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87 Cards in this Set

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What are the three chemical families of opiods?
phenanthrenes
phenylheptylamines/diphenylheptanes
phenlpiperadines
they all start with phen-
How does acetominophen work?
inhibits synthesis of prostaglandins in the CNS and peripherally blocks pain impulse generation

- also inhibits hypothalamic heat regulating center
Acetaminophen needs to be separated from what drug by 2 hours because it will decrease its absorption?
cholestyramine
its a cholesterol med
What can happen with chronic overuse of acetaminophen? What can happen with acetaminophen use and chronic alcohol consumption? What can occur w/doses >4g?
Nephrotoxicity (b/c PGs are dilatory in kidneys)

Hepatotoxicity (>3 drinks/day or >4g tylenol)
Nephrotoxicity is more common with APAP or NSAIDS?
NSAIDS
Which non opiod pain reliever should be used w/caution in pts with G6PD deficiency?
APAP
What is the plateau effect and how does it relate to tylenol?
anything >1000 mg is useless
What is phenylbutazone?
NSAID developed due to dyspepsia associated with ASA (first NSAIDS) - not used anymore b/c bone marrow toxicity
prototypical NSAID
What replaced phenylbutazone historically (because phenylbutazone was toxic to bone marrow)?
Indomethacin
What was the prototypical NSAID
phenylbutazone
What are the nonselective NSAID families?
Carboxylic acids
Enolic acids
Proprionic acids
Acetic Acid Derivatives
Fenamates
Napthylkanones
Which NSAIDS are in the family of carboxylic acids?
Aspirin
Choline magnesium trisalicylate
Salsalate
Diflunisal
Which family of nonselective NSAIDS is usually initial and second line therapies for mild-moderate pain?
Proprionic acids (ibuprofen, naproxen)
Which NSAIDS are enolic acids?
Piroxicam
Meloxicam
Why aren't Piroxicam and Meloxicam often first line?
$$$
Which NSAIDS are proprionic acids?
Ibuprofen
Naproxen
Ketorolac
Fenoprofen
Ketoprofen
Flurbiprofen
Oxaprozin
What is the only IV NSAID available?
Ketorolac (Toradol)
Which NSAIDS are Acetic Acid Derivatives?
Indomethacin
Diclofenac

Tometin
Sulindac
Diclofenac/Misoprostol
Etodolac
What are Indomethacin and Diclofenac good for? What is the problem with these two drugs?
Good for serious musculoskeletal/joint problems

but. .. a lot of SEs
What NSAID is a Fenamate? Napthylkanone?
Meclofenamate (fenamate)
Nabumetone (napthylkanone)
Only one in each family
Which NSAIDS have the longest half life?
Piroxicam (enolic acid)
Nabumetone (napthylkanone)
Oxaprozin (proprionic acid)
Which COX enzyme is only expressed during times of inflammation?
COX-2
Ibuprofen is a strong inhibitor of ___________
2C9
may turn off metabolism of warfarin
What NSAID besides ibuprofen is a strong inhibitor of 2C9?
piroxicam
Which enolic acid and proprionic acid have a weaker cytochrome interaction than ibuprofen and piroxicam?
Naproxen and Meloxicam
ibuprofen and piroxicam are strong inhibitors of 2C9
NSAIDS do what to lithium?
increase it

(kidney sense lithium and Na the same and NSAIDS lead to Na retention. . . lithium retention too)
Are intermittent NSAIDS a big problem with lithium?
no, chronic use will inc lithium levels
how do NSAIDS affect diuretics?
they decrease the efficacy of thiazides and loops (and ACEs/ARBs)
Name 3 factors that inc risk of GI bleed w/NSAIDS.
ETOH
steroids
antiplatelet agents
Why should you use caution when prescribing an NSAID in a patient with renal insufficiency?
they need the vasodilatory effect of PG (don't use if high creat!)
What are two contraindications to NSAID use?
1. Pg! (3rd trimester)
2. Recent CABG (DMR)
Which nonselective NSAIDS are safer in terms of GI effects (like gastritis, ulceration)
Nonacetylated salicylates

Indomethacin > naproxen > ibuprofen > meloxicam
Which NSAIDS are "ok" for pts with asthma and ASA sensitvity?
choline magnesium trisalicylate or celecoxib
Name adverse reactions of nonselective NSAIDS.
1. precipitation of asthma and anaphylactoid rxn in ASA-sensitive pt
2. inc BT (reversible platelet dysfunction)
3. hepatotoxicity
4. nephrotoxicity
5. AIN
6. ATN
Which NSAID is most associated with nephrotoxicity?
ketorolac
Which NSAID should you only use up to 5 days because of a certain toxicity?
ketorolac (toradol) - nephrotoxicity
What is misoprostol?
a prostaglandin analog used to minimize GI side effects of NSAIDS
What is Arthrotec?
diclofenac + misoprostol
When is misoprostol contraindicated?
pregnancy
What med is FDA approved for prevention of NSAID ulcers?
PPIs (lansoprazole and esomeprazole)
NOT H2 blockers
Do Cox-2 selective NSAIDS bind the platelet?
No
Which are more clinically effective for pain, COX-2 selective agents or nonselective?
they're the same
What are the contraindications to using a COX-2 selective NSAID?
Recent CABG
Pg (3rd trimester)

