Vriligy 60 mg contains dapoxetine, a medication primarily used to treat premature ejaculation in men. Understanding how Vriligy is metabolized in the body can provide insights into its effectiveness and potential interactions with other substances. Here’s a detailed look at the metabolism of Vriligy 60 mg:

1. Absorption

• Rapid Absorption: After oral administration, dapoxetine is quickly absorbed into the bloodstream, typically reaching peak plasma concentrations within 1 to 2 hours. This rapid absorption is beneficial for its intended use, as it allows for timely administration before sexual activity.

2. Distribution

• Volume of Distribution: Vriligy 60 mg has a moderate volume of distribution, indicating that it is distributed throughout the body tissues. It is also highly protein-bound, primarily to albumin and alpha-1 acid glycoprotein, which influences its bioavailability and effectiveness.

3. Metabolism

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  Liver Metabolism: Dapoxetine is extensively metabolized in the liver, primarily by the cytochrome P450 enzyme system, specifically CYP2D6. Other enzymes, such as CYP3A4 and CYP2C19, also play a role in its metabolism. This metabolic pathway results in the formation of various metabolites, some of which may have pharmacological activity.

  
  


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  First-Pass Metabolism: Due to significant first-pass metabolism, the bioavailability of dapoxetine is relatively low, ranging between 40% to 80%. This means that a portion of the drug is metabolized before it enters systemic circulation, which can affect its overall efficacy.

  
  

4. Excretion

• Renal Excretion: The metabolites of dapoxetine are primarily excreted through the kidneys. Approximately 60% of an administered dose is eliminated via urine, with the rest eliminated through feces. The half-life of dapoxetine is about 20 hours, which can vary based on individual metabolic differences.

5. Impact of Liver and Kidney Function

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  Liver Impairment: Individuals with liver dysfunction may experience altered metabolism and increased plasma concentrations of dapoxetine, necessitating caution and possible dosage adjustments.

  
  


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  Kidney Function: Since dapoxetine and its metabolites are excreted through the kidneys, impaired renal function may also affect the drug's elimination, increasing the risk of side effects.

  
  

6. Drug Interactions

• CYP450 Inhibitors and Inducers: Medications that inhibit or induce the CYP450 enzymes can affect the metabolism of dapoxetine. For instance, co-administration with CYP2D6 inhibitors can lead to increased levels of dapoxetine, enhancing the risk of side effects. Conversely, inducers may decrease its effectiveness.