Exam 4 - NSAIDs Flashcards
Function of Cyclooxygenase (COX)
Enzyme that converts arachidonic acid into prostaglandins
Two groups of cyclooxygenase inhibitors
1 - NSAIDs
2 - Acetaminophen
Two subgroups of NSAIDs
1st gen NSAIDS (inhibit cox1 and cox2)
2nd gen NSAIDS (selective for inhibiting cox2)
Examples of NSAIDs
Aspirin
Celecoxib
Ibuprofen
Naproxen
Advil
Drugs without anti inflammatory properties
Acetaminophen
Action of first generation NSAIDS
Inhibit cox1 and cox2
What are first generation NSAIDs used for?
To treat inflammatory disorders
(Especially rheumatoid arthritis, osteoarthritis, bursitis)
Alleviate mild to moderate pain
Suppress fever
Prototype NSAID
Aspirin
Therapeutic uses of aspirin
Analgesic
Antipyretic
Anti-inflammatory
(Suppression of platelet aggregation, protects in thrombotic disorders)
Unique characteristic about aspirin that other NSAIDs do not have
Protects against MI and stroke
Adverse effects of Aspirin
GI effects: gastric upset, GI bleeding
Renal impairment
Salicylism (ringing in ears, N&V)
Reye’s syndrome in children
Hypersensitivity reaction
Risks of taking Aspirin during pregnancy
Anemia
Postpartum hemorrhage
May prolong labor
Drug interactions with Aspirin
Anticoagulants: Warfarin, Heparin
Glucocorticoids
Alcohol
Ibuprofen
ACE inhibitors and ARBs
Principle indications for non-Aspirin first gen NSAIDs
Rheumatoid arthritis
Osteoarthritis
Class of Ibuprofen
First generation NSAID
Safety alert for all first generation NSAIDs
Associated with increased risk of GI bleeding that can lead to hospitalization or death
Function of Second generation NSAIDs
Just as effective as first generation in suppressing inflammation and pain
Side effects of second generation NSAIDs
Impaired renal function
HTN
Edema
*Increases risk for MI and Stroke
(Somewhat lower risk for GI side effects)
Prototype for second generation NSAIDs
Celecoxib (Celebrex)
*Uses of Celebrex
Osteoarthritis
Rheumatoid arthritis
Acute pain
Dysmenorrhea
Familial adenomatous polyposis
Adverse effects of Celebrex
GI ulceration
Renal impairment
Sulfonamide allergy
Cardiovascular impact (stroke, MI, etc.)
*Contraindicated in pregnancy
What is Celebrex not a great choice for long term management of pain?
*Because of cardiovascular risks
Drug interactions with Celebrex
*Warfarin (and other anticoagulants)
May decrease diuretic effect of furosemide
May decrease antihypertensive effect of ACE inhibitors
May increase levels of lithium
Levels may increase by fluconazole
Therapeutic uses of Acetaminophen (Tylenol)
Analgesic
Antipyretic
(Does not have anti inflammatory or anti rheumatic actions)
Action of Acetaminophen
Inhibits prostaglandin synthesis in CNS
Adverse effects of Tylenol
Very few at normal doses:
*Hepatotoxicity
Overdose: *hepatic necrosis
S/S of hepatic necrosis
Early: N&V, diarrhea, sweating, abdominal pain
Late: hepatic failure, coma, death
Treatment for Tylenol overdose
*Acetylcysteine (Mucomyst)
Drug interactions with Acetaminophen
Alcohol
Warfarin