**also consider HTN, CRI, CHF, CAD, PUD, TIA
Why are all NSAIDS (selective and nonselective) contraindicated in the 3rd trimester of pg?
premature closure of PDA
What is the difference between side effects of COX-2 selective and nonselective NSAIDS?
they're the same except COX-2 is a little less GI risk and there are no cytochrome interactions
What are 2 side effectst that are unique to COX-2 selective NSAIDS?
1. possible sulfa allergy
2. may be prothrombotic
What is considered prolonged opioid admininistration?
>1mo (rapid d/c will result in withdrawal S/S)
What drug is an opioid antagonist?
Naloxone
Which drugs are partial agonists at opioid receptors?
Buprenorphine
Nalbuphine
Butophanol
Pentazocine
Which partial agonist opioid is available PO?
pentazocine
Which opioids are Phenanthrenes?
oxymorphone
hydromorphone
morphine
oxycodone
hydrocodone
codeine
Which opioids are Phenylheptylamines / diphenylheptanes?
methadone
propoxyphene

Which opiods are Phenlpiperadines?
meperidine
fentanyl
diphenoxylate
loperamide
Which phenanthrenes are strong agonists?
oxymorphone
hydromorphone
morphine
Which phenanthrenes are mild-moderate agonists?
oxycodone
hydrocodone
codeine
Which phenylheptylamines / diphenylheptanes are strong agonists?
methadone
only one drug in this classifications
Which phenlyheptylamine/ diphenylheptane is a mild-moderate agonist?
propoxyphene
Which phenylpiperadines are strong agonists?
meperidine
fentanyl
Which phenylpiperadines are mild-moderate agonists?
diphenoxylate
loperamide
antidiarrheals
When might it be appropriate to us meperidine (demerol)? When is it not appropriate?
May have to use if allergy, or for acute chole because other opiate clamps sphincter of oddi; not appropriate in general, especially for the elderly (seizures)
Trade name of propoxyphene
Darvocet (propoxyphene/APAP) - this phenylheptamine / diphenylheptane is almost always given with APAP
If pt is taking a lot of vicodin what must you monitor? What can you do about it?
vicodin = hydrocodone/APAP -> monitor 4g APAP limit

Can just give oxycodone (no APAP)
Dilaudid = ?
Numorphan = ?
Demerol = ?
Dolophine = ?
hydromorphone
oxymorphone
meperidine
methadone
WHich opiod is available in a transdermal patch or lozenge?
fentanyl
Which opiods are converted to active metabolites by 2D6?
codeine, hydrocodone, oxycodone
What are the 2 specific actions of opiods on the neuron?
1. close Ca channels on presynaptic nerve terminals to reduce release of NTs
2. hyperpolarize the neuron by opening K+ channels on postsynaptic neurons --> inhibiting them
What is important to consider when giving morphine to a pt with biliary colic?
morphine clamps the sphincter making PE less reliable
What might an opioid relieve besides pain?
acute pulmonary edema - mechanism not fully understood

cough

diarrhea
Which opioids are antitussives?
codeine
dextromethorphan NOT effective
Which opioids can be used to treat diarrhea?
diphenoxylate/atropine
loperamide
How does loperamide work?
GI tract has mu receptors - loperamide with choke off peristalsis
Why is atropine added to diphenoxylate for the treatment of diarrhea?
atropine dose is too low to be antidiarrhea but is felt to decrease the chance for addiction potential
How will an SSRI affect codeine, hydrocodone, or oxycodone?
may not be able to convert these opiods to morphine since SSRIs inhibit 2D6
Name several patients that you would worry about the respiratory depressive effects of opioids?
COPD
asthma
inc ICP
What physical exam sign is indicative of opioid overdose?
pinpoint pupils (miosis) - give naloxone!
What are the central side effects of opiods?
analgesia
euphoria
sedation
respiratory depression
cough suppression
miosis
N/V
What are the peripheral side effects of opiods?
constipation
biliary colic?
urinary retention
flushing/itching
In which patients is urinary retention from opiods from increased urethral and bladder tone most likely?
post-op
What is tramadol?
a synthetic analgesic agent with weak mu agonist effects and some inhibitory action on NE/5HT reuptake in the CNS
With which analgesic is vertigo common?
tramadol
What are the CYP interaction(s) of tramadol?
2D6 substrate
tramadol should NOT be given with what drug? Why?
MAOIs; seratonin syndrome
What drugs besides MAOIs should you be careful when giving with tramadol?
linezolid
SSRIs
TCAs
What drug is "expensive tylenol"? (if pt not getting relief - believe them!)
propoxyphene (Darvocet)
what is normeperidine?
the metabolite of meperidine that builds up causing dysphoria, irritability, myoclonus, and seizures
Meperidine should NEVER be given with what other drug?
MAOI
same as tramadol
In which patients is meperidine especially inappropriate?
renal dysfunction
>75