Clofenac20 gm

Clofenac is a non-steroidal anti-inflammatory drug (NSAID) used for the relief of pain and inflammation in a range of musculoskeletal and gynecological conditions.

Established / Approved Uses

• Relief of signs and symptoms of osteoarthritis
• Relief of signs and symptoms of rheumatoid arthritis
• Relief of signs and symptoms of ankylosing spondylitis

Guideline-Supported / Widely Accepted Uses

• Acute musculoskeletal pain, including sprains, strains, and post-traumatic pain and swelling
• Primary dysmenorrhea (painful menstrual cramps)
• Post-operative pain and inflammation (short-term use)

Clofenac is not an antibiotic and has no role in treating infections.

Each formulation of Diclofenac Sodium contains diclofenac sodium as the active pharmaceutical ingredient. It is available in several dosage forms and strengths, including immediate-release and sustained/delayed-release tablets, injection ampoules, suppositories, topical gel, and ophthalmic drops, depending on local market availability.

Common strengths include 25 mg, 50 mg, 75 mg, and 100 mg (sustained-release) oral tablets, and 75 mg/3 mL injectable solution.

Clofenac is a phenylacetic acid derivative belonging to the non-steroidal anti-inflammatory drug (NSAID) class. It is a non-selective inhibitor of cyclooxygenase (COX-1 and COX-2) enzymes, which are responsible for the synthesis of prostaglandins involved in pain, inflammation, and fever.

It is widely used for its analgesic, anti-inflammatory, and antipyretic properties in the management of chronic inflammatory joint disease and acute pain conditions. Clofenac is available in oral, injectable, rectal, ophthalmic, and topical formulations, allowing flexible use depending on the clinical situation.

Clofenac belongs to the therapeutic class of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), specifically the phenylacetic acid derivative group. It is a non-selective cyclooxygenase (COX-1 and COX-2) inhibitor, distinguishing it from selective COX-2 inhibitors (e.g., celecoxib).

Diclofenac Sodium works by non-selectively inhibiting the cyclooxygenase (COX-1 and COX-2) enzymes, which blocks the conversion of arachidonic acid to prostaglandins and thromboxanes. This reduces the mediators responsible for pain, inflammation, and fever at the site of tissue injury.

After oral administration, Diclofenac Sodium is well absorbed from the gastrointestinal tract, is highly protein-bound (>99%), undergoes extensive hepatic metabolism (primarily via CYP2C9), and is eliminated mainly via the kidneys and bile. Peak plasma concentrations are typically reached within 1-2 hours for immediate-release formulations.

Clofenac tablets should be swallowed whole with a full glass of water, preferably with food or milk to minimize gastrointestinal upset. Enteric-coated and sustained-release tablets must not be crushed, split, or chewed. Injectable Clofenac is administered by deep intramuscular injection into the gluteal muscle by a healthcare professional, generally not for more than 1-2 days. Topical gel is applied to intact, clean, dry skin over the affected area only.

Clofenac has several clinically significant drug interactions:

• Anticoagulants (e.g., warfarin) and antiplatelet agents: Increased risk of serious bleeding; monitor closely if co-administered.
• Aspirin and other NSAIDs: Increased risk of GI bleeding and ulceration without added therapeutic benefit; concurrent use should generally be avoided.
• ACE inhibitors, ARBs, and diuretics: Clofenac may reduce their antihypertensive and natriuretic effects and increase the risk of renal impairment, especially in volume-depleted patients.
• Lithium: Clofenac can reduce lithium clearance, leading to elevated, potentially toxic lithium levels; monitor lithium levels.
• Methotrexate: Clofenac may reduce methotrexate clearance and increase its toxicity, especially at higher methotrexate doses.
• Digoxin: Clofenac may increase serum digoxin concentrations; monitor digoxin levels.
• Cyclosporine: Increased risk of nephrotoxicity.
• CYP2C9 inhibitors (e.g., voriconazole, fluconazole): May increase plasma concentrations of Clofenac.

Most adverse effects of Clofenac are mild and transient, but some can be serious. Common side effects include:

• Gastrointestinal: epigastric pain, dyspepsia, nausea, diarrhea, flatulence
• Headache and dizziness
• Elevated liver enzymes
• Fluid retention and edema
• Skin rash

Less common but serious effects include gastrointestinal ulceration/bleeding/perforation, cardiovascular thrombotic events (myocardial infarction, stroke), hepatotoxicity, renal impairment, hypertension, anaphylactic reactions, and severe skin reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis). See Precautions and Warnings for details.

