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Psychopharmacology > Chapter 11: Opioids > Flashcards

Chapter 11: Opioids Flashcards

1
Q

Opioid drugs are narcotic analgesics, meaning?

A

They provide pain reduction without producing unconsciousness.
State of relaxation or sleep

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2
Q

High doses of opioid drugs, seeing that they are narcotic analgesics, cause what?

A

Coma and death

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3
Q

Opioid drugs produce a sense of

A

Euphoria

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4
Q

Opioid drugs are the best ______ known.

A

Painkillers

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5
Q

Opium is an extract of the _____.

A

Poppy plant

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6
Q

Recreational use of opium is mentioned in _____

A

The Odyssey (9th century B.C.)

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7
Q

Active ingredients of opium

A

Morphine and Codeine

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8
Q

Morphine named after

A

Roman god, “Morpheus”

God of dreams

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9
Q

Codeine has _____ analgesic effects than morphine, _____ side effects and is considered a _____.

A

Less; fewer; potent cough suppressant

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10
Q

Heroin has been used for thousands of years, _____ for both recreation and medicine

A

Egyptians

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11
Q

Eating or smoking opium in ancient _____ countries to replace alcohol consumption, which was prohibited.

A

Islamic

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12
Q

Laudanum was used in 1680 for _____. Ingredients?

A 
Pain relief and cough suppressant
Considered addictive today
Ingredients:
2 oz strained opium
1 oz saffron
1 dram of cinnamon and cloves dissolved in 1 pint of canary wine
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13
Q

Year _____, _____ Act - Opiates and Cocaine
First law to _____ substances. Doctors could no longer treat addiction with _____ because addiction was not classified a medical issue. Revenue generated via _____

A

1914; Harrison

Control; agonists; tax

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14
Q

Structural modification: Heroin

A

When we realized morphine was addictive, heroin was synthesized from morphine to replace it. Considered semi-synthetic because you needed morphine to make it. However, formulation increased its lipid solubility and it was able to reach the brain faster. IV heroin much more potent. More addictive

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15
Q

Heroin is synthesized into _____ in the brain

A

morphine

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16
Q

Morphine to Codeine: _____ group for hydroxyl (OH) group

A

methoxy (CHO3)

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17
Q

Morphine to Codeine: _____ group for hydroxyl (OH) group

A

methoxy (CH3O)

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18
Q

Taking buprenorphine would present any opioid with _____.

A

competition at the receptors site

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19
Q

Naloxone is released and _____ the effects of buprenorphine or any other opioid that is taken to enhance the effects

A

blocks

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20
Q

(1) Partial agonists
What’s the name?
Bind to the receptors with _____
_____ biological effect as compared to full agonist.
_____ potent and efficacious, _____ risk of respiratory depression

A

Buprenorphine

high affinity; reduced; less; reduced

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21
Q 
(2) Pure antagonists
What's the name?
Structurally similar to \_\_\_\_\_
Administration produces \_\_\_\_\_
Can prevent or reverse the effect of \_\_\_\_\_.
A

Naloxone (narcan)
morphine/heroine
no effect; opioids

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22
Q

What makes up suboxone?

Considered a _____

A

Buprenorphine + naloxone.

Partial agonist; Antagonist is activated if sublingual route is avoided (route of administration)

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23
Q

What makes up suboxone?

Considered a _____

A

Buprenorphine + naloxone.

Partial agonist; Antagonist is activated if sublingual route is avoided (route of administration)

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24
Q

Opioids medically
-Routes of administration
_____% of individuals prescribed pain meds become addicted

A

IM or oral

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25
Q

Opioids recreationally
-Routes of administration
_____ bioavailability
_____ onset

A

Inhalation, intranasal, subcutaneous injection
Higher bioavailability
Faster onset

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26
Q

Effects of opioids on the CNS are related to _____.

A

dose and rate of absorption

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27
Q

Low dose opioids:

Effects

A

Pain relief, constricted pupils

Drowsiness, inability to concentrate, dreamy sleep, decreased sensitivity to the environment.

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28
Q

Low dose opioids

Hypothalamus:

A

Decreased appetite, drop in BT, reduced sex drive, hormone disregulation

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29
Q

Low dose opioids

Limbic system effects

A

Anxiety, aggressiveness, and feelings of inadequacy. Increase subsequent drug use

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30
Q

Psychological pain may be derived from actions within the _____

A

limbic system

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31
Q

Increased subsequent drug use encouraged through _____

A

Negative reinforcement

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32
Q

Increased subsequent drug use encouraged through _____

A

Negative reinforcement

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33
Q

GI Tract: drugs are now designed so they don’t cross the _____

A

BBB

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34
Q 
High dose opioids:
Effects
Morphine affects regions of the \_\_\_\_\_
Morphine also affects the \_\_\_\_\_. 
     Causes \_\_\_\_\_
     Severe bacterial and parasitic diseases.
Effect is resistant to \_\_\_\_\_
A

Sedative effects become stronger, unconsciousness
Decreased body temperature and blood pressure, coma, respiratory failure
brainstem; GI tract; constipation
tolerance

35
Q

_____ becomes a classic sign of OD..ultimately occurs due to respiratory failure.

A

Pupil constriction

36
Q

GI Tract: drugs are now designed so they don’t cross the _____

A

BBB

37
Q

4 opioid receptors

A

μ (mu)
δ (delta)
κ (kappa)
NOP-R

38
Q

The 4 opioid receptors are slow-acting or _____

A

Metabotropic

39
Q

μ (mu) has a high affinity for

A

Morphine

40
Q

μ (mu) produce analgesic effects when located in

A

Thalamus, periaqueductal gray, median raphe, spinal cord

41
Q

μ (mu) produce Positive reinforcement effects when located in

A

Nucleus accumbens

42
Q

μ (mu) receptors in the brainstem causes

A

Respiratory depression, cough suppressant, nausea, vomiting

43
Q

δ-receptors are predominantly found in _____.

