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20) Drugs of Abuse Flashcards

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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
Types of benzodiazepines and half lives
- Short (less than 12 h) - Intermediate (12-24 h) - Long (more than 24 h) - Benzodoazepine-like drugs (more selective to GABA)
26
Short acting benzodiazepines
- Midazolam - Triazolam (Halcion) - Alprazolam (Xanax) - Oxazepam
27
Short acting benzodiazepines indications
- Procedural sedation - Anesthesia induction - Sleep-onset insomnia - Very high potential for dependence
28
Intermediate benzodiazepines indications
- Sleep onset and sleep maintenance - Anxiety disorders - High to very high potential for dependence
29
Intermediate benzodiazepines
- Temazepam (Restoril)
30
Long acting benzodiazepines
- Lorazepam (Ativan; some classify it as intermediate because it has the shorted of the long acting) - Diazepam (Valium) - Clonazepam (Klonopin) - Chlordiazepoxide (Librium) - Tetrazepam
31
Long acting benzodiazepines indications
- Anxiety and panic attacks - Stress disorders - Night - Seizures - Muscles relaxation - Epilepsy - Alcohol withdrawal symptoms - High potential for dependence
32
Benzodiazepine-like drugs
- Zolpidem (Ambien) (4h) - Zaleplon (Sonata) (1h) - Eszopiclone - Lunesta (6h)
33
Benzodiazepine-like drugs indications
- Sleep disorders | - High potential for dependence
34
Benzodiazepine side effects
- Drowsiness, sleepiness, or dizziness - Increased appetite - Next-day hangover effect - Anterograde amnesia - Drug tolerance  - Paradoxical excitability (increase irritability in elderly)
35
Benzodiazepine contraindications
- Myasthenia gravis | - Narrow angle glaucoma
36
Benzodiazepine overdose symptoms
- CNS depression - Respiratory depression - Hypotension - Ataxia
37
Benzodiazepine overdose antidote
- Flumazenil
38
Benzodiazepine withdrawal symptoms
- Sweating - Nausea, vomiting, and anorexia - Hypertension - Seizures - Tremors - Memory impairment - Psychosis, hallucinations - Depressive moods
39
Types of barbiturates and their half lives
- Ultra short (15min - 3h) - Short (3-6h) - Intermediate (6-12h) - Long (12-24h)
40
Ultra-short acting barbiturates
- Methohexital | - Thiopental
41
Ultra-short acting barbiturates indications
- General anesthesia - Status epilepticus - Decrease increase pressure for brain edema - Sedation
42
Short acting barbiturates
- Pentobarbital | - Secobarbital
43
Short acting barbiturates indications
- Short term insomnia | - Pre-anesthetic anesthesia
44
Intermediate acting barbiturates
- Amobarbital - Butalbital - NOT USED (no indications)
45
Long acting barbiturates
- Phenobarbital | - Primidone
46
Long acting barbiturates indications
Phenobarbital - Seizures - Ethanol withdrawal - Pre-anesthetic sedation Primidone - Seizures - Tremors
47
Barbiturate side effects
- Hypotension - Respiratory depression and/or apnea  - Laryngospasm, bronchospasm (due to histamine release) - Painful injection - Dependence - Cytochrome P450 induction
48
Barbiturate overdose symptoms
- Impaired consciousness - Coma - Respiratory failure - Cardiovascular depression
49
Barbiturate overdose antidote
- Sodium bicarbonate (NaHCO3)
50
Barbiturates contraindications
- Myasthenia gravis | - Asrgma
51
Primary targets underlying the actions of the opioid analgesics
- µ, κ, and δ receptors
52
Opioids have other actions including
- Disinhibition in dopaminergic pathways in the CNS
53
The most abused drugs in the opioid group
- Heroin - Morphine - Codeine - Oxycodone - Meperidine and fentanyl (among health professionals)
54
Opioid overdose is managed with
- Parenteral naloxone or nalmefene | - Ventilatory support
55
When opioids binds to opioid receptors, it stimulates
- Potassium (K) conductance - Prevents AP and inhibits calcium conductance - Prevents release of NTs glutamate and substance P
56
Stimulants
- Caffeine and nicotine - Amphetamines - Cocaine
57
Action of cocaine in the CNS
