Intro to Pharmacology

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Celecoxib

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Intro to Pharmacology

Definition

Celecoxib is a nonsteroidal anti-inflammatory drug (NSAID) that selectively inhibits the enzyme cyclooxygenase-2 (COX-2), which plays a key role in inflammation and pain signaling. By targeting COX-2, celecoxib provides effective relief from pain and inflammation associated with conditions such as arthritis while minimizing gastrointestinal side effects commonly seen with non-selective NSAIDs.

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5 Must Know Facts For Your Next Test

  1. Celecoxib is commonly prescribed for osteoarthritis, rheumatoid arthritis, acute pain, and dysmenorrhea.
  2. Unlike traditional NSAIDs, celecoxib has a lower risk of causing gastrointestinal bleeding or ulcers due to its selective inhibition of COX-2.
  3. It is metabolized in the liver primarily by cytochrome P450 enzymes, which can interact with other medications.
  4. Celecoxib may be associated with an increased risk of cardiovascular events, so it's important to evaluate a patient's heart health before prescribing it.
  5. The drug is typically taken orally and can be used in combination with other medications for enhanced pain management.

Review Questions

  • How does the selective inhibition of COX-2 by celecoxib compare to non-selective NSAIDs in terms of side effects?
    • Celecoxib selectively inhibits COX-2, which helps provide pain relief with a reduced risk of gastrointestinal side effects like ulcers and bleeding that are often seen with non-selective NSAIDs. Non-selective NSAIDs inhibit both COX-1 and COX-2 enzymes, leading to greater gastrointestinal irritation because COX-1 is involved in protecting the stomach lining. Thus, celecoxib offers a more targeted approach to managing inflammation and pain while being safer for long-term use in patients prone to digestive issues.
  • Discuss the implications of celecoxib's metabolism via cytochrome P450 enzymes on drug interactions.
    • Celecoxib is metabolized primarily by cytochrome P450 enzymes, specifically CYP2C9. This means that it can interact with other drugs that are either substrates or inhibitors of these enzymes. For example, if a patient is taking medications that inhibit CYP2C9, this can lead to elevated levels of celecoxib in the bloodstream, increasing the risk of adverse effects. Therefore, healthcare providers must carefully review a patient's medication history to prevent harmful drug interactions when prescribing celecoxib.
  • Evaluate the benefits and risks associated with the long-term use of celecoxib for chronic inflammatory conditions.
    • Long-term use of celecoxib for chronic inflammatory conditions such as arthritis provides significant benefits in terms of effective pain relief and improved quality of life. However, there are notable risks including potential cardiovascular events such as heart attacks or strokes, especially in patients with pre-existing heart conditions. Furthermore, while celecoxib has a lower risk of gastrointestinal side effects compared to traditional NSAIDs, it still poses some risk for renal impairment and hypertension. Patients should be closely monitored to balance the therapeutic benefits against these potential risks.

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