Niperten
Niperten: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Niperten
ATX code: C07AB07
Active ingredient: bisoprolol (bisoprolol)
Manufacturer: KRKA-RUS, LLC (Russia)
Description and photo update: 2018-25-10
Prices in pharmacies: from 82 rubles.
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Niperten is a selective beta 1 -adrenergic blocker.
Release form and composition
Niperten is available in the form of film-coated tablets: white, biconvex, with a dividing line on one side; 2.5 mg - oval, 5 mg and 10 mg - round; the core of the tablet when broken is a mass with a rough structure of almost white or white color (10 pcs. in blisters, in a cardboard box 2, 3, 5 or 10 packs).
1 tablet contains:
- active substance: bisoprolol fumarate - 2.5 mg, 5 mg or 10 mg;
- auxiliary components: microcrystalline cellulose, sodium carboxymethyl starch, povidone, colloidal silicon dioxide, magnesium stearate;
- shell composition: macrogol 400, hypromellose, talc, titanium dioxide (E171).
Pharmacological properties
Pharmacodynamics
Niperten has beta-adrenergic blocking, hypotensive, antianginal, antiarrhythmic effects. The active ingredient of the drug - bisoprolol, a selective beta 1 adrenoblokatorom has a selective effect on the beta 1 -adrenergic receptors in the therapeutic range and beyond. It does not possess its own sympathomimetic activity, does not have a membrane stabilizing effect. Has a slight affinity for beta 2 -adrenergic receptors involved in the regulation of metabolism, and beta 2 -adrenergic receptors of vascular and bronchial smooth muscles. Therefore, bisoprolol as a whole does not affect metabolic processes in which beta 2 are involved-adrenergic receptors, and airway resistance.
Bisoprolol has no pronounced negative inotropic effect.
After ingestion of a single dose, the maximum effect occurs after 3-4 hours, the therapeutic effect lasts for 24 hours.
The maximum decrease in blood pressure (BP) is usually achieved after 2 weeks of therapy.
The action of bisoprolol blocks beta 1 -adrenergic receptors of the heart, reducing the activity of the sympathoadrenal system.
In coronary artery disease (coronary heart disease) without signs of CHF (chronic heart failure), a single dose of bisoprolol by mouth causes a reduction in heart rate (HR), reduces the stroke volume of the heart, reducing the ejection fraction and myocardial oxygen demand. Increased total peripheral vascular resistance decreases with prolonged use of Niperten. A decrease in renin activity in blood plasma is considered one of the components of the antihypertensive action of beta-blockers.
Pharmacokinetics
In the gastrointestinal tract, bisoprolol is almost completely absorbed (more than 90%). During the initial passage through the liver, approximately 10% of the taken dose of the drug is metabolized. The bioavailability of bisoprolol after oral administration is approximately 90%. Concomitant food intake does not affect bioavailability. Has a linear kinetics, its concentration in blood plasma is proportional to the dose taken in the range from 5 to 20 mg. The maximum concentration in blood plasma is reached in 2-3 hours.
The volume of distribution is 3.5 l / kg.
Plasma protein binding is approximately 30%.
It is metabolized without subsequent conjugation via the oxidative pathway to form polar water-soluble metabolites. The main metabolites have no pharmacological activity. About 95% of bisoprolol is metabolized by the CYP3A4 isoenzyme, a small part by the CYP2D6 isoenzyme.
The total clearance of bisoprolol is 15 l / h. In unchanged form, about 50% of the active substance is excreted through the kidneys. In the liver, the second part (50%) of bisoprolol is metabolized, which in the form of metabolites is also excreted through the kidneys.
The half-life is 10-12 hours.
Indications for use
- arterial hypertension;
- stable angina pectoris with ischemic heart disease;
- chronic heart failure.
