Eicosanoids, NSAIDs, Acetaminophen Flashcards
Leukotrienes
5-LOX found in leukocytes, mast cells, and dendritic cells
Associated with asthma and anaphylactic shock
COX 1
Expressed in most cells
COX 2
Inducible–expressed at sites of inflammation
Produces PGI2
Action of prostanoids on smooth muscle
Relaxation: PGI2, PGD2, PGE2
Constriction: TXA2, PGF2a, PGE2
Action of prostanoids on platelets
Stabilization: PGI2, PGD2, PGE2
Aggregation: TXA2, PGE2
Acton of prostanoids on GI
Cytoprotective
Increase mucus and bicarb
Increase motility
Action of prostanoids on CNS
PGE2 causes fever
Wakefulness
Decreased NE release
Sensitize pain pathways
Action of prostanoids on eye
PGE and PGF decrease intraocular pressure by increasing aqueous humor outflow
NSAIDS block
synthesis of all prostanoids
Misoprostol
PGE1 analog
Used for NSAID induced ulcer, to maintain PDA patency
Contraindicated in pregnancy
Epoprostenol
PGI2 analog
Used for pulmonary hypertension
Latonoprost
PGF2a analog
Used for treatment of glaucoma
Dinoprostine and Carboprost
PGF2a analog
Used to induce labor or abortion
NSAIDs
nonselective, competitive inhibitor of COX 1 and COX 2
Aspirin is the only irreversible inhibitor
4 indications of NSAID
analgesic, antipyretic, anti inflammatory, anti platelet aggregation
Aspirin doses and uses
80mg: anti-platelet for post MI and decrease TIA risk
300mg: analgesix and antipyretic
3-5g: anti inflammatory
Aspirin and ETC
Acts as an uncoupler: causes combined acidosis in toxic doses
OD management of aspirin
Supportive–no antidote
Adverse effects of chronic aspirin use
GI irritation, exacerbation of asthma due to over action of LOX, angioedema and rash hypersensitivity, renal toxicity due to decreased prostaglandins
Who should you not give aspirin to
Asthmatics and children <18 (Reye Syndrome risk)
Other NSAID uses
Analgesic, antipyretic, anti inflammatory
Not anti platelet
Acetaminophen
Blocks CNS COX; no peripheral COX inhibition so no antiplatelet or bronchospasm or anti inflammatory
Minimal GI distress and no uncoupling
Hepatotoxicity of acetaminophen
requires >10-15g in adults
Antidote of acetaminophen OD
N-acetylcysteine: must be given within 10 hours