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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

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

A

-brain injury
-emphysema
due to it depresses respiration

24
Q

clinical indications for morphine

A
  • post operative pain
  • cancer pain
  • other pain–sickle cell crisis, trauma
25
Q

mu agonists–group 1

A
  • full agonists, parenteral and oral
  • morphine
  • methodone
  • meperidine
  • hydromorphone
  • oxymorphone
  • levorphanol
26
Q

mu agonists group 2

A

full agonists, short acting

  • fentanyl
  • sufentanil
  • remifentanyl
27
Q

mu agonists–group 3

A
  • codeine–related
  • hydrocodone
  • oxycodone
28
Q

group 1 what differs from morphine in efficacy

A

-morphine-10
-meperidine-60
hydromorphine-1.5
-oxymorphone-1.5
-levorphanol- 2-3

29
Q

morphine has high first pass metabolism (low oral bioavailability)–what group has good oral bioavailbaility?

A
  • methadone

- levorphanol

30
Q

morphine metabolism–active metabolites

A
  • via UGT 1A1 and 2B7
  • M3 glucuronide
  • M6 glucuronide
  • hydromorphone (via dehydrogenase)
31
Q

morphine metabolism–inactive metabolites

A
  • via CYP 3A4

- normorpine

32
Q

methadone

A
  • full mu agonist
  • longer t/12 (27 hours vs 2 for morphine)
  • better bioavailability (90% vs 20% for morphine)
33
Q

methadone useful for?

A
  • withdrawl/maintenance

- detoxification

34
Q

methadone side effect??

A
  • QT interval prolongation (in acute overdose or long term treatment)
  • unrelated to its interaction with mu Rs (blocks flow of K ions)
35
Q

Meperidine–distinctions as mu agonist?

A
  • pupil dilation (those who abuse this drug can escape detection)
  • Normeperdine–toxic metabolites–accum and causes seizures
36
Q

Group 2 short acting full agonists potency?

A
  • fentanyl
  • sufentanil
  • remifentanil–very short acting
  • 100% more potent than morphine
37
Q

remifentanil used for?

A
  • analgesia for childbirth
  • metabolized by plasma and tissue esterases–rapid metabolism in fetus lowers risk for neonatal depression
  • rapid onset
38
Q

Fentanyl–characteristics

A
  • 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
Q

group 3 codeine and its relatives–characteristics

A
  • partial agonists
  • less potential for drug dependence and respiratory depression
  • bioavailability–50% (vs 20% for morphine)
  • moderate pain
  • anti-tussive (mu-independent)
40
Q

safer antitussive agent?

A
  • dextromethophan–independent of opioid Rs

- not analgesic; not addictive

41
Q

which does codeine cause death sometimes?

A
  • active metabolite via CP2D6–morphine
  • inactive–morcodiene
  • some people are ultrafast metabolizers
42
Q

codeine metabolism differs

A
  • ultrafast-CYP2D6 duplication and ultrafast allele
  • intermediate–CYP 2D6–heterozygous
  • -poor metabolizers–CYP2D6–gene deltions, slow allele
43
Q

morphine–active metabolite

A
  • M6G, M3G

- hydromorphone

44
Q

codeine–active metabolite

A

morphine

45
Q

meperidine active metabolite

A

-normeperidine (toxic)

46
Q

doesnt have active metabolites

A

hydromorphone

oxymorphone

47
Q

opioids used as anti-diarrheals

A
  • loperamide
  • diphenoxylate
  • mu opioid receptors in gut
  • have poor solubility; poor penetration of BBB
48
Q

Tramadol

A
  • moderate mu agonist
  • moderate pain
  • inhibits catecholamine reuptake (caution in patients on SRI anti-depressants)
  • associated with seizures
49
Q

Pentazocine

A
  • mixed-K agonist + mu partial agonist/delta antagonist
  • supra-spinal analgesia
  • can precipitate withdrawl in abusers
  • SE–tachycardia, hallucinations
50
Q

Buprenorphine

A
  • mu partial agonist plus K an delta antagonist
  • analgesia
  • can precipitate withdrawl in abusers
  • office-based detox/maintenance in combo with naloxone
51
Q

heroin is what?

A
  • di-acetylmorphine

- penetrates BBB rapidly–exaggerated euphoria–addiction liability

52
Q

addiction program

A
  • methadone
  • buprenorphine
  • naltrexone
53
Q

opioid overdose symptoms

A

-respiratory rate

54
Q

mu R antagonists

A
  • Naloxone (iV)
  • Naltrexone (po)
  • occupy but dont activate mu receptors
  • competitive
55
Q

antidote for opioid overdose??

A
  • Naloxone (IV

- Naltrexone (po)

56
Q

major issue re post surgery and chronic use of opioids

A
  • constipation

- opioids inhibit coordinated peristalsis–nausea, vomiting, costipation

57
Q

treatment for opioid–induced constipation

A
  • Methylnalrexone
  • cant cross BBB
  • peripheral acting opioid antagonist

NS2 Test 3 (14 decks)

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