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Pharm Block 3 > CNS Stimulants > Flashcards

CNS Stimulants Flashcards

1
Q

Methylxanthine compound found in coffee, cocoa, and kola nut

A

Caffeine*

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2
Q

Mechanism of action of caffeine*

A
  • Blocks adenosine* receptors (equilibrium-competitive antagonist) of both postsynaptic and presynaptic adenosine receptors
  • Inhibition of phosphodiesterase
  • Induces release of Ca from intracellular stores (endoplasmic reticulum)
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3
Q

CNS effects of caffeine*

A
  • increased alertness and capacity for tasks requiring sustained attention
  • decreased fatigue and drowsiness
  • can cause nervousness, restlessness, and tremors
  • high doses can stimulate medullary respiratory, vasomotor and vagal centers
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4
Q

Peripheral actions of caffeine*

A
  • stimulates myocardium – positive chronotropic and inotropic effects
  • dilates coronary and general systemic blood vessels but constricts cerebral blood vessels
  • diuretic effect
  • increases gastric secretion
  • modest bronchodilator activity
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5
Q

Therapeutic usefulness of caffeine*

A
  • aid to stay awake

- treatment of headache

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6
Q

Toxicity and chronic use of caffeine*

A

Toxicity/overdose:
- excessive CNS stimulation, nervousness, insomnia, excitement

Chronic use:

  • Tolerance development to stimulant effects of caffeine
  • Physical dependence develops at a dose of 2 cups of coffee a day
    • withdrawal symptoms: fatigue/sleepiness; headaches; nausea; vomiting(rare)
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7
Q

Compounds that act through enhancement of catecholaminergic neuro-transmission

A

Sympathomimetic stimulants

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8
Q

Examples of sympathomimetic stimulants

A

methylphenidate, cocaine, amphetamine* nonamphetamine*

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9
Q

Psychoactive alkaloid present in coca plant

A

cocaine*

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10
Q

Chemistry of cocaine*

A
  • weak base, unprotonated form (unionized) predominates at alkaline pH
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11
Q

How do you test for cocaine* use

A

look for metabolites in urine

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12
Q

Metabolism of cocaine*

A
  • metabolized primarily by serum and liver esterases
  • can also be demethylated at the nitrogen
  • very short half-life (50min)
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13
Q

Mechanism of action of cocaine*

A
  • potent inhibitor of the reuptake of norepinephrine, dopamine, and serotonin
  • its receptor on transporter for dopamine, competes for binding of the endogenous ligand resulting in increased ligand in the synapse
  • central reinforcing effects believed due to action on dopamine synapses in the ventral striatum
  • increases tyrosine and tryptophan hydroxylase
  • local anesthetic; vasoconstrictor
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14
Q

Pharmacological effects of cocaine*

A
  • Peripheral sympathomimetic - due to increased NE
    • vasoconstriction; tachycardia
  • Increased alertness; vigilance (increased NE in CNS)
  • Euphoria, feelings of elation, well being and competency
    • Due to increase in DA in mesolimbic circuit
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15
Q

Toxicity and chronic use of cocaine*

A
  • Tolerance and physical dependence occurs with heavy use
  • Withdrawal symptoms - mild
  • Neurotoxicological effects - damage to dopamine systems?
  • Overdose can cause seizures ad/or cardiovascular effects
  • Fetal effects are more significant than alcohol
    • Low birth weight
    • Learning and emotional problems
    • attachment disorder
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16
Q

Cocaine* abuse

A
  • Psychological dependence - high abuse liability
    • Very reinforcing
    • Results in drug craving and drug seeking
17
Q

Therapeutic use of cocaine*

A

Local anesthesia in upper respiratory track

18
Q

Chemistry of amphetamine* and amphetamine-like drugs

A
  • most are alpha-methyl phenethylamine derivatives

- weak base

19
Q

Does amphetamine* and amphetamine-like drugs or cocaine* have longer durations of action

A

amphetamine* and amphetamine-like drugs (4-6 hours)

20
Q

Metabolism of amphetamine* and amphetamine-like drugs

A
  • Deamination to benzoic acid (predominate route)

- Also excreted unchanged as amphetamine*-base excretion increased in acid urine

21
Q

MOA of amphetamine* and amphetamine-like drugs

A
  • Release NE, DA, and Serotonin
  • Blocks transmitter reuptake into presynaptic terminals
  • Direct partial agonist of alpha-adrenergic receptors
  • MAO inhibition (at high doses)
22
Q

Pharmacological properties of amphetamine* and amphetamine-like drugs

A
  • Wakefulness, alertness, decreased fatigue (more done, but more errors)
  • Enhance athletic and intellectual performance
  • Elevation of mood; increased self-confidence
  • Increase in motor and speech activities; speed
  • Respiratory stimulation
  • Decrease in appetite
  • Peripheral sympathomimetic effects
23
Q

Methamphetamine*

A
  • amphetamine* with better CNS bioavailability, more CNS effect, higher abuse liability
24
Q

Methylphenidate*

A
  • not actually an amphetamine* but structurally and mechanistically very similar
25
Q

Used for narcolepsy

A

Amphetamine*

26
Q

Used for ADHD

A

Amphetamine* and methylphenidate

27
Q

Side effects of amphetamine* and amphetamine-like drugs

A

insomnia, abdominal pain, anorexia, weight loss, suppression of growth, fever

28
Q

Toxicity of amphetamine* and amphetamine-like drugs

A
  • acute toxicity

Pharm Block 3 (10 decks)

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