Non opiates 1 Flashcards
name a type of nociceptive pain and how you would treat first line
osteoarthritis, burns - acetaminophen
name a type of inflammatory pain and how you would treat first line
osteoarthritis, RA - NSAIDs
name a type of neuropathic pain and how you would treat first line
diabetic neuropathy, postherpetic neuralgia - antidepressants
name a type of functinoal pain and how you would treat first line
fibromyalgia, tension headaches - non-opiates
what is backup therapy for any type of pain?
opiates
MOA fo acetaminophen
blocks NMDA binding to a glutamate receptor
do opiates generally have a ceiling dose?
no
what is acetaminophen used for?
treatment of mild to moderate pain and fever
which is better for inflammation: ASA or acetaminophen
ASA
If a pt is taking a lot of combos with acetaminophen, are you worried about toxicity?
yes
describe the kinetics of acetaminophen
excellent absorption, uniform distribution, near complete elimination via the kidney
does acetaminophen need renally adjusted
nope
how is acetaminophen excreted?
relys on glucuronidation in the liver
ADR of acetaminophen
rash is possible, no other problems really
how does acetaminophen cause an overdose?
NAPQ1 normally binds to glutathione and now goes to other cells and kills them
how long do you have after acetaminophen toxicity to administer acetylcysteine?
4 hours
Describe stage 1 acetaminophen toxicity
first 24 hours; anorexia, n/v, malaise, hypokalemia
describe stage 2 acetaminophen toxicity
days 2-3; better anorexia, n/v, get abdominal pain, hepatic tenderness, elevated transaminases, elevated bilirubin and prolonged PT
describe stage 3 acetaminophen toxicity
days 3-4; anorexia, n/v, encephalopathy, anuria, jaundice, hepatic failure, metabolic acidosis, coaguloathy, renal failure, pancreatitis
describe stage 4 acetaminophen toxicity
day 5; clinical improvement and recovert or MSOF and death
90% mortality rate with this much acetaminophen
300mcg/ml
max dose of acetaminophen
4g/day
what does acetylcysteine smell like
sulfur
why is IV preparation of acetylcysteine better than oral
oral needs 17 doses, lasts 72 hours (good), need to mix with a drink and drink with a straw
fatal dose of acetaminophen
20-25g
how many tabs is 10-15g of tylenol
20-30tabs
what are the NSAID categories
propionic acids, acetic acids, enolic acid, fenamic acid, naphthylakanones, diaryl heterocyclic compounds
name the propionic acids
ibuprofen, flurbiprofen, naproxen, ketoprofen
name the acetic acids
indomethacin, diclofenac, sulindac, ketorolac
name the enolic acids
piroxicam, meloxicam
name the fenamic acids
mefenamic acid, meclofenamic acid
name the naphthylakanone
nabumetone
came the diaryl heterocyclic compounds
celecoxib
what is the only injectable NSAID
ketorolac
uses for nabumetone
arthritis pain - not severe
MOA of NSAIDs
block Cox1 (maintenance) and cox2 (antiinflammatory)
ceiling dose of NSAIDs per day
2400mg/day
are NSAIDs toxic to the GI system?
1-2% rate of upper gI complications
uses for ibuprofen
relief of fever, OA, mild-moderate pain, rheumatoid disorders
uses for naproxen
gout, mild-moderate pain, OA, rheumatologic disorders
uses for ketorolac
short term (5 days or less) management of moderate to severe pain requiring analgesia at the opiate level
what should be given to a pt if they require opiates but have an allergy?
ketorolac 10-15mg
ADR of ketorolac
acute psychotic rxn with 30mg (can also happen with advil in large doses)
time to peak effect of NSAIDs
2-3 hours after
are NSAIDs strongly or weakly bound to proteins?
strongly - 99% are bound to albumin
t1/2 of ibuprofen
1-4 hours
t1/2 of peroxicam
50 hours
describe the kinetics of NSAIDs
rapidly absorbed, widely distributed, hepatic biotransformatino and renal elimination
ADR of NSAIDs
GI, platelets, renal, CV, CNS, uterus (prolongatino of pregnancy), hypersensitivity
what are the effects of cox2 on cardiac dysfunctino
increases mortality
benefits of using celebrex
lower GI toxicity
indications for celebrex
pain management, OA pian, RA
what is celebrex a derivativ of?
sulfa
what was the first tolerable systemic analgesic
Aspirin
what is the 8th NSAID category?
salicylates
name the salicylates
aspirin, magnesium salicylate, choline magnesium trisalicylate, salsalate, diflunisal
which salicylate derivative doesn’t metabolize to salicylic acid in vivo
diflunisal
which analgesic is 3-4x more potent than aspirin
diflunisal
what schedule are opiates?
schedule II
what are the mu receptor agonists?
opiates
why are mu receptor agonists at a lower risk of dependence than other opiates?
lower affinity of parent compound for mu opiate receptor site
what are immediate release mu receptor agonists used for?
manangement of moderate to moderately severe pain in adults
what are extended release mu receptor agonists used for?
management of moderate to moderately severe chronic pain in adults who require around the clock treatment of pain for an extended period of time
when are mu receptor agonists dosed renally?
CrCl below 30ml/minm also required in hepatic impairment
how iare mu receptor agonists metabolised?
3A4
drug interactions with mu receptor agonists
CYP3A4 inhibitors or inducers (may alter tramadol levels), trmamadol may enhance effects of SSRIs causing serotonin syndrome
who has a lower chance of ADR with mu receptor agonists?
older pts
max dose of tramadol
400mg/day (>65 y/o then 300mg/day)
what are the mixed agonists/antagonists?
buprenorphine, butorphanol, nalbuphine, pentazocine
what drug is a strong antagonist of kappa receptors?
nalbuphine
Is nalbuphine a mu receptor agonist or antagonist?
antagonist
what is nalbuphine structurally related to?
oxymorphone and naloxone
what are benefits of using nalbuphine?
less likely to cause dysphoria (like pentazocine), less likely to cause cardiac problems (like pentazocine and butorphanol), 1:1 ratio to morphine, not a controlled substance
route of administration options for nalbuphine
SC, IM, IV
what is buprenorphine a derivative of?
thebaine
how much more potent is buprenorphine than morpphine?
25-50X, longer DOA, longer dissociation times from opioid receptors
is buprenorphine a controlled substance?
yes, C-III
if buprenorphine-related respiratory depression is in place, is naloxone useful?
no
ROA for buprenorphine
injection, transdermal for moderate to severe pain relief
ADR of mized agonists/antagonists
CNS (sedation, drowsiness, dizziness, n/v), respiratory depression
with which drug is respiratory depression more noted: nalbuphine or buprenorphine
buprenorphine
