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Behavioural Pharmacology (ADCS 3140) > Exam 3 > Flashcards

Exam 3 Flashcards

1
Q

Explain Centrally Acting Opiates/ Opioids

Introduction

A
  • Opiates a large group of naturally occurring compounds from opium, the latex from the opium poppy
  • Main psychoactive opiates in opium are: Morphine, Codeine, Thebaine
  • Afghanistan largest illegal producer of opium
  • India, Turkey, and Australia largest legal producers
  • Lethbridge Opium production (Same conditions to grow opium)
  • Opium used as far back as 5,000 BCE
  • Used in ancient Asia, Egypt, Arabia, Greece, Rome
  • Introduced to western medicine 1500s
  • Morphine isolated from opium in 1805 and codeine isolated in 1832
  • Opium often combined with alcohol to laudanum
  • 1/400 North Americans addicted in early 1900s (women and children)
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2
Q

The latex from the opium poppy is what?

A

Papaver Somniferum

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3
Q

Opium was historically used for…

A
  • Pain relief, surgical analgesia, insomia, depression, and diarrhea
  • Religious and ritualistic context
  • Suicide and executions (combined with hemlock)
  • Recreational use
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4
Q

Women and children were

A

addicted to opiates and opium

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5
Q

Opiates/ Opioids used for executions was combined with…

A

Hemlock

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6
Q

Mrs. Winslow’s Soothing Syrup AKA

A

Baby Killer (1tsp fatal)

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7
Q

1895-1915 state provincial laws

A

eliminated the over-the-counter availabilty of opiates and opioids

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8
Q

Recreational use of opioids in Canada was made illegal in

A

1908

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9
Q

Recreational use of opium was made illegal in the U.S. in

A

1914

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10
Q

Why was recreational use of opium made illegal?

A

Addiction concerns and widespread use amongst immigrant chinese labourers and increasing recreational use in non-chinese

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11
Q

Opioids are…

A

Synthetic

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12
Q

Opiates are…

A

Natural (Codeine, Morphine, Thebine)

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13
Q

First Synthetic Opioid

A

Heroin

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14
Q

Heroin

A
  • Made form morphine 1874
  • Reaches brain faster, 2-3 times more potent than morphine
  • Introduced as a substitute for codeine and morphine to suppress coughing from tuberculosis and pneumonia
  • Mistakenly believed to have fewer side effects
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15
Q

Oxycodone

A
  • OcyContin, Percocet
  • Thebaine
  • 1916
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16
Q

Hydromorphone

A
  • Dilaudid
  • From Morphine (Kadrian)
  • 1922
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17
Q

Methadone

A
  • Synthetic Opioid
  • 1939
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18
Q

Pethidine

A
  • Demerol
  • Synthetic opioid
  • 1939
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19
Q

Pentazocine

A
  • Talwin
  • 1959
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20
Q

Fentanyl

A
  • Sublimaze
  • 1959
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21
Q

Naloxone

A
  • Narcan
  • 1961
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22
Q

Naltrexone

A
  • Trexan
  • ReVia
  • 1965
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23
Q

Loperamide

A
  • Imodium
  • 1969
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24
Q

Buprenorphine

A
  • Suboxone
  • 1969
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25
Q

Carfentanil

A
  • 1974
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26
Q

Modern Uses of Opiates and Opioids

A
  • Pain relief
  • Coughing
  • Diarrhea
  • Anesthesia
  • Opiate/ Opioid addiction (drug substitute)
  • Opiate/ Opioid O.D.
  • Alcohol, Gambling addiction (anti-craving-)
  • Executions (U.S.)
  • Chemical Weapons
  • Euphoria (Recreational use and abuse)
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27
Q

What is used for U.S. executions (Modern)

A

Fentanyl combined with potassium chloride to stop heart

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28
Q

Opiates/ Opiods are taken

A

Orally, Intravenously (Mainlined), intramuscular, subcutaneous, smoked, snorted

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29
Q

True or False: More absortion when taken orally because it is lipid soluble

A

False

Less complete absorption when taken orally because tends to be lipid ins

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30
Q

What is the Neuromechanism of Opiates?

A

Mimics endogenous and natural opioids. Endogenous opioids are distributed throughout the Central Nervous System, particularly in areas that involve pain like spinal chord and midbrain, and mood (limbic system), also found in stomach and intestines

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31
Q

What endogenous/ natural opioids are mimicked?

fins

A

endorphins, dysnorphins, and enkephalins

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32
Q

Natural Opioids function as…

Neuro

A

Neurotransmitters, neurohormones, and neuroegulators

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33
Q

True or False: Overall role of opioids/ opiates are complex and not well understood

A

True

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34
Q

Body releases…

Exercise and Stress

A

Cortisol toincrease glucose in blood to aid muscles

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35
Q

Brain releases…

Exercise and Stress

A

BNDF to protect neurons from cortisol and stimulate neuronal growth for learning, memory, and thinking
Endorphins and endocannabinoids to block pain

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36
Q

What happens after exercise ends?

