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Pharmacology > Pain > Flashcards

Pain Flashcards

1
Q

APAP mechanism of action and is best for what type of pain?
Ex?
SE/interaction

A

inhibit prostaglandin synthesis in CNS and block pain impulses in periphery for mild-mod pain. Usually initial therapy in most instances

Ex: low back pain and osteoarthritis

SE: liver so reduced x50-75% in renal/liver disease or ETOH intake

interact= warfarin if > 2000mg/day APAP

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2
Q

aspirin mechanism of action and is best for what type of pain?
Ex?
SE/interaction

A

inhibit COX-1/COX-2 preventing prostaglandin synthesis
mild-mod pain

SE- GI irritation/bleeding limits use.

Hypersensitivity (asthma, nasal polyps, chronic urticaria at increased risk)
cross-sensitivity of other NSAIDs

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3
Q

NSAIDs mechanism of action and is best for what type of pain?
Ex of meds & conditions?
SE

A

inhibit COX-1/COX-2 preventing prostaglandin synthesis
mild-mod pain.
ibuprofen, ketorolac

Ex:
** Preferred for pain mediated by prostaglandins **
RA, menstrual cramps, post-surgical pain, bony metastasis. NOT used in neuropathic pain

SE: flat-dose response curve (higher doses no greater efficacy) but increase SE. GI (PUD, bleeding, hepatic, renal, platelet, Na retention, CNS dysfunction

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4
Q

NSAID contraindication/pt at increased risk of SE

A

increased risk GI: elderly, PUD, coagulopathy, high dose steroids

nephrotoxicity in elderly & Cr clearance < 50mL/min or those on diuretics

CAUTION w/ reduced cardiac output d/t Na retention & pt on antihypertensives, warfarin, lithium

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5
Q

COX-1 and COX-2 effects

A

COX-1: contributes to GI/renal toxicity
COX-2: anti-inflammatory

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6
Q

Concern w/ NSAID and aspirin

A

NSAID reduce cardioprotective effect of aspirin d/t compete in inhibition of COX-1

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7
Q

opioids for mod pain

A

codeine, hydrocodone, tramadol, partial agonists

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8
Q

opioids for severe pain

A

morphine & hydromorphone

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9
Q

ex pure opioid agonist and benefit

A

morphine
analgesia increases w/ doses and doesn’t provide ceiling effect

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10
Q

partial opioid agonists benefit/faults & ex

A

less conformational change & receptor activation
when dose increases, analgesia will plateau so increases will not provide additional relief but will increase SE
ex: burprenorphine, butorphanol, tramodol

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11
Q

opioids to avoid/decreased metabolism or clearance in hepatic disease

A

methadone, meperidine, pentazocine

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12
Q

meperidine/Normeperidine SE and who should AVOID

A

normeperidine (metabolite) can= tremors, myoclonus, delirium, seizures
AVOID in elderly, renal impair, PCA device, or > 1-2 days intermittent dosing

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13
Q

methadone mechanism of action, SE/concerns

A

several mechanisms: U agonist, NMDA agonist, inhibit reuptake serotonin & norepinephrine
long half life x30 hours = longer dosing intervals

concern w/ accumulation w/ repeated dose= challenging dose conversion, concern w/ respiratory depression
arrhythmia d/t prolonged QT

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14
Q

tramadol mechanism of action & similar efficacy to what drug? Tx what type of pain?
contraindication?!

A

U agonist & inhibit serotonin & norepinephrine
similar to codeine/APAP

pain= neuropathic & chronic

INCREASE RISK OF SEIZURE; contraindicated in seizure disorder, increased risk, w/ drugs lower seizure threshold
AVOID w/ SSRI= serotonin syndrome

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15
Q

nociplastic pain and ex

A

pain sensitivity d/t abnormal processing or functioning of CNS in response to NORMAL stimuli
ex: fibromyalgia and IBS

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16
Q

what fibers produce first, fast, sharp pain after nociceptor activation

A

A8-fibers

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17
Q

what fibers produce second pain described as dull, aching, burning, and diffuse after nociceptor activation

A

C-fibers

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18
Q

theory behind counterirritants & tanscutaneous electrical nerve stimulation (TENS) in pain management

A

brain can only process limited number of signals at one time so other sensory stimuli can alter pain perception

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19
Q

allodynia

A

pain from stimulus that normally doesn’t cause pain like light touch in neuropathic pain

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20
Q

acute pain should be treated aggressively before dx established EXCEPT in what conditions?

