Niperten
In this article, you can read the instructions for using the drug Niperten. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Niperten in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Niperten in the presence of existing structural analogs. Use to treat heart failure and reduce blood pressure in adults, children, as well as during pregnancy and lactation. Composition of the preparation.
Niperten - selective beta1-adrenoblocker, without its own sympathomimetic activity, does not have a membrane-stabilizing action. Reduces the activity of renin plasma, reduces the need for myocardium in oxygen, reduces heart rate (at rest and with exercise).Has antihypertensive, antiarrhythmic and antianginal action. Blocking in low doses beta1-adrenoreceptors of the heart, reduces catecholamine-stimulated formation of cAMP from ATP, reduces the intracellular current of calcium ions, has a negative chrono-, dromo-, batmo- and inotropic effect, reduces AV-conduction and excitability.
When the therapeutic dose is exceeded, beta2-adrenergic blocking action exerts.
At the beginning of the use of the drug in the first 24 hours, the OPSS increases (as a result of the reciprocal increase in the activity of alpha-adrenergic receptors and elimination of stimulation of beta2-adrenergic receptors), returns to baseline in 1-3 days, and decreases with prolonged use. The hypotensive effect is associated with a decrease in the minute volume of blood, sympathetic stimulation of peripheral vessels, restoration of sensitivity in response to a decrease in blood pressure and influence on the central nervous system. With arterial hypertension therapeutic effect occurs after 2-5 days, stable effect is observed 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, diastole lengthening, and improvement in myocardial perfusion.By increasing the end diastolic pressure in the left ventricle and increasing the tension of the ventricular muscle fibers, the need for oxygen 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 AV conduction (mainly in the antegrade and, to a lesser extent, retrograde direction via the AV node) and by additional paths.
When used at average therapeutic doses, in contrast to nonselective beta-blockers, it exerts a less pronounced effect on organs containing beta2-adrenoreceptors (pancreas, skeletal muscles, smooth muscle of peripheral arteries, bronchi and uterus), and carbohydrate metabolism; does not cause retention of sodium ions in the body; the severity of atherogenic action does not differ from that of propranolol.
Composition
Bisoprolol fumarate + excipients (Niperten).
Amlodipine besylate + Bisoprolol fumarate (Niperten Kombi).
Pharmacokinetics
Absorption is 80-90%, food intake does not affect absorption. Binding to plasma proteins is about 30%. Permeability through the blood-brain barrier (BBB) and the placental barrier is low. 50% of the dose is metabolized in the liver with the formation of inactive metabolites. About 98% is excreted by the kidneys, while 50% is excreted unchanged; less than 2% - with bile.
Indications
- arterial hypertension (pressure reduction);
- IHD: prevention of angina attacks;
- chronic heart failure.
Forms of release
Tablets coated with 2.5 mg, 5 mg, 10 mg (Niperten).
Tablets coated with a coating of 5 mg + 5 mg, 5 mg + 10 mg, 10 mg + 5 mg, 10 mg + 10 mg (Niperten Kombi).
Instructions for use and dosage
The drug is taken orally, in the morning on an empty stomach, without chewing, once.
Arterial hypertension and ischemic heart disease: prevention of angina pectoris attacks
The recommended dose is 5 mg once a day. If necessary, increase the dose to 10 mg once a day. The maximum daily dose is 20 mg.
In patients with impaired renal function with CC less than 20 ml / min, or with severe impairment of liver function, the maximum daily dose is 10 mg.
Dose adjustments in elderly patients are not required.
Chronic heart failure
The initiation of treatment for chronic heart failure with Niperten requires a special period of dosing. The prerequisites for initiating therapy are as follows:
- chronic heart failure without signs of exacerbation in the preceding 6 weeks;
- practically unchanged baseline 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 indicated dose selection scheme. Individual response of the patient 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 table. 2.5 mg once a day;
- 2 weeks - 2.5 mg once a day;
- 3 week - 3.75 mg once a day;
- 4-7 weeks - 5 mg once a day;
- 8-11 weeks - 7.5 mg once a day;
- 12 weeks and further - 10 mg once a day as maintenance therapy.
The maximum recommended dose of Niperten is 10 mg once a day. After the beginning of treatment with the drug at a dose of 1.25 mg (1/2 table.2.5 mg) the patient should be observed for about 4 hours (heart rate control, blood pressure, conduction abnormalities on the ECG, symptoms of worsening of chronic heart failure).
