DESCRIPTION
A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.
CATEGORIES
Anti-Inflammatory Agents, Non-Steroidal,Cyclooxygenase Inhibitors.
CHEMICAL FORMULA
C14H11Cl2NO2
COMPOSITION
Diclofenac sodium 50 mg
INDICATION
For the acute and chronic treatment of signs and symptoms of osteoarthritis and rheumatoid arthritis.
PHARMACODYNAMICS
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
MECHANISM
The antiinflammatory effects of diclofenac are believed to be due to inhibition of both leukocyte migration and the enzyme cylooxygenase (COX-1 and COX-2), leading to the peripheral inhibition of prostaglandin synthesis. As prostaglandins sensitize pain receptors, inhibition of their synthesis is responsible for the analgesic effects of diclofenac. Antipyretic effects may be due to action on the hypothalamus, resulting in peripheral dilation, increased cutaneous blood flow, and subsequent heat dissipation.
ABSORPTION
Completely absorbed from the gastrointestinal tract.
VOLUME DISTRIBUTION
1.3 L/kg
METABOLISM
Hepatic
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.
HALF LIFE
2 hours
TOXICITY
Symptoms of overdose include loss of consciousness, increased intracranial pressure, and aspiration pneumonitis. LD50=390mg/kg (orally in mice)
FOOD INTERACTIONS
avoid alcohol
SIDE EFFECTS
Headache. Belly pain. Upset stomach or throwing up. Many small meals, good mouth care, sucking hard, sugar-free candy, or chewing sugar-free gum may help. Hard stools (constipation). Drinking more liquids, working out, or adding fiber to your diet may help. Talk with your doctor about a stool softener or laxative. Loose stools (diarrhea). Harm to the liver may rarely happen.