Anti Inflammatory Drugs: NSAIDS & Acetaminophen (75) Flashcards
Tissue injury causes the relapse of (5)
-prostaglandins
-bradykinin
-histamine
-leukotriennes
-serotonin
Most importantly tissue injury causes release of…
Prostaglandins
What are signs of inflammation
-vasodilation
-increased vascular permeability
-chemotaxis
-pain
A stimulus like damage causes release of phospholipase A2 which interacts with ____ to create ___
Interacts with PHODPHOLIPIDS to create ARACHIDONIC ACID
ARACHIDONIC acid is metabolized by _____ to create PGH2 or different variations
Cyclooxygenase
What are the two versions of cyclooxygenase
COX-1 and COX-2
PG stands for
Prostaglandin
What does COX-1 do
Physiological functions
-GI, renal, platelet function, blood vessels
What does COX-2 do
Inflammation
Which of the COX is inhibition undesirable?
COX-1 since it is related to regular physiological functions
NSAIDS stands for
Non steroidal anti inflammation drugs
Where do NSAIDS work in the action of creating prostaglandins?
NSAIDS stop the metabolism of ARACHIDONIC acid, by competition inhibition of COX
Is the inhibition of COX reversible or permanent?
Reversible
NSAIDS can block
Either one or both COX
What are the properties of NSAIDS groups
-analgesic
-anti inflammatory
-antipyretic
Indications of NSAIDs
-relief of mild to moderate pain
-fever
-gout, RA, osteoarthritis
Non selective NSAIDs target
Inhibitbition of both COX 1 and 2
Non selective NSAIDs are used for
-alleviating mild to moderate pain
-inflammatory disorders
The downside of non selective NSAIDs are
That they suppress inflammation but pose risks of serious harm
Examples of non selective NSAIDs
-acetylsalicylic acid (ASA or ASPRIN)
-ibuprofen (Advil)
-naproxen (Aleve)
NSAIDs can be used in
Combination
-codeine, caffeine
Acetylsalicylic acid is the
Standard NSAID agains which all others are compared
Acetylsalicylic acid is created from
Salicylic acid- Willow bark, and other plants ‘
Acetyl- added on in that era to create a drug
Where does the name ASPRIN come from
Acetalation spiraea
Acetylsalicylic acid properties
-anti inflammatory
-analgesic
-antipyretic
-antiplatelet
Antiplatelet properties of Acetylsalicylic acid
A special property of Acetylsalicylic acid
-COX will be inhibited for the life time of the platelet (eight days)
Positives of Acetylsalicylic acid being an antiplatelet
Heart attack
-prolonged use can reduce the risk of heart attack
Acetylsalicylic acid is different to other NSAIDs because it
Irreversibly inhibits COX
Daily dose for prophylactic use of Acetylsalicylic acid
80 to 160mg
Contraindications and cautions Acetylsalicylic acid
-pregnancy
-bleeding disorders
-operations
-renal dysfunction
-gastrointestinal
Contraindications and cautions Acetylsalicylic acid: pregnancy
In late trimester connected with low weight, intracranial bleed, and even death
Contraindications and cautions Acetylsalicylic acid: bleeding disorders
Hemophilia, as it is an ntiplatelet
Contraindications and cautions Acetylsalicylic acid: operations
Discontinue one week before operations (antiplatelet)
Contraindications and cautions Acetylsalicylic acid: renal
Renal dysfunction
-relies on PG in kidney dysfunction
-can exacerbate function
Contraindications and cautions Acetylsalicylic acid: gastrointestinal
Increases ulcerations and bleeding
How does Acetylsalicylic acid cause bleeding and ulcers
-increases acidity in stomach
-deeper ulcer causes bleeding
-can vomit up coffee grounds or have dark stool
Why does someone develop ulcers on Acetylsalicylic acid
The stomach has ow pH but intact stomach wall
-this is due to PGE2 and PGI2 which increase protective mucus and dilate blood to increase cell health
-the loss of PG in the Acetylsalicylic acid properties will get rid of this stomach wall health
AE of Acetylsalicylic acid
-Reyes syndrome
-renal
Reye’s syndrome
Viral infections, being young, and taking Acetylsalicylic acid can increase risk of Reye’s syndrome
-which causes vomiting, liver damage, CNS encephalopathy
AE of Acetylsalicylic acid: renal
Reduction in creatinine clearance
AE of Acetylsalicylic acid: renal
Reduction in creatinine clearance
Salicylate toxicity
Use of several NSAIDs
-adults: tinnitus, hearing loss
-children: hyperventilation