Contraindications
- acute heart failure;
- the stage of decompensation of chronic heart failure, which requires inotropic therapy;
- atrioventricular (AV) block II – III degree (without a pacemaker);
- sinoatrial blockade;
- sick sinus syndrome;
- cardiogenic shock;
- bradycardia with a heart rate of less than 60 beats per minute;
- severe arterial hypotension (systolic blood pressure below 100 mm Hg);
- chronic obstructive pulmonary disease, severe bronchial asthma;
- Raynaud's syndrome (pronounced disorders of the peripheral arterial circulation);
- pheochromocytoma (in the absence of concomitant therapy with alpha-blockers);
- metabolic acidosis;
- period of breastfeeding;
- age up to 18 years;
- hypersensitivity to the components of the drug.
Care should be taken when prescribing Niperten: patients using desensitizing therapy, with Prinzmetal angina pectoris, 1st degree AV blockade, restrictive cardiomyopathy, heart valve disease with severe hemodynamic disorders, congenital heart disease, patients with chronic heart failure who have suffered myocardial infarction during the next 3 months, with hyperthyroidism, type 1 diabetes mellitus, diabetes mellitus with significant fluctuations in blood glucose levels, severe renal failure, severe liver dysfunction, psoriasis (including history), if a strict diet is required.
During pregnancy, the appointment of Niperten is possible only in cases where the expected benefit from therapy for the mother exceeds the threat of undesirable effects in the fetus.
Instructions for the use of Niperten: method and dosage
Niperten tablets are taken orally, swallowing whole (without chewing), drinking a sufficient amount of liquid, 1 time per day in the morning, regardless of the meal.
The doctor prescribes the dose of the drug individually, taking into account the patient's condition and heart rate.
Recommended dosage in the treatment of arterial hypertension and stable angina pectoris: initial dose - 5 mg once a day. If necessary to achieve the desired therapeutic effect, the daily dose can be increased to 10 mg. The maximum daily dose is 20 mg.
A prerequisite for the appointment of Niperten for the treatment of chronic heart failure is the absence of signs of exacerbation. The standard regimen for its treatment, in addition to the use of beta-blockers, includes angiotensin-converting enzyme inhibitors, if they are intolerant - angiotensin II receptor antagonists, cardiac glycosides.
Treatment with the drug should be started in accordance with a special dose titration regimen under regular medical supervision. Doctor's supervision allows to determine the degree of tolerance of the prescribed dose and the possibility of its increase after individual adaptation. You can increase the dose only if the previous one is well tolerated.
Recommended dosage of Niperten: initial dose - 1.25 mg (1/2 tablet in a dose of 2.5 mg) once a day. With good individual tolerance of the initial dose within 14 days, it can be increased to 2.5 mg (each subsequent dose increase should be carried out with an interval of at least 14 days), then to 3.75 mg, to 5 mg, to 7.5 mg and with good tolerance - up to 10 mg.
If the patient's condition worsens after increasing the dose of the drug, it is necessary to continue treatment with the previous dose.
The maximum daily dose for the treatment of chronic heart failure is 10 mg.
During the titration period, the patient should be provided with regular monitoring of heart rate, blood pressure.
Since against the background of the use of Niperten, aggravation of the symptoms of the disease is possible from the first days of treatment, it is necessary to carefully monitor the degree of their severity.
If the maximum recommended dose of the drug is poorly tolerated, it can be gradually reduced.
With a temporary deterioration in the course of the disease, the development of arterial hypotension or bradycardia during or after titration of the dose of the drug, it is first of all necessary to adjust the doses of concomitant therapy. If necessary, a temporary decrease in the dose of bisoprolol or its cancellation is indicated.
Treatment can be continued or resumed only after the patient's condition has stabilized.
The duration of treatment for all indications is usually long-term.
Dose adjustment in elderly patients, as well as in case of impaired renal or liver function of mild to moderate severity, is usually not required.
In severe liver disease and impaired renal function with creatinine clearance (CC) less than 20 ml / min, the maximum daily dose of Niperten should not exceed 10 mg. With extreme caution, the dose should be increased in this category of patients.
