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NSAIDS Dr.B.M.PUROHIT Assistant Professor (Pharmacology) P.D.U.MEDICAL COLLEGE, Rajkot (GUJARAT). 360001 [email_address]
INTRODUCTION ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Which are the features of inflammation… ? ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
So both phenomenon are beneficial
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object]
PGG2 MEMBRANE PHOSPHOLIPID ARACHIDONIC ACID 12-HPETE PHOSPHOLIPASE CHEMICAL AND MECHANICAL STIMULIE 5-HPETE PGH2 ISOMERASE THROMBOXANE SYNTHEASE PROSTACYCLINE SYNTHEASE CYCLOXYGENASE PATHWAY LIPOXYGENASE PATHWAY 15-HPETE PGD2 PGE2 PGF2 α TXA2 TXB2 PGI2 LTB4 LTA4 LTC4 LTD4 LTE4 LTF4
[object Object],[object Object]
PGG2 MEMBRANE PHOSPHOLIPID ARACHIDONIC ACID 12-HPETE PHOSPHOLIPASE CHEMICAL AND MECHANICAL STIMULIE 5-HPETE PGH2 ISOMERASE THROMBOXANE SYNTHEASE PROSTACYCLINE SYNTHEASE CYCLOXYGENASE PATHWAY LIPOXYGENASE PATHWAY 15-HPETE PGD2 PGE2 PGF2 α TXA2 TXB2 PGI2 LTB4 LTA4 LTC4 LTD4 LTE4 LTF4
Summary of the  chart… ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object]
They are Opposite !!! Store it in your mind !!!
It is not possible to remember everything !! Don’t  worry !!
[object Object],[object Object],[object Object]
PAIN ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
CLASSIFICATION ,[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object]
SOMATIC SENSORY CORTEX ` Amygdala Hypothalamus Midbrain periaqueductal gray matter Parabrachial nucleus Medullary  Reticular  formation Locus cerulous Raphe nuclei Dorsal horn of the spinal cord Anterolateral  System
[object Object],[object Object],[object Object],[object Object],[object Object]
Pharmacological/Physiological Effects I. Cardiovascular   System
II. PLATELETS
NORMALLY IN GIT… NSAIDS blocks this So PGS have PROTECTIVE effect on GIT
RESPIRATORY SYSTEM
GI TRACT
V. Reproductive Organs
[object Object],[object Object],[object Object],[object Object],Pharmacological/Physiological Effects
PGS produce PAIN…  how ?
PGS produces FEVER….. How ? ,[object Object],[object Object],[object Object]
PGs PRODUCES INFLAMMATION … HOW ? INFLAMMATION
Mechanism Of Action : NSAIDS MOST IMPORTANT MECHANISM Efficacy of these mechanisms is doubtful.. So you are not required to remember everything!! Just keep in mind that such mechanisms exist !!
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],So NON SPECIFIC NSAIDS produces bleeding tendency and peptiuc ulcer
SALICYLATES
Analgesic activity ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
NSAIDS blocks.. REDUCES THE INTENSITY OF PAIN
ANTIPYRETIC ACTIVITY ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],NSAIDS inhibits PGE2 synthesis and reduces fever
GIT ,[object Object],[object Object],[object Object],[object Object],[object Object]
ANTIINFLAMMATORY ACTIVITY ,[object Object],[object Object],[object Object],[object Object],[object Object]
BLOOD AND PLATELETS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
URICOSURIC ACTION ,[object Object],[object Object]
PHARMACOKINETICS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],So little central action.
[object Object],[object Object],[object Object],[object Object],PHARMACOKINETICS Salicylate Deacetylation Salicylic acid
[object Object],PHARMACOKINETICS Salicylate Glycine conjugation Glucuronic acid conjugation Oxidized to Gentisic acid
[object Object],[object Object],[object Object],[object Object],ADVERSE REACTION Cell Membrane Phospholipids Arachidonic Acid Prostaglandin H 2 Phospholipase A 2 Cyclooxygenase I&II Leucotriens  Inflammation  Bronchospasm  NSAIDS
GIT
KIDNEY
REYE’S SYNDROME
Aspirin Toxicity - Salicylism
MANAGEMENT OF SALICYLISM ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
USES ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
ANTIRHEUMATIC Antirheumatic action
ANTIPLATELET ACTION  ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
NOW IT’S TIME TO REVISE ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Diflunisal  ,[object Object],[object Object],[object Object]
PARACETAMOL ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
NAC SUPPLIES GLUTATHIONES so detoxifies toxic metabolites !! NAC  “MAY”directly conjugates with quinones/epoxide.  MAY BE… NAC has additional antioxidant and antiinflammatory activity
[object Object],[object Object],PARACETAMOL   ( acetaminophen)
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
SELECTIVE COX-2 INHIBITORS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],BANNED BECAUSE OF CARDIOVASCULAR MORATLITY
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
TOPICAL NSAIDS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Selection of NSAID
NSAIDS.

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NSAIDS.