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Pharmacology > Pain Management > Flashcards

Pain Management Flashcards

1
Q

Nociceptive Pain

A

Injury/inflammation of somatic/visceral tissues. Skin, bone, organ. Stiff, throbbing, dull, sore. Responds well to opiods

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2
Q

Neuropathic pain

A

Changes in peripheral or CNS. Numbness, tingling, shock-like, shooting.

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3
Q

Endogenous opiods

A

enkephalins, endomorphins, dynorphins

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4
Q

Opioid agents MOA

A

G protein (opioid receptors) decrease cAMP/CA, decrease release of neurotransmitters

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5
Q

Opioid receptor types

A

mu-1: mostly analgesia
mu-2: sedation, constipation, antidiuretic, respiratory depression, bradycardia, euphoria, physical dependance
delta: analgesia, mood
kappa, sigma, epsilon

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6
Q

Analgesic ladder

A

Step 1: non-opioid, +/- adjuvant analgesic
Step 2: opioid for mild to moderate pain +/- non-opioid, +/- adjuvant analgesic
Step 3: Opioid for moderate to severe pain, +/- non-opioid, +/- adjuvent analgesic

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7
Q

Acetaminophen

A

APAP. MOA: elevates pain threshold; peripherally blocks pain impulse generation. Inhibits Cox1 and 2 in CNS (NOT PERIPHERY)
Dose: 1gm qid scheduled for OA, 325-650 q4-6 h prn for pain/fever. MDD: 4g/d
DI: alcohol, warfarin

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8
Q

NSAIDs

A

Salcylates, Propionic Acids (IBU), Indole (Indomethacin), Acetic acid (Ketorolac)

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9
Q

Salcylates

A

Aspirin, choline salicylate, magnesium salicylate, salsalate, sodium salicylate, diflunisal.
More likely to cause hypersensativities in those suceptible.

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10
Q

NSAID use

A

Analgesic, anti-inflammatory and antipyretic
Widely used for arthritis and pain
Have ceiling effect
No addiction potential

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11
Q

Cox 1 and Cox 2

A

Inhibiting Cox 1 = s/es
Inhibiting Cox 2 = good stuff
Celebrex is cox 2 only, everything else has both. If you push cox 2 too high, you can lose specificity and get s/es.

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12
Q

NSAIDs MOA

A

Decrease CNS pain impulses received
Inhibits prostaglandin synthesis and release
Reduces inflammation–inhibits leukocyte migration and lysosomal enzyme release
Blocks hypothalamus pain impulses
Decrease body temperature (antipyretic)

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13
Q

Aspirin

A

Peak 0.25-2hr
325-650mg tid/qid
MDD: 6-8g
LOTS OF GI!

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14
Q

Ibu

A

peak: 1-2hr
Dose: 200-800mg TID/qid
MDD: 3200mg

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15
Q

Naproxen

A

peak: 2-4 hr
Dose: 250-500 mg BID/TID
MDD: 1250mg

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16
Q

NSAID GI Risk factors

A

> 60yo, gx of GI (PUD and GIB), concomitant corticosteroid or anticoagulant use
Serious underlying dz
Chronic NSAID use and high dose NSAID

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17
Q

Misoprostol

A

GI cytoprotection
MOA: synthetic prostaglandin EI, with antisecretory effect on gastric acid secretion and mucosal protective properties
Abortifacient properties: contraindicated in pregnancy!

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18
Q

PPIs/H2 Blockers

A

omeprazole or pepcid with non-selective NSAIDs may be considered to decrease GI adverse effects

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19
Q

ASA ADRs

A

ASA sensitivity triad: 20% of asthmatics are sensitive to aspirin and other NSAIDs
Rhinosinusitis: sinusitis with nasal polyps
Low dose ASA inhibits platelet aggregation for life of platelet (7d)
ADRs: painless GI bleed, gout, Reyes syndrome, Aspirin toxicity (hyperthermia, hyperventilation, resp alkalosis, first sx: tinnitus)
DIs: increase lithium levels, warfarin increases GI bleed/platelet, ACE inhibitors increase renal dz, decreased diuretic effects

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20
Q

Indomethacin

A

Higher incidence of SEs than other NSAIDs

Used for gout: 50mg TID and decrease as pain decreases

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21
Q

Ketorolac

A

Toradol
Used with morphine sulfate to decrease opiate dose, mostly post-op
IV*, PO, IM
LIMIT 5 DAYS TOTAL THERAPY!!!
Contraindications: PUD, labor/delivery, minor pain
DOSE DOWN: >65 yo, Renal impairment, <50kg
Risks: fatal cardiovascular thrombotic event, GI bleed, renal failure, cerebrovascular bleeding

