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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
What is absorption?
how fast the drug gets into the system
26
What is distribution?
how well the drug gets to its site of action
27
What is metabolism?
how quickly the drug gets broken down
28
What is excretion?
rate at which drug (metabolites) are eliminated from the body
29
What is the absorption consideration?
drugs/routes of administration with faster onset are more likely to be abused (e.g. heroin vs. morphine, IV vs. oral)
30
What is the distribution consideration?
drugs can get sequestered in fat and plasma, requiring larger doses
31
What is the metabolism consideration?
dictates dosing schedule - first pass metabolism affects bioavailability (e.g. naloxone) - drugs can induce/inhibit the metabolism of themselves or other drugs
32
What two things does high efficacy mu opioid receptor agonists (narcotics) do?
cause stupor and drowisness
33
What are my 6 HIGH efficacy agonist?
1. Heroin 2. Morphine 3. Methadone 4. Meperidine 5. Fentanyl 6. Remifentanil
34
What is unique about Heroin?
- Not used in the U.S. (U.K.) - Crosses the BBB faster than morphine - Converted to morphine in the brain - Schedule I
35
What is unique about Morphine?
- Patient controlled analgesia | - Schedule II
36
What is unique about Methadone?
- Used for heroin addicts (sub therapy) - Good F - Long lasting (t 27) - Schedule II
37
What is unique about Meperidine?
- anticholinergic activity (mydriasis and tachycardia) | - Schedule II
38
What is unique about Fentanyl?
- 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
What is unique about Remifentanil?
- Metabolized by plasma esterases - 8-20min t1/2 EXTREMELY SHORT!!! - rare abuse - Schedule II
40
What are my 3 moderate efficacy mu agonists?
1. Codeine 2. Hydrocodone 3. Oxycodone
41
What is unique about codeine?
- plant derived opioid - often used w/ acetomenophen (Tylenol) or ibuprophen (Nurofen Plus) - Schedule III
42
What is unique about hydrocodone?
- semi synthetic opioid from codeine - often used with acetomenophen (Vicodin) or ibuprophen (Vicoprofen) - Schedule II
43
What is unique about Oxycodone?
- do NOT crush, cut, or chew - OxyContin= OPIOID ABUSE EPIDEMIC -CYP450 converts oxycodone to oxymorphone (high efficacy) -Schedule II
44
Acetaminophen + codeine
Tylenol III
45
Acetaminophen + hydrocodone
Vicodin, Lorteb
46
Acetaminophen + meperidine
Demerol
47
Acetaminophen + oxycodone
Percocet, Tylox
48
Acetaminophen + pentazocine
Talacen
49
Aspirin + codeine
Ascriptin
50
Aspirin + oxycodone
Percodan
51
Aspirin + pentazocine
Talwin
52
When should patients not take Tylenol?
when taking a opioid containing acetaminophen
53
Opioid agonist + NSAID=
additive or synergistic effects
54
What are my 4 partial/low efficacy agonist?
1. Pentazocine 2. Nalbuphine 3. Buprenorphine 4. Buprenorphine + naloxone
55
Schedule IV low efficacy agonist?
Pentazocine
56
What is the unscheduled low efficacy drug?
Nalbuphine
57
What is the only drug opioid not regulated in the U.S.?
Nalbuphine
58
What low efficacy agonist is often used by dx abusers due to its less potential to cause respiratory effects?
buprenorphine
59
Experienced opioid abusers will use buprenorphine by what route?
IV
60
What is unique about buprenorphine?
- 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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