Pharm 22 Objectives Flashcards
What are eicosanoids?
signaling molecules made up of 20-carbon fatty acids found in the cell membrane
How are eicosanoids produced?
Inflammation causes arachidonic acid to create eicosanoids
What are the three main types of eicosanoids?
Prostaglandins (COX)
Thromboxane (COX)
Leukotrienes (Lipoxygenase)
What are the steps inhibited by NSAIDs?
Drugs such as NSAIDs block the synthesis of prostaglandins and COX
Role of eicosanoids in: smooth muscle function
stimulates uterine contractions
and
Increases GI motility
Role of eicosanoids in: platelet function
Maintains bicarbonate gel layer lining of GI mucosa
Role of eicosanoids in: renal function
increase sodium and water excretion
Role of eicosanoids in: inflammation, pain, and fever
Actives specific prostanoid receptors in target tissue
released by physical trauma or chemical stimuli
promote tissue inflammation
affect smooth muscle and platelet aggregation
target tissues vary by PG, some PBs bind to sites better than others
Role of COX-2
mediate pain, fever, and inflammation
What is the main target of NSAIDs
COX-2
Role of COX-1
Support and protects GI mucosa
Increases mucosal blood flow, production of mucus, and bicarbonate
Stimulates epithelial cells that line GI tract
COX-1 catalyzes thromboxane A2 in platelets which results in
a trigger for platelet aggregation
Advantages of selective COX-2 inhibitors?
Less GI distress
Less incidence of GI Bleed
Clinical utilization of COX-2 selective NSAIDS
Osteoarthritis (100-200mg daily/100mg BID)
Rheumatoid arthritis (100-200mg BID)
Dysmenorrhea (400mg x 1/200mg BID)
Acute Pain (400mg x1/200mg BID)
Disadvantages of selective COX-2 inhibitors?
Cost
Increase risk for cardiac events
Prescription is needed
Advantages for nonselective COX inhibitors
minimal downiness
Anti-inflammatory action
No risk of abuse or diversion
OTC choices are available
Disadvantages for nonselective COX inhibitors
Only best for mild to moderate pain
Anti-inflammatory action is delayed about 3-5 days
GI tox and renal effects
Analgesic dose of aspirin?
300 - 600 mg q6 hrs