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ABFT Exam > Module 9: Opiates & Opioids > Flashcards

Module 9: Opiates & Opioids Flashcards

1
Q

opium poppy

A

Papaver Somniferum

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2
Q

Miosis

A

Pinpoint pupils (constricted)

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3
Q

Follows 1st-pass metabolism when taken orally
Low oral bioavailability (more potent when taken other ways)
Slow to cross blood-brain barrier
Metabolite of codeine and heroin
Duration of action: 4-5 hours

A

Morphine

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4
Q

Endogenous Opioid Peptide that bind to mu opioid receptors.

A

Endorphins

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5
Q

Endogenous Opioid Peptide that bind to delta opioid receptors primarily.

A

Enkephalins

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6
Q

Endogenous Opioid Peptide that bind to kappa opioid receptors primarily.

A

Dynorphins

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7
Q

3 types of Opioid receptors

A

Mu, Kappa, Delta

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8
Q

Peak of Opioid Abstinence Syndrome

A

36-72 hours

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9
Q

Duration of Opioid Abstinence Syndrome

A

7-10 days

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10
Q

Beginning of Opioid Abstinence Syndrome

A

6-8 hours

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11
Q

Category of Opioids including morphine, codeine, hydromorphone, etc.

A

Phenanthrenes

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12
Q

Category of Opioids including Fentanyl, sufentanil, furanryl fentanyl, etc.

A

Phenylpiperidines

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13
Q

Opioid Classifications (mode of action)

A

Agonist, Antagonist, Mixed Agonist/Antagonist

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14
Q

Agonist
Highest oral bioavailability
10-15% metabolized to morphine
Duration of analgesia: 3-4 hours

A

Codeine

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15
Q

Agonist
2-3 times more potent than morphine (penetrates BBB)
poor oral biovavailbility
rapid metabolism to 6MAM (half life = 2-6 min) then to morphine

A

Heroin

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16
Q

Agonist Derivative of Codeine
metabolized to hydromorphone and dihydrocodeine
Duration of analgesia: 3-5 hours

A

Hydrocodone

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17
Q

Agonist
metabolite of hydrocodone and morphine (minor)
More potent than morphine
Duration of analgesia: 4-5 hours

A

Hydromorphone

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18
Q

Agonist
Derived from thebaine
15% metabolized to oxymorphone
Duration of analgesia: 3-4 hours

A

Oxycodone

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19
Q

Agonist
Metabolite of Oxycodone
Duration of analgesia: 3-4 hours

A

Oxymorphone

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20
Q

Agonist
Most potent and fast-acting opioid
50-200x more potent than Morphine
Transdermal patches can give delayed concentrations for 12-24 hrs
Duration of analgesia: 1-15. hours

A

Fentanyl

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21
Q

Agonist
Long elimination half life
Metabolizes to EDDP and EDMP
Duration of analgesia: 4-6 hours

A

Methadone

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22
Q

Atypical opioid agonist
Metabolite (o-dm-) is 2x more potent (contributes to toxicity)
Duration of analgesia: 4-6 hours

A

Tramadol

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23
Q

Agonist used to decrease diarrhea
Doesn’t have effects like morphine except in high doses (do to opioid receptor activities)
“poor man’s methadone”

A

Loperamide

24
Q

Antagonist
Narcan
Rapid action (minutes)
Short duration of action (2 hours)

A

Naloxone

25
Q

Antagonist
Used to treat addition after withdrawal complete
Used for chronic alcoholics

A

Naltrexone

26
Q

Mixed Agonist/Antagonist
Produces withdrawal if an opioid agonist is also taken
Partial agonist at mu receptor and kappa antagonist
Available in preparation w/ naloxone (Suboxone) or by itself (Buprenex)
Inactive metabolite (nor-)

A

Buprenorphine

27
Q

Location of opioid metabolism in body.

A

Liver

Metabolized to more polar compounds

28
Q

Primary mechanisms of metabolism of opiods.

