Arylacetic Acid Derivatives

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Chapter: Essential pharmacology : Nonsteroidal Anti-inflammatory Drugs And Antipyreticanalgesics

Diclofenac sodium : An analgesic antipyretic anti-inflammatory drug, similar in efficacy to naproxen. It inhibits PG synthesis and is somewhat COX2 selective. The antiplatelet action is short lasting. Neutrophil chemotaxis and superoxide production at the inflammatory site are reduced.


ARYLACETIC ACID DERIVATIVES

 

Diclofenac Sodium

 

An analgesic antipyretic anti-inflammatory drug, similar in efficacy to naproxen. It inhibits PG synthesis and is somewhat COX2 selective. The antiplatelet action is short lasting. Neutrophil chemotaxis and superoxide production at the inflammatory site are reduced.

 

It is well absorbed orally, 99% protein bound, metabolized and excreted both in urine and bile. The plasma t½ is ~2 hours. However, it has good tissue penetrability and concentration in synovial fluid is maintained for 3 times longer period than in plasma, exerting extended therapeutic action in joints.

 

Adverse Effects of diclofenac are generally mild: epigastric pain, nausea, headache, dizziness, rashes. Gastric ulceration and bleeding are less common. Reversible elevation of serum aminotransferases has been reported more commonly; kidney damage is rare.

 

Diclofenac is among the most extensively used NSAID; employed in rheumatoid and osteoarthritis, bursitis, ankylosing spondylitis, toothache, dysmenorrhoea, posttraumatic and postoperative inflammatory conditions—affords quick relief of pain and wound edema.

 

Dose: 50 mg TDS, then BD oral, 75 mg deep i.m. VOVERAN, DICLONAC, MOVONAC 50 mg enteric coated tab, 100 mg S.R. tab, 25 mg/ml in 3 ml amp. for i.m. inj. DICLOMAX 25, 50 mg tab, 75 mg/3 ml inj.

 

Diclofenac  potassium:  VOLTAFLAM  25,  50  mg  tab,

 

ULTRAK 50 mg tab; VOVERAN 1% topical gel.

 

DICLONAC, VOVERAN OPHTHA 0.1% eye drops.

 

Aceclofenac

 

A somewhat COX2 selective congener of diclofenac having similar properties. Enhancement of glycosaminoglycan synthesis may confer chondroprotective property.

 

Dose: 100 mg BD; ACECLO, DOLOKIND 100 mg tab, 200 mg SR tab.

 

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