Aritel - instructions for use, dose, side effects, contraindications

Excipients: potato starch 24 mg, silicon dioxide colloid 1.8 mg; lactose monohydrate 63.1 mg, magnesium stearate 0.6 mg, povidone K-30 4.5 mg, microcrystalline cellulose 21 mg;

composition of film shell: celiac AQ-02140 6 mg, including: hypromellose (hydroxypropylmethylcellulose) 3.3 mg, dye sunset sunset yellow 0.042 mg, Macrogol-400 (polyethylene glycol 400) 0.54 mg, marogue-6000 (polyethylene glycol 6000) 0.84 mg, titanium dioxide 1.278 mg.

Dosage of 10 mg

1 tablet, film-coated, 10 mg contains:

active substance: bisoprolol fumarate 10 mg;

Excipients: potato starch 36 mg, silicon dioxide colloid 2.7 mg, lactose monohydrate 91.7 mg, magnesium stearate 0.9 mg, povidone K-30 6.7 mg; microcrystalline cellulose 32 mg;

composition of film shell: celiac AQ-02140 9 mg, including: hypromellose (hydroxypropylmethylcellulose) 4.95 mg, dye sunset sunset yellow 0.063 mg, macrogol-400 (polyethylene glycol 400) 0.81 mg, macrogol-6000 (polyethylene glycol 6000) 1.26 mg; titanium dioxide 1.917 mg.

Description:

The tablets are round biconvex, covered with a film coating of light orange color. On the cross-section - almost white.

Pharmacotherapeutic group:Beta1-blocker selective

ATX: & nbsp

C.07.A.B Selective beta-blockers

C.07.A.B.07 Bisoprolol

Pharmacodynamics:

Selective beta₁- adrenoblocker, without its own sympathomimetic activity, does not possess membrane-stabilizing action. Has only a slight affinity for beta₂-adrenoreceptors of smooth muscles of bronchi and vessels, and also to beta₂adrenoreceptors involved in the regulation of metabolism. Consequently, bisoprolol in general, does not affect the resistance of the respiratory tract and the metabolic processes in which beta is involved₂adrenoreceptors.

As a rule, the maximum reduction in blood pressure (BP) is achieved 2 weeks after the initiation of therapy.

Bisoprolol reduces the activity of the sympathoadrenal system by blocking beta₁-adrenoceptors of the heart.

With a single oral administration in patients with coronary heart disease without signs of chronic heart failure (CHF) Bisoprolol reduces the heart rate (heart rate), reduces shock volume of blood and, as a result, reduces the ejection fraction and the need for myocardium in oxygen. With prolonged therapy, initially increased total peripheral vascular resistance (OPSS) is reduced. Reduction of renin activity in blood plasma is considered as one of the components of anti-hypertensive action of beta-blockers.

Pharmacokinetics:

Suction. Bisoprolol almost completely (more than: 90%) is absorbed from gastrointestinal tract. Its bioavailability due to minor metabolism during the "first passage" through the liver (at about 10%) is approximately 90% after ingestion. Eating does not affect bioavailability. Bisoprolol demonstrates linear kinetics, and its concentrations in the blood plasma are proportional to the dose taken in the dose range from 5 to 20 mg. The maximum concentration in the blood plasma is achieved in 2-3 hours.

Distribution. Bisoprolol distributed fairly widely. The volume of distribution is 3.5 l / kg. The connection with plasma proteins is approximately 30%.

Metabolism. Metabolized by the oxidative pathway without subsequent conjugation. All metabolites are polar (water-soluble) and are excreted kidneys. The main metabolites found in blood plasma and urine are not show pharmacological activity. Data obtained as a result of experiments with microsomes of human liver in vitro, show that bisoprolol is metabolized primarily by isoenzyme CYP3A4 (about 95%), and the isoenzyme CYP2D6 plays only a minor role.

Excretion. Bisoprolol clearance is determined by the balance between excretion by the kidneys in an unchanged form (about 50%) and metabolism in the liver (about 50%) to metabolites that are also excreted by the kidneys. The total ground clearance is 15 liters per hour. The half-life is 10-12 hours.

