation;
- arterial hypotension;
- bronchial asthma;
- psoriasis;
- pheochromocytoma.
Analogues of the drug Concor
In therapy cardiac diseases substitute tablets are medicines containing bisoprolol, or belonging to the group of selective drugs. Such drugs have a similar effect, but differ in dosage, contraindications, side effects. Selective drugs that replace Concor are:
- bisogamma;
- coronal;
- bisocard;
- aritel;
- bidop;
- biol;
- bisoprolol;
- cordinorm;
- coronal;
- niperten;
- tirese;
- corbis;
- bisomor.
Where to buy and how much do the pills cost
Concor is sold freely in pharmacies, sold without a doctor's prescription. The cost of the drug varies from 179 to 200 rubles. for a pack of 2.5 mg tablets, 30 pcs., from 230 to 426 rubles. - 5 mg 30 pcs., from 342 to 456 rubles. - 5 mg 50 pcs., from 490 to 465 rubles. - 10 mg 30 pcs. The price of the medicine depends on the manufacturer (Norway, Hungary or Germany). Before taking Concor, consult with your doctor and carefully study the annotation.
Trade name of the drug: Concor ®
International non-proprietary name:
bisoprololDosage form:
coated tablets film sheathCompound:
1 film-coated tablet, 5 mg contains:
Core
Active substance: bisoprolol fumarate 2:1 (bisoprolol hemifumarate) - 5 mg
Excipients:
shell
Iron dye yellow oxide (E 172), dimethicone 100, macrogol 400, titanium dioxide (E 171), hypromellose 2910/15.
1 film-coated tablet, 10 mg contains:
Core
Active substance: bisoprolol fumarate 2:1 (bisoprolol hemifumarate) - 10 mg
Excipients: anhydrous colloidal silicon dioxide, magnesium stearate, crospovidone, microcrystalline cellulose, corn starch, anhydrous calcium hydrogen phosphate.
shell
Iron dye red oxide (E 172), iron dye yellow oxide (E 172), dimethicone 100, macrogol 400, titanium dioxide (E 171), hypromellose 2910/15.
Description
Film-coated tablets, 5 mg:
Pale yellow, heart-shaped, biconvex, film-coated tablets scored on both sides.
Film-coated tablets, 10 mg:
Light orange, heart-shaped, biconvex film-coated tablets, scored on both sides.
Pharmacotherapeutic group:
beta 1 - selective blockerATX code: C07AB07
Pharmacotherapeutic properties
Pharmacodynamics
Selective beta 1 - blocker, without its own sympathomimetic activity, does not have a membrane stabilizing effect. Reduces plasma renin activity, reduces myocardial oxygen demand, reduces heart rate (HR) (at rest and during exercise). It has antihypertensive, antiarrhythmic and antianginal effects. Blocking in low doses beta 1-adrenergic receptors of the heart, it reduces the formation of cAMP from ATP stimulated by catecholamines, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect (inhibits conduction and excitability, slows down atrioventricular conduction).
With an increase in the dose above the therapeutic one, it has a beta 2 -adrenergic blocking effect.
The total peripheral vascular resistance at the beginning of the drug, in the first 24 hours, slightly increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors), which after 1-3 days returns to the original, and decreases with long-term administration.
The hypotensive effect is associated with a decrease in the minute volume of blood, sympathetic stimulation of peripheral vessels, a decrease in the activity of the renin-angiotensin system (has great importance for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease blood pressure(BP) and influence on the central nervous system (CNS). With arterial hypertension, the effect occurs after 2-5 days, stable action - after 1-2 months.
The antianginal effect is due to a decrease in myocardial oxygen demand as a result of a decrease in heart rate, a slight decrease in contractility, a prolongation of diastole, and an improvement in myocardial perfusion. The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity sympathetic nervous system, increased levels of cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown in atrioventricular (AV) conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through the atrioventricular node) and along additional pathways.
When used in medium therapeutic doses, unlike non-selective beta-blockers, it has a less pronounced effect on organs containing beta 2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause retention of sodium ions (Na+) in the body.
Pharmacokinetics
Suction. Bisoprolol is almost completely (>90%) absorbed from gastrointestinal tract. Its bioavailability due to negligible "first pass" metabolism through the liver (at the level of about 10%-15%) is about 85-90% after oral administration. Eating does not affect bioavailability. Bisoprolol exhibits linear kinetics, with plasma concentrations being proportional to the administered dose over the dose range of 5 to 20 mg. The maximum plasma concentration is reached after 2-3 hours.
