Analgesia Flashcards
principles of pain therapy (pre-opioid crisis)
give scheduled
verify effectiveness
allow for dose titration
not “1-2 tabs” without indicating when to use 2 vs 1
for severe pain, provide ___
long acting analgesics ATC
short acting analgesics PRN for break through pain
non-opioids
NSAIDs
Acetaminophen
adjuvant therapy
anticonvulsants (gabapentin)
TCAs
SSRI
SNRI
opiates
codeine
morphine
opioids
propxyphene tramaodl hydromorphone oxycodone fentanyl meperidine methadone
MOA of NSAIDs
inhibition of cylooxygenase (COX)
most NSAIDs are ___
nonselective for COX1 and COX2
COX1 is ___
cyto-protective
COX 2 is ___
inflammatory
use NSAIDs for ____ pain
mild-moderate
ceiling effects
additional drug gives no additional analgesia; only increases SE (NSAIDs)
class side effects
GI upset
GI irritation/ulceratio
edema
renal impairment
after one class of drug fails, ___
try another
Dual MOA work in ___
synergy
With combo NSAIDs, efficacy > ___
sum of the individual components
In NSAID combos, dose titration is often limited by ___
non-opioid
NSAID combos being limited by non-opioid is often the cause of ___
unintended overdose
most hepatic failures with NSAIDs are from ___
excessive opioid/APAP use
usual max of acetaminophen
4g/d (soon to be 3g/d per FDA)
usual max for Aspirin
4g/d (higher for anti-inflammatory)
usual max for ibuprofen
3.2g/d
salicylic acids (aspirin) is a ___
weak anti-inflammatory agent
aspirin is contraindicated if ___
<16 years (risk of Reye’s Syndrome0
low dose aspirin
81mg
anti-inflammatory dose of aspirin
3.6-5.4 g/d
propionic acids (ibuprofen) are ___
anti-inflammatory, antipyretic, analgesic
max inflammatory dose of ibuprofen
3.2g/d
max pain/fever/dysnemorrhea dose of ibuprofen
1.2 g/d
only commonly injectable NSAID
ketorolac (toradol)
ketorolac is used for ___
mod-severe pain
NSAID useful for post-op pain
ketorolac
ketorolac is only used for___
5 days due to increased risk of GI bleed
ketorolac usual dose
30mg IVP q6
max dose of ketoroalc
120mg/d
dise reduction of ketorolac:
patients >65
body weight <50 kg
“moderately elevated” serum creatinine
mefenamic acid is used for ___
mild-mod pain
avoid ___ when using mefenamic acid
alcohol (enhances mucosal irritation)
this NSAID is little used
mefenamic acid
NSAIDs mainly used for acute and chronic RA and OA
piroxicam
advantage of piroxicam is
long half life
piroxicam allows for ___
daily dosing
reduce dose of piroxicam with ___
hepatic dysfunction
only remaining selective COX2 inhibitor
celecoxib
Rofecoxib increased number of ___
cardiac events (AMIS)
CoX2 inhibitors are very useful in
non-cardiac patients (orthopedics)
Acetaminophen is an effective ___
analgesic, antipyretic
APAP has little ___
anti-inflammatory activity
many ____ following overdose on APAP
hepatic failures
recommended max dose of APAP
4g/d (3g/d soon?)
