Cycloxygenase Inhibitors Flashcards
Cyclooxygenase Inhibitors:
Nonsteroidal Anti-inflammatory Drugs and Acetaminophen
Cyclooxygenase Inhibitors Uses
➢ Suppress inflammation
➢ Relieve pain
➢ Reduce fever
Cyclooxygenase Inhibitors adverse effects
➢ Gastric ulceration
➢ Bleeding
➢ Renal impairment
Classification of Cyclooxygenase Inhibitors
Drugs with anti-inflammatory properties or Drugs without anti-inflammatory properties
Drugs with anti-inflammatory properties -
NSAIDs: nonsteroidal anti-inflammatory drugs (Aspirin, celecoxib, ibuprofen, and naproxen)
Drugs without anti-inflammatory properties -
Acetaminophen
First-Generation NSAIDs:
(aspirin, ibuprofen (Motrin)
Inhibit COX-1 and COX-2
Used to treat inflammatory disorders (rheumatoid arthritis, osteoarthritis, bursitis)
➢ Alleviate mild to moderate pain
➢ Suppress fever
➢ Relieve dysmenorrhea
Suppress inflammation but have risk of serious harm
Aspirin
Nonselective inhibitor of cyclooxygenase
Aspirin Therapeutic uses
➢ Analgesic, antipyretic, anti-inflammatory
➢ Suppression of platelet aggregation - Protects in thrombotic disorders
➢ Dysmenorrhea
➢ Cancer prevention
➢ Prevention of Alzheimer’s disease
Aspirin Adverse effects
➢ Gastrointestinal effects (now is given enteric coated)
➢ Bleeding
➢ Renal impairment
➢ Salicylism
➢ Reye’s syndrome
➢ Pregnancy - Anemia, postpartum hemorrhage, may prolong labor
➢ Hypersensitivity reaction
Aspirin Drug interactions
➢ Anticoagulants: warfarin and heparin
➢ Glucocorticoids (increase risk of gastric ulcer)
➢ Alcohol (can cause more problems with gastric ulcers)
➢ Ibuprofen (same thing)
➢ ACE inhibitors and ARBS (lead to renal impairment)
Nonaspirin First-Generation NSAIDs
Aspirin-like drug with fewer GI, renal, and hemorrhagic effects than aspirin
20+ nonaspirin NSAIDs available (all similar, but for unknown reasons, patients tend to do better on one drug or another
Inhibit COX-1 and COX-2 – inhibition is reversible (unlike with aspirin)
Principal indications – rheumatoid arthritis and osteoarthritis
Do not protect against MI and stroke
First-Generation NSAIDs
ibuprofen (Advil, Motrin) naproxen (Naprosyn) naproxen plus lansoprazole (Prevacid) ketorolac (Toradol) Indomethacin (Indocin)
Second-Generation NSAIDs
Just as effective as traditional NSAIDs at suppressing inflammation and pain
Somewhat lower risk for GI side effects
Can impair renal function and cause hypertension and edema
Increase the risk for MI and stroke
Celecoxib (Celebrex)
Second-generation COX-2 inhibitor—fewer adverse effects than first-generation drugs
Because of cardiovascular risks, last-choice drug for long-term management of pain
Celecoxib (Celebrex) Uses
➢ Osteoarthritis ➢ Rheumatoid arthritis ➢ Acute pain ➢ Dysmenorrhea ➢ Familial adenomatous polyposis
Celecoxib (Celebrex) adverse effects
➢ Dyspepsia
➢ Abdominal pain
➢ Renal toxicity
➢ Sulfonamide allergy
➢ Cardiovascular impact (stroke, MI, and other serious events)
➢ Contraindicated in pregnancy, allergy to sulfonamides, aspirin or any NSAID
➢ Use with caution if any liver impairment
Celecoxib (Celebrex) drug interactions
➢ Warfarin
➢ May decrease diuretic effect of furosemide
➢ May decrease antihypertensive effect of ACE inhibitors
➢ May increase levels of lithium
➢ Levels of celecoxib may be increased by fluconazole
Acetaminophen (Tylenol) therapeutic use **
➢ Analgesic, antipyretic***
➢ Does not have any anti-inflammatory or antirheumatic actions
➢ Not associated with Reye’s syndrome
Acetaminophen (Tylenol) action
➢ Inhibits prostaglandin synthesis in central nervous system
Acetaminophen (Tylenol) adverse effects
➢ Very few at normal doses
➢ Hepatotoxicity- With overdose or in patients with liver failure (when combined with alcohol)
➢ Overdose – hepatic necrosis
• S/S of hepatic failure, coma, death
• Early symptoms: N/V, diarrhea, sweating, abdominal pain
Acetaminophen (Tylenol) drug interactions
➢ Alcohol
➢ Warfarin
(both cause more liver damage)
Treatment for overdose: **
acetylcysteine (Mucomyst) - loosens up secretions, can give inhalation, given orally for tylenol toxicity
Acetaminophen (Tylenol)
Most COX inhibitors – especially COX-2 inhibitors – increase
the risk for MI and stroke
AHA recommends a
stepped-care approach
Rye’s Syndrome**
occurs in childhood, 30% mortality rate; can lead to hepatic ajury and damage to the brain - encephelopathy; so don’t ever treat childhood fever w/ aspirin*
saclicylism
ringing in the ear, when aspirin levels climb above therapetuic levels, number 1 symptom is tennitus
acute poisonings of aspirin are
salicylism
what is the only injectable NSAID
ketorolac (Toradol); great for post op pts with patin and if pt is addicted to morphine