A

N-dealkylation, conjugation of hydroxyl groups, hydrolysis

29
Q

3 Opioids where the metabolites account for most of the desired effects

A

Codeine, Heroin, Tramadol

30
Q

Isozyme largely responsible for first-pass metabolism of Opiods

A

CYP2D6

31
Q

Morphine is primarily excreted as:

A

Morphine-3-glucuronide (inactive)

*Morphine-6-glucuronide (more potent than morphine)

**Think about how codeine is less potent and that differs from morphine at 3 group also

32
Q

Opioid effects on:

Pupils
Eye Reaction to Light
Pulse
Blood Pressure
Body Temperature

A

Pupils - constricted
Eye Reaction to Light - little to none
Pulse - down
Blood Pressure - down
Body Temperature - down

33
Q

3 main signs of opioid ODs

A

CNS depression (respiratory depression)
Coma
Pinpoint Pupils

34
Q

Compound present indicates ingestion of poppy seeds

A

Thebaine

35
Q

The opioid receptor that produces central depression, analgesia, miosis, reduced gastrointestinal motility

A

Mu

36
Q

Opioid used clinically since 1957, but recommended for removal from the U.S. drug market in 2010.

A

Propoxyphene

37
Q

When codeine is taken as a parent drug, approximately _______ is metabolized to morphine.

A

10%

38
Q

Semisynthetic analgesic agonist derived from codeine that is used in cough syrups:

A

Hydrocodone

39
Q

In the hair matrix, 6-MAM has been detected in hair of heroin users at typically _______ concentrations than for morphine.

The same
smaller
greater
6-MAM not present in hair

A

Greater

40
Q

Opioids are _______ in nature.
Basic, Neutral, or Acidic

A

Basic

41
Q

Organic solvents are often used to extract opioids from aqueous mixtures in the pH range of:

A

8-10

42
Q

True or False: Opiates cause pupil dilation.

A

False

They cause constriction.

43
Q

Has less potency relative to morphine:

Hydrocodone, Oxycodone, Fentanyl, Codeine, Methadone

A

Codeine

44
Q

_______ is the major metabolic route for opioids that contain available hydroxyl (OH) groups.

Sulfation, Demethylation, Glucuronidation, Dealkylation, Methylation

A

Glucuronidation

45
Q

True or False: Only the levorotatory isomer of morphine is a potent analgesic.

A

True

46
Q

Successfully used for the treatment of respiratory depression after postsurgical opioid administration:

Buprenorphine, Levorphanol, Methadone, Nalbuphine, Fentanyl

A

Nalbuphine

47
Q

This metabolite is more potent than morphine:

Morphine-6-glucuronide, Codeine, Tramadol,
Morphine-3-glucuronide, Morphine

A

Morphine-6-glucuronide

48
Q

Acidic hydrolysis of conjugated metabolites should be done with caution as this analyte may be degraded.

Dihydrocodeine, Oxymorphone, Hydromorphone, 6-MAM, Codeine

A

6-MAM

49
Q

Opioid Metabolism takes place primarily in the _______.

Liver, Brain, Kidney, Urine, Spinal Fluid

A

Liver

50
Q

This drug the longest half-life out of the listed choices.

Morphine, Tramadol, Methadone, Hydrocodone, Fentanyl

A

Methadone

51
Q

This opioid has approximately 100-200x the analgesic potency of morphine.

A

Fentanyl

52
Q

True or False: Rapid deaths are often characterized by a higher ratio of the concentrations of free morphine to total morphine.

A

True

Total morphine includes conjugated morphine - body has had time to process and metabolize morphine. Free morphine has not been conjugated for excretion.

53
Q

Typical pKa values for Opioids are:
1.2-3.4
3.2-4.6
7.6-8.9
9.2-10.6
>10

A

7.6-8.9

54
Q

Used to manage intestinal upset and has been used to lessen withdrawal or produce euphoric effects:

Alfentanil, Loperamide, Difenoxin, Hydromorphone, Diphenoxylate

A

Loperamide

55
Q

The presence of a low concentration of codeine relative to morphine may indicate the use of _______.

Codeine only
Morphine only
Codeine and morphine
Heroin
A, C and D

A

A, C and D

*Think: morphine does not metabolize to codeine so it can’t be only morphine. Codeine metabolizes to Morphine.

56
Q

True or False: All opioids are highly protein bound.

A

False

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