Curafen

White to off white bi-convex film-coated tablet engraved with "ACME" on one side and other side being plain.
Each Film-Coated Tablet contains: Diclofenac Sodium BP 100 mg.

Pharmacology: Pharmacodynamics: Diclofenac sodium is a non-steroidal agent with marked analgesic/anti-inflammatory properties. It is an inhibitor of prostaglandin synthetase, (cyclo-oxygenase). Diclofenac sodium in vitro does not suppress proteoglycan biosynthesis in cartilage at concentrations equivalent to the concentrations reached in human beings.
Pharmacokinetics: Absorption: Diclofenac is 100% absorbed after oral administration compared to IV administration as measured by urine recovery. However, due to first-pass metabolism, only about 50% of the absorbed dose is systemically available. Food has no significant effect on the extent of diclofenac absorption. There is usually a delay in the onset of absorption of 1 to 4.5 hours and a reduction in peak plasma levels of <20%.
Distribution: The apparent volume of distribution of Diclofenac sodium is 1.4 L/kg.
Diclofenac is more than 99% bound to human serum proteins, primarily to albumin. Serum protein binding is constant over the concentration range (0.15-105 μg/mL) achieved with recommended doses.
Diclofenac diffuses into and out of the synovial fluid. Diffusion into the joint occurs when plasma levels are higher than those in the synovial fluid, after which the process reverses and synovial fluid levels are higher than plasma levels. It is not known whether diffusion into the joint plays a role in the effectiveness of Diclofenac.
Metabolism: Five Diclofenac metabolites have been identified in human plasma and urine. The metabolites include 4'-hydroxy-, 5-hydroxy-, 3'-hydroxy-, 4',5-dihydroxy- and 3'-hydroxy-4-methoxy-Diclofenac. The major Diclofenac metabolite, 4'-hydroxy-Diclofenac, has very weak pharmacologic activity. The formation of 4'-hydroxy-Diclofenac is primarily mediated by CPY2C9. Both Diclofenac and its oxidative metabolites undergo glucuronidation or sulfation followed by biliary excretion. Acylglucuronidation mediated by UGT2B7 and oxidation mediated by CPY2C8 may also play a role in Diclofenac metabolism. CYP3A4 is responsible for the formation of minor metabolites, 5-hydroxy- and 3'-hydroxy-Diclofenac. In patients with renal dysfunction, peak concentrations of metabolites 4'-hydroxy- and 5-hydroxy-Diclofenac were approximately 50% and 4% of the parent compound after single oral dosing compared to 27% and 1% in normal healthy subjects.
Excretion: Diclofenac is eliminated through metabolism and subsequent urinary and biliary excretion of the glucuronide and the sulfate conjugates of the metabolites. Little or no free unchanged Diclofenac is excreted in the urine. Approximately 65% of the dose is excreted in the urine and approximately 35% in the bile as conjugates of unchanged Diclofenac plus metabolites. Because renal elimination is not a significant pathway of elimination for unchanged Diclofenac, dosing adjustment in patients with mild to moderate renal dysfunction is not necessary. The terminal half-life of unchanged Diclofenac is approximately 2 hours.

For the relief of painful and inflammatory conditions due to rheumatoid arthritis, tendinitis, osteoarthritis, bursitis, and other articular or periarthritic disorders.

Adult: One tablet once a day after meals. Diclofenac sodium SR should not be fragmented, nor should they be chewed. If necessary, the daily dose can be increased to 150 mg by taking in addition, either of 2 Diclofenac sodium 25 mg tablet/capsule or 1 Diclofenac sodium 50 mg tablet/capsule, or suppositories. To be dispensed on physician's prescription.

There is no typical clinical picture resulting from Diclofenac overdosage. Overdosage can cause symptoms such as headache, nausea, vomiting, epigastric pain, gastrointestinal hemorrhage, diarrhea, dizziness, disorientation, excitation, coma, drowsiness, tinnitus, fainting or convulsions. In the case of significant poisoning acute renal failure and liver damage are possible. Management of acute poisoning with NSAIDs, including Diclofenac, essentially consists of supportive measures and symptomatic treatment. Supportive measures and symptomatic treatment should be given for complications such as hypotension, renal failure, convulsions, gastrointestinal disorder, and respiratory depression. Special measures such as forced diuresis, dialysis or hemo-perfusion are probably of no help in eliminating NSAIDs, including Diclofenac, due to the high protein binding and extensive metabolism. Activated charcoal may be considered after ingestion of a potentially toxic overdose, and gastric decontamination (e.g. vomiting, gastric lavage) after ingestion of a potentially life threatening overdose.

Diclofenac sodium is contraindicated in peptic ulcer, previous sensitivity to Diclofenac sodium and in asthmatic patients in whom attacks of asthma, urticaria or acute rhinitis are precipitated by Aspirin or other nonsteroidal anti-inflammatory agents with prostaglandin synthesis inhibiting activity.

Precaution should be taken in patients with symptoms/history of gastro-intestinal disease, impaired hepatic, cardiac or renal function, pregnancy, porphyria and patients who are taking diuretics, anticoagulant, or anti-diabetics. During prolonged treatment, periodical monitoring of liver function should be carried out and blood counts are recommended. Possibility of hypersensitivity reactions to sodium disulphite particularly in patients with asthma.

Occasional gastrointestinal disorders, headache, dizziness or vertigo, rash, elevation of SGOT/SGPT, rare peptic ulcer, gastro-intestinal bleeding, hepatitis, hypersensitivity reactions. In isolated cases, disturbances of sensation, erythema multiforme, purpura, abnormalities of renal function, blood dyscrasias may occur.

Special Precautions for Disposal and Other Handling: Any unused medicine should be disposed properly. Consult the pharmacist or local waste management center for more details about how to safely discard expired or unused medicines.

Store at temperatures not exceeding 30°C.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

M01AB05 - diclofenac ; Belongs to the class of acetic acid derivatives and related substances of non-steroidal antiinflammatory and antirheumatic products.

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