Disease modifying anti-rheumatic drugs (DMARDs) or slow acting anti-rheumatic drugs (SAARDs)
1. Slow the course of the disease and can induce remission.
2. Reduce or prevent the joint damage.
Drugs to be choosen:
Many experts start therapy with the conventional drugs i.e. methotrexate or hydroxychloroquine. But if these do not work properly then they go to the newer agents i.e. anakinra, adalimumab, leflunomide, and infliximab. Often it is also prescribed that the combination therapy is more effective.
Sunday, April 10, 2011
Acetaminophen
Action:
It inhibits prostaglandin synthesis in CNS (so analgesic and anti-pyretic) but has less effect on COX so (weak anti-inflammatory).
Therapeutic Uses:
It is used as analgesic and anti-pyretic. It is analgesic /anti-pyretic of choice for children with viral infections or chicken pox.
Drug interactions:
It does not antagonize the uricosuric agent (probenecid) and so may be used in patients with gout who are taking this drug.
Pharmacokinetics:
Rapidly absorbed from GI tract. 1st pass metabolism occurs in the luminal cells of the intestine and in the hepatocytes. It is conjugated in the liver to form inactive glucoronidated or sulfated metabolites. It is excreted in the urine.
Adverse effects:
It may cause skin and minor allergic reactions. Prolonged use may cause renal tubular necrosis and hypoglycemic coma.
It inhibits prostaglandin synthesis in CNS (so analgesic and anti-pyretic) but has less effect on COX so (weak anti-inflammatory).
Therapeutic Uses:
It is used as analgesic and anti-pyretic. It is analgesic /anti-pyretic of choice for children with viral infections or chicken pox.
Drug interactions:
It does not antagonize the uricosuric agent (probenecid) and so may be used in patients with gout who are taking this drug.
Pharmacokinetics:
Rapidly absorbed from GI tract. 1st pass metabolism occurs in the luminal cells of the intestine and in the hepatocytes. It is conjugated in the liver to form inactive glucoronidated or sulfated metabolites. It is excreted in the urine.
Adverse effects:
It may cause skin and minor allergic reactions. Prolonged use may cause renal tubular necrosis and hypoglycemic coma.
Celecoxib
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
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
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.
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