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Pharmacology Test 3 > Opioids for Pain > Flashcards

Opioids for Pain Flashcards

1
Q

Ad fibers

A
  • pain
  • thinly myelinated
  • 6-30m/sec
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2
Q

C fibers

A
  • pain
  • unmyelinated
  • .5-2m/sec
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3
Q

Consequences of Pain Processing

A

1) modulation of peripheral receptor/ion channel properties
2) modified gene expression
3) decreased threshold for AP generation

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4
Q

Spinoreticular tract

A

spine -> reticular formation

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5
Q

Spinothalamic tract

A
  • localizing type of pain

- regional identity

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6
Q

Mu (MOP)

A
  • mediates analgesia
  • respiratory depression
  • miosis
  • euphoria
  • sedation
  • decreased gastrointestinal motility
  • physical dependence
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7
Q

Kappa (KOP)

A
  • mediates analgesia
  • enteric: decreased gastro motility
  • ** DYSPHORIA/DISOREIENTATION/ANXIETY ***
  • – no used much in clinical settings
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8
Q

Delta (DOP)

A
  • caused siezures in rats: not for human use
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9
Q

Must “classic” opiates bind to an exert their actions at ___ receptor categories

A
  • all 3 receptor categories

- to different degrees

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10
Q

Opiod Motif

A
  • YGGFM

- YGGFL

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11
Q

Enkephalins
Dynorphins
B-Endorphins

A
  • cross reactions

- not very specific

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12
Q

Phernathrenes

A

5 rings

  • heroin
  • codeine
  • hydrocodone
  • oxycodone
  • ** RAPID CNS PENETRATIONS ***
  • v fast at getting into brain and causing effect
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13
Q

Morphinans

A

4 rings

  • levophanol
  • butorphanol
  • levallorphan
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14
Q

Benzomorphans

A

3 rings

- pentazcine

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15
Q

Diphenoxylate

A

Phenylpiperidines

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16
Q

Merepiridine

A

Phenylpiperidines

17
Q

Fentanyl

A

Phenylpiperidines

18
Q

Loperamide

A

Phenylpiperidines

19
Q

Primary Actions of Opiates

A
  • Analgesia
  • Pupil constriction
  • Respiration
  • Cough
  • Euphoria
  • Sedation
  • Nausea
  • GI tract
  • Biliary tract
  • Bladder
  • Uterus
20
Q

Analgesia

A
  • reduce reactive component of pain
  • reduce sensory threshold
  • more effective against continuous dull pain than sharp, intermittent pain
21
Q

Respiration

A
  • reduce sensitivity of medullary control center

- primary action on repiratiory rate (<3,4/min leading to death)

22
Q

Cough

A
  • antitussive
  • receptors not stereospecific
  • dextromethorphan is antitussive but produces no respiratory depression
23
Q

Dextromethorphan & Respiration

A

dextromethorphan is antitussive but produces no respiratory depression

24
Q

Euphoria

A
  • generally seen with a patient in pain or an addict

- occasionally dysphoric

25
Q

Methadone

A
  • synthetic my agonist
  • 85% oral bioavailability
  • t1/2 25-52 hours (long t1/2, less withdrawal)
    — withdrawal mild though prolonged compared to morphine
  • pharmacological actions virtually identical to morphine
  • cross-tolerance and dependence with morphine
    ** oral maintenance programs for heroin users **
    — heroine wont work if they’re on methadone (because of cross-tolerance)
26
Q

Fentanyl

A
  • highly potent mu agonist
  • actions similar to morphine but 100x more potent
  • used in anesthesia
    — rapid onset, short duration of action
  • transdermal patches and oral lozenge
27
Q

Oxycodone

A
  • semi-synthetic moderate mu agonist
  • need biotransformation for activity
  • high oral bioavailability
  • metabolites can accumulate and cause renal failure
  • widely used to treat terminal cancer
28
Q

Oxymorphone

A
  • Very potent mu agonist (10x more than morphine)

- prominent euphoric effects

29
Q

Pentazocine

A
  • kappa agonist (causes anxiety)
  • weak mu partial agonist
  • less effective than morphine
  • used for mild-to-moderate pain
  • low abuse potential; can’t get high off it
30
Q

Buprenorphine

A
  • high affinity mu partial agonist
  • prolonged t1/2 due to slow dissociation from mu receptor
  • slow mild withdrawal
  • FDA approved as an alternative to methadone for treatment of opioid dependence
31
Q

Additional Opiate Agonist Indications

A
  • Cough (dextromethorphan)

- Diarrhea (Loperamide)

32
Q

Dextromethorphan

A
  • used to treat cough
  • does NOT bind to the mu receptor
  • binds to the receptor which mediates cough suppression
  • no abuse potential
  • large TI
33
Q

Loperamide

A
  • diarrhea
  • acts locally to diminish the peristaltic refleX
  • poorly absorbed, restricted to gut
  • not absorbed enough elsewhere to cause effect (poor CNS penetration)
  • low abuse potential
34
Q

Pharmacological activity of opioid antagonists dependent on:

A
  • whether endogenous opioids have been released
  • whether an opiate agonist has been administered previously
  • the pharmacological profile of the opiate
  • the degree to which physician dependence to an opiate has developed
35
Q

Halo one, Naltrexone, and Nalmefene

A

ANTAGONISTS at MOP, KOP, and DOP
— work against all receptors
- reversibility of a drug’s effect
- no pharmacological utility when used alone
- reverse all pharmacological effects mediated by mu and kappa receptors
- precipitates withdrawal syndrome in patients physically dependent

36
Q

Naloxone

A
  • short t1/2

- repeated doses may be needed

37
Q

Naltrexone and Nalmefene

A
  • longer t1/2
38
Q

Naloxone and Nalmefene absorption

A
  • not well absorbed orally

- better IV

Pharmacology Test 3 (9 decks)

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