- Blocks uptake of dopamine, noradrenaline, and serotonin - Blocking the dopamine transporter (DAT) by increasing dopamine concentrations in the nucleus accumbens has been implicated in the rewarding effects of cocaine
58
Action of amphetamines
- 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
Caffeine and nicotine overdose effects
- Excessive CNS stimulation with tremor, insomnia, and nervousness - Cardiac stimulation and arrhythmias - Respiratory paralysis (nicotine)
60
Caffeine withdrawal symptoms
- Lethargy - Irritability - Headache
61
Nicotine withdrawal symptoms
- Anxiety | - Mental discomfort
62
Amphetamines (Adderall) MOA
- Alter transporters of CNS amines including dopamine, norepinephrine, and serotonin, and increase their release
63
Amphetamine overdose effetcs
- Agitation - Restlessness - Tachycardia - Hyperthermia - Hyperreflexia - Possibly seizures
64
Amphetamine withdrawal symptoms
- 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
Cocaine MOA
- Inhibitor of the CNS transporters of dopamine, norepinephrine, and serotonin - Has marked amphetamine-like effects (“super-speed”); euphoria, self-confidence, and mental alertness
66
Cocaine overdose effects
- 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
Cocaine withdrawal symptoms
- Severe depression of mood is common and strongly reinforces the compulsion to use the drug
68
Phencyclidine (PCP, “angel dust”) and ketamine (“special K”)
- Hallucinogens known as ‘club drugs’ - Non-competitive antagonists at the glutamate NMDA receptor (excitatory synapse) - No actions on dopaminergic neurons in the CNS
69
PCP effects and dangers
- Most dangerous of the hallucinogenic agents | - Psychotic reactions, impaired judgment often leads to reckless behavior
70
PCP overdose effetcs
- Marked hypertension, and seizures which may be fatal.
71
Miscellaneous hallucinogenic agents
- Lysergic acid diethylamide (LSD) - Mescaline - Psilocybin
72
Miscellaneous hallucinogenic agents actions
- None of these drugs act on dopaminergic pathways in the CNS - Do not cause dependence
73
LSD actions
- Activates the serotonin 5-HT2A receptor in the prefrontal cortex - Enhances glutamatergic transmission onto pyramidal neurons - Excitatory afferents mainly come from the thalamus constitute a link to enhanced perception
74
Perceptual and psychological effects of LSD
- Somatic effects, particularly nausea, weakness, and paresthesias - Panic reactions (“bad trips”) may also occur
75
Marijuana
- Psychoactive constituents in crude extracts of the cannabis plant - Include the cannabinoid compounds tetrahydrocannabinol (THC), cannabidiol (CBD), and cannabinol (CBN) - Hashish is a partially purified material that is more potent
76
Marijuana products disinhibition actions
- Disinhibition of dopamine neurons | - Mainly by presynaptic inhibition of GABA neurons in the brainstem
77
Two types of cannabinoid receptors
- CB1 receptor - CB2 receptor - Both are G protein-coupled receptors
78
CB1 receptor
- Found primarily in the brain | - Also in some peripheral tissues
79
CB2 receptor
- Found primarily in peripheral tissues | - Also expressed in neuroglial cells
80
THC appears to alter mood and cognition through
- Agonist actions on the CB1 receptors leading to Dopamine release
81
CNS effects of marijuana
- 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
Marijuana and withdrawal
- Withdrawal state has been noted only in heavy users of marijuana - The dangers of marijuana use concern its impairment of judgment and reflexes
83
Potential therapeutic effects of marijuana
- Ability to decrease intraocular pressure | - Antiemetic actions
84
Dronabinol
- A controlled-substance formulation of THC | - Used to combat severe nausea
85
Rimonabant
- An inverse agonist that acts as an antagonist at cannabinoid receptors - Approved for use in the treatment of obesity
86
Anabolic steroids
- Controlled substances based on their potential for abuse | - Effects sought by abusers are increase in muscle mass and strength rather than euphoria