A
  • Cortisol returns to normal levels
  • Endorphins, endocannbainoids, and BDNF still elevated
  • Produces a sense of well-being
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37
Q

12 hours of mood elevation can be achieved by

A

a 20 minute work-out

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38
Q

Name the 4 types of opioid receptors

A
  • Mu (euphoria
  • Kappa
  • Delta
  • NOP
39
Q

What is the primary effect of the opioid receptor?

A

activation is reduction or inhibition of neurotransmission, particularly neurotransmitter release

40
Q

Spinal chord

A

Inhibit substance P release

41
Q

Ventral Tegmental Area

A

Inhibits GABA neurons thus disinhibiting dopaminergic neurons and increasing dopamine input in nucleus accumbens

42
Q

Main Effects of Opioids and Opiates

Physical

A
  • Analgesia
  • Relief of anxiety, euphoria, lose all concerns
  • Decreased respiration (including coughing)
  • Constipation
  • Reduced Sex Drive
  • Decreased pupil size
  • Mental clouding, drowsiness
43
Q

What is a less effective non-opiate alternative?

A

Dextromethorphan

44
Q

Thousands of Overdose Deaths/ Year

A
  • Respiratory suppression
  • 80% associated with other drugs (stimulants and alcohol)
  • Increasing since 2000, peak during pandemic (2020-2021)
45
Q

Highest Opioid Death Rates in Canada

A
  • Fentanyl and Carfentanil users
  • Yukon, British Columbia, Alberta
  • Young and Middle-Aged males
  • Indigenous
  • Stimulant users (cocaine and meth)
46
Q

True or False: Lethbridge does not have the highest death rate per capita in North America

A

False they have the highest

47
Q

What is the fatal dose of fentanyl

A

2mg or 2000mcg

48
Q

fatal dose of carfentanil

A

0.02mg or 20mcg

49
Q

Opiates/ opioids differ in ____ degree pass through blood-brain barier, which opioid receptor they act on, whether they are agonists or antagonists, and duration

A

Potency

50
Q

Opioids are mostly metabolized by…

A

The liver and excreted by kidneys

51
Q

Opioids and Opiates for pain, sedation, and coughing

A
  • Codeine
  • Morphine
  • Pentazocine
  • Oxycodone
  • Hydromorphone
  • Heroin/ Diamorphine
  • Fentanyl
  • Carfentanil
52
Q

Opiates and Opioids for Addiction

A
  • Buprenorphine
  • Naltrexone
  • Naloxone
53
Q

Opiates and Opioids for Diarrhea

A

Loperamide

54
Q

Long-Term Effects of Occasional Opioid Use

A
  • Not associated with long-term effects
55
Q

Long-Term Effects of Reccurent Opioid Use

A
  • Profound tolerance and strong physical and psychological dependence
  • Crime
  • Severe withdrawal symptoms (excitation, nausea, insomnia, hypersensitivity to pain, rarely fatal)
  • Constipation, indigestion, nausea
  • Increased risk of sexual dysfunction, fatigue, depression, sleep apnea, neuropsychological deficits, increased sensitivity to pain due to neuroadaptation
  • Use of needles can lead to vein collapse, hepatitis, blood poisoning, AIDS (unclean needles)
56
Q

Harm Minimization for Opioid/ Opiate Use

A
  • Supervised injection sites
  • ARCHES
57
Q

Periferally Acting Analgesics

A
  • Often subclassified into NSAIDs and atipyretics
  • Most common are aspirin, acetaminophen, ibuprofen, naproxen, and voltarin
  • Most widely used medications in the world
  • All but acetaminophen work primarily on the body and peripheral nervous system
  • For pain, inflammation, fever, differences between them in efficacy profile
  • More effective for pain when combined with caffeine
  • Increased risk for gastrointestinal bleedin, stroke, and heart attack, adverse effects on kidneys and liver
  • Fatal in large doses
  • Inhibit enzymes related to prostaglandins
  • Minimal tolerance and dependence
  • Most available over the counter
58
Q

What are prostaglandins

A

Lipids having hormone-like effects to mediate pain, inflammation and fever

59
Q

Aspirin

A
  • Found in willobark and spiraea
  • Used for pain and fever for thousands of years
  • Most commonly used peripherally acting analgesic
  • No cardiovascular risk other than PAA, daily low dose helps to stop blood clots and prevent heart attacks
  • Useful in preventing certain cancers (colorectal)
  • Increases risk of gastrointestinal bleeding and kidney problems
  • Shouldn’t be given to children and teens. Associated with Reye Syndrome
60
Q

What is Reye Syndrome?