Distribution. Bisoprolol is distributed quite widely. The volume of distribution is 3.5 l/kg. Communication with proteins of a blood plasma reaches approximately 35%; capture by blood cells is not observed.
Metabolism. Metabolized by the oxidative pathway without subsequent conjugation. All metabolites are highly polar and are excreted by the kidneys. The main metabolites found in blood plasma and urine do not show pharmacological activity. Data obtained from experiments with human liver microsomes in vitro show that bisoprolol is metabolized primarily by CYP3A4 (about 95%), and CYP2D6 plays only a small role.
Withdrawal. The clearance of bisoprolol is determined by the balance between its excretion through the kidneys in the form of an unchanged substance (about 50%) and oxidation in the liver (about 50%) to metabolites, which are then also excreted by the kidneys. The total clearance is 15.6 ± 3.2 l / h, and the renal clearance is 9.6 ± 1.6 l / h. The half-life is 10-12 hours.
Indications for use
The drug Concor ® should not be used to treat patients with the following conditions:
Carefully: liver failure, chronic kidney failure, Prinzmetal's angina; myasthenia gravis, thyrotoxicosis, diabetes, atrioventricular block I degree, depression (including history), psoriasis, elderly age. Use during pregnancy and lactation
During pregnancy, Concor should only be recommended if the benefit to the mother outweighs the risk of side effects in the fetus.
As a rule, beta-blockers reduce blood flow in the placenta and may affect the development of the fetus. The blood flow in the placenta and uterus should be carefully monitored, as well as the growth and development of the unborn child, and in the case dangerous manifestations regarding pregnancy or fetus, take alternative therapeutic measures. The newborn should be carefully examined after delivery. In the first three days of life, symptoms of low blood glucose and heart rate may occur. Data on the excretion of bisoprolol in breast milk or the safety of exposure to bisoprolol in infants is not. Therefore, taking Concor is not recommended for women during breastfeeding. Dosage and administration
The tablets should be taken with a small amount of liquid in the morning before, during or after breakfast. Tablets should not be chewed or crushed into powder. Treatment of arterial hypertension and angina pectoris
In all cases, the regimen and dosage is selected by the doctor for each patient individually, in particular, taking into account the heart rate and the patient's condition.
The usual starting dose is 5 mg (1 tablet Concor ® 5 mg) once a day. If necessary, the dosage can be increased to 10 mg once a day.
In the treatment of arterial hypertension and angina pectoris, the maximum recommended dose is 20 mg Concor ® once a day. Treatment of chronic heart failure
The beginning of the treatment of chronic heart failure with Concor ® requires a special titration phase and regular medical supervision.
Prerequisites for treatment with Concor ® the following:
Treatment of chronic heart failure with Concor ® begins in accordance with the following titration scheme. This may require individual adaptation depending on how well the patient tolerates the prescribed dose, i.e. the dose can be increased only if the previous dose was well tolerated.
* To ensure the above dosing regimen at subsequent stages of treatment, it is recommended to use the drug Concor ® .
The maximum recommended dose in the treatment of chronic heart failure is 10 mg Concor ® 1 time per day. Patients are advised to take the dose of the drug selected by the doctor if no adverse reactions occur.
After starting treatment with the drug at a dose of 1.25 mg (1/2 tablet of Concor KOR), the patient should be observed for about 4 hours (control of heart rate, blood pressure, conduction disturbances, signs of worsening heart failure).
During the titration phase or after it, a temporary worsening of the course of heart failure, fluid retention in the body, arterial hypotension or bradycardia may occur. In this case, it is recommended, first of all, to pay attention to the selection of the dosage of concomitant basic therapy (optimize the dose of diuretic and / or ACE inhibitor) before reducing the dosage of Concor ® . Treatment with Concor ® should be interrupted only if absolutely necessary.
After stabilization of the patient's condition, re-titration should be carried out, or treatment should be continued. Duration of treatment for all indications
Treatment with Concor ® is usually a long-term therapy. If necessary, treatment can be interrupted and resumed subject to certain rules.
