Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

BAHS-504 PHARMACOLOGY EXAM 2 > OPIOID ANALGESICS > Flashcards

OPIOID ANALGESICS Flashcards

1
Q

name 2 strong opioid agonist drugs

1.

2.

A
  1. morphine
  2. methadone (dolophine)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

name a moderate opioid agonist drug

A

codeine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

name 2 mixed opioid agonist-antagonist drugs

1.

2.

A
  1. Pentazocine (Talwin)
  2. Buprenorphine (Buprenex)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

name 2 opioid antagonist drugs

1.

2.

A
  1. Naloxone (Narcan)
  2. Naltrexone (Re Via)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

name the two categories that pain can be divided into:

1.

2.

A
  1. acute pain
  2. chronic pain
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

acute pain can be further divided into two more categories. name them:

1.

2.

A
  1. phasic pain
  2. tonic pain
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

define phasic pain

A

sharp pricking types of pain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

define tonic pain

A

dull, throbbing, aching pain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

definition:

an unpleasant sensory and emotional experience that normally serves to alert an individual to actual or potential tissue damage

A

pain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

definition:

a state of not being able to fel pain, without the loss of consciousness

A

analgesia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

definition:

durgs that reduce pain and induce analgesia

A

analgesics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

definition:

durgs derived from the juice of the opium poppy, such as morphine and codeine

A

opiates

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

definition:

natural or synthetic compounds with actions that mimic those of morphine

A

opioids

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

definition:

endogenous opioid peptides, such as endorphins, dynorphins, and enkaphalins

A

opiopeptins

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

definition:

a term dervied from the Greek word for stupor. used primarily as a legal term for drugs that cause dependence

A

narcotic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

indications for therapeutic uses of opioids:

1.

2.

3.

4.

A
  1. relief of intense pain
  2. relief of cough
  3. treatment of diarrhea
  4. treatment of acute pulmonary edema
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

mechanism of action:

how do opioids produce analgesia?

A

opioids interact with (endogenous) opioid receptors, which are activated by endogenous opioid peptides (opiopeptins: endorphines, dynorphins, and enkaphalins)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

where are opioid receptors primary localized?

A

brain and spinal cord regions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

what purpose do opioid receptors serve?

A

opioid receptors are involved in the transmission and modulation of pain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

name the three major families of endogenous opioid peptides:

1.

2.

3.

A
  1. enkaphalins
  2. dynorphins
  3. endorphins
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

when are opioid peptides released?

A

during stress such as pain or anticipation of pain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

what functions do endogenous opioid peptides serve?

A

act as peptide neurotransmitters, participating in the modulation of pain, stress, mood, reinforcement, dependence and homeostatic processes such as eating

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

name the three types of opioid receptors

1.

2.

3.

A
  1. Delta receptors (OP1/DOP)
  2. Kappa receptors (OP2/KOP)
  3. Mu receptors (OP3/MOP)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

how many transmembrane domains to the three primary opioid receptors have?

A

7 transmembrane domains

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

what are the three major opioid receptors primarily attached to?

A

inhibitory types of G-proteins

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

describe the presynaptic action of the three major opioid receptors

A

inhibits voltage-gated calcium channels an d decreases the release of neurtransmitters from presynaptic terminals of nociceptive primary afferents

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

descibe the postsynaptic action of mu receptors

A

activates an inwardly rectifying potassium channel (leading to hyperpolarization) and thus inhibits postsynaptic, second-order pain transmission neurons

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

mu receptors have high affinity for:

1.

2.

3.

A
  1. morphine and related opioid drugs
  2. enkephalins
  3. beta-endophin

endorphins>enkephalins>dynorphins

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

delta receptors have a high affinity for:

1.

2.

A
  1. enkephalins
  2. beta-endophin

enkephalins>endorphins & dynorphins

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

kappa receptors have a high affinity for:

1.

A
  1. dynorphin

dynorphins >> endorphins and enkephalins

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

what is the role of mu receptors?

A

mediate opioid-induced analgesia and positve reinforcement, as well as respiratory depression, miosis, decreased GI motility, and neuroendocrine effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

what is the role of delta receptors?

A

antinociception, motor integration, and cognitive function

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

what is the role of kappa receptors?

A

regulation of food uptake, temperature control, GI motility, pain perception, and neuroendocrine function

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

how is phasic pain produced?

A

noxious stimuli – heat, mechanical and chemical irritants

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

what pain pathway does phasic pain follow?

