Bisoprolol

The effectiveness and tolerability of bisoprolol may be affected by concomitant use of other medications. This interaction can also occur when two drugs are taken within a short period of time. The doctor must be informed about taking other medications, even if taken without a doctor's prescription (i.e., over-the-counter drugs).

Combinations not recommended

Treatment of CHF

Class I antiarrhythmic drugs (for example, quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone), when used simultaneously with bisoprolol, can reduce AV conduction and myocardial contractility.

All indications for use of the drug Bisoprolol

Blockers of “slow” calcium channels (SCBC) such as verapamil and, to a lesser extent, diltiazem, when used simultaneously with bisoprolol, can lead to a decrease in myocardial contractility and impaired AV conduction. In particular, intravenous administration of verapamil to patients taking beta-blockers can lead to severe arterial hypotension and impaired AV conduction.

Centrally acting antihypertensives (such as clonidine, methyldopa, moxonidine, rilmenidine) can lead to a decrease in heart rate and cardiac output, as well as vasodilation due to a decrease in central sympathetic tone. Abrupt withdrawal, especially before discontinuation of beta-blockers, may increase the risk of developing “rebound” arterial hypertension.

Combinations requiring special caution

Treatment of arterial hypertension and angina pectoris

All indications for use of the drug Bisoprolol

BMCC dihydropyridine derivatives (for example, nifedipine, felodipine, amlodipine) when used simultaneously with bisoprolol may increase the risk of arterial hypotension. In patients with CHF, the risk of subsequent deterioration in cardiac contractility cannot be excluded. Class III antiarrhythmic drugs (eg, amiodarone) may worsen AV conduction disturbances.

The effect of beta-blockers for topical use (for example, eye drops for the treatment of glaucoma) may enhance the systemic effects of bisoprolol (lowering blood pressure, lowering heart rate).

Parasympathomimetics, when used simultaneously with bisoprolol, may enhance AV conduction disturbances and increase the risk of developing bradycardia.

The hypoglycemic effect of insulin or oral hypoglycemic agents may be enhanced. Signs of hypoglycemia - in particular tachycardia - may be masked or suppressed. Such interactions are more likely when using non-selective beta-blockers.

Agents for general anesthesia may increase the risk of cardiodepressive effects, leading to arterial hypotension (see section "Special Instructions").

Cardiac glycosides, when used simultaneously with bisoprolol, can lead to an increase in impulse conduction time, and thus to the development of bradycardia.

Nonsteroidal anti-inflammatory drugs (NSAIDs) may reduce the antihypertensive effect of bisoprolol.

The simultaneous use of Bisoprolol with beta-agonists (for example, isoprenaline, dobutamine) may lead to a decrease in the effect of both drugs.

The combination of bisoprolol with adrenergic agonists that affect beta and alpha adrenergic receptors (for example, norepinephrine, epinephrine) may enhance the vasoconstrictor effects of these drugs that occur with the participation of alpha adrenergic receptors, leading to an increase in blood pressure. Such interactions are more likely when using non-selective beta-blockers.

Antihypertensive drugs, as well as other drugs with a possible antihypertensive effect (for example, tricyclic antidepressants, barbiturates, phenothiazines) may enhance the antihypertensive effect of bisoprolol.

Mefloquine, when used simultaneously with bisoprolol, may increase the risk of bradycardia.

MAO inhibitors (except MAO B inhibitors) may enhance the antihypertensive effect of beta-blockers. Concomitant use may also lead to the development of a hypertensive crisis.

Allergens used for immunotherapy or allergen extracts used in skin testing increase the risk of anaphylactic reactions.

The clearance of lidocaine and xanthines (except theophylline) may be reduced due to a possible increase in their concentration in the blood plasma, especially in patients with an initially increased clearance of theophylline under the influence of smoking.

The effect of non-depolarizing muscle relaxants and the anticoagulant effect of coumarins may be prolonged during treatment with bisoprolol.

When used simultaneously with rifampicin, a slight decrease in the half-life of bisoprolol is possible due to the induction of hepatic isoenzymes of cytochrome P450 by rifampicin. Usually no dose adjustment is required.

Non-hydrogenated ergot alkaloids and ergotamine increase the risk of developing peripheral circulatory disorders.

Sulfasalazine increases the concentration of bisoprolol in the blood plasma.

