Half-Life of Nadolol
The half-life of nadolol is approximately 20 to 24 hours in patients with normal renal function. 1
Pharmacokinetic Profile of Nadolol
Nadolol is a nonselective beta-adrenergic receptor blocking agent with several key pharmacokinetic properties:
- Absorption: Variable oral absorption, averaging about 30% bioavailability
- Distribution: Approximately 30% of nadolol in serum is reversibly bound to plasma protein
- Metabolism: Unlike many other beta-blockers, nadolol is not metabolized by the liver
- Excretion: Excreted unchanged, principally by the kidneys
- Half-life: 20 to 24 hours in patients with normal renal function 1
Factors Affecting Nadolol's Half-Life
The half-life of nadolol can vary significantly based on several factors:
- Renal function: Since nadolol is primarily excreted unchanged by the kidneys, its half-life increases significantly in patients with renal failure 1
- Age: In children, the serum half-life may be shorter (3.2-4.3 hours) compared to adults 2
- Kidney disease: In patients with chronic kidney disease, the half-life can increase to 18.2-68.6 hours (up to double the normal half-life) 2
Clinical Implications of Nadolol's Half-Life
The long half-life of nadolol has several important clinical implications:
Once-daily dosing: The extended half-life allows for once-daily administration in both hypertension and angina pectoris 1, 3
Steady-state concentrations: Steady-state serum concentrations are achieved in six to nine days with once-daily dosing in individuals with normal renal function 1
Dose adjustments: Dosage adjustments are necessary for patients with renal impairment due to the prolonged half-life 1
Extracorporeal removal: During hemodialysis, the half-life of nadolol is reduced to approximately 3.56 hours (range 3.0-8.5 hours), indicating that it can be effectively removed by hemodialysis 4, 2
Comparison to Other Beta-Blockers
Nadolol's half-life of 20-24 hours is longer than many other beta-blockers, making it one of the few beta-blocking drugs that have clearly been shown to be effective with once-daily administration 3. This contrasts with other beta-blockers that may require multiple daily doses for optimal effect.
Common Pitfalls
Renal function assessment: Failing to assess renal function before prescribing nadolol can lead to drug accumulation and toxicity in patients with kidney impairment
Drug interactions: The bioavailability of nadolol can be significantly reduced by co-administration of green tea 2
Enterohepatic circulation: Nadolol undergoes enterohepatic circulation, and activated charcoal can decrease its bioavailability 2
Abrupt discontinuation: As with other beta-blockers, abrupt discontinuation of nadolol in patients with coronary artery disease can lead to exacerbation of angina, and in some cases, myocardial infarction and ventricular dysrhythmias 1
Understanding nadolol's long half-life is crucial for appropriate dosing, especially in patients with renal impairment, and helps explain its suitability for once-daily administration in clinical practice.