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FSC370 > Stimulants > Flashcards

Stimulants Flashcards

1
Q

How do stimulants work?

A

Increase existing levels of neurotransmitters in the CNS

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2
Q

By what mechanisms can stimulants increase existing levels of neurotransmitters?

A

Blocking reuptake
Stimulating release
Preventing breakdown

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3
Q

What are effects of stimulants?

A

Increase alertness, decrease fatigue, improve mood and increase self-confidence

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4
Q

What can low doses of CNS stimulants often lead to?

A

Euphoria, exaggerated reflexes, compensation for some fatigue

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5
Q

What can high doses of CNS stimulants cause?

A

Dizziness, loss of coordination, hallucinations, paranoia, anxiety

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6
Q

What is cocaine harvested from?

A

Coca plant

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7
Q

Where is cocaine predominantly found and why?

A

South America
Elevation creates better yield

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8
Q

What were some recommendations for cocaine use by Sigmond Freud in Uber Coca?

A

Mental stimulant
Possible treatment for digestive disorders
Appetite stimulant
Treatment for morphine and alcohol addiction
Local anesthetic

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9
Q

Describe the effects of cocaine when taken orally.

A

Highly susceptible to first-pass metabolism
Much slower peak
Less intense high

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10
Q

Describe the basic pharmacology of cocaine

A

Cocaine alkaloid extracted from coca leaves and then converted to hydrochloride salt and crystallized

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11
Q

Considering that cocaine HCl is water-soluble, what are possible administration routes for cocaine?

A

Orally
Insufflation/snorting
IV injection

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12
Q

Is cocaine heat stable? What is the significance of this?

A

No.
Cannot be smoked

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13
Q

What is freebasing?

A

Smoking cocaine obtained by dissolving in water, adding alkaline solution (e.g., ammonia), extracting cocaine base with organic solvent, typically ether.

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14
Q

In addition to freebasing, what is another way for cocaine to be smoked?

A

Mix dissolved cocaine HCl with baking soda, heat the mixture, then dry it
Crack

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15
Q

Describe the important factors in the strong addictive properties of cocaine

A

Cocaine is lipophilic and readily passes through blood-brain barrier.
Smoking results in large surge of cocaine in the brain that is not reflected in peripheral blood concentrations

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16
Q

Describe the mechanisms of cocaine action

A

Blocks reuptake of dopamine (DA), norepinephrine (NE), and serotonin (5-HT)
DA, NE and 5-HT are cleared from synaptic cleft by membrane transporters
Cocaine binds to transporters, inhibiting function
Increased transmission

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17
Q

Rank the transporter affinities of cocaine

A

5-HT
DA
NE

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18
Q

What is considered the most important factor for cocaine’s stimulating, reinforcing and addictive properties?

A

Blocking DA reuptake

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19
Q

What is a cocaine binge?

A

When cocaine is taken in multiple hits over several hours or days.

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20
Q

What causes cocaine to lose effectiveness in a binge?

A

saturation of reuptake transmitters

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21
Q

What happens during the accumulation of dopamine in the synaptic cleft?

A

Downregulation of dopamine receptors

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22
Q

What causes the crash/craving phase of cocaine?

A

Without cocaine, reduced DA receptor numbers are insufficient for normal activation

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23
Q

What are the common routes of administration for cocaine?

A

Insufflation, IV, smoking

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24
Q

What is the most common administration route for cocaine in North America?

A

Smoking and snorting

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25
Q

What are other possible routes of administration? Why are they less common?

A

Chewing of coca leaves or coca paste
Primarily of regional and cultural use
Oral administration gives less intense high

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26
Q

What are the effects of cocaine dependent on

A

Mode of administration and dose

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27
Q

How does the speed of the onset of cocaine effects affect the high and duration?

A

Faster onset = stronger high = shorter duration

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28
Q

What is the half-life of cocaine?

A

Average 1 hour
range 30-90 mins

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29
Q

What does cocaine metabolize into?

A

Benzolecgonine

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30
Q

What is the half-life of benzoylecgonine?

A

5-7 hours

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31
Q

In which situations does cocaine break down into benzoylecgonine?

A

In vivo and in vitro

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32
Q

What affects the interpretation of cocaine blood concentrations?

A

Instability of cocaine makes interpretation difficult

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33
Q

What does a high blood concentration of cocaine and low blood concentration of bze indicate?

A

Recent use

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34
Q

What does a low blood concentration of cocaine and high bze concentration indicate?

