NIPERTEN PILLS 2.5MG
NIPERTEN PILLS 2.5MG - 30 tabs
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Active ingredients: Bisoprolol fumarate (2: 1) 2.5 mg.
Excipients: microcrystalline cellulose, sodium carboxymethyl starch, povidone, anhydrous colloidal silicon dioxide, Magnesium stearate.
The composition of the film shell: hypromellose, macrogol, titanium dioxide, talc.
Mechanism of action
NIPERTEN - selective beta1-adrenoblocker, without its own sympathomimetic activity, does not have a membrane-stabilizing effect. It reduces plasma renin activity, reduces myocardial oxygen demand, decreases heart rate (at rest and under load). It has hypotensive, antiarrhythmic and antianginal effects. By blocking the β1-adrenoreceptors of the heart in low doses, it reduces catecholamine-stimulated cAMP formation from ATP, reduces the intracellular current of Calcium ions, has a negative chrono, dromo, batmo and inotropic effect, reduces AV conduction and excitability.
If the therapeutic dose is exceeded, it has a beta2-adrenergic blocking effect.
At the beginning of the drug use, in the first 24 hours OPSS increases (as a result of the reciprocal increase in α-adrenoreceptor activity and the removal of β2-adrenoreceptor stimulation), after 1-3 days it returns to its original level, and after prolonged use it decreases. The hypotensive effect is associated with a decrease in minute blood volume, sympathetic stimulation of peripheral vessels, restoration of sensitivity in response to a decrease in blood pressure and effects on the central nervous system. In case of arterial hypertension, the therapeutic effect occurs after 2-5 days, a stable effect is noted 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 and a decrease in myocardial contractility, a prolongation of diastole, and an improvement in myocardial perfusion. By increasing the end-diastolic pressure in the left ventricle and increasing the stretching of the muscle fibers of the ventricles, oxygen demand may increase, especially in patients with chronic heart failure.
The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers, and slowing down of AV conduction (mainly in the antegrade and, to a lesser extent, in the retrograde direction through AV node) and along additional paths.
When used in moderate therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on organs containing β2-adrenoreceptors (pancreas, skeletal muscles, smooth muscles of the peripheral arteries, bronchi and uterus),and carbohydrate metabolism; does not cause the delay of sodium ions in the body; the severity of atherogenic action does not differ from that of propranolol.
Indications and usage
- arterial hypertension;
- ischemic heart disease: prevention of strokes;
- chronic heart failure.
- shock (including cardiogenic);
- pulmonary edema;
- acute heart failure;
- chronic heart failure in the stage of decompensation;
- AV blockade II and III degree;
- sinoatrial block;
- severe bradycardia;
- Prinzmetal angina;
- Cardiomegaly (without signs of heart failure);
- arterial hypotension (systolic blood pressure less than 100 mm Hg, especially in myocardial infarction);
- severe forms of bronchial asthma and COPD in history;
- simultaneous administration of MAO inhibitors (with the exception of MAO type B);
- late stages of impaired peripheral circulation;
- Raynaud's disease;
- pheochromocytoma (without the simultaneous use of alpha-blockers);
- metabolic acidosis;
- age up to 18 years (efficiency and safety have not been established);
- hypersensitivity to the drug;
- hypersensitivity to other beta-blockers.
The drug should be used with caution in case of liver failure, chronic renal failure, myasthenia, thyrotoxicosis, diabetes mellitus, AV-blockade of the first degree, and depression (includingin history), psoriasis, allergic reactions (in history) in elderly patients.
Pregnancy and Breastfeeding
Use during pregnancy and lactation is possible in the case when the expected benefit of therapy for the mother exceeds the risk of side effects in the fetus or infant.
It should be borne in mind that the drug can cause fetal delay, fetal hypoglycemia, bradycardia.
There is no data on the allocation of bisoprolol with breast milk. Therefore, if necessary, use of the drug during lactation breastfeeding should be stopped.
Dosage and administration
The drug is taken orally, in the morning on an empty stomach, without chewing, once.
Hypertension and coronary artery disease: prevention of strokes of angina pectoris
The recommended dose is 5 mg 1 time / day. If necessary, increase the dose to 10 mg 1 time / day. The maximum daily dose is 20 mg.
In patients with impaired renal function with CC less than 20 ml / min, or with severely impaired liver function, the maximum daily dose is 10 mg.
Dose adjustment in elderly patients is not required.
Chronic heart failure
The beginning of the treatment of chronic heart failure with the drug Niperten requires a mandatory special period of selection of doses. The prerequisites for starting therapy are as follows:
- chronic heart failure without signs of exacerbation in the previous 6 weeks;
- practically unchanged basic therapy in the previous 2 weeks;
- treatment with optimal doses of ACE inhibitors (and vasodilators, in case of intolerance to ACE inhibitors), diuretics and, if necessary, cardiac glycosides.
Treatment is prescribed in accordance with the specified dosage regimen. An individual patient's response to the prescribed therapy is possible, i.e. the dose can be increased only if the previous dose is well tolerated. 1. week 1.25 mg 1/2 pill 2.5 mg 1 time / day.
2 week 2.5 mg 1 time / day.
3 week 3.75 mg 1 time / day.
4-7 week 5 mg 1 time / day.
8-11 week 7.5 mg 1 time / day.
12 week and then 10 mg 1 time / day. as maintenance therapy
The maximum recommended dose of the drug Niperten is 10 mg 1 time / day. After starting treatment with the drug in a dose of 1.25 mg (1/2 pill 2.5 mg), the patient should be monitored for about 4 hours (monitoring heart rate, blood pressure, ECG abnormalities, symptoms of worsening chronic heart failure).
