CNS Pharmacology Flashcards

1
Q

Major function of CNS

A

Processing info and generating the appropriate response

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2
Q

Name the excitatory CNS Neurotransmitters

A

Acetylcholine
Dopamine
Glutamate (Most abundant)
(Nor)epinephrine

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3
Q

Name the inhibitory CNS neurotransmitters

A

Gamma-aminobutyric acid

Serotonin

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4
Q

Drug classes causing CNS depression (incr inhibition, decr excitation)

A
(From lowest effect to greatest)
Anesthetics (general)
Narcotics
Hypnotics
Sedatives
Tranquilizers
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5
Q

Drug classes causing CNS stimulation (incr excitation, decr inhibition)

A

(From lowest effect to greatest)
Analeptics
Psychomotor Stimulants
Convulsants

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6
Q

The balance between excitation and inhibition in the brain can mean life or death? True or False

A

True

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7
Q

What is the process of CNS excitability by Glutamate?

A

When GLU activates the NMDA receptor > influx of Ca + Na > excitation

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8
Q

What is the mechanism of GABA inhibitory effect on neurons?

A

When you activate GABA a receptor > influx of Cl > decr ability of cell to respond/dampens cell’s activity

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9
Q

What is going on neurologically with a seizure?

A

Excessive and abnormal brain cell activity arising from too much excitation or too little inhibition

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10
Q

What is the mechanism of action of anti-convulsants?

A

Acts to limit the initiation or spread of a seizure by working to enhance GABA > reduces excitability of the neurons

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11
Q

Phenobarbital

A

Barbiturate

Acts as anticonvulsant at doses below those that produce anesthesia

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12
Q

What are the general effects of tranquilizers-sedatives?

A

They often work synonymously to decrease anxiety and produce a mild sense of drowsiness; calming effect or chemical restraint

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13
Q

What are the classes of tranquilizers-sedatives?

A

Phenothiazine, butyrophenone, and benzodiazepines (GABA)

  • acepromazine
  • diazepam
  • midazolam
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14
Q

What are hypnotic sedatives?

A

Agents that produce calm (sedative) and sleep (hypnosis); dose-dependent spectrum of sleep, CNS depression, and sedation ; NOT anesthesia

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15
Q

Uses of Narcotics

A

Induces deep sleep; drug class = morphine

- patients cannot be easily aroused from sleep

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16
Q

What does it mean that the effects of CNS depressants can be additive or synergistic?

A

This may cause global depression of critical CNS functions (e.g. Alertness, breathing, CV control) and lead to unexpected coma and/or death

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17
Q

Adrenaline’s function

A

Fight or flight NT

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18
Q

Function of Norepinephrine

A

Concentration NT

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19
Q

Dopamine’s function

A

Pleasure NT

20
Q

Serotonin’s function

A

Mood NT

21
Q

GABA’s function

A

Calming NT

22
Q

Acetylcholine’s function

A

Learning NT

23
Q

Glutamate’s function

A

Memory NT

24
Q

Endorphin’s function

A

Euphoria NT

25
Q

What NTs are classified as monoamines (biogenetic amines)?

A
Epinephrine
Norepinephrine 
Dopamine
Histamine
Serotonin
26
Q

What NTs are classified as amino acids & derivatives?

A

Aspartate
Glycine
GABA
Glutamate

27
Q

What NTs are classified as neuropeptides?

A
ACTH
Endorphins
Somatostatin
Aldosterone
Enkephalins
TRH
28
Q

What are monoamines?

A

Substances that act as peripheral transmitters as well as those that act almost entirely within the CNS (dopamine)

  • synthesis, release, and elimination mechanisms in CNS are identical to peripheral neurons
  • DO NOT CROSS BBB
  • broken down by MOA
29
Q

What is the biosynthetic precursor of dopamine, EPI, and NE? Elimination method?

A

L-tyrosine; uptake or MAO

30
Q

What is the biosynthetic precursor of Histamine? Elimination method?

A

L-histadine; HMT

31
Q

What is the biosynthetic precursor of Serotonin? Elimination method?

A

L-tryptophan; uptake or MAO

32
Q

Define catecholamine

A
  • generally considered to be excitatory transmitters (esp. NE and DA) for most brain functions
  • drugs may activate or block receptors
33
Q

What is an example of a catecholamine used therapeutically?

A

Imipramine- inhibitor of CA + uptake (NE, EP, DA)

- used for narcolepsy, cataplexy (stimulates arousal)

34
Q

What is an example of a monoamine oxidase inhibitor?

A

Selegiline - used to treat canine cognitive dysfunction

35
Q

What are the effects of acetylcholine antagonists on CNS?

A

CNS depression, delirium, short-term memory loss

36
Q

Define serotonin (5-HT)

A
  • synthesized from L-tryptophan
  • eliminated similar to CA > degraded by MAO and uptake by 5-HT transporters
  • many 5-HT receptors
  • effects: regulation of mood, appetite, sleep/wake cycles, sensory perception
37
Q

Examples of serotonin therapeutic agent

A

Fluoxetine: SSRI
Used for OCD, aggression

  • clomipramine: NERI & SSRI
  • used for separation anxiety
38
Q

What are the effects of serotonin syndrome?

A

High body temp, tachycardia, diarrhea, and agitation

39
Q

What are the CNS effects of GABA agonists?

A

CNS depression

40
Q

GABA antagonists cause what CNS effects?

A

CNS Excitation

41
Q

Examples of GABA Therapeutic agents

A

-Barbiturates: GABA agonists
Uses: sedation, euthanasia
-Benzodiazepines: GABA agonist
Uses; anxiety, sedation

42
Q

Other examples of Catecholamine Therapeutic agents:

A
Acepromazine: DA antagonist
Uses: sedative
- Reserpine: destroys CA vesicles
Uses: sedative (works well in horses)
-Xylazine: alpha2 agonist
Uses: sedative/analgesic
43
Q

Drugs that block excitatory amino acids (EAAs) have what effects?

A

Decreased excitation or inhibition

44
Q

Example of an EAA Therapeutic Agent

A

Ketamine: NMDA receptor

Dissociative anesthetic

45
Q

Drugs in the same Rx class can have marked differences in ability to cross BBB? True or False?

A

True