Treatment should not be interrupted suddenly, especially in patients with ischemic disease hearts. If it is necessary to stop treatment, then the dosage of the drug should be reduced gradually. Special groups patients
Impaired kidney or liver function:
Treatment of arterial hypertension or angina pectoris:
Elderly patients:
Dose adjustment is not required. Side effect
Frequency adverse reactions, given below, was determined according to the following:
-very often: ≥1/10;
- often: >1/100.<1/10;
- infrequently:> 1/1000.<1/100:
-rarely: >1/10 OOO.<1/1000:
-rarely:<1/10 ООО. включая отдельные сообщения. The cardiovascular system
Very often: decrease in heart rate (bradycardia, especially in patients with chronic heart failure); often: arterial hypotension (especially in patients with chronic heart failure), manifestation of angiospasm (increased peripheral circulatory disorders, feeling of coldness in the extremities (paresthesia); infrequently: impaired atrioventricular conduction, orthostatic hypotension, decompensation of heart failure with the development of peripheral edema. Nervous system
At the beginning of the course of treatment, disorders of the central nervous system may temporarily appear, infrequently: dizziness, headache, asthenia, increased fatigue, sleep disturbances. as well as mental disorders (infrequently - depression, rarely hallucinations, nightmares, convulsions). Usually these phenomena are mild and disappear, as a rule, within 1-2 weeks after the start of treatment. organs of vision
Rare: blurred vision, decreased tearing (should be taken into account when wearing contact lenses): very rarely: conjunctivitis. Respiratory system
Rare: allergic rhinitis. Uncommon: Bronchospasm in patients with asthma or obstructive airway disease. Gastrointestinal tract
Often: nausea, vomiting, diarrhea, constipation, dryness of the oral mucosa; rarely: hepatitis. Musculoskeletal system
Infrequently: muscle weakness, cramps in the calf muscles, arthralgia. allergic reactions
Rare: hypersensitivity reactions such as pruritus. skin redness, sweating, rash. Very rare: alopecia. Beta-blockers can exacerbate psoriasis. genitourinary system
Very rare: erectile dysfunction. Laboratory indicators
Rarely: increased levels of liver enzymes in the blood (ACT, ALT), increased levels of triglycerides in the blood. In some cases: thrombocytopenia, agranulocytosis. Overdose
Symptoms: arrhythmia, ventricular extrasystole, severe bradycardia, atrioventricular block. pronounced decrease in blood pressure, acute heart failure, hypoglycemia, acrocyanosis, difficulty breathing, bronchospasm, dizziness, fainting, convulsions.
Treatment: gastric lavage and the appointment of adsorbing drugs; symptomatic therapy: with developed atrioventricular blockade - intravenous administration of 1-2 mg of atropine, epinephrine or setting up a temporary pacemaker; with ventricular extrasystole - lidocaine (class IA drugs are not used); with a pronounced decrease in blood pressure - the patient should be in the Trendelenburg position; if there are no signs of pulmonary edema - plasma-substituting solutions intravenously, if ineffective - the introduction of epinephrine, dopamine, dobutamine (to maintain the chronotropic and inotropic action and eliminate a pronounced decrease in blood pressure); in heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - intravenous diazepam; with bronchospasm - beta 2 - adrenostimulants inhalation. Interaction with other drugs
The effectiveness and tolerability of drugs may be affected by the simultaneous use of other drugs. Such an interaction can also occur when two drugs are taken after a short period of time. The doctor must be informed that you are taking other medicines, even if you are taking them without a prescription.
Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol.
Iodine-containing radiopaque diagnostic agents for intravenous administration increase the risk of developing anaphylactic reactions.
Phenytoin when administered intravenously, drugs for inhalation general anesthesia (hydrocarbon derivatives) increase the severity of the cardiodepressive effect and the likelihood of lowering blood pressure.
The effectiveness of insulin and oral hypoglycemic drugs may change during treatment with bisoprolol (masks the symptoms of developing hypoglycemia: tachycardia, increased blood pressure).
The clearance of lidocaine and xanthines (except for difillin) may decrease due to a possible increase in their plasma concentration, especially in patients with initially increased clearance of theophylline under the influence of smoking. Non-steroidal anti-inflammatory drugs, glucocorticosteroids and estrogens weaken the hypotensive effect of bisoprolol (Na + retention, blockade of prostaglandin synthesis by the kidneys).
Cardiac glycosides, methyldopa, reserpine and guanfacine, calcium channel blockers (verapamil, diltiazem), amiodarone and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, atrioventricular block, cardiac arrest and heart failure.
Nifedipine can lead to a significant decrease in blood pressure.
Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure.
The action of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins during treatment with bisoprolol may be prolonged.