avoid APAP in patients with ___
alcoholic liver disease
MOA Of APAP
inhibits both COX isozymes
COX inhibition may be more pronounced in the ___
brain
APAP inhibits ____
hypothalamic heat-regulating center
when adjusting APAP for renal impairment, ___
metabolites accumulate
CrCl 10-50 give APAP ___
q6h
CrCL <10 give APAP ___
q8h
infant drop dose of APAP
100mg/mL
injection dose of APAP
Afirmed: 1000mg/100mL (post op x 4 doses, $$$)
dose of injection APAP adults / adolescents >50kg
1000mg q6h
MAX 4G/D
Injection (Afirmed) adults adolescents <50 kg dose
15mg/kg q6 OR 5mg/kg Q4
MAX 75 mg/kg/d
child dosing for APAP
10-15mg/kg/d
APAP toxicity tx
oral therapy: Mac (Mucomyst)
IV therapy: (Acetadote)
long term acetaminophen use during pregnancy resulted in ___
2 fold increased risk of offspring having ADHD
APAP used for <8d during pregnancy was assc w/ ___
decreased risk in ADHD
remeasured pain score 2 hr post dose most reduction to least reduction
oxycodone
hydrocodone
codeine
MOA of Opioid receptors
mu-classical analgesic receptor
opioid receptors are the basis of ___
mixed agonist-antagonist agents
opiates = ___
natural agents from opium (codeine, morphine)
opioids = ___
modifications of natural opiates (synthetics)
mixed opioid agonists-antagonists
buprenorphine
butorphanol
pentazocine
nalbuphine
mixed agents are __
little used
exception ot mixed opioid agonists not being used is __
nalbuphine
nalbuphine is more effective in ___
females
nalbuphine has a ceiling effect on ___
respiratory depression
napbuphine is used in ___
labor/delivery
endorphins are derived from __
small endogenous peptide hormones
endorphins account for ___
variability of response to pain
opiate/opioid side/adverse effects
nausea itching sedation/cognitive impairment respiratory depression meiosis decreased GI peristalsis
tolerance does not develop to
opioid AEs
opioids for mild-moderate pain
tramadol
codeine
hydrocodone
tramadol is a ___
weak opioid analgesic – useful for chronic pain
ultram is ___
immediate release
ultracet is __
tramadol 37.5mg/acetaminophen 325mg
ultram
ER tabs
increase dosage of tramadol over ___
weeks – high incidence of N/V (limits usefulness for acute pain)
tarmadol has a ___ MOA
dual
tramadol is useful for __
neuropathic pain
tramadol is now a ___
controlled substance
2014–CIII
codeine is a ___
weak alagesic, antitussive
60mg codeine produces less analgesia than ___
aspirin 650mg
codeine is metabolized by __
CYP2D6 to morphine
cyp2d6 inhibitors ___
decrease codeine’s effect
antiemetic phenothaizenes
thorazine, compazine, phenergan)
cyp2d6 inhibitors
haloperidol, fluoxetine, paroxetine
10% of the population lack the ___ enzyme
cyp2d6
codeine is available alone or in combination w/
acetaminophen
hydrocodone is only available ___ w/ ___
PO with acetaminophen
Norco dose of acetaminophen
325mg
hydrocodone:
norco
lortab
vicoden
hydrocodone allows better ___
pain relief and longer duration than codeine
hydrocodone is metabolized by __
cyp2d6 to hydromorphone (dilaudid)
63% of unintentional overdoses involve combination products, most commonly ___
hydrocodone
opioids for moderate to severe pain
morphine hydromorphone oxycodone meperidine methadone fentanyl
morphine prototype pure ___
mu receptor agonist
morphine has 2 active metabolites, both __ eliminated
renally
morphine-3-glucuronide is a ___
neurotoxin
morphine-6-glucuronide provides ___
analgesia 2-4x that of morphine
morphine induces ___
histamine release (hypotension, pruritus)
morphine has a significant _____
first-pass effect
morphine has a parenteral-to-oral dose ratio of:
1:3
dose of morphine sulfate injection
2mg/mL
dosage forms of morphine sulfate
injection immediate release tabs SR capsules (Kadian) CR tabs (MS Contin) Oral solution (Roxanol)
5-7x more potent than morphin
hydromorphone (dilaudid)
hydromorphone (dilaudid) often results in ___
iatrogenic overdoses
hydromorphone’s imported SE profile:
less histamine erelease
no active opioid metabolites
sustained released form of hydromorphone
exalgo
8, 12, 16, 32 mg CR tabs
alcohol destroyed time-release mechanism of SR Palladone causing –
overdoses
dose of injectable dilaudid
2mg/mL
oxycodone is more potent w/ fewer side effects than ___
morphine
oxycodone is metabolized by ___
cyp2d6 to oxymorphone (also active)
oxycodone is useful in patients with ___
cyp2d6 deficiency or on inhibitors
oxycodone is useful in nonresponders to ___
non-responders to codeine and hydrocodone
dosage forms of oxycodone
oxycodone IR roxicodone oxycodone CR with acetaminophen with aspirin
meperidine is not recommended as ___
1st line agent
meperidine is ___ causing more rapid onset, shorter duration (2-3h)
lipophilic
meperidine is metabolized to active metabolite ___
normeperidine (neurotoxic)
meperidine has long ___
metabolite half life
meperidine causes
euphoria, irritability, seizures
toxicity of meperidine is not reversed by ____
opiate antagonists
meperidine metabolites is __ eliminated
renally
meperidine is contraindicated in patients on ___
MAOIs (serotonin syndrome)
meperidine may be used in patients with serious ___
opiate allergies
meperidine is useful in controlling ___
post anesthesia shivering
methadone has unique pharacology:
racemic mix of I and D isomers.
