Bisoprol 2.5 mg tablets number 50 *

Author Ольга Кияница

2017-05-11

Amount in a package 50
Product form Pills
Manufacturer Farmak OJSC (Ukraine, Kiev)
Registration certificate UA/3214/01/03
The main medicament Bisoprol
morion code 289658

Bisoprolol (Bisoprolol) Instructions for use

Composition:

active ingredient : bisoprolol; 1 tablet contains bisoprolol fumarate, recalculated on 100% substance 2.5 mg, 5 mg, 10 mg;
auxiliary substances (2.5 mg tablets): microcrystalline cellulose, calcium hydrogen phosphate, crospovidone, silicon colloidal anhydrous dioxide, magnesium stearate;

auxiliaries (5 mg and 10 mg tablets): lactose monohydrate, microcrystalline cellulose, calcium hydrogen phosphate, crospovidone, silicon dioxide, colloidal anhydrous, yellow sunset FCF (E 110), magnesium stearate.

Dosage form

Tablets.

Basic physical and chemical properties:

Pills of 2.5 mg of white color, round form with biconvex surface, with or without risk. On the surface of the tablets, marble is allowed;

5 mg round-shaped tablets with biconvex surface, pale pink, with or without risk. On the surface of the tablets, impurities are allowed;

tablets of 10 mg round form with a flat surface, with a facet and a rash, a pale pink color. On the surface of the tablets, impurities are allowed.

Pharmacotherapeutic group

Selective β-adrenergic blockers. Code ATX C07A B07.

Pharmacological properties

Pharmacodynamics.

Bisoprolol is a highly selective ß1 blocker. When applied in therapeutic doses, it has no internal sympathomimetic activity and clinically expressed membrane-stabilizing properties. It has antianginal and hypotensive effects. Reduces myocardial oxygen demand by reducing heart rate and reducing cardiac output and lowering blood pressure, increasing the supply of myocardium with oxygen by reducing diastolic blood pressure and diastolic elongation. The drug has a very low affinity with the ß2 receptors of smooth muscle of the bronchi and vasculature, as well as with the β2 receptors of the endocrine system.

The maximum effect of bisoprolol occurs 3-4 hours after ingestion. The half-life of the plasma is 10-12 hours, which results in a 24-hour efficacy after a single dose. The maximum antihypertensive effect is achieved after 2 weeks of administration.

Pharmacokinetics.

Suction After ingestion Bisoprol is well adsorbed from the gastrointestinal tract. Bioavailability is about 90% after oral administration and does not depend on food intake. The pharmacokinetics of bisoprolol and plasma concentration are linear in the dose range from 5 mg to 20 mg. The maximum concentration in the plasma (Cmax) is reached in 2-3 hours.

Distribution. The volume of distribution is 3.5 l / kg. Binding to plasma proteins is about 30%.

Metabolism and elimination. Bisoprolol is excreted from the body in two ways: 50% biotransformed into the liver with the formation of inactive metabolites and is excreted by the kidneys, 50% is excreted by the kidneys in the unaltered form. In vitro studies using human liver microsomes have shown that bisoprolol is metabolised with CYP3A4 (~ 95%), CYP2D6 plays only a minor role. The total clearance of bisoprolol is 15 l / h. The half-life is 10-12 hours.

Indications

  • Arterial hypertension;
  • ischemic heart disease (angina pectoris);
  • chronic heart failure with systolic left ventricular dysfunction, in combination with ACE inhibitors, diuretics, and, if necessary, cardiac glycosides.

Contraindications

  • Acute heart failure or heart failure in a state of decompensation requiring inotropic therapy;
  • cardiogenic shock;
  • atrioventricular blockade of degrees II and III (except for patients with an artificial rhythm driver);
  • syndrome of weakness of the sinus node;
  • pronounced synodrial blockade;
  • symptomatic bradycardia;
  • symptomatic arterial hypotension;
  • severe form of bronchial asthma or severe chronic obstructive pulmonary disease;
  • late stages of disturbance of peripheral circulation or Raynaud's disease;
  • untreated pheochromocytoma;
  • metabolic acidosis;
  • increased sensitivity to bisoprolol or other components of the drug.

Interaction with other drugs and other types of interactions

Combinations that are not recommended for use.

Treatment of chronic heart failure.

- Class A antiarrhythmics (eg quinidine, disopyramide, lidocaine, phenytoin, flecainid, propafenone): a negative effect on atrioventricular conduction and inotropic myocardial function.

All indications.

