Diclofenac: Potent Pain Relief and Anti-Inflammatory Action
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Diclofenac is a widely prescribed nonsteroidal anti-inflammatory drug (NSAID) renowned for its efficacy in managing pain and reducing inflammation. It functions by inhibiting cyclooxygenase (COX) enzymes, thereby decreasing the production of prostaglandins, which are mediators of pain, fever, and inflammatory processes. Available in various formulations including oral tablets, topical gels, and injectable solutions, diclofenac is a cornerstone in the treatment of acute and chronic musculoskeletal conditions, postoperative pain, and inflammatory disorders such as rheumatoid arthritis. Its well-established pharmacokinetic profile and rapid onset of action make it a preferred choice among clinicians for providing symptomatic relief and improving functional outcomes in appropriately selected patients.
Features
- Active ingredient: Diclofenac sodium or diclofenac potassium
- Drug class: Nonsteroidal anti-inflammatory drug (NSAID)
- Available formulations: Oral tablets, delayed-release tablets, topical gel, solution for injection, suppositories
- Mechanism of action: Reversible inhibition of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes
- Half-life: Approximately 2 hours (short-acting NSAID)
- Bioavailability: ~50-60% (oral); variable for topical formulations
- Metabolism: Hepatic, primarily via CYP2C9
- Excretion: Urinary (65%) and biliary (35%)
Benefits
- Provides rapid and effective relief from moderate to severe pain
- Reduces inflammation and swelling in musculoskeletal and joint disorders
- Improves mobility and functional capacity in arthritis patients
- Offers multiple administration routes for tailored therapeutic approaches
- Demonstrates well-established efficacy in diverse pain syndromes
- Cost-effective compared to many newer analgesic alternatives
Common use
Diclofenac is commonly prescribed for the management of various pain and inflammatory conditions. It is particularly effective in treating osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis, where it helps reduce joint pain, stiffness, and swelling. The medication is frequently used for acute musculoskeletal injuries such as sprains, strains, and tendinitis. Additionally, diclofenac finds application in managing postoperative pain, dental pain, and primary dysmenorrhea. Topical formulations are specifically indicated for localized pain relief in osteoarthritis of superficial joints, while injectable forms are utilized in hospital settings for rapid pain control. The selection of formulation depends on the condition being treated, severity of symptoms, and patient-specific factors.
Dosage and direction
Dosage varies significantly based on formulation and indication. For oral tablets (immediate-release), the typical adult dosage is 50mg three times daily or 75mg twice daily. Delayed-release tablets are usually prescribed as 75mg once or twice daily, or 100mg once daily. The maximum recommended daily dose is 150mg for all oral formulations. Topical gel (1% or 3%) should be applied four times daily to the affected area, with total daily dose not exceeding 32g for 1% gel or 16g for 3% gel. Injectable solution is typically administered as a 75mg deep intramuscular injection once or twice daily. For all formulations, diclofenac should be taken with food or milk to minimize gastrointestinal irritation. Treatment should be initiated at the lowest effective dose for the shortest duration necessary to control symptoms.
Precautions
Patients should be carefully evaluated before initiating diclofenac therapy. Cardiovascular risk assessment is crucial, as NSAIDs may increase the risk of serious thrombotic events, myocardial infarction, and stroke. Gastrointestinal monitoring is essential due to the risk of bleeding, ulceration, and perforation. Renal function should be assessed, particularly in elderly patients, those with dehydration, or those taking concomitant nephrotoxic medications. Hepatic function requires monitoring as transaminase elevations may occur. Patients with asthma may experience exacerbations due to potential cross-reactivity with other NSAIDs. Caution is advised in patients with hypertension, heart failure, or edema. Regular follow-up and the lowest effective dose for the shortest possible duration are recommended to minimize risks.
Contraindications
Diclofenac is contraindicated in patients with known hypersensitivity to diclofenac, aspirin, or other NSAIDs. It should not be used in patients who have experienced asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs. The drug is contraindicated in the setting of coronary artery bypass graft (CABG) surgery. Additional contraindications include active gastrointestinal bleeding or ulceration, severe heart failure, severe hepatic impairment (Child-Pugh Class C), and advanced renal disease. Third trimester pregnancy represents an absolute contraindication due to risk of premature closure of the ductus arteriosus. Concomitant use with other NSAIDs, including selective COX-2 inhibitors, is contraindicated.
