Chapter 44: Anti-inflammatory and antigout drugs Flashcards
salicylates
aspirin
diflunisal (Dolobid)
salsalate (Salistab)
choline salicylate (Arthropan)
Acetic Acid Derivatives
diclofenac sodium (Voltaren) indomethacin (Indocin) sulindac (Clinoril) tolmetin (Tolectin) etodolac (Lodine) ketorolac (Toradol) meclofenamate (generic only) mefenamic acid (Ponstel)
Cyclooxygenase-2 Inhibitors
celecoxib (Celebrex)
Enolic Acid Derivatives
nabumetone (Relafen)
meloxicam (Mobic)
piroxicam (Feldene)
Propionic Acid Derivatives
fenoprofen (Nalfon) flurbiprofen (Ansaid) ibuprofen (Motrin, Advil, others) ketoprofen (Orudis KT) naproxen (Naprosyn, Aleve) oxaprozin (Daypro)
NSAIDs: FDA-APPROVED
INDICATIONS
- Acute gout
- Acute gouty arthritis
- Ankylosing spondylitis
- Bursitis
- Fever
- Juvenile rheumatoid arthritis
- Mild to moderate pain
- Osteoarthritis
- Primary dysmenorrhea
- Rheumatoid arthritis
- Tendinitis
- Various ophthalmic uses
NSAIDs relieve pain, headache, and inflammation by
blocking
the chemical activity of the enzyme called cyclooxygenase
(COX).
This greater enzyme specificity of the COX-2
inhibitors allows for the
beneficial antiinflammatory effects
while reducing the prevalence of adverse effects associated with
the nonspecific NSAIDs, such as gastrointestinal ulceration
The leukotriene pathway is
inhibited by some antiinflammatory
drugs, but not by salicylates.
All NSAIDs can be…
ulcerogenic and induce gastrointestinal
bleeding due to their activity against tissue COX-1.
Aspirin has the unique property
irreversible inhibitor of COX-1
receptors within the platelets themselves…
reduced formation of thromboxane A2, a substance that normally
promotes platelet aggregation
NSAIDs
are sometimes combined with an opioid
They tend to have an opioid-sparing effect when given together
with opioids, because the drugs attack pain using two different
mechanisms. This often allows less opioids to be used
NSAIDs show a ceiling effect
limits their effectiveness;
that is, any further increase in the dosage beyond a certain
level increases the risk for adverse effects without a corresponding
increase in the therapeutic effect
Contraindications to NSAIDs
Contraindications to NSAIDs include known drug allergy and
conditions that place the patient at risk for bleeding, such as rhinitis
(risk for epistaxis [nosebleed]), vitamin K deficiency, and
peptic ulcer disease. Patients with documented aspirin allergy
must not receive NSAIDs.
adverse effects of the NSAIDs is their effect
on the gastrointestinal tract
Symptoms can range from mild
symptoms such as heartburn to the most severe gastrointestinal
complication, gastrointestinal bleeding. Most fatalities associated
with NSAID use are related to gastrointestinal bleeding.