A

the ascending pain transmission pathway

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

describe A-alpha and A-beta fibers of primary afferent axons

A

myelinated

large diameter

detect proprioception and light touch

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

describe A-delta fibers of primary afferent neurons

A

lightly myelinated

medium diameter

detect nocioception (mechanical, thermal, chemical)

thermal threshold ~ 53ºC (type I)

thermal threshold ~ 43ºC (type II)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

describe C fibers of the primary afferent axon

A

unmyelinated

small diameter

innocuous temperature, itch

nociception (mechanical, thermal, chemical)

thermal threshold ~43ºC

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

trace the ascending pain transmission pathway of phasic pain

A

the stimulus is transmitted through the fast-conducting, thinly myelinated A-delta fibers that enter the spinal through the dorsal horn. the pathway immediately crosses over and proceeds along the lateral spinothalamic tract

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

trace the ascending pain transmission pathway of tonic pain

A

sensory input is transmitted through the unmyelinated, slow-conducting C fibers that enter the spinal cord through the dorsal horn. the major ascending pathways for tonic pain are mutisynaptic pathways of the spinorectal and paleospinothalamic tracts

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

trace the descending pain modulatory pathways

A

the major descending pathways project from the cortex to midbrain periaquectoal gray (PAG), which then make connections to neurons extending into the rostroventral region of the medulla (RVM). the PAG and the RVM have extensinve reciprocal connections and provide descending projections to the dorsal horn of the spinal cord

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
42
Q

what role do descending pathways play on ascending pain transmission neurons?

A

descending pathways play an inhibitory role on the ascending pain transmission neurons

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
43
Q

how do opioids produce direct analgesic effect on the spinal cord?

A

inhibit the relase of excitatory nerutoransmitters from primary afferents and inhibit the dorsal horn pain transmission neurons

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
44
Q

name two places where opioid receptors are found in the ascending pain transmission pathways

A

primary afferents

spinal cord pain transmission neurons

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
45
Q

where are opioid receptors found in the descending pain modulatory pathway?

A

the PAG (periaqueductal gray) in the midbrain and the RVM (rostroventral region of the medulla)

46
Q

how do opioids produce an indirect analgesic effect on the spinal cord?

A

inhibit the inhibitory (GABAergic) interneurons in the descending pathways, thus activating the pain inhibitory neurons that project to the spinal cord, leading to the inhibition of pain transmission neurons

47
Q

what actions do opioid receptors produce at the brainstem?

A

cough center of the medulla

respiratory control center

chemoreceptor trigger zone

control of blood pressure

control of pupillary diameter

control of respiration

nausea and vomiting

48
Q

name three sites where opioid receptor distribution/ action is linked to side effects

A

brain stem, hypothalamus, GI tract

49
Q

what actions do opioid receptors produce at the hypothalamus?

A

neuroendocrine secretion

50
Q

what actions do opioid receptors produce at the GI tract?

A

increase smooth muscle tone

decrease motility

51
Q

what effects do opioids have on the CNS?

(7)

A
  1. analgesia
  2. euphoria or dysphoria
  3. sedation
  4. respiratory depression
  5. cough suppression
  6. miosis
  7. emesis
52
Q

what are the cardiovascular effects of opioids?

A

hypotension and vasodilation

53
Q

what are the gastrointestinal effects of opioids?

A

(increased intestinal smooth muscle tone)

constipation and relief of diarrhea

54
Q

what administration method can you use to minimize the negative cardiovascular effects of opioids?

A

epidural administration

55
Q

what are the genitourinary effects of opioids?

A

urinary retention, prolongation of labor

56
Q

what are the neuroendocrine effects of opioids?

A

stimulation of antidiuretic hormone and prolactin release

inhibition of luteinizing hormone release

57
Q

what are the dermal effects of opioids?

A

flushing, pruritis, urticaria (hives)

58
Q

define tolerance

A

decreased responsiveness to a drug

59
Q

what effects of opioids can a tolerance be built up for?

A

analgesic, euphoric, sedative, emetic and respiratory dependent effects

60
Q

what effects of opioid use can you not build a tolerance for?

A

miotic and constipating actions

61
Q

can cross tolerance be built among opioid analgesics?

A

yes

62
Q

definde dependence

A

an adaptive state that requires the presence of a drug to maintain cellular homeostasis

63
Q

describe the effects of withdrawal syndrome

A

strong flu like symptoms,

goose flesh (cold-turkey)

muscle tremors and twitches (kicking the habit)

abdominal cramps and diarrhea

increased HR and BP

hyperventilation

anxiety and hostility

64
Q

what are strong opioid agonists useful in treating?

A

severe pain

65
Q

what receptors do strong opioid agonists show the highest affinity for?

A

mu-receptors

66
Q

what is the major active ingredient in opium?

A

morphine (10%)

67
Q

what is the duration of action of morphine?

A

4-6hr

68
Q

what is morphine’s active metabolite?

A

morphine-6-glucuronide

69
Q

what is morphine most useful in treating?

A

severe pain associated with trauma, myocardial infarction, and cancer

70
Q

acetylmorphine is better known as:

A

heroin

71
Q

what effect does acetylation have on heroin?

