Pharmacological action Bystolic 5 mg
Cardioselective beta-blocker with vasodilating III generation properties. The active substance is a racemate consisting of two enantiomers: D-nebivolol and L-nebivolol. Nebivolol is a competitive and selective β1-adrenergic blocker (affinity for the β1-adrenoceptor to 288 times higher than that of β2-adrenergic receptors), in addition, has a mild vasodilating effect by modulating the release of relaxing factor (NO) from vascular endothelium. Nebivolol reduces heart rate and blood pressure at rest and during exercise, reduces end-diastolic left ventricular pressure, reduces the PR improves diastolic cardiac function (reduced filling pressure), increases the ejection fraction, is an antianginal effect in patients with coronary artery disease.
The optimal antihypertensive effect appears after 1-2 weeks of treatment. In some cases, the maximum effect is achieved after 4 weeks.
Pharmacokinetics Bystolic 5 mg
After oral administration, nebivolol is rapidly absorbed from the gastrointestinal tract. Food intake has no effect on absorption. Bioavailability is an average of 12% in those with fast metabolism and is almost complete in those with slow metabolism.
Css in plasma in most patients (those with fast metabolism) is reached within 24 h, and for gidroksimetabolitov – after a few days. Plasma concentrations of 1-30 mg / l is proportional to dose.
Binding to plasma proteins (mainly albumin), about 98%.
Bystolic is actively metabolized in part to the formation of active gidroksimetabolitov. The metabolism of nebivolol is done by alicyclic and aromatic hydroxylation, N-dealkylation and glyukuronirovaniya also formed glucuronides gidroksimetabolitov. The rate of metabolism of nebivolol by aromatic hydroxylation of genetically determined oxidation polymorphism and dependent on CYP2D6.
A week after the introduction of 38% (number of unchanged active substance is less than 0.5%) the dose is excreted by the kidneys and 48% – through the intestines.
People with fast metabolism T1 / 2 from the plasma of nebivolol averages 10 hours, those with a slow metabolism – in 3-5 times higher.
People with fast metabolism values of T1 / 2 gidroksimetabolitov from plasma averages 24 hours, those with a slow metabolism – 2 times higher.
Statement Bystolic 5 mg
Essential (primary) hypertension, coronary artery disease.
Dosage and administration Bystolic 5 mg
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 increased to 10 mg / day.
For patients older than 65 years of the initial dose is 2.5 mg / day. If necessary, the daily dose can be increased to 5 mg.
Side effect Bystolic 5 mg
From the central and peripheral nervous system: headache, dizziness, fatigue, paresthesia, depression, decreased ability to concentrate, drowsiness, insomnia, nightmares, hallucinations.
Part of the digestive system: nausea, constipation, diarrhea, dry mouth.
Cardio-vascular: bradycardia, orthostatic hypotension, dyspnea, edema, heart failure, AV-block, cardiac arrhythmias, Raynaud’s syndrome, cardialgia.
Allergic reactions: skin rash.
Other: bronchospasm (including the absence of obstructive lung diseases in anamnesis), photodermatosis, rash, rhinitis.
Contraindications Bystolic 5 mg
Bronchial asthma, chronic heart failure in decompensated, untreated phaeochromocytoma, severe liver problems, depression, angiospastic angina (Prinzmetal’s angina), peripheral vascular disease obliterative syndrome (intermittent claudication), hypotension, cardiogenic shock, bradycardia (heart rate less than 50 beats. / min), SSS, AV-block II and III level, myasthenia gravis, muscle weakness, childhood and adolescence to 18 years, hypersensitivity to nebivolol.
Pregnancy and breast feeding Bystolic 5 mg
Pregnancy is possible only under strict indications (due to the possible development of neonatal bradycardia, hypotension, hypoglycemia, and respiratory paralysis). Acceptance of nebivolol should be discontinued for 48-72 hours before delivery. In those cases where it is not possible, to ensure strict observation of the newborn within 48-72 hours after birth.
Cautions
Used with caution in patients with renal failure, hyperthyroidism, allergies, psoriasis, people aged over 65 and patients with diabetes mellitus.
Abolition of beta-blockers should be gradual, over 10 days (up to 2 weeks in patients with coronary artery disease).
At the beginning of treatment should be monitored daily blood pressure and heart rate.
The effectiveness of beta-blockers lower in smokers than in nonsmokers.
Bystolic does not affect glucose levels in patients with diabetes, but the action of nebivolol may be masked by some signs of hypoglycemia (tachycardia, palpitations), caused by the use of hypoglycemic drugs.
If necessary, use of nebivolol in patients with psoriasis should carefully evaluate the potential benefits of therapy and the possible risk of exacerbation of psoriasis.
Beta-blockers should be used cautiously with increased thyroid function due to the fact that under the influence of beta-blockers can be neutralized by the tachycardia.
Nebivolol may exacerbate symptoms of peripheral circulation.
Patients who wear contact lenses should be aware that during treatment with beta-blockers may reduce tear production.
For surgical intervention should notify the anesthesiologist that the patient is taking beta-blockers.
Control of glucose in the blood plasma should be one every 4-5 months (in diabetics).
Monitoring of laboratory parameters of renal function should be one every 4-5 months (elderly patients).
Use in children is not recommended.
Effects on ability to drive and control mechanisms
Nebivolol does not affect the speed of psychomotor reactions. In patients receiving nebivolol may sometimes dizziness and fatigue, so patients taking nebivolol should refrain from activities in potentially hazardous activities.
Drug Interactions Bystolic 5 mg
While the use of antiarrhythmic drugs of class I, amiodarone may enhance the negative inotropic action and inhibition of AV-conduction.
While the use of calcium channel blockers (verapamil and diltiazem) increases the negative inotropic effect and inhibition of AV-conduction.
At / in the introduction of verapamil in patients receiving nebivolol there is a threat of cardiac arrest.
While the use of sympathomimetics suppressed pharmacological activity of nebivolol.
When applied simultaneously with the means to anesthesia may suppress reflex tachycardia and increased risk of hypotension.
With the simultaneous use of tricyclic antidepressants, barbiturates, phenothiazine derivatives may increase the antihypertensive action of nebivolol.
While the use of cimetidine may increase the concentration of nebivolol in plasma.