- Calcium antagonists such as verapamil, to a lesser extent, diltiazem: a negative effect on the contractile function of the myocardium and atrioventricular conductivity. Intravenous administration of verapamil can lead to pronounced arterial hypotension and atrioventricular blockade in patients taking β-blockers.

- Hypotensive drugs with a central mechanism of action (clonidine, methyldopa, moxinidine, rilmenidine): can lead to worsening of heart failure. With combination therapy, the sudden withdrawal of these agents may increase the risk of reflex hypertension.

To the ambinities that should be used with caution.

Treatment for arterial hypertension or coronary heart disease (angina pectoris).

- Class I antiarrhythmics (eg quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone): may increase the adverse effect on atrioventricular conduction and inotropic myocardial function.

All indications.

- Calcium antagonists such as dihydropyridine (eg nifedipine, felodipine, amlodipine): may increase the risk of arterial hypotension. The possibility of increasing the negative influence on the inotropic function of the myocardium in patients with heart failure is not excluded.

- Class III antiarrhythmics (eg amiodarone): may increase the effect on atrioventricular conductivity.

- Local ß-blockers (for example, those that are present in eye drops for the treatment of glaucoma): the effect of bisoprolol may be aggravated.

- Parasympathomimetics: the time for atrioventricular conduction may increase and the risk of bradycardia may increase.

- Insulin and oral hypoglycemic agents: the effect of these drugs is intensified. Signs of hypoglycaemia can be disguised.Such interaction is more likely with the use of nonselective β-blockers.

- Means for anesthesia: the risk of depression of the function of the myocardium and the occurrence of arterial hypotension increases.

- Cardiac glycosides (digitalis preparations): can reduce the frequency of heart contractions, increase the time of atrioventricular conduction.

- Nonsteroidal anti-inflammatory drugs (NSAIDs): may weaken the hypotensive effect of bisoprolol.

- ß-sympathomimetics (eg, isoprenaline, dobutamine): administration in combination with Bisoprol can reduce the therapeutic effect of both agents.

- Sympathomimetics that activate α- and β-adrenergic receptors (e.g. adrenaline, norepinephrine): increase arterial pressure. Such interaction is more likely with the use of nonselective β-blockers.

- Tricyclic antidepressants, barbiturates, phenothiazine increase the risk of arterial hypotension.

Combinations to take into account.

- Mefloquine: may increase the risk of developing bradycardia.

- MAO inhibitors (with the exception of MAO type B inhibitors): increase the hypotensive effect of ß-blockers. There is a risk of hypertensive crisis.

Application features

The drug should be used with caution in patients with the following conditions:

- bronchospasm (with bronchial asthma or chronic obstructive pulmonary disease);

- diabetes mellitus with sharp fluctuations in blood glucose levels, with symptoms of hypoglycemia (tachycardia, palpitations, sweating) may be hidden;

- strict diet;

- conducting desensitizing therapy;

- Atrioventricular block of the I degree;

- angina pectoris;

- disturbance of peripheral circulation (at the beginning of therapy it is possible to increase complaints);

- general anesthesia.

It is necessary to warn an anesthetist about taking beta-adrenergic blockers. In patients with a general anesthetic, the use of β-blockers reduces the incidence of arrhythmias and myocardial ischemia during anesthesia, intubation and postoperative period. It is recommended to continue the use of β-blockers during the intraoperative period. An anesthetist should consider the potential interaction with other drugs, which can lead to bradyarrhythmia, reflex tachycardia and reduce the possibilities of the reflex mechanism for compensating for the drop in pressure. In the event of bisoprolol cancellation before surgery, the dose should be gradually reduced and stopped taking 48 hours before the general anesthesia.

Currently, there is not enough therapeutic experience in the treatment of chronic heart failure in patients with the following diseases and pathological conditions: type I diabetes, severe renal impairment, severe liver function disorders, restrictive cardiomyopathy, congenital heart defects, hemodynamically significant acquired valve heart defects, heart attack myocardium in the last 3 months.

Combinations of bisoprolol with calcium antagonists such as verapamil or diltiazem with class 1 antiarrhythmic drugs and centrally acting hypotensive agents are not recommended (see section "Interaction with other drugs and other types of interactions").

With bronchial asthma or other chronic obstructive pulmonary diseases, accompanying therapy with bronchodilators is indicated. In some cases, with higher doses of ß2-sympathomimetics, higher doses of the respiratory tract may require higher doses of bronchial asthma patients.

Like other ß-blockers, bisoprolol can increase sensitivity to allergens and increase anaphylactic reactions. In such cases, adrenaline treatment does not always have a positive therapeutic effect.

Patients with psoriasis (including history) should use β-blockers (eg bisoprolol) after careful study of the benefit / risk ratio.

