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Pharmacology 2100 > Opiods > Flashcards

Opiods Flashcards

1
Q

what are the endogenous opioids

A

endorphins
enkephalins
dynorphins

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2
Q

how do opioids work

A
  1. hyperpolarization of nerves by openign potassium and calcium channels in neurons
  2. inhibition of ascending pathways in CNS
  3. excitation of descending adrenergic and seratonerigic pathways
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3
Q

pharmacological effect of opioids*

A 
inhibition of pain and pain perceptions 
sedation adn anxiolysis 
depression of respiration 
cough suppression 
reduction of intestinal motility
pupillary constriction 
nasuea and vomiting at first
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4
Q

what is the main cause of death from opioid overdose

A

depression of respiration

clinically useful at end of life COPD

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5
Q

what can opioids be used for

A

pain
diarrhea
coughing
panic breathign - COPD

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6
Q

how do you give opioids

A

by the mouth
by the clock
by the ladder

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7
Q

what is the WHO pain ladder

A

mild pain 0-3: acetaminophen and NSAIDS
moderate pain 4-6: mild opioid codiene
severe pain 7-10: strong opioid morphine
must keep all of the pain controls all the way up the ladder bc work in different ways

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8
Q

oral dosing has first pass metabolism so is less effective than IV so why is it still recommended

A

longer term effect requiring less frequent doses
avoids highs and thus is less addictive
oral dosing safer

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9
Q

why do you dose by the clock

A

takes less drug to maintain a person drug free than to bring pain down again
avoids euphoria associated with release of pain so less addictive
avoids development of chronic pain syndromes from pain pathway rewiring

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10
Q

why do you dose by the ladder

A

assures safest and least potent drug required for any case is used
avoids addictive potential bc strong opioids not used until required

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11
Q

codeine

A

weakest commonly used opioid with little addiction risk
very low potency
pain, diarrhea, coughing, inhibit breathing

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12
Q

tramadol mechanism of action

A

activates gamma opioid receptor
weak inhibitor of NE and serotonin
less potential for addiciton, greater pain control

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13
Q

oral morphine

A

poor availability due to first pass metabolism
onset cna take an hour
lasts 3 hours

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14
Q

IV morphine

A

twice as potent

can be immediate onset or take 2 hours

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15
Q

oxycodone

A

similar potency to morphine but oral bioavailability
longer half life
dosed at half morphine dose

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16
Q

forms of oxycodone

A

slow release - oxycotin

with tylenol - percocet, high overdose risk

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17
Q

hydromorphine

A 
oral onset half an hour 
IV lasts 3 hours 
peak effect in an hours 
more potent than morphine
used in surgical settings
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18
Q

fentanyl

A

very lipophilic and potent
sublingual for acute temporary pain 1-2 hrs
transdermal used for long term severe 72 hrs

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19
Q

sufentanyl

A

more potent than fentanyl

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20
Q

naltrexone

A

oral opioid inhibitor
reverses psychotomimetic effects of opiate agonists, reverses hypotension and cardiovascular instability
completely shuts off opioid receptor

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21
Q

what can naltrexone be used to treat

A

alcohol addiction

22
Q

naloxone

A

potent opioid antagonist
blocks opioid binding
dont work orally so put in opioids to prevent OD from injection
used for emergency respiratory depression
short half life

23
Q

methadone

A

requires special training
less addictive
more potent than morphine
used where patient developed resistance or toxicity to others

24
Q

why does methadone have high risk of overdose

A

half life of 5 days but only effective for 6-12 hours

accumulates

25
Q

how do you switch from one opioid to another

A

find the equivalent dose and then use 70% of it

26
Q

when should you discontinue therapy

A

intolerable side effects
high doses of opioids with no analgesia
evidence of addiction
patient to comfortable makes no effort to increase function may require cognitive bahavoural program

27
Q

what is tolerance

A

reduced potency of analgesic effects of opioids following repeated admin
related to opioid receptor regulation

28
Q

symptoms of opioid withdrawl

A 
yawning 
sweating 
tremor
fever
increase HR 
insomnia 
cramps 
dilated pupils
29
Q

how do you avoid dependence

A

decrease dose by 20-30% a day

30
Q

what is addiction

A

psychological dependence

31
Q

how does NE and serotonin mediate pain

A

inhibit pain signals from reaching higher levels of the brain

32
Q

how are tricyclic antidepressants used to treat pain

A

increase serotonin and NE in synapse
take 1-3 weeks so used for chronic
also good to treat comorbidities of depression

33
Q

selective serotonin reuptake inhibitors side effects and examples

A

inhibits s reuptake
suicide, sexual dysfunction, impaired platelet aggregation
paroxetine, fluxoxetine, sertraline

34
Q

serotonis and NE reuptake inhibitors side effects and example

A

suicidality
serotonin syndrome
venlafaxine

35
Q

alpha adrenergic agonists

A

clonidine and tizantidine

many side effects

36
Q

what drugs act on descending pathways

A

all antidepressants

alpha adrenergic agonist

37
Q

what is peripheral sensitization

A

spontaneous peripheral nerve activity mediated by sodium channel, drugs work here by blocking sodium channels

38
Q

what are classes of drugs that dampen the sodium channels on nerves

A

carbamazepine
tricycle antidepressants
topiramate
lidocaine

39
Q

carbamazepine

A

anticonvulsant

limits influx of sodium ions across the cell membrane

40
Q

topiramate

A

anticonvulsant

limits sodium ions across the cell membrane and antagonizes glutamate receptors

41
Q

lidocaine

A

sodium channel blocker

42
Q

what are descending inhibitory pathways

A

NE, serotonin, and endorphines inhibit pain signlas from reaching higher levels of brain , drugs work here by inhibiting reuptake or stimulating the adrenergic system

43
Q

what is central sensitization

A

release of excitatory NTs in the dorsal horn of the spinal cord, increased calcium transport causes spontaneous impulses and a pain message to the brain

44
Q

what are meds that prevents central sensitization and how

A

decrease calcium channel activity by binding to alpha2-delta subunit of presynaptic neurons
gabapentin and pregablin

45
Q

what is another way to preven tcentral sensitization

A

NMDA antagonists for receptors in the spinal cord
ketamin
dextromethorphan
methadone

46
Q

ketamine

A

NMDA receptor antagonist
decreases central sensitization and modulation by lowering threshold for nerve transduction
reduces effects of substnace p

47
Q

what are the excitatory NT

A

glutamate and substance P

48
Q

dextromethorphan

A

low affinity uncompetitive NMDA antagonists
binds opioid receptors
could cause serotonin syndrome

49
Q

methadone

A

opioid agonist, blocks NMDA receptors, inhibits NE reuptake

50
Q

what are advantages of methadone

A

less need for opioid escalation
not active metabolites
highly lipophilic, high bioavailability

Pharmacology 2100 (13 decks)

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