Niperten, 2.5mg 100 pcs

Hypertension (high blood pressure), Cardialgia (heart pain), Arrhythmia, Tachycardia, Heart failure

• Arterial hypertension.
• Ischemic heart disease: stable angina.
• Cronic heart failure.

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Active ingredient

Composition

On 1 tablet 2.5 mg/5 mg/10 mg

nucleus:

Active substance:

Bisoprolol fumarate 2.50 mg/5, 00 mg/10.00 mg

Associates: microcrystalline cellulose, sodium carboxymethyl starch, povidone-K30, colloidal silicon dioxide, magnesium stearate

coating film: hypromellose, macrogol 400, titanium dioxide (E 171) 0.42 mg, talc

How to take, the dosage

Orally, once daily with a small amount of liquid, in the morning, regardless of the time of meal.

The tablets should not be chewed or crushed into a powder.

Arterial hypertension and stable angina pectoris

In all cases, the mode of taking and the dose are chosen individually by the doctor for each patient, particularly considering the heart rate and the patient’s condition.

Usually the starting dose is 5 mg of Niperten® once a day. If necessary, the dose may be increased to 10 mg once daily.

In the treatment of arterial hypertension and stable angina pectoris, the maximum recommended dose is 20 mg of Niperten® once daily.

Cronic heart failure

The standard treatment regimen for CHF includes the use of angiotensin-converting enzyme (ACE) inhibitors or angiotensin II receptor antagonists (if ACE inhibitors are intolerant), β-adrenoblockers, diuretics, and, optionally, cardiac glycosides. The initiation of CNS treatment with Niperten® requires a special titration phase and regular medical monitoring.

A precondition for Niperten® treatment is stable chronic heart failure without signs of exacerbation.

The treatment with Nipperten® begins in accordance with the following titration scheme. Individual adaptation may be required depending on how well the patient tolerates the prescribed dose, i.e. the dose may be increased only if the previous dose was well tolerated.

The recommended starting dose is 1.25 mg (1/2 tablet of 2.5 mg) once daily. Depending on individual tolerance, the dose should be gradually increased to 2.5 mg, 3.75 mg, 5 mg, 7.5 mg, and 10 mg once daily. Each subsequent dose increase should be carried out at least in 2 weeks.

If the increase in dose is not well tolerated by the patient, it is possible to reduce the dose.

The maximum recommended dose for the treatment of CHF is 10 mg of Niperten® once daily.

During titration, regular monitoring of BP, HR and severity of CHF symptoms is recommended. The worsening of CHF symptoms is possible from the first day of using the drug.

If patients do not tolerate the maximum recommended dose of Niperten®, a gradual dose reduction should be considered.

During or after the titration phase, a temporary worsening of CHF, arterial hypotension, or bradycardia may occur. In this case it is recommended first of all to correct doses of drugs of concomitant therapy. A temporary decrease of Niperten® dose or its discontinuation may also be required.

After the patient’s condition stabilizes, the dose should be titrated again or the treatment should be continued.

Length of treatment for all indications of Niperten®

Treatment duration for all indications of Niperten®

Treatment with Niperten® is usually a long-term therapy.

Special patient groups

Kidney or liver function disorder

Dose adjustment is usually not necessary in mild to moderate hepatic or renal dysfunction.

In severe renal impairment (CKR less than 20 ml/min) and in patients with severe liver disease, the maximum daily dose is 10 mg. Increasing the dose in such patients should be carried out with special caution.

Elderly patients

Dose adjustment is not required.

Children

Since there is insufficient data on the use of Niperten® in children, it is not recommended to use the drug in children under 18 years of age.

There are currently insufficient data regarding the use of Niperten® in patients with CHF combined with type 1 diabetes mellitus, severe renal and/or liver function impairment, restrictive cardiomyopathy, congenital heart disease or heart valve malformation with significant hemodynamic disturbances. Also, there are still insufficient data regarding patients with CHF with myocardial infarction within the last 3 months.

Interaction

The efficacy and tolerability of bisoprolol may be affected by the simultaneous use of other drugs. Such interaction may also occur when two drugs are taken at short intervals.

The physician should be informed about taking other medications, even if they are taken without a prescription (i.e., over-the-counter medications).

Not recommended combinations

Treatment of chronic heart failure

Class I antiarrhythmic drugs (e.g., quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone) when used concomitantly with bisoprolol may decrease AV conduction and myocardial contractility.

All indications for use of the drug Niperten®

Slow calcium channel blockers (CMBs) such as verapamil and, to a lesser extent, diltiazem when used concomitantly with bisoprolol may result in decreased myocardial contractility and impaired AV conduction. In particular, intravenous administration of verapamil in patients taking β-adrenoblockers may lead to severe arterial hypotension and AV blockade. Hypotensive agents of central action (such as clonidine, methyldopa, moxonidine, rilmenidine) may lead to a slowed HR and decreased cardiac output, as well as to vasodilation due to a decrease in the central sympathetic tone. Abrupt withdrawal, especially before withdrawal of β-adrenoblockers, may increase the risk of “ricochet” arterial hypertension.