A

head or abdominal injury where pain might assist in differential diagnosis

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21
Q

mild, mod, severe on pain scale

A

1-3 mild
4-6 moderate
7-10 severe

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22
Q

how much to reduce APAP dose in renal/hepatic dysfunction

A

50-75%

23
Q

max APAP daily dose normal and elderly

A

normally= 4000mg/day
elderly= 3000mg/day

24
Q

ketorolac

A

NSAID
oral & parenteral dosage forms
limit use to 5 days d/t risk of serious GI SE

25
Q

What does flat-dose response curve mean with NSAIDs

A

higher doses produce no greater efficacy than moderate doses by result in increased adverse effects

26
Q

what receptor does pure opioid agonist bind to

A

u receptors to produce analgesia that increases with dose without a ceiling effect

27
Q

example of partial opioid agonists at u receptor

A

buprenorphine, butorphanol, tramadol

28
Q

partial opioid agonists with high affinity for k receptors & most likely SE

A

pentazocine, nalbuphine, butorphanol
more likely to cause psychomimetic effects (as hallucinations or paranoid delusions)

29
Q

opioids to avoid in renal disease d/t decreased clearance

A

meperidine and morphine

30
Q

serotonin syndrome

A

Agitation or restlessness
Insomnia
Confusion
Rapid heart rate and high blood pressure
Dilated pupils
Loss of muscle coordination or twitching muscles
High blood pressure
Muscle rigidity
Heavy sweating
Diarrhea
Headache
Shivering
Goose bumps

Severe serotonin syndrome can be life-threatening. Signs include:
High fever
Tremor
Seizures
Irregular heartbeat
Unconsciousness

31
Q

how to calculate dose of of iv morphine and usual starting dose morphine IV in opioid naive pts

A

10mg/70kg of body weight
5-10mg IV morphine every 4 hours

32
Q

how to dose rescue doses

A

10% to 20% of total daily opioid requirement and should be every 2-6 hours PRN

33
Q

how to increase opioid dose and when to switch to sustained release

A

based off pain; 50-100% or 30-50 % increase; some base it off number of rescue doses needed in 24 hours

switch to sustained release if tx needed for more than a few days in CANCER related pain

34
Q

what to reduce dose by when converting to sustained release of SAME ROUTE (oral to oral for ex)

A

reduce by 25% to avoid over sedation
reduce by 25-50% to account for incomplete cross tolerance

35
Q

first line tx for chronic pain

A

nonpharmacological tx and nonopioids

36
Q

onset of oral opioids

A

45 mins

37
Q

common opioids given via PCA pump & when commonly used

A

morphine, fentanyl, hydromorphone
commonly used for postop and sometimes refractory chronic pain

38
Q

when is epidural analgesia usually used

A

lower extremity procedures and pain

39
Q

common SE of epidural analgesia and tx for it
other SE

A

pruritis treated with naloxone
other SE: respiratory depression, hypotension, urinary retention

40
Q

what to do if using epidural analgesics on narcotic-dependent patients

A

systemic analgesics must be used to prevent withdrawal bc the opioid is not absorbed and remains in epidural space

41
Q

dosing of epidural analgesia vs IV and intrathecal

A

epidural dosing 10 times LESS than IV dosing
intrathecal 10 times LESS than epidural dosing

ex: 10mg IV morphine = 1mg epidural morphine = 0.1mg intrathecal

42
Q

most common analgesia in moderate pain

A

opioid and nonopioid combo

43
Q

opioid allergy & drug selection with it

A

RARE and not to be confused with pruritus associated with opioids. Cross sensitivity unlikely so if allergic to drug in one chemical class of opioids, can select another agent in another chemical class
drug selection= mixed agonists/antagonists should be treated as morphine line agents

44
Q

how and when to taper off opioids

A

pain resolved, ssx SUD, lack of improvement of pain, > 50 MME/day, overdose, early sign of overdose

reduce by 10% per week

45
Q

Patients with CYP450 pharmacogenetic variations & what opioids are substrates of it

A

may respond differently to opioids ranging from unresponsiveness > toxicity

codeine, hydrocodone, morphine, methadone, oxycodone are substrates of CYP450

46
Q

what two meds affect metabolism of methadone d/t CYP3A4

A

increased by phenytoin
decreased by cimetidine

47
Q

first line tx for neuropathic pain

A

gabapentin or pregabalin, lidocaine TD, or TCAs

48
Q

other options for neuropathic pain

A

SNRIs duloxetine & venlafaxine has been successful for diabetes peripherally neuropathy

49
Q

tx for central neuropathic pain

A

baclofen or clonidine

50
Q

what kind of pain C-fibers cause

A

transmission of chronic pain

51
Q

What stimulates nociceptors

A

Nociceptors may be stimulated by mechanical, chemical, or thermal stimuli.

52
Q

What do A-fibers transmit

A

A-fibers are responsible for the transmission of acute, sharp pain.

53
Q

where does modulation of pain occur

A

Modulation of pain impulses may occur in the dorsal horn, the brain, and the descending
(efferent) system.

Pharmacology (12 decks)

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