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Pharmacology 2 > Opioid Analgesics, Local Anesthetics, & Muscle Relaxants > Flashcards

Opioid Analgesics, Local Anesthetics, & Muscle Relaxants Flashcards

1
Q

What year was morphine discovered?

A

1806

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2
Q

What is the active form of opium poppies?

A

morphine

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3
Q

Why was morphine discovery so important?

A

revolutionized battlefield injuries

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4
Q

What year was opioids regulated?

A

1970

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5
Q

When was extended formulations developed for opioIds?

A

1990s

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6
Q

Why was extended formulations developed for opioids?

A

to make them WITHOUT ABUSE

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7
Q

What do ascending pain pathways do?

A

Fast transmission of cold, pressure, and acute pain

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8
Q

What do c-fibers pain pathways do?

A

slow transmission of heat, neuropathic, and second pain

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9
Q

What do descending inhibitory pain pathway?

A

central modulation of incoming pain signals by serotonin (5-HT) and norepinephrine (NE)

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10
Q

Burning, deep, diffuse, long lasting pain is felt in what pathway?

A

C fibers

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11
Q

Sharp, immediate, short lived pain is felt in what pathway?

A

ascending A fibers

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12
Q

Incoming pain signs is felt in what pathway?

A

descending inhibitory

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13
Q

Analgesia?

A

REDUCED perception of pain, despite knowledge that the pain is still there (tolerability)

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14
Q

What are the 2 mechanisms by which opioids work on the pain pathways?

A

1) blocking ascending by inhibiting primary and secondary afferent pain fibers
2) indirectly enhancing the activity of descending inhibitory pain

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15
Q

What are 3 opioid receptor subtypes?

A

Mu, Delta, and Kappa

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16
Q

What most opioid receptor subtype?

A

Mu

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17
Q

Why isn’t delta agonist used?

A

due to induced CONVULSIONS

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18
Q

Why isn’t kappa agonist used?

A

due to severe Dyseuphoria effects

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19
Q

Where is a single Kappa agonist used in for itch (psoriasis)?

A

in Japan

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20
Q

What is a pro-drug for morphine?

A

heroin

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21
Q

What are three strong agonist?

A
  • Fentanyl
  • Morphine
  • Methadone
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22
Q

What are two moderate agonist?

A

Oxycodone and codeine

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23
Q

What is one weak agonist?

A

Propoxyphene

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24
Q

What is two mixed agonist and antagonist?

A

buprenorphine and nalbuphine

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25
Q

What is absorption?

A

how fast the drug gets into the system

26
Q

What is distribution?

A

how well the drug gets to its site of action

27
Q

What is metabolism?

A

how quickly the drug gets broken down

28
Q

What is excretion?

A

rate at which drug (metabolites) are eliminated from the body

29
Q

What is the absorption consideration?

A

drugs/routes of administration with faster onset are more likely to be abused (e.g. heroin vs. morphine, IV vs. oral)

30
Q

What is the distribution consideration?

A

drugs can get sequestered in fat and plasma, requiring larger doses

31
Q

What is the metabolism consideration?

A

dictates dosing schedule

  • first pass metabolism affects bioavailability (e.g. naloxone)
  • drugs can induce/inhibit the metabolism of themselves or other drugs
32
Q

What two things does high efficacy mu opioid receptor agonists (narcotics) do?

A

cause stupor and drowisness

33
Q

What are my 6 HIGH efficacy agonist?

A
  1. Heroin
  2. Morphine
  3. Methadone
  4. Meperidine
  5. Fentanyl
  6. Remifentanil
34
Q

What is unique about Heroin?

A
  • Not used in the U.S. (U.K.)
  • Crosses the BBB faster than morphine
  • Converted to morphine in the brain
  • Schedule I
35
Q

What is unique about Morphine?

A
  • Patient controlled analgesia

- Schedule II

36
Q

What is unique about Methadone?

A
  • Used for heroin addicts (sub therapy)
  • Good F
  • Long lasting (t 27)
  • Schedule II
37
Q

What is unique about Meperidine?

A
  • anticholinergic activity (mydriasis and tachycardia)

- Schedule II

38
Q

What is unique about Fentanyl?

A
  • Driving overdose epidemic
  • Very potent x100 morphine (much less of dx needed)
  • PRIMARILY FOR CANCER PAIN
  • t1/2 shorter than heroin
  • Transdermal used to decrease abuse
  • Schedule II
39
Q

What is unique about Remifentanil?

A
  • Metabolized by plasma esterases
  • 8-20min t1/2 EXTREMELY SHORT!!!
  • rare abuse
  • Schedule II
40
Q

What are my 3 moderate efficacy mu agonists?

A
  1. Codeine
  2. Hydrocodone
  3. Oxycodone
41
Q

What is unique about codeine?

A
  • plant derived opioid
  • often used w/ acetomenophen (Tylenol) or ibuprophen (Nurofen Plus)
  • Schedule III
42
Q

What is unique about hydrocodone?

A
  • semi synthetic opioid from codeine
  • often used with acetomenophen (Vicodin) or ibuprophen (Vicoprofen)
  • Schedule II
43
Q

What is unique about Oxycodone?

A
  • do NOT crush, cut, or chew
  • OxyContin= OPIOID ABUSE EPIDEMIC
    -CYP450 converts oxycodone to oxymorphone (high
    efficacy)
    -Schedule II
44
Q

Acetaminophen + codeine

A

Tylenol III

45
Q

Acetaminophen + hydrocodone

A

Vicodin, Lorteb

46
Q

Acetaminophen + meperidine

A

Demerol

47
Q

Acetaminophen + oxycodone

A

Percocet, Tylox

48
Q

Acetaminophen + pentazocine

A

Talacen

49
Q

Aspirin + codeine

A

Ascriptin

50
Q

Aspirin + oxycodone

A

Percodan

51
Q

Aspirin + pentazocine

A

Talwin

52
Q

When should patients not take Tylenol?

A

when taking a opioid containing acetaminophen

53
Q

Opioid agonist + NSAID=

A

additive or synergistic effects

54
Q

What are my 4 partial/low efficacy agonist?

A
  1. Pentazocine
  2. Nalbuphine
  3. Buprenorphine
  4. Buprenorphine + naloxone
55
Q

Schedule IV low efficacy agonist?

A

Pentazocine

56
Q

What is the unscheduled low efficacy drug?

A

Nalbuphine

57
Q

What is the only drug opioid not regulated in the U.S.?

A

Nalbuphine

58
Q

What low efficacy agonist is often used by dx abusers due to its less potential to cause respiratory effects?

A

buprenorphine

59
Q

Experienced opioid abusers will use buprenorphine by what route?

A

IV

60
Q

What is unique about buprenorphine?

A
  • can be combined with naloxene
  • can manage pain even at low dose
  • Used more over sea
  • Schedule V

Pharmacology 2 (9 decks)

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