Sunday, April 10, 2011

Ketorolac

Action:

Similar to NSAIDs.

Administration:
It can be administered

• Orally

• Intramuscularly (for post operative pain)

• Topically (for allergic conjunctivitis)

Pharmacokinetics:
It undergoes metabolism in the liver. The drug and its metabolites are excreted in the urine.

Adverse effects:
It is similar to NSAIDs.

Diclofenac

Action:

It is more potent in action than naproxen and indomethacin. It is cyclooxygenase inhibitor.

Pharmacokinetics:
It accumulates in the synovial fluid. It is excreted into urine.

Therapeutic Uses:
It is used for the long term treatment of:
• Rheumatoid arthritis
• Osteoarthritis
• And ankylosing spondylitis.

Adverse effects:
Its adverse effects are similar to those of the NSAIDs.

Fenamates

They are used as a pain releiver.

Adverse effects:


• Diarrhea

• Hemolytic anemia (rare)

Oxicam derivatives

Action:

Meloxicam is relatively COX-2 selective.

Therapeutic uses:
(Similar to that of Acetic acid derivatives)

Pharmacokinetics:
These have usually longer half lives. Piroxicam and its metabolites are excreted in the urine whereas meloxicam and its metabolites are excreted equally in the urine and feces.

Adverse effects:
It may cause GI disturbances.

Sulindac

It is used for:


• Rheumatoid arthritis

• Ankylosing spondylitis

• Osteoarthritis

• And acute gout.

Indomethacin

It is used for:


• Acute gouty arthritis

• Ankylosing spondylitis

• And osteoarthritis of the hip.

Propionic acid derivatives

Mechanism of Action:

These are reversible inhibitors of cyclooxygenase.

Action:
These inhibit the synthesis of prostaglandins but not that of leukotrienes.

Pharmacokinetics:
It is absorbed orally. It has the ability to bind to plasma albumin. It undergoes hepatic metabolism and excreted by the kidney.

Therapeutic Uses:
It is used as anti-inflammatory mostly in the chronic treatment of rheumatoid arthritis and osteoarthritis. It is also anti-pyretic and anti-inflammatory.

Adverse effects:
• Headache, tinnitus and dizziness.
• GI disturbance ranging from dyspepsia to bleeding.