Indication
Nebivolol is indicated in the treatment of essential hypertension and adjunct in stable mild to moderate heart failure in patients over 70 years.
Pharmacology
Nebivolol is a ?-adrenergic receptor blocking agent. Nebivolol is a racemate of two enantiomers, d-Nebivolol and l-Nebivolol. Nebivolol exhibits high selectivity for ?1-adrenergic receptors and has vasodilating activity due to a direct action on the endothelium, involving nitric oxide release. It lacks intrinsic sympathomimetic and membrane-stabilising activity.
Dosage
Adults: 5 mg daily, maximum recommended dose 40 mg once daily.Renal Impairment: In patients with severe renal impairment the recommended initial dose is 2.5 mg once daily; titrate up slowly if needed.Hepatic Impairment: In patients with moderate hepatic impairment, the recommended initial dose is 2.5 mg once daily; titrate up slowly if needed.Geriatric Patients: It is not necessary to adjust the dose in the elderly.Pediatric Use: Safety and effectiveness of Nebivolol in pediatric patients have not been established.
Interaction
Use caution when Nebivolol is co-administered with CYP2D6 inhibitors (quinidine, propafenone, fluoxetine, paroxetine, etc.), Do not use Nebivolol with other ?-blockers, both digitalis glycosides and ?-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.
Contradiction
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.
Side Effect
The most common side effects are headache, nausea and bradycardia.
Pregnancy
Pregnancy category C and not recommended during nursing.
Precaution
Patients with inadequate cardiac function, well-compensated heart failure, myasthenia gravis. Patients undergoing major surgery involving general anaesth. May mask signs and symptoms of hypoglycaemia and hyperthyroidism. Abrupt withdrawal may exacerbate angina symptoms and/or precipitate MI and ventricular arrhythmias in patients with coronary artery disease. Pregnancy and lactation.
Overdose
Symptoms: Bradycardia, hypotension, cardiac failure, dizziness, fatigue, hypoglycaemia, vomiting, bronchospasm, heart block. Management: Symptomatic and supportive treatment. IV atropine may be given for bradycardia, if it persists, admin IV isoproterenol cautiously. For hypotension, admin IV fluids and vasopressors. IV glucagon may also be useful. A ?2-agonist and/or aminophylline for bronchospasm. Admin IV glucose for hypoglycaemia and an IV cardiac glycoside and diuretic may be used for CHF.
Storage
Store between 20-25? C. Protect from light.?Keep out of the reach of children.