Tri- and tetracyclic antidepressants, antipsychotics (neuroleptics), ethanol, sedatives and hypnotics increase CNS depression. Simultaneous use with MAO inhibitors is not recommended due to a significant increase in the hypotensive effect. A break in treatment between taking MAO inhibitors and bisoprolol should be at least 14 days. Non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.
Ergotamine increases the risk of developing peripheral circulatory disorders; sulfasalazine increases the concentration of bisoprolol in the blood plasma; rifampicin shortens the half-life. special instructions
Do not stop treatment abruptly and do not change the recommended dosage without first consulting your doctor, as this can lead to a temporary deterioration in the activity of the heart. Treatment should not be interrupted suddenly, especially in patients with ischemic heart disease. If discontinuation of treatment is necessary, the dosage should be reduced gradually.
Monitoring the condition of patients taking Concor ® should include measuring heart rate and blood pressure (at the beginning of treatment - daily, then 1 time in 3-4 months), ECG, determination of blood glucose in patients with diabetes mellitus (1 time in 4-5 months ). In elderly patients, it is recommended to monitor kidney function (1 time in 4-5 months). The patient should be taught how to calculate heart rate and instruct about the need for medical advice if the heart rate is less than 50 bpm.
Before starting treatment, it is recommended to conduct a study of the function of external respiration in patients with a burdened bronchopulmonary history.
Patients using contact lenses should take into account that during treatment, a decrease in the production of lacrimal fluid is possible.
When used in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (if effective alpha-blockade has not been previously achieved). In thyrotoxicosis, Concor ® may mask certain clinical signs of thyrotoxicosis (eg, tachycardia). Abrupt discontinuation of the drug in patients with thyrotoxicosis is contraindicated, as it can exacerbate symptoms. In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal levels.
While taking clonidine, its reception can be stopped only a few days after the abolition of Concor ® .
It is possible to increase the severity of the hypersensitivity reaction and the lack of effect from the usual doses of epinephrine against the background of an aggravated allergic history. If it is necessary to carry out planned surgical treatment, the drug should be discontinued 48 hours before general anesthesia. If the patient took the drug before surgery, he should choose a drug for general anesthesia with a minimally negative inotropic effect.
Reciprocal activation of the vagus nerve can be eliminated by intravenous atropine (1-2 mg).
Drugs that reduce catecholamine reserves (including reserpine) can enhance the effect of beta-blockers, so patients taking such combinations of drugs should be under constant medical supervision to detect a pronounced decrease in blood pressure or bradycardia. Patients with bronchospastic diseases can be prescribed cardioselective blockers in case of intolerance and / or ineffectiveness of other antihypertensive drugs. If the dose of the drug is exceeded, there is a risk of developing bronchospasm.
If increasing bradycardia (heart rate less than 50 beats / min.), A pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), atrioventricular blockade is detected in elderly patients, it is necessary to reduce the dose or stop treatment. It is recommended to stop therapy if depression develops.
You can not abruptly interrupt treatment because of the risk of developing severe arrhythmias and myocardial infarction. Cancellation of the drug is carried out gradually, reducing the dose for 2 weeks or more (reduce the dose by 25% in 3-4 days). It is necessary to cancel the drug before examining the content of catecholamines, normetanephrine and vanillinmandelic acid in the blood and urine; titers of antinuclear antibodies. Influence on the ability to drive a car and complex mechanisms
Bisoprolol does not affect the ability to drive a car in the study of patients suffering from diseases of the coronary vessels of the heart. However, due to individual reactions, the ability to drive a car or work with technically complex mechanisms may be impaired. Particular attention should be paid to this at the beginning of treatment, after changing the dose, and also with the simultaneous use of alcohol. Release form
Film-coated tablets, 5 and 10 mg.
10 tablets in a blister of aluminum foil and PVC, 3, 5 or 10 blisters, together with instructions for use, are placed in a cardboard box. Storage conditions
Store at a temperature not exceeding 30°C.
Keep out of the reach of children. Best before date
5 years. Do not use after the expiration date. Terms of dispensing from pharmacies
On prescription. Manufacturer
Merck KGaA, Germany Manufacturer's address:
Frankfurter Strasse 250 64293 Darmstadt, Germany
Frankfurterstrasse 250 64293 Darmstadt, Germany Presented in Russia and the CIS:
"Nycomed Austria GmbH", Austria: 119048 Moscow, st. Usacheva, d. 2, building 1
