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Pharmacology > 20) Drugs of Abuse > Flashcards

20) Drugs of Abuse Flashcards

1
Q

Physical (physiologic) versus psychological dependence (old/new terms)

A
  • Physical (physiologic) = dependence

- Psychological = addiction

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2
Q

Addiction (definition)

A
  • Compulsivedrug usingbehavior
  • Personalsatisfaction
  • Formerly psychological dependence
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3
Q

Dependence (definition)

A
  • Signsandsymptoms (frequentlyoppositeofthosecausedbyadrug) when chronic use stops/dose lowers
  • Formerlyphysical/physiologicdependence
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4
Q

Tolerance (definition)

A
  • Adecreasedresponsetoadrug

- Necessitateslargerdosestoachievethesameeffect

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5
Q

Dopamine hypothesis of addiction

A
  • Dopamine involved with reward
  • Excessive stimulation may cause reinforcement such that the rewarded behavior may become compulsive (common feature of addiction)
  • Most addictive drugs involve dopamine effects in the CNS
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6
Q

Neuropharmacologic classification of addictive drugs by primary target (names)

A
  • DA, dopamine
  • GABA, γ-aminobutyric acid
  • GHB, γ-hydroxybutyric acid
  • GPCRs, G-protein-coupled receptors
  • THC, Δ9-tetrahydrocannabinol
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7
Q

Schedule I drug criteria

A
  • No medical use

- High addiction potential

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8
Q

Schedule I drug examples

A
  • Flunitrazepam
  • Heroin
  • LSD
  • Mescaline
  • PCP
  • MDA, MDMA
  • STP
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9
Q

Schedule II drug criteria

A
  • Medical usage

- High addiction potential

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10
Q

Schedule II drug examples

A
  • Amphetamines
  • Cocaine
  • Methylphenidate
  • Short acting barbiturates
  • Strong opioids
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11
Q

Schedule III drug criteria

A
  • Medical use

- Moderate abuse potential

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12
Q

Schedule III drug examples

A
  • Anabolic steroids
  • Barbiturates
  • Dronabinol
  • Ketamine
  • Moderate opioid agonists
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13
Q

Schedule IV drug criteria

A
  • Medical use

- Low abuse potential

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14
Q

Schedule IV drug examples

A
  • Benzodiazepines
  • Chloral hydrate
  • Mild stimulants (phentermine, sibutramine, etc.)
  • Most hypnotics (zaleplon, zolpidem, etc.)
  • Weak opioids
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15
Q

Sedativedrug effects/actions

A
  • Decreases activity
  • Moderates excitement
  • Calms recipient
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16
Q

Hypnotic drug effects/actions

A
  • Produces drowsiness

- Facilitates onset/maintenance of sleep state resembling natural sleep

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17
Q

The sedative-hypnotics include

A
  • Ethanol
  • Barbiturates
  • Benzodiazepines
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18
Q

Benzodiazepines are commonly prescribed drugs for

A
  • Anxiety

- They are schedule IV

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19
Q

Benzodiazepines and barbiturates MOA/activity

A
  • Indirect GABA-A agonists

- Increase frequency of Cl- channels –> increase hyperpolarization of the membrane

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20
Q

Primary actions of sedative-hypnotics

A
  • Facilitate effects of GABA

- Also enhance brain dopaminergic pathways (possibly related to the development of addiction)

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21
Q

Sedatives and hypnotics effects

A
  • CNS depressants

- Effects are enhanced by concomitant use of ethanol and/or opioid analgesics

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22
Q

Acute overdoses on sedatives and hypnotics commonly result in death via

A
  • Depression of medullary respiratory and cardiovascular centers
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23
Q

Flunitrazepam(Rohypnol/date rape drug)

A
  • Potent, rapid-onset benzodiazepine

- Marked amnestic properties

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24
Q

Flunitrazepam (Rohypnol) added to alcoholic beverages

A
  • Chloral hydrateorf-hydroxybutyrate(GHB; sodium oxybate)

