Nebivolol

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Nebivolol Brand Name– Bystolic

What is Nebivolol

Nebivolol is a beta-1 selective (cardioselective) adrenergic antagonist.

Unlike propranolol, which nonspecifically blocks beta-1 and beta-2 adrenoreceptors, or atenolol, which has more affinity for the beta-1 adrenoreceptor but at higher doses loses its beta-1 specificity, nebivolol has an even higher affinity for the beta-1 adrenoreceptor at therapeutic doses and also possesses vasodilatory properties due to nitric oxide modulation.

Nebivolol possesses antioxidant properties, is lipophilic, and lacks intrinsic sympathomimetic activity (ISA).

Unlike other beta-blocking agents, nebivolol decreases vascular peripheral resistance, improves left ventricular performance, and is not associated with an acute decrease in cardiac output sometimes seen with the initiation of other beta blockers.

Nebivolol has been studied in patients with hypertension and heart failure and is approved in Europe for mild to moderate, uncomplicated hypertension and mild to moderate heart failure.

Nebivolol has specifically been evaluated in elderly patients with a clinical history of chronic heart failure with either preserved or reduced left ventricular ejection fraction.

The primary outcome of the SENIORS trial, Study of the Effects of Nebivolol Intervention on Outcomes and Rehospitalization in Seniors with heart failure (N=2135, mean age 76.1 years), was a composite of all cause mortality or cardiovascular hospital admission (time to first event).

The composite end point occurred in 31.1% of the nebivolol group compared 35.3% of the placebo group (hazard ratio 0.86, 95% CI 0.74—0.99; P=0.039). No significant differences in age, gender, or ejection fraction was seen on the effect of nebivolol on the primary outcome.

Death (all causes) occurred in 15.8% of the nebivolol group and 18.1% of the placebo group (HR 0.88, 95% CI 0.71—1.08; P=0.21).

Nebivolol (Bystolic™) was approved in the US in December 2007 for the treatment of hypertension, either alone or in combination with other antihypertensive agents.

Indications

  • hypertension
  • migraine prophylaxis

For the treatment of hypertension either alone or in combination with other agents

Side Effects

  1. abdominal pain
  2. angioedema
  3. asthenia
  4. AV block
  5. bradycardia
  6. bronchospasm
  7. chest pain (unspecified)
  8. diaphoresis
  9. diarrhea
  10. dizziness
  11. drowsiness
  12. dyspnea
  13. elevated hepatic enzymes
  14. fatigue
  15. headache
  16. hypercholesterolemia
  17. hypertension
  18. hypertriglyceridemia
  19. hyperuricemia
  20. hypotension
  21. impotence (erectile dysfunction)
  22. insomnia
  23. myocardial infarction
  24. nausea
  25. palpitations
  26. paresthesias
  27. peripheral edema
  28. peripheral vasoconstriction
  29. pruritus
  30. psoriasis
  31. pulmonary edema
  32. rash
  33. renal failure (unspecified)
  34. sinus tachycardia
  35. syncope
  36. thrombocytopenia
  37. tremor
  38. urticaria
  39. vasculitis
  40. vertigo
  41. vomiting
  42. withdrawal

Monitoring Parameters

  • blood pressure
  • heart rate
  • LFTs
  • serum creatinine

Contraindications

  • abrupt discontinuation
  • acute bronchospasm
  • acute heart failure
  • AV block
  • bradycardia
  • breast-feeding
  • cardiogenic shock
  • children
  • coronary artery disease
  • diabetes mellitus
  • geriatric
  • hepatic disease
  • hyperthyroidism
  • infants
  • neonates
  • peripheral vascular disease
  • pheochromocytoma
  • pregnancy
  • renal impairment
  • sick sinus syndrome
  • surgery
  • thyrotoxicosis

Nebivolol is contraindicated in patients with known nebivolol hypersensitivity or hypersensitivity to any of the product excipients.