Side effects
- from the nervous system: weakness, fatigue, dizziness, sleep disorders, headache, anxiety, depression, confusion, short-term memory loss, asthenia, hallucinations, myasthenia gravis, convulsions, tremors, with Raynaud's syndrome and intermittent claudication - paresthesia in the limbs;
- on the part of the organ of vision: decreased secretion of lacrimal fluid, soreness and dryness of the eyes, blurred vision, conjunctivitis;
- from the cardiovascular system: palpitations, sinus bradycardia, weakening and / or impaired myocardial conduction, arrhythmias, development or worsening of chronic heart failure (shortness of breath, swelling of the feet, ankles), orthostatic hypotension, lowering blood pressure, chest pain, symptoms of angiospasm (cooling of the lower extremities, increased disturbance of peripheral circulation, Raynaud's syndrome), withdrawal syndrome (increased blood pressure, increased angina attacks), AV blockade (up to complete transverse blockade and cardiac arrest);
- from the digestive system: changes in taste, abdominal pain, dryness of the oral mucosa, nausea, vomiting, diarrhea, constipation, liver dysfunction (yellowness of the skin or sclera, dark urine, cholestasis), increased activity of ACT (aspartate aminotransferase) and ALT (alanine aminotransferase), increased bilirubin levels;
- on the part of the respiratory system: nasal congestion, while taking high doses - difficulty breathing and / or with a predisposition - laryngospasm, bronchospasm;
- from the endocrine system: hypothyroid state; in non-insulin dependent diabetes mellitus - hyperglycemia, in patients receiving insulin - hypoglycemia;
- allergic reactions: urticaria, pruritus, rash;
- dermatological reactions: skin hyperemia, increased sweating, exacerbation of psoriasis symptoms, exanthema, alopecia, psoriasis-like reactions;
- from the musculoskeletal system: back pain, cramps (including the calf muscles), arthralgia;
- from the reproductive system: decreased potency, weakened libido;
- from the hematopoietic system: thrombocytopenia (hemorrhage, unusual bleeding), leukopenia, agranulocytosis;
- from the side of metabolism: an increase in triglyceride levels.
Overdose
Symptoms: marked lowering of blood pressure, AV blockade, bronchospasm, severe bradycardia, acute heart failure, hypoglycemia. The effect of a single dose of a high dose of bisoprolol among individual patients has varying degrees of severity; patients with chronic heart failure can have a potentially high sensitivity.
Treatment: discontinuation of the drug, the appointment of supportive symptomatic therapy. With severe bradycardia, intravenous (IV) administration of atropine is indicated. If the therapeutic effect is insufficient, the patient should be careful to introduce a drug that has a positive chronotropic effect, if necessary, temporarily install a pacemaker. With a pronounced decrease in blood pressure, the patient is injected intravenously with plasma-substituting solutions and vasopressor drugs. With AV block, the patient is prescribed epinephrine, adrenaline or other alpha and beta adrenergic agonists under close supervision; if the condition does not stabilize, an artificial pacemaker is installed. For bronchospasm, bronchodilators are used, including aminophylline and / or beta 2-adrenomimetics. In case of hypoglycemia, dextrose or glucose must be injected intravenously. With an exacerbation of the course of chronic heart failure, the patient needs to inject diuretics, drugs with a positive inotropic effect, vasodilators.
special instructions
The use of Niperten requires regular medical monitoring of the patient's condition, especially at the beginning of therapy. Monitoring includes measuring heart rate and blood pressure, conducting an ECG, determining the concentration of glucose in the blood in patients with diabetes mellitus, in elderly patients it is recommended to check the functional state of the kidneys.
The patient should know how to calculate the heart rate and be informed that if the heart rate is less than 60 beats per minute, it is necessary to consult a doctor.
It is impossible to abruptly interrupt treatment and change the recommended dose of the drug without first consulting a doctor. If it is necessary to cancel therapy, the dose of bisoprolol should be reduced gradually so as not to cause a deterioration in cardiac activity, especially in patients with ischemia.
With concomitant therapy with clonidine, its intake should be discontinued no earlier than a few days after discontinuation of Niperten.
If depression develops while taking beta-blockers, drug therapy is recommended to be discontinued.