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22
Q

Cox 2 inhibitors

A 
Fewer GI s/es
Celecoxib (celebrex): 100mg QD to 200mg
Sulfonamide: hypersensitivity
Preg Cat D
Renal=related ADE similar to noselective agents
Increased CV risk
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23
Q

Combination therapy

A

Prostaglandins and opiate receptors–enhances pain relief, lower doses of each agent, better s/e profile.
Very effective in treating bone metastatic pain in advanced ca
not as common as APAP combination products
Oxycodone/Ibu
Oxycodone/Aspirin
Hydrocodone/Ibu

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24
Q

Opiates

A

Phenanthrenes
Phenylpiperidine
Diphenhylheptane

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25
Q

Phenanthrenes

A

Morphine, codeine, hydrocodone, oxycodone

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26
Q

Phenylpiperidine

A

Fentanyl, meperidine, sufentanil, alfentanil

27
Q

Diphenylheptane

A

Methadone,QT prolongation

28
Q

Opioid analgesics

A

Morphinans (levolrophanol, butorphanol)
Benzomorphans (Pentazocine) irritant, do not administer subq
Phenantrenes: morphine, hydromorphone, oxymorphone, buprenorphine

29
Q

Opioid absorption notes

A

Well absorbed
Fentanyl has low oral bioavialability: no PO
Codeine and oxycodone: reduced 1st pass
Meperidine: large Vd in elderly–DO NOT USE

30
Q

Opioid metabolism

A

Converted mostly to glucuronides which are excreted by kidneys
Morphine –> active metabolites M3G and M6G accumulation may lead to ADRs in reduced kidney function. the length that it helps pain, it is still in system; accumulation if given again for more pain can cause seizures!

31
Q

Short-acting vs long-activing

A

LAs have fewer peaks/troughs fluctuations–steady drug levels for steady pain
LAs have less end of dose failure
LAs increased interval –increased adherence
SAs may have fewer ADRs

32
Q

Opioid MOA

A

opiod agonists inhibit the release of excitatory transmitters from the primary afferents and directly inhibits the dorsal horn pain transmission neuron.

33
Q

Opioid receptor types

A

Mu receptor: associated with opiate addiction; activation produces analgesia, euphoria; respiratory depression, sedation and miosis; slowed GI transit
Kappa: activation produces analgesia; pychosis–abuse potential; slowed GI transit
Delta: activation in humans not well characterized

34
Q

Full opioid agonists

A

activates mu receptor
highly reinforcing, most abused
no ceiling
will not reverse or antagonize effects of other opioids w/in the class
Agents: morphine, hydromorphone, codeine, oxycodone, methadone, fentanyl
Acute use effects: Constipation! euphoria, vomiting, drowsiness, depressed respiration
Large dose effects: non-responsive, slowed hear/respiration
Chronic use: physical/psycological dependence, lethargy, reduction in BM

35
Q

Opioid addiction

A

Pyschological dependance: euphoria, sedation. 5 Cs: chronic, loss of Control, Compulsive use, Craving, Continued use despite personal harm
Diversion: diverting drugs from original purpose–recreational use

36
Q

Morphine

A

Equivalent IM dose: 10mg
Equivalent PO dose: 30mg
Usual dose: 10-30mg po, 2.5-15mg IM/IV
Duration of action: 3-5 hr

37
Q

Opioid conversions

A

Convert to total daily dose equivalent of PO morphine (30mg)

Reduce 25-50% for cross-tolerance (except methadone!)

38
Q

Hydrocodone

A

Vicodin, Norco, Lortab, Lorcet

39
Q

Codeine

A

Tylenol #2, #3, #4 (Codeine/APAP 15mg/300mg, 30mg/300mg, 60mg/300mg
1-2 tabs q4-6hrs PRN for pain
Codeine is metabolized to morphine

40
Q

Oxycodone

A

Percocet (oxy + APAP), Oxycodone IR (immediate release), Oxycontin (Oxycodone sustained release)
20mg PO oxycodone = 30mg po morphine

41
Q

Fentanyl

A

Cleanest opioid
Transdermal, transmucosal, sublingual, inj, intranasal, buccal mucosa
Can be used as alt to meperidine for post-op shivering

42
Q

Fentanyl patch dosing

A

DO NOT ADJUST DOSE MORE FREQUENTLY THATN Q3 DAYS after inital dose or every 6 days thereafter
Tmax up to 72 hours
upon d/c, 17hrs needed for 50% decrease in levels, cleared in 4-5 days.
Start with lowest possible dose

43
Q

Fentanyl patch black box warning

A 
CIs: opiate naive (week or more being on morphine or more more than 60mg/day); acute or post op pain; OP surgery; mild pain
Intact skin application
Do not cut
Temp dependent
Abuse potential
Dispose properly
44
Q

Other fentanyl formulations

A

BREAKTHROUGH PAIN IN CANCER PTS ONLY
q4h dosing prn BTP
Actiq–lozenge on a stick
Fentora: buccal tablet

45
Q

Methadone

A

Longest terminal T1/2 (about 1 d)
May accumulate during titration to steady state
ADRs: qt prolongation, hypotension
60mg/d is for W/D, 60mg several x/day is for pain
DIs!