Interactions

  • Abiraterone
  • Acetaminophen; Aspirin, ASA; Caffeine
  • Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
  • Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
  • Acetaminophen; Diphenhydramine
  • Adenosine
  • Albiglutide
  • Aldesleukin, IL-2
  • Alemtuzumab
  • Alfentanil
  • Alfuzosin
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Alogliptin; Metformin
  • Alpha-blockers
  • Alpha-glucosidase Inhibitors
  • Alprostadil
  • Amifostine
  • Amiodarone
  • Amlodipine
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Celecoxib
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amobarbital
  • Amyl Nitrite
  • Antithyroid agents
  • Apomorphine
  • Apraclonidine
  • Aripiprazole
  • Artemether; Lumefantrine
  • Articaine; Epinephrine
  • Asenapine
  • Aspirin, ASA
  • Aspirin, ASA; Butalbital; Caffeine
  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Citric Acid; Sodium Bicarbonate
  • Aspirin, ASA; Dipyridamole
  • Aspirin, ASA; Omeprazole
  • Aspirin, ASA; Oxycodone
  • Aspirin, ASA; Pravastatin
  • Atazanavir
  • Atazanavir; Cobicistat
  • Baclofen
  • Belladonna Alkaloids; Ergotamine; Phenobarbital
  • Beta-agonists
  • Bismuth Subsalicylate
  • Bismuth Subsalicylate; Metronidazole; Tetracycline
  • Bosentan
  • Bretylium
  • Brexpiprazole
  • Bupivacaine
  • Bupivacaine Liposomal
  • Bupivacaine; Lidocaine
  • Bupropion
  • Bupropion; Naltrexone
  • Cabergoline
  • Caffeine; Ergotamine
  • Canagliflozin; Metformin
  • Carbetapentane; Chlorpheniramine
  • Carbetapentane; Chlorpheniramine; Phenylephrine
  • Carbetapentane; Diphenhydramine; Phenylephrine
  • Carbidopa; Levodopa
  • Carbidopa; Levodopa; Entacapone
  • Cariprazine
  • Ceritinib
  • Cevimeline
  • Chloroprocaine
  • Chlorpheniramine
  • Chlorpheniramine; Codeine
  • Chlorpheniramine; Dextromethorphan
  • Chlorpheniramine; Dextromethorphan; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Phenylephrine
  • Chlorpheniramine; Pseudoephedrine
  • Chlorpromazine
  • Chlorthalidone; Clonidine
  • Choline Salicylate; Magnesium Salicylate
  • Cimetidine
  • Cinacalcet
  • Citalopram
  • Clevidipine
  • Clonidine
  • Clozapine
  • Co-Enzyme Q10, Ubiquinone
  • Cobicistat
  • Cocaine
  • Codeine; Phenylephrine; Promethazine
  • Codeine; Promethazine
  • Conivaptan
  • Crizotinib
  • Dacomitinib
  • Dapagliflozin; Metformin
  • Darifenacin
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Delavirdine
  • Desflurane
  • Desvenlafaxine
  • Dexmedetomidine
  • Dextromethorphan; Diphenhydramine; Phenylephrine
  • Dextromethorphan; Promethazine
  • Dextromethorphan; Quinidine
  • Diazoxide
  • Digoxin
  • Dihydroergotamine
  • Diltiazem
  • Dipeptidyl Peptidase-4 Inhibitors
  • Diphenhydramine
  • Diphenhydramine; Hydrocodone; Phenylephrine
  • Diphenhydramine; Ibuprofen
  • Diphenhydramine; Naproxen
  • Diphenhydramine; Phenylephrine
  • Dipyridamole
  • Disopyramide
  • Donepezil
  • Donepezil; Memantine
  • Doxazosin
  • Dronedarone
  • Dulaglutide
  • Duloxetine
  • Dutasteride; Tamsulosin
  • Eliglustat
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Empagliflozin; Linagliptin; Metformin
  • Empagliflozin; Metformin
  • Enalapril; Felodipine
  • Encainide
  • Enflurane
  • Epoprostenol
  • Ergonovine
  • Ergotamine
  • Ertugliflozin; Metformin
  • Escitalopram
  • Estradiol
  • Estradiol Cypionate; Medroxyprogesterone