- Sufficient dosage renders the victim incapable of resisting rape

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25
Q

Types of benzodiazepines and half lives

A
  • Short (less than 12 h)
  • Intermediate (12-24 h)
  • Long (more than 24 h)
  • Benzodoazepine-like drugs (more selective to GABA)
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26
Q

Short acting benzodiazepines

A
  • Midazolam
  • Triazolam (Halcion)
  • Alprazolam (Xanax)
  • Oxazepam
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27
Q

Short acting benzodiazepines indications

A
  • Procedural sedation
  • Anesthesia induction
  • Sleep-onset insomnia
  • Very high potential for dependence
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28
Q

Intermediate benzodiazepines indications

A
  • Sleep onset and sleep maintenance
  • Anxiety disorders
  • High to very high potential for dependence
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29
Q

Intermediate benzodiazepines

A
  • Temazepam (Restoril)
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30
Q

Long acting benzodiazepines

A
  • Lorazepam (Ativan; some classify it as intermediate because it has the shorted of the long acting)
  • Diazepam (Valium)
  • Clonazepam (Klonopin)
  • Chlordiazepoxide (Librium)
  • Tetrazepam
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31
Q

Long acting benzodiazepines indications

A
  • Anxiety and panic attacks
  • Stress disorders
  • Night
  • Seizures
  • Muscles relaxation
  • Epilepsy
  • Alcohol withdrawal symptoms
  • High potential for dependence
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32
Q

Benzodiazepine-like drugs

A
  • Zolpidem (Ambien) (4h)
  • Zaleplon (Sonata) (1h)
  • Eszopiclone
  • Lunesta (6h)
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33
Q

Benzodiazepine-like drugs indications

A
  • Sleep disorders

- High potential for dependence

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34
Q

Benzodiazepine side effects

A
  • Drowsiness, sleepiness, ordizziness
  • Increased appetite
  • Next-day hangover effect
  • Anterograde amnesia
  • Drug tolerance
  • Paradoxical excitability (increase irritability in elderly)
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35
Q

Benzodiazepine contraindications

A
  • Myasthenia gravis

- Narrow angle glaucoma

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36
Q

Benzodiazepine overdose symptoms

A
  • CNS depression
  • Respiratory depression
  • Hypotension
  • Ataxia
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37
Q

Benzodiazepine overdose antidote

A
  • Flumazenil
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38
Q

Benzodiazepine withdrawal symptoms

A
  • Sweating
  • Nausea, vomiting, andanorexia
  • Hypertension
  • Seizures
  • Tremors
  • Memory impairment
  • Psychosis, hallucinations
  • Depressive moods
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39
Q

Types of barbiturates and their half lives

A
  • Ultra short (15min - 3h)
  • Short (3-6h)
  • Intermediate (6-12h)
  • Long (12-24h)
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40
Q

Ultra-short acting barbiturates

A
  • Methohexital

- Thiopental

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41
Q

Ultra-short acting barbiturates indications

A
  • General anesthesia
  • Status epilepticus
  • Decrease increase pressure for brain edema
  • Sedation
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42
Q

Short acting barbiturates

A
  • Pentobarbital

- Secobarbital

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43
Q

Short acting barbiturates indications

A
  • Short term insomnia

- Pre-anesthetic anesthesia

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44
Q

Intermediate acting barbiturates

A
  • Amobarbital
  • Butalbital
  • NOT USED (no indications)
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45
Q

Long acting barbiturates

A
  • Phenobarbital

- Primidone

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46
Q

Long acting barbiturates indications

A

Phenobarbital

  • Seizures
  • Ethanol withdrawal
  • Pre-anesthetic sedation

Primidone

  • Seizures
  • Tremors
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47
Q

Barbiturate side effects

A
  • Hypotension
  • Respiratory depressionand/orapnea
  • Laryngospasm,bronchospasm(due tohistaminerelease)
  • Painful injection
  • Dependence
  • Cytochrome P450induction
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48
Q

