Metabolism of losartan

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Description of losartan

Losartan is a medication used to treat high blood pressure (hypertension) and to help protect the kidneys from damage due to diabetes. It belongs to a class of drugs known as angiotensin II receptor blockers (ARBs). Losartan works by blocking the action of angiotensin II, a hormone that constricts blood vessels and causes blood pressure to rise. By blocking angiotensin II, losartan helps to relax and widen blood vessels, allowing blood to flow more easily and lowering blood pressure.

Losartan is usually taken by mouth and may be prescribed alone or in combination with other medications to achieve the desired blood pressure control. It is important to take losartan regularly as directed by your healthcare provider to get the full benefit of the medication.

Metabolism in the body

Losartan is metabolized in the liver by the cytochrome P450 enzyme system, primarily by the CYP2C9 and CYP3A4 isoenzymes. The main metabolite produced is the active metabolite, E-3174, which also possesses antagonistic activity on the angiotensin II receptor. This active metabolite contributes significantly to the overall pharmacological effects of losartan.

After oral administration, losartan undergoes extensive first-pass metabolism, leading to a low systemic bioavailability of about 33%. The metabolites of losartan and E-3174 are eliminated primarily via the feces (about 35% of the dose) and the urine (about 60% of the dose).

  • Metabolism primarily occurs in the liver
  • Main metabolite is the active metabolite E-3174
  • Active metabolite contributes to the pharmacological effects
  • Low systemic bioavailability due to first-pass metabolism
  • Elimination via feces (35%) and urine (60%)
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Metabolism in the body

Losartan is metabolized in the liver to its active metabolite, E-3174, primarily by CYP2C9. This metabolite has a greater affinity for the AT1 receptor than losartan itself, leading to enhanced pharmacological activity. The metabolism of losartan is subject to genetic variability, with certain individuals metabolizing the drug more rapidly or slowly.

Key Points:

  • Losartan is metabolized in the liver by CYP2C9.
  • The active metabolite, E-3174, has a higher affinity for the AT1 receptor.
  • Genetic factors can influence the rate of metabolism of losartan.
Metabolism Details
Enzyme CYP2C9 in the liver
Active Metabolite E-3174
Genetic Variability May impact metabolism rate

Pharmacokinetics of losartan

Pharmacokinetics of losartan

Losartan is absorbed quickly and undergoes extensive first-pass metabolism in the liver, converting it to its active metabolite, E-3174. The bioavailability of the active metabolite is about 33%, and peak plasma concentrations are achieved in about 1 hour.

Losartan and its metabolites are primarily excreted in the urine and feces, with approximately 35% of the dose eliminated in the urine and 58% in the feces. The elimination half-life of losartan is about 2 hours, while the active metabolite has a longer half-life of 6-9 hours.

Impact on health

Impact on health

Losartan has a positive impact on health by effectively lowering blood pressure and helping to manage hypertension. As an angiotensin II receptor blocker, it works by blocking the effects of angiotensin II, a hormone that constricts blood vessels and raises blood pressure. By reducing the effects of angiotensin II, losartan helps to relax blood vessels, lower blood pressure, and improve blood flow.

Moreover, losartan has been shown to have additional benefits beyond just lowering blood pressure. Studies suggest that losartan may also have protective effects on the heart and kidneys, reducing the risk of cardiovascular events and kidney damage in patients with hypertension. This makes losartan a valuable medication for patients looking to not only control their blood pressure but also reduce the risk of complications associated with hypertension.

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