Pregnancy: Clofenac should be avoided during pregnancy unless clearly necessary. Use in the first and second trimesters should occur only if the potential benefit justifies the potential risk to the fetus, and only after consulting a physician. Clofenac is contraindicated in the third trimester of pregnancy because NSAIDs can cause premature closure of the fetal ductus arteriosus and other fetal renal effects.

Lactation: Clofenac passes into breast milk in small amounts. Use during breastfeeding should occur only if clearly needed and under medical supervision, weighing the benefit to the mother against potential risk to the infant.

Clofenac carries important warnings that require caution:

• Cardiovascular risk: NSAIDs, including Clofenac, can increase the risk of serious cardiovascular thrombotic events such as myocardial infarction and stroke, which can be fatal. This risk may increase with duration of use and in patients with existing cardiovascular disease or risk factors. Clofenac should be avoided in patients with recent myocardial infarction unless benefits are judged to outweigh risks.
• Gastrointestinal risk: Serious GI adverse events, including bleeding, ulceration, and perforation of the stomach or intestines, can occur at any time, with or without warning symptoms, and are more common in elderly patients and those with prior peptic ulcer disease.
• Hepatotoxicity: Elevations of liver enzymes and, rarely, severe hepatic reactions (including liver failure) have been reported. Liver function should be monitored during prolonged therapy.
• Renal effects: Clofenac can cause renal impairment, particularly in patients with pre-existing renal disease, heart failure, liver dysfunction, volume depletion, or in the elderly. Adequate hydration should be maintained.
• Fluid retention and hypertension: Clofenac may cause new-onset or worsening of pre-existing hypertension and fluid retention/edema, and can blunt the effect of some antihypertensive medications.
• Clofenac should be used with caution in patients with a history of GI disease, bleeding disorders, asthma, or cardiovascular risk factors.

Symptoms of Clofenac overdose may include lethargy, drowsiness, nausea, vomiting, and epigastric pain, and in more severe cases gastrointestinal bleeding, hypertension, acute renal failure, respiratory depression, or coma. There is no specific antidote for Clofenac overdose.

In case of suspected overdose, seek immediate medical attention or contact emergency services/a poison control center. Treatment is supportive and symptomatic; a physician may consider measures such as activated charcoal if the patient presents soon after ingestion. Do not attempt home treatment for a suspected overdose.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Elderly: Elderly patients are at greater risk of serious GI, cardiovascular, and renal adverse effects with Clofenac. The lowest effective dose should be used for the shortest possible duration, with closer clinical monitoring.

Renal impairment: Use with caution and at reduced doses in mild-to-moderate renal impairment; avoid in severe renal impairment. Monitor renal function.

Hepatic impairment: Use with caution in mild-to-moderate hepatic impairment; avoid in severe hepatic impairment. Monitor liver function periodically during prolonged use.

Pediatric patients: See Pediatric Uses.

Pregnancy and lactation: See Pregnancy and Lactation.

Clofenac should be used for the shortest duration consistent with the individual treatment goal, due to dose- and duration-related cardiovascular and gastrointestinal risks. For acute pain or dysmenorrhea, short courses of a few days are typical. For chronic conditions such as osteoarthritis or rheumatoid arthritis, long-term use requires periodic clinical reassessment and monitoring of renal function, liver function, and blood pressure by a physician.

Non-Steroidal Anti-Inflammatory Drug (NSAID); Phenylacetic acid derivative; Non-selective COX-1/COX-2 inhibitor

Diclofenac Sodium exerts its therapeutic effect by non-selectively inhibiting the cyclooxygenase (COX-1 and COX-2) enzymes involved in the arachidonic acid pathway. This inhibition decreases the synthesis of prostaglandins and thromboxanes, mediators responsible for pain, inflammation, fever, and platelet aggregation, resulting in analgesic, anti-inflammatory, and antipyretic effects.

The safety and efficacy of oral Clofenac have not been formally established for general pediatric use in most markets. For juvenile idiopathic (rheumatoid) arthritis, weight-based dosing (approximately 1-3 mg/kg/day in divided doses) has been used under the supervision of a pediatric rheumatology specialist in some settings. Clofenac should not be used in children outside specialist guidance, and topical/rectal formulations are generally not recommended in young children.