Prostaglandins And Other Eicosanoids Flashcards
LTC4 and LTD4
Bronchoconstrictiors important in anaphylaxis and cause edema
LTB4
Chemotactic factor in inflammation
Zileuton
Lox inhibitor - blocks synthesis asthma prophylaxis
Montelukast zarfirlukast
Leukotriene receptor inhibitors
Blocks CydLT1 receptors reduces bronchoconstriction in asthma
Asthma prophylaxis
TXA2
Causes platelet aggregation vasoconstriction
Epoprostenol
PGI2 - causes vasodilation and reduces platelet aggregation
Used in pulmonary HTN and anti platelet agent in extra corporeal dialysis
Misoprostol
PGE1 caused increased HCO3 and mucus secretion in stomach and uterine contraction
Protective agent in peptic ulcer disease
Abortifacient
Alprostadil
Pge1
Injectable form for erectile dysfunction
PGE1
Relaxes smooth muscle in ductus arteriosus
Transpositions of great vessels to maintain patent ductus until surgery
Dinoprostone
PGE2
Low concentrations contract
Higher ones relax uterine and cervical smooth muscle
Used for abortions and cervical ripening
Latanoprost
PGF2
Increases outflow of aqueous humor reduces intraocular pressure
Used in glaucoma
Color change in iris
No selective cox1 and cox 2 inhibitors
Ibuprofen, indomethacin , naproxen
Reversibly inhibit both cox
Aspirin
Irreversibly inhibit cox 1 and cox 2
Celecoxib
Selectively reversibly inhibits cox 2
PGI2
Prostacyclin formed by cox2 promotes vasodilation and inhibits platelet aggregation
Acetaminophen
MOA: unclear may inhibit a cox3
Has analgesic effects and antipyretic . Lacks anti-inflammatory or anti platelet
Ketorolac
Cox 1 selective
IM used for moderate to severe pain since it’s equal to morphine
Not an anti inflammatory
Short term use and not before surgery
Flurbiprofen
Relatively cox 1 selective
Ketoprofen
Non selective
Aspirin
Non selective
Naproxen
Non selective
Ibuprofen
Non selective
Indomethacin
Non selective
Sulindac
Non selective
Celecoxib
Relatively cox 2 selective
Rofecoxib
Cox 2 selective withdrawn from market
Valdecoxib
Cox 2 selective withdrawn from market
What is the cv risk with cox 2 selective inhibitors
Cox-1 in platelets makes thromboxane which causes aggregation
Cox-2 makes prostacyclins PGI2 - which inhibits aggregation so if it’s blocked there is wayyyy too much TXA2 but not enough PGI2 and you get clots.
Naproxen has the least cv risk
Tramadol
Not anti inflammatory
Not antipyretic
Is analgesic
Weak opioid agonist and inhibits NE and 5-HT uptake
Acetaminophen toxicity
Metabolized by cyp450
Results in benzoquinone imminent hat normally reacts with glutathione to form non toxic metabolites. Large does deplete the glutathione and the metabolite reacts with sulfhydryl groups in hepatic proteins to cause necrosis
