Instruction for use: Nebilet

Trade name of the drug – Nebilet

Dosage Form: tablets

Active substance:Nebivololum

ATX

C07AB12 Nebivolol

Pharmacotherapeutic group: Beta1-selective blocker [Beta-blockers]

The nosological classification (ICD-10)

I10 Essential (primary) hypertension: hypertension; Arterial hypertension; Arterial hypertension crisis course; Essential Hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Essential hypertension; Primary hypertension; Arterial hypertension, complications of diabetes; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; arterial Hypertension; malignant Hypertension; Hypertonic disease; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; Isolated systolic hypertension

I15 Secondary hypertension: Arterial hypertension, complications of diabetes; hypertension; The sudden increase in blood pressure; Hypertensive disorders of blood circulation; hypertensive condition; hypertensive crises; hypertension; arterial Hypertension; malignant Hypertension; hypertensive crises; accelerated hypertension; malignant hypertension; The aggravation of hypertensive disease; Transient hypertension; hypertension; Arterial hypertension; Arterial hypertension crisis course; renovascular hypertension; Hypertension symptomatic; Renal hypertension; Renovascular hypertension; renovascular hypertension; Symptomatic hypertension

I25.9 Chronic ischemic heart disease, unspecified: CHD; Insufficiency of coronary circulation; Coronary atherosclerosis in patients with coronary artery disease

Composition (per tablet):

5.45 mg of nebivolol hydrochloride

(Equivalent to 5mg of nebivolol)

Excipients: lactose monohydrate; corn starch; MCC; silicon dioxide; magnesium stearate; polysorbate 80; hydroxypropylmethylcellulose; sodium carboxymethylcellulose

in blister 7 or 14 pcs .; in box 1, 2 or 4 blisters.

Description

Round, biconvex tablets almost white, with unilateral notch for division.

Characteristic

Cardioselective beta1-blocker.

Pharmacological Properties of Nebilet

Pharmachologic effect - antianginal, antihypertensive, anti-arrhythmic.

It lowers high blood pressure at rest, during physical exertion, stress. Competitive and selectively blocks the synaptic and extrasynaptic beta1-adrenergic receptors, making them inaccessible to the catecholamines, modulates the release of endothelial vasodilator factor (NO). Hypotensive action is due also decrease the activity of the renin-angiotensin system (not directly correlated with the change in renin activity in blood plasma). In the early days of treatment increases the round, in the future, long-term use, it is normal or reduced. The hypotensive effect develops after 2-5 days, stable operation is noted after 1-2 months. Reduces myocardial oxygen demand (slowing of heart rate and a decrease in pre- and afterload) reduces the number and severity of angina attacks and increase exercise tolerance. Antiarrhythmic effect is due to inhibition of the pathological automatism of the heart (including in the pathological focus) and slowing AV conduction.

Pharmacokinetics

After intake of rapidly absorbed from the gastrointestinal tract (food intake has no effect on the absorption). Bioavailability - 12% in those with "fast" (the effect of "first pass" through the liver) metabolism and almost full - in subjects with "slow". Communication with proteins for D-nebivolol - 98.1%, for the L-nebivolol - 97.9%. It is metabolized to form the active metabolite by acyclic and aromatic hydroxylation and N-dealkylation partial; the resulting hydroxy- and amino derivatives conjugated with glucuronic acid and excreted in the form of O- and N-glucuronyl. T1 / 2 gidroksimetabolitov - 24 hours, nebivolol enantiomers - 10 hours (for those with "fast" metabolism); for persons with a "slow" - 48 hours and 30-50 hours, respectively. Excreted by the kidneys (38%) and gut (48%).

Indications of Nebilet

Arterial hypertension, ischemic heart disease.

Contraindications

Hypersensitivity, bronchial asthma, heart failure (decompensation), severe liver dysfunction, hypotension, bradycardia, cardiogenic shock, sick sinus syndrome, AV block II and III degree, pheochromocytoma, Prinzmetal angina, depression, obliterating peripheral vascular disease ( "intermittent" claudication), myasthenia gravis, muscle weakness, up to age 18 years (effectiveness and safety have been established).