Possible side effect
The most common adverse reactions involve the gastrointestinal system, including dyspepsia (10-15%), nausea (5-10%), abdominal pain (5-8%), and diarrhea (3-5%). Serious but less frequent side effects include gastrointestinal bleeding (0.5-1%), ulceration, and perforation. Cardiovascular side effects may include hypertension exacerbation, fluid retention, and increased risk of thrombotic events. Renal effects can manifest as reduced renal function, interstitial nephritis, and nephrotic syndrome. Hepatic enzyme elevations occur in 5-15% of patients, with severe hepatotoxicity being rare (<0.1%). Dermatological reactions include rash (2-3%), photosensitivity, and rarely, serious skin reactions such as Stevens-Johnson syndrome. Central nervous system effects may include headache, dizziness, and rarely, aseptic meningitis.
Drug interaction
Diclofenac exhibits numerous clinically significant drug interactions. Concurrent use with other NSAIDs or aspirin increases gastrointestinal toxicity without therapeutic benefit. Anticoagulants like warfarin and novel oral anticoagulants may have enhanced effects, increasing bleeding risk. ACE inhibitors, ARBs, and diuretics may have reduced antihypertensive effects and increased nephrotoxicity risk. Lithium levels may increase due to reduced renal clearance. Methotrexate toxicity may be enhanced due to decreased renal clearance. Cyclosporine and tacrolimus may experience increased nephrotoxicity. Selective serotonin reuptake inhibitors may increase bleeding risk. Corticosteroids potentiate gastrointestinal ulcer risk. Phenytoin levels may be affected through protein displacement interactions.
Missed dose
If a dose is missed, it should be taken as soon as remembered, unless it is nearly time for the next scheduled dose. In that case, the missed dose should be skipped and the regular dosing schedule resumed. Patients should not double the dose to make up for a missed one. For medications taken multiple times daily, if rememberance occurs within 2-3 hours of the missed dose, it can be taken; otherwise, wait for the next scheduled dose. The clinical significance of a single missed dose is generally minimal for chronic conditions, but consistency in dosing helps maintain stable therapeutic effects. Patients should maintain a dosing diary or use reminder systems if missed doses occur frequently.
Overdose
Diclofenac overdose may manifest as headache, nausea, vomiting, epigastric pain, gastrointestinal bleeding, drowsiness, dizziness, tinnitus, apnea, metabolic acidosis, coma, convulsions, or acute renal failure. In massive overdoses, cardiovascular collapse, respiratory depression, and hepatic necrosis may occur. Management is primarily supportive and symptomatic. Gastric lavage may be considered if presentation occurs within 1 hour of ingestion. Activated charcoal can be effective if administered promptly. Hemodialysis is not effective due to high protein binding. Forced diuresis, alkalinization of urine, or hemoperfusion are generally not beneficial. Specific treatments may include intravenous fluids for hypotension, blood transfusion for significant bleeding, and anticonvulsants for seizures. Liver function tests and renal function should be monitored closely.
Storage
Diclofenac should be stored at controlled room temperature (20-25°C or 68-77°F), protected from light and moisture. Oral tablets should be kept in their original container with the lid tightly closed. Topical gels should not be exposed to high temperatures or freezing conditions. Injectable solutions should be stored according to manufacturer specifications, typically refrigerated until use. All formulations should be kept out of reach of children and pets. Do not transfer medications to unlabeled containers. Discard any medication that has passed its expiration date or shows signs of deterioration (discoloration, unusual odor, or changed consistency). Proper disposal through medication take-back programs is recommended to prevent environmental contamination and accidental ingestion.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. The content is not intended to be a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read herein. Drug information changes frequently, and the manufacturer’s prescribing information should be consulted for complete details. Individual patient responses to medications vary, and only a healthcare professional can determine appropriate therapy based on specific clinical circumstances.
Reviews
Clinical studies and meta-analyses consistently demonstrate diclofenac’s efficacy in pain management. A comprehensive Cochrane review of 176 studies found diclofenac 150mg daily significantly superior to placebo for osteoarthritis pain relief. Rheumatology guidelines frequently recommend diclofenac as first-line therapy for inflammatory arthritis. Patient-reported outcomes show significant improvements in pain scores and quality of life measures. However, real-world evidence highlights the importance of careful patient selection and monitoring due to potential adverse effects. Comparative effectiveness research positions diclofenac as among the most effective NSAIDs for pain relief, though with a need for balanced risk-benefit assessment. Long-term observational studies confirm its position as a mainstay in analgesic therapy when used appropriately with adequate safety monitoring.