NebitaTM 2.5 Tablet: Each film coated tablet contains Nebivolol Hydrochloride INN
equivalent to Nebivolol 2.5 mg.
NebitaTM 5 Tablet: Each film coated tablet contains Nebivolol Hydrochloride INN
equivalent to Nebivolol 5 mg.
Pharmacodynamics: Nebivolol is a β-adrenergic receptor blocking agent. Nebivolol is a
racemate of two enantiomers, d-Nebivolol and l-Nebivolol. Nebivolol has unique
pharmacologic properties, including very high selectivity for β-1 receptor and nitric
oxide-mediated vasodilatory effect.
Pharmacokinetics: Nebivolol is metabolized by a number of routes, including
glucuronidation and hydroxylation by CYP2D6. The active isomer (d-Nebivolol) has an
effective half-life of about 12 hours in extensive metabolizers (most people), and 19
hours in poor metabolizers. Mean peak plasma Nebivolol concentrations occur
approximately 1.5 to 4 hours. Plasma protein binding of Nebivolol is approximately
98%, mostly to albumin.
Nebivolol is indicated in the treatment of essential hypertension and adjunct in stable
mild to moderate heart failure in patients over 70 years.
DOSAGE AND ADMINISTRATION
Hypertension: 5 mg daily; elderly initially 2.5 mg daily, increased if necessary to 5 mg
daily. Adjunct in heart failure: Initially 1.25 mg once daily, then if tolerated increased at
intervals of 1–2 weeks to 2.5 mg once daily, then to 5 mg once daily, then to max. 10
mg once daily.
Nebivolol is contraindicated in the following conditions: severe bradycardia, heart
block greater than first degree, patients with cardiogenic shock, decompensated
cardiac failure, sick sinus syndrome, patients with severe hepatic impairment, patients
who are hypersensitive to any component of this product.
The most common side effects are headache, nausea and bradycardia.
Use caution when Nebivolol is co-administered with CYP2D6 inhibitors (quinidine,
propafenone, fluoxetine, paroxetine, etc.). Do not use Nebivolol with other β-blockers,
both digitalis glycosides and β-blockers slow atrioventricular conduction and decrease
heart rate. Concomitant use can increase the risk of bradycardia, Nebivolol can
exacerbate the effects of myocardial depressants or inhibitors of AV conduction, such
as certain calcium antagonists (verapamil and diltiazem), or antiarrhythmic agents,
such as disopyramide.
USE IN PREGNANCY AND LACTATION
β-blockers may cause intra-uterine growth restriction, neonatal hypoglycaemia, and
bradycardia; the risk is greater in severe hypertension. If beta-blockers are used close
to delivery, infants should be monitored for signs of β-blockade. Nebivolol is advised
to avoid during breast-feeding due to possible risk of toxicity due to β-blockade.
Safety and effectiveness of Nebivolol in pediatric patients have not been established.
If overdose occurs, provide general supportive and specific symptomatic treatment.
Bradycardia: Administer IV atropine. Hypotension: Administer IV fluids and
vasopressors. Intravenous glucagon may be useful. Heart Block (second or third
degree): Monitor and treat with isoproterenol infusion. Congestive Heart Failure:
Initiate therapy with digitalis glycoside and diuretics. Bronchospasm: Administer
bronchodilator therapy such as a short acting inhaled β2-agonist and/or
aminophylline. Hypoglycemia: Administer IV glucose.
Store in a cool and dry place (200C -250C). Protect from light and moisture. Keep
medicine out of the reach of children.
NebitaTM 2.5 Tablet: Each box contains 30 tablets in blister pack.
NebitaTM 5 Tablet: Each box contains 30 tablets in blister pack.
Brand: Square Pharmaceuticals Ltd