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Flashcards in Drugs of Abuse Deck (106):
1

Psychomotor stimulants

Cocaine, amphetamines

2

Opiates and opioids

Heroin, morphine, codeine, oxycodone, hydromorphone

3

Cannabinoids

Marijuana

4

Sedatives

Barbituates, benzodiazepines

5

Hallucinogens

LSD, mescaline "club drugs"

6

Three signs of dependence

Abuse
Craving
Legal Problems

7

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

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

8

Mild Substance Use Disorder

2-3 symptoms

9

Moderate Substance use disorder

4-5 symptoms

10

Severe substance use disorder

5+ symptoms

11

Withdrawal

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

12

Drug Tolerance

Decreased effect with repeated use of the drug
Need to use more drug to have the same effect

13

Where does the mesolimbic dopamine system originate

The VTA

14

Where does the mesolimbic dopmaine system project to

The nucleus accumbens
The amygdala
The prefrontal cortex

15

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

Release of dopamine

16

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

more

17

What are the two ways to get withdrawal?

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

18

What are some medical uses of cocaine?

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)

19

Cocaine MOA

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

20

Amphetamine MOA

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)

21

Historical uses for amphetamines

Treat asthma, narcolepsy, obesity

22

What is amphetamine?

synthetic phenylethylamine

23

Acute effects of psychostimulants (cocaine, amphetamines)

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

24

Onset, magnitude (potency), and duration depend on____

route of administration (smoked, injected, inhaled)

25

If taken IV, cocaine reaches peak in ___

15 seconds

26

What is the half-life of cocaine?

40-80 mins

27

Where is cocaine metabolized?

Liver (cholinesterases)

28

What is cocaine metabolized into?

Benzoylecgonine

(can be monitored in biological fluids)

29

How long can you detect cocaine in the urine?

up to 8 days after use

30

Cocaine in the presence of ethanol makes what compound

Cocaethylene

31

What are the characteristics of cocaethlyene?

Produces more euphoria
Long duration of action than cocaine

32

What is the risk of cocaetylene?

More cardiotoxic
Can cause cardiac arrest

33

What are the consequences of long term use of psychostimulants?

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

34

Overdose signs and symptoms of psychostimulants

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

35

Withdrawal signs and symptoms of psychostimulants

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

36

Treatment of cocaine withdrawal (acute withdrawal=symptomatic treatment)

Bromocriptine (dopamine agonist)
Benzodiazepines (in pts with severe agitation and sleep disturbance)

37

Treatment of long term cocaine addiction

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

38

What is opium derived from?

Extracts of juice of the opium poppy, Papaver somniferum

39

Opioid MOA

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

40

Opioid potential routes of adminitration

Oral
IV
Snorting
Smoking
Subcutaneous ("skin popping")

41

How long do Heroin's effects last?

3-5 hours

42

Average addict uses ___ times/day?

2-4

43

Signs of Opioid Overdose

Unconsciouness
Miosis
Hypotension
Bradycardia
Respiratory depression***
Pulmonary edema****

44

Opioid cross tolerance

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

45

Metabolism of Heroin (why it is so addictive!)

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

46

When does Heroin withdrawal begin?

12 hours after last dose

47

When does Heroin withdrawal peak?

1 1/2 - 3 days

48

When does Heroin withdrawal finish?

Usually over by 5-7 days

49

Heroin and protract abstinence syndrome

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

50

Can Heroin withdrawal be life threatening?

YES! also very painful

51

Opioid withdrawal symptoms

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

Treatment of opioid addiction

Self-help groups
Inpatient detox
Individual therapy
Prescription opioids
Pharmacotherapy

53

Goals of pharmacotherapy

Cure of withdrawal or overdose
Create window of opportunity for pt to receive psycho-social intervention

54

Treatment of Opioid Overdose

Naloxone

55

MOA of Nalaxone

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

56

Individuals treated for overdose with Nalaxone must be____-

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

57

Treatment of Opioid Dependence

Naltrexone

58

MOA of Naltrexone

u-opioid antagonist with long half-life

(heroin self-administration no longer rewarding)

59

What is Naltrexone FDA approved for?

Opioid dependence
Alcohol dependence

60

Contraindication for Naltrexone

Avoid in pts with liver failure

61

Treatment with Methadone
(for opioid)

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

62

MOA of methadone

u-opioid receptor agonist with long half life

63

Treatment with Buprenorphine (for opioid)

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

64

What happens when Buprenorphine is misused intravenously

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

65

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

Can leads to abrupt withdrawal syndrome

66

Active constituent of marijuana

THD (delta-9-tetrahydrocannabinol)

67

MOA of THC

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

68

Acute effects of marijuana

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

Adverse effects of marijuana use

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

70

Treatment of marijuana abuse is symptomatic

Anxiolytics
Antipsychotics
Cognitive behavioral therapy

71

Characteristics of Type A Alcohol Dependence

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

72

Characteristics of Type B Alcohol Dependence

Early onset (

73

Primary diseases associated with chronic alcohol use

Alcohol poisoning
Alcoholic heart disease
Alcoholic gastritis
Alcoholic liver cirrhosis
Alcoholic nerve disease
Alcoholic psychoses

74

Secondary diseases associated with chronic alcohol us

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

75

Effects of alcohol on neural circuits

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

Treatment stages of alcohol dependence

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

77

Treating symptoms of alcohol withdrawal

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

78

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

Lorazepam

79

Minor alcohol withdrawal symptoms

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

80

Seizures from alcohol withdrawal

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

81

Alcoholic hallucinations

12-48 hours after
Visual, auditory, tactile

82

Delirium tremens

49-96 hours after (can last 5 days)
Withdrawal from long-term alcohol consumption or benzodiazepine withdrawal

83

Symptoms of delirium tremens

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

84

Treatment of delirium tremens

Benzodiazepines with long half-life (diazepam, lorazepam)

85

FDA approved therapies for alcohol dependence

Disulfiram
Naltrexone
Acamprosate

86

Disulfiram

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

87

Risk of disulfiram

Hepatotoxicity
Does not increase abstinence

88

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

ALDH2*2

89

Naltrexone

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

90

Avoid naltrexone in which types of patients?

pts taking disulfiram
pts dependent on opioids

91

Acamprosate

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

92

Side effects of acamprosate

Diarrhea, allergic reactions, irregular heart beats

93

Contraindication of acamprosate

Severe renal disease
(dose adjust in patients with moderate renal disease)

94

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

Acamprosate (80% success)

95

Therapeutic use of benzodiazepines

severe anxiety, panic attacks, phobias
insomnia, muscular disorders, alcohol withdrawal, epilepsy

96

MOA of benzodiazepines

indirect agonist of GABA receptor

97

Benzodiazepine Withdrawal symptoms

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

98

Treatment of benzodiazepine withdrawal

diazepam
(long half-life--gradually taper off the drug)

99

Nicotine

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

100

Treatment of nicotine addiction

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

101

Varenicline (Chantix)

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

102

Symptoms of hallucinogens

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

103

Do hallucinogens induce dependence or addiction?

NO!

104

Molecular target of hallucinogens

Serotonin receptors (5-HT2A in cortex)

105

Treatment for non-psychotic agitation (due to hallucinogens)

anti-anxiety drugs (diazepam)

106

Treatment for severe agitation (due to hallucinogens)

Anti-psychotic drugs