Bystolic
Bystolic
Bystolic (Nebivolol)Pharmacological action
Cardioselective beta adrenoblocker of the third generation. Hypotensive and antianginal an effect has.
The active substance represents a racemate consisting from : D-nebivolola and L-nebivolola, each of which possesses special properties. Now is proved, that nitrogen (NO) regulates a vascular homeostasis and supports a normal basal tonus of vessels, normalising reactance of vessels and BP level. Possessing reducing adhesion of thrombocytes effect. Besides, being a strong antioxidant, antiatherosclerotic effect.
Bystolic reduces the CARDIAC CONTRACTIONS RATE and a BP in a condition of rest and at a load, reduces final diastolic pressure of a left ventricle, improves diastolic function of heart (reduces pressure of filling), enlarges emission fraction.
Hypotensive action of a preparation is shown in the first days of treatment.
Bystolic does not influence on a-adrenoretseptory.
Experimental researches in vitro and in vivo have shown, that the preparation does not possess sympathomimetic activity.
At healthy volunteers Bystolic does not reduce size of a developed maximum load or endurance. The preparation does not influence a lipide spectrum and glucose level in a blood plasma.
At long (within 3 years) accustoming therapies to Bystolic did not develop.
Indications
- An arterial hypertensia;
- Ischemic heart disease.
Dosage regimen
The average daily dose makes 2 mg (1/2-1 tablets. 1 time/24h) for adults. The hypotensive effect becomes expressed through 1-2 weeks of treatment, and in some cases - by 4th week of treatment.
Application of a preparation in the form of monotherapy or as a part of the combined antihypertensive therapy is possible.
If necessary a daily dose it is possible to enlarge about 10 mg (2 tablets. In one step).
At patients with renal insufficiency, and also at patients 65 years the initial dose aged is more senior makes 2.5 mg/days
The tablet should be accepted at a time days irrespective of food intake, not chewing and washing down with liquid enough.
Side effect
From party TSNS and peripheric nervous system: a headache, giddiness, feeling of weariness, paresthesia (from 1 % to 10 %); depression, depression of ability to concentration of attention, drowsiness, a sleeplessness, dreadful dreamings, hallucinations.
From the alimentary system: a nausea, a constipation, a diarrhoeia, dryness in a mouth (more than 1 %).
From cardiovascular system: a bradycardia, an orthostatic hypotension, a dyspnea, edemas, a heart failure, AV-blockade, disturbances of a rhythm of heart, cardialgias.
Allergic reactions: a dermal eruption.
The other: a bronchospasm (including in the absence of obstructive diseases of lungs in the anamnesis), a photodermatosis, a hyperhidrosis, a rhinitis.
Contraindications
- A bronchial asthma;
- A chronic heart failure in a decompensation stage;
- An uncured pheochromocytoma;
- Serious disturbances of function of a liver;
- Depressions;
- An angiospastic stenocardia;
- Obliterating diseases of peripheric vessels (Charcot's syndrome);
- An arterial hypotension;
- A cardiogenic shock;
- A bradycardia (the CARDIAC CONTRACTIONS RATE less than 50 blows/mines);
- AV-blockade II and III degrees;
- A myasthenia, muscular delicacy;
- Children's and teenage age till 18 years;
- A hypersensibility to Nebivolol.
Pregnancy and lactemia
Bystolic appointment at pregnancy is possible only under strict indications (in connection with possible development in newborns of a bradycardia, an arterial hypotension, a hypoglycaemia and a breath paralysis). Preparation reception is necessary for stopping for 48-72 h to sorts. When it is impossible, it is necessary to provide strict observation over newborns during 48-72 h after sorts.
Special indicatings
With care prescribe a preparation to patients with renal insufficiency, thyroid gland hyperfunction, allergic diseases, a psoriasis, to persons aged is more senior 65 years and a sick diabetes.
Cancellation of beta adrenoblockers should be spent gradually, within 10 days (till 2 weeks at patients from an ischemic heart disease).