46
Q

Methadone dosing

A

Initial Dose: 2.5mg po q6-8h or 5mg q12h
Analgesic onset: 30-60min
Analgesic duration: 4-12 hours; increases with continued use and cumulative effects

47
Q

Methadone-to-morphine equivalency

A

For gradual conversion to methadone

Oral morphine 500mg/day: consult w/ pain specialist

48
Q

Hydromorphone

A 
A rapid onset morphine
About 8x more potent than morphine
No active metabolite
Good choice for PCA, post-op analgesia
If giving IV, start w/ .25-.5mg
Available PO, not ideal for long-term use
49
Q

Hydromorphone ER

A

8, 12, 16mg tabs
1x/day dose for opioid tolerant pts
ONLY USED in patients on TDD equivalent 12mg hydromorphone ~60mg po morphine (reduce by 50%)

50
Q

Oxymorphone

A

Opana
IR dose: 5-20mg po q4-6h
ER dose: 5mg q12h
1.5mg oxymorphone ~10mg morphine

51
Q

Meperidine

A

Demerol
Little role in pain management, no role in elderly
Toxic metabolite normeperidine can cause suizures, serotinin tox, tachycardia
Useful for post op shivering
Greatest histamine release risk

52
Q

Propoxyphene alternatives

A

Episodic pain: APAP, NSAIDs, hydrocodone/APAP

Chronic pain: sustained release morphine, methadone, sustained release oxycodone, fentanyl

53
Q

Other opiod-like compounds

A

Antitussives

Antidiarrheal (diphenoxylate/atropine, tincture of opium, paregoric aka camphorated tincture)

54
Q

Opioid CNS effects

A

Analgesia: reduce both sensory and affective components
Dysphoria/euphoria
Sedation
Respiratory depression
Antitussive
Miosis
N/V
Periph vasodilation, cerebral vasodilation
Orthostatic hypotension
Increase GI tone, decrease activity, smooth muscle spasm

55
Q

Opioid potential risky pts

A

Head injuries–CO2 retention leads to increased intracranial pressure
Pregnancy
Impaired pulm function
Impaired hepatic/fenal fx
Endocrine dz–addison’s or hypothyroidism may have prolonged and exaggerated responses to opioids

56
Q

Opioid use in renal failure

A

avoid morphine, hydromorphone, codeine
Methadone seems safe–start low and go slow
fentanyl is probably safe

57
Q

Opioid OD

A

acute opioid intoxication: miosis (pinpoint pupils), resp depression, excessive sedation, stupor, coma
Treat with Naloxone (pure antagonist)

58
Q

Opioid DIs

A

Sedative-hypnotics
Antipsychotic drugs
MAOIs
Anything that causes respiratory depression or CNS depression

59
Q

Opioid receptors partial agonists

A

Activates the receptor at lower levels
Is less reinforcing
Is less abused, esp with naloxone
Includes buprenorphine, whose affinity is very strong and it will displace full agonists like heroin and methadone. it has a slow dissociation, so it stays on the receptor for a long time and blocks heroin or methadone from binding ; prolonged therapeutic effect for opioid dependence tx
At higher doses, even when partial agonists bind ALL mu receptors, maximal agonist effect is never achieved.
Buprenorphine WILL NOT show as morphine positive on screen!

60
Q

Opioid w/d syndrome

A

dysphoric mood, N/V, body aches, lacrimation, rhinorrhea, pupillary dilation, sweating, piloerection, diarrhea, yawning, mild fever, insomnia, irritability, craving

61
Q

Opioid recepter antagonists

A

occupies w/o activating
not reinforcing
blocks abused agonist opioid types
includes naloxone and naltrexone (used for alcoholism)

62
Q

Antiemetic ajuvents

A

Metoclopramine, promethazine, ondansetron

63
Q

Constipation ajuvents

A

1st line: increase fluids and fiber, increase activity
Senna 2 tabs/d
may add docusate 200mg daily for hard stools
Other options: milk of magnesia, bisacodyl suppository, fleets enema prn

64
Q

Other pain adjuvant meds

A

TCAs, SSRI/NRI, anticonvulsants (gabapentin, topamax, lyrica), steroids, topical, muscle relaxants, alpha 2 adrenergic agonists (clonidine)

Pharmacology (10 decks)

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