Lehne Chapter 71

Question 1

Cyclooxygenase Inhibitors

Answer 1

Uses​

Suppress inflammation​

Relieve pain​

Reduce fever​

Adverse effects​

Gastric ulceration​

Bleeding​

Renal impairment
Mechanism of action​

Inhibit cyclooxygenase (COX), the enzyme that converts arachidonic acid into prostanoids (prostaglandins and related compounds)​

Inhibition of COX-1 (“good COX”)​

Gastric ulceration​

Bleeding​

Renal impairment

Question 2

Inhibition of COX-1: Beneficial effects

Answer 2

Protection against myocardial infarction (MI) and stroke

Question 3

Inhibition of COX-2 (“bad COX”): Largely beneficial effects:

Answer 3

Suppression of inflammation​

Alleviation of pain and reduction of fever​

Protection against colorectal cancer

Question 4

Classification of ​

Cyclooxygenase Inhibitors

Answer 4

Drugs with antiinflammatory properties​

Nonsteroidal antiinflammatory drugs (NSAIDs) ​

Aspirin, celecoxib, ibuprofen, and naproxen ​

Drugs without antiinflammatory properties​

Acetaminophen

Question 5

First-Generation NSAIDs

Answer 5

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 pose risk of serious harm

Question 6

Aspirin

Answer 6

Nonselective inhibitor of cyclooxygenase​

Therapeutic uses​

Analgesic, antipyretic, antiinflammatory​

Suppression of platelet aggregation​

Protects in thrombotic disorders​

Dysmenorrhea​

Cancer prevention​

Prevention of Alzheimer’s disease
Adverse effects​

Gastrointestinal (GI) effects​

Bleeding​

Renal impairment​

Salicylism: Tinnitus (ringing in the ears), sweating, headache, and dizziness​

Reye’s syndrome​

Pregnancy​

Anemia, postpartum hemorrhage; may prolong labor​

Hypersensitivity reaction
Drug interactions​

Anticoagulants: Warfarin and heparin​

Glucocorticoids​

Alcohol​

Ibuprofen​

ACE inhibitors and ARBs​

Acute poisoning​

Immediate threats to life: Respiratory depression, hyperthermia, dehydration, and acidosis. Treatment is largely supportive.

Question 7

Nonaspirin First-Generation NSAIDs

Answer 7

Aspirin-like drugs 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

Question 8

Ibuprofen [Advil, Motrin]

Answer 8

Inhibits cyclooxygenase and has antiinflammatory, analgesic, and antipyretic actions ​

Indications: Fever, mild to moderate pain, arthritis​

Generally well tolerated​

Low incidence of adverse effects ​

SAFETY ALERT: All first-generation NSAIDs are associated with an increased risk of GI bleeding that can lead to hospitalization or death

Question 9

Second-Generation NSAIDs

Answer 9

Just as effective as traditional NSAIDs in suppressing inflammation and pain​

Somewhat lower risk for GI side effects​

Can impair renal function and cause hypertension and edema​

Increased risk of MI and stroke

Question 10

Celecoxib [Celebrex]

Answer 10

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​

Uses ​

Osteoarthritis​

Rheumatoid arthritis​

Acute pain​

Dysmenorrhea​

Familial adenomatous polyposis
Adverse effects​

Dyspepsia​

Abdominal pain​

Renal impairment​

Sulfonamide allergy​

Cardiovascular impact (stroke, MI, and other serious events)​

Use in pregnancy
Drug interactions​

Warfarin​

May decrease diuretic effect of furosemide​

May decrease antihypertensive effect of ACE inhibitors​

May increase levels of lithium​

Celecoxib levels may be increased by fluconazole

Question 11

Acetaminophen [Tylenol]

Answer 11

Therapeutic uses​

Analgesic, antipyretic​

Does not have any antiinflammatory or antirheumatic actions​

Not associated with Reye’s syndrome​

Action​

Inhibits prostaglandin synthesis in central nervous system
Adverse effects​

Very few at normal doses​

Stevens-Johnson syndrome (SJS), acute generalized exanthematous pustulosis (AGEP), and toxic epidermal necrolysis (TEN)​

Hepatotoxicity​

With overdose or in patients with liver failure​

Overdose: Hepatic necrosis​

Signs and symptoms of hepatic failure, coma, death​

Early symptoms: Nausea and vomiting, diarrhea, sweating, abdominal pain​

Treatment for overdose: Acetylcysteine (Mucomyst)
Drug interactions​

Alcohol​

Warfarin​

Vaccines

Question 12

AHA Statement on COX Inhibitors

Answer 12

Most COX inhibitors, especially COX-2 inhibitors, increase the risk for MI and stroke​

American Heart Association (AHA) recommends a stepped-care approach