Barbiturate overdose symptoms

A
  • Impaired consciousness
  • Coma
  • Respiratory failure
  • Cardiovascular depression
49
Q

Barbiturate overdose antidote

A
  • Sodium bicarbonate(NaHCO3)
50
Q

Barbiturates contraindications

A
  • Myasthenia gravis

- Asrgma

51
Q

Primary targets underlying the actions of the opioid analgesics

A
  • µ, κ, and δ receptors
52
Q

Opioids have other actions including

A
  • Disinhibition in dopaminergic pathways in the CNS
53
Q

The most abused drugs in the opioid group

A
  • Heroin
  • Morphine
  • Codeine
  • Oxycodone
  • Meperidineandfentanyl (among health professionals)
54
Q

Opioid overdose is managed with

A
  • Parenteral naloxone or nalmefene

- Ventilatory support

55
Q

When opioids binds to opioid receptors, it stimulates

A
  • Potassium (K) conductance
  • Prevents AP and inhibits calcium conductance
  • Prevents release of NTs glutamate and substance P
56
Q

Stimulants

A
  • Caffeine and nicotine
  • Amphetamines
  • Cocaine
57
Q

Action of cocaine in the CNS

A
  • Blocks uptake of dopamine, noradrenaline, and serotonin
  • Blocking thedopamine transporter (DAT) by increasing dopamine concentrations in the nucleus accumbens has been implicated in the rewarding effects of cocaine
58
Q

Action of amphetamines

A
  • Substrate of the DAT
  • Competitively inhibits DA transport
  • In the cell, interferes with the vesicular monoamine transporter (VMAT) and impedes the filling of synaptic vesicles
  • Thus vesicles are depleted and cytoplasmic DA increases
  • Leads to a reversal of DAT direction, strongly increasing nonvesicular release of DA, and further increasing extracellular DA concentrations
59
Q

Caffeine and nicotine overdose effects

A
  • Excessive CNS stimulation with tremor, insomnia, and nervousness
  • Cardiac stimulation and arrhythmias
  • Respiratory paralysis (nicotine)
60
Q

Caffeine withdrawal symptoms

A
  • Lethargy
  • Irritability
  • Headache
61
Q

Nicotine withdrawal symptoms

A
  • Anxiety

- Mental discomfort

62
Q

Amphetamines (Adderall) MOA

A
  • Alter transporters of CNS amines including dopamine, norepinephrine, and serotonin, and increase their release
63
Q

Amphetamine overdose effetcs

A
  • Agitation
  • Restlessness
  • Tachycardia
  • Hyperthermia
  • Hyperreflexia
  • Possibly seizures
64
Q

Amphetamine withdrawal symptoms

A
  • Increased appetite
  • Sleepiness, exhaustion
  • Mental depression
  • Treatment: anti-depressant
  • Chronic high-dose abuse leads to a psychotic state (with delusions and paranoia); necrotizing arteritis, leading to cerebral hemorrhage and renal failure.
65
Q

Cocaine MOA

A
  • Inhibitor of the CNS transporters of dopamine, norepinephrine, and serotonin
  • Has marked amphetamine-like effects (“super-speed”); euphoria, self-confidence, and mental alertness
66
Q

Cocaine overdose effects

A
  • Cardiac toxicity is partly due to blockade of norepinephrine reuptake by cocaine
  • Local anesthetic action contributes to the production of seizures
  • Vasoconstriction may lead to severe hypertensive episodes, resulting in myocardial infarcts and strokes
67
Q

Cocaine withdrawal symptoms

A
  • Severe depression of mood is common and strongly reinforces the compulsion to use the drug
68
Q

Phencyclidine (PCP, “angel dust”) and ketamine (“special K”)

A
  • Hallucinogens known as ‘club drugs’
  • Non-competitive antagonists at the glutamate NMDA receptor (excitatory synapse)
  • No actions on dopaminergic neurons in the CNS
69
Q