With a burdened bronchopulmonary history, the appointment of the drug should be carried out on the basis of the results of the study of the function of external respiration.
Treatment of patients with bronchial asthma or chronic obstructive pulmonary disease should be carried out against the background of concomitant therapy with bronchodilating agents. In addition, in bronchial asthma, an increase in airway resistance is possible, requiring a higher dose of beta 2 -adrenomimetics.
Smoking reduces the effectiveness of Niperten.
It should be borne in mind that the drug, by weakening adrenergic compensatory regulation, can increase sensitivity to allergens and the severity of allergic reactions, including anaphylactic reactions. The use of epinephrine or adrenaline in this case is not always effective.
When performing a surgical operation using general anesthesia drugs, it is necessary to proceed with a gradual withdrawal of the drug in advance in order to complete it 48 hours before the start of general anesthesia. The anesthesiologist should be informed about the treatment with Niperten.
With pheochromocytoma (adrenal tumor), the administration of the drug is indicated only against the background of the use of alpha-blockers.
Bisoprolol may mask the symptoms of an overactive thyroid gland.
When using contact lenses, a possible decrease in tear production should be considered.
When prescribing a drug, it is necessary to inform the doctor about all the drugs that the patient already takes daily. Even if it is necessary to use over-the-counter drugs during the period of treatment with Niperten, you should get a preliminary consultation with a specialist.
Influence on the ability to drive vehicles and complex mechanisms
Taking into account the possibility of the development of side effects of an individual nature, which can lead to a violation of the speed of psychomotor reactions, the patient's ability to drive vehicles or complex mechanisms, it is recommended to be especially careful at the beginning of therapy, with the next change in the dose of Niperten, and the simultaneous use of alcohol.
Application during pregnancy and lactation
Since beta-blockers contribute to a decrease in blood flow in the placenta and can affect the development of the fetus, the appointment of Niperten during pregnancy is possible only in the exceptional case when the intended therapeutic effect, according to the doctor, outweighs the potential threat of developing undesirable effects in the fetus.
In the case of using bisoprolol, it is necessary to monitor the blood flow in the uterus and placenta, the growth and development of the fetus. When symptoms threatening pregnancy and / or the fetus appear, the patient is recommended to be transferred to alternative therapy using drugs with a proven safety profile in the treatment of pregnant women. After giving birth, the newborn should be carefully examined, since during the first three days of life, he may develop symptoms of bradycardia and hypoglycemia.
According to the instructions, Niperten is contraindicated for use during breastfeeding.
If necessary, the appointment of the drug during lactation, breastfeeding should be discontinued.
Pediatric use
Due to the lack of sufficient information on the use of the drug in children, the appointment of Niperten in patients under the age of 18 is contraindicated.
With impaired renal function
With mild to moderate severity of renal dysfunction, dose adjustment of Niperten is usually not required.
In severe renal impairment (CC less than 20 ml / min), the maximum daily dose is 10 mg. With extreme caution, the dose should be increased in this category of patients.
For violations of liver function
In case of mild to moderate hepatic dysfunction, dose adjustment is usually not required.
In severe liver disease, the maximum daily dose of Niperten should be 10 mg. Increasing the dose in this category of patients should be done with caution.
Use in the elderly
No dose adjustment of Niperten is required in elderly patients.
The need to reduce the dose or stop taking the drug in elderly patients arises with bronchospasm, systolic blood pressure below 100 mm Hg, symptoms of increasing bradycardia (heart rate less than 60 beats per minute), AV blockade, ventricular arrhythmias, severe renal dysfunction and / or liver.
Drug interactions
Combinations of Niperten not recommended:
- class I antiarrhythmics (including disopyramide, quinidine, lidocaine, propafenone, phenytoin, flecainide) - in patients with chronic heart failure, they can reduce myocardial contractility, AV conduction;
- calcium channel blockers such as verapamil and (to a lesser extent) diltiazem - can cause, in the treatment of all indications, a decrease in myocardial contractility and a violation of AV conduction;
- clonidine, methyldopa, moxonidine, rilmenidine (antihypertensive drugs of central action) - a combination with them can help to reduce heart rate, reduce cardiac output, lead to vasodilation against a background of decreased central sympathetic tone; their abrupt withdrawal, especially before the cessation of the use of beta-blockers, increases the risk of developing rebound arterial hypertension.
