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Drugs💊🤪 > Opiates/Opioids (Final Exam) > Flashcards

Opiates/Opioids (Final Exam) Flashcards

1
Q

What type of drugs are opioids?

A

analgesics and sedative-hypnotics

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2
Q

While they are the best pain killers known that cause euphoria, at high doses Opioids can lead to…

A

coma and death

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3
Q

What type of flower specifically is the source of “opiates”?

A

The opium poppy

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4
Q

Raw opium contains about 10% _______ or about 0.5% ______

A

morphine; codeine

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5
Q

What are the routes of administration for opium?

A

oral and smoking

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6
Q

True or false: Opium has been used for medical purposes since before recorded history?

A

True

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7
Q

A drug that used opium in the 1680s was called Laudanum which was weak due to tinctures of opium. What are tinctures?

A

Tinctures = medicine made by dissolving a drug in alcohol

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8
Q

What was Laudanum used for in the US until 1914?

A

primarily for pain; also diarrhea and coughing

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9
Q

Recreationally, raw opium is usually ________?

A

smoked

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10
Q

What are the principal active ingredients in opoim?

A

Morphine and codeine (natural source)

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11
Q

What is morphine used for medically?

A

Medical use as an analgesic (schedule 2)

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12
Q

What is codeine used for medically?

A

some analgesic effects, really good for cough (schedule 2 or 3 based on dose)

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13
Q

What form of opioid is heroin?

A

semi-synthetic

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14
Q

What is heroin derived from and what is it formed by?

A

Heroin is derived from morphine, and it is a semi-synthetic opioid formed from adding two acetyl groups to morphine

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15
Q

What did bayer first advertise heroin as?

A

A less addictive replacement for morphine

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16
Q

Facts about Heroin:

A
  • Heroin is illegal in the US (schedule 1)
    -Heroin can be smoked, snorted, or taken IV (fastest)
    -The purity of street heroin varies because it may include adulterants to enhance the effects (ex: fentanyl)
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17
Q

What do the two acetyl groups added to morphine do?

A

increases lipid solubility and speed to the brain

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18
Q

Which is more potent? Heroin or morphine?

A

Heroine is 2-4x more potent than morphine when taken IV

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19
Q

What is desomorphine? Potency in relation to morphine?

A

It is Krokodil aka “flesh-eating drug” and it is 8-10 times more potent than morphine

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20
Q

Is desomorphine natural, synthetic, or semi-synthetic?

A

semi-synthetic

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21
Q

Fentanyl is a synthetic opioid used to treat pain that has a high potency. It is ____x more potent than morphine and ___ more potent than heroin

A

100; 50

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22
Q

illicit fentanyl and opioids are laced with what drug?

A

xylazine aka “tranq”

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23
Q

What could happen as a result of xylazine intake?

A

increased risk of respiratory depression and overdose

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24
Q

Prescription opioids are used for what two purposes?

A

analgesic and antitussive (cough)

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25
Q

What three things does chronic use of opioids increase potential for?

A

abuse, addicion, and overdose

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26
Q

What has there been a large increase in over the past 20 years?

A

opioid overdose deaths

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27
Q

What is one factor that contributed to the prescription opioid and heroin epidemic?

A

Purdue aggressively marketed OxyContin (controlled release oxycodone)

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28
Q

True or False: A large percentage of people with opioid prescriptions become addicted

A

False! Only about 3% of people that have a prescription for pain have an addiction

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29
Q

Factors leading to opioid crisis:

A

-Chronic use of Rx opioids
-Lacing of heroin with fentanyl

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30
Q

Recreational routes of administration for opioids

A

-IV injection
-SC injection
-smoking/inhalation
-snorting

31
Q

IV heroin reaches the brain much faster than morphine due to _____ ________

A

lipid solubility

32
Q

difference in half-life between morphine and methadone

A

Morphine and most oral Rx: 2-4 hours

Methadone (oral (drank)): 24 hours due to depot binding

33
Q

Effects of low doses of opioids

A

-analgesia
-suppression of cough reflex
-reduced GI motility (constipation)
-euphoria
-some dysphoria (unpleasant feelings)
-Nausea/vomiting

also: slowed respiration, pupil constriction, drowsiness, decreased concentration

34
Q

Effects of high doses of opioids

A

-unconsciousness
-pinpoint pupils
-reduced temperature and blood pressure
-respiratory depression
-reversed rapidly by naloxone (antagonist for opioid receptors)

35
Q

Withdrawal are (similar or opposite) to acute effects?

A

Opposite

(Rebound hyperactivity in GI tract, autonomic nervous system, brain, and spinal cord)

36
Q

Is opioid withdrawal deadly?