A

Recent use OR prior use

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35
Q

What does low cocaine blood concentration and low bze concentration indicate?

A

Recent use of small amount?

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36
Q

What are typical aspects of the cocaine high?

A

Feelings of exhilaration and euphoria
A sense of wellbeing
Enhanced alertness
Heightened energy
Great self-confidence

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37
Q

What may contribute to the street violence associated with cocaine use?

A

Increased aggressive behaviour

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38
Q

What generally produces mild to moderate effects of cocaine?

A

Single, low to moderate doses in naive subjects or in users who have not yet progressed to heavy, chronic use

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39
Q

When are severe effects of cocaine most likely?

A

With high dosages, particularly in chronic users

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40
Q

What state of mind can cocaine induce?

A

Temporary paranoid psychosis with delusions and hallucinations

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41
Q

What are the risk factors for cocaine psychosis?

A

Male
Increased dose and/or increased duration of use
IV route

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42
Q

What are cocaine bugs?

A

Sensation that hundreds of bugs are crawling over or under the user’s skin

43
Q

What is the hallucination of cocaine bugs called?

A

Delusional parasitosis

44
Q

Describe the structure of amphetamine

A

The parent compound of a family of synthetic psychostimulants that are structurally related to DA.

45
Q

What is the mechanisms of amphetamine and methamphetamine action?

A

Both are indirect agonists of the catecholaminergic systems

46
Q

What are the two actions of amphetamines and methamphetamine?

A

Molecules enter DA nerve terminals via uptake by DAT and cause vesicles to release DA.
DA is then transported out of the cell by a reversale of the DAT.
Result is very high DA in the synaptic cleft.

47
Q

When and where did methamphetamine hydrochloride in a crystalline form suitable for smoking begin showing up?

A

1980s
Hawaii

48
Q

What are methamphetamine HCl crystals called?

A

Ice or crystal

49
Q

Why is meth “ice” used?

A

Inexpensive to make and highly addictive

50
Q

What is methamphetamine usually synthesized from?

A

Peseudoephedrine

51
Q

Describe an amphetamine “run”

A

Some users (“speed freaks”) go on binges (“runs”) of repeated IV injections to experience recurrent highs.

52
Q

What happens during an amphetamine run?

A

Drug is typically injected about every 2 hours for as long as 3 to 6 days, with little sleep or eating

53
Q

What is speedball?

A

IV amphetamine or methamphetamine combined with heroin

54
Q

Describe the rate of metabolism for amphetamine and methamphetamine

A

Slow

55
Q

Why do users of amphetamines obtain a longer-lasting high than do users of cocaine?

A

Amphetamines have long half-lives

56
Q

Why do amphetamines have potent sympathomimetic actions?

A

NE-releasing effects occur in the brain and sympathetic nervous system

57
Q

Describe the behavioural and neuronal effects of amphetamine

A

Heightened alertness
Increased confidence
Feelings of exhilaration
Reduced fatigue
Generalized sense of well-being
Delay in sleep onset
Sustained physical effort without rest
Highly reinforcing

58
Q

Why are amphetamines banned in athletic competitions?

A

Can enhance athletic performance

59
Q

When and where was crystallized meth first discovered?

A

Japan 1919

60
Q

What were the original effects of meth determined to be?

A

Alleviate fatigue
Induce alertness
Well-being

61
Q

Why was meth popular in WWII?

A

Used by pilots to sustain them on long missions

62
Q

What effects does methamphetamine have in addition to its effects on DA?

A

Influences serotonin and norepinephrine levels

63
Q

What can long-term effects on serotonin levels by meth lead to?

A

Changes in behaviour and increased aggression

64
Q

Name the stereoisomers of meth

A

I- and d-

65
Q

What is the use of I-Meth (levomethamphetamine)?

A

Used clinically, e.g., Vicks inhaler

66
Q

What is the use of D-Meth (dextromethamphetamine)?

A

Available via prescription

67
Q

What isomer is generally used in abused meth?

A

mixture of d-Meth, which is much more active centrally, and I-Meth

68
Q

What is Desoxyn?

A

Meth still prescribes in US

69
Q

What is Desoxyn prescribed for?

A

Weight loss
Narcolepsy
ADHD

70
Q

What are the possible routes of administration for meth?

A

Smoking
Inhalation
Injection
Oral

71
Q

What are the short-term effects of meth?

