Anti-inflamatory Drugs: NSAIDs & Acetaminophen - Ch. 75 Flashcards
What does tissue injury cause the release of?
Prostaglandins
bradykinin
histamine
leukotriennes
serotonin
What does the release of autacoids (e.g, histamine, bradykinin) cause?
Vasodilation, increased vascular permeability, chemotaxis, pain
What does NSAID stand for?
Non-Steroidal Anti-inflammatory Drugs
NSAIDs are what kind of inhibitor?
Cyclooxygenase inhibitors
What is the mechanism of action of NSAIDs?
Blocks either or both cyclooxygenase (COX) enzymes which limit the undesirable inflammatory effect of prostaglandins and related substances
What are the COX enzymes?
COX-1 and COX-2
Converts arachidonic acid into prostanoids (prostaglandins and other related compounds)
What properties do NSAIDs have?
Analgesic
Anti-inflammatory
Antipyretic
What are NSAIDs used for?
Relief of mild to moderate pain
Arthritis
Acute gout
Bone, joint, muscle pain
Dysmenorrhea
Fever
What do Non-selective NSAIDs do?
Inhibit COX-1 and COX-2, suppress inflammation but pose serious harm
What are Non-selective NSAIDs used for?
Alleviate mild to moderate pain
Inflammatory disorders (Rheumatoid arthritis, osteoarthritis, bursitis)
Examples of Non-selective NSAIDs?
Acetylsalicylic acid (ASA) - Aspirin
ketorolac (Toradol)
sodium salicylate
Ibuprofen (Motrin, Advil)
Naproxen (Aleve)
Diclofenac sodium (Voltaren)
What is the standard NSAID that others are compared to?
Acetylsalicylic acid (ASA) - Aspirin
Where is salicylic acid prepared from?
Willow bark and other plants
What plant does Aspirin come from?
Acetalation spirea
Propertoies of Aspirin?
Analgesic
Anti-inflammatory
Antipyretic
Antiplatelet
Why is ASA (Aspirin) different to other NSAIDs?
It irreversibly inhibits COX
-Other NSAIDs reversibly inhibit COX
Aspirin is the only NSAID used for what?
Antiplatelet purposes
What is treated with Aspirin for antiplatelet purposes?
MI, stroke and other thromboembolic events
What is the dose of aspirin for antiplatelet purposes?
*0-160 mg daily prophylactic
When is the use of aspirin contraindicated, or should it be used cautiously?
Pregnancy
Almost all bleeding disorders, hemophilia
Discontinue 1 week before operations
Caution in renal dysfunction
Why is aspirin use contraindicated during pregnancy?
In late trimester its use is connected to low weight, intracranial bleeds and death
ASA (Asprin) adverse effects?
-Gastrointestinal effects
-Influenza and chickenpox in kids/teens due to the possibility of Reye’s syndrome
-Renal problems
What Gastrointestinal adverse effects are associated with ASA (Aspirin)?
-Ulcerations and erosions
Dyspepsia, heartburn, epigastric distress, nausea
-GI bleeding
What symptoms are associated with Reye’s syndrome (ASA adverse effect)?
Vomiting
Liver damage
CNS problems (encephalopathy)
-Confusion, seizures, coma
What renal adverse effects are associated with ASA (Aspirin)?
Reductions in creatinine clearance (indicates kidney damage)
Acute tubular necrosis with renal failure
What NSAIDs can lead to Salicylate toxicity?
ASA, Na salicylate, Mg salicylate
Effects of Salicylate toxicity in adults?
Tinnitus and hearing loss
Effects of Salicylate toxicity in children?
Hyperventilation (CNS stimulation)
What drugs interact with ASA (aspirin)?
Anticoagulants
Glucocorticoids
Non-ASA NSAIDs
How does ASA (Aspirin) interact with anticoagulants?
Causes increased bleeding
How does Aspirin interact with Glucocorticoids?
Causes gastric ulcers
How does aspirin interact with Non-ASA NSAIDs?
Reduces antiplatelet effects of ASA
***Do not mix ASA and other NSAIDs is used for antiplatelet effects
What are non-ASA NSAIDs?
ASA-like drugs with fewer GI, renal and hemorrhagic effects than ASA
20+ non-ASA NSAIDs available
What is the emchanism of action of Non-ASA NSAIDs?