BISOPROLOL-PRANA (tablets)

and with all this, the pressure drops sharply - to 90/40, and the pulse at the same time - 163 beats per minute, Oy!
And it has happened that after a minor load, for example playing volleyball, something similar happens. At first this happened once every six months and I did not pay attention to it, but after this phenomenon began to repeat almost every month, I was forced to see a doctor. The cardiologist wrote out a prescription and at the same time a referral for examination and treatment to the hospital, and that’s how I ended up in the cardiology department of the hospital. And after discharge, I discovered in the epicrisis, signed by the head of the department, that I needed to take Bisoprolol tablets for a year, half a tablet of 5 mg dosage once a day every day. The diagnosis is tachycardia, the pills seem to be suitable, but the annotation says that in addition to lowering the heart rate, they also reduce blood pressure, and my blood pressure has always been slightly below normal -110/70. Therefore, I was very surprised when I discovered this drug at home, in the discharge summary, and just in case, I went to the clinic, also to a cardiologist, for a consultation. The doctor firmly assured and confirmed that this medicine would suit me and there was no reason to worry. Although I laughed that Bisoprolol is somewhat outdated today and now there are more modern analogues, and indeed on the Internet I found information that Bisoprolol was discovered back in the sixties of the last century. But there are few side effects, “relatively” of course, and what worried me most was the situation with blood pressure. Probably in my eyes, after all, the doctor read the doubts and immediately offered to get this drug for free at the departmental pharmacy and wrote out a prescription for it. I had to agree, there is only one life. This box contained 3 plates of ten tablets each. I cut the tablets in half every morning with a knife along the line marked on them. In principle, it’s convenient, and I put the remaining half of the tablet back into the blister for storage. Well, I washed them down with water from this cooler. The package lasted me exactly two months. Our medicine’s manufacturer is the pharmaceutical company Pranafarm LLC, Samara. I can’t describe the taste of the tablets, since I swallowed them without chewing. This is what the doctor prescribed, and I had no desire to chew them. Probably bitter, like all pills. And now about health. The pills helped. My heart calmed down, my blood pressure did not drop two months after I started taking Bisoprolol, and my health improved. True, I just can’t forget the words of the head of the cardiology department upon discharge from the hospital: “We will meet again.” Now I decided to take a short break from taking Bisoprolol, let my tummy rest a little from the chemicals. The bottom line is clear to me: the medicine is good, but I will not recommend it, do not self-medicate, go to the doctor if you find similar symptoms as mine, although it helped me. Don't get sick, take care of yourself, have a good mood.

Bisoprolol-Prana, 30 pcs., 10 mg, film-coated tablets

Monitoring of patients taking the drug BISOPROLOL-PRANA should include measuring heart rate and blood pressure (at the beginning of treatment - daily, then - once every 3-4 months), conducting an ECG, determining the concentration of glucose in the blood in patients with diabetes mellitus (once every 4 months). -5 months). In elderly patients, it is recommended to monitor renal function (once every 4–5 months).

The patient should be taught how to calculate heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min.

Before starting treatment, it is recommended to conduct a study of external respiratory function in patients with a burdened bronchopulmonary history.

In approximately 20% of patients with angina, β-blockers are ineffective. The main reasons: severe coronary atherosclerosis with a low ischemic threshold (heart rate less than 100 beats/min) and increased end-diastolic volume of the left ventricle, disrupting subendocardial blood flow.

In smokers, the effectiveness of β-blockers is lower.

Patients using contact lenses should take into account that during treatment the production of tear fluid may decrease.

When used in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (if effective α-blockade is not previously achieved).

In thyrotoxicosis, bisoprolol may mask certain clinical signs of thyrotoxicosis (for example, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated because it can increase symptoms.

In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not enhance insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentrations to normal levels.

When taking clonidine at the same time, it can be discontinued only a few days after discontinuation of the drug BISOPROLOL-PRANA.

It is possible that the severity of the hypersensitivity reaction may increase and there will be no effect from usual doses of epinephrine against the background of a burdened allergic history.

If planned surgical treatment is necessary, the drug should be discontinued 48 hours before the start of general anesthesia. If the patient took the drug before surgery, he should choose a drug for general anesthesia with minimal negative inotropic effect.

Reciprocal activation of the vagus nerve can be reversed by intravenous atropine (1–2 mg).

Medicines that reduce the supply of catecholamines (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 β-blockers in case of intolerance and/or ineffectiveness of other antihypertensive drugs. Overdose is dangerous for the development of bronchospasm.

If increasing bradycardia (less than 50 beats/min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), or AV blockade is detected in elderly patients, it is necessary to reduce the dose or stop treatment.

It is recommended to discontinue therapy if depression develops.

Treatment should not be abruptly interrupted due to the risk of developing withdrawal syndrome (severe arrhythmias and myocardial infarction). Cancellation is carried out gradually, reducing the dose over 2 weeks or more (reduce the dose by 25% in 3-4 days). It should be discontinued before testing the content of catecholamines, normetanephrine and vanillylmandelic acid in the blood and urine, and titers of antinuclear antibodies.

