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Summary Pharmacokinetics explained
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  • Course
  • Pharmacology
  • Institution
  • University Of Pretoria (UP)
  • Book
  • Rang & Dale\'s Pharmacology

I want to help you get through all the different drug classes in Pharmacology. I have found that students struggle to get through the amount of work. These summaries helped me get through my Honours Degree. I will soon graduate with my Masters of Science in Neurogenetics. You got this!

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Document information

  • Yes
  • June 19, 2019
  • 2
  • 2014/2015
  • Summary

Subjects

  • pharmacokinetics
  • drug metabolism
  • pharmacology
  • pk

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NSAIDS inhibit COX, thereby inhibiting prostaglandin synthesis

SALICYLIC ACID PROPIONIC ACID OTHERS SELECTIVE COX-2 ANALGESIC
DERIVATIVES DERIVATIVES INHIBITORS ONLY

 Aspirin  Ibuprofen  Diclofenac  Etoricoxib
 Naproxen  Indomethacin  Celecoxib  Paracetamo
 Nabumetone  Lumiracoxib l




Mechanism of action:



ANALGESIC action

 Peripheral actions predominate
 Associated with anti-inflammatory action
 Results from inhibition of prostaglandin synthesis in inflamed tissues
 Prostaglandins potentiate the pain caused by inflammatory mediators

Anti-inflammatory action:

 Attenuates inflammation (NOT abolish)
 Rheumatoid arthritis
 Not alter the course of the disease

Anti-pyretic action:

 Aspirin prevents temperature-raising effects of IL-1
 Prevent ↑ in brain prostaglandins levels

On COX:

 Enzymes with a long channel (wider in COX2)
 Block the channel by binding to arginine halfway down (hydrogen bonds)
 Reversibly inhibits enzyme by preventing access of arachidonic acid
 Aspirin acetylates enzyme at serine 530 (irreversible)



PARACETAMOL:

 ↓ Cytoplasmic peroxide tone
 Peroxide: activate haem enzyme  ferryl form

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