Combinations requiring extreme caution

Treatment of arterial hypertension and angina

Class I antiarrhythmic drugs (e.g., quinidine, disopyramide, lidocaine, phenytoin, flecainide, propafenone) when used concomitantly with bisoprolol may decrease AV conduction and myocardial contractility.

All indications for use of Niperten®

BMCCs, dihydropyridine derivatives (e.g., nifedipine, felodipine, amlodipine) when used simultaneously with bisoprolol may increase the risk of arterial hypotension. In patients with CHF the risk of subsequent deterioration of cardiac contractive function should not be excluded.

Class III antiarrhythmic agents (e.g., amiodarone) may increase AV conduction disturbances.

The effects of β-adrenoblockers for topical use (e.g., eye drops to treat glaucoma) may increase the systemic effects of bisoprolol (BP reduction, heart rate slowing).

Parasympathomimetics concomitantly used with bisoprolol may increase AV conduction disturbances and risk of bradycardia.

Hypoglycemic effect of insulin or oral hypoglycemic agents may increase. Signs of hypoglycemia, particularly tachycardia, may be masked or suppressed. Such interactions are more likely when using non-selective β-adrenoblockers.

Means for general anesthesia may increase the risk of cardiodepressive effects, leading to arterial hypotension (see section “Special Precautions”).

Cardiac glycosides concomitantly used with bisoprolol may prolong pulse conduction time and thereby lead to bradycardia.

Non-steroidal anti-inflammatory drugs (NSAIDs) may decrease the antihypertensive effect of bisoprolol.

Concomitant use of Niperten® with β-adrenomimetics (e.g., isoprenaline, dobutamine) may decrease the effect of both drugs. The use of bisoprolol with adrenomimetics affecting α- and β-adrenoreceptors (e.g. norepinephrine, epinephrine) may increase the vasoconstrictor effects of these drugs that occur with α-adrenoreceptors, leading to increased BP. Such interactions are more likely when using non-selective β-adrenoblockers.

Hypotensive agents, as well as other agents with possible antihypertensive effects (e.g., tricyclic antidepressants, barbiturates, phenothiazines) may enhance the antihypertensive effect of bisoprolol.

Mefloquine concomitantly with bisoprolol may increase the risk of bradycardia.

Monoamine oxidase inhibitors (MAOIs) (except MAOI B inhibitors) may increase the antihypertensive effect of β-adrenoblockers. Concomitant use may also lead to the development of a hypertensive crisis.

Special Instructions

Desensitizing therapy, Prinzmetal angina pectoris, hyperthyroidism, type 1 diabetes mellitus and diabetes mellitus with significant fluctuations in blood glucose concentration, grade I AV blockade, severe renal failure (creatinine clearance (CK) less than 20 ml/min), Severe liver function abnormalities, psoriasis, restrictive cardiomyopathy, congenital heart disease or heart valve defect with significant hemodynamic abnormalities, CHF with myocardial infarction during last 3 months, severe forms of chronic obstructive pulmonary disease, a strict diet

As there is not enough data on the use of Niperten® in children, it is not recommended to use in children under 18 years of age.

Kidney or liver function impairment

With mild to moderate liver or kidney function impairment, no dose adjustment is usually required.

In severe renal impairment (CKR less than 20 ml/min) and in patients with severe liver disease, the maximum daily dose is 10 mg. Increasing the dose in such patients should be carried out with special caution.

Elderly patients

Dose adjustment is not required.

Do not stop treatment with Nipperten® abruptly or change the recommended dose without consulting your doctor first, as this may cause a temporary worsening of heart function. Treatment should not be interrupted suddenly, especially in patients with CHD. If discontinuation of treatment is necessary, the dose should be reduced gradually.

If clonidine is used concomitantly, it may only be discontinued several days after Nipperten® is withdrawn.

In the initial stages of treatment with Niperten®, patients require continuous monitoring.

Monitoring of patients taking Nipperten®, should include measurement of HR and BP (daily at the beginning of treatment, then once every 3-4 months), electrocardiogram, determination of blood glucose concentration in diabetic patients (once every 4-5 months). In elderly patients it is recommended to monitor the kidney function (once every 4-5 months).

Patients should be instructed on how to calculate heart rate and should be advised to consult a physician if heart rate is less than 60 bpm.

Niperten® should be used with caution in the following cases:

diabetes mellitus with significant fluctuations in plasma glucose concentration: Symptoms of a marked decrease in glucose concentration (hypoglycemia) such as tachycardia, palpitations, or increased sweating may be masked;

strict diet;

desensitizing therapy;

AV blockade degree I;

Prinzmetal angina;

mild to moderate peripheral arterial circulatory disorders (at the beginning of therapy an increase of symptoms may occur);

psoriasis (including history).

If elderly patients are identified with increasing bradycardia (HR less than 60 bpm), marked BP decrease (systolic BP below 100 mmHgtetry), AV blockade, bronchospasm, ventricular arrhythmias, severe hepatic and/or renal dysfunctions, the drug dose should be decreased or the treatment should be discontinued.

It is recommended to stop therapy if depression develops due to taking β-adrenoblockers.