With the simultaneous use of Niperten:
- nifedipine, amlodipine, felodipine and other dihydropyridine derivatives, calcium channel blockers increase the risk of arterial hypotension;
- class III antiarrhythmics (including amiodarone) can cause increased abnormalities in AV conduction;
- beta-blockers for topical use (including eye drops for the treatment of glaucoma) can potentiate the systemic effects of bisoprolol (lowering blood pressure, reducing heart rate);
- parasympathomimetics increase the risk of increased AV conduction disorders and bradycardia;
- hypoglycemic agents for oral administration, insulin can increase its activity, while the signs of hypoglycemia can be suppressed or masked;
- agents for general anesthesia increase the risk of cardiodepressive action, causing arterial hypotension;
- cardiac glycosides can cause an increase in impulse conduction time and lead to the development of bradycardia;
- non-steroidal anti-inflammatory drugs can reduce the hypotensive effect of bisoprolol;
- isoprenaline, dobutamine and other beta-agonists may cause a decrease in their effect and the effect of bisoprolol;
- norepinephrine, epinephrine and other adrenergic agonists that affect alpha- and beta-adrenergic receptors can enhance their vasoconstrictor effects and cause an increase in blood pressure;
- antihypertensive drugs and drugs with antihypertensive activity, such as barbiturates, tricyclic antidepressants, phenothiazines, can enhance the antihypertensive effect of bisoprolol;
- mefloquine increases the risk of developing bradycardia;
- MAO (monoamine oxidase) inhibitors, in addition to MAO-B inhibitors, can enhance the antihypertensive effect of beta-blockers and the development of a hypertensive crisis.
Analogs
Niperten's analogues are: Aritel, Bidop, Bisoprolol, Bisokard, Biol, Concor, Corbis, Coronal, Tirez.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Niperten
Reviews about Niperten are mostly positive. The drug has a sufficient therapeutic effect in severe hypertension, reduces heart rate.
The disadvantages of the drug, patients include the development of side effects. The frequency and speed of their occurrence depends on the dose taken.
Price for Niperten in pharmacies
The price of Niperten for a package containing 30 tablets at a dose of 2.5 mg is about 128 rubles, at a dose of 5 mg - 152 rubles, at a dose of 10 mg - 210 rubles. The price for a package containing 100 tablets at a dose of 2.5 mg is approximately 270 rubles, at a dose of 5 mg - 322 rubles, at a dose of 10 mg - 475 rubles.
Niperten: prices in online pharmacies
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Drug name Price Pharmacy |
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Niperten 2.5 mg film-coated tablets 30 pcs. 82 RUB Buy |
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Niperten 5 mg film-coated tablets 30 pcs. RUB 88 Buy |
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Niperten 10 mg film-coated tablets 30 pcs. 92 RUB Buy |
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Niperten tablets p.p. 2.5mg 30 pcs. RUB 104 Buy |
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Niperten tablets p.p. 5mg 30 pcs. 130 RUB Buy |
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Niperten 2.5 mg film-coated tablets 100 pcs. 173 r Buy |
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Niperten tablets p.p. 10mg 30 pcs. 202 RUB Buy |
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Niperten tablets p.p. 2.5mg 100 pcs. 233 r Buy |
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Niperten 5 mg film-coated tablets 100 pcs. 244 RUB Buy |
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Niperten Combi 5 mg + 5 mg tablets 30 pcs. 269 r Buy |
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Niperten tablets p.p. 5mg 100 pcs. 281 r Buy |
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Niperten tablets p.p. 10mg 100 pcs. 433 r Buy |
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Niperten 10 mg film-coated tablets 100 pcs. 433 r Buy |
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Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
