pharmacopeia
GET
/api/v1/drug/nebivolol
2D structure
1-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)-2-[[2-(6-fluoro-3,4-dihydro-2H-chromen-2-yl)-2-hydroxyethyl]amino]ethanol
SMILES C1CC2=C(C=CC(=C2)F)OC1C(CNCC(C3CCC4=C(O3)C=CC(=C4)F)O)O
InChIKey KOHIRBRYDXPAMZ-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

The mechanism of action of the antihypertensive response of nebivolol has not been definitively established. Possible factors that may be involved include: (1) decreased heart rate, (2) decreased myocardial contractility, (3) diminution of tonic sympathetic outflow to the periphery from cerebral vasomotor centers,(4) suppression of renin activity and (5) vasodilation and decreased peripheral vascular resistance.

Indications

Sourced from openFDA
  • Nebivolol is a beta-adrenergic blocking agent indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.( 1.1 ) 1.1 Hypertension Nebivolol tablets are indicated for the treatment of hypertension, to lower blood pressure [ see Clinical Studies ( 14.1 ) ].ICD-10: I10

Contraindications

Sourced from openFDA
  • Nebivolol Tablets is contraindicated in the following conditions: Severe bradycardia Heart block greater than first degree Patients with cardiogenic shock Decompensated cardiac failure Sick sinus syndrome (unless a permanent pacemaker is in place) Patients with severe hepatic impairment (Child-Pugh >B) Patients who are hypersensitive to any component of this product.contraindicated

Dosage & administration

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Can be taken with and without food. Individualize to the needs of the patient and monitor during up-titration. ( 2 ) Hypertension: Most patients start at 5 mg once daily. Dose can be increased at 2-week intervals up to 40 mg. ( 2.1 ) 2.1 Hypertension The dose of nebivolol tablets must be individualized to the needs of the patient. For most patients, the recommended starting dose is 5 mg once daily, with or without food, as monotherapy or in combination with other agents. For patients requiring further reduction in blood pressure, the dose can be increased at 2-week intervals up to 40 mg. A more frequent dosing regimen is unlikely to be beneficial. Renal Impairment In patients with severe renal impairment (ClCr less than 30 mL/min) the recommended initial dose is 2.5 mg once daily; titrate up slowly if needed. Nebivolol tablets have not been studied in patients receiving dialysis [ see Clinical Pharmacology ( 12.4 ) ]. Hepatic Impairment In patients with moderate hepatic impairment, the recommended initial dose is 2.5 mg once daily; titrate up slowly if needed. Nebivolol tablets have not been studied in patients with severe hepatic impairment and Therefore it is not recommended in that population [ see Clinical Pharmacology ( 12.4 ) ]. 2.2 Subpopulations Geriatric Patients It is not necessary to adjust the dose in the elderly [ see use in Specific Populations ( 8.5 ) ]. CYP2D6 Polymorphism No dose adjustments are necessary for patients who are CYP2D6 poor metabolizers.

Warnings & precautions

Sourced from openFDA

Acute exacerbation of coronary artery disease upon cessation of therapy: Do not abruptly discontinue. ( 5.1 ) Diabetes: May mask symptoms of hypoglycemia and alter glucose levels; monitor (5.5) 5.1 Abrupt Cessation of Therapy Do not abruptly discontinue nebivolol therapy in patients with coronary artery disease. Severe exacerbation of angina, myocardial infarction and ventricular arrhythmias have been reported in patients with coronary artery disease following the abrupt discontinuation of therapy with β-blockers. Myocardial infarction and ventricular arrhythmias may occur with or without preceding exacerbation of the angina pectoris. Caution patients without overt coronary artery disease against interruption or abrupt discontinuation of therapy. As with other β-blockers, when discontinuation of nebivolol is planned, carefully observe and advise patients to minimize physical activity.Taper nebivolol over 1 to 2 weeks when possible. If the angina worsens or acute coronary insufficiency develops, re-start nebivolol promptly, at least temporarily. 5.2 Angina and Acute Myocardial Infarction Nebivolol was not studied in patients with angina pectoris or who had a recent MI. 5.3 Bronchospastic Diseases In general, patients with bronchospastic diseases should not receive β-blockers. 5.4 Anesthesia and Major Surgery Because beta-blocker withdrawal has been associated with an increased risk of MI and chest pain, patients already on beta-blockers should generally continue treatment throughout the perioperative period.

Adverse reactions

Sourced from openFDA

Most common adverse reactions ( 6.1 ): Headache, fatigue To report SUSPECTED ADVERSE REACTIONS, contact Modavar Pharmaceuticals LLC at 1-800-688-4697, or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Studies Experience Nebivolol tablets have been evaluated for safety in patients with hypertension and in patients with heart failure. The observed adverse reaction profile was consistent with the pharmacology of the drug and the health status of the patients in the clinical trials. Adverse reactions reported for each of these patient populations are provided below. Excluded are adverse reactions considered too general to be informative and those not reasonably associated with the use of the drug because they were associated with the condition being treated or are very common in the treated population. The data described below reflect worldwide clinical trial exposure to nebivolol tablets in 6,545 patients, including 5,038 patients treated for hypertension and the remaining 1,507 subjects treated for other cardiovascular diseases. Doses ranged from 0.5 mg to 40 mg. Patients received nebivolol tablets for up to 24 months, with over 1,900 patients treated for at least 6 months, and approximately 1,300 patients for more than one year. HYPERTENSION : In placebo-controlled clinical trials comparing nebivolol tablets with placebo, discontinuation of therapy due to adverse reactions was reported in 2.8% of patients treated with nebivolol and 2.2% of patients given placebo.

