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Pharm > Drugs of Abuse > Flashcards

Drugs of Abuse Flashcards

1
Q

Psychomotor stimulants

A

Cocaine, amphetamines

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2
Q

Opiates and opioids

A

Heroin, morphine, codeine, oxycodone, hydromorphone

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3
Q

Cannabinoids

A

Marijuana

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4
Q

Sedatives

A

Barbituates, benzodiazepines

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5
Q

Hallucinogens

A

LSD, mescaline “club drugs”

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6
Q

Three signs of dependence

A

Abuse
Craving
Legal Problems

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7
Q

Criteria (within 12 months) for Substance Use Disorder by DSM-V

A 
Tolerance
Withdrawal
Use of larger amounts than intended
Persistent desire
Inability to control use
Excessive time spent 
Normal activities given up
Use despite knowledge of problems drug cause
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8
Q

Mild Substance Use Disorder

A

2-3 symptoms

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9
Q

Moderate Substance use disorder

A

4-5 symptoms

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10
Q

Severe substance use disorder

A

5+ symptoms

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11
Q

Withdrawal

A

A marker of physiological dependence

Signs and symptoms emerge when use of the drug is stopped, or are reversed when drug is administered again

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12
Q

Drug Tolerance

A

Decreased effect with repeated use of the drug

Need to use more drug to have the same effect

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13
Q

Where does the mesolimbic dopamine system originate

A

The VTA

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14
Q

Where does the mesolimbic dopmaine system project to

A

The nucleus accumbens
The amygdala
The prefrontal cortex

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15
Q

what happens when the VTA nucleus accumbens is activated by drugs of dependence

A

Release of dopamine

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16
Q

The shorter amount of time between injection of drug and delivery of the compound to brain, the ___ “high” somebody feels

A

more

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17
Q

What are the two ways to get withdrawal?

A

1) Give an antagonist
2) Let the drug naturally decay
No longer binding the receptor

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18
Q

What are some medical uses of cocaine?

A

1) stimulant of CNS
2) Freud used to treat depression
3) appetite suppressant (obesity)
4) topical anesthetic (historically- eye/nasal surgery, currently nasal/lacrimal duct surgery)

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19
Q

Cocaine MOA

A

Cocaine inhibits the dopamine transporter on the presynaptic terminal > causes levels of dopamine in the synaptic cleft to increase (particularly in the nucleus accumbens)

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20
Q

Amphetamine MOA

A

Amphetamines inhibit the VMAT2 (vesicular monoamine transporter 2)
DA not placed in presynaptic vesicles, high levels of dopamine in cell, travel reversely through the dopamine transporter (DAT) > causes increased levels of dopamine in the presynaptic cleft (particularly nucleus accumbens)

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21
Q

Historical uses for amphetamines

A

Treat asthma, narcolepsy, obesity

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22
Q

What is amphetamine?

A

synthetic phenylethylamine

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23
Q

Acute effects of psychostimulants (cocaine, amphetamines)

A 
Rush
Euphoria and arousal
Increased energy
Feelings of competency
Decreased feelings of fatigue/boredom
Decreases appetite
Increased HR, BP, temp
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24
Q

Onset, magnitude (potency), and duration depend on____

A

route of administration (smoked, injected, inhaled)

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25
Q

If taken IV, cocaine reaches peak in ___

A

15 seconds

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26
Q

What is the half-life of cocaine?

A

40-80 mins

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27
Q

Where is cocaine metabolized?

A

Liver (cholinesterases)

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28
Q

What is cocaine metabolized into?

A

Benzoylecgonine

can be monitored in biological fluids

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29
Q

How long can you detect cocaine in the urine?

A

up to 8 days after use

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30
Q

Cocaine in the presence of ethanol makes what compound

A

Cocaethylene

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31
Q

What are the characteristics of cocaethlyene?

A

Produces more euphoria

Long duration of action than cocaine

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32
Q

What is the risk of cocaetylene?

A

More cardiotoxic

Can cause cardiac arrest

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33
Q

What are the consequences of long term use of psychostimulants?

A

Sensitization
Tolerance
Impairment of neurocognitive functions
Increased risk of autoimmune/connective tissue diseases (lupus, goodpasture, SJS)

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34
Q

Overdose signs and symptoms of psychostimulants

A 
Hyperactivity
Sweating
Dilated pupils
Agitation/tremor
Tachycardia/chest pain
Cardiac Arrhythmia*******
Hypertension
Hyperpyrexia
Stereotypical behavior
Seizures/coma
Paranoia/tactiel hallucinations
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35
Q

Withdrawal signs and symptoms of psychostimulants

A 
Anxiety and agitation
Insomnia and hypersomnia
Fatigue and depression
Sweating
Muscle cramps
Hunger
Erectile dysfunction
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36
Q

Treatment of cocaine withdrawal (acute withdrawal=symptomatic treatment)

A

Bromocriptine (dopamine agonist)

Benzodiazepines (in pts with severe agitation and sleep disturbance)

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37
Q

Treatment of long term cocaine addiction

A

No FDA approved pharma Rx
Cognitive Behavioral Therapes (functional analysis, skills training)
Development of vaccine against cocaine?

