Nebivolol Teva pills 5mg N28
Condition: New product
1000 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Nebivolol
Release form
Pills
Composition
Active ingredient: Nebivolol (Nebivolol) Active ingredient concentration (mg): 5
Pharmacological effect
Cardioselective beta1-adrenoblocker of the third generation with vasodilating properties. The active substance is a racemate consisting of two enantiomers: D-nebivolol and L-nebivolol. D-nebivolol is a competitive and highly selective blocker of β1-adrenoreceptors; L-nebivolol has a mild vasodilating effect by modulating the release of the vasodilating factor (NO) from the vascular endothelium. Nebivolol lowers heart rate and blood pressure at rest and under load, reduces the end diastolic pressure of the left ventricle, reduces OPSS, improves heart diastolic function (decreases filling pressure ), increases the ejection fraction; causes an antianginal effect in IBS patients. The hypotensive effect is also due to a decrease in the activity of the renin-angiotensin system (does not directly correlate with changes in renin activity in blood plasma). The antiarrhythmic effect is due to the suppression of pathological heart automatism (including in the pathological focus) and AV retardation -conductivity. A stable hypotensive effect develops after 1-2 weeks of regular use of the drug, and in some cases after 4 weeks, a stable effect is noted after 1-2 months.
Pharmacokinetics
After ingestion, nebivolol is rapidly absorbed from the gastrointestinal tract. Food intake does not affect absorption. Bioavailability averages 12% in people with a fast metabolism (the effect of the first passage through the liver) and is almost complete in people with a slow metabolism. In the blood plasma, both enantiomers are primarily associated with albumin. D-nebivolol plasma protein binding is 98.1%, L-nebivolol - 97.9%. Metabolized by acyclic and aromatic hydroxylation and partial N-dealkylation. The resulting hydroxy and amino derivatives are conjugated with glucuronic acid and excreted as O- and N-glucuronides. They are excreted by the kidneys (38%) and through the intestine (48%). In persons with a fast T1 / 2 hydroxymetabolite metabolism, 24 hours, the necivolol enantiomers are 10 h; in persons with slow metabolism: hydroxymetabolites - 48 hours, necivolol enantiomers - 30-50 hours. Excretion of unchanged nebivolol in urine is less than 0.5%.
Indications
Arterial hypertension. CHD: prevention of strokes of angina. Chronic heart failure (as part of combination therapy).
Contraindications
Acute heart failure; chronic heart failure in the stage of decompensation (requiring iv injection of drugs with a positive inotropic effect); severe arterial hypotension (systolic blood pressure less than 90 mm Hg. Art.); SSSU, including sinoatrial blockade; AV-blockade II and III degree (without an artificial pacemaker); bradycardia (heart rate less than 60 beats / min); cardiogenic shock; pheochromocytoma (without the simultaneous use of alpha-blockers); metabolic acidosis; severe liver dysfunction; a history of bronchospasm and bronchial asthma; severe obliterating diseases of peripheral vessels (intermittent claudication, Raynaud's syndrome); myasthenia gravis; depression; children and adolescents up to 18 years; Hypersensitivity to nebivolol.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
Use during pregnancy is possible only under strict indications (due to the possible development of newborn bradycardia, arterial hypotension, hypoglycemia and respiratory paralysis). Reception of nebivolol should be stopped 48-72 hours before delivery. In cases where this is not possible, strict monitoring of newborns should be ensured within 48-72 hours after delivery.
Dosage and administration
Adults for oral administration - 2. 5-5 mg / day in the morning. The optimal effect develops after 1-2 weeks of treatment, and in some cases - after 4 weeks. If necessary, the daily dose is increased to 10 mg / day. For patients over the age of 65, the initial dose is 2. 5 mg / day. If necessary, the daily dose can be increased to 5 mg.
