Anti-inflammatories and Corticosteroids Flashcards
Prostaglandins are produced in almost all tissues and act _____
locally
(they don’t circulate in the blood)
Function of Prostaglandins
- Modulate pain, inflammation, and fever
- Control physiologic functions such as acid secretion and mucus production in the GI tract, uterine contractions, and renal blood flow
- Released in allergic and inflammatory processes and direct inflammatory response
_____ is the primary precursor of prostaglandins
and is a component of the phospholipids of cell membranes
Arachidonic acid
Free arachidonic acid is released from _____
tissue phospholipids by phospholipase A2
Prostaglandins are synthesized from
arachidonic acid via the _____
cyclooxygenase pathway
COX enzymes functions
COX-1: Responsible for the physiologic production of prostanoids; “housekeeping functions, regulates normal cellular processes
COX-2: Causes elevated production of prostanoids that occur during chronic inflammation and cancer, Expressed in tissue such as brain, kidney, and bone
T/F COX-1 and COX-2 have differences
in binding site shape which allow
for selective inhibitors
T
NSAIDs (Nonsteroidal Anti-inflammatory Drugs) MOA
● Inhibit the synthesis of prostaglandins
● Primarily inhibit the cyclooxygenase enzymes that catalyze the first step in prostanoid biosynthesis
Aspirin is a _____ NSAID
Non-Selective NSAID
NSAID analgesic effects:
○ PGE2 sensitizes nerve endings so NSAIDs decrease PGE2 synthesis, which decreases pain sensation
○ Inhibiting COX-2 which is released during inflammation and injury and is thought to cause the analgesic effect
NSAIDs lower body temp by impeding ____
synthesis; essentially resetting the thermostat
towards normal
PGE2
Non-Selective NSAIDs
● Aspirin (ASA)
● Ibuprofen (Ibu, Motrin, Advil)
● Naproxen (Aleve)
● Diclofenac (Voltaren)
● Ketoprofen (Orudis)
● Piroxicam (Feldene)
● Meloxicam (Mobic)
● Indomethacin (Indocin)
● Ketorolac (Toradol)
NSAIDS most important effects
Anti-inflammatory
Analgesic
Antipyretic
Contraindications for NSAIDS
● NSAID induced asthma orurticaria
● Aspirin triad
● 3rd Trimester of Pregnancy
● CABG surgery periop use
● Hypersensitivity to NSAIDs
Additional contraindication for Indomethacin (NSAID)
Neonatal: renal impairment, active bleeding, necrotizing enterocolitis, congenital heart
disease
Additional contraindication for Ketorolac (NSAIDS)
Pre-op major surgery, CABG periop pain, labor
and delivery, coagulation disorders
NSAIDS BBWs:
- increase risk of serious and potentially fatal GI adverse events such as bleeding, ulcers, and stomach or intestine perforation
- increase risk of serious and potentially fatal
cardiovascular thrombotic events, including MI and stroke; contraindicated for CABG perioperative pain
____ is an NSAID with indications for more moderate to severe pain
Ketoralac