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BMB Test 1 > B7.005 Prework 3: Opioids > Flashcards

B7.005 Prework 3: Opioids Flashcards

1
Q

what is an opioid

A

any drug, natural or synthetic that acts at opioid receptors

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2
Q

mu receptors

A

produce analgesic, sedative, and euphoric effects of opiates as well as side effects

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3
Q

delta receptors

A

contribute to analgesia at spinal levels

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4
Q

kappa receptors

A

may contribute to analgesia, but primarily result in dysphoria

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5
Q

action of opioid drugs at the different receptors

A

various opioid compounds have different affinities for these sites and may be full or partial agonists, antagonists, or have mixed activity

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6
Q

clinical uses of opioids

A

analgesics
cough suppressants
antidiarrheal

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7
Q

where are opioid receptors located

A

brain
spinal cord
various peripheral tissues

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8
Q

CNS pharmacological effects of prototype drug: morphine

A 
analgesia
euphoria/dysphoria
sedation
resp depression
cough suppression
miosis (parasympathetic activation)
truncal rigidity (impairs ventilation)
nausea and vomiting
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9
Q

peripheral pharmacological effects of prototype drug: morphine

A 
arterial and venous dilation
decreased gut motility (constipation)
biliary colic (cholinergic)
decreased renal blood flow
decreased uterine tone
endocrine alterations
-increased ADH, PRL, somatotropin
-decreased LH
histamine release
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10
Q

toxicity of opioids

A 
resp depression (primary cause of death)
dysphoria 
nausea and vomiting
constipation
seizures
tolerance / withdrawal / addiction
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11
Q

important differences between opioid drugs

A

potency
efficacy
duration of action
oral bioavailability

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12
Q

equianalgesic dose

A

equal to 10 mg morphine

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13
Q

low efficacy opioids

A

low efficacy for analgesia and produce only “side effects”
don’t cross the BBB
used as anti-diarrheals

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14
Q

high efficacy analgesic opioids

A 
used for severe pain (trauma, post surgical, MI)
morphine
methadone
meperidine
fentanyl
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15
Q

morphine

A

prototype drug
poor oral bioavailability due to 1st pass effect
duration: 4-5 hours
hepatic metabolism, renal excretion

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16
Q

morphine metabolite

A

glucuronidated metabolite M-6G is even more potent, but has poor BBB penetration

17
Q

methadone

A

longer acting than morphine: 6 hrs, plasma t1/2 24 hr
good oral bioavailability
used as maintenance in addicts, but also for pain

18
Q

meperidine

A

duration: 2-4 hr
antimuscarinic > may cause tachycardia
metabolized to an active metabolite that is psychoactive and can cause seizures

19
Q

fentanyl

A 
short acting
duration: 1-1.5 hr
100x more potent than morphine
primarily acts at mu receptors
poor oral bioavailability
transdermal available
20
Q

low to medium efficacy analgesic opioids

A

administered orally
used for moderate pain (broken bones, dental procedures)
often formulated with aspirin, APAP, or ibuprofen
codeine
hydrocodone
oxycodone
tramadol

21
Q

codeine

A

low efficacy
metabolized to morphine by CYP2D6
ineffective in people with decreased enzyme levels

22
Q

hydrocodone

A

moderate efficacy

23
Q

oxycodone

A

moderate-high efficacy
available in ER formation
high levels of addiction (esp with ER)

24
Q

tramadol

A

low efficacy
also inhibits NE and 5HT reuptake
may have efficacy for neuropathic pain

25
Q

partial agonist or mixed agonist-antagonist analgesic opioids

A

believed to have less addictive potential and risk of resp depression
used for moderate to severe pain
used for opioid addiction

26
Q

buprenorphine

A

mu partial agonists

27
Q

pentazocine

A

kappa agonist

mu partial agonist or antagonist

28
Q

antidiarrheal opioids

A

poor permeation of the BBB
diphenoxylate
loperamide (OTC)
eluxadoline

29
Q

eluxadoline

A

mu and kappa agonist
delta antagonist
used for IBD with diarrhea

30
Q

antitussive opioids

A

poor permeation of the BBB
codeine
dextromethorphan (OTC)

31
Q

opioid drug of abuse

A

heroin

no medical uses

32
Q

opioid antagonists

A

naloxone
naltrexone
reverse the effects of opioids after overdose
prevent opioids from having an effect
can induce withdrawal when administered IV or in high dose

33
Q

naloxone

A

IV

intranasal

34
Q

naltrexone

A

oral

depot injection

35
Q

opioid antagonists for constipation

A

poor BBB penetration
increase risk of bowel perf
-methylnaltrexone (subQ)
-naloxegol (oral)

36
Q

contraindications / interactions associated with opioids

A

head injuries
-vasodilation can increase intracranial pressure
pregnancy
-fetal addiction, sedation
impaired pulmonary function (except acute pulmonary edema)
hepato- or renal compromised patients
increased sedation and resp depression with sedatives or antipsychotics

BMB Test 1 (29 decks)

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