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Some studies suggest lisinopril has a plasma half-life of 12-13 hours, while other studies indicate a terminal serum half-life of approximately 40 hours.
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Lisinopril is a widely used angiotensin-converting enzyme (ACE) inhibitor, primarily prescribed for the treatment of hypertension and congestive heart failure. Understanding its pharmacokinetics, particularly its half-life, is crucial for optimizing its therapeutic efficacy and safety.
The effective half-life of lisinopril, which is crucial for its accumulation in the body, averages around 12.6 hours . This effective half-life is distinct from the terminal serum half-life, which is approximately 40 hours . The terminal phase is believed to reflect the binding of lisinopril to ACE, rather than its pharmacologically active duration.
Lisinopril reaches a steady state after two daily doses, administered every 24 hours . This rapid attainment of steady state is beneficial for maintaining consistent therapeutic levels in the bloodstream.
Lisinopril is not metabolized by the liver and is eliminated primarily through the kidneys . It undergoes glomerular filtration, tubular secretion, and reabsorption. This renal route of elimination underscores the importance of kidney function in the drug's pharmacokinetics.
In patients with impaired renal function, the half-life of lisinopril is significantly prolonged. For instance, in individuals with severe renal failure, the effective half-life can be doubled or even tripled compared to those with normal renal function. This necessitates dosage adjustments to prevent drug accumulation and potential toxicity in such patients.
Given its effective half-life, lisinopril is typically administered once daily, which simplifies the dosing regimen and enhances patient compliance . However, in patients with renal impairment, lower doses are recommended to avoid excessive accumulation.
Lisinopril's bioavailability is approximately 25% and is not significantly affected by food intake . This allows for flexible dosing schedules without the need to coordinate with meals.
The pharmacokinetics of lisinopril, particularly its effective half-life of 12.6 hours, supports its once-daily dosing regimen, making it a convenient option for patients. However, careful consideration is required for patients with renal impairment to adjust dosing appropriately. Understanding these pharmacokinetic properties ensures the safe and effective use of lisinopril in clinical practice.
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