8) Inflammation Flashcards
What is the class for Acetylsalicylic acid (ASA, Aspirin)
Salicylate
What is the mechanism for Acetylsalicylic acid (ASA, Aspirin)
Acetyl-salicylic acid irreversibly acetylates COX-1 and -2; metabolite (salicylic acid) reversibly inhibits COX-1 and -2
What are the therapeutics for Acetylsalicylic acid (ASA, Aspirin)
Antiplatelet, analgesic and antipyretic, and anti-inflammatory (in ascending order of amount taken); often taken as a “baby aspirin” to prevent MI, CVA
What are the important side effects for Acetylsalicylic acid (ASA, Aspirin)
GI irritation, bleeding and anemia, hepatotoxicity, and salicylate toxicity
What are the other side effects for Acetylsalicylic acid (ASA, Aspirin)
Nephrotoxicity in elderly or hypovolemic patients; rare hypersensitivity reaction
What is the class for Diflunisal (Dolobid)
Salicylate
What is the mechanism for Diflunisal (Dolobid)
Difluorophenyl derivitive of salicylic acid, which reversibly inhibits COX-1 and -2
What are the therapeutics for Diflunisal (Dolobid)
Osteoarthritis, musculoskeletal strains/sprains, pain after dental extraction, and postepisiotomy pain
What are the important side effects for Diflunisal (Dolobid)
Fewer GI side effects and less effect on platelets than aspirin
What is the class for Acetaminophen (Tylenol)
Para-amino phenol
What is the mechanism for Acetaminophen (Tylenol)
Reversibly inhibits COX-1 and -2 (favors COX-1)
What are the therapeutics for Acetaminophen (Tylenol)
Analgesic and antipyretic effect similar to aspirin, but weak anti-inflammatory effects
What are the important side effects for Acetaminophen (Tylenol)
Renal tubular necrosis if chronically abused with other NSAIDs; hepatic necrosis with overdose
What are the other side effects for Acetaminophen (Tylenol)
GI irritation (less than aspirin)
What are the miscellaneous for Acetaminophen (Tylenol)
Poor function in presence of peroxides (as found in sites of inflammation); mostly metabolized via conjugation, but minor pathway via P450 enzymes may lead to toxic intermediate (N-acetyl-benzoquinoneimine)
What is the class for Indomethacin (Indocin)
Indole
What is the mechanism for Indomethacin (Indocin)
Reversibly inhibits COX-1 and -2 (favors COX-1)
What are the therapeutics for Indomethacin (Indocin)
Rhematoid arthritis (10X as potent as aspirin), ankylosing spondylitis, osteoarthritis, acute gout
What are the important side effects for Indomethacin (Indocin)
At times, thrombocytopenia, aplastic anemia, and severe frontal headaches
What are the other side effects for Indomethacin (Indocin)
Nephrotoxicity in elderly or hypovolemic patients
What is the class for Sulindac (Clinoril)
Indole
What is the mechanism for Sulindac (Clinoril)
Reversibly inhibits COX-1 and -2 (favors COX-1)
What are the therapeutics for Sulindac (Clinoril)
Rhematoid arthritis, ankylosing spondylitis, osteoarthritis, acute gout
What are the important side effects for Sulindac (Clinoril)
At times, thrombocytopenia, aplastic anemia, and severe frontal headaches
What are the other side effects for Sulindac (Clinoril)
Nephrotoxicity in elderly or hypovolemic patients