Monday, September 30, 2013

Aspirin Some Learning Aspects

Aspirin is is the prototype of traditional NSAIDs.Aspirin was first isolated by Felix Hoffmann, a chemist with the German company Bayer in 1897. It was officially approved by the FDA in 1939.




1.Which component of Aspirin react with Cycloxygenase ?
Aspirin on hydrolysis during phase 1 of metabolism produce acetyl and salisylic acid. Acetyl group binds to cycloxygenase and make it inactive.
2.What happen if Viral disease patient take aspirine?
In the viral infection, aspirin is usually associated with Reye syndrome, which is an often fatal, fulminating hepatitis with cerebral edema.In this case Acetoaminophen and Ibuprofen are appropriate in this condition.
3.Aspirin is FDA pregnancy category C or D?
 Aspirinis classified as FDA pregnancy category C risk during the first and second trimesters and category D during  the third trimester.
5. Aspirin both inhibit the platelet aggregation as well as promote aggregation through TXA2 and PGI2 inhibition.Then Why its inhibitory effect is more pronounced?
TXA2 enhances platelet aggregation, whereas  PGI2decreases it. Low doses (81 to 325 mg daily) of aspirin can  irreversibly inhibit thromboxane production in platelets via  acetylation of cyclooxygenase . Because platelets  lack nuclei, they cannot synthesize new enzyme, and the lack of  thromboxane persists for the lifetime of the platelet (3–7 days). As   a result of the decrease in TXA2production, platelet aggregation  (the first step in thrombus formation) is reduced, producing an antiplatelet effect with a prolonged bleeding time. Finally, aspirin also inhibits cyclooxygenase in endothelial cells, resulting  in reduced PGI2 formation. However, endothelial cells possess 
nuclei and are able to re-synthesize new cyclooxygenase.
6. What is oil of wintergreen?
Methyl salisylate is called as oil of wintergreen. It is used externally as a cutaneous counter irritant in liniments.
7.Gastrointestinal side effects may be reduced?
1. Taken with food
2. Drink large amount of fluid.
3.Misprostol or Proton pump inhibitor use
8.Aspirin is not appropriate in Gout why?
Being an organic acid, salicylate is secreted into the urine and can affect uric acid excretion. Namely, at low doses of aspirin, uric acid secretion is decreased, whereas at high doses, uric acid secretion is increased. Therefore, aspirin should be avoided in patients with gout.

9.Aspirin and Asthma! What's the dilemma?
As cyclooxygenase is inhibited by Aspirin.So degredation of arachidonic acid by enzyme is also decrease.It looks beneficial in some conditions. But there is another point of thinking that this effect of aspirin also providing more substrate to Lipooxygenase which may induce asthma like conditions by diverting arachidonic acid to produce excess LTC4and D4.

10.Can we compare aspirin analgesic effect with codeine ?
It is simply to say 600 mg of aspirin is almost equally with 60 mg of codeine to produce same analgesia.

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