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PSYT 301 FINAL > Opioids > Flashcards

Opioids Flashcards

1
Q

What is the difference between an opiate and opioid?

A

Opiates is a term restricted to natural opium products, whereas opioids refers to all natural, semi-synthetic and synthetic opium drugs.

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2
Q

Where does opium originate from?

A

The poppy plant

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3
Q

What was the original/historic purpose of opium?

A

It was characterized as a narcotic analgesic, producing a sense of relaxation and acting as the best known painkiller

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4
Q

What is the main active ingredient found in the opium poppy?

A

Morphine

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5
Q

List some of the different opiates/opioids derived from opium

A

1) Natural: opium, morphine, codeine, thebaine
2) Semi-synthetic: heroin, oxycodone
3) Synthetic: fentanyl, methadone, meperidine

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6
Q

How does codeine differ from morphine?

A
  • weaker analgesic
  • less side effects
  • cough suppressant
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7
Q

How does heroin differ from morphine?

A
  • more potent (2-4x stronger)
  • IV administration
  • quicker action
  • lipid soluble
  • metabolized into morphine
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8
Q

How does naloxone differ from morphine?

A
  • opioid receptor antagonist + partial inverse agonist
  • used during opioid overdose
  • completely blocks drug effect, which can lead to negative withdrawal symptoms
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9
Q

Define: Partial inverse agonist

A

An inverse agonist is a drug that binds to the same receptor as an agonist but induces a pharmacological response opposite to that of the agonist.
This is unlike an antagonist which only blocks the receptor and does not produce its own effect.

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10
Q

ADME: Opioid absorption

A
  • only a small fraction crosses the BBB
  • readily crosses the placenta (can lead to NAS in baby)
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11
Q

How are opioids administered medically vs recreationally?

A

1) Medical: IM, PO
2) Recreational: subcutaneous, intra-nasal, IV

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12
Q

ADME: Opioid metabolism and excretion

A
  • metabolized directly by the liver
  • metabolites excreted in urine after 24h
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13
Q

T or F: The psychological and behavioural effects of opioids depend on the dose and the speed of absorption.

A

True.
Dose-dependent and vary with the speed of absorption.

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14
Q

List some of the psychological and behavioural effects at low opioid doses.

A

1) Pain relief
2) Respiratory depression (!!)
3) Miosis
4) Sleepiness

Subjective effects:
5) Reduced sensitivity to environment
6) Decreased focus

Psychological pain:
7) Reduced anxiety
8) Reduced feeling of inadequacy
9) Reduced hostility

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15
Q

Which opioid effect will typically lead to death?

A

Respiratory depression.

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16
Q

What are some hypothalamic effects caused by morphine?

A

1) Reduced appetite
2) Lower body temperature
3) Decreased sex drive
4) Hormonal changes

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17
Q

List some of the effects at high doses of opioids.

A

Begins with euphoria, but then…

1) Dysphoria
2) Agitation
3) Anxiety
4) Nausea and vomiting
5) Sedation
6) Drastic decrease in body temperature
7) Drastic decrease in blood pressure
8) Severe respiratory depression
9) Miosis

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18
Q

Which opioid effect is resistant to tolerance?

A

Constipation.

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19
Q

What is loperamide?

A

A semi-synthetic opioid used to treat diarrhea.

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20
Q

List the four subtypes of metabotropic opioid receptors.

A

1) Mu
2) Kappa
3) Dela
4) NOP-R

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21
Q

List the roles of the mu opioid receptor and associated brain regions.

A

1) Morphine-induced analgesia → PAG, medial thalamus, median raphe, spinal cord
2) Positive reinforcement → NAcc
3) Cardiovascular and respiratory depression, cough control, nausea and vomiting → brainstem
4) Sensorimotor integration → thalamus, striatum

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22
Q

T or F: Mu receptors have a low affinity for morphine.

A

False.
Mu receptors have a high affinity for morphine and its derivatives. These receptors are widely spread in the brain and spinal cord.

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23
Q

List the roles of the delta opioid receptor and associated brain regions.

A

1) Olfaction
2) Motor integration
3) Reinforcement
4) Cognitive function

→ NAcc, PFC, substantia nigra, striatum, olfactory areas

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24
Q

T or F: Overlapping of the delta receptors with mu receptors suggests modulation of spinal analgesic response.

A

True.

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25
Q

List the roles of the kappa opioid receptor and associated brain regions.

