CNS Flashcards by Noah Huff

Q

Excitatory NTs

A

Acetylcholine
Glutamate
Substance P
Enkephalins

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Q

Inhibitory NTs

A

Norepinephrine
Dopamine
Serotonin
GABA

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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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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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Q

Benzodiazepines MOA

A

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

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Q

Benzodiazepines side effects

A

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

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Q

Alprazolam (Xanax)

A

benzodiazepine, short duration, used for anxiety

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Q

Lorazepam (Ativan)

A

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

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Q

Temazepam (Restoril)

A

benzodiazepine, Short duration, used for sleep

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Q

Clonazepam (Klonopin)

A

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

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Q

Chlordiazepoxide (Librium)

A

benzodiazepine, long duration, used for alcohol withdrawal

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Q

Diazepam (Valium)

A

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

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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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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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Q

Barbiturates side effects

A

sedation, Narrow therapeutic index,
High abuse potential, Ataxia

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Q

Phenobarbital (Luminal)

A

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

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Q

Butalbital (Fioricet or Esgic)

A

barbiturate, used for Headaches

In combination with acetaminophen and caffeine

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Q

Primidone (Mysoline)

A

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

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Q

Zolpidem (Ambien)

A

Z drug, used for sleep

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

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Q

Zaleplon (Sonata)

A

z drug, used for sleep
high fat meal delay absorption

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Q

Eszopiclone (Lunesta)

A

Z drug, common use: sleep
Longer acting

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Q

Z drugs MOA

A

Selective agonist of GABAA receptor

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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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Q

Buspirone MOA

A

serotonin agonist

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Buspirone indications

general anxiety disorder

Buspirone limitations

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

Buspirone advantages

Well tolerated Low risk of tolerance / dependence

Pharmacokinetics of Antidepressants

Onset of action: 2-4 weeks Full Effect: ~3 months Initial increase in suicidal thoughts and behaviors

Selective Serotonin Receptor Inhibitor (SSRI) MOA

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

Selective Serotonin Receptor Inhibitor (SSRI) side effects

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

Citalopram (Celexa)

SSRI, Depression, anxiety, cardiac toxicity

Escitalopram (Lexapro)

SSRI, Depression, anxiety

Fluoxetine (Prozac)

SSRI, Depression, anxiety, self tapers

Paroxetine (Paxil)

SSRI, Depression, anxiety, more drowsiness

Sertraline (Zoloft)

SSRI, Depression, anxiety

Vortioxetine (Trinetellix)

SSRI, Depression, anxiety, severe GI side effects

Vilazodone (Viibyrd)

SSRI, Depression, anxiety, severe GI side effects

Serotonin-Norepinephrine Receptor Inhibitor (SNRI) MOA

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

Serotonin-Norepinephrine Receptor Inhibitor (SNRI) side effects

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

Duloxetine (Cymbalta)

SNRI, used for Depression, neuropathic pain, fibromyalgia

Milnacipran (Savella)

SNRI, fibromyalgia

Venlafaxine (Effexor XR)

SNRI, used for depression, anxiety, PTSD

Desvenlafaxine (Pristiq)

SNRI, used for Depression, vasomotor symptoms

Tricyclic Antidepressants (TCA) MOA

Inhibit the reuptake of serotonin, norepinephrine, and dopamine into the presynaptic nerve Effect many other receptors resulting in more side effects and toxicity

Tricyclic Antidepressants (TCA) side effects

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

Amitriptyline (Elavil)

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

Desipramine (Norpramin)

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

Nortriptyline (Pamelor)

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

Imipramine (Tofranil)

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

Clomipramine (Anafranil)

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

Doxepin (Silenor)

TCA, used for antihistamine

Monoamine Oxidase Inhibitor (MAOI) MOA

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

Monoamine Oxidase Inhibitor (MAOI) side effects

Orthostatic hypotension Confusion, delirium Hypertensive crisis (food interaction)

Phenelzine (Nardil)

MAOIs, used for depression, not commonly used

Tranylcypromine (Parnate)

MAOI, used for depression, not commonly used

Selegiline (Zelapar, Emsam)

MAOI, used for parkinsons, Selective for MAOb

Bupropion (Wellbutrin) and side effects

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

Trazadone (Desyrel) and side effects

Other antidepressant used for Insomnia, depression Mixed serotonin receptor activity side effects: Sedation, dizziness, OH*

Mirtazapine (Remeron) and side effects

Other antidepressant used for Appetite stimulation, insomnia, depression Serotonin and alpha2 antagonist side effects: Sedation, weight gain, OH*

Lithium

for bipolar disorder, Well distributed to all tissues in the body - Not metabolized - Excreted in urine concerns: Lithium toxicity

Symptoms of Lithium Toxicity

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

Mechanism of Antipsychotics

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

Extrapyramidal Effects of antipsychotics

Akathisia Dystonia Pseudoparkinsonism Tardive dyskinesia

First Generation Antipsychotics

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

Chlorpromazine (Thorazine)

first generation antipsychotics, used for Antipsychotic

Fluphenazine (Prolixin)

first generation antipsychotics used for Antipsychotic, Tourette's

Haloperidol (Haldol)

first generation antipsychotics used for Antipsychotic, aggressive behavior, nausea

Thiothixene (Navane)

first generation antipsychotics used for antipsycotic

Second Generation Antipsychotics

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

Clozapine (Clozaril)

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

Risperidone (Risperdal)

Second Generation Antipsychotics used for Antipsychotic

Quetiapine (Seroquel)

Second Generation Antipsychotics used for Sleep, delirium, antipsychotic

Olanzapine (Zyprexa)

Second Generation Antipsychotics used for Antipsychotic (increased metabolic AE)

Ziprasidone (Geodon)

Second Generation Antipsychotics used for Antipsychotic

Aripiprazole (Abilify)

Second Generation Antipsychotics used for Antipsychotic, depression

Short-acting Intramuscular Antipsychotics

Acute psychosis Onset is minutes and last a few hours

Long-acting Intramuscular Antipsychotics

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

Serotonin syndrome symptoms

Hyperreflexia Clonus Mydriasis Diaphoresis Shivering Diarrhea

Neuroleptic Malignant Syndrome symptoms

Rigidity Catatonia Stupor