Effect on the ability to drive a car and other mechanical means

The question of the possibility of engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions should be decided only after assessing the patient’s individual response to the drug (especially at the beginning of treatment, due to the possibility of developing dizziness).

Bisoprolol tablet p/o film 2.5 mg 30 pcs vertex

Pharmacological group:

Beta1-adrenergic blocker selective.
Pharmacodynamics:
Bisoprolol is a selective beta1-blocker without its own sympathomimetic activity and does not have a membrane-stabilizing effect. Reduces plasma renin activity, reduces myocardial oxygen demand, and reduces heart rate (heart rate) (at rest and during exercise). It has antihypertensive, antiarrhythmic and antianginal effects. By blocking beta1-adrenergic receptors of the heart in low doses, it reduces the catecholamine-stimulated formation of cyclic denosine monophosphate (cAMP) from adenosine triphosphate, reduces the intracellular flow of calcium ions, has a negative chrono-, dromo-, bathmo- and inotropic effect (inhibits conductivity and excitability, slows down the atrioventricular (AV) ) conductivity).

When increasing the dose above the therapeutic one, it has a beta2-adrenergic blocking effect.

Total peripheral vascular resistance at the beginning of drug use (in the first 24 hours) increases slightly (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors), after 1-3 days it returns to the original level, and with long-term use it decreases.

The antihypertensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, a decrease in the activity of the sympathoadrenal system (of great importance for patients with initial hypersecretion of renin), restoration of sensitivity in response to a decrease in blood pressure (BP) and an effect on the central nervous system (CNS) . In case of arterial hypertension, the effect occurs after 2-5 days, stable effect – 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, prolongation of diastole, and improved myocardial perfusion.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown of AV conduction (mainly in the antegrade and, to a lesser extent, in the retrograde directions through AV node) and along additional paths.

When used in average therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on organs containing beta2-adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate metabolism, does not cause delay sodium ions in the body.

The maximum effect of the drug is achieved 3-4 hours after oral administration. Even when bisoprolol is prescribed once a day, its therapeutic effect persists for 24 hours, thanks to a 10-12-hour half-life (T1/2) from the blood plasma. As a rule, the maximum reduction in blood pressure is achieved 2 weeks after the start of treatment.

Pharmacokinetics:

Suction

Bisoprolol is almost completely (more than 90%) absorbed from the gastrointestinal tract. Its bioavailability due to negligible first pass metabolism through the liver (at approximately 10%) is approximately 90% after oral administration. Eating does not affect absorption. Bisoprolol exhibits linear kinetics, with its plasma concentrations being proportional to the dose taken in the range from 5 to 20 mg. The maximum concentration in blood plasma is achieved after 2-3 hours.

Distribution

Bisoprolol is distributed quite widely. The volume of distribution is 3.5 l/kg. The binding to plasma proteins reaches approximately 35%; no uptake by blood cells is observed. Permeability through the blood-brain barrier and placental barrier is low.

Metabolism

Metabolized via the oxidative pathway without subsequent conjugation. All metabolites have strong polarity and are excreted by the kidneys. The main metabolites found in blood plasma and urine do not exhibit pharmacological activity. Data obtained from experiments with human liver microsomes in vitro show that bisoprolol is metabolized primarily by the CYP3A4 isoenzyme (about 95%), with the CYP2D6 isoenzyme playing only a minor role.

Removal

The clearance of bisoprolol is determined by the balance between its excretion through the kidneys in the form of 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/hour, with renal clearance being 9.6 ± 1.6 l/hour. T1/2 is 10-12 hours.

Pharmacokinetics in special groups of patients

Patients with impaired liver and kidney function

Since excretion occurs equally in the kidneys and liver, no dosage adjustment is required in patients with impaired liver function or renal failure.

Elderly patients

The pharmacokinetics of bisoprolol is linear and does not depend on age.

Patients with chronic heart failure (CHF) In patients with CHF, the level of bisoprolol in the blood plasma is higher, and T1/2 increases to 17 hours compared to healthy volunteers.

There is no information on the pharmacokinetics of bisoprolol in patients with CHF and concurrent impairment of liver or kidney function.

How to take Bisoprolol

Bisoprolol should be taken exactly as prescribed by your doctor.

If you have any doubts about taking the drug, you should consult your doctor or pharmacist before use.

Treatment with Bisoprolol requires regular medical supervision. This is especially important at the beginning of treatment, during dose increases and when stopping treatment.

Bisoprolol tablets should be taken with a small amount of water in the morning, with or without food. Do not crush or chew the tablets.

Treatment with Bisoprolol is usually long-term.

Adults including the elderly:

Treatment with Bisoprolol should start with a low dose and increase gradually.