During or after the dose selection period, a temporary deterioration in the course of chronic heart failure, fluid retention, hypotension, or bradycardia may occur. In this case, it is recommended, first of all, to pay attention to the selection of the dose of concomitant basic therapy (to optimize the dose of diuretic and / or ACE inhibitor), before lowering the dose of the drug Hypertension. Treatment with the drug should be interrupted only if absolutely necessary.
After stabilization of the patient's condition, it is necessary to re-titrate, or continue treatment.
Nervous system: fatigue, weakness, dizziness, headache, sleep disorders, depression, anxiety, confusion or short-term memory loss, hallucinations, asthenia, myasthenia gravis, paresthesias in the extremities (in patients with intermittent claudication and Raynaud's syndrome), tremor, convulsions.
Special senses: blurred vision, decreased secretion of tear fluid, dry and sore eyes, conjunctivitis.
Cardiovascular: sinus bradycardia, palpitations, myocardial conduction disturbance, AV-blockade (up to the development of complete transverse blockade and cardiac arrest), arrhythmias, weakening of myocardial contractility, development (worsening) of chronic heart failure (swelling of the ankles, feet, shortness of breath), decrease in blood pressure, orthostatic hypotension, manifestation of angiospasm (increased disturbance of the peripheral circulation, cooling of the lower extremities, Raynaud's syndrome), chest pain, withdrawal syndrome (increased angina pectoris attacks, increased blood pressure).
From the digestive system: dry oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, abnormal liver function (dark urine, sclera or skin jaundice, cholestasis), increased ALT and ACT, increased bilirubin, changes in taste.
On the part of the respiratory system: nasal congestion, difficulty breathing when administered in high doses (loss of selectivity) and / or in predisposed patients - laryngo and bronchospasm.
On the part of the endocrine system: hyperglycemia (in patients with insulin-dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), a hypothyroid state.
Allergic reactions: skin itch, rash, urticaria.
Dermatological reactions: increased sweating, skin hyperemia, rash, psoriasis-like skin reactions, exacerbation of psoriasis symptoms, alopecia.
From the musculoskeletal system: convulsions (including calf muscles), back pain, arthralgia.
From the reproductive system: weakening of libido, reduced potency.
From the hemopoietic system: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia.
Metabolism: increase in triglycerides.
Allergens used for immunotherapy or allergen extracts for skin tests increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving bisoprolol.
Iodine-containing radiopaque agents for iv administration increase the risk of Anaphylactic reactions.
Phenytoin with the on / in the introduction, means for inhalation anesthesia (derivatives of hydrocarbons) increase the severity of the cardiodepressive action of bisoprolol and the likelihood of lowering blood pressure.
Nipertenis alters the effectiveness of insulin and hypoglycemic agents for oral administration, masks the symptoms of developing hypoglycemia (tachycardia, increased blood pressure).
Bisoprolol reduces the clearance of Lidocaine and xanthines (except for theophylline) and increases their concentration in the blood plasma, especially in patients with initially elevated clearance of theophylline under the influence of smoking.
The hypotensive effect is weakened by NSAIDs (sodium ion retention and blockade of prostaglandin synthesis by the kidneys), GCS and estrogens (sodium ion retention).
Cardiac glycosides, methyldopa, reserpine and guanfacine, blockers of slow calcium channels (verapamil, diltiazem), Amiodarone and other antiarrhythmic drugs increase the risk of developing or worsening bradycardia, AV-blockade, cardiac arrest and heart failure.
Nifedipine can lead to a significant decrease in blood pressure.
Diuretics, clonidine, sympatholytic, hydralazine and other antihypertensive drugs can lead to an excessive decrease in blood pressure.
It prolongs the action of non-depolarizing muscle relaxants and increases the anticoagulant effect of coumarins.
Three - and tetracyclic antidepressants, antipsychotics (neuroleptics), ethanol, sedatives and hypnotic drugs increase the depression of the central nervous system.
It is not recommended simultaneous use with MAO inhibitors, due to a significant increase in the hypotensive effect, the interval in treatment between taking MAO inhibitors and bisoprolol should be at least 14 days.
Unhydrogenated ergot alkaloids increase the risk of developing disorders of the peripheral circulation.
Ergotamine increases the risk of developing impaired peripheral circulation; Sulfasalazine increases the concentration of bisoprolol in the blood plasma; rifampicin reduces.
Symptoms: arrhythmia, ventricular premature beats, severe bradycardia, AV blockade, marked reduction in blood pressure, chronic heart failure, cyanosis of the finger or palm nails, difficulty in breathing, bronchospasm, dizziness, fainting, convulsions.
Treatment: gastric lavage and the appointment of absorbent funds. Symptomatic therapy: with developed AV blockade - in / in the introduction of 1-2 mg of atropine, epinephrine or temporary staging of a pacemaker; for ventricular premature beats, lidocaine (class I A drugs are not used); with a decrease in blood pressure - the patient should be in the position of Trendelenburg; if there are no signs of pulmonary edema - in / in the introduction of plasma-substituting solutions, with ineffectiveness - administration of epinephrine, dopamine, dobutamine (to maintain chronotropic and inotropic action and eliminate pronounced decrease in blood pressure); in heart failure - cardiac glycosides, diuretics, glucagon; with convulsions - in / in diazepam; with bronchospasm - beta2-adrenostimulators inhalation.
The drug should be stored out of the reach of children at a temperature not higher than 30 ° C.