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NS2 Test 3 > Pharmacology of Opioid Narcotic Analgesics and Related Drugs > Flashcards

Pharmacology of Opioid Narcotic Analgesics and Related Drugs Flashcards

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1
Q

opioid narcotic mu R antagonists

A
  • Nalozone
  • Naltrexone
  • Methyl naltrexone (GI specific)
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2
Q

opioid partial agonists or mixed agonists/antagonists

A
  • Buprenorphine
  • Buprenorphine–naloxone
  • pentaxocine
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3
Q

insolube, poorly absorbed opioid R agonists used for diarrhea?

A
  • loperamide

- diphenoxylate

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4
Q

common opioid related anti-tussive agents (cough suppression)

A
  • codeine
  • dextromethorphan
  • hydrocodone
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5
Q

pain impulse pathway

A

-afferent signal pathway (opioid R unoccupied)
-increases Ca influx
increases glutamate discharge
-increases NMDA R NA influx

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6
Q

opioid agonist-mediated signaling pathway

A
  • blunts signal (opioid agonist occupying opioid Rs)
  • blunts Ca influx
  • blunts glutamate discharge
  • increases K efflux
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7
Q

full agonists to mu opioid receptors

A
  • fentanyl (more potent)

- morphine

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8
Q

-partial agonist/mixed to mu opioid receptors

A

-Buprenorphine

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9
Q

Antagonists to mu opioid receptors

A
  • Naloxone

- Naltrexone

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10
Q

mild pain–what treatment

A
  • NSAID

- acetaminophen

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11
Q

moderate pain–or persisting or uncontrolled–what treatment?

A
  • Codeine

- with/without acetaminophen, tramadol

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12
Q

severe oaub–or persisting or uncontrolled–what treatment

A

Morphine

fentanyl

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13
Q

acetaminophen, NSAIDS used for?

A

tissue injury

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14
Q

opioids (morphine) used for?

A

tissue injury=acute stimuli=nerve injury

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15
Q

anticonvulsants–used for?

A

nerve injury

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16
Q

what is the prototype mu agonist?

A

morphine

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17
Q

mu R clinical effect

A
  • analgesia (supra-spinal)
  • euphoria
  • CNS and respiratory depression
  • drug dependence
  • miosis
  • GI, uterine motility
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18
Q

Kappa R clinical effet

A
  • analgesia (spinal)
  • sedation
  • miosis
  • GI, uterine motility
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19
Q

tolerance to morphine (mu agonists)

A

-analgesia
-euphoria
-sedation
-nausea
-resp depression
(have to increase dose or rotate to diff opioid)

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20
Q

no tolerance to morphine (mu agonists)

A
  • mioisis

- constipation

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21
Q

morphine side effect

A
  • respiratory depression
  • causes acidosis (high H), low HCO3, high PCO2
  • along with hyperkalemia
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22
Q

morphine depresses what?

A

sensitivity to CO2! –respiration

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23
Q

contraindications to morphine

Study These Flashcards
A

-brain injury
-emphysema
due to it depresses respiration

24
Q

clinical indications for morphine

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A
  • post operative pain
  • cancer pain
  • other pain–sickle cell crisis, trauma
25
mu agonists--group 1
- full agonists, parenteral and oral - morphine - methodone - meperidine - hydromorphone - oxymorphone - levorphanol
26
mu agonists group 2
full agonists, short acting - fentanyl - sufentanil - remifentanyl
27
mu agonists--group 3
- codeine--related - hydrocodone - oxycodone
28
group 1 what differs from morphine in efficacy
-morphine-10 -meperidine-60 hydromorphine-1.5 -oxymorphone-1.5 -levorphanol- 2-3
29
morphine has high first pass metabolism (low oral bioavailability)--what group has good oral bioavailbaility?
- methadone | - levorphanol
30
morphine metabolism--active metabolites
- via UGT 1A1 and 2B7 - M3 glucuronide - M6 glucuronide - hydromorphone (via dehydrogenase)
31
morphine metabolism--inactive metabolites
- via CYP 3A4 | - normorpine
32
methadone
- full mu agonist - longer t/12 (27 hours vs 2 for morphine) - better bioavailability (90% vs 20% for morphine)
33
methadone useful for?
- withdrawl/maintenance | - detoxification
34
methadone side effect??
- QT interval prolongation (in acute overdose or long term treatment) - unrelated to its interaction with mu Rs (blocks flow of K ions)
35
Meperidine--distinctions as mu agonist?
- pupil dilation (those who abuse this drug can escape detection) - Normeperdine--toxic metabolites--accum and causes seizures
36
Group 2 short acting full agonists potency?
- fentanyl - sufentanil - remifentanil--very short acting * 100% more potent than morphine
37
remifentanil used for?
- analgesia for childbirth - metabolized by plasma and tissue esterases--rapid metabolism in fetus lowers risk for neonatal depression - rapid onset
38
Fentanyl--characteristics
- rapid onset and distribution - short duration of action - tranmucosal (lollipop) - transdermal patch delivery (slows onset, prolongs delivery)--caution-resp depression--abuse potential via heating patches
39
group 3 codeine and its relatives--characteristics
- partial agonists - less potential for drug dependence and respiratory depression - bioavailability--50% (vs 20% for morphine) - moderate pain - anti-tussive (mu-independent)
40
safer antitussive agent?
- dextromethophan--independent of opioid Rs | - not analgesic; not addictive
41
which does codeine cause death sometimes?
- active metabolite via CP2D6--morphine - inactive--morcodiene - some people are ultrafast metabolizers
42
codeine metabolism differs
- ultrafast-CYP2D6 duplication and ultrafast allele - intermediate--CYP 2D6--heterozygous - -poor metabolizers--CYP2D6--gene deltions, slow allele
43
morphine--active metabolite
- M6G, M3G | - hydromorphone
44
codeine--active metabolite
morphine
45
meperidine active metabolite
-normeperidine (toxic)
46
doesnt have active metabolites
hydromorphone | oxymorphone
47
opioids used as anti-diarrheals
- loperamide - diphenoxylate - mu opioid receptors in gut - have poor solubility; poor penetration of BBB
48
Tramadol
- moderate mu agonist - moderate pain - inhibits catecholamine reuptake (caution in patients on SRI anti-depressants) - associated with seizures
49
Pentazocine
- mixed-K agonist + mu partial agonist/delta antagonist - supra-spinal analgesia - can precipitate withdrawl in abusers - SE--tachycardia, hallucinations
50
Buprenorphine
- mu partial agonist plus K an delta antagonist - analgesia - can precipitate withdrawl in abusers - office-based detox/maintenance in combo with naloxone
51
heroin is what?
- di-acetylmorphine | - penetrates BBB rapidly--exaggerated euphoria--addiction liability
52
addiction program
- methadone - buprenorphine - naltrexone
53
opioid overdose symptoms
-respiratory rate
54
mu R antagonists
- Naloxone (iV) - Naltrexone (po) - occupy but dont activate mu receptors - competitive
55
antidote for opioid overdose??
- Naloxone (IV | - Naltrexone (po)
56
major issue re post surgery and chronic use of opioids
- constipation | - opioids inhibit coordinated peristalsis--nausea, vomiting, costipation
57
treatment for opioid--induced constipation
- Methylnalrexone - cant cross BBB - peripheral acting opioid antagonist

NS2 Test 3 (14 decks)

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