Cocaine Flashcards

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1
Q

What arethe effects of psychostimulants?

A
  • Alertness, wakefulness, and
    locomotion
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1
Q

What are stimulants?

A
  • Psychoactive drugs producing a
    temporary increase in mental function
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2
Q

Name some psychomotor stimulants

A

Cocaine, amphetamines, caffeine, nicotine

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3
Q

Describe crack cocaine

A

Surge of ‘crack’ cocaine use in the
80’s described by many as an
epidemic

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4
Q

Describe the chemistry of cocaine

A
  • Isolated as a water soluble HCl salt (cocaine HCl)
  • Administered by oral, IV, or intranasal routes
  • Can be recrystallized as a free base structure
  • Can be precipitated by heating with baking soda
  • ‘Crack’ cocaine
  • Freebase and crack cocaine delivered by inhalation
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5
Q

Describe cocaine pharmacokinetics

A

Inhalation (smoking) or intranasal (snorting)
result in rapid access to the CNS.

Metabolized by esterases, CYP450 in liver.

Cocaethylene is an active metabolite formed
in the presence of alcohol – longer lasting
than cocaine and greater cardiotoxic effects.

Methylecgonidine is produced by pyrolysis
(heating) of cocaine and is detectable in urine

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6
Q

Describe BBB permeability of cocaine

A

Cocaine is amphipathic– meaning it has both hydrophilic and lipophilic nature

Inhalation and intranasal admin both result in rapid uptake into brain and
pronounced psychoactive effects

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7
Q

Describe cocaine effects

A

Euphoria

Dysphoria
* anxiety

Psychosis
* Paranoia
* Formication

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8
Q

Describe psychomotor stimulation

A

Cocaine
administration results in marked locomotor
hyperactivity.

Cocaine administration results in stereotyped
behaviours. Common stereotypies include head
bobbing, pacing, repetitive rearing, excess
grooming.

Comparable effects in humans include
compulsive activities such as obsessive
cleaning, sorting, organizing.

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9
Q

Describe cocaine in animal models

A

Cocaine administration causes
hyperactivity in rodents – simple
measurement of intoxication

  • Animals will self-administer to the
    point of personal neglect, anorexia,
    and increased mortality
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10
Q

Describe cocaine mechanism

A
  • Cocaine is an SNDRI (serotonin, norepinephrine, and
    dopamine reuptake inhibitor).
  • Cocaine blocks neurotransmitter reuptake such as at the
    dopamine transporter (DAT).
  • Also causes decrease in monoamine synthesis through
    presynaptic autoreceptors.
  • At elevated doses cocaine blocks Na+ channels and can
    be used as a topical anaesthetic.
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11
Q

Describe tolerance

A
  • Cocaine tolerance develops acutely and transiently
  • Intermittent use produces sensitization rather than tolerance
  • In animal models:
  • Continuous infusion via minipump results in tolerance to the effects of cocaine
  • Daily use (intermittent) sensitizes the psychomotor and reinforcing effects
  • Both animals and humans show cross-sensitization to other stimulants (esp.
    amphetamines)
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12
Q

Describe cocaine withdrawal

A
  • Three phases observed in binge users of cocaine:
  • Binge use refers to episodic use for extended periods (hours or days)
    without interruption (or sleep)
  1. Crash (15-30 minutes following final dose)
  2. Withdrawal (hours-days after final dose)
  3. Extinction
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13
Q

Describe cocaine crash

A
  • Many of the effects of withdrawal may in fact be psychological rather than physiological
    as we cannot demonstrate dependence in animals
  • Acute withdrawal effects of a crash:
  • Dysphoria, agitation, anxiety, and depression
  • Gives way to fatigue after brief period (may be a few hours)
  • Exhaustion results in hypersomnolence (prolonged sleep)
  • Sleep can be interrupted by brief periods of waking and hyperphagia
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14
Q

Describe dysphoric syndrome symptoms

A

Gradual onset of a dysphoric syndrome – boredom, anergia, anhedonia, anxiety, and
increased craving

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15
Q

Describe cocaine toxicity

A
  • Acute overdose results from several main effects:
  • Reduced seizure threshold
  • Due to general increase in neurotransmitter release
  • Cardiovascular effects
  • Increased heart rate and blood pressure can increase risk of stroke, cerebral hemorrhage, tachycardia
    and arrhythmia
  • Hyperthermia