Use in specific populations

Sourced from openFDA

• Lactation: Breastfeeding is not recommended. ( 8.2 ) 8.1 Pregnancy Risk Summary Available data regarding use of nebivolol tablets in pregnant women are insufficient to determine whether there are drug-associated risks of adverse developmental outcomes. There are risks to the mother and fetus associated with poorly controlled hypertension in pregnancy.The use of beta blockers during the third trimester of pregnancy may increase the risk of hypotension, bradycardia, hypoglycemia, and respiratory depression in the neonate [see Clinical Considerations] . Oral administration of nebivolol to pregnant rats during organogenesis resulted in embryofetal and perinatal lethality at doses approximately equivalent to the maximum recommended human dose (MRHD). The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. Clinical Considerations Disease-associated maternal and/or embryo/fetal risk Hypertension in pregnancy increases the maternal risk for pre-eclampsia, gestational diabetes, premature delivery, and delivery complications (e.g., need for cesarean section, and post-partum hemorrhage).

Pharmacokinetics

Sourced from openFDA
Metabolism
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 CYP2D6 extensive metabolizers (most people), and 19 hours in poor metabolizers and exposure to d-nebivolol is substantially increased in poor metabolizers.

Overdosage

Sourced from openFDA

In clinical trials and worldwide post marketing experience there were reports of nebivolol overdose. The most common signs and symptoms associated with nebivolol tablets over dosage are bradycardia and hypotension. Other important adverse reactions reported with nebivolol tablets overdose include cardiac failure, dizziness, hypoglycemia, fatigue and vomiting. Other adverse reactions associated with β-blocker overdose include bronchospasm and heart block. The largest known ingestion of nebivolol tablets worldwide involved a patient who ingested up to 500 mg of nebivolol tablets along with several 100 mg tablets of acetylsalicylic acid in a suicide attempt. The patient experienced hyperhydrosis, pallor, depressed level of consciousness, hypokinesia, hypotension, sinus bradycardia, hypoglycemia, hypokalemia, respiratory failure and vomiting. The patient recovered. Because of extensive drug binding to plasma proteins, hemodialysis is not expected to enhance nebivolol clearance. If overdose occurs, provide general supportive and specific symptomatic treatment.

Approval history

Sourced from openFDA
  • Dec 17, 2007NDANDA021742Allergan
  • Apr 16, 2015ANDAANDA203659Ani Pharms
  • Jul 29, 2015ANDAANDA203828Indchemie Health
  • May 25, 2017ANDAANDA203821Glenmark Pharms Ltd
  • Nov 3, 2020ANDAANDA203825Hetero Labs Ltd Iii
  • Dec 17, 2021ANDAANDA211053Aurobindo Pharma Ltd
  • Dec 17, 2021ANDAANDA208717Cadila Pharms Ltd
  • Mar 15, 2022ANDAANDA213830Unichem

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
33,036 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Fatigue1,8345.6%
  2. 2Diarrhoea1,7715.4%
  3. 3Dyspnoea1,6975.1%
  4. 4Drug Ineffective1,6064.9%
  5. 5Nausea1,5944.8%
  6. 6Headache1,4234.3%
  7. 7Dizziness1,3794.2%
  8. 8Acute Kidney Injury1,2803.9%
  9. 9Off Label Use1,2503.8%
  10. 10Asthenia1,0853.3%
  11. 11Fall1,0383.1%
  12. 12Hypotension9482.9%
  13. 13Hypertension9212.8%
  14. 14Malaise8882.7%
  15. 15Vomiting8772.7%

Literature

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Recent PubMed references pinned to Nebivolol as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 128 ClinicalTrials.gov registrations naming Nebivolol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Nebivolol. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

Frequently asked questions

How does Nebivolol work?
The mechanism of action of the antihypertensive response of nebivolol has not been definitively established. Possible factors that may be involved include: (1) decreased heart rate, (2) decreased myocardial contractility, (3) diminution of tonic sympathetic outflow to the periphery from cerebral vasomotor centers,(4) suppression of renin activity and (5) vasodilation and decreased peripheral vascular resistance.
What is Nebivolol used for?
According to FDA labeling, Nebivolol carries indications including: Nebivolol is a beta-adrenergic blocking agent indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.( 1.1 ) 1.1 Hypertension Nebivolol tablets are indicated for the treatment of hypertension, to lower blood pressure [ see Clinical Studies ( 14.1 ) ].. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Nebivolol?
Nebivolol is classified as Beta blocking agents, selective, beta-Adrenergic Blocker, Adrenergic beta-Antagonists, Decreased Blood Pressure.
What are the brand names for Nebivolol?
Nebivolol is marketed under brand names including Bystolic, Byvalson.
What are the contraindications for Nebivolol?
Nebivolol labeling lists contraindications including: Nebivolol Tablets is contraindicated in the following conditions: Severe bradycardia Heart block greater than first degree Patients with cardiogenic shock Decompensated cardiac failure Sick sinus syndrome (unless a permanent pacemaker is in place) Patients with severe hepatic impairment (Child-Pugh >B) Patients who are hypersensitive to any component of this product.. Always consult the full prescribing information and a clinician.
Note. Data for nebivolol is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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