Pregnancy and breast-feeding

During pregnancy and lactation should be used with caution under strict indications, under the supervision of a physician.

Side effect

Headache, dizziness, fatigue, paresthesia (frequency of 1-10%), nausea, dry mouth, diarrhea or constipation (more than 1% of cases). Bradycardia, orthostatic hypotension, heart failure, edema, cardiac arrhythmias, Raynaud's syndrome, AV block, false angina, depression, decreased attention, somnolence, insomnia, "nightmarish" dream, hallucinations, allergic reactions, photodermatosis, rash, bronchospasm (in tonnes. h. in the absence of previously obstructive pulmonary disease), rhinitis.

Interaction

The combination with anesthetics cause cardiodepressivny effect and increase the risk of hypotension. With simultaneous use with antihypertensive drugs, nitroglycerin blockers "slow" calcium channels may develop sudden hypotension (special care should be taken in combination with prazosin); with antiarrhythmics, reserpine, alpha-methyldopa, clonidine, guanfacine - increasing the severity of bradycardia; with cardiac glycosides - summation chrono and Dromotropic; with clonidine - increased syndrome "cancel".

Inductors microsomal oxidation (rifampicin, barbiturates) is reduced, and inhibitors (cimetidine) to the concentration in the blood plasma.

Dosage and Administration

Inside, regardless of meals, drinking plenty of fluids, at one and the same time of day. The average daily dose - 2.5-5 mg. Take 1 time per day. Patients with renal insufficiency or in patients older than 65 years in the recommended initial dose of 2.5 mg / day; if necessary, the daily dose can be increased to 10 mg.

Overdose

Symptoms of an overdose of beta-blockers: decrease in blood pressure, nausea, vomiting, cyanosis, sinus bradycardia, AV block, heart failure, cardiogenic shock, cardiac arrest, bronchospasm, loss of consciousness, coma.

In clinical practice, overdose effects were observed.

Treatment: gastric lavage, the appointment of activated carbon, in the case of severe hypotension, bradycardia and heart failure - in / in the introduction of beta-agonists with an interval of 2-5 minutes to achieve the desired effect. In the absence of effect - dopamine, dobutamine, norepinephrine. Then 1-10 mg of glucagon production transvenous intracardial pacemaker. When bronchospasm - in / in a beta2-adrenergic stimulants. When ventricular arrhythmia - lidocaine (IA class of drugs are not used). In convulsions - in / diazepam.

Precautionary measures

In patients with angina discontinue therapy should be gradually - within 1-2 weeks. When angina recommended dose should provide a resting heart rate in the range of 55-60 beats per minute, with a load - no more than 110 beats per minute. Smokers have lower efficacy of the drug. To use caution in patients with renal insufficiency in the elderly (over 65 years), diabetes (possible masking signs of lowering blood glucose - nervousness, tremor, palpitations), while hyperthyroidism (masked by an increase in heart rate), a tendency to allergies ( may increase anaphylactic reactions). In psoriasis prescribed only after thorough analysis of the relation between the possible risks and benefits of the drug.

Monitoring of patients taking the drug, including monitoring of heart rate and blood pressure (at the beginning of the reception every day, then - 1 every 3-4 months), blood glucose in patients with diabetes (1 every 4-5 months), and renal function in older patients (1 every 4-5 months), the state of the peripheral circulation.

Treatment of pregnant women need to be halted for 48-72 hours before delivery. If this is not possible, it is necessary to ensure close monitoring of the newborn for 48-72 hours after delivery (development of bradycardia, hypotension, hypoglycemia, respiratory paralysis in newborns).

Special instructions

Patients who use contact lenses, you should keep in mind that in the context of drug treatment may decrease the production of tear fluid.

Nebilet is recommended for use in patients with hypertension stage I admitted to practice flight.

Manufacturer

"Berlin-Chemie AG / Menarini Group", Germany.

Storage conditions of Nebilet

At a temperature of 15-30 ° C.

Keep out of the reach of children.

Shelf life

3 years.

Do not use beyond the expiration date printed on the package.