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38
Q

What is opium derived from?

A

Extracts of juice of the opium poppy, Papaver somniferum

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39
Q

Opioid MOA

A

Inhibit the GABAergic interneurons by binding u receptors > double inhibition > elevated DA levels in nucleus accumbens

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40
Q

Opioid potential routes of adminitration

A 
Oral
IV
Snorting
Smoking 
Subcutaneous ("skin popping")
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41
Q

How long do Heroin’s effects last?

A

3-5 hours

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42
Q

Average addict uses ___ times/day?

A

2-4

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43
Q

Signs of Opioid Overdose

A 
Unconsciouness
Miosis
Hypotension
Bradycardia
Respiratory depression***
Pulmonary edema****
44
Q

Opioid cross tolerance

A

Tolerance to one opioid is usually associated with tolerance to other opioids

45
Q

Metabolism of Heroin (why it is so addictive!)

A

Metabolized to 6-monoacetylmorphine > metabolized to morphine (2 drugs in one!)

46
Q

When does Heroin withdrawal begin?

A

12 hours after last dose

47
Q

When does Heroin withdrawal peak?

A

1 1/2 - 3 days

48
Q

When does Heroin withdrawal finish?

A

Usually over by 5-7 days

49
Q

Heroin and protract abstinence syndrome

A

Lingering symptoms of withdrawal can persist for months and are associated with relapse

50
Q

Can Heroin withdrawal be life threatening?

A

YES! also very painful

51
Q

Opioid withdrawal symptoms

A 
Anxiety and dysphoria
Craving and drug-seeking
Sleep disturbance
Nausea, vomiting, diarrhea
Lacrimation*
Rhinorrhea*
Yawning*
Piloerection*
Sweating
Mydriasis
Cramps
Hyperpyrexia (high fever)
Involuntary movement*

*specific to heroin withdrawal

52
Q

Treatment of opioid addiction

A 
Self-help groups
Inpatient detox
Individual therapy
Prescription opioids
Pharmacotherapy
53
Q

Goals of pharmacotherapy

A

Cure of withdrawal or overdose

Create window of opportunity for pt to receive psycho-social intervention

54
Q

Treatment of Opioid Overdose

A

Naloxone

55
Q

MOA of Nalaxone

A

u-opioid competitive antagonist with very high affinity but short half-life

56
Q

Individuals treated for overdose with Nalaxone must be____-

A

Kept under observation for duration of the opioids drug’s effects

57
Q

Treatment of Opioid Dependence

A

Naltrexone

58
Q

MOA of Naltrexone

A

u-opioid antagonist with long half-life

heroin self-administration no longer rewarding

59
Q

What is Naltrexone FDA approved for?

A

Opioid dependence

Alcohol dependence

60
Q

Contraindication for Naltrexone

A

Avoid in pts with liver failure

61
Q

Treatment with Methadone

for opioid

A

Prevents withdrawal symptoms and cravings, has a cross tolerance with other opioids
Only dispensed in federally licensed clinics (daily visits)

62
Q

MOA of methadone

A

u-opioid receptor agonist with long half life

63
Q

Treatment with Buprenorphine (for opioid)

A

Given in formulation with nalaxone, has high affinity for receptors and dissociates slowly
Take Sublingually

64
Q

What happens when Buprenorphine is misused intravenously

A

Will result in withdrawal symptoms (due to presence of Naloxone)

65
Q

What happens if buprenorphine is initiated prior to onset of acute withdrawal signs

A

Can leads to abrupt withdrawal syndrome

66
Q

Active constituent of marijuana

A

THD (delta-9-tetrahydrocannabinol)

67
Q

MOA of THC

A

Inhibits GABAergic interneurons by binding the CB1 receptors >stimulation of DA release in nucleus accumbens

68
Q

Acute effects of marijuana

A 
sedation, relaxation
Mood alteration
Altered perception and time estimation
impaired judgement, memory, and concentration
Increase heart rate, dry mouth
Increased appetite
Injection of the conjunctiva
69
Q

Adverse effects of marijuana use

A

Panic, delirium, paranoia, poor judgement, tolerance, personality chances, gateway to other drug abuse

70
Q

Treatment of marijuana abuse is symptomatic

A

Anxiolytics
Antipsychotics
Cognitive behavioral therapy

71
Q

Characteristics of Type A Alcohol Dependence

A 
Late onset (>25)
Few familial 
Milder form
Environmental influence
Minimal criminality
72
Q