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

Indications:

- Chronic heart failure (CHF);

- arterial hypertension;

- ischemic heart disease: prevention of attacks of stable angina pectoris.

Contraindications:

Hypersensitivity to bisoprolol or to any of the excipients and other beta-blockers; deficiency of lactase, lactose intolerance, glucose-galactose malabsorption; cardiogenic shock; collapse; acute heart failure; chronic heart failure in the stage of decompensation,requiring inotropic therapy; atrioventricular blockade of II and III degree, without an electrocardiostimulator; sinoatrial blockade; syndrome of weakness of the sinus node; pronounced bradycardia (heart rate less than 50 beats per minute); severe forms of bronchial asthma or chronic obstructive pulmonary disease; marked decrease in blood pressure (systolic blood pressure less than 90 mmHg); expressed, violations of peripheral circulation or Raynaud's syndrome; pheochromocytoma (without simultaneous use of alpha-adrenoblockers); metabolic acidosis; lactation period; simultaneous administration of monoamine oxidase inhibitors (MAO) (with the exception of MAO inhibitors (-) B); simultaneous application with floktaphenin and sultopride; age to 18 years (efficacy and safety not established).

Carefully:Desensitizing therapy; angina of Prinzmetal; hyperthyroidism; Type 1 diabetes mellitus and diabetes mellitus with significant fluctuations in blood glucose concentration; AV blockade of the 1st degree; marked renal failure (creatinine clearance less than 20 ml / min); severe liver dysfunction; psoriasis; restrictive cardiomyopathy;Congenital heart disease or heart valve disease with severe hemodynamic disorders; chronic heart failure with myocardial infarction during the last 3 months; pheochromocytoma (with concomitant use of alpha-blockers); strict diet.

Pregnancy and lactation:

During pregnancy, the drug Aritel® should be recommended for use only if the benefit to the mother exceeds the risk of side effects in the fetus. As a rule, beta-adrenoblockers reduce blood flow in the placenta and can affect the development of the fetus. The blood flow in the placenta and uterus should be monitored, and the growth and development of the unborn child should be monitored, and in case of appearance of undesirable phenomena in the relationship of pregnancy and / or fetus - to take alternative therapies. You should carefully examine the newborn after delivery. In the first three days of life, symptoms of hypoglycemia and bradycardia may occur.

There is no data on the isolation of bisoprolol in breast milk. Therefore, taking Arilit® is not recommended for women during lactation. If you need to take Aritel® during lactation,Breastfeeding should be discontinued.

Dosing and Administration:

Preparation Aritel® is taken orally, in the morning on an empty stomach, once a day with a sufficient amount of liquid, in the morning before breakfast, during or after it. Tablets should not be chewed or ground into a powder.

Chronic heart failure

The beginning of treatment with CHF with Arilit® requires a special phase of titration and regular medical supervision.

A prerequisite for treatment with Arilit® is stable chronic heart failure without signs of exacerbation.

Treatment of CHF with Aritel® begins according to the following titration scheme. Individual adaptation may be required depending on how well the patient tolerates the prescribed dose, i. E. The dose can be increased only if the previous dose is well tolerated.

To ensure the appropriate titration process at the initial stages of treatment, it is recommended to use the drug in smaller doses. The recommended initial dose is 1.25 mg (¹/₂ tablets of 2.5 mg) once a day.Depending on the individual tolerability dose should be gradually increased to 2.5 mg, 3.75 mg (1¹/₂ tablets of 2.5 mg), 5 mg, 7.5 mg (1 tablet of 5 mg and ¹/₂ tablets of 2.5 mg) and 10 mg once a day with an interval of not less than 2 or more weeks.

If the increase in the dose of the drug is poorly tolerated by the patient, a dose reduction is possible.

The maximum daily dose for the treatment of CHF is 10 mg 1 time per day.

During titration, regular monitoring of blood pressure, heart rate and symptoms of increased severity of CHF is recommended. The aggravation of symptoms of CHF is possible from the first day of application of the drug.

During the titration phase or after it, temporary deterioration of the course of CHF, arterial hypotension or bradycardia may occur. In this case, it is recommended, first of all, to correct the dose of concomitant therapy. It may also be necessary to temporarily reduce the dose of Arilit® or to cancel treatment.