The respiratory system

Before starting therapy, it is recommended to investigate the external respiratory function in patients with a history of bronchopulmonary complications.

Concurrent use of bronchodilators is indicated in bronchial asthma or COPD. Patients with bronchial asthma may have increased airway resistance, requiring a higher dose of β2-adrenomimetics.

The effectiveness of β-adrenoblockers is lower in “smokers.” In patients with COPD, bisoprololol prescribed in complex therapy to treat heart failure should be started with the lowest possible dose, and patients should be closely monitored for the appearance of new symptoms (e.g., dyspnea, exercise intolerance, cough).

Allergic reactions

β-adrenoblockers, including the drug Niperten®, may increase sensitivity to allergens and the severity of anaphylactic reactions because of impaired adrenergic compensatory regulation of them by β-adrenoblockers. Therapy with epinephrine (adrenaline) does not always give the expected therapeutic effect.

General anesthesia

When performing general anesthesia, the risk of β-adrenoreceptor blockade should be considered. If it is necessary to discontinue therapy with Niperten® before surgical intervention, this should be done gradually and completed 48 hours before general anesthesia. You should tell your anesthesiologist that you are taking Nipperten®.

Pheochromocytoma

In patients with an adrenal tumor (pheochromocytoma), Niperten® may be used only against the background of concurrent use of α-adrenoblockers.

Hyperthyroidism

When treated with Niperten®, symptoms of thyroid hyperfunction (hyperthyroidism) may be masked.

Patients who use contact lenses should consider that tear fluid production may decrease with treatment.

The drug Niperten® has no effect on driving according to the results of a study in patients with CHD. However, due to individual reactions, the ability to drive vehicles or operate complex machinery may be impaired. This should be paid special attention to at the beginning of treatment, after changing the dose, as well as in case of concurrent use of alcohol.

Synopsis

Tablets 2.5 mg:Oval, biconvex, film-coated white tablets with a ridge on one side.

Fracture appearance: a rough mass of white or almost white color with white film coating.

Tablets 5 mg and 10 mg: Round, biconvex, film-coated white tablets with a ridge on one side.

Fracture appearance: rough mass of white or almost white color with white film coating.

Contraindications

hypersensitivity to bisoprolol or any of the excipients (see “Composition”).

Acute heart failure, chronic heart failure under decompensation requiring inotropic therapy.

cardiogenic shock.

Grade II and III atrioventricular (AV) block, no pacemaker.

Sinus node weakness syndrome.

Sinoatrial block.

Severe bradycardia (HR

Side effects

The frequency of adverse reactions below was determined according to the following criteria recommended by the World Health Organization: very common (≥ 1/10); common (≥ 1/100 to < 1/10); infrequent (≥ 1/1000 to < 1/100); rare (≥ 1/10000 to < 1/1000); very rare (< 1/10000).

Nervous system disorders:

often: dizziness*, headache*;

rarely: loss of consciousness.

Mental disorders:

infrequently: depression, insomnia;

rarely: hallucinations, nightmares.

Visual organ disorders:

rare: decreased tear production (to be considered when wearing contact lenses);

very rare: conjunctivitis.

Hearing organ and labyrinth disorders:

rare: hearing disorders.

Heart and vascular disorders:

Overdose

Symptoms

The most common symptoms of overdose are: AV blockade, marked bradycardia, marked BP decrease, bronchospasm, acute heart failure and hypoglycemia.

Sensitivity to single high-dose bisoprolol administration varies widely among individual patients and is likely to be highly sensitive in patients with CHF.

Treatment

If an overdose occurs, the first step is to discontinue the drug and begin supportive symptomatic therapy.

In severe bradycardia: intravenous injection of atropine. If the effect is insufficient, a drug with positive chronotropic effect may be administered with caution. Sometimes a temporary artificial rhythm driver may be needed.

In case of a significant decrease of BP: intravenous administration of plasma exchange solutions and vasopressor drugs.

In AV blockade: the patients should be constantly monitored and treated with α- and β-adrenomimetics, such as epinephrine (adrenaline). If necessary, an artificial pacemaker should be placed.

In case of exacerbation of CHF course: intravenous administration of diuretics, drugs with positive inotropic effect, and vasodilators.

In case of bronchospasm: use of bronchodilators, including β2-adrenomimetics and/or aminophylline.

In hypoglycemia: intravenous administration of dextrose (glucose).

Pregnancy use

Pregnancy

During pregnancy, the drug Niperten® should be recommended for use only if the benefit to the mother exceeds the risk of side effects in the fetus and/or child.

Generally, β-adrenoblockers decrease placental blood flow and may affect fetal development. Blood flow in the placenta and uterus should be monitored and the growth and development of the unborn child should be monitored, and if adverse events with respect to pregnancy and/or fetus occur, alternative therapies with a proven safety profile for use during pregnancy should be adopted. The newborn should be carefully evaluated after delivery. Symptoms of bradycardia and hypoglycemia may occur during the first three days of life.

Breastfeeding

There is no data on excretion of bisoprolol into breast milk. Therefore, Niperten® is not recommended for women during breastfeeding. If administration of Niperten® during lactation is necessary, breastfeeding should be stopped.

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