Chapter 44: Anti-inflammatory and antigout drugs Flashcards
(39 cards)
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.
black box warning per wilkipedia
It is the strongest warning that the FDA requires, and signifies that medical studies indicate that the drug carries a significant risk of serious or even life-threatening adverse effects
The drug
misoprostol (Cytotec)
has proved successful
in preventing the gastric ulcers and hence gastrointestinal
bleeding that can occur in patients receiving NSAIDs. Misoprostol
is a synthetic prostaglandin E1 analogue that inhibits
gastric acid secretion and also has a cytoprotective component
NSAIDs can compromise existing renal function
Renal toxicity
can occur in patients who are dehydrated, those with heart failure
or liver dysfunction, and those taking diuretics or angiotensin-
converting enzyme inhibitors.
NSAIDs: ADVERSE EFFECTS
Cardiovascular
Moderate to severe noncardiogenic pulmonary edema
Gastrointestinal Dyspepsia, heartburn, epigastric distress, nausea, vomiting, anorexia, abdominal pain, gastrointestinal bleeding, mucosal lesions (erosions or ulcerations)
Hematologic Altered hemostasis through effects on platelet function
Hepatic Acute reversible hepatotoxicity
Renal Reduction in creatinine clearance, acute tubular
necrosis with renal failure
Other Skin eruption, sensitivity reactions, tinnitus, hearing
loss
salicylism
Salicylate toxicity, usually from aspirin
Chronic salicylate intoxication is also
known as salicylism and results from either short-term administration
of high dosages or prolonged therapy with high or even
lower dosages
ACUTE OR CHRONIC
SALICYLATE INTOXICATION:
SIGNS AND SYMPTOMS
Cardiovascular Increased heart rate
Central nervous Tinnitus, hearing loss, dimness of vision, headache,
dizziness, mental confusion, lassitude,
drowsiness
Gastrointestinal Nausea, vomiting, diarrhea
Metabolic Sweating, thirst, hyperventilation, hypoglycemia
or hyperglycemia
The most common manifestations of chronic salicylate
intoxication in adults
tinnitus and hearing loss.
children are hyperventilation and central nervous system
(CNS) effects such as dizziness, drowsiness, and behavioral
changes.
- Little or no toxicity: less than 150 mg/kg
- Mild to moderate toxicity: 150 to 300 mg/kg
- Severe toxicity: 300 to 500 mg/kg
- Life-threatening toxicity: over 500 mg/kg
A serum salicylate concentration measured 6 hours or
longer after the ingestion may be used in conjunction with the
Done nomogram to estimate the severity of intoxication and
help guide treatment
NSAID-induced
hyperkalemia or hyponatremia can also occur.
pg 711 ?