PCP effects and dangers

A
  • Most dangerous of the hallucinogenic agents

- Psychotic reactions, impaired judgment often leads to reckless behavior

70
Q

PCP overdose effetcs

A
  • Marked hypertension, and seizures which may be fatal.
71
Q

Miscellaneous hallucinogenic agents

A
  • Lysergic acid diethylamide(LSD)
  • Mescaline
  • Psilocybin
72
Q

Miscellaneous hallucinogenic agents actions

A
  • None of these drugs act on dopaminergic pathways in the CNS
  • Do not cause dependence
73
Q

LSD actions

A
  • Activates the serotonin 5-HT2Areceptor in the prefrontal cortex
  • Enhances glutamatergic transmission onto pyramidal neurons
  • Excitatory afferents mainly come from the thalamus constitute a link to enhanced perception
74
Q

Perceptual and psychological effects of LSD

A
  • Somatic effects, particularly nausea, weakness, and paresthesias
  • Panic reactions (“bad trips”) may also occur
75
Q

Marijuana

A
  • Psychoactive constituents in crude extracts of the cannabis plant
  • Include the cannabinoid compoundstetrahydrocannabinol (THC),cannabidiol (CBD),and cannabinol (CBN)
  • Hashishis a partially purified material that is more potent
76
Q

Marijuana products disinhibition actions

A
  • Disinhibition of dopamine neurons

- Mainly by presynaptic inhibition of GABA neurons in the brainstem

77
Q

Two types ofcannabinoid receptors

A
  • CB1 receptor
  • CB2receptor
  • Both areG protein-coupled receptors
78
Q

CB1receptor

A
  • Found primarily in the brain

- Also in some peripheral tissues

79
Q

CB2receptor

A
  • Found primarily in peripheral tissues

- Also expressed inneuroglial cells

80
Q

THC appears to alter mood and cognition through

A
  • Agonist actions on the CB1receptors leading to Dopamine release
81
Q

CNS effects of marijuana

A
  • Feeling of being “high,” with euphoria, uncontrollable laughter, changes in perception, and achievement of a dream-like state
  • Vasodilation occurs, and the pulse rate is increased
  • Habitual users show a reddened conjunctiva
82
Q

Marijuana and withdrawal

A
  • Withdrawal state has been noted only in heavy users of marijuana
  • The dangers of marijuana use concern its impairment of judgment and reflexes
83
Q

Potential therapeutic effects of marijuana

A
  • Ability to decrease intraocular pressure

- Antiemetic actions

84
Q

Dronabinol

A
  • A controlled-substance formulation of THC

- Used to combat severe nausea

85
Q

Rimonabant

A
  • An inverse agonist that acts as an antagonist at cannabinoid receptors
  • Approved for use in the treatment of obesity
86
Q

Anabolic steroids

A
  • Controlled substances based on their potential for abuse

- Effects sought by abusers are increase in muscle mass and strength rather than euphoria

87
Q

Excessive use of steroids can have adverse effects

A

Anticipated androgenic adverse effects

  • Acne
  • Premature closure of the epiphyses
  • Masculinization in females are
  • Hepatic dysfunction has been reported
  • Anabolic steroids may pose an increased risk of myocardial infarction
88
Q

Behavioral manifestations of excessive steroid use

A
  • Increases in libido

- Aggression (“road rage”)

89
Q

Signs withdrawal syndrome associate with steroid use

A
  • Fatigue

- Depression of mood

90
Q

Classes of drugs that treat dependence and addiction

A
  • Opioid antagonists
  • Synthetic opioid
  • Partial μ-receptor agonist
  • N-receptor partial agonist
  • Benzodiazepines
  • NMDA receptor antagonist
  • Cannabinoid receptor antagonist
91
Q

Opioid antagonists

A
  • Naloxone

- Naltrexone

92
Q

Synthetic opioids

A
  • Methadone
93
Q

Partial μ-receptor agonists

A
  • Buprenorphine
94
Q

N-receptor partial agonists

A
  • Varenicline
95
Q

Benzodiazepines

A
  • Oxazepam

- Lorazepam

96
Q

NMDA receptor antagonists

A
  • Acamprosate
97
Q

Cannabinoid receptor agonists

A
  • Rimonabant
98
Q

Naloxone MOA/effects/clinical impact

A
  • Antagonists of opioid receptors
  • Reverse or block effects of opioids
  • Opioid overdose
99
Q