A

Euphoria
Increased energy levels
Restlessness and irritability
Increased heart rate/blood pressure
Hyperthermia

72
Q

Describe the methamphetamine rush

A

Smoking, inhalation and injection produce rapid effects and the initial rush can last up to 5 mins

73
Q

Describe the meth high

A

Duration of a longer lasting drug-induced high can last over 12 hours

74
Q

What are the long-term effects of meth?

A

Psychosis - paranoid delusions, hallucinations
Aggressive behaviour
Changes in brain functions
Severe tooth decay (“meth mouth”)

75
Q

What is the half-life of meth?

A

12 hours

76
Q

Compare meth and cocaine

A

Meth has a slower metabolism
Smoking meth can induce a high lasting well over 8 hours, cocaine high usually lasts up to one hour
This can lead to prolonged effects and may be associated with an increased risk of psychosis

77
Q

What is MDMA (3,4-methylenedioxy-methamphetamine)?

A

A synthetic drug that alters mood and perception

78
Q

Describe the chemical structure of MDMA.

A

Chemically similar to both stimulants and hallucinogens

79
Q

What are the general effects of MDMA?

A

Produces feelings of increased energy, pleasure, emotional warmth
Distorted sensory and time perception

80
Q

Where was MDMA initially popular?

A

Nightclub scene and raves

81
Q

Since MDMA has properties that fit into stimulant and hallucinogen categories of drugs, what is it often categorized as?

A

An entactogen

82
Q

Describe the 5-HT mechanisms of MDMA.

A

Enhances 5-HT neurotransmission, which is important for characteristic effects of MDMA
Increased social interaction, friendliness, empathy

83
Q

What are the effects of the DA mechanisms of action of MDMA?

A

Produces increased energy/activity and acts in the reward system to reinforce behaviours

84
Q

What are the effects of the NE mechanism of action of MDMA?

A

Increases heart rate and blood pressure

85
Q

Through which route of injection is MDMA rapidly absorbed?

A

Oral

86
Q

What is the half-life of MDMA?

A

6-8

87
Q

How long do the psychoactive effects of MDMA last?

A

2-4 hours

88
Q

Which lasts longer in MDMA - objective impairment of mental function or subjective effects?

A

Objective

89
Q

Describe the long term toxicity of MDMA.

A

Increase in 5-HT in the synapse leads to improved mood and sensory alterations
At high doses the extensive release of 5-HT may produce acute psychotic symptoms AND chemical damage to cells.

90
Q

What are the long-term psychiatric problems of MDMA?

A

Greater impulsivity and lack of self-control
Panic attacks
Paranoia
Hallucinations
Severe depression

91
Q

What is molly? Ecstasy?

A

Molly - powdered MDMA
Ecstasy - pill form of MDMA

92
Q

Why is it unlikely someone will use MDMA for the intent of SA?

A

Can make you more reactive
No memory loss
Not sedating

93
Q

How could MDMA be used for SA?

A

Those on it may be more sexually aroused, feel loved, and thus ‘consent’ to sex

94
Q

What is the traditional definition of drug-facilitated SA?

A

Offenses in which victims are subjected to nonconsensual sexual acts while they are incapacitated or unconscious due to the effects alcohol and/or drugs, and are therefore unable to consent

95
Q

Why is a complainants state of incapacitation an important consideration in cases of SA?

A

It has implications for the issue of being able to provide consent

96
Q

What is methylphenidate (ritalin)

A

CNS stimulant

97
Q

What is methylphenidate’s mechanism of action?

A

To release and increase dopamine

98
Q

Describe the mechanism of action of methylphenidate in the brain.

A

Binds to DAT and NET, blocking reuptake of DA and NE, elevating extracellular levels of both transmitters and stimulating overall catecholaminergic neurotransmission

99
Q

What is the abuse potential of methylphenidate?

A

High

100
Q

When are the effects of ritalin similar to those of cocaine? Why?

A

When used intranasally
Leads to a rapid release of synaptic dopamine producing a significant high

101
Q

What are the psychiatric symptoms of methylphenidate acute toxicity?

A

Euphoria
Delirium
Confusion
Toxic psychosis
Hallucinations

Extreme anger with threats have also been reported

102
Q

What are the guidelines for abuse prevention of Ritalin?

A

Shared responsibility between physician, parents and patient (usually a child)
Education about abuse potential
Strict use by patient only
Extreme consequences of abuse should be addressed

103
Q
A

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