Anti-Inflammatories Flashcards
Anti-inflammatory drugs target?
Eicosanoids
glucocorticoids inhibit what release?
Arachadonic acid and metabolism
NSAIDS inhibit what only?
cyclo-oxygenases: COX1 and COX2
CysLT1 receptor antagonists block?
LTC4, LTD4 actions
Cox1 found?
all cells
COX2 found?
inducible
inflamm cells, smooth muscle, endothelium, fibroblasts
What condition has high COX2?
tumours
CB1 and CB2 (Canabinoids) receptors effects?
analgesia
anti-inflamm
sedation
appetite stim
Why not prostaglandins as drugs? Eg.?
unstable and expensive
eg. PGI2 (pulmonary hypertension)
PGE1
NSAIDS do 3 main things and 1 extra sometimes
- anti-inflamm
- analgesic
- anti-pyretic
- anti-aggregatory (aspirin)
NSAIDS curative?
Nope. Palliative
what is preferred for antipyretic?
paracetamol
4 big adverse effects of NSAIDS?
- GI
- bleeding time
- renal
- pulmonary
PGE2 does what?
GI: increase mucus reduce acid promote blood flow promote angiogenesis
NSAIDS inhibit which prostaglandins?
PGE2
PGI2
how do NSAIDS affect bleeding time?
- decreases thromboxane A2 synthesis
2. impaired platelet aggregation
how do NSAIDS affect renal?
decreased prostaglandin dilatation so compromised blood flow
NSAIDS can cause what kind of pulmonary effects?
bronchoconstriction in 10% of asthmatics d/t overproduction of leukotrienes
Aspirin contraindicated in 3 things:
- Reye’s Syndrome (kids causes hepatotoxicity)
- Tinnitis
- Gout
Apirin 2 special features?
- irreversible binding in platelets: increase PGI2, less TxA2
- Aspirin triggered Lipoxins for inflamm resolution
Aspirin lasts how long in blood?
few hours
How much is low-dose aspirin?
80mg per day
Aspirin triggered Lipoxin formed how?
acetylated COX2 and Ligands for FPR2
Aspirin in kids?
Not under 12 years old
Paracetamol an anti-inflammatory?
Nope
purpose of paracetamol?
- analgesic
2. antipyretic
Celecoxib inhibits what?
COX2>COX1
less GI
less anti-platelets (platelets are COX1)
COX-2 selectivity first year of a study?
No divergence then saw effect 2nd year
Which COX is the main prostacyclin producer with blood flow?
COX2, COX1 in stasis
Indication for glucocorticoids 2 main:
Addison’s
Anti-inflammatory
Anti-inflammatory use of glucocorticoids?
- asthma
- topical
- hypersensitivity: severe allergic reactions
- rheumatoid arthritis
glucocorticoids decrease inflamm how?
targets NFkB to decrease cytokines
Neural endopeptidase
GILZ
glucocorticoids adverse effects?
immunosuppression
ulcers
slow wound healing
The ‘mabs’ neutralize what? used in what?
TNF-alpha
used for Rheumatoid arthritis