Nebivolol

Indications
 Oral
Hypertension
Adult: 5 mg daily. May increase dose at intervals of 2 wk to a max of 40 mg once daily, if needed.
Elderly: >65 yr: Initially, 2.5 mg daily.
Renal impairment: Initially, 2.5 mg daily. Maintenance: Increase to 5 mg daily if required.
Oral
Heart failure
Adult: Initially, 1.25 mg once daily. May double dose every 1-2 wk up to a max of 10 mg once daily.
Elderly: Initially 1.25 mg once daily. If tolerated, double the dose every 1-2 wk up to a max of 10 mg once daily.

Special Populations: Management of HTN in renal impairment: Initially, 2.5 mg daily.
Contraindications
 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.
Warnings / Precautions
 Elderly. History of anaphylaxis to various allergens, 1st degree AV block, peripheral arterial disease, DM, compensated heart failure, myasthenia gravis, history of psychiatric illness, renal impairment. May mask signs of hyperthyroidism (e.g. tachycardia).
Adverse Reactions
 Peripheral oedema, bradycardia, chest pain; headache, fatigue, dizziness, insomnia; rash; hypercholesterolaemia, decreased HDL levels, hyperuricaemia, increased triglyceride levels, increased uric acid levels; diarrhoea, nausea, abdominal pain; thrombocytopenia; paraesthesia, weakness; increased BUN; dyspnoea.
Potentially Fatal: Anaphylaxis.
Overdose Reactions
 Symptoms: Severe hypotension, bradycardia, heart failure, bronchospasm, hypoglycaemia. Management: Treat initially with IV fluids. Sympathomimetics, glucagon or a pacemaker may be used to treat toxic bradycardia, asystole, and/or hypotension. Other treatment is symptomatic and supportive. Not dialysable.
Drug Interactions
 Attenuation of reflex tachycardia and increased risk of hypotension with volatile halogenated anaesthetics. Increased risk of hypotension with dihydropyridine-type calcium antagonists. Hypotensive effect may be increased with antipsychotics, TCAs, barbiturates and phenothiazines. Effects may be reduced with sympathomimetic agents. Increased levels/effects with CYP2D6 inhibitors e.g. paroxetine, fluoxetine, thioridazine and quinidine.
Potentially Fatal: Additive negative influence on contractility and AV conduction with verapamil and diltiazem type drugs; profound hypotension and AV block with IV verapamil. Exacerbation of heart failure with centrally-acting antihypertensive, abrupt withdrawal may increase risk of rebound hypertension. Increased effect on AV conduction with antiarrhythmic drugs. Increased risk of hypertension, severe bradycardia and heart block when used with sympathomimetics with mixed α- and β-adrenergic effects.
See Below for More nebivolol Drug Interactions
Food Interactions
 Hypertension may be exacerbated by bayberry, blue cohosh, cayenne, ephedra, ginger, American ginseng, kola and licorice. Antihypertensive effect may be increased by black cohosh, California poppy, coleus, golden seal, hawthorn, mistletoe, periwinkle, quinine and shepherd's purse.
Mechanism of Actions
 Nebivolol exhibits a high selectivity for β1-adrenergic receptors and acts by reducing the peripheral vascular resistance by modulating nitric oxide release.
Absorption: Absorbed rapidly from the GI tract (oral). Peak plasma concentrations after 0.5-4 hr.
Distribution: Protein-binding: 98%. Enters breast milk.
Metabolism: Hepatic: Extensively by alicyclic and aromatic hydroxylation, N-dealkylation and glucuronidation.
Excretion: Via urine and faeces (as metabolites). Elimination half-life: 10 hr (nebivolol), 24 hr (hydroxy metabolites).
Administration
 May be taken with or without food.
Storage Conditions
 Oral: Store at 20-25°C (68-77°F). Protect from light.
ATC Classification
 C07AB12 - nebivolol ; Belongs to the class of selective beta-blocking agents. Used in the treatment of cardiovascular diseases.
Storage
 Oral: Store at 20-25°C (68-77°F). Protect from light.
Available As
  • Nebivolol 10 mg
  • Nebivolol 2.5 mg
  • Nebivolol 5 mg

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