How long does losartan last
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Duration of Losartan's Effects: Pharmacokinetics and Efficacy
Pharmacokinetics of Losartan and Its Metabolite E-3174
Losartan, an angiotensin II receptor antagonist, is rapidly absorbed after oral administration, reaching peak plasma concentrations within 1 to 2 hours 2. The drug undergoes extensive first-pass metabolism, with approximately 14% of the dose converted to its active metabolite, E-3174, which is significantly more potent than losartan itself 2. The terminal half-life of losartan ranges from 1.5 to 2.5 hours, while E-3174 has a longer half-life of 6 to 9 hours, contributing to the drug's prolonged effects 12.
Duration of Antihypertensive Effects
The antihypertensive effects of losartan are primarily due to its active metabolite, E-3174, which maintains higher plasma concentrations and a longer half-life compared to losartan 12. Studies have shown that the pharmacokinetics of losartan and E-3174 remain consistent with repeated dosing, indicating stable drug levels over time 12.
Extended-Release Formulations
To enhance the duration of losartan's antihypertensive effects, extended-release formulations have been developed. For instance, Losartan Cronos, a bilayer tablet containing both immediate and extended-release components, has been shown to provide effective blood pressure control over a 24-hour period 3. This formulation ensures a sustained release of the drug, maintaining therapeutic levels throughout the day and improving patient adherence 3.
Clinical Efficacy and Safety
Clinical trials have demonstrated that losartan, administered once daily, effectively reduces blood pressure and provides end-organ protection in various conditions such as diabetic nephropathy, heart failure, and post-myocardial infarction 256. The drug is well-tolerated, with a safety profile comparable to placebo, and does not require dosage adjustments for age, sex, or mild hepatic impairment 25.
Conclusion
Losartan's antihypertensive effects are primarily driven by its active metabolite, E-3174, which has a longer half-life and higher potency. While the immediate-release form of losartan may require twice-daily dosing for some patients, extended-release formulations like Losartan Cronos can provide effective 24-hour blood pressure control. Overall, losartan is a safe and effective option for managing hypertension and related conditions.
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Most relevant research papers on this topic
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.
RCTClinical 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[Abpm and duration of the antihypertensive effect: a study with a new formulation of sustained release losartan (CRONOS)].
Losartan Cronos effectively reduces blood pressure and pulse pressure without significant heart rate changes, and its effect lasts for 24 hours, suggesting daily monodose administration.
Biochemical effects of losartan, a nonpeptide angiotensin II receptor antagonist, on the renin-angiotensin-aldosterone system in hypertensive patients.
Long-term blockade of the feedback Ang II receptor in hypertensive patients leads to modest increases in plasma renin activity and Ang II, but does not affect the antihypertensive response to the antagonist.
RCTHighly CitedClinical safety and tolerability of losartan.
Losartan is a safe and tolerable treatment for hypertension, even in patients with concomitant illnesses, and can be considered as a first-line therapy or alternative therapy for those experiencing side effects with other agents.
RCT
Large Human TrialLosartan in heart failure. Hemodynamic effects and tolerability. Losartan Hemodynamic Study Group.
Oral losartan improves hemodynamic effects in patients with symptomatic heart failure, with the greatest effect seen at 50 mg dose.
RCTHighly CitedLOSARTAN/AMLODIPINE IN ARTERIAL STIFFNESS SHOWS DOMINANT EFFICACY IN REDUCING 24 HOURS BRACHIAL AND CENTRAL BP COMPARED WITH LOSARTAN/HYDROCHLOROTHIAZID OR IN NORMAL ARTERY
Losartan/amlodipine combination therapy is more effective in reducing 24 hours brachial and central blood pressure in patients with advanced arterial stiffness compared to losartan/hydrochlorothiazide or normal arterial patients.
RCTLosartan's Protective Effects in Stroke‐Prone Spontaneously Hypertensive Rats Persist Durably After Treatment Withdrawal
Long-term oral losartan treatment effectively protects against stroke and mortality in stroke-prone spontaneously hypertensive rats, with lasting effects even after treatment discontinuation.
Non-RCT
Animal StudyEffects of losartan on renal and cardiovascular outcomes in patients with type 2 diabetes and nephropathy.
Losartan significantly reduces the risk of kidney damage and end-stage renal disease in patients with type 2 diabetes and nephropathy, while maintaining overall cardiovascular health.
RCTLarge Human TrialHighly CitedEffect of Long-Term Losartan Administration on Renal Haemodynamics and Function in Hypertensive Patients
Long-term losartan administration effectively lowers blood pressure and maintains renal function in mild to moderate hypertensive patients, but these effects diminish after 1 year of treatment.
RCT