The control of a BP and CARDIAC CONTRACTIONS RATE in the beginning of reception of a preparation should be daily.
At an angina of exertion the preparation dose should provide the CARDIAC CONTRACTIONS RATE in rest within 55-60 blows/mines, at a load - no more than 110 blows/minutes
Efficiency of beta adrenoblockers at smokers more low, than at the non-smoking.
Bystolic does not render influence on level of a glucose at patients with a diabetes, however under the influence of a preparation there can be disguised certain signs of a hypoglycaemia (a tachycardia, tachycardia), caused by application of hypoglycemic preparations.
At the decision of a question on Bystolic appointment patients with a psoriasis should correlate carefully prospective advantage of application of a preparation and possible risk of an exacerbation of a psoriasis.
The patients wearing contact lenses, should consider, that against application of beta adrenoblockers probably depression of production of a plaintive liquid.
At carrying out of surgical interventions it is necessary to warn the anaesthesiologist that the patient accepts beta adrenoblockers.
The control of laboratory indicators
The control of the maintenance of a glucose in a blood plasma it is necessary to spend 1 time in 4-5 months (at sick of a diabetes).
The control of laboratory indicators of function of kidneys it is necessary to spend 1 time in 4-5 months (at patients of advanced age).
Use in pediatrics
Clinical data about efficiency and safety of Bystolic application at children are absent, therefore it is not recommended to prescribe a preparation of the given category of patients.
Influence on ability to driving of motor transport and to management of mechanisms
Research works have shown, that Bystolic does not render influence on rate of psychomotor reactions. To pilots of flight structure with the soft form of an arterial hypertensia (admitted to flight work) Bystolic prescribe in an initial dose of 2.5 mg. In further (not earlier than in 2 weeks) at good shipping of treatment and the insufficient control of a BP probably rising of a dose on 2.5 mg. A recommended dose - the Preparation it is necessary to accept 5 mg/days of 1 time/24h during the period from 7.00 till 11.00 mornings.
Against preparation reception giddiness and feeling of weariness, therefore to the patients Bystolic accepting are sometimes possible, it is necessary to abstain from employment by potentially dangerous kinds of activity.
Overdosage
In clinical practice cases of an overdosage of a preparation are noted.
Possible symptoms: BP depression, a nausea, vomiting, a cyanosis, a sinus bradycardia, AV-blockade, a heart failure, a cardiogenic shock, a cardiac standstill, a loss of consciousness, a coma.
Treatment: a gastric lavage, the activated coal.
Medicinal interaction
At simultaneous application of beta adrenoblockers with blockers of calcium channels amplifies negative action on contractility of a myocardium and AV-conductivity. Introduction of verapamil against Bystolic reception is contraindicative i.v.
At simultaneous application with antiarrhytmic preparations of a class I and with Amiodaronum probably intensifying of negative inotropic action and elongation of time of carrying out of excitation on auricles.
At simultaneous Bystolic application with warm glycosides it is not taped intensifyings of influence on AV-conductivity retardation.
Simultaneous Bystolic application and anaesthetic drugs can cause suppression of a reflex tachycardia and enlarge risk of development of an arterial hypotension.
Clinically significant interaction of Bystolic preparation is not established.
Pharmacokinetic interaction
At application in a combination to the preparations inhibiting return capture of a serotonin, or other preparations biotransformed with participation of isoenzyme CYP2D6, the Bystolic metabolism is slowed down.
At simultaneous Bystolic application did not render influence on pharmacokinetic parametres of digoxin.
At simultaneous Bystolic application with Cimetidinum concentration Nebivolol in a blood plasma is enlarged (data about influence on pharmacological effects of a preparation are absent).
It is not established clinically significant interaction of Bystolic preparation and warfarin.
At simultaneous application sympathomimetic agents suppress Bystolic activity.
Conditions and periods of storage
B.Preparat's list should be stored in a dry, cool place, at temperature not above 25 C. The Period of validity - 3 years.
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