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Pharmacology > CNS > Flashcards

CNS Flashcards

1
Q

Excitatory NTs

A

Acetylcholine
Glutamate
Substance P
Enkephalins

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2
Q

Inhibitory NTs

A

Norepinephrine
Dopamine
Serotonin
GABA

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3
Q

Sedative Hypnotics

A

two categories, Benzodiazepines, Nonbenzodiazepines. main uses are for sleep, anxiety, seizures. highly lipid soluble, metabolized via liver (adipose sequestering, active metabolites)

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4
Q

GABA Receptor

A

Ion channel receptor, GABA binds and allows more chloride ions to enter the cell. This causes the cell to be hyperpolarized, Sedative hypnotics either mimic GABA or enhance the binding of GABA

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5
Q

Benzodiazepines MOA

A

Bind to the benzodiazepine receptor and facilitate opening of the GABA receptor

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6
Q

Benzodiazepines side effects

A

sedation, Anterograde amnesia (memory loss), Tolerance and dependence, Residual effects ( drowsiness, confusion, psychomotor slowing)

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7
Q

Alprazolam (Xanax)

A

benzodiazepine, short duration, used for anxiety

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8
Q

Lorazepam (Ativan)

A

benzodiazepine, Short duration, used for sleep, anxiety, seizures, alcohol withdrawal

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9
Q

Temazepam (Restoril)

A

benzodiazepine, Short duration, used for sleep

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10
Q

Clonazepam (Klonopin)

A

benzodiazepine, intermediate duration, used for Anxiety, sleep, seizure (ODT)

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11
Q

Chlordiazepoxide (Librium)

A

benzodiazepine, long duration, used for alcohol withdrawal

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12
Q

Diazepam (Valium)

A

benzodiazepine, Long duration, used for Muscle relaxant, anxiety, sleep, seizure (rectal)

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13
Q

Benzodiazepines and Older Adults

A

Decreased metabolism, Increased susceptibility to side effects, Increased body fat leading to more adipose sequestering

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14
Q

Barbiturates MOA

A

Binding site on the GABA receptor and increase the duration the GABA receptor is open

Antagonize glutamate

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15
Q

Barbiturates side effects

A

sedation, Narrow therapeutic index,
High abuse potential, Ataxia

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16
Q

Phenobarbital (Luminal)

A

barbiturate, Used for seizures, alcohol withdrawal, half life = days

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17
Q

Butalbital (Fioricet or Esgic)

A

barbiturate, used for Headaches

In combination with acetaminophen and caffeine

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18
Q

Primidone (Mysoline)

A

barbiturate, used for Essential tremors, seizures
Metabolized to phenobarbital, avoid in elderly

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19
Q

Zolpidem (Ambien)

A

Z drug, used for sleep

IR and CR formulations; Females receive higher blood levels than males

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20
Q

Zaleplon (Sonata)

A

z drug, used for sleep
high fat meal delay absorption

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21
Q

Eszopiclone (Lunesta)

A

Z drug, common use: sleep
Longer acting

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22
Q

Z drugs MOA

A

Selective agonist of GABAA receptor

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23
Q

Z drugs side effects

A

sedation,

Complex sleep behavior (black box)
Psychomotor slowing (increased in elderly)
Psychiatric and behavioral effects

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24
Q

Buspirone MOA

A

serotonin agonist

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25
Q

Buspirone indications

A

general anxiety disorder

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26
Q

Buspirone limitations

A

Moderate efficacy
Slow onset (2-4 weeks)
Frequent dosing

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27
Q

Buspirone advantages

A

Well tolerated
Low risk of tolerance / dependence

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28
Q

Pharmacokinetics of Antidepressants

A

Onset of action: 2-4 weeks

Full Effect:
~3 months

Initial increase in suicidal thoughts and behaviors

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29
Q

Selective Serotonin Receptor Inhibitor (SSRI) MOA

A

Inhibit the reuptake of serotonin into the presynaptic nerve (to leave more in synaptic cleft)
Selective for serotonin synapses

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30
Q

Selective Serotonin Receptor Inhibitor (SSRI) side effects

A

Nausea and diarrhea
Jitteriness, anxiety, headache
Sexual dysfunction
Withdrawal effects if abruptly stopped
Increase suicidal thoughts

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31
Q

Citalopram (Celexa)

A

SSRI, Depression, anxiety, cardiac toxicity

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32
Q

Escitalopram (Lexapro)

A

SSRI, Depression, anxiety

33
Q

Fluoxetine (Prozac)

A

SSRI, Depression, anxiety, self tapers

34
Q

Paroxetine (Paxil)

A

SSRI, Depression, anxiety, more drowsiness

35
Q

Sertraline (Zoloft)

A

SSRI, Depression, anxiety

36
Q

Vortioxetine (Trinetellix)

A

SSRI, Depression, anxiety, severe GI side effects

37
Q

Vilazodone (Viibyrd)

A

SSRI, Depression, anxiety, severe GI side effects

38
Q

Serotonin-Norepinephrine Receptor Inhibitor (SNRI) MOA

A

Selectively inhibit the reuptake of serotonin and norepinephrine into the presynaptic nerve
Effects vary between the drugs in this class

39
Q

Serotonin-Norepinephrine Receptor Inhibitor (SNRI) side effects

A

Nausea and diarrhea
Increased HR, BP, CNS activation (insomnia, agitation)
Sweating
Sexual dysfunction
Increase suicidal thoughts

40
Q

Duloxetine (Cymbalta)

A

SNRI, used for Depression, neuropathic pain, fibromyalgia

41
Q

Milnacipran (Savella)

