Nebivolol

Indications

Nebivolol is used for: Heart failure, Hypertension

Adult Dose

Oral Hypertension Adult: Initially, 5 mg once daily. May increase dose at intervals of 2 wk if needed. Max: 40 mg once daily. Elderly: >65 yr Initially, 2.5 mg once daily increased to 5 mg once daily if required. Oral Heart failure Adult: Initially, 1.25 mg once daily. May double dose every 1-2 wk if tolerated. Max: 10 mg once daily. Hepatic impairment 2.5 mg/day PO initially; increased cautiously

Child Dose

Renal Dose

Renal impairment: CrCl <30 mL/min: Initially, 2.5 mg once daily. Maintenance: Increased to 5 mg once daily if required.

Administration

May be taken with or without food.

Contra Indications

Hepatic impairment, sick sinus syndrome, 2nd and 3rd degree heart block (without a pacemaker), history of asthma, metabolic acidosis, severe peripheral arterial disease, severe bradycardia, cardiogenic shock or decompensated heart failure, untreated phaeochromocytoma. Pregnancy and lactation.

Precautions

Patients w/ 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 w/ coronary artery disease. Pregnancy and lactation. Monitoring Parameters Monitor ECG, BP and blood glucose in diabetic patients. Lactation: Not known whether drug is excreted into breast milk; use not recommended

Pregnancy-Lactation

Interactions

Increased plasma concentrations w/ potent CYP2D6 inhibitors (e.g. paroxetine, fluoxetine, propafenone, thioridazine, quinidine). Concomitant use w/ antiarrhythmic drugs (e.g. amiodarone, disopyramide) or nondihydropyridine Ca channel blockers (e.g. diltiazem, verapamil) may cause conduction disturbance. Additive negative effects on AV conduction and heart rate w/ other beta-adrenergic blocking agents or digoxin. Concurrent admin w/ catecholamine-depleting agents (e.g. reserpine) may result in additive hypotension or bradycardia. Abrupt withdrawal of clonidine may increase risk of rebound HTN.

Adverse Effects

Side effects of Nebivolol : 1-10% Headache (6-9%),Fatigue (2-5%),Dizziness (2-4%),Diarrhea (2-3%),Nausea (1-3%),Increased triglyceride levels and insulin resistance, decreased high-density lipoprotein (HDL) levels (1%),Insomnia (1%),Peripheral edema (1%),Weakness (1%) <1% Bradycardia.Chest pain,Dyspnea Potentially Fatal: Anaphylaxis.

Mechanism of Action

Nebivolol exhibits high selectivity for beta1-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.