Side effects
The frequency of adverse reactions listed below was determined accordingly to the following (classification of the World Health Organization): very often - at least 10%; often not less than 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including individual messages. Since the cardiovascular system (CVS): infrequently - bradycardia, worsening of CHF, slowing of atrioventricular conduction, atrioventricular block, marked reduction of blood pressure, orthostatic hypotension, cardiac rhythm disturbances, cardialgia, progression of concomitant intermittent claudication, peripheral heart failure, cardiac arrhythmia, progression of concomitant intermittent claudication, peripheral heart failure, cardiac arrhythmiaOn the part of the nervous system: often - fatigue, headache, dizziness, paresthesia; infrequently - nightmares, decreased ability to concentrate, drowsiness, insomnia, depression; very rarely - hallucinations, fainting. From the senses: infrequently - weakening of vision. On the part of the respiratory system: often - shortness of breath; infrequently - bronchospasm, rhinitis. On the part of the digestive system: often - dryness of the oral mucosa, constipation, nausea, diarrhea; infrequently - vomiting, flatulence. On the part of the skin: very rarely - exacerbation during psoriasis, photodermatosis, hyperhidrosis. Allergic reactions: rarely - pruritus, erythematous rash; very rarely - angioedema. From the reproductive system: infrequently - impotence.
Overdose
Overdose of the drug is not described.
Interaction with other drugs
With simultaneous use with class I antiarrhythmic drugs, amiodarone, it is possible to enhance the negative inotropic effect and suppress AV conductivity. When used simultaneously with calcium channel blockers (verapamil and diltiazem), negative inotropic effect and AV conductivity are suppressed. against the reception of nebivolol, there is a threat of cardiac arrest (simultaneous use is contraindicated). With the simultaneous use of nebivolol with antihypertensives, nitro Glycerol or blockers of slow calcium channels can develop severe arterial hypotension (special caution is necessary when combined with prazosin). When used simultaneously with sympathomimetics, the pharmacological activity of nebivolol is suppressed. simultaneous use with tricyclic antidepressants, barbiturates, phenothiazine derivatives zhno amplification antihypertensive action nebivolola.Pri simultaneous application with cimetidine may increase the plasma concentrations of nebivolol krovi.Pri simultaneous application nebivolol with drugs that inhibit the reuptake of serotonin, or by other means,biotransforming with CYP2D6 isoenzyme, plasma concentration of nebivolol increases, nebivolol metabolism slows down, which may increase the risk of developing bradycardia. Symptoms of hypoglycemia (tachycardia) can be masked when nebivolol is used together with insulin and hypoglycemic oral administration.
special instructions
Nebivolol should be used with caution in patients with renal insufficiency, diabetes mellitus, hyperthyroidism, history of allergies, psoriasis, COPD, AV-grade I blockade, Prinzmetal angina, as well as in patients over the age of 75. Cancellation of beta-adrenergic blockers should be carried out gradually, within 10 days (up to 2 weeks in patients with coronary artery disease). At the beginning of treatment, blood pressure and heart rate should be monitored daily. The effectiveness of beta-blockers in smokers is lower than in non-smokers. Nebivolol does not have influences glucose levels in patients with diabetes, but nebivolol may mask certain signs of hypoglycemia (tachycardia, heart palpitations) caused by hypoglycemic drugs. If nebivolol is needed in patients with psoriasis, the expected benefit of therapy and the possible risk should be carefully evaluated. exacerbation of psoriasis. Beta-blockers should be used with caution with increased thyroid function due to the fact that under the influence of Eta-adrenergic blockers of tachycardia can be leveled. Nebivolol can exacerbate the symptoms of impaired peripheral circulation. Patients wearing contact lenses should take into account that when using beta-adrenergic blockers it is possible to reduce the production of tear fluid. beta-adrenergic blockers. Glucose control in plasma should be carried out 1 time in 4-5 months (in patients with diabetes mellitus). Laboratory monitoring is indicated her kidney function should be performed 1 time in 4-5 months (in elderly patients) .Primenenie children rekomenduetsya.Vliyanie not on ability to drive vehicles and management mehanizmamiNebivolol not affect the speed of psychomotor reactions.With nebivolol intake, dizziness and tiredness are sometimes possible, so patients taking nebivolol should refrain from practicing potentially hazardous activities.