A

A brain disease associate with aspirin in children and teens

61
Q

Acetaminophen

A
  • Tylenol
  • 1955
  • Less risk of gastrointestinal bleeding
  • Higher risk of liver damage and fatal OD due to liver failure (500 deaths/ year U.S.)
  • Not effective for inflammation, less effective for pain relief
  • Increase cardiovascular problems and kidney damage
  • Unlike other analgesics effects mostly in Central Nervous System
62
Q

Ibuprofen

A
  • 1974 (relatively new)
  • Gastrointestinal irritation (less than aspirin), increased cardiovascular risk, increased risk of kidney damage
  • May help prevent Parkinson’s
63
Q

Naproxen

A
  • 1976 (relatively new)
  • Longer duration than other peripherally acting analgesics
  • Low risk of cardiovascular problems
  • Increased risk of gastrointestinal bleeding and kindey problems
64
Q

What are Psychotherapeutic Drugs?

A
  • Exotic compounds also prescribed in historical times for mental disorders
  • Most operated via placebo effect
  • Exception; Opium, Alcohol, Cannabis, Willow bark
65
Q

morphine

1804

A

Pain, depression, and insomnia

66
Q

Chloroform & Ether

1840s

A

Pain

67
Q

Aspirin

1899

A

Pain

68
Q

Phenobarbital

1912

A

Seizures

69
Q

Amphetamines

1935

A

Narcolepsy, Depression

70
Q

Lithium

1949

A

Mania

71
Q

Chlorpromazine

1953

A

Schizophrenia

72
Q

MAOI

1957

A

Depression

73
Q

Tricyclic Antidepressants

1957

A

OCD, Anxiety, Depression

74
Q

I-Dopa

1961

A

Parkinson’s Disease

75
Q

Diazepam

1968

A

Anxiety

76
Q

Naltrexone

A

1894

77
Q

1980s

A
  • New Antidepressants
  • Antianxiety
  • Antipsychotics
78
Q

1987

A

Prozac/ Fluoxetine

79
Q

2006

A

Varenicline (Champix)

80
Q

Current Prevalence of Mental Health Medication

A
  • Significant increase in rx psychotropics in past 30 years
  • Primarily due to increased use of antidepressants
  • Signficant increase in children and adolescents as well (mostly due to stimulant medication for ADHD), although this has leveled off recently
  • Billions currently spent on antidepressants, antianxiety, antipsychotics, and stimulant drugs
81
Q

In 2019, adults…

A
  • 14% rx opiate/ opioid
  • 11% rx sedative
  • 10% antidepressant
  • 2% rx stimulant
82
Q

Increase of Psychotropic use due to…

A
  • Family physicians being main mental health practitioners
  • Quick fix
  • Short-term effectiveness
  • Wide range of mental health conditions that can be treated
  • Mild to short-term side effects
83
Q

6% of U.S. adults were prescribed psychotropic medication in…

A

1990

84
Q

What is an issue with the increase of psychiatric drugs?

A
  • Increasing the chronicity of mental health problems
  • Very difficult to withdraw from the drug
85
Q

Demographic Correlates of Mental Health Medication Usage

A
  • Higher in Western countries
  • Higher in North America compared the Europe
  • Higher in females
  • Higher in whites
86
Q

Psychotropics are the first line treatment for…

A
  • Bipolar types I and II
  • Schizophrenia
  • Severe depression
87
Q

Psychotropics also effective in short-term for other mental heath problems. However…

A

Long-term mental health tends to be worse compared to people who have went to psychotherapy or received no medication at all

88
Q

Psychotherapeutic drugs should always be…

A

The last resort

89
Q

Physicians refer to…

A

Compendium of Pharmaceuticals and Specialties (CPS)

90
Q

ADHD medications

A
  • Methylphenidate (Ritalin, Concerta)
  • Amphetamines (Dexedrine, Vyvanse)

Both medications have 1/day administration

91
Q

How does ADHD medication work?

A
  • Increases on-task behaviour and decreases disruptive behaviour
  • Equivocal impacts of academic achievement
92
Q

Side Effects of ADHD Medication

A
  • Appetite suppression
  • Insomnia
  • Small growth retardation
  • Motor and vocal tics, may produce permanent tics
  • 1.5% risk of psychosis
  • Abuse potential
93
Q

New formulation of Vyvanse

A

Converted to dextroamphetamine after enzymatic break-down in red blood cells

94
Q
A

Behavioural Pharmacology (ADCS 3140) (5 decks)

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