NEBIVOLOL HYDROCHLORIDE
Clinical safety rating: safe
Animal studies have demonstrated safety
Selective beta-1 adrenergic receptor antagonist with nitric oxide-mediated vasodilatory activity via stimulation of beta-3 receptors.
| Metabolism | Primarily metabolized by CYP2D6 via aromatic hydroxylation and glucuronidation; active hydroxylated metabolites contribute to pharmacological effect. |
| Excretion | Approximately 38% renal, 48% fecal (unchanged drug and metabolites); extensive hepatic metabolism (CYP2D6) with glucuronidation; <1% excreted unchanged in urine. |
| Half-life | Terminal elimination half-life: 12-19 hours in extensive metabolizers; up to 30-50 hours in poor CYP2D6 metabolizers; clinically, once-daily dosing is effective due to pharmacodynamic half-life >40 hours. |
| Protein binding | 98% bound primarily to albumin, minor binding to alpha1-acid glycoprotein. |
| Volume of Distribution | Vd: 10-12 L/kg (extensive distribution into tissues, particularly lung and liver). |
| Bioavailability | Oral bioavailability: 12-96% (mean ~30%) due to extensive first-pass metabolism; food intake reduces rate but not extent; bioavailability is increased in poor CYP2D6 metabolizers. |
| Onset of Action | Oral: 1-2 hours for beta-blockade (reduction in heart rate and blood pressure); maximal effect at 4-6 hours. |
| Duration of Action | 24-hour duration with once-daily dosing; antihypertensive effect persists for >24 hours; significant beta-blockade still present at 48 hours after last dose. |
5 mg orally once daily. May be initiated at 2.5 mg in patients with renal impairment or those at risk of hypotension. Titrate at 2-week intervals up to 40 mg once daily.
| Dosage form | TABLET |
| Renal impairment | For GFR <30 mL/min/1.73 m²: initial dose 2.5 mg once daily; titrate cautiously. For GFR 30-59 mL/min/1.73 m²: no adjustment required. Hemodialysis: not dialyzable; administer post-dialysis. |
| Liver impairment | Child-Pugh Class A: initiate at 2.5 mg once daily; titrate cautiously. Child-Pugh Class B or C: contraindicated due to increased exposure. |
| Pediatric use | Not FDA-approved for pediatric use. Limited data: doses of 0.1-0.3 mg/kg once daily have been studied in hypertensive children; maximum 5 mg daily. |
| Geriatric use | Initiate at 2.5 mg once daily; titrate slowly. Monitor for hypotension, bradycardia, and falls. Consider reduced clearance and comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Other drugs that lower heart rate or blood pressure can have additive effects Can cause bradycardia and heart failure.
| Breastfeeding | Present in breast milk; M/P ratio unknown. Due to limited data and potential for infant bradycardia and hypoglycemia, caution advised. Use only if clearly needed. |
| Teratogenic Risk | First trimester: Limited human data; animal studies show no teratogenicity at doses 1.7 mg/kg/day (rat) and 0.8 mg/kg/day (rabbit). Second/third trimester: Beta-blockers may cause fetal bradycardia, hypoglycemia, and growth restriction. Avoid in pregnant women with heart failure unless benefit outweighs risk. |
■ FDA Black Box Warning
No FDA black box warning.
| Common Effects | Nausea Headache Fatigue Constipation Diarrhea Dizziness Breathlessness Edema swelling |
| Serious Effects |
["Severe bradycardia","Heart block greater than first degree (except in patients with a functioning artificial pacemaker)","Cardiogenic shock","Decompensated heart failure","Sick sinus syndrome (unless pacemaker present)","Hypersensitivity to nebivolol or any component","Severe hepatic impairment (Child-Pugh Class B or C)"]
| Precautions | ["Abrupt discontinuation may exacerbate angina or myocardial infarction in patients with coronary artery disease","Can mask symptoms of hyperthyroidism and hypoglycemia","May cause bradycardia, heart block, or hypotension","Caution in patients with compensated heart failure; may worsen symptoms","Use with caution in patients with bronchospastic disease, peripheral vascular disease, or diabetes","Risk of anaphylactic reactions and severe cutaneous adverse reactions"] |
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| Fetal Monitoring |
| Maternal: Heart rate, blood pressure, signs of heart failure. Fetal: Heart rate, growth assessment via ultrasound; monitor for bradycardia and hypoglycemia in neonate. |
| Fertility Effects | No human data on fertility impairment. Animal studies show no adverse effects on fertility in rats at doses up to 1.7 mg/kg/day. |