Acetylsalicylic acid is not given too
Children generally
Interactions with Acetylsalicylic acid
-anticoagulants increase bleeding
-glucocorticoids increase gastric ulcers
-non ASA NSAIDs can reduce antiplatelet effects
Important not to mix NSAIDs if Acetylsalicylic acid is being used for
Antiplatelet effect
Non Acetylsalicylic acid NSAIDs have fewer
-fewer GI, renal, hemorrhagic effects
-many different types
Non ASA NSAIDs inhibit COX 1 and 2, is it reversible or permanent
Reversible unlike ASA
Non ASA NSAIDs do not
Protect against MI and stroke
Selective NSAIDs are able to target just one COX, which one is that
COX 2, which is good because this will stop inflammation and hopefully not affect the physiological functions with COX 1 inhibition
What was the purpose of creating selective NSAIDs
Hoping to solve GI problems associated with non selective NSAIDs
COX 2 inhibitors example
Celecoxib
Selective NSAIDs are just as effective as
Traditional NSAIDS in suppressing inflammation and pain
Selective NSAIDs have a lower risk of
GI adverse effects
-but would be better to just not take the drug in general
Selective NSAIDs can impair
Renal function and cause hypertension and edema
Selective NSAIDs can increase the risk of
MI and stroke
How can someone reduce GI ulceration when using NSAIDs
Misoprostol
How are NSAIDs antipyretic
Inhibit prostaglandin E2 production within the area of the brain that control temperature
Before beginning NSAID therapy, nurses should assess for
-GI lesions or peptic ulcer disease
-bleeding disorders
—> especially long term
Clients taking NSAIDs long term, for the occurrence of
Any unusual bleeding
-dark or black, color, tarry stool
Enteric coated tablets should not
Be crushed or chewed
Salicylates are NOT to be given to
Children under age 12
Non opioid analgesics
Acetaminophen
Acetaminophen
Analgesic and antipyretic
-but is NOT an anti inflammatory
-no antiplatelet
Mechanism and action of acetaminophen
We dont really know
acetaminophen inhibits
COX
-but only in the CNS
acetaminophen has no
-peripheral therapeutic sites of action
-no AE associated with NSAIDs like GI ulceration or excessive bleeding
Maximum dosage of acetaminophen per day for an adult
4000 mg
Maximum acetaminophen for 11 to 12 year olds
2400
acetaminophen should be used in extreme caution in
Alcohol absorbers
Single tablet amount of acetaminophen
325, 500, 650mg
Tylenol combinations with codeine
All have 300mg of acetaminophen
Contraindications of acetaminophen
-severe hepatic disease
-renal disease
-alcoholism
-drug allergy
Toxicity of acetaminophen
OTC prescription which can risk overdose both intentionally or unintentional use
Overdose is usually due to
Hepatic necrosis
-drug induced hepatitis
Long term ingestion of large doses also causes
Nephropathy
acetaminophen should not be used with other drugs containing
acetaminophen
-easy to overdose since many drugs need/contain acetaminophen
What other warning is found on acetaminophen bottles
Liver warning- severe or possibly fatal liver damage if
-taking more than recommend dose
-other drugs with acetaminophen
-while drinking thee or more alcoholic drinks every day
Symptoms of liver damage may include
-yellowing of skin, eyes, dark urine
-sweating, nausea, vomiting, stomach pain
-unusual tiredness, loss of appetite
How is acetaminophen metabolized normally
acetaminophen had a major pathway which creates non toxic metabolites
How is acetaminophen metabolized when taken with alcohol
when taking alcohol with acetaminophen, it creates toxic metabolites that are broken down by glutathione creating a non toxic metabolite
How are toxic metabolites turned into nontoxic metabolites
Glutathione
What do toxic metabolites do
-alter proteins
-damage DNA
-death of cells
Glutathione is depleted by
Alcohol and acetaminophen overdose
What can be done when someone is overdosing on acetaminophen
Take acetylcysteine to increase amounts of glutathione
Acetylcysteine must be taken in what amount of time
8 to 10 hours
Dangerous interactions may occur if acetaminophen is taken with
Alcohol
Acetaminophen should not be take in the prescience of
-liver dysfunction, chronic Alcoa is
-possible liver failure or severe renal disease
-taking other hepatotoxic drugs
