NON- STEROIDAL ANTI INFLAMMATORY DRUGS -PHARMACOLOGY CLASSSIFICATION ,ASPIRIN -USES AND ADVERSE EFFECTS

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 NON -STEROIDAL ANTI INFLAMMATORY DRUG 

  • They are non-opioid analgesics 
  • They have anti-pyretic ,uricosuria properties

CLASSIFICATION 

A)NON SELECTIVE COX-INHIBITOR :

ACETIC ACID ACID :

 KETOROLAC,INDOMETHACIN,NABUMETONE

ENOLIC ACID :

PIROXICAM

PYRAZOLONE :

PHENYLBUTAZONE

OXYPHENBUTAZONE

FENAMATE :

MEPHENAMIC ACID

PROPIONIC ACID :

IBUPROFEN

KETOPROFEN

NAPROXEN

FLURBIPROFEN

SALICYLATE:

ASPIRIN

B)PREFERENTIAL COX-2 INHIBITORS  :

DICLOFENAC

ACECLOFENAC

ETODOLAC

NIMESULIDE

MELOXICAM


C)SELECTIVE COX - 2 INHIBITOR :

PARECOXIB

CELECOXIB

ETORICOXIB

D)ANALGESICS WITH ANTI-PYRETIC WITH POOR ANTI-INFLAMMATORY ACTION:

PARA AMINOPHENOL DERIVATIVE :PARACETAMOL (ACETAMINOPHEN)

PYRAZOLONE DERIVATIVES:METAMIZOL

PROPIPHENAZONE

BANZOXAZOCINE DERIVATIVE :NEFOPAM







MECHANISM OF ACTION:

  • When any infectious agent (stimuli)enters the  body it affect phospholipid bilayer ( important component of cell membrane)it stimulate enzyme phospholipase A2  ,it destroys phospholipids to arachidonic acid it enters two pathway either cyclooxygenase  pathway or lipoxygenase pathway :

COX pathway it gets converted to prostaglandin G2 -further converted to PGH2 with help of prostaglandin isomerase gets converted to PGD2,PGE2,PGF2 ALPHA

COLLECTIVELY CALLED AS PROSTAGLANDIN 

  • PGE2 AND PGF2 ALPHA :Is responsible for fever ,pain and inflammation ,when nsaid is used it inhibits cox enzyme thereby decreasing the potential of PGE2 AND PGF2 Inhibiting pain ,analgesic effect ,anti-pyretic and anti inflammatory effect .
  • NSAID are COX Inhibitors ,COX there are two subtypes COX-1 AND COX-2 (Produced by inflammatory cells ) COX-1 (FOUND IN STOMACH and responsible for production of mucus  in the stomach ,protection against acid )

NOTE:

  • If Nsaid is non-selective it will inhibit cox-1 and cox-2 ,INHIBITOPN OF COX-1 is harmful as it increases the risk of ulcer ,that's the reason why doctors prescribe antacid as supplement 

LIPOOXYGENASE PATHWAY :

  • Arachidonic acid gets converted to leukotriene A4 

COX-1 found in :Normal cell ,COX-2 found in inflammatory cell 






ASPIRIN :

  • Analgesic ,relieves pain of inflammatory origin
  • When compared to morphine is less analgesic
  • Its protype drug of salicylates 

USES:

  • ANTIPYRETIC ACTION:
  • In presence of fever ,decreases temperature 

ANTI-INFLAMMATORY :

  • Sign ,symptom of inflammation 
  • Enhance cellular metabolism
  • Aspirin is gastric irritant 
  • In pregnant women it delays labor 

ADVERSE EFFECT :

  • Acute salicylate poisoning -in adults
  • decreases synthesis of clotting factor 
  • nausea ,vomiting





PHARMACOLOGICAL ACTION:

  • BLOOD: platelet aggregation prevented
  • GASTROINTESTINAL SYSTEM : Gastric mucosal damage
  • RESPIRATION: Increases oxygen consumption 






CONTRAINDICATION OF ASPIRIN :

  • Hypertensive patient
  • Asthmatic
  • Peptic ulcer
  • In children with Reye syndrome
  • Hepatic necrosis
  • Pregnancy near or at term
  • Breastfeeding mother 



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