During the period of selection of doses or after it there may be a temporary worsening of the course of chronic heart failure, fluid retention in the body, arterial hypotension or bradycardia. In this case, it is recommended, first of all, to pay attention to the choice of the dose of concomitant basic therapy (to optimize the dose of diuretic and / or ACE inhibitor), before reducing the dose of Niperten. Treatment with the drug should be discontinued only in case of emergency.
After stabilization of the patient's condition, a repeated titration should be performed, or the treatment should be continued.
Side effect
- increased fatigue;
- weakness;
- dizziness;
- headache;
- sleep disorders;
- depression;
- anxiety;
- confusion or short-term memory loss;
- hallucinations;
- asthenia;
- myasthenia gravis;
- paresthesia in the extremities (in patients with intermittent claudication and Raynaud's syndrome);
- tremor;
- convulsions;
- impaired vision;
- decrease in secretion of tear fluid;
- dryness and soreness of the eyes;
- conjunctivitis;
- sinus bradycardia;
- palpitation;
- violation of myocardial conductivity;
- AV-blockade (until the development of complete transverse blockade and cardiac arrest);
- arrhythmias;
- weakening of myocardial contractility;
- development (aggravation) of chronic heart failure (swelling of the ankles, feet, shortness of breath);
- a decrease in blood pressure;
- orthostatic hypotension;
- manifestation of angiospasm (increased peripheral circulatory disturbance, coldness of the lower limbs, Raynaud's syndrome);
- chest pain;
- withdrawal syndrome (increased angina attacks, increased blood pressure);
- dryness of the oral mucosa;
- nausea, vomiting;
- abdominal pain;
- constipation or diarrhea;
- impaired liver function (dark urine, icteric sclera or skin, cholestasis);
- increased activity of ALT and ACT;
- increased bilirubin levels;
- changes in taste;
- nasal congestion;
- difficulty breathing when given in high doses;
- laryngo- and bronchospasm;
- Hyperglycemia (in patients with non-insulin-dependent diabetes mellitus);
- hypoglycemia (in patients receiving insulin);
- hypothyroid condition;
- itching;
- rash;
- hives;
- increased sweating;
- hyperemia of the skin;
- psoriasis-like skin reactions;
- exacerbation of psoriasis symptoms;
- alopecia;
- convulsions (including calf muscles);
- back pain;
- arthralgia;
- weakening of libido;
- decreased potency;
- thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, and leukopenia.
Contraindications
- shock (including cardiogenic);
- collapse;
- pulmonary edema;
- acute heart failure;
- chronic heart failure in the stage of decompensation;
- AV-blockade of 2 and 3 degrees;
- sinoatrial blockade;
- syndrome of weakness of the sinus node (SSSU);
- severe bradycardia;
- angina of Prinzmetal;
- cardiomegaly (no signs of heart failure);
- arterial hypotension (systolic blood pressure less than 100 mm Hg, especially with 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 peripheral circulation;
- Raynaud's disease;
- pheochromocytoma (without simultaneous use of alpha-blockers);
- metabolic acidosis;
- age under 18 years (effectiveness and safety not established);
- hypersensitivity to the components of the drug;
- hypersensitivity to other beta-blockers.
Application in pregnancy and lactation
The use of Niperten in pregnancy and during lactation is possible when the expected benefit of therapy for the mother exceeds the risk of side effects in the fetus or infant.
There is no data on the isolation of bisoprolol with breast milk. Therefore, if you need to use the drug during lactation, breastfeeding should be discontinued.
Use in children
Contraindicated in children and adolescents under the age of 18 years (efficacy and safety not established).
Application in elderly patients
With caution should be used in elderly patients.
special instructions
It is necessary to monitor the condition of patients receiving Niperten: measurement of heart rate and blood pressure (at the beginning of treatment - every day, then - once every 3-4 months), ECG, glucose level in patients with diabetes (1 time in 4-5 months ). In elderly patients, it is recommended to monitor kidney function (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 heart rate 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 marked coronary atherosclerosis with low ischemia threshold (heart rate less than 100 beats per minute) 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 a reduction in tear fluid production is possible against the background of treatment.
When using the drug in patients with pheochromocytoma, there is a risk of developing paradoxical arterial hypertension (unless an effective alpha-adrenoblockade has been previously achieved).