Patients with pheochromocytoma prescribe the drug Bisoprol only on the background of pretreatment with α-blockers.Symptoms of thyrotoxicosis may be masked against the background of the drug. When using Bisoprol, a positive result can be achieved during doping control.

At the beginning of the treatment, the drug should be monitored regularly.

If necessary, the drug should be completed slowly, gradually reducing the dose.

Treatment with Bisoprol should not be stopped suddenly unless there is clear evidence for this.

Bisoprol 5 mg and 10 mg tablets contain lactose, therefore this drug is not recommended for patients with rare congenital galactose intolerance, with lactase deficiency or glucose-galactose malabsorption syndrome.

Use during pregnancy or breastfeeding

During pregnancy, the drug is only used when the expected benefit to the mother outweighs the potential risk to the fetus. As a rule, β-blockers reduce blood flow to the placenta and may affect the development of the fetus. If treatment with β-blocker is necessary, it is desirable that it be a β1-selective blocker. It is necessary to control utero-placental blood flow and fetal growth.

After birth, the newborn should be under close observation. Symptoms of hypoglycemia and bradycardia can be expected within the first 3 days.

There is no data on excretion of bisoprolol in breast milk or breastfeeding safety, so it is not recommended to use Bisoprol during breastfeeding.

Ability to influence the speed of reaction when driving motor vehicles or other mechanisms.

In some cases, the drug may affect the ability to drive vehicles or work with complex mechanisms. Particular attention should be paid at the start of treatment, when changing the dose of the drug or when interacting with alcohol.

Method of administration and dose

Pills should be taken without chewing, in the morning on an empty stomach or during breakfast, drinking with a little water.

Arterial hypertension; ischemic heart disease (angina pectoris).

The recommended dose is 5 mg per day. In the case of moderate hypertension (diastolic pressure up to 105 mm Hg), a dose of 2.5 mg is recommended.

If necessary, the daily dose may be increased to 10 mg per day. The maximum recommended dose is 20 mg per day.

The change and correction of the dose is set by the doctor individually, depending on the patient's condition.

Bisoprol must be used with caution in patients with arterial hypertension or coronary heart disease, which is accompanied by heart failure.

Chronic heart failure with systolic dysfunction of the left ventricle in combination with ACE inhibitors, diuretics, and, if necessary, cardiac glycosides.

Standard therapy for chronic heart failure: ACE inhibitors (or angiotensin receptor blockers for intolerance to ACE inhibitors), β-adrenergic receptor blockers, diuretics and, if necessary, cardiac glycosides.

Bisoprol is prescribed for the treatment of patients with chronic heart failure without signs of exacerbation.

Treatment of chronic heart failure Bisoprolol begins in accordance with the following titration scheme and may adjust to the individual reactions of the organism (see Table 1).

- 1.25 mg * bisoprolol fumarate 1 time per day for 1 week, increasing to

- 2.5 mg bisoprolol fumarate 1 time per day for the next 1 week, increasing to

- 3.75 mg * bisoprolol fumarate 1 time per day for the next 1 week, increasing to

- 5 mg bisoprolol fumarate 1 time per day for the next 4 weeks, increasing to

- 7.5 mg * bisoprolol fumarate 1 time per day for the next 4 weeks, increasing to

- 10 mg bisoprolol fumarate once daily as maintenance therapy.

Week of titration Dosage titration (mg)

1st week 1.25 *

2nd week 2.5 *

3rd week 3.75 *

4th week 5

5th week 5

6th week 5

7th week 5

8th week 7.5 *

9th week 7.5 *

10th week 7.5 *

11th week 7.5 *

12th week 10

* Use bisoprolol preparations with the possibility of such dosing.

The maximum recommended dose of bisoprolol fumarate is 10 mg once a day.

At the beginning of treatment for chronic chronic failure, regular monitoring is required. During the titration phase, monitoring of vital signs (blood pressure, heart rate) and symptoms of progression of heart failure are required.

Modification of treatment.

If during the titration phase or after it there is a deterioration of heart failure, arterial hypotension or bradycardia develops, the dose adjustment of the preparation is recommended: a temporary decrease in the dose of bisoprolol or possibly a pause of treatment may be required. After stabilizing the patient's condition, treatment with the drug continues.

The course of treatment with Bisoprol is long.

You should not stop treatment suddenly and change the recommended dose without consulting your doctor, as this may result in a deterioration in the patient's condition. If necessary, treatment with the drug should be completed slowly, gradually reducing the dose.

Patients with hepatic and renal insufficiency.

