Diclofenac Sodium Tablets

Mechanism

Diclofenac Sodium inhibits cyclooxygenase (COX-1 and COX-2) enzymes, reducing prostaglandin synthesis. This leads to decreased inflammation, pain relief, and fever reduction. It also reduces sensitization of nerve endings, providing analgesic effects. Diclofenac: Inhibits prostaglandin synthesis, reducing inflammation and pain.

Pharmacokinetics

• Absorption: Rapidly absorbed orally; peak plasma concentration in 1–2 hours.
• Distribution: Highly protein-bound (~99%); accumulates in synovial fluid.
• Metabolism: Extensively metabolized in the liver via CYP2C9.
• Excretion: 65% via urine, 35% via bile/feces.
• Half-life: 1–2 hours, but therapeutic effect persists longer due to tissue binding.

Side Effects

• Gastrointestinal: Nausea, vomiting, gastritis, peptic ulcers, GI bleeding.
• Cardiovascular: Hypertension, edema, increased risk of MI or stroke.
• Renal: Reduced renal perfusion, nephrotoxicity, fluid retention.
• Hepatic: Elevated liver enzymes, rare hepatotoxicity.
• Others: Headache, dizziness, rash, photosensitivity.

Contraindication

• Hypersensitivity to NSAIDs or muscle relaxants
• Severe hepatic impairment
• Pregnancy & lactation (use under medical supervision)

Interaction

• Anticoagulants (Warfarin, Heparin): Increased bleeding risk.
• Antihypertensives (ACE inhibitors, Diuretics): Reduced efficacy, increased nephrotoxicity.
• Other NSAIDs or Corticosteroids: Higher risk of GI bleeding.
• Methotrexate: Increased toxicity due to reduced clearance.
• Lithium: Elevated lithium levels due to reduced renal clearance.

Warning and Precautions

• Use lowest effective dose for shortest duration.
• Take after meals to reduce GI irritation.
• Monitor renal and hepatic function during prolonged therapy.
• Contraindicated in patients with peptic ulcer disease, severe heart failure, or hypersensitivity to NSAIDs.

Dosage

As directed by the Physician.