In thyrotoxicosis, bisoprolol may mask certain clinical signs of thyrotoxicosis (eg, tachycardia). Sharp abolition in patients with thyrotoxicosis is contraindicated, since it is possible to increase symptoms.
In diabetes mellitus can mask tachycardia caused by hypoglycemia.Unlike nonselective beta-blockers, it does not actually increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose to normal levels.
With the simultaneous use of clonidine, its administration can be stopped only a few days after the abolition of Niperten.
It is possible to increase the severity of the reaction of hypersensitivity and the lack of effect from the usual doses of epinephrine against the background of a burdened allergological anamnesis.
If it is necessary to conduct routine surgical treatment, the drug can be withdrawn 48 hours before the start of the general anesthesia. If the patient has taken the drug before surgery, he should choose a drug for general anesthesia with a minimum negative inotropic effect.
Reciprocal activation of the vagus nerve can be eliminated by intravenous administration of atropine (1-2 mg).
Drugs that reduce the reserves of catecholamines (including reserpine), can enhance the action of beta-blockers, so patients receiving such combinations of drugs require constant monitoring of the doctor for the detection of a pronounced lowering of blood pressure or bradycardia.
Patients with bronchospastic diseases can be assigned cardioselective beta-blockers in case of intolerance and / or inefficiency of other antihypertensive agents. Overdosing is dangerous by the development of bronchospasm.
If elderly patients are diagnosed with an increasing bradycardia (less than 50 beats per minute), a marked decrease in blood pressure (systolic blood pressure below 100 mm Hg), AV blockade, it is necessary to reduce the dose or stop treatment.
It is recommended to stop therapy with the development of depression.
You can not abruptly interrupt treatment because of the danger of developing a withdrawal syndrome (severe arrhythmia 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).
Niperten should be discontinued before the study of blood and urine levels of catecholamines, normetanephrine and vanillin-mandelic acid, antinuclear antibody titers.
Impact on the ability to drive vehicles and manage mechanisms
The question of the possibility of practicing potentially dangerous activities requiring increased attention and speed of psychomotor reactions should be addressed only after assessing the patient's individual response to the drug (especiallyat the beginning of treatment, in connection with the possibility of developing dizziness).
Drug Interactions
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 intravenous administration increase the risk of anaphylactic reactions.
Phenytoin with IV introduction, means for inhalation anesthesia (derivatives of hydrocarbons) increase the severity of cardiodepressant action of bisoprolol and the likelihood of lowering blood pressure.
Niperten changes 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 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 weakens non-steroidal anti-inflammatory drugs (NSAIDs) (sodium ion delay and blockade of prostaglandin synthesis by the kidneys), glucocorticosteroids (GCS), and estrogens (sodium ion delay).
Cardiac glycosides, methyldopa, reserpine and guanfacine, slow calcium channel blockers (verapamil, diltiazem), Amiodarone and other antiarrhythmic drugs increase the risk of developing or aggravating bradycardia, AV blockade, cardiac arrest and heart failure.
Nifedipine in combination with Nipertenum can lead to a significant reduction in blood pressure.
Diuretics, clonidine, sympatholytics, hydralazine and other antihypertensives can lead to excessive lowering of blood pressure.
Lengthens the effect of nondepolarizing muscle relaxants and increases the anticoagulant effect of coumarins.
Tri- and tetracyclic antidepressants, antipsychotics (antipsychotics), ethanol (alcohol), sedative and hypnotic drugs increase the CNS depression.
It is not recommended simultaneous use with MAO inhibitors, due to a significant increase in antihypertensive effect, a break in treatment between the intake of MAO inhibitors and bisoprolol should be at least 14 days.
Unhydrated ergot alkaloids increase the risk of peripheral circulatory disorders.
Ergotamine increases the risk of peripheral circulatory disorders; Sulfasalazine increases concentrationbisoprolol in the blood plasma; rifampicin decreases.
Analogues of the drug Niperten
Structural analogs for the active substance:
- Alotendin;
- Aritel;
- Aritel Cor;
- Bidop;
- Bidop Kor;
- Biol;
- Biprol;
- Bisogamma;
- Bisocardium;
- Bisomore;
- Bisoprolol;
- Bisoprolol fumarate;
- Concor;
- Concor Cor;
- Corbis;
- Cordinorm;
- Cordinorm Cor;
- Coronale;
- Niperten Combi;
- Thyrez.