non sterodial anti inflammatory drugs Flashcards

Question

5 imporatnt NSAID and their half lives

Answer 1

Aspirin(2h) iduprofen 2h naproxen 15 paracetamol 2 celecoxib 10

Answer 2

XTraditional NSAIDs block:  Vasodilatation, which contributes to redness, heating and edema  Increased vascular permeability, which contributes to swelling  Pain associated with inflammation

Answer 3

PGE2 sensitization of peripheral nociceptive fibres by blocking cox1/2, reduce the pain transmission  NSAIDs block sensitization, but not direct nociceptive activation, may explain why NSAIDs have an “Analgesic Ceiling”.-- means only can suppress mild pain and if too high, cannot supress  NSAIDs also have additional analgesic action in the CNS

Answer 4

when there is Infection, tissue damage, inflammation, Neutrophils release Cytokines (IL-1β, TNF-α), NSAID block COX1/2 so PGE2 at hypothalamus will not cause Fever NSAIDs do not alter normal body temperature. Body’s “thermostat” reset

Answer 5

Aspirin As Anti-platelet Drug effectve as a blood thinner and prevent heart attack and stroke under normal condition, the blood fluid and there is TXA2 promotes platelet aggregation, leading to stroke and heart attack. and PGI2 inhibits platelet aggregation. thus when aspirin binds irrevicisbke to COX , TXA2 more than PGI2, it result in blood thinning

Answer 6

 GI Tract: N&V, gastric upset, and gastric ulceration, mainly due to COX-1 inhibition: ↓ PGE2  Pseudo-allergic reaction: skin rash, nasal congestion, anaphylactic shock  Bleeding due to blood thinning by aspirin  All non-aspirin NSAIDs have increased risks of heart attack/stroke  Aspirin-linked Reye’s Syndrome in children with viral infection  Aspirin-induced asthma in susceptible asthmatics, associated with viral URTI  Kidney: acute renal failure, hypernatremia, H2O retention, edema, hyperkalemia, ↓ glomerular filtration rate (GFR)  Pregnancy toxicity: 1st trimester (risk of miscarriage) and 3rd trimester (premature closure of ductus arteriosus)  High dose: Dizziness, deafness, tinnitus

Answer 7

mediator for astma, certain subjects take aspirin and develop asthma

Answer 8

Coxibs celecoxibs safer for the gi tract

Answer 9

Expectation of complete GI tract sparing with COX-2 selective inhibitors not realised Renal toxicity due to constitutive expression of both COX-1 & COX-2 in the kidney. Note that all NSAIDs are COX-2 inhibitors: contraindicated in third trimester of pregnancy causing premature closure of ductus arteriosus (fetal lung bypass) - patent ductus arteriosus requires PGE2 production **Relative increase in TXA2 favours platelet aggregation, which may increase risk of thrombosis (heart attack and stroke). COX-2 inhibitors impair wound healing and hence may exacerbate ulcers - healing requires COX-2 and PGE2.

Answer 10

CNS-selective COX (may be COX-3) inhibitor Anti-pyretic Action, do not have much inflammatory effect, painkiller and lowers fever, relatively safe liver converts into p aminophenol then into AM404 which is a agonist endogenous receptor analgesic actions

Answer 11

Good analgesic  Potent antipyretic  Spares the GI tract  Side-effects few and uncommon  Few drug-drug interactions  Relatively safe for pediatric use

Answer 12

 Weak anti-inflammatory  Toxic doses cause N&V, and hepatotoxicity by overdose or chronic alcohol use/abuse  Allergic skin reactions sometimes occur

non sterodial anti inflammatory drugs Flashcards

(36 cards)