Docsity
Docsity

Prepare for your exams
Prepare for your exams

Study with the several resources on Docsity


Earn points to download
Earn points to download

Earn points by helping other students or get them with a premium plan


Guidelines and tips
Guidelines and tips

NSAIDs and Eicosanoids, Study Guides, Projects, Research of Medical Sciences

The effect of NSAIDs on different organs and how they work. It also describes the biosynthesis of prostaglandins and the two main pathways involved. the major rules of eicosanoids and their pharmacokinetics and pharmacodynamics. It also explains the pharmacological action of NSAIDs and their effect on inflammation, analgesia, and anti-pyretic action. The document also describes the use of NSAIDs in maintaining a patent ductus arteriosus in newborns and the contraindications of aspirin. It also lists different groups of NSAIDs and their doses.

Typology: Study Guides, Projects, Research

2022/2023

Available from 02/11/2023

professor_x
professor_x 🇮🇳

238 documents

1 / 54

Toggle sidebar

This page cannot be seen from the preview

Don't miss anything!

bg1
pf3
pf4
pf5
pf8
pf9
pfa
pfd
pfe
pff
pf12
pf13
pf14
pf15
pf16
pf17
pf18
pf19
pf1a
pf1b
pf1c
pf1d
pf1e
pf1f
pf20
pf21
pf22
pf23
pf24
pf25
pf26
pf27
pf28
pf29
pf2a
pf2b
pf2c
pf2d
pf2e
pf2f
pf30
pf31
pf32
pf33
pf34
pf35
pf36

Partial preview of the text

Download NSAIDs and Eicosanoids and more Study Guides, Projects, Research Medical Sciences in PDF only on Docsity!

Objectives e What’s inflammation ? e How does NSAIDs work ? e Effect of NSAIDs on different organs ° Groups of NSAIDs e Acetaminophen e The specific chemical mediators vary with the type of inflammation and include : Amines : histamine and 5Hydroxytryptamine (serotonin ) Lpids : prostaglandines ( PGs ) , thromboxanes ( TXs ) and leukotrienes ( LTs ) . Small peptides : Bradykinin . Larger peptides : interleukin 1 and tumor necrosis factor o N.B Anti inflammatory drugs act by interfere with the action of specific mediator important in inflammation . e Non Steroidal anti inflammatory drugs ( NSAIDs ) have analgesic ( pain killer ) , anti pyretic ( fever reducing ) and anti inflammatory effect . e Steroidal anti inflammatory : Corticosteroids Acetaminophen ( paracetamol ) isnot considered an NSAID because it has a very weak anti inflammatory activity . e Two main pathways are involved in the biosynthesis of eicosanoids . 1- PGs and TXs are synthesized by cyclic pathway . 2- LTs are synthesized by linear pathway . Arachidonic acid esterified in membrane phospholipids Free radicals Diverse physical, chemical, inflammatory, and mitogenic stimuli ———B> | Phospholipase Az ‘ ; , ; Isoprostanes Epoxyeicosatrienoic acids (EETs) bee 5 1 COOH Cytochrome K P450 AA an eo 4 cis D5,8,11,14) Pe ee Lipoxygenases Cyclooxygenases (LOX) (COX) \ en Prostaglandins Leukotrienes Prostacyclin Prostanoids Lipoxins Thromboxane Source: Bertram G. Katzung: Basic & Clinical Pharmacology, Fourteenth Edition Copyright © McGraw-Hill Education. All rights reserved. e Major rules of Eicosanoids : PGs Modulate pain , inflammation and fever . Control acid secertion and mucus production in the GIT Control renal blood flow. Control uterine contraction . Prostacyclin ( PGIs ) Inhibit platelet aggregation . Induce vasodilation . TXs Induce platelet aggregation . Induce vasconstriction . LTs Powerful bronchoconstriction . Increase vascular permeability . e Pharmacokinetics Most are excreted renally . e Pharmacodynamics Inhibit of COX activity Aspirin is an irreversibly inhibitor of COX enzyme while other NSAIDs are reversible inhibitors . e Effect of NSAIDs on different organs bleeding and ulceration Normally NSAIDs inhibit COX1 patients with high risk for GI events : NSAIDs with PPI or Misoprostol ( PG analogue ) Patient counseling © TXAs enhance platelet aggregation © PGls decrease platelet aggregation Dose of aspirin ? Afferent Arteriole PGs; Increase GFR (VD) NSAIDs; Decrease GFR (VC) = , Efferent Arteriole Angiotensin tl; Increase GFR (VC) ACEts; Decrease GFR (VD) Bowman's capsule proximal convoluted tubule GCloretolar Filiathon | Bowman's Capsle L etteren’ atteriale G\omerviar keg (visceral \o Firtoinon Rote padocytes ( yet) (GFR) 2 aout ; simple sqpamnov§ epithelium oe Riltrane ereiucs) (parieval \oyer\ : loy Kidteys eon mnore \2Sem\ [tn (\cotn'e\dreys) NEW BRITAIN EMERGENCY MEDICAL SERVICES 7A AC ATYEMAY Normally : there is a balance between PGIs and TXA2 In heart cells PGIs is mediated by COX2 TXAz2 is mediated by COX1 SO NSAIDs with a very high degree of COX1 selectivity such as ASPIRIN have a cardiovascular protective effect . NSAIDs with a very degree of COX2 selectivity have a high risk for cardiovascular events ( MI and strock ) e Aspirin in high dose = 325 mg inhibit PGl2 production and may carry a risk for CVS events . N.B ALL NSAIDs aren't without CVS risk Naproxen appears to be the least CVS risk .