Naloxone characteristics

A
  • Short half-life (1–2 h)
100
Q

Naltrexone clinical impact/characteristics

A
  • Treatment of alcoholism

- Half-life like morphine (4h)

101
Q

Methadone MOA/effects/clinical impact

A
  • Slow-acting agonist at μ opioid receptors
  • Acute effects like morphine
  • Substitution therapy for opioid addicts
102
Q

Methadone characteristics

A
  • Variable but longer half-life

- Toxicity: Like morphine regarding acute and chronic effects including withdrawal

103
Q

Buprenorphine MOA/effects/clinical impact

A
  • Partial agonist at μ opioid receptors
  • Attenuates acute effects of morphine and other strong opioids
  • Substitution therapy for opioid addicts
104
Q

Buprenorphine characteristics

A
  • Long half-life (>40 h)

- Formulated with nalorphine to avoid illicit IV use

105
Q

Varenicline MOA/effetcs/clinical impact

A
  • Partial agonist at AChNreceptor subtype
  • Blocks rewarding effects of nicotine
  • Smoking cessation
106
Q

Varenicline characteristics

A
  • Nausea and vomiting
  • Psychiatric changes
  • Seizures in high dose
107
Q

Oxazepam and lorazepam MOA/effects/clinical impact

A
  • Modulators of GABA A receptors
  • Enhance GABA functions in the CNS
  • Attenuate withdrawal symptoms including seizures fromalcoholand other sedative-hypnotics
108
Q

Oxazepam and lorazepam characteristics

A
  • Half-life 4–15 h

- Lorazepam kinetics not affected by liver dysfunction

109
Q

Acamprostate MOA/effects/clinical impact

A
  • Antagonist at glutamate NMDA receptors
  • May block synaptic plasticity
  • Treatment of alcoholism
110
Q

Acamprostate characteristics

A
  • Allergies, arrhythmias, variable BP effects
  • Headaches
  • Impotence
  • Hallucinations in elderly
111
Q

Rimonabant MOA/effects/clinical impact

A
  • Inverse agonist at CB1 receptors
  • Decrease GABA and glutamate release in CNS
  • Treatment of obesity
112
Q

Rimonabant characteristics

A
  • Major depression

- Increased suicide risk

113
Q

Amphetamines,methylphenidate, cocaine overdose effects

A
  • Agitation
  • Hypertension,tachycardia
  • Delusions,hallucinations
  • Hyperthermia
  • Seizures,death
114
Q

Common cocaine overdose effects

A
  • Cardiacarrhythmias
  • Myocardialinfarction
  • Stroke
115
Q

Amphetamines,methylphenidate, cocaine withdrawal symptoms

A
  • Apathy,irritability
  • Increasedsleeptime
  • Disorientation
  • Depression
116
Q

Barbiturates,benzodiazepines, ethanol overdose effects

A
  • Slurredspeech,drunkenbehavior
  • Dilatedpupils
  • Weakandrapid pulse
  • Clammyskin
  • Shallowrespiration
  • Coma,death
117
Q

Barbiturates,benzodiazepines, ethanol withdrawal symptoms

A
  • Anxiety
  • Insomnia
  • Delirium, tremors (excited hallucinatory state associated with ethanol)
  • Seizures
  • Death
118
Q

Heroin, other strong opioids overdose effects

A
  • Constrictedpupils
  • Clammyskin
  • Nausea
  • Drowsiness
  • Respiratory depression
  • Coma,death
119
Q

Heroin, other strong opioids withdrawal symptoms

A
  • Nausea
  • Chills,cramps
  • Lacrimation,rhinorrhea
  • Yawning
  • Hyperpnea
  • Temor, muscle jerks

Pharmacology (27 decks)

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