Action:
Inhibition of COX-2 by celecoxib is time dependent and reversible.
Pharmacokinetics:
It is readily absorbed orally. Its peak concentration is approximately 3 hours. It is metabolized in the liver by cytochrome P450 (CYP2C9). It is excreted in feces and urine. Its half life is 11 hours, so its dose is adjusted according to once a day.
Adverse Effects:
It may cause abdominal pain, Diarrhea, Dyspepsia and Kidney toxicity may also occur.
Drug interactions:
It inhibits CYP2D6 and so can elevate levels of ß-blockers, anti-depressants and anti-psychotic drugs.
Fluconozole, fluvastatin and zafirlukast may increase serum level of celecoxib.
Precautions:
It should be avoided in patients;
- with chronic renal insufficiency
- Severe heart disease
- Volume depletion
- Hepatic failure
Sunday, April 10, 2011
COX-2 selective NSAIDs
COX-2 is better in providing space for inhibitors than COX-1.
Uses:
It is used as a pain reliever.
Adverse effects:
It may cause renal insufficiency and hypertension.
Uses:
It is used as a pain reliever.
Adverse effects:
It may cause renal insufficiency and hypertension.
Diflunisal
It is diflurophenyl derivative of salicylic acid.
Action:
3-4 times more potent than aspirin but cannot be used as antipyretic.
Pharmacokinetics:
It is not metabolized to salicylate and therefore cannot cause salicylate intoxication. It cannot enter CNS, so cannot relieve fever.
Action:
3-4 times more potent than aspirin but cannot be used as antipyretic.
Pharmacokinetics:
It is not metabolized to salicylate and therefore cannot cause salicylate intoxication. It cannot enter CNS, so cannot relieve fever.
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.
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.
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.
Subscribe to:
Posts (Atom)
-
Q: What do you know about ergot alkaloids? Ans: These include alkaloids which we get from the ergot fungus Claviceps purpurea or derived ...
-
(For detailed study of Pharmaceutical Incompatibility Click here) Multiple Choice Questions (MCQs) from Pharmaceutical Incompatibility in ...
-
Multiple Choice Questions (MCQs) of Powders and Granules from Pharmaceutics 1. _______ powders consist of more than one ingredients. a. Si...
