Pain Non-COX (2) Flashcards
Acetaminophen how works and 4 effects
Inhibs prostaglandins in CNS but min effect on COX in periphery
analgesic
antipyretic
weak anti-inflam
no anti-platelet effects
Acetaminophen is rapidly absorbed in the GI subject to _________ and can attack the ________. It’s excreted in ______
1st pass metabolism
attack of the liver
urine
N-acetylcystine
Tx for acetaminophen OD
don’t exceed 3G acetaminophen/24hrs
schedule __ drugs are a high risk for abuse, you need a new prescription every month…(4 ex)
II
morphine, oxycodone, methadone, meperidine
Mu receptor agonists cause.. (7)
resp depression, phys depression, tolerance, constipation, euphoria, miosis; primary analgesic response
Kappa receptor agonists cause… (4)
spinal-level analgesia and sedation, w/o respiratory depression, miosis
Sigma receptor agonist cause… (4)
vasomotor stimulation, psychotomimetic effects, miosis,
BINDS NON-OPIOID AGENTS
Delta receptor agonists cause…
Enkephalins (natural opioids) more selective w/the delta receptors in the periphery
Pure agonists bind __ receptors to produce analgesia that inc with dose w/o ceiling effect
Name the 3 groups
mu
Phenanthrenes
Phenylpiperidine
Diphenylheptane
Partial agonists/antagonists partially stimulate the mu receptor and antagonize the ___ receptor
kappa
reduced sfx at mu receptor, psychomimetric effects d/t kappa antagonism
possible w/drawl sx in pt dependent on pure agonists
Name the 2 strong phenanthrenes
morphine
hydromorphone (dilaudid)
what is the strong phenylheptylamine
methadone
Most widely used phenylpiperdines are strong agonists, but _________ and _________ specifically
meperidine and fentanyl
Morphine action
Mu receptor
works in CNS and GI, inhibs pain by inhib NT release
extensive 1st pass effect
Morphine effects (3)
suppress cough
relieves diarrhea (eventual constipation)
histamine release
PT on morphine needs to be monitored for
respiratory or CV depression
Meperidine action
Binds to opioid receptors and kappa
antimusc activity, can precipitate tremors or sz.
causes mydriasis rather than miosis seen in morphine b/c kappa effect
Meperidine is usually given__________, it is excreted in _________; caution 1/2 life longer in ______and _____ pts
post surgery
excreted in urine
inc in liver and kidney
Meperidine contraindicated in pts taking _________ in past 2-3 wks
3 other meds also interact
MAOI (metabolize NE=bp changes, excitatory and rigidity)
barbiturates
chlorpromazine
phenytoin
Meperidine NOT to be used in pts with_______
chronic pain (build up of metabolite)
with meperidine moniter pt for________
sx of jerking/twitching (indicates normeperidine accumulation)
Methadone action
greatest action at mu receptor
equal potency to morphine with less euphoria
analgesic substituted for morphine/heroin to control w/drawl
methadone is a good addiction tx because
less euphoric
1/2 life is loooonnng (therefore inc risk for toxicity)
2 cautions with Methadone
variable kinetics
wide range of dose equivalents
7 signs of methadone withdrawal
lacrimation rhinorrhea diaphoresis yawning restlessness insomnia dilated pupils
Fentanyl is more/less potent
more potent than morphine
Fentanyl is used for ___________ combined with droperidol.
anesthesia
esp patches in post-operative pain
Fentanyl cautions..(3)
abuse
lack of titration
variable absorption
Fentanyl has more/less allergy risk
LESS allergy risk b/c no histamine release
prefered in pts with CV issues
Fentanyl causes _____ depression and when taken with P450 inhib effect of fentanyl is _____
CNS depression
increased
what are the three mild-moderate phenanthrenes
codeine
oxycodone
hydrocodone
what are the 3 mild-moderate phenypiperidines
diphenoxylate
diphenoxylate
loperamide
2 partial agonist/antagonist phenanthrenes
nalbuphine
buprenorphine
what is the partial agonist/antagonist morphinans
butorphanol
what is the partial agonist/antagonist benzomorphans
pentazocine
buprenorphine action
20x more potent than morphine (long acting)
partial mu agonist
can antagonize resp dep caused by morphine
butorphanol and nalbuphine action
analgesic, also 20x more potent than morphine
kappa agonist~ spinal analgesia
Pentazoxine action
mild mu and kappa agonist
sigma activity may account for dysphoria
made in an attempt to have little or no abuse potential
Naloxone binding
Pure antagonist
high affinity for mu receptor and competitive antagonist of kappa and delta..
naloxone use
no effect in normal individuals but in pts taking opiates it can reverse OD, respiratory depression and coma
DOA up to 48 hours
Tramadol
weak mu agonist
inhibit NE/SE CNS reuptake
what are the 4 centrally acting skeletal musc relaxants and why are they used
cyclobenzaprine
baclofen
tizanidine
carisoprodol
releif from musc spasm and hyper-reflexia
centrally acting skeletal musc relaxants are metabolized by ________, and the 3 side effects are
hepatic metabolism
drowziness and xerostomia
N/V seen in Baclofen
Peripherally acting skeletal musc relaxants are aka ________________ agents
neuromuscular blocking agents
what are the 2 peripheral neuromuscular blocking agents
succinylcholine
Vecuronium
how do neuromusc blocking agents work?
block the transmission of cholinergics between somatic motor neuron and skeletal fibers at neuromuscular jxn