Characteristics of Type B Alcohol Dependence

A

Early onset (

73
Q

Primary diseases associated with chronic alcohol use

A 
Alcohol poisoning
Alcoholic heart disease
Alcoholic gastritis
Alcoholic liver cirrhosis
Alcoholic nerve disease
Alcoholic psychoses
74
Q

Secondary diseases associated with chronic alcohol us

A 
Cancer (lip, mouth, pharynx, esophagus, larynx, liver, stomach)
Diabetes
GI disease
Heart disease
Liver disease
Pancreatitis
75
Q

Effects of alcohol on neural circuits

A

Indirectly increasing dopamine levels in mesocorticolimbic system
Indirect activation of opioid receptors
Increases effect of GABA > (decreased GABA receptors)
Inhibits the effects of glutamate (>upregulation of NMDA receptors)

76
Q

Treatment stages of alcohol dependence

A
  1. identification (CAGE)
  2. detoxication/withdrawal
  3. Rehab
  4. Aftercare
77
Q

Treating symptoms of alcohol withdrawal

A

Benzidiazepines (indirect agonist of GABA)
Diazepams (long half-life)
Lorazepam (shorter half-life)

78
Q

Which drug is preferable to treat alcohol withdrawal in a patient with cirrhosis?

A

Lorazepam

79
Q

Minor alcohol withdrawal symptoms

A

6-36 hrs after
CNS hyperactivity
anxiety, headache, sweating, palpitations, GI upset, insomnia, nausea

80
Q

Seizures from alcohol withdrawal

A

6-48 hours after
tonic-clonic seizures (3%)
status epilecticus
life threatening

81
Q

Alcoholic hallucinations

A

12-48 hours after

Visual, auditory, tactile

82
Q

Delirium tremens

A

49-96 hours after (can last 5 days)

Withdrawal from long-term alcohol consumption or benzodiazepine withdrawal

83
Q

Symptoms of delirium tremens

A

Confusion, hallucinations, tremors of extremities, fever, tachycardia, HTN, diaphoresis

84
Q

Treatment of delirium tremens

A

Benzodiazepines with long half-life (diazepam, lorazepam)

85
Q

FDA approved therapies for alcohol dependence

A

Disulfiram
Naltrexone
Acamprosate

86
Q

Disulfiram

A

Alcohol aversion therapy

inhibit ALDH > increased levels of acetaldehyde > nausea, dizziness, headache, hypotension, vomiting

87
Q

Risk of disulfiram

A

Hepatotoxicity

Does not increase abstinence

88
Q

Which genetic variant of the ALDH enzyme to asians have which protects against alcohol dependence?

A

ALDH2*2

89
Q

Naltrexone

A

Long acting opioid antagonist
Blocks release of dopamine from nucleus accumbens
Reduces alcohol cravings

90
Q

Avoid naltrexone in which types of patients?

A

pts taking disulfiram

pts dependent on opioids

91
Q

Acamprosate

A

Restores balance between neuronal excitation and inhibition (mechanism unknown)
-decreases glutamate, increases GABA

92
Q

Side effects of acamprosate

A

Diarrhea, allergic reactions, irregular heart beats

93
Q

Contraindication of acamprosate

A

Severe renal disease

dose adjust in patients with moderate renal disease

94
Q

What is the BEST drug on the market for treating alcohol dependence?

A

Acamprosate (80% success)

95
Q

Therapeutic use of benzodiazepines

A

severe anxiety, panic attacks, phobias

insomnia, muscular disorders, alcohol withdrawal, epilepsy

96
Q

MOA of benzodiazepines

A

indirect agonist of GABA receptor

97
Q

Benzodiazepine Withdrawal symptoms

A 
anxiety, agitation
Increased sensitivity to light/sound
Muscle cramps
sleep disturbance
dizziness
Myoclonic jerks
98
Q

Treatment of benzodiazepine withdrawal

A

diazepam

long half-life–gradually taper off the drug

99
Q

Nicotine

A

selective agonist of the nicotinic acetylcholine receptor > stimulates dopaminergic neurons in VTA, increases DA release in nucleus accumbens

100
Q

Treatment of nicotine addiction

A

Nicotine patches, nasal spray, nicotine lozengem varenicline (chantix)

101
Q

Varenicline (Chantix)

A

Non-nicotine medication
Partial agonist that binds subunits of nicotine Ach receptors
Relieves cravings and withdrawal symptoms
Binds with greater affinity than nicotine

102
Q

Symptoms of hallucinogens

A

Changes of sensation, illusions, hallucinations, create fantasies, living nightmares

103
Q

Do hallucinogens induce dependence or addiction?

A

NO!

104
Q

Molecular target of hallucinogens

A

Serotonin receptors (5-HT2A in cortex)

105
Q

Treatment for non-psychotic agitation (due to hallucinogens)

A

anti-anxiety drugs (diazepam)

106
Q

Treatment for severe agitation (due to hallucinogens)

A

Anti-psychotic drugs

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