A

forebrain structures

44
Q

Possible effects of δ-receptors (4)

A

Modulating olfaction, motor integration, reinforcement, and cognitive function.

45
Q

Areas of overlap with μ-receptors suggest modulation of both _____ and _____.

A

spinal and supraspinal analgesia

46
Q

κ- receptors located in hypothalamus and pituitary gland cause

A

Pain perception, gut motility, temperature control, neuroendocrine fx.

47
Q

The endogenous ligand for opioid receptors

A

Endorphins and enkephalins

48
Q

The ligand for kappa opioid receptors is

A

dynorphin

49
Q

Peptides made from large precursor peptides
Manufactured in _____
Packaged with enzymes called _____

A

POMC and proenkyphalin
Soma
Proteases

50
Q

3 ways opioids inhibit nerve activity

A
  1. Postsynaptic inhibition
  2. Axoaxonic inhibition
  3. Presynaptic autoreceptors
51
Q

All four types of opioid receptor are also coupled to inhibitory _____

A

G proteins (Gi)

52
Q

Axoaxonic inhibition

A

Receptors activate G proteins, close Ca2+ channels

Reducing the release of neurotransmitter

53
Q

Adenylyl cyclase inhibitions will inhibit

A

second messenger cAMP

54
Q

All four types of opioid receptor are also coupled to inhibitory _____

Which may be partly responsible for opioid-induced ion channel changes.

A

G proteins (Gi)

55
Q

G proteins inhibit

A

adenylyl cyclase

56
Q

Adenylyl cyclase inhibitions will inhibit

A

second messenger cAMP.

57
Q

cAMP inhibition

A

May be partly responsible for opioid-induced ion channel changes.

58
Q

With electrical self-stimulation, opioids _____ threshold

A

reduce

59
Q

Opioids have significant _____ properties.

A

Reinforcing

60
Q

With self-administration, pre-treatment with an opioid _____ responding

A

Reduces

61
Q

With self-administration, pre-treatment with naloxone _____ responding

A

Increases

62
Q

The _____ pathway contributes to opioid reinforcement.

A

dopaminergic mesolimbic

63
Q

Administration of opioids and β-endorphin:
_____ cell firing and release of DA in NAcc
_____ threshold of electrical self-stimulation
Produces _____

A

Increase; reduces; CPP

64
Q

Administration of the κ- agonist (dynorphin):
_____ rate of cell firing and release of DA in NAcc
_____ threshold of electrical self-stimulation
Produces _____

A

Decreases; Increases; conditioned place avoidance

65
Q

Long-Term Opioid Use leads to _____ that produce _____.

A

neuroadaptive changes that produce tolerance, sensitization, dependence

66
Q

κ-receptors (dynorphin) can reduce the release of DA via same mechanisms as opioid drugs and β-endorphin
Causes _____

A

dysphoria

67
Q

Rapid tolerance to

A

analgesia

68
Q

No tolerance for

A

constipation or pupil constriction

69
Q

Cross-tolerance among the opioids also exists such as in _____

A

Heroin and codeine

70
Q

Rapid tolerance to

A

analgesia

71
Q

No tolerance for

A

constipation or pupil constriction

72
Q

The locus coeruleus and the periaqueductal gray (PAG) associated with _____

A

physical withdrawal

73
Q

Long-term opioid use: Sensitization
_____ in drug effects that occurs with repeated administration.
_____ or _____ can become sensitized

A

Increase; craving or desire

74
Q

Aversive affects (mental) of withdrawal associated with

A

NAcc

75
Q

The locus coeruleus and the periaqueductal gray (PAG) associated with _____

A

physical withdrawal

76
Q

The classic hypothesis of opioid tolerance and dependence was first developed by _____ in _____

A

Himmelsbach in 1943.

77
Q

When opioids withdrawn, system

A

rebounds

78
Q

After two days of morphine exposure:

The cells adapted to producing _____ cAMP.

A

more

79
Q

When morphine was removed or nalaxone added:

Levels of cAMP _____ significantly.

A

increased

80
Q

Withdrawal can be suppressed by increasing synthesis of _____

A

endorphins

81
Q

Electroacupuncture EA restored the low levels of _____ for precursor peptides in the spinal cord, hypothalamus, and PAG

A

mRNA

82
Q

Most common and effective treatment program for opioid addiction

A

Methadone maintenance program (relieves craving)

83
Q

Ibogaine

A

Alleviates withdrawal

Psychopharmacology (6 decks)

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