A

SNRI, fibromyalgia

42
Q

Venlafaxine (Effexor XR)

A

SNRI, used for depression, anxiety, PTSD

43
Q

Desvenlafaxine (Pristiq)

A

SNRI, used for Depression, vasomotor symptoms

44
Q

Tricyclic Antidepressants (TCA) MOA

A

Inhibit the reuptake of serotonin, norepinephrine, and dopamine into the presynaptic nerve

Effect many other receptors resulting in more side effects and toxicity

45
Q

Tricyclic Antidepressants (TCA) side effects

A

blurred vision
Sedation, confusion, delirium (elderly)
Orthostatic hypotension
Cardiac toxicity (arrhythmias)

46
Q

Amitriptyline (Elavil)

A

TCA, used for Migraine, neuropathic pain, postherpetic neuralgia, insomnia, depression

47
Q

Desipramine (Norpramin)

A

TCA, used for Migraine, neuropathic pain, postherpetic neuralgia, insomnia, depression

48
Q

Nortriptyline (Pamelor)

A

TCA, used for Migraine, neuropathic pain, postherpetic neuralgia, insomnia, depression

49
Q

Imipramine (Tofranil)

A

TCA, used for Migraine, neuropathic pain, postherpetic neuralgia, insomnia, depression

50
Q

Clomipramine (Anafranil)

A

TCA, used for Migraine, neuropathic pain, postherpetic neuralgia, insomnia, depression

51
Q

Doxepin (Silenor)

A

TCA, used for antihistamine

52
Q

Monoamine Oxidase Inhibitor (MAOI) MOA

A

MAO breaks down neurotransmitters
MAOA and MAOB
MAOIs prevent the breakdown of neurotransmitters resulting in an increase in neurotransmitters in the nerve ending

53
Q

Monoamine Oxidase Inhibitor (MAOI) side effects

A

Orthostatic hypotension
Confusion, delirium
Hypertensive crisis (food interaction)

54
Q

Phenelzine (Nardil)

A

MAOIs, used for depression, not commonly used

55
Q

Tranylcypromine (Parnate)

A

MAOI, used for depression, not commonly used

56
Q

Selegiline (Zelapar, Emsam)

A

MAOI, used for parkinsons, Selective for MAOb

57
Q

Bupropion (Wellbutrin) and side effects

A

Other antidepressant
used for Depression, smoking cessation
side effects n/v, tremor, seizure, insomnia

58
Q

Trazadone (Desyrel) and side effects

A

Other antidepressant

used for Insomnia, depression

Mixed serotonin receptor activity

side effects: Sedation, dizziness, OH*

59
Q

Mirtazapine (Remeron) and side effects

A

Other antidepressant

used for Appetite stimulation, insomnia, depression

Serotonin and alpha2 antagonist

side effects: Sedation, weight gain, OH*

60
Q

Lithium

A

for bipolar disorder,

Well distributed to all tissues in the body
- Not metabolized
- Excreted in urine

concerns: Lithium toxicity

61
Q

Symptoms of Lithium Toxicity

A

altered mental status, GI, cardiac symptoms are signs of lithium toxicity

62
Q

Mechanism of Antipsychotics

A

Dopamine antagonist
-Block postsynaptic dopamine receptors
-Newer agents also block serotonin receptors

First generation high affinity for D2

Second generation inhibit serotonin receptors and have weak affinity for D2

63
Q

Extrapyramidal Effects of antipsychotics

A

Akathisia
Dystonia
Pseudoparkinsonism
Tardive dyskinesia

64
Q

First Generation Antipsychotics

A

Typical antipsychotics, Effective for positive symptoms, Increased side effects, Orthostasis improves after a few days

65
Q

Chlorpromazine (Thorazine)

A

first generation antipsychotics, used for Antipsychotic

66
Q

Fluphenazine (Prolixin)

A

first generation antipsychotics
used for Antipsychotic, Tourette’s

67
Q

Haloperidol (Haldol)

A

first generation antipsychotics
used for Antipsychotic, aggressive behavior, nausea

68
Q

Thiothixene (Navane)

A

first generation antipsychotics
used for antipsycotic

69
Q

Second Generation Antipsychotics

A

Atypical antipsychotics, Effective for positive, negative, and cognitive symptoms, More metabolic side effects than 1st generation, Orthostasis improves after a few days

70
Q

Clozapine (Clozaril)

A

Second Generation Antipsychotics
used for Antipsychotic (later line due to side effects

71
Q

Risperidone (Risperdal)

A

Second Generation Antipsychotics
used for Antipsychotic

72
Q

Quetiapine (Seroquel)

A

Second Generation Antipsychotics
used for Sleep, delirium, antipsychotic

73
Q

Olanzapine (Zyprexa)

A

Second Generation Antipsychotics
used for Antipsychotic (increased metabolic AE)

74
Q

Ziprasidone (Geodon)

A

Second Generation Antipsychotics
used for Antipsychotic

75
Q

Aripiprazole (Abilify)

A

Second Generation Antipsychotics
used for Antipsychotic, depression

76
Q

Short-acting Intramuscular Antipsychotics

A

Acute psychosis
Onset is minutes and last a few hours

77
Q

Long-acting Intramuscular Antipsychotics

A

Improve adherence leading to decreased hospitalizations and relapses
Traditional side effects in addition to injection related side effects

78
Q

Serotonin syndrome symptoms

A

Hyperreflexia
Clonus
Mydriasis
Diaphoresis
Shivering
Diarrhea

79
Q

Neuroleptic Malignant Syndrome symptoms

A

Rigidity
Catatonia
Stupor

Pharmacology (10 decks)

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