A

makes it more lipid soluble and fast acting

72
Q

what category of controlled substances is heroin?

A

heroin is a Schedule I Controlled Substance

73
Q

what type of opioid agonists are methadone, meperidine, and fentanyl?

A

strong opioid agonists

74
Q

dolophine is better known as:

A

methadone

75
Q

what opioid is the most orally effective, and what is it’s duration of action

A

methodone; orally, the duration of action is 15-20hr

76
Q

what is methadone most commonly used to treat?

A

detoxification and controlled withdrawal of addicts from heroin and morphine

77
Q

which strong opioid agonist is less potent than morphine?

A

meperidine

78
Q

demerol is more commonly known as

A

demerol

79
Q

what is the duration of action of meperidine

A

2-4hr

80
Q

what is meperdine most commonly used to treat?

A

used as an obstetric or postsurgical analgesic

81
Q

what opioid, otherwise known as sublimaze, is 80X more potent than morphine?

A

fentanyl

82
Q

describe two characteristics that make fentanyl preferable as an adjunct to general anesthesia

A

rapid onset (< 5min)

very short duration of action (15-30min)

83
Q

describe how moderate opioid agonists compare to strong opioid agonists

A

moderate opioid agonsits are less potent and have lower abuse potential

84
Q

what are moderate opioids most commonly used to treat?

A

moderate pain (in combination with non-opioid analgesics)

85
Q

what opioid is present at ~ 0.5% concentration in opuim?

A

codeine

86
Q

how is codeine metabolized to produce analgesic effects?

A

codeine is metabolized to morphine for analgesic activity

87
Q

what is codeine commonly given with (orally) for treatment of mild to moderate pain?

A

aspirin and acetaminophen

88
Q

what opioid is commonly mixed with cough syrups to alleviate or prevent coughs?

A

codeine

89
Q

which moderate opioid agonist, otherwise known as Ralivia, is a synthetic analog of codeine?

A

tramadol

90
Q

describe the mechanism of action of tramadol

A

moderate mu-receptor agonist

weak inhibitor of NE and seratonin reuptake

91
Q

what moderate opioid agonist is a great alternative for patients who may not tolerate NSAIDs?

A

tramadol

92
Q

definition:

drugs that have a partial agonist or antagonist activity at mu-receptors and show agonist or antagonist activity at kappa-receptors

A

mixed agonist-antagonist

93
Q

definition:

drugs that can only produce a submaximal response

A

partial agonists

94
Q

what action do partial agonists have in the absence of a full agonist?

A

agonist action

95
Q

what action do partial agonists have in the presence of full agonists?

A

antagonist action

96
Q

what are the advantages of mixed opioid agonist-antagonists?

A

ceiling to respiratory depression

lower abuse potential

97
Q

what are the disadvantages of mixed opioid agonist-antagonists?

A

dysphoric at high doses

difficult to antagonize

98
Q

which mixed agonist-antagonist, also known as talwin, is a kappa-receptor agonist with weak mu-receptor antagonist properties?

A

pentazocine

99
Q

which mixed opioid agonist-antagonist, also known as buprenex, is a partial agonist at mu-receptors and an antagonist at kappa-receptors

A

buprenorphine

100
Q

how is pentazocine formulated for use as a preanesthetic medication?

A

parenteral formulation

101
Q

how is pentazocine administered for treating moderate to severe pain?

A

orally administered

102
Q

which mixed agonist-antagonist precipitates withdrawal syndrome in a morphine abuser?

A

pentazocine

103
Q

which mixed opioid agonist-antagonist is resistant to naloxone reversal?

A

buprenorphine

104
Q

which mixed opioid agonist-antagonist is used to manage cocaine addicition and heroin abuse?

A

buprenorphine

105
Q

which opioid antagonist has a half-life/duration of action of 1-2hrs?

A

naloxone

106
Q

which opioid antagonist has a half-life of 10hr?

A

naltrexone

107
Q

narcan is a competitive opioid antagonist otherwise known as

A

naloxone

108
Q

ReVia is a competitive opioid antagonist also known as

A

naltrexone

109
Q

describe how naloxone effects normal individuals vs. opiate abusers

A

no effects in normal individuals, but precipitates withdrawal symptoms in opiate abusers

110
Q

how is naloxone most commonly used?

A

intravenous injection is used for reversing the coma and respiratory depression of opiod overdose.

111
Q

which opioid antagonist has a 24 hr duration of action?

A

naltrexone

112
Q

which opioid antagonist is used as a “maintenance” drug for addicts in treatment programs and used to treat chronic alcoholics by decreasing cravings for alcohol?

A

naltrexone

BAHS-504 PHARMACOLOGY EXAM 2 (6 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions