NSAIDs Flashcards
What catalyzes the synthesis of prostaglandins from arachidonic acid?
Cyclooxygenase (COX)
Where is COX-1 located? (3)
Gastric mucosa
Platelets
Renal parenchyma
What is COX-1 responsible for? (3)
GI mucosal integrity
Platelet aggregation
Renal function
What are 3 attributes of COX-2?
Pain-inducing enzyme
Mediates inflammation, pain, fever, and carcinogenesis
Released in response to injury, illness, diet
What is the mechanism of action of NSAIDs?
What is important to understand regarding NSAIDs activity? (2)
Inhibition of Cyclooxygenase
NSAIDs block both COX enzymes without specificity
CEILING EFFECT–Exceeding the recommended dose only increases the risk of toxicity
Describe the pharmokinetics of NSAIDs: (4)
Well absorbed in GI
Not a lot of 1st pass metabolism (makes PO similar to IV dose)
Highly protein bound
Elimination: ASP lost within hour, but duration for 24 hours.
What are the advantages of NSAIDs? (10)
Decrease activation of peripheral nociceptors
Absence of dependence or addiction
Synergistic with opioids
Preemptive analgesia
NO depression of ventilation
Less N/V
Long duration of action
Less variability
No pupil changes
Absence of cognitive effects
What are the disadvantages of NSAIDs? (7)
Gastric ulceration
Renal dysfunction
Hepatocellular injury
Asthma exacerbation
Allergic reactions
Bone healing
Drug Interactions
Why are NSAIDs contraindicated for asthma pts?
When prostaglandins are blocked, can bronchoconstrict enhancing effects of asthma.
What are GI related adverse effects? (5)
Dyspepsia, N/V, pain, peptic ulcer, GI hemorrhage
What NSAIDs are nonspecific? (5)
inhibit both COX-1 and -2
Ibuprofen (Motrin)
Naproxen (Aleve)
Aspirin (Acetylsalicylic Acid)
Acetaminophen (Tylenol)
Ketorolac (Toradol)
When do you discontinue NSAIDs prior to surgery?
7-10 days
Note: Platelet life is 7-10 days.
What are attributes of ASA (acetylsalicylic acid)? (2)
Irreversible acetylation of COX enzyme
Rapid GI absorption
What condition is ASA a first line DOC?
Fever
How low of a dose can is anti-platelet function observed?
40mg
What are the clinical uses of ASA?
Analgesic
Antipyretic
Antiplatelet function
What are the side effects of ASA?
GI upset
Prolonged bleeding time
Prolonged Prothrombin Time (PT)
Aspirin Induced Asthma
What are other concerns of ASA? (5)
CNS Toxicity
SAFE for renal pts
Allergic rxn is rare
Prolonged labor, increased hemorrhage
REYE’S SYNDROME–potentially fatal disease affecting the brain as well as other organs
What may we want to give instead of ASA/ASP during pollen season?
Tylenol
What is a safe alternative to aspirin for pediatric patients and those with peptic ulcers?
Acetominophen
What is the maximum dose of IV acetominophen?
1000mg q 6 hrs
max 4g q 24 hrs
What type of pain is acetaminophen good for? (2)
Mgmt of mild to moderate pain
Mgmt of severe pain with opioids
What is a major adverse side effect of acetaminophen?
Hepatic Toxicity
How does acetaminophen contrast to ASA?
No gastric irritation
No platelet aggregation effects
