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Diclofenac potassium is a new nonsteroidal anti-inflammatory drug with significant anti-inflammatory and analgesic effects. Its mechanism of action is mainly to inhibit the synthesis of prostaglandins. After joint and muscle sprain, tooth extraction and operation, sterile inflammation, tissue edema and pain can be caused. With the generation of inflammation, prostaglandins synthesized and released in the injured area will increase. Diclofenac potassium can reduce the prostaglandins synthesized and released locally after injury, and play an anti-inflammatory and analgesic role.
| Aspect | Details |
|---|---|
| Mechanism of Action | Diclofenac potassium is a nonsteroidal anti-inflammatory drug (NSAID) that inhibits the activity of cyclooxygenase (COX-1 and COX-2) enzymes, reducing the synthesis of prostaglandins. It also modulates cytokine activity and affects ion channels related to pain perception. |
| Pharmacokinetics | – Absorption: Completely absorbed orally, but first-pass metabolism results in a systemic bioavailability of about 50%.<br>- Distribution: Widely distributed in tissues with a plasma protein binding rate of over 99%.<br>- Metabolism: Primarily metabolized to the 4′-hydroxy metabolite by CYP2C9, with additional pathways involving acetylation by UGT2B7 and oxidation by CYP2C8.<br>- Excretion: Mainly excreted via bile, with a small amount excreted in urine as unchanged drug. |
| Indications | Used for the relief of mild to moderate pain and the treatment of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and dysmenorrhea. |
| Drug Interactions | – Co-administration with antacids, H₂-receptor antagonists, or proton pump inhibitors can reduce gastrointestinal adverse effects.<br>- May increase toxicity when used with lithium, digoxin, methotrexate, or anticoagulants. |
| Adverse Effects | Common side effects include gastrointestinal discomfort (e.g., nausea, vomiting, gastric ulcers), headache, and dizziness. Long-term use may increase the risk of cardiovascular events. |
| Discontinuation | After discontinuation, patients may need to switch to alternative analgesics, such as other NSAIDs, acetaminophen, or opioids. |
| Storage Conditions | Store at room temperature, avoiding moisture and high heat. |
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