NSAIDS

NSAIDS Dr.B.M.PUROHIT Assistant Professor (Pharmacology) P.D.U.MEDICAL COLLEGE, Rajkot (GUJARAT). 360001 [email_address]

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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

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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

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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]

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They are Opposite !!! Store it in your mind !!!

It is not possible to remember everything !! Don’t worry !!

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]

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

Pharmacological/Physiological Effects I. Cardiovascular System

NORMALLY IN GIT… NSAIDS blocks this So PGS have PROTECTIVE effect on GIT

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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

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

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]

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ANTIRHEUMATIC Antirheumatic action

ANTIPLATELET ACTION ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]

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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]

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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)

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SELECTIVE COX-2 INHIBITORS ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],BANNED BECAUSE OF CARDIOVASCULAR MORATLITY

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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]

NSAIDS

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NSAIDS