  • Etomidate
  • Exenatide
  • Fedratinib
  • Felodipine
  • Fenoldopam
  • Fingolimod
  • Fish Oil, Omega-3 Fatty Acids (Dietary Supplements)
  • Flecainide
  • Fluorescein
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fluphenazine
  • food
  • Fospropofol
  • Galantamine
  • General anesthetics
  • Ginger, Zingiber officinale
  • Givosiran
  • Glipizide; Metformin
  • Glucagon
  • Glyburide; Metformin
  • Guanabenz
  • Guanfacine
  • Haloperidol
  • Halothane
  • Hydralazine; Isosorbide Dinitrate, ISDN
  • Icosapent ethyl
  • Iloperidone
  • Iloprost
  • Imatinib
  • Incretin Mimetics
  • Indinavir
  • Insulin Degludec; Liraglutide
  • Insulin Glargine; Lixisenatide
  • Insulins
  • Intravenous Lipid Emulsions
  • Isocarboxazid
  • Isoflurane
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Isosorbide Dinitrate, ISDN
  • Isosorbide Mononitrate
  • Isradipine
  • Ivabradine
  • Ketamine
  • Lacosamide
  • Lanreotide
  • Lasmiditan
  • Levobupivacaine
  • Levodopa
  • Levothyroxine
  • Levothyroxine; Liothyronine (Porcine)
  • Levothyroxine; Liothyronine (Synthetic)
  • Lidocaine
  • Lidocaine; Prilocaine
  • Linagliptin; Metformin
  • Linezolid
  • Liothyronine
  • Liraglutide
  • Lithium
  • Lixisenatide
  • Lofexidine
  • Lopinavir; Ritonavir
  • Lorcaserin
  • Lovastatin; Niacin
  • Lurasidone
  • Magnesium Salicylate
  • Mefloquine
  • Meglitinides
  • Meperidine; Promethazine
  • Mepivacaine
  • Mepivacaine; Levonordefrin
  • Mestranol; Norethindrone
  • Metformin
  • Metformin; Pioglitazone
  • Metformin; Repaglinide
  • Metformin; Rosiglitazone
  • Metformin; Saxagliptin
  • Metformin; Sitagliptin
  • Methacholine
  • Methohexital
  • Methylergonovine
  • Methysergide
  • Milrinone
  • Mirabegron
  • Nefazodone
  • Nesiritide, BNP
  • Neuromuscular blockers
  • Niacin, Niacinamide
  • Niacin; Simvastatin
  • Nicardipine
  • Nifedipine
  • Nimodipine
  • Nisoldipine
  • Nitrates
  • Nitroglycerin
  • Nitroprusside
  • Non-Ionic Contrast Media
  • Nonsteroidal antiinflammatory drugs
  • Octreotide
  • Olanzapine
  • Ombitasvir; Paritaprevir; Ritonavir
  • Oritavancin
  • Oxymetazoline
  • Paliperidone
  • Panobinostat
  • Paroxetine
  • Pasireotide
  • Pazopanib
  • Pentoxifylline
  • Perindopril; Amlodipine
  • Perphenazine
  • Perphenazine; Amitriptyline
  • Phenelzine
  • Phenoxybenzamine
  • Phentolamine
  • Phenylephrine; Promethazine
  • Pilocarpine
  • Pimozide
  • Pirfenidone
  • Pramlintide
  • Prazosin
  • Prilocaine
  • Prilocaine; Epinephrine
  • Procainamide
  • Procaine
  • Promethazine
  • Propofol
  • Quinidine
  • Quinine
  • Ranolazine
  • Rasagiline
  • Remifentanil
  • Reserpine
  • Rifampin
  • Risperidone
  • Ritonavir
  • Rivastigmine
  • Rolapitant
  • Ropivacaine
  • Salsalate
  • Selegiline
  • Semaglutide
  • Sertraline
  • Sevoflurane
  • SGLT2 Inhibitors
  • Sildenafil
  • Silodosin
  • Siponimod
  • Sotalol
  • Sufentanil
  • Sulfonylureas
  • Sympathomimetics
  • Tacrine
  • Tamsulosin
  • Tasimelteon
  • Terazosin
  • Terbinafine
  • Tetrabenazine
  • Tetracaine
  • Thalidomide
  • Thiazolidinediones
  • Thiopental
  • Thioridazine
  • Thiothixene
  • Thyroid hormones
  • Tipranavir
  • Tizanidine
  • Trandolapril; Verapamil
  • Tranylcypromine
  • Trazodone
  • Vemurafenib
  • Verapamil
  • Yohimbine
  • Ziprasidone

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