CNS Pharmacology II: Stimulants & Depressants Flashcards

1
Q

What is a Psychoactive / Psychotropic drug?

A

Drugs that affects mood and behaviour

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2
Q

Which neurotransmitters are Amphetamines structurally similar to?

A

Dopamine & Noradrenaline

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3
Q

What are THREE ways in which Amphetamines increase DA and NA transmission?

A
  1. Increase secretion of DA and NA
  2. Compete with DA and NA degradative enzymes
  3. Competing with DA and NA re-uptake systems
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4
Q

Which neurons are mainly stimulated by amphetamines?

A

Noradrenergic neurons of the ANS

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5
Q

What FOUR ways do amphetamines act on Dopamine (DA) synapses?

A
  1. Compete with DA uptake carrier
  2. Compete with DA uptake into synaptic vesicles
  3. Inhibit DA degradation (at higher conc. via MAO)
  4. Bind to DA re-uptake transporter, causing it to act in reverse and transport free DA out of the nerve terminal
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6
Q

What TWO ways do amphetamines act on Noradrenaline (NA) synapses?

A
  1. Increase release of NA into synaptic cleft
  2. Inhibit NA re-uptake transporter
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7
Q

What are the FOUR Dopamine pathways in the brain?

A
  1. Nigrostriatal Pathway
  2. Mesolimbic Pathway
  3. Mesocortical Pathway
  4. Tuberoinfundibular
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8
Q

Which areas of the brain, known as the Reward Pathway, do drugs of abuse modify the action of DA in?

A
  • Ventral Tegemental Area (VTA)
  • Nucleus Accumbens
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9
Q

Which receptor in the CNS is Nicotine an agonist for?

A

Nicotinic Acetylcholine Receptor (nACh)

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10
Q

What does ACh release in DA neurons cause?

A

INCREASED DA release

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11
Q

Which nACh receptor is believed to be linked with addiction?

A

a4β2

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12
Q

What is the mechanism of action of Cocaine on DA or NA neurons?

A
  1. Cocaine binds to DA and NA re-uptake transporters, which inhibits DA and NA removal from synaptic cleft and degradation by MAO
  2. DA and NA remain in synaptic cleft activating the post-synaptic receptors and enhancing neurotransmission
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13
Q

What are TWO examples of Methylxanthines?

A
  1. Caffeine
  2. Theophylline
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14
Q

Which neurotransmitter are Methylxanthines structurally similar to?

A

Adenosine
* Inhibitory NT

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15
Q

How do Caffeine and Theophylline act on Adenosine receptors?

A

Non-Selective Antagonists of the A1 and A2 receptors

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16
Q

Which drug is used to treat ADHD?

A

Methylphenidate (Ritalin)

17
Q

How do CNS depressants work?

A

Increase GABA transmission, which inhibits post-synaptic neuron activity

18
Q

What is Ethanol’s effects on CNS neurons?

A
  • Increase inhibitory neurotransmission: GABA, Glycine, Adenosine
  • Decrease excitatory neurotransmission: Glutamate (NMDA receptors)
19
Q

What is the mechanism of action of Benzodiazepines?

A
  • Benzo binds to GABAa receptor at allosteric site
  • Benzo enhances affinity and response to GABA
  • Benzo facilitates opening of GABA-activated Cl- channels
  • Benzo increase frequency of channel opening
20
Q

What are Benzodiazepines with LONG half-lives useful for?

A

Anxiolytics
* Rapid onset of action with long lasting action

21
Q

What are Benzodiazepines with SHORT half-lives useful for?

A

Insomnia
* Rapid onset or sedative effects that dissipate with sleep

22
Q

What drug blocks the binding and action of Benzodiazepines?

A

Flumazenil
* Benzo Antagonist

23
Q

Which SIX neutron types are Opioid Receptors found?

A
  1. Glutamate
  2. NA
  3. ACh
  4. GABA
  5. 5-HT
  6. Substance P
24
Q

How does Morphine induce euphoria in GABA and DA neurons?

A
  • Inhibits GABA release
  • Reduced inhibition of DA neurons (increased DA in synaptic cleft)
25
Q

What are TWO examples of Opioid antagonists?

A
  1. Naloxone
  2. Naltrexone

(Competitive Antagonism)