Anti-inflammatories (year 2) Flashcards
name the drugs that can be used as anti-inflammtories
NSAIDs glucocorticoids anticytokines immunosuppressants antihistamine
what is the mode of action of NSAIDs?
inhibit COX enzyme
what does the COX enzyme do?
forms prostanoids from arachidonic acid
what does the prostanoid group contain?
prostaglandins and thromboxanes
what three effects do NSAIDs have?
anti-inflammatory
analgesic
antipyretic
what prostaglandin do NSAIDs reduce that reduces inflammation?
prostaglandin E2 and prostacyclin
what does a decrease in prostaglandin E2 and prostacyclin causes?
reduced vasodilation and oedema
how does a decrease in prostaglandins result in analgesia?
decrease in sensitisation of nociceptive nerve endings to inflammatory mediators
why do NSAIDs have a lot of adverse effects?
prostaglandins are important in normal homeostatic function
what are some of the normal functions prostaglandins?
gastric protection - mucus production and proton pump inhibitor
platelet aggregation
renal blood flow autoregulation
which of the COX enzymes is a constitutive enzyme and which is an induced enzyme?
constitutive - 1
induced - 2
what is a constitutive enzyme?
one found in most tissues with a role in homeostasis
which COX is mainly responsible for the mediators of inflammation?
COX-2
inhibition of which COX enzyme are most of the side effects of NSAIDs due to?
1
describe the absorption of NSAIDs
weak acids that are readily absorbed from the GI tract
how are NSAIDs transported in blood?
bound to albumin
why is the fact NSAIDs are distributed bound to albumin important?
changes in protein alters the transport and efficacy of the drug
if given with another drug that is bound to albumin then they compete
how are NSAIDs eliminated from the body?
hepatic phase I and II metabolism
excreted in urine/faeces