Inhibit COX-1 and COX-2 but inhibition is reversible
What are non-ASA NSAIDs unable to protect against?
MI and stroke
-No antiplatelet properties
In general, what adverse effects are associated with NSAIDs?
Gastrointestinal ulceration
Blockade of platelet aggregation -bleeding problems
Inhibition of prostaglandin-mediated renal function
Hypersensitivity reactions
In general, when is NSAID use contraindicated?
Conditions with bleeding as a risk
e.g, Vitamin K deficiency, peptic ulcer disease
Severe renal or hepatic disease
Breastfeeding
What is COX-2 responsible for?
Inflammatory mediators
Examples of selective COX-2 inhibitor NSAIDs?
Celecoxib (Celebrex)
Rofecoxib (Vioxx) -Withdrawn in 2004
Selective COX-2 inhibitors are just as effective as traditional NSAIDs in supressing what?
Inflammation and pain
Selective COX-2 inhibiots might lower the risk for what?
GI adverse effects but not really
What can selctive COX-2 inhibitors impair?
Renal function and cause hypertension and edema
Selective COX-2 inhibitors increase the risk for what?
MI and stroke
How is NSAID GI ulceration reduced?
Mistoprostol (Cytotec)
What is Mistoprostol?
SYnthetic prostaglandin
Used in combination with NSAIDs to reduce ulceration
What does Antipyretic mean?
Reduces fever
How do NSAIDs produce antipyretic effects?
Inhibit prostaglandin E2 production within the area of the brain that controls temperature
Before begining NSAID therapy the nurse should?
Assess for conditions that may be contraindications to therapy, especially:
-GI lesions or peptic ulcers
-Bleeding disorders
The client should notify or watch for if what occurs when using NSAIDs?
GI pain or evidence of GI bleeding
Occurance of any unusual bleeding such as in stool
What does bleeding in stool look like?
Dark or black colour, tarry
Enteric-coated NSAID tablets should not be _________ or ________?
Crushed or chewed
Salicylates are not given to children under which age and why?
Age 12
-Reye’s syndrome
What are the properties of Acetaminophen (Tylenol)
Analgesic
Antipyretic
What properties do NSAIDs have that acetaminophen doesn’t?
Anti-inflammatory
Anti-platelet
Acetaminophen is an alternative to what?
NSAIDs
What is the mechanism of action of Acetaminophen (Tylenol)?
Inhibits COX that is only present in CNS
What kind of sites of action does Acetaminophen NOT have?
Peripheral therapeutic sites
What is absent with acetaminophen use?
Adverse effects associated with NSAIDs like GI ulceration and excessive bleeds
How does Acetaminophen produce antipyretic effects?
Same as NSAIDS
-Inhibits prostaglandin E2 production within the area of the brain that controls temperature
What is the maximum amount an adult can take of acetaminophen per day?
4000mg
What is the maximum amount of acetaminophen that children ages 11-12 can take per day?
2400mg
-Is a sliding scale bc its Based on age and weight
Who should take extreme caution when taking acetaminophen?
Alcohol abusers
Single-ingredient acetaminophen tabs are provided. In what doses are they provided?
325mg, 500mg and 650mg
Single-ingredient acetaminophen tabs reach what very quickly?
Maximum
Tylenol 1,2,3 or 4 in combination with codeine is supplied in what doses?
Codeine 8.15, 30, 60mg
Acetaminophen 300mg
When is acetaminophen use contraindicated?
Severe hepatic disease
Severe renal disease
Alcoholism
Drug allergy
What does acetaminophen toxicity overdose cause?
Hepatic necrosis (drug-induced hepatitis)
Long-term ingestion of large doses also causes nephropathy
What is the reccomended antidote for Acetaminophen overdose?
Acetylcysteine (Mucomyst)
How does Acetylcysteine (Mucomyst) work?
Protects the liver from acetaminophen-induced damage
When is the max protection of Acetylcysteine (Mucomyst)?
within 8-10 hours (IV or PO)
When can Acetylcysteine (Mucomyst) be given?
Anytime, even in late presentation at 24hours
Dangerous interactions of acetaminophen may occur if taken with what?
Alcohol
Acetaminophen should not be taken in the presence of?
Liver dysfunction, chronic alcoholism
Possible liver failure or sever renal disease
When taking other hepatotoxic drugs
