Non opiates 1 Flashcards by Erin Frank

name a type of nociceptive pain and how you would treat first line

osteoarthritis, burns - acetaminophen

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name a type of inflammatory pain and how you would treat first line

osteoarthritis, RA - NSAIDs

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name a type of neuropathic pain and how you would treat first line

diabetic neuropathy, postherpetic neuralgia - antidepressants

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name a type of functinoal pain and how you would treat first line

fibromyalgia, tension headaches - non-opiates

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what is backup therapy for any type of pain?

opiates

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MOA fo acetaminophen

blocks NMDA binding to a glutamate receptor

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do opiates generally have a ceiling dose?

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what is acetaminophen used for?

treatment of mild to moderate pain and fever

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which is better for inflammation: ASA or acetaminophen

ASA

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If a pt is taking a lot of combos with acetaminophen, are you worried about toxicity?

yes

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describe the kinetics of acetaminophen

excellent absorption, uniform distribution, near complete elimination via the kidney

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does acetaminophen need renally adjusted

nope

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how is acetaminophen excreted?

relys on glucuronidation in the liver

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ADR of acetaminophen

rash is possible, no other problems really

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how does acetaminophen cause an overdose?

NAPQ1 normally binds to glutathione and now goes to other cells and kills them

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how long do you have after acetaminophen toxicity to administer acetylcysteine?

4 hours

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Describe stage 1 acetaminophen toxicity

first 24 hours; anorexia, n/v, malaise, hypokalemia

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describe stage 2 acetaminophen toxicity

days 2-3; better anorexia, n/v, get abdominal pain, hepatic tenderness, elevated transaminases, elevated bilirubin and prolonged PT

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describe stage 3 acetaminophen toxicity

days 3-4; anorexia, n/v, encephalopathy, anuria, jaundice, hepatic failure, metabolic acidosis, coaguloathy, renal failure, pancreatitis

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describe stage 4 acetaminophen toxicity

day 5; clinical improvement and recovert or MSOF and death

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90% mortality rate with this much acetaminophen

300mcg/ml

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max dose of acetaminophen

4g/day

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what does acetylcysteine smell like

sulfur

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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

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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?

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

Non opiates 1 Flashcards

(81 cards)