Prostanoids and NSAIDs Flashcards
Major Prostaglandins
Prostanoid Acid and PGI2 (Prostacyclin)
Prostaglandin Synthases
Cox 1 - Constitutive
Cox 2 - Induced
NSAIDs
Analgesic Anti-pyretic Anti-inflammatory All inhibit COX (Some may inhibit LOX) Short-term relief
Salicylic Acid Derivatives
ASA
Diflunisal
Par-aminophenol Derivatives
Acetaminophen (Not Anti-Inflammatory)
Indole and Irdene Acetic Acids
Etodolac
Heteroaryl Acetic Acids
Diclofenac
Ketorolac
Arylpropionic Acid
Ibuprofen
Naproxen
Flurbiprofen
Ketoprofen
Anthraniic Acids (Fenamates)
Mefanamic Acid
Enolic Acids
Mecloxicam
Alkanones
Nabumetone
Diarylheterocycles (COX2 Selective Inhibitors)
Celecoxib
Prostaglandin
Hyperalgesia
Allodynia
Spontaneous pain
Aspirin
Irreversible acetylation of serene in active site of both cyclo-oxygenases; Acetylation of COX2 alters enzymatic action to produce 15-epi-lipoxins and resolvins
May induce asthma
Anaphylactoid reaction: Arachidonic acid to Prostaglandin (COX inhibit) switch to Leukotrienes (LOX)
NSAID Platelet Function
Blocks
Aspirin - Irreversible block of thromboxane synthesis in platelets and effect lasts until new platelets form (7days); NSAID - Reversibly inhibits COX so short term thromboxane effect
COX2 inhibitors - Reduce PGI2 protective effect, Blood clots, Cardiac arrest, Death (Inhibit COX2 in endothelial cells - Reduce beneficial vasodilatory activity of PGI2 and prevent platelet aggregation (No effect on COX1)