A

1) Pain perception
2) Gut motility
3) Dysphoria
4) Water balance
5) Feeding
6) Temperature control
7) Neuroendocrine function

→ striatum, amygdala, hypothalamus, pituitary

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26
Q

List the roles of the NOP-R opioid receptor and associated brain regions.

A

1) Analgesia
2) Feeding
3) Learning
4) Motor function
5) Neuroendocrine regulation

→ High concentration in the cerebral cortex and the limbic areas
→ Amygdala, hippocampus, hypothalamus, PAG, thalamus, raphe nuclei, spinal cord

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27
Q

Which opioid receptor is often linked to withdrawal symptoms?

A

Kappa.

28
Q

What is the endogenous ligand for each opioid receptor subtype?

A

1) Mu: endomorphins, endorphins
2) Delta: enkephalin, endorphins
3) Kappa: dynorphins
4) NOP: nociceptin / orphanin FQ

29
Q

The four opioid receptor subtypes are linked to which protein?

A

Inhibitory G protien (Gi)

30
Q

How do endogenous opioids exert inhibitory action?

A

1) Postsynaptic inhibition
→ decrease in firing rate
→ inhibits neurotransmission
2) Axoaxonic inhibition
→ neuromodulation on other axons (closing of Ca++ channels, thus refraining vesicles from binding)
3) Presynaptic autoreceptors
→ inhibit signal to release more neurotransmitters
→ reduced postsynaptic effect

31
Q

How do opioids reduce pain? List the three mechanisms.

A

1) By two descending pathways from the PAG (!!)
2) In the spinal cord by small inhibitory interneurons
3) At higher level sites in the brain (emotional and hormonal aspect)

32
Q

How do opioids produce a reinforcing effect?

A

Opioids contribute to the mesolimbic DA pathway through inhibition of GABA neurons which increase VTA cell firing and thus DA release from the NAcc

33
Q

T or F: Kappa agonists, such as dynorphin, produce the largest reinforcing effect.

A

False.
They produce the opposite effect by inhibiting DA release.

34
Q

T or F: Pharmacodynamic tolerance is observed before metabolic tolerance to opioids.

A

True.
This will often be seen for the analgesic effects, but not really for pupil dilation.

35
Q

T or F: Cross-tolerance is observed between opioid receptor subtypes.

A

True.

36
Q

T or F: With opioid abuse, the liking of the drug undergoes sensitization, whereas the wanting of the drug decreases as tolerance develops.

A

False.
The wanting increases even when the high decreases over time and the liking decreases.
→ The craving undergoes sensitization
→ The liking remains the same or decreases as tolerance develops

37
Q

What is physical dependence? What does it look like in the context of opioids?

A

Physical dependence refers to a neuroadaptive state that occurs in response to the long-term occupation of opioid receptors.

38
Q

Once someone has built physical dependence to opioids, what happens once they stop taking the drug?

A

When the drug is no longer present, cell function not only returns to normal but also overshoots basal levels and opposite symptoms are seen.

39
Q

T or F: Antagonist-induced withdrawal is the “easiest” to deal with.

A

False.
It is quicker and more severe.

40
Q

T or F: Opioid withdrawal is oftentimes lethal.

A

False.

41
Q

Which factors can affect one’s withdrawal?

A

1) Dose
2) Frequency
3) Duration
4) Overall health
5) Personality

42
Q

T or F: The withdrawal of long-acting opioids tend to take more time but show less severe symptoms.

A

True.

43
Q

List the locations of withdrawal symptoms.

A

1) PAG
2) Locus coeruleus
3) NAcc

44
Q

List possible treatment options.

A

1) Support groups
2) Rehabilitation facilities for harm reduction
3) Cognitive therapy
→ mindfulness, reappraisal, CBT
4) Neurostimulation
→ modulation of dlPFC for craving reduction
→ tDCS of dlPFC
5) MI
6) Medication-assisted treatment

45
Q

Define: Abstinence

A

Abstinence broadly refers to a state of voluntary or involuntary non-engagement in a behaviour.

46
Q

Define: Harm reduction

A

An approach that emphasizes engaging directly with people who use drugs to prevent overdose and infectious disease transmission, improve their physical, mental, and social wellbeing, and offer low-threshold options for accessing substance use disorder treatment and other health care services.

47
Q

T or F: Therapy is often the only source of treatment that successfully treats OUD.

A

False.
The only con with therapy as a treatment for opioid dependence is that, in some cases, it cannot be the sole form of treatment because it does not help with severe physical withdrawal symptoms from detoxing.

48
Q

What are opioid agonist treatments (OAT)? What are some important properties/characteristics?