Arterial hypertension; ischemic heart disease. For patients with mild or moderate hepatic or renal impairment, dosage adjustment is usually not necessary. For patients with severe renal insufficiency (creatinine clearance less than 20 ml / min) and for patients with severe hepatic insufficiency, the dose should not exceed a daily dose of 10 mg.

Chronic heart failure. There is no data on the pharmacokinetics of bisoprolol in patients with chronic heart failure, along with impaired liver and / or renal function, therefore caution should be exercised in increasing the dose.

Older patients do not require dose adjustments.

Where are you.

There are no clinical data on the efficacy and safety of the use of the drug for the treatment of children.

Overdose

The most common symptoms of overdose with the drug are bradycardia, arterial hypotension, acute heart failure, hypoglycemia, and bronchospasm. There is a wide variation in the individual sensitivity to a single high dose bisoprolol, patients with heart failure may be more sensitive to the drug.

In case of overdose, cases of development of atrioventricular blockade of the III degree and dizziness were also recorded.

In case of overdose, immediately see a doctor.

Depending on the degree of overdose, treatment is discontinued and supportive and symptomatic therapy is performed.There is limited evidence that bisoprolol is difficult to dialysis.

With bradycardia: intravenous administration of atropine. If the reaction is absent, with caution or vvodyat yzoprenalyn Another drug with polozhytelnыm hronotropnыm effect. In cases ysklyuchytelnыh vvodyat Artificial vodytel rhythm.

If hypotension arteryalnoy: pryem vasoconstrictive drugs, intravenous glucagon Introduction.

In atryoventrykulyarnoy block II and III degree: Introduction yzoprenalyna infusion; Need at - kardyostymulyatsyya.

When exacerbations hronycheskoy cardiac failure: Introduction of intravenous diuretic funds and vazodylatatorov.

When bronchospasm, bronholytycheskye Preparations (for example, yzoprenalyn), β2-adrenomymetyky and / or aminophylline.

When hypoglycemia: Introduction of intravenous glucose.

Adverse reactions

Co storony heart: bradycardia, cardiac insufficiency signs uhudshenyya (in patsyentov hronycheskoy with cardiac insufficiency, hypertension or arteryalnoy yshemycheskoy heart illness); atryoventrykulyarnoy violations conduction, bradycardia (in patsyentov arteryalnoy with hypertension or heart illness yshemycheskoy).

Co storony nervous system: dizziness * Headache pain *, syncope.

Co storony bodies of view: slezovыdelenyya Reduction (Need a uchytыvat at noshenyy contact-lens), conjunctivitis.

Co storony organs of hearing, hearing uhudshenye.

Co storony dыhatelnoy system: bronchospasm in asthma patsyentov with bronhyalnoy in anamneze and chronic obstructive disease dыhatelnыh tracks; allerhycheskyy rynyt.

Co storony pyschevarytelnoho tract: nausea, vomiting, diarrhea, constipation.

Co storony kozhy and fabrics soedynytelnыh: hypersensitivity reactions - itching, pokrasnenye, vыsыpanyya, alopetsyya. In Treatment ß-blockers uhudshenye Can be observed in psoriasis patients STATUS video psoriatic vыsыpanyya.

Co storony osteo-mыshechnoy system: mыshechnaya weakness, cramps.

Co storony liver: hepatitis.

Co storony vascular system: oschuschenye Kholod or onemenyya in the extremities, hypotension (especially in patsyentov with cardiac insufficiency), orthostatic hypotension.

Co storony Reproductive system: violation potentsyy.

Psyhycheskye disorders: depression, sleep violations, nochnыe koshmarы, galljucinacii.

Laboratory indicators: Increase urovnja triglycerides in the blood Increase pechenochnыh activity of enzymes in the blood plasma (AST, ALT).

Sharing disorders: weakness (in patsyentov hronycheskoy with cardiac insufficiency) * Fatigue, weakness (in patsyentov arteryalnoy with hypertension or heart illness yshemycheskoy).

* Only for Otnosytsya patsyentam arteryalnoy with hypertension or heart illness yshemycheskoy. These symptoms voznykayut Usually early in therapy, low vыrazhenы and disappear in techenye First 1-2 weeks.

In cases of occurrence or phenomena pobochnыh nezhelatelnыh reactions neobhodimo nemedlenno proynformyrovat doctor.

Shelf life

2 years (tablets of 2.5 mg). 3 years (tablets 5 mg and 10 mg). Do not apply after the expiry date stated on the packaging.

Storage conditions

Store in original packaging at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Packaging

10 tablets in blister. 2, 3 or 5 blysterov in packs.

Vacation category

By recipe


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