After stabilization of the patient's condition, a repeated titration of the dose should be performed, or the treatment should be continued.

Arterial hypertension and ischemic heart disease (prevention of attacks of stable angina)

With arterial hypertension and ischemic heart disease, the drug is prescribed 5 mg once a day. If necessary, increase the dose to 10 mg once a day.

In the treatment of hypertension and angina maximum The daily dose is 20 mg 1 time / day.

It is possible to use the drug bisoprolol in another dosage form (tablets of 2.5 mg with a risk).

In all cases, the regimen and dose are selected by the doctor for each patient individually, in particular, taking into account the individual characteristics and the patient's condition.

Special patient groups

Impaired renal or hepatic function:

If a mild or moderate degree of liver or kidney function does not normally require dose adjustment.

In severe renal impairment (creatinine clearance less than 20 ml / min) and in patients with severe liver disease, the maximum daily dose is 10 mg. An increase in the dose in such patients should carried out with extreme caution.

Elderly patients:

Correction of the dose is not required.

To date, there is insufficient data on the use of Arilit® in patients with CHF associated with type 1 diabetes mellitus, expressed renal and / or hepatic impairment, restrictive cardiomyopathy, congenital heart disease, or hemodynamically conditioned heart disease. Also still not sufficient data were obtained regarding patients with CHF with myocardial infarction during the last 3 months.

Side effects:

The incidence of adverse reactions listed below was determined as follows:

- very often ≥ 1/10;

- often ≥ 1/100, <1/10;

- infrequently ≥1 / 1000, <1/100;

- rarely ≥ 1/10 000, <1/1000;

- Very rarely <1/10 000, including individual messages.

From the central nervous system

Often: dizziness *, headache *.

Rarely: loss of consciousness.

Common violations

Often: asthenia (in patients with CHF), increased fatigue *.

Infrequently: asthenia (in patients with hypertension or angina pectoris).

Mental disorders

Infrequently: depression, insomnia.

Rarely: hallucinations, nightmares.

From the nervous system

Infrequent: increased fatigue, asthenia, dizziness, headache.

Rarely: loss of consciousness.

From the skin

Rarely: hypersensitivity reactions, such as pruritus, rash, hyperemia of the skin.

Very rarely: alopecia. Beta-blockers can contribute to exacerbation of symptoms of psoriasis or cause a psoriasis-like rash.

From the genitourinary system

Rarely: a violation of potency, weakening of libido, Peyronie's disease, cystitis, renal colic, polyuria.

From the side of the musculoskeletal system

Infrequently: muscle weakness, muscle cramps.

From the digestive system

Often: nausea, vomiting, diarrhea, constipation.

Rarely: hepatitis.

On the part of the organs of hematopoiesis

In some cases - thrombocytopenia, agranulocytosis.

From the respiratory system

Infrequent: bronchospasm in patients with bronchial asthma or airway obstruction in anamnesis.

Rarely: allergic rhinitis.

From the sense organs

Rarely: decreased lachrymation (should be considered when wearing contact lenses).

Very rarely: conjunctivitis.

From the side of the hearing organ

Rarely: hearing impairment.

From the side of the cardiovascular system

Very often: bradycardia (in patients with CHF).

Often: aggravation of symptoms of CHF flow (in patients with CHF), sensation of cooling and numbness in the extremities, marked decrease in blood pressure, especially in patients with CHF.

Infrequently: violation AV conductivity; bradycardia (in patients with hypertension or angina pectoris); aggravation of symptoms of CHF flow (in patients with arterial hypertension or angina pectoris), orthostatic hypotension.

Influence on the fetus

Intrauterine growth retardation, hypoglycemia, bradycardia.

From the side of the reproductive system

Rarely: a violation of potency.

Laboratory indicators

Rarely: an increase in the concentration of triglycerides and the activity of "hepatic" transaminases in the blood (aspartate aminotransferase (ACT), alanine aminotransferase (ALT)).

* In patients with hypertension or angina, these symptoms usually appear at the beginning of the course of treatment, are not pronounced and take place within 1-2 weeks after the start of treatment.

Overdose:

Symptoms

The most common symptoms of an overdose are: AV blockade, bradycardia, decreased blood pressure, bronchospasm, acute heart failure and hypoglycemia.