A

OAT works by replacing short-acting opioids with longer-acting opioid medication.
→ do not result in a high
→ affect the body slowly and for longer
→ longer half-life
→ prevent opioid withdrawal symptoms for 24-36 hours
→ helps eliminate cravings for opioid drugs

49
Q

T or F: The ideal OAT drug has a short half-life.

A

False.
You want to prescribe an agonist that has a high half-life in order to minimize withdrawal symptoms.

50
Q

List the three most common OATs.

A

1) Methadone
2) Buprenorphine
3) Diacetylmorphine (Heroin)

51
Q

List some benefits and limitations of methadone.

A

Benefits:
1) high bioavailability
2) relatively long elimination
3) half-life = 24 hours
4) prevents withdrawal symptoms
5) full agonist
6) helps with cross-dependence withdrawal
7) helps with cross-tolerance
8) PO administration

Limitations:
1) potential risk of overdose (no ceiling effect)
2) dose obtained at the pharmacy
3) must be taken under supervision
4) specific training required for physicians

52
Q

List some benefits and limitations of buprenorphine.

A

Benefits:
1) long elimination
2) helps relieve withdrawal symptoms
3) lower risk of overdose (ceiling effect, partial agonist)
4) comes in many forms

Limitations:
1) must be combined with naloxone
2) negative perception when naloxone is included

53
Q

List some benefits and limitations of diacetylmorphine.

A

Benefits:
1) in theory, responds to the specific needs of patients who do not respond to available medication-assisted treatments

Limitations:
1) restricted access
2) short half-life
3) treatment modalities are complicated (frequent visits, supervised, controlled space)

54
Q

What is Suboxone?

A

A combination of buprenorphine and naloxone, which work chemically to decrease the severity of withdrawal symptoms and reduce a patient’s dependence on opioids in the long term.

→ helps avoid buprenorphine misuse

55
Q

What is Subutex?

A

Only buprenorphine.

56
Q

What are opioid antagonist treatments? What are some characteristics/properties?

A

Opioid antagonist drugs are one of the most powerful tools in the treatment of opioid addiction. They work by blocking one or more of the opioid receptors in the CNS.

→ help people who are addicted to opioids manage withdrawal symptoms or even recover from an opioid overdose

57
Q

List the two most common opioid antagonist treatments. What’s the biggest difference between the two?

A

1) Naloxone → fast-acting
2) Naltrexone → long-lasting

58
Q

List some benefits and limitations of naloxone.

A

Benefits:
1) appropriate for overdose intervention
2) can temporarily stop the effects of opioid use
3) nasal spray form (NARCAN)
4) easy to administer

Limitations:
1) costly nasal spray formula
2) legal and medical authorization required
3) lots of personnel needed

59
Q

List some benefits and limitations of naltrexone.

A

Benefits:
1) effectively antagonizes heroin
2) relatively long duration of action (4 hours)
3) works for long-term treatment
4) decreases cravings

Limitations:
1) does not eliminate cravings
2) chronic exposure may result in upregulation of opioid receptors, thereby increasing their sensitivity

60
Q

What are safer supply services?

A

Safer supply services provide prescribed medications to people who use drugs, overseen by a health care practitioner, with the goal of preventing overdoses and saving lives.
They are provided in a less clinical and more flexible way compared to other care options for substance use, such as opioid agonist treatment (OAT).

61
Q

T or F: If prescribed opioids for chronic pain, it is highly unlikely to develop OUD.

A

False.
We often see medically prescribed opioids for chronic pain leading to iatrogenic OUD.

62
Q

T or F: Studies have shown that long-term opioid use has few damaging effects on organ systems.

A

True/False.
True, but we have limited data on the long-term effects (very few longitudinal studies conducted) and emerging data shows the effects on brain matter.

63
Q

T or F: Longitudinal studies have demonstrated WM recovery with opioid abstinence after inpatient treatment.

A

True.

64
Q

T or F: Longitudinal opioid abstinence is associated with state-like and cue-induced measures of craving.

A

False.
It is associated with state-like but not cue-induced measures of craving.

65
Q

What mechanisms are cytokines involved in?

A

1) Neuroimmune effects
2) Neuroinflammatory effects
3) BBB disruption

66
Q

How can cytokines be useful when studying OUD?

A

It is difficult to see the impact of stress on a patient when in a clinical setting, thus cytokines can act as an indirect measure of stressor and thus allow us to better measure white matter volume.

67
Q
A

PSYT 301 FINAL (4 decks)

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