NSAIDs (Shelby 🐈) Flashcards
Name! That! NSAID!
Relatively short acting
Decreases arachidonic acid bioavailability
Diclofenac (Voltaren)
Name! That! NSAID!
Potent, worst side effect profile
Indomethacin (Indocin)
a very small portion of acetaminophen is metabolized this way:
A small portion is metabolized by the P450 system creating a free radical which is normally conjugated with glutathione and excreted
How long can a patient be on Ketorolac (Toradol)
5 days
How is Piroxican (Feldene), Meloxicam (Mobic) a better option NSAID for patients with hepatic disease
Decreases oxygen radical production
Effects of acetaminophen in the body
normal doses NOT overdose
CNS effects only
no GI problems, no kidney adverse effects, no inhibition of blood clotting like NSAIDs
What is the main effect of Specific inhibitors of COX-2 enzymes
Inhibition of the production of prostacyclin by endothelial cells
Name! That! NSAID!
Very potent and very long acting - single daily dosing is possible
Naproxen (Naprosyn)
acetaminophen is MOSTLY metabolized this way:
glucoronidated in the liver and excreted by the kidney
What is Ketorolac (Toradol) used for
postsurgical pain
Can be combined with opioids to reduce side effects from opioids (constipation)
DOC for small children with fever
acetaminophen
What does acetaminophen do?
What does it NOT do?
Very good analgesic and antipyretic agent
Not an NSAID- does not have an anti-inflammatory effect
Name! That! NSAID!
Not in the US, very potent and effective
Phenylbutazone
Why do Specific inhibitors of COX-2 enzymes have less GI side effects than aspirin
Reduced effect on GI because they are not inhibiting COX-1, which produces the GI protecting prostaglandins
Name! That! NSAID!
Can be combined with opioids to reduce side effects from opioids (constipation)
Ketorolac (Toradol)
Patient has active PUD, what can you give them?
**********
acetaminophen and/or opioids only
NO NSAIDs
Name! That! NSAID!
Decreases oxygen radical production, better for patients with hepatotoxicity
Piroxican (Feldene), Meloxicam (Mobic)
Name! That! NSAID!
First choice drug, lowest incidence of side effects
Ibuprofen (Motrin)
Diclofenac (Voltaren) is often combined with _______ to decrease GI side effects
misoprostol (Arthrotec)
Benefit of Celecoxib (Celebrex)
Downside of Celecoxib (Celebrex)
Benefit: Less effect on GI (less cox-1 inhibition)
Downside: increased risk of cardiovascular disease (imbalance of prostacyclin and thromboxane)
What happens if glutathione is exhausted in regards to acetaminophen excretion
the free radicals will cause severe liver necrosis
Name! That! NSAID!
Extensively bound to plasma proteins, displacement causes adverse drug reactions with bound drugs (warfarin, anti-diabetics, etc)
Naproxen (Naprosyn)
Name! That! NSAID!
Prodrug, long half life
Nabumetone (Felafen)
acetaminophen overdose antidote:
N-acetylcysteine (Mucomyst)
Why should patients that are chronic alcoholics NOT take acetaminophen
If there is an increased production of the metabolite as in chronic alcoholism, which induces the P450 system, this also leads to severe liver damage
acetaminophen overdose causes:
fatal hepatic necrosis
How does Indomethacin (Indocin) reduce inflammation in addition to being a cox blocker
Reduces PMN migration – additional anti-inflammatory effect
Inhibits phospholipase A – decreases synthesis of prostaglandins from arachidonic acid
Patient has history of PUD, but it is not currently active. What can you give them
***************
Celecoxib with or without antacids or some NSAIDs with Misoprostol or “-prazols”
What is the only Specific inhibitor of COX-2 enzymes that is available in the US
Celecoxib (Celebrex)
What is the major side effect caused by the imbalance between thromboxane and prostacyclin with Specific inhibitors of COX-2 enzymes
Excess Thromboxane in the absence of prostacyclin promotes the development of cardiovascular problems
Name! That! NSAID!
The reversible binding inhibits the irreversible binding of aspirin – decreases effects on platelet aggregation, should not be combined
Ibuprofen (Motrin)
No history of PUD
What can you give them
***************
any NSAID
A 78 year old man is taking daily aspirin for stroke prevention. One day he decides to go to Tijuana to see a donkey show. He has a few margaritas while he is down there and tries to wave down a prostitute on the street at the end of the night. He ends up waving down an undercover Mexican cop and is arrested for the solicitation of a prostitute. The cop suddenly gets the urge that he has to IMMEDIATELY diarrhea from the tacos he hate for dinner. He leaves the man in his unlocked cop car so the old man decides to make a run for it. He leaps across the border and sprains his ankle. He limps into an urgent care and the NP decides not to ask any questions but just give him some Ibuprofen and tell him to get a life. What is going to happen?
- The ibuprofen is going to INHIBIT the aspirins effect on platelets, and he is going to have a stroke
- He is going to have an STI
- He is going to get extradited to Mexico to serve time in a Mexican prison, where he will likely get more STIs
Name! That! NSAID!
Cannot be used longer than 5 days due to GI side effects
Ketorolac (Toradol)
Name! That! NSAID!
Long half life
Inhibits PMN migration
and
Lymphocyte function
Piroxican (Feldene), Meloxicam (Mobic)
Name! That! NSAID!
Potent – can be used for postsurgical pain
Ketorolac (Toradol)
Name! That! NSAID!
Reduces PMN migration
and
Inhibits phospholipase A
Indomethacin (Indocin)
Why do you not combine Ibuprofen (Motrin) and Aspirin
The reversible binding of Ibuprofen inhibits the irreversible binding of aspirin – decreases effects on platelet aggregation, should not be combined
What is the problem with Specific inhibitors of COX-2 enzymes
Creates and imbalance between thromboxane and prostacyclin
Excess Thromboxane in the absence of prostacyclin promotes the development of cardiovascular problems
Name! That! NSAID!
Used for patent ductus arteriosus
Indomethacin (Indocin)
