Nebivolol information from DrugsUpdate
P - Contraindicated in pregnancy
L - Contraindicated in lactation
FI - Food *
Nebivolol is a β1 receptor blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and, in Europe, also for left ventricular failure. It is highly cardioselective under certain circumstances.
Pharmacodynamics
Pharmacokinetics
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 hours.
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 hours (nebivolol), 24 hours (hydroxy metabolites).
Nebivolol Indications / Nebivolol Uses
Information Not Available
Nebivolol Adverse Reactions / Nebivolol Side Effects
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.
Precautions
Monitor
Closely monitor patients receiving anesthetic agents that depress myocardial function.
Overdosage
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.
Special 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).
Other 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.
Other Interactions
Food Interaction
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.
Dosage
Oral
Hypertension
Adult: 5 mg daily. May increase dose at intervals of 2 weeks to a max of 40 mg once daily, if needed.
Elderly: >65 years: 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 weeks up to a max of 10 mg once daily.
Elderly: Initially 1.25 mg once daily. If tolerated, double the dose every 1-2 weeks up to a max of 10 mg once daily.
Food(before/after)
May be taken with or without food
List of Contraindications
Nebivolol and Pregnancy
Contraindicated in pregnancy
Nebivolol and Lactation
Contraindicated in lactation
Nebivolol and Children
Safety and efficacy not established
Nebivolol and Geriatic
No overall difference in efficacy or adverse reactions between older and younger patients.
Nebivolol and Other 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.
Storage
Oral
Store at 20-25°C (68-77°F). Protect from light
Lab interference
Oral
Store at 20-25°C (68-77°F). Protect from light
FOLLOW US:
