What is the half life of losartan

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Half-Life of Losartan: Pharmacokinetics and Metabolism

Introduction to Losartan Pharmacokinetics

Losartan is a widely used angiotensin II receptor antagonist, primarily prescribed for managing hypertension and heart failure. Understanding its pharmacokinetics, including its half-life, is crucial for optimizing therapeutic regimens and ensuring effective patient care.

Losartan Absorption and Metabolism

Upon oral administration, losartan is rapidly absorbed, reaching peak plasma concentrations within 1 to 2 hours . Approximately 14% of the administered dose is converted into its active metabolite, E-3174, which is significantly more potent than losartan itself 12.

Half-Life of Losartan and Its Metabolite

The terminal half-life of losartan ranges from 1.5 to 2.5 hours 256. This relatively short half-life necessitates consideration of its active metabolite, E-3174, which has a longer half-life of approximately 6 to 9 hours 136. The extended half-life of E-3174 contributes to the prolonged pharmacological effects of losartan, making it effective for once-daily dosing in clinical practice.

Pharmacokinetic Variability

The pharmacokinetics of losartan and E-3174 are linear and dose-proportional, with no significant changes observed with repeated administration 15. Factors such as age, sex, and race do not significantly affect the pharmacokinetics of losartan, and no dosage adjustments are necessary for patients with mild hepatic impairment or varying degrees of renal insufficiency .

Clinical Implications

The relatively short half-life of losartan itself, combined with the longer half-life of its active metabolite, E-3174, supports its use in once-daily dosing regimens. This pharmacokinetic profile ensures sustained antihypertensive effects and contributes to the drug's favorable safety and efficacy profile 136.

Conclusion

In summary, losartan has a terminal half-life of 1.5 to 2.5 hours, while its active metabolite, E-3174, has a longer half-life of 6 to 9 hours. This pharmacokinetic characteristic underpins the drug's effectiveness in managing hypertension and heart failure with once-daily dosing. Understanding these parameters is essential for optimizing losartan therapy and achieving desired clinical outcomes.

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Clinical Pharmacokinetics of Losartan

Losartan is a rapidly absorbed oral angiotensin-receptor antagonist with a favorable drug-drug interaction profile, reducing blood pressure effectively and offering end-organ protection without significant adverse effects.

Highly Cited

2005·

215citations

·D. Sica et al.

The clinical pharmacology of losartan in Japanese subjects and patients.

Losartan's long-lasting blocking effect on angiotensin II action is due to the plasma levels of its active metabolite, E-3174, rather than its main component, losartan.

RCT

1996·

42citations

·M. Nakashima et al.

Losartan: a selective angiotensin II type 1 (AT1) receptor antagonist for the treatment of heart failure.

Losartan is a selective angiotensin II type 1 receptor antagonist with excellent tolerability and potential for improved survival in heart failure patients compared to captopril.

1998·

28citations

·K. Dickstein et al.

Randomized two way crossover open label study to compare the bioequivalence of LOSARDIL 100 TM (Drug International Ltd, Bangladesh) and COZAAR TM (Merck Sharp & Dhome Ltd, UK) in Bangladeshi normal male volunteers

LOSARDIL 100TM and COZAAR TM are bioequivalent in terms of absorption in healthy male Bangladeshi volunteers.

RCT

2023·

0citations

·Uttam Kumar Sarker et al.

Pharmacokinetics and biochemical efficacy after single and multiple oral administration of losartan, an orally active nonpeptide angiotensin II receptor antagonist, in humans.

Losartan is a potent orally active angiotensin II antagonist with a relatively long duration of action, without significant adverse reactions observed in healthy male volunteers.

Non-RCTHighly Cited

1993·

153citations

·M. Ohtawa et al.

Pharmacokinetics of Intravenous and Oral Losartan in Patients with Heart Failure

Losartan's pharmacokinetics in patients with heart failure are similar to those in healthy subjects, with no significant accumulation of the drug or its active metabolite.

Observational Study

1998·

21citations

·M. Lo et al.

Phenotypic and genotypic investigations of a healthy volunteer deficient in the conversion of losartan to its active metabolite E‐3174

A rare deficit in drug metabolism was observed in a healthy volunteer, suggesting a rare deficit in drug metabolism and potentially impacting the effectiveness of losartan.

Observational StudyHighly Cited

1999·

75citations

·J. McCrea et al.

Preparation and evaluation of buccal patches of losartan potassium using hydrophilic polymers

Losartan potassium buccal films prepared using hydrophilic polymers show sustained release and slower permeation through goat cheek mucosa, improving oral bioavailability.

In Vitro Study

2016·

0citations

·R. Rajesh

Pharmacokinetics of losartan, an angiotensin II receptor antagonist, and its active metabolite EXP3174 in humans

Losartan and its metabolite EXP3174 show similar pharmacokinetics in humans, with EXP3174 having a longer half-life and lower oral bioavailability.

Non-RCTHighly Cited

1995·

269citations

·M. Lo et al.

Phenobarbital minimally alters plasma concentrations of losartan and its active metabolite E‐3174

Phenobarbital minimally alters plasma concentrations of losartan and its active metabolite E-3174, but does not significantly affect the half-life values of these drugs.

RCT

1996·

34citations

·M. R. Goldberg et al.

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