A

it is not life threatening

37
Q

True or False: there is cross-dependence and cross tolerance for all opioids

A

True

38
Q

______ duration opioid causes longer withdrawal with ______ intensity

A

lower; lower

39
Q

Factors driving tolerance

A

-metabolic tolerance
-pharmacodynamic tolerance
-psychological tolerance

40
Q

Treatment options for opioids

A

-detoxification
-pharmacological support (opioid agonists and antagonists)
-group/individual counseling
-harmful reduction programs

41
Q

What is the pharmacodynamic action for all opioid drugs?

A

Bind to opioid receptors in the central nervous system and periphery

42
Q

The first endogenous opioid discovered was…?

A

beta-endorphin

43
Q

what type of neurotransmitters are all endogenous opioids?

A

peptide neurotransmitters

44
Q

What are the types of endogenous opioids that act as NT and hormones?

A

endorphins, enkephalins, and dynorphins

45
Q

How many gene families (that encode long propeptides) are all opioid peptides products of?

A

4 families

46
Q

Endogenous peptide synthesis

A

peptides are made in the soma, cleaved and packaged into vesicles in the Golgi, and then transported into terminals

47
Q

Release of peptide transmitters (aka endogenous opioids)

A

Neuropeptides are not typically the only transmitter at a synapse. Instead, they are co-released together with a classical neurotransmitter

48
Q

inactivation of peptide transmitters

A

after release, peptides are degraded together with a classical neurotransmitter

49
Q

Where are opioid receptors located?

A

in both the CNS and periphery

50
Q

Bioassay for opioids

A

ability of opioids to influence contractions of guinea pig intestine (ileum) strongly predicts human analgesic properties

51
Q

the 4 major types of opioid receptors

A

mu, delta, kappa, nociceptin/orphanin FQ

52
Q

What receptor do abused opioids bind to?

A

the mu-opioid receptor

53
Q

Are opioid receptors ionotropic or metabotropic?

A

all are metabotropic receptors and all are Gi coupled

opioid binding causes inhibition of AC and actions at G-protein-gated ion channels (opening K+ and closing Ca2+ channels)

54
Q

Opioid _______ can be presynaptic or postsynaptic

A

receptors

55
Q

What occurs in the brain regions where endogenous opioids are found?

A

pain and emotion signaling

56
Q

Locations of opioid receptors

A

CNS, PNS, Periphery

57
Q

Opioid Agonists and Antagonists

A

Agonists: many Rx and abused opioid drugs

Competitive Antagonists: naloxone, naltrexone (SHIFTS CURVE RIGHT)

Partial agonists: buprenorphine

58
Q

Genetic knockout of mu receptor that leads to loss of morphine effects:

A

-spinal analgesia
-supraspinal analgesia
-reward
-withdrawal
-respiratory depression
-inhibition of GI motility
-psychomotor activation

59
Q

Analgesia effects of opioids due to actions at:

A
  1. Spinal Cord: opioids inhibit incoming pain signal
  2. Periaqueductal gray
  3. Forebrain: sensory and emotional response to pain
60
Q

Reward associated with Mu receptors

A

-strongly implicated in reward and euphoria
-strong self-administration and CPP for selective mu receptor agonists

61
Q

Evidence that DA does mediate opioid reward

A

-mu agonists: increase VTA DA cell firing and DA release in striatum (NAc)
-DA antagonists: sometimes reduce opioid CPP and self-administration

62
Q

Evidence that DA does not mediate opioid reward

A

-DA receptor antagonists and 6-OHDA lesions do not have large effects of heroin self-administration
-DA-deficient mice still show morphine CPP

63
Q

Respiratory control levles

A
  1. fundamental drive generated by brainstem
    2.conscious modulations from cortex
    3.subconscious modulations from blood chemoreceptors
64
Q

What is considered the “gold standard” in antitussive therapy (cough suppression)

A

Codeine

65
Q

What was developed as a non-addictive substitute for codeine that does not act at opioid receptors?

A

Dextromethorphan (DM)

66
Q

Mechanisms of opioid-induced nausea

A
  1. trigger zone is area postrema (has weak BBB)
  2. increased vestibular sensitivity
  3. Delayed gastric emptying
67
Q

What causes pupil constriction?

A

opioid disinhibition of brainstem nuclei

68
Q

Where do opioid drugs act to produce their major effects? Analgesia

A

spinal cord, periaqueductal gray, forebrain

69
Q

Where do opioid drugs act to produce their major effects? Reward

A

Brain- dopamine neurons

70
Q

Where do opioid drugs act to produce their major effects? Gastrointestinal

A

stomach, small/large intestine

71
Q

Where do opioid drugs act to produce their major effects? Respiratory Depression

A

brainstem, cortex, blood chemoreceptors

72
Q

Where do opioid drugs act to produce their major effects? Cough suppression

A

brainstem and sensory nerves

73
Q

Where do opioid drugs act to produce their major effects? Nausea and Vomiting

A

area postrema, vestibular system, and GI

74
Q

Where do opioid drugs act to produce their major effects? Pupil constriction

A

brainstem

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