Treatment

When an overdose occurs, it is first necessary to stop taking the drug and begin supporting symptomatic therapy.

With a pronounced bradycardia: intravenous administration of atropine. If the effect is insufficient, with caution, you can enter a drug that has a positive chronotropic effect. Sometimes it may be necessary to temporarily set up an artificial pacemaker.

With a pronounced decrease in blood pressure: intravenous injection of plasma-substituting solutions and the appointment of vasopressors.

When AV blockade: patients should be under constant observation and receive treatment with beta-adrenomimetics, such as epinephrine. If necessary - staging an artificial driver rhythm.

With exacerbation of CHF flow: intravenous injection of diuretics, drugs with a positive inotropic effect, as well as vasodilators.

When bronhospazme: use of bronchodilators, including beta₂-sympathomimetics and / or aminophylline.

When hypoglycemia: intravenous dextrose (glucose).

Interaction:

Unrecommended combinations

- in the treatment of chronic heart failure:

Antiarrhythmic drugs of the first class (for example, quinidine, disopyramide, lidocaine, phenytoin; flecainide, propafenone) with simultaneous application with bisoprolol may reduce AV conduction and contractility of the heart.

- in the treatment of chronic cardiac insufficiency, arterial hypertension: stable angina:

Blockers "slow" calcium channel (BCCI) verapamil type and to a lesser extent, diltiazem, while the use of bisoprolol can lead to a decrease of myocardial contractility and AV conduction disturbance.In particular, intravenous administration of verapamil to patients taking beta-blockers can lead to severe arterial hypotension and AV blockade.

Hypotensive means of central action (such as clonidine, methyldopa, moxonidine, rilmenidine) can lead to a decrease in heart rate and a decrease in cardiac output, as well as to vasodilation due to a decrease in the central sympathetic tone. Abrupt cancellation, especially before the abolition of beta-blockers can increase the risk of developing "ricochet" arterial hypertension.

Combinations requiring special care

- when treating arterial hypertension of stable angina:

- in the treatment of chronic heart failure, arterial hypertension, stable angina:

BCCC derivatives of dihydropyridine (for example, nifedipine, felodipine, amlodipine) with simultaneous application with bisoprolol may increase the risk of developing arterial hypotension.In patients with chronic heart failure, the risk of subsequent deterioration of the contractile function of the heart can not be ruled out.

Antiarrhythmic drugs of the III class (for example, amiodarone) can enhance the disturbance of AV conduction.

The action of beta-blockers for topical application (eg, eye drops for the treatment of glaucoma) can enhance the systemic effects of bisoprolol (lowering blood pressure, decreasing heart rate).

Parasympatomimetics with simultaneous application with bisoprolol may increase the disturbance of AV conduction and increase the risk of developing bradycardia.

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

Means for general anesthesia may increase the risk of cardiodepressive action, leading to hypotension (see section "Special instructions").

Cardiac glycosides with simultaneous application with bisoprolol may lead to an increase in the time of the impulse and, thus, to the development of bradycardia.

Non-steroidal anti-inflammatory drugs (NSAIDs) can reduce the antihypertensive effect of bisoprolol.

Simultaneous use of the drug with beta-adrenomimetics (for example, isoprenaline, dobutamine) can lead to a decrease in the effect of both drugs.

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

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

Mefloquine with simultaneous application with bisoprolol may increase the risk of developing bradycardia.

MAO inhibitors (with the exception of MAO inhibitors (-) B) can enhance the antihypertensive effect of beta-blockers. Simultaneous application can also lead to the development of hypertensive crisis.

Contraindicated combinations

Floktaphenin: beta-adrenergic blockers may interfere compensatory cardiovascular reactions with hypotension caused by floktaphenin.

Sultopride: There is a risk of ventricular arrhythmia.

Special instructions:

Do not interrupt drug treatment abruptly and do not change recommended dose without prior consultation with your doctor, since this can lead to a temporary worsening of the heart. Treatment should not be interrupted suddenly, especially in patients with ischemic heart disease. If cessation of treatment is necessary, then the dose should be reduced gradually.

Control of patients receiving bisoprolol, should include monitoring of heart rate and blood pressure (at the beginning of treatment - every day, then once every 3-4 months), ECG, blood glucose concentration in patients with diabetes mellitus (1 every 4-5 months). In elderly patients it is recommended to follow the function of the kidneys (once every 4-5 months). It is necessary to teach the patient how to calculate heart rate and instruct about the need for medical consultation at a heart rate of less than 50 beats per minute.

Before the start of treatment, it is recommended to perform an external respiration function in patients with a history of bronchopulmonary anamnesis.

Approximately in 20% of patients with angina pectoris beta-adrenoblockers are ineffective. The main causes are severe coronary atherosclerosis with a low threshold of ischemia (heart rate less than 100 beats / min) and an increased end-diastolic volume of the left ventricle, which breaks the subendocardial blood flow.

In "smokers" the effectiveness of beta-blockers is lower.

Patients who use contact lenses should take into account that, on the background of treatment, tear fluid production can be reduced.

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

With hyperthyroidism, the drug can mask certain clinical signs of hyperthyroidism (hyperthyroidism), for example, tachycardia. Abrupt withdrawal of the drug in patients with hyperthyroidism is contraindicated, since it can strengthen symptoms.

In diabetes mellitus can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it does not actually increase insulin-induced hypoglycemia and does not delay the recovery of glucose in the blood to normal levels.

With the simultaneous administration of clonidine, its administration can be stopped only a few days after the withdrawal of the drug Aritel®. It is possible to increase the severity of hypersensitivity reactions and absence of effect from usual doses of epinephrine (adrenaline) on the background of a burdened allergological anamnesis.

In case of necessity of carrying out of planned surgical treatment, the drug cancellation is carried out 48 hours before the general anesthesia. If the patient has taken the drug before surgery, he should choose a medicine for general anesthesia with a minimum negative inotropic effect. An anesthetist should be warned that you are taking Arilit®.

Reciprocal activation of the vagus nerve can be eliminated by intravenous administration of atropine (1-2 mg).

Drugs that reduce catecholamine stocks (including reserpine), can enhance the action of beta-blockers, so patients who take such combinations of drugs should be under constant medical supervision for the diagnosis of arterial hypotension or bradycardia.Patients with bronchospastic diseases can be prescribed cardioselective adrenoblockers in case of intolerance and / or ineffectiveness of other antihypertensive agents, but strict monitoring of dosage should be carried out.

Overdosing is dangerous by the development of bronchospasm.

In the case of an increasing bradycardia (less than 50 beats per minute), arterial hypotension (systolic blood pressure below 100 mm Hg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe liver and kidney damage, it is necessary to reduce the dose or stop treatment. It is recommended to stop therapy with the development of depression caused by the use of beta-blockers.

Do not abruptly interrupt treatment because of the risk of developing severe arrhythmias and myocardial infarction. Abolition is carried out gradually, reducing the dose for 2 weeks or more (reduce the dose by 25% in 3-4 days).

It should be abolished before the study of blood and urine levels of catecholamines, normetanephrine and vanillin-mandelic acid; titers of antinuclear antibodies.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, care must be taken when driving vehicles and engaging in other potentiallydangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 5 mg, 10 mg.

Packaging:

For 10 or 30 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

For 3, 6, 10 contiguous cell packs of 10 tablets or 1, 2, 3 contour packs of 30 tablets together with the instructions for use are placed in a pack of cardboard.

Storage conditions:

At a temperature of no higher than 25 ° C in the manufacturer's packaging.

Keep out of the reach of children.

Shelf life:

3 years.

Terms of leave from pharmacies:On prescription

Registration number:LS-002540

Date of registration:26.07.2011 / 10.08.2017

Expiration Date:Unlimited

The owner of the registration certificate:CANONFARMA PRODUCTION, CJSC CANONFARMA PRODUCTION, CJSC Russia

Manufacturer: & nbsp

CANONFARMA PRODUCTION, CJSC Russia

Representation: & nbspCANONFARMA PRODUCTION CJSC CANONFARMA PRODUCTION CJSC Russia

Information update date: & nbsp12.09.2017

Illustrated instructions

Instructions

Aritel® (Aritel®)