CORGARD
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CORGARD (CORGARD).
Nonselective beta-adrenergic receptor antagonist; competitively blocks beta1- and beta2-adrenergic receptors, leading to decreased heart rate, myocardial contractility, and blood pressure. Also prolongs sinoatrial node refractory period and inhibits renin release.
| Metabolism | Primarily excreted unchanged by the kidneys; minimal hepatic metabolism. Not extensively metabolized by CYP450 enzymes. |
| Excretion | Renal (unchanged, ~85-90%); fecal (<5%); biliary (<2%). |
| Half-life | Terminal elimination half-life: 20-24 hours (may extend to 40 hours in renal impairment). Clinical context: Allows once-daily dosing; steady-state achieved in 5-7 days. |
| Protein binding | ~30%, bound to albumin (minimal). |
| Volume of Distribution | 2-3 L/kg (large Vd indicates extensive tissue distribution; negligible CNS penetration due to hydrophilicity). |
| Bioavailability | Oral: ~30-40% (due to incomplete absorption and first-pass metabolism). |
| Onset of Action | Oral: 1-2 hours (beta-blockade); IV: rapid (minutes). |
| Duration of Action | Oral: 24-36 hours; IV: up to 8-12 hours. Clinical note: Nadolol's long duration permits once-daily dosing for hypertension and angina; abrupt withdrawal may precipitate rebound hypertension or ischemia. |
| Action Class | Quinolones/ Fluroquinolones |
| Brand Substitutes | Wocipflo 500mg Tablet, Strox 500mg Tablet, Ciprodac 500 Tablet, Alciflox 500mg Tablet, Cifran OD 500mg Tablet |
40 mg orally once daily for hypertension; initial dose 40 mg once daily for angina, titrate up to 80-240 mg once daily. Maximum dose 320 mg/day.
| Dosage form | TABLET |
| Renal impairment | CrCl >50 mL/min: no adjustment; CrCl 31-50 mL/min: 40 mg every 48 hours; CrCl 10-30 mL/min: 20 mg every 48 hours; CrCl <10 mL/min: 20 mg every 72 hours. |
| Liver impairment | No specific Child-Pugh adjustments; use with caution in severe impairment due to reduced metabolism. |
| Pediatric use | Not FDA-approved for pediatric use. Limited data: 1-2 mg/kg/day orally in divided doses; maximum 80 mg/day. |
| Geriatric use | Initial dose 20 mg orally once daily; titrate slowly due to increased sensitivity and comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CORGARD (CORGARD).
| Breastfeeding | Nadolol is excreted in breast milk. M/P ratio: approximately 2.0. Limited human data; potential for infant bradycardia and hypoglycemia. Use with caution, monitor infant for adverse effects. |
| Teratogenic Risk | FDA Pregnancy Category D. First trimester: Risk of congenital anomalies (e.g., cardiovascular defects) based on human data. Second and third trimesters: Potential fetal bradycardia, intrauterine growth restriction, hypoglycemia, and neonatal hypotension. Avoid use unless benefit outweighs risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
Abrupt discontinuation may exacerbate angina and increase risk of myocardial infarction or ventricular arrhythmias in patients with coronary artery disease.
| Serious Effects |
Bronchial asthma, sinus bradycardia, heart block greater than first degree, cardiogenic shock, overt cardiac failure, hypersensitivity to nadolol.
| Precautions | Use caution in patients with bronchospastic diseases, diabetes mellitus (may mask hypoglycemia), hyperthyroidism (may mask tachycardia), and peripheral vascular disease. Monitor renal function; dose adjustment required in impairment. Avoid abrupt withdrawal. |
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| Monitor maternal blood pressure and heart rate throughout pregnancy. Fetal heart rate monitoring and ultrasound assessment of fetal growth during second and third trimesters. Neonatal monitoring for bradycardia, hypoglycemia, and respiratory depression after delivery. |
| Fertility Effects | No specific data on fertility impairment in humans. In animal studies, no adverse effects on fertility observed. Beta-blockers may rarely affect libido or sexual function. |