CNS Pharmacology Flashcards by Payton Bayless

Major function of CNS

Processing info and generating the appropriate response

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Name the excitatory CNS Neurotransmitters

Acetylcholine
Dopamine
Glutamate (Most abundant)
(Nor)epinephrine

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Name the inhibitory CNS neurotransmitters

Gamma-aminobutyric acid

Serotonin

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

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

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

(From lowest effect to greatest)
Analeptics
Psychomotor Stimulants
Convulsants

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

True

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What is the process of CNS excitability by Glutamate?

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

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What is the mechanism of GABA inhibitory effect on neurons?

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

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What is going on neurologically with a seizure?

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

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What is the mechanism of action of anti-convulsants?

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

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Phenobarbital

Barbiturate

Acts as anticonvulsant at doses below those that produce anesthesia

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What are the general effects of tranquilizers-sedatives?

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

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What are the classes of tranquilizers-sedatives?

Phenothiazine, butyrophenone, and benzodiazepines (GABA)

acepromazine
diazepam
midazolam

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What are hypnotic sedatives?

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

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Uses of Narcotics

Induces deep sleep; drug class = morphine

- patients cannot be easily aroused from sleep

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

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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Adrenaline’s function

Fight or flight NT

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Function of Norepinephrine

Concentration NT

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Dopamine’s function

Pleasure NT

Serotonin’s function

Mood NT

GABA’s function

Calming NT

Acetylcholine’s function

Learning NT

Glutamate’s function

Memory NT

Endorphin’s function

Euphoria NT

What NTs are classified as monoamines (biogenetic amines)?

``` Epinephrine Norepinephrine Dopamine Histamine Serotonin ```

What NTs are classified as amino acids & derivatives?

Aspartate Glycine GABA Glutamate

What NTs are classified as neuropeptides?

``` ACTH Endorphins Somatostatin Aldosterone Enkephalins TRH ```

What are monoamines?

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

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

L-tyrosine; uptake or MAO

What is the biosynthetic precursor of Histamine? Elimination method?

L-histadine; HMT

What is the biosynthetic precursor of Serotonin? Elimination method?

L-tryptophan; uptake or MAO

Define catecholamine

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

What is an example of a catecholamine used therapeutically?

Imipramine- inhibitor of CA + uptake (NE, EP, DA) | - used for narcolepsy, cataplexy (stimulates arousal)

What is an example of a monoamine oxidase inhibitor?

Selegiline - used to treat canine cognitive dysfunction

What are the effects of acetylcholine antagonists on CNS?

CNS depression, delirium, short-term memory loss

Define serotonin (5-HT)

- 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

Examples of serotonin therapeutic agent

Fluoxetine: SSRI Used for OCD, aggression - clomipramine: NERI & SSRI - used for separation anxiety

What are the effects of serotonin syndrome?

High body temp, tachycardia, diarrhea, and agitation

What are the CNS effects of GABA agonists?

CNS depression

GABA antagonists cause what CNS effects?

CNS Excitation

Examples of GABA Therapeutic agents

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

Other examples of Catecholamine Therapeutic agents:

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

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

Decreased excitation or inhibition

Example of an EAA Therapeutic Agent

Ketamine: NMDA receptor | Dissociative anesthetic

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

True