87
Excessive use of steroids can have adverse effects
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
Behavioral manifestations of excessive steroid use
- Increases in libido | - Aggression (“road rage”)
89
Signs withdrawal syndrome associate with steroid use
- Fatigue | - Depression of mood
90
Classes of drugs that treat dependence and addiction
- Opioid antagonists - Synthetic opioid - Partial μ-receptor agonist - N-receptor partial agonist - Benzodiazepines - NMDA receptor antagonist - Cannabinoid receptor antagonist
91
Opioid antagonists
- Naloxone | - Naltrexone
92
Synthetic opioids
- Methadone
93
Partial μ-receptor agonists
- Buprenorphine
94
N-receptor partial agonists
- Varenicline
95
Benzodiazepines
- Oxazepam | - Lorazepam
96
NMDA receptor antagonists
- Acamprosate
97
Cannabinoid receptor agonists
- Rimonabant
98
Naloxone MOA/effects/clinical impact
- Antagonists of opioid receptors - Reverse or block effects of opioids - Opioid overdose
99
Naloxone characteristics
- Short half-life (1–2 h)
100
Naltrexone clinical impact/characteristics
- Treatment of alcoholism | - Half-life like morphine (4h)
101
Methadone MOA/effects/clinical impact
- Slow-acting agonist at μ opioid receptors - Acute effects like morphine - Substitution therapy for opioid addicts
102
Methadone characteristics
- Variable but longer half-life | - Toxicity: Like morphine regarding acute and chronic effects including withdrawal
103
Buprenorphine MOA/effects/clinical impact
- Partial agonist at μ opioid receptors - Attenuates acute effects of morphine and other strong opioids - Substitution therapy for opioid addicts
104
Buprenorphine characteristics
- Long half-life (>40 h) | - Formulated with nalorphine to avoid illicit IV use
105
Varenicline MOA/effetcs/clinical impact
- Partial agonist at AChN receptor subtype - Blocks rewarding effects of nicotine - Smoking cessation
106
Varenicline characteristics
- Nausea and vomiting - Psychiatric changes - Seizures in high dose
107
Oxazepam and lorazepam MOA/effects/clinical impact
- Modulators of GABA A receptors - Enhance GABA functions in the CNS - Attenuate withdrawal symptoms including seizures from alcohol and other sedative-hypnotics
108
Oxazepam and lorazepam characteristics
- Half-life 4–15 h | - Lorazepam kinetics not affected by liver dysfunction
109
Acamprostate MOA/effects/clinical impact
- Antagonist at glutamate NMDA receptors - May block synaptic plasticity - Treatment of alcoholism
110
Acamprostate characteristics
- Allergies, arrhythmias, variable BP effects - Headaches - Impotence - Hallucinations in elderly
111
Rimonabant MOA/effects/clinical impact
- Inverse agonist at CB1 receptors - Decrease GABA and glutamate release in CNS - Treatment of obesity
112
Rimonabant characteristics
- Major depression | - Increased suicide risk
113
Amphetamines, methylphenidate, cocaine overdose effects
- Agitation - Hypertension, tachycardia - Delusions, hallucinations - Hyperthermia - Seizures, death
114
Common cocaine overdose effects
- Cardiac arrhythmias - Myocardial infarction - Stroke
115
Amphetamines, methylphenidate, cocaine withdrawal symptoms
- Apathy, irritability - Increased sleep time - Disorientation - Depression
116
Barbiturates, benzodiazepines, ethanol overdose effects
- Slurred speech, drunken behavior - Dilated pupils - Weak and rapid pulse - Clammy skin - Shallow respiration - Coma, death
117
Barbiturates, benzodiazepines, ethanol withdrawal symptoms
- Anxiety - Insomnia - Delirium, tremors (excited hallucinatory state associated with ethanol) - Seizures - Death
118
Heroin, other strong opioids overdose effects
- Constricted pupils - Clammy skin - Nausea - Drowsiness - Respiratory depression - Coma, death
119
Heroin, other strong opioids withdrawal symptoms
- Nausea - Chills, cramps - Lacrimation, rhinorrhea - Yawning - Hyperpnea - Temor, muscle jerks

Pharmacology (27 decks)

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