化合物信息

Drug Groups

approved

Description

A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt. [PubChem]

Indication

For the acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis.

Pharmacology

Diclofenac is an acetic acid nonsteroidal antiinflammatory drug (NSAID) with analgesic and antipyretic properties. Diclofenac is used to treat pain, dysmenorrhea, ocular inflammation, osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and actinic keratosis

Toxicity

Symptoms of overdose include loss of consciousness, increased intracranial pressure, and aspiration pneumonitis. LD₅₀=390mg/kg (orally in mice)

Affected Organisms

Biotransformation

Hepatic

Absorption

Completely absorbed from the gastrointestinal tract.

Half Life

2 hours

Protein Binding

More than 99%

Elimination

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.

Distribution

* 1.3 L/kg

Clearance

* oral cl=622 mL/min [healthy]
* renal cl <1 mL/min [healthy]

References

External Links