I isomer of methadone –>
opioid activity
d isomer of methadone –>
NMDA antagonist & NE/5HT reuptake inhibitor
methadone is useful for __
neuropathic pain
methadone has the longest half life :
12-190h; usually ~24h
methadone is useful in treatment of
opiate addiction (dosed q24h)
analgesia from methadone only lasts ___
4-8h
dose methadone q___ for analgesia
6-8h
fentanyl is __x more potent than morphine and is dosed in __
100x; mcg
fentanyl is extremely ___
lipophilic.
fentanyl has __ onset and __ duration
rapid onset; short duration (30-60 minutes)
___ has many fewer adverse reactions than morphine or dilaudid
fentanyl
fentanyl has minimum ___
histamine release, hypotensive effect
dosage forms of fentanyl
injection
lozenge
transdermal
duragesic cautions are not usually used in ___
opiate naive pateints
monitor respiratory rate using duragesic cautions for ___
24h
replace duragesic cautions q __h
72h
look for multiple patches when ___
discharging patients (don’t just continue adding additional patches.)
fentanyl is only used for ___
standing chronic (cancer) pain
naloxone is a pure ___
mu receptor antagonist
naloxone is used to reverse ____
sedation/respiratory depression but ALSO REVERSES ANALGESIA
administration of naloxone
dilute 0.4mg to >10mL saline
administer via SLOW IVP (1mL/1-2m)
monitor respiratory rate
stop when respiratory rate increasess
____ is used to establish useful analgesic regimens
equianalgesisc dosing
nonpharmalogic therapy and nonopijoid pharmacologic therapy are perferred for ___
chronic pain
when staring opioids for chronic pain, clinicians should ___
prescribe immediate release opioids instead of ER/long-acting
when prescribing opioids for acute pain, use ___
the lowest effective dose of IR opioids for 3-7d
evaluate benefits and harms within ___ of starting opioids for chronic pain and again every ___
1-4 wks
every 3 mo or more frequently
incorporate strategies to mitigate risk of opioid addiction such as:
naloxone
monitor a patient’s ____
controlled substance use
use drug urine drug screening before starting ____
opioid therapy and at least annually.
avoid prescribing opioids and ___ concurrently
benzodiazepines
offer or arrange evidence based treatment for patients with ___
opioid-use disorder (OUD)
buprenorphine is a partial ___
opioid agaonist
buprenorphine helps relieve ___
withdrawal sx
buprenorphine may begin with __
opioids in the patient’s system
naltrexone is an ___
opioid antagonist
naltrexone may precipitate ___
withdrawal symptoms
naltrexone is only available in ___ and ___
PO daily and IM monthly
must be opioid free to start __
naltrexone
methadone is ___
log-acting opioid agonsit
methadone transfers opioid addiction to longer ___
half-life agonist, allowing taper
methadone requires ___
daily PO dosing