Your doctor will decide how to increase your dose and this is usually done as follows:

1.25 mg bisoprolol once a day for one week, then
2.5 mg bisoprolol once a day for one week, then
3.75 mg bisoprolol once a day for one week, then
5 mg bisoprolol once a day for four weeks, then
7.5 mg bisoprolol once a day for four weeks, then
10 mg bisoprolol once daily for maintenance therapy

The maximum recommended daily dose is 10 mg of bisoprolol.

Depending on how well you tolerate the drug, your doctor may also decide to lengthen the interval between dose increases. If your condition worsens or you can no longer tolerate the effects of this drug, you may need to reduce your dose or stop treatment. In some patients, a maintenance dose of less than 10 mg of bisoprolol may be sufficient.

Usually the doctor's prescription is correct in this situation.

If you must stop treatment completely, your doctor will, as usual, advise you to gradually reduce your dose as otherwise your condition may worsen.

If you have used more Bisoprolol than recommended

If you take more Bisoprolol tablets than recommended, immediately tell your doctor. Your doctor will decide what measures are needed.

Symptoms of overdose may include palpitations, difficulty breathing, dizziness, or trembling (due to low blood sugar).

If you forget to take Bisoprolol

Do not take a double dose to make up for a missed dose. Take your scheduled dose the next morning.

If you stop taking Bisoprolol a

You should not stop taking bisoprolol unless your doctor advises you to. Otherwise, your condition may become much worse.

If you have any additional questions about the use of the drug, you should contact your doctor or pharmacist.

Possible side effects

Like other medicines, bisoprolol can cause side effects, although not everyone gets them.

To prevent serious side effects from developing, talk to your doctor right away if side effects are severe, develop suddenly, or get worse quickly.

The most serious side effects related to cardiac function are:

slow heart rate or bradycardia (may affect more than 1 in 10 people),
worsening heart failure (may affect 1 in 10 people),
slow or irregular heartbeat (may affect 1 in 100 people).

If you experience dizziness, or weakness, or difficulty breathing, please tell your doctor as soon as possible.

Additional side effects are listed by frequency of occurrence.

Common (may occur in 1 in 10 people);

fatigue, weakness, dizziness, headache,
feeling of coldness or numbness in the arms or legs,
low blood pressure,
gastrointestinal problems such as nausea, vomiting, diarrhea or constipation.

Uncommon (may affect 1 in 100 people):

sleep disorders,
depression,
dizziness when standing up
respiratory problems in patients with bronchial asthma or chronic lung diseases,
muscle weakness, muscle cramps.

Rare (may affect 1 in 1,000 people):

hearing problems,
allergic rhinitis,
reduction of lacrimation,
inflammation of the liver, which can lead to yellowing of the skin or whites of the eyes,
disturbances in the levels of various lipids and liver markers in the blood,
allergic reactions such as itching, swelling, rash,
erectile dysfunction,
nightmares, hallucinations,
fainting.

Very rare (may affect 1 in 10,000 people):

irritation and redness of the eyes (conjunctivitis),
hair loss,
development and worsening of psoriasis.

Side Effect Reporting:

If you notice any side effects, tell your doctor, pharmacist or pharmacist, including any side effects not listed in this leaflet. You can also report side effects by going to the website www.arpimed.com and filling out the appropriate form “Report a side effect or ineffectiveness of a drug” and to the Scientific Center for Expertise of Medicines and Medical Technologies named after. Academician E. Gabrielyan by going to the website www.pharm.am to the “Report a side effect of a drug” section and fill out the form “Card of reporting a side effect of a drug.” Scientific center hotline phone number: +37410237665; +37498773368.

How to store Bisoprolol

Store out of reach of children, protected from moisture and light at a temperature of 15-25º C.
Shelf life – 3 years. Do not take Bisoprolol after the expiration date indicated on the drug packaging. When indicating the expiration date, we mean the last day of the specified month.

Medicines should not be disposed of in wastewater or sewer systems. Ask your pharmacist how to dispose of any medicine you no longer need. These measures are aimed at protecting the environment.

Package contents and additional information

What Bisoprolol contains

Active substance: bisoprolol fumarate – 5 mg

Other components: core - microcrystalline cellulose, povidone, sodium starch glycolate, magnesium stearate, corn starch, Aerosil 200; shell - purified talc, propylene glycol, titanium dioxide, hypromellose, yellow dye E-110, red dye E-129.

What Bisoprolol looks like and contents of the package :

Yellow-orange heart-shaped tablets.

Description of packaging

10 film-coated tablets in blister packs (PVC/aluminium). 3 blister packs (30 tablets) together with an insert leaflet are placed in a cardboard package.

Vacation conditions

Available with prescription