NADOLOL
Clinical safety rating: caution
Animal studies have proved adverse effects but may be safe for humans
Non-selective beta-adrenergic receptor antagonist (beta-blocker) that competitively blocks beta1 and beta2 receptors, reducing heart rate, myocardial contractility, and blood pressure.
| Metabolism | Not significantly metabolized; excreted unchanged by the kidneys. |
| Excretion | Renal (unchanged drug) 75-85%; fecal/biliary <5% |
| Half-life | Terminal elimination half-life: 14–24 hours (average 20 hours); prolonged in renal impairment (up to 45 hours) allowing once-daily dosing |
| Protein binding | 30%, primarily bound to albumin |
| Volume of Distribution | 1.9 L/kg; extensive extravascular distribution with low tissue binding |
| Bioavailability | Oral: 30–40% (range 20–50%) due to first-pass metabolism; not highly variable |
| Onset of Action | Oral: 1–2 hours; peak effect at 6–9 hours |
| Duration of Action | 24 hours (once-daily dosing); longer in renal impairment |
40 to 80 mg orally once daily, may be increased at 3-7 day intervals up to 240 mg once daily.
| Dosage form | TABLET |
| Renal impairment | CrCl >50 mL/min: no adjustment; CrCl 31-50 mL/min: administer every 24 hours; CrCl 10-30 mL/min: administer every 24-36 hours; CrCl <10 mL/min: administer every 40-60 hours. |
| Liver impairment | No specific dosage adjustment guidelines for Child-Pugh scores; use with caution and monitor for bradycardia and hypotension. |
| Pediatric use | Hypertension: initial 1 mg/kg orally once daily (max 80 mg/day); may increase every 3-5 days to 2-3 mg/kg once daily (max 120 mg/day). |
| Geriatric use | Start at 20 mg orally once daily; increase slowly due to increased sensitivity to beta-blockade and potential renal impairment. |
| 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 Abrupt withdrawal may exacerbate angina pectoris or cause myocardial infarction.
| Breastfeeding | Nadolol is excreted into breast milk. The M/P ratio is approximately 0.3-1.7, with low relative infant dose (<2% of maternal weight-adjusted dose). No adverse effects reported in nursing infants. However, monitor for bradycardia and hypoglycemia. Use with caution, weighing benefits vs. risk. |
| Teratogenic Risk | Nadolol is a non-selective beta-blocker. In the first trimester, there is limited data but increased risk of intrauterine growth restriction (IUGR), preterm birth, and fetal bradycardia. In the second and third trimesters, nadolol crosses the placenta and may cause fetal bradycardia, hypoglycemia, and respiratory depression in the neonate. Beta-blocker use has been associated with persistent pulmonary hypertension in the newborn. Overall, use only if clearly needed, considering fetal risks. |
■ FDA Black Box Warning
No FDA black box warning.
| Common Effects | angina |
| Serious Effects |
["Bronchial asthma or bronchospastic conditions","Sinus bradycardia","Heart block greater than first degree","Cardiogenic shock","Overt cardiac failure","Hypersensitivity to nadolol"]
| Precautions | ["Abrupt withdrawal may exacerbate angina or precipitate myocardial infarction in patients with coronary artery disease.","May mask signs of hyperthyroidism or hypoglycemia.","Use with caution in patients with bronchospastic disease (e.g., asthma) due to beta2 blockade.","Can cause bradycardia, heart block, or worsen heart failure.","May exacerbate peripheral vascular disease."] |
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| Fetal Monitoring | Monitor maternal heart rate, blood pressure, and signs of heart failure. Fetal monitoring includes ultrasound for growth restriction, amniotic fluid index, and fetal heart rate monitoring (especially for bradycardia). Neonatal monitoring is recommended for bradycardia, hypoglycemia, and respiratory depression. |
| Fertility Effects | No known adverse effects on fertility in humans. Beta-blockers may theoretically affect sexual function, but no specific data on nadolol impacting female or male fertility. |