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Pharm 585 > MCP CNS Meds: Part 1 > Flashcards

MCP CNS Meds: Part 1 Flashcards

1
Q

How do CNS drugs work?

A

They alter or modulate the CNS via binding to receptors and/or affecting neurotransmitter levels

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2
Q

Symptoms of Depression

A
  • S: sleep
    • Insomnia or hypersomnia
  • I: Interest
    • Depressed mood, loss of interest of pleasure
  • G: Guilt
    • Feelings of worthlessness
  • E: Energy
    • Fatigue
  • ​​C: Concentration
    • Diminished ability to think or make decisions
  • A: Appetite
    • Weight change
  • P: Psychomotor
    • Psychomotor retardation or agitation
  • S: Suicidality
    • Precoccupation with death, hoplesness
  • Plus depressed mood
  • To be diagnosed, a person will have 5/9 of these and 1 will be depressed mood
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3
Q

Lifestyle and Non-Pharmacologic Treatment for Depression

A
  • Exercise
  • Avoid Stressors
  • Cognitive Behavioral Therapy (CBT)
  • Light Therapy (SAD)
  • All of these therapies are often used in addition to pharmacologic therapy
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4
Q

General Onset for Anti-Depressants

A
  • Onset: 2-6 weeks
  • Physical Effects (1-2 wks): increases energy and regulation of appetite
  • Psychological Effects (2-6 wks): Improved mood
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5
Q

General Administration for Antidepressants

A
  • Should NOT d/c drug abruptly; need to taper down (or up)
  • Therapy generally must continue for at least 6-9 months after sx improvement
  • Best to avoid combining alcohol with anti-depressants
    • Pt may feel more depressed or anxious, can enhance SEs potential for DDIs (MAOIs, other sedatives)
    • May be okay to have occasional drink, depending on individual patient’s situation
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6
Q

General Side Effects for Anti-Depressants

A
  • People have very different rxns
  • Sexual side effects should be condsidered
  • Monitoring Suidical Risk for all antidepressants
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7
Q

General DDI for Anti-Depressants

A
  • Not to be used with MAOI: 14 day without period required
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8
Q

Black Box Warning on all Anti-Depressants

A
  • Increased risk of suicidal thinking in children, adolescants, and young adults (18-24 yo) with MDD and other psychiatric disorders
  • Depression and certain other pschiatric disorders are themselves associated with increases in risk of suicide
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9
Q

Monitoring Parameters for all Anti-Depressants

A
  • Appropriately monitor patients of all ages who are started on antidepressant therapy and closely observe for clinical worsening, suicidality, or unusal changes in behavior
  • Advise families and caregivers of the need for close observation and comunication with prescriber
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10
Q

The risk of suicide is increased when

A
  • Treatment is initiated
  • Dose is increased or decreased
  • Some paitents will take action once their energy level has increased in response to therapy, but before further improvement in mood has occured
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11
Q

MedGuide Take Away Points on Depression

A
  • Depression or other serious mental illnesses are the most important causes of suicide
  • Watch for new or sudden changes in mood, behavior, actions, thoughts, or feelings, especially if severe
    • Keep in contact with HC provider even between appt
    • Rely on close friends and loved ones
    • National Suicide prevention lifeline
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12
Q

SSRIs MOA

A
  • Blocks pre-synaptic reuptake of serotonin
  • Increases concentration of serotonin in the synapse
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13
Q

SSRIs: Primary Indication, Administration, SE, Important Tidbit

A
  • Primary Indications
    • MDD
    • Various Anxiety Disorders
  • Administration
    • Same time each day (AM or PM determined whether makes sleepy/awake)
    • w or w/o food (via pt response)
  • Side Effects
    • Nausea, loss of appetit, weight gain, somnolence or insomnia, sexual dysfunction, slight potential for QT prolongation
  • Important: Can cause serotonin syndrome
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14
Q

Serotonin Syndrome

A
  • Life-Threatening condition associated with increased serotenergic activity in teh CNS
  • Symptoms:
    • high body temp, fast heart beat, agitiation or restlessness, confusion, loss of coordination, D/N/V
  • Occurs most often when more than one medication that affects serotonin are taken togethers
    • increased release of serotonin
    • or the amount of time that serotonin stays in the brain is prolonged
  • MAOIs carry the greatest risk, and symptoms can persist for several days
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15
Q

SSRI drugs

A
  • Citalopram (Celexa)
  • Escitalopram (Lexapro)
  • Fluoxetine (Prozac)
  • Paroxetine (Paxil)
  • Sertraline (Zoloft)
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16
Q

Citalopram

A
  • Celexa
  • Consits of two stereoisomers
  • Dosage limits due to QT prolongation
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17
Q

Escitalopram

A
  • Lexapro
  • S-enantiomer of citalopram
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18
Q

Fluoxetine

A
  • Prozac
  • Most stimulation agent of SSRIs (Take in AM)
  • Appetite suppression common SE
  • Longs 1/2 life (careful in elderly)
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19
Q

Paroxetine

A
  • Paxil
  • Potentially assoc. w/ more sexual SE and weight gain than other SSRIs
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20
Q

Sertraline

A
  • Zoloft
  • Initial doses (25-50mg/day)
  • Usally must be increased for full therapeutic effects (goal: 100-200 mg/day)
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21
Q

Serotonin-Norepinephrine Reuptake Inhibitors (SNRIs): MOA

A
  • MOA: Blocks serotonin and NE reuptake and is a weak inhibitor of dopamine
22
Q

SNRIs Drugs

A
  • Venlafaxine (Effexor)
  • Duloxetine (Cymbalta)
23
Q

SNRI: Primary indication, Administration, Imporatant Tidbit

A
  • Primary Indication
    • MDD
    • Various Anxiety Disorders
    • Duloxetine
      • Nerve Pain
  • ​Administration
    • Same time each day
    • Venalfaxine: XR may be swallowed whole or sprinkled on applesauce
  • Important: Can Cause Serotonin Syndrome
24
Q

SNRI: SE

A
  • GI complaints, insomnia, headache, some sexual dysfunction, increased risk of bleeding (particularly with aspirin or NSAIDs)
  • Venlafaxine:
    • Take with food
    • Hypertension: escpecially with higher doses
  • Duloxetine
    • incerased risk of hepatotoxicity
25
Q

TriCyclic Anti-Depressants: MOA

A
  • MOA: Increases the synaptic concentration of seotonin and/or norepinephrine by inhibitor of their reuptake by the nerve terminal
26
Q

TCA Drugs

A
  • Amitriptyline (Elavil)
  • Nortriptyline (Pamelor)
  • nortriptyline is the active metabolite of amitriptyline
27
Q

TCA: indications, onset, administration, important tidbit

A
  • Indications:
    • Primary: nerve pain, sleep
    • Secondary: depression, anxiety
  • Onset: up to 4 wks
  • Administration
    • Best is taken at night
  • Important: Can Causes Serotonin Syndrome
28
Q

TCA: SE and Monitoring

A
  • SE:
  • Sedation
  • Anti-Cholingergic effects
  • Weight Gain
  • Orthostatic Hypotension
    • ​Less prominent with nortriptyline
  • Severe: AV conduction changes
  • Monitoring:
    • 30 day supply enough to fatally overdose
    • Overdose can lead to the 3 C’s
      • Coma
      • Convulsions
      • Cardiotoxicity
29
Q

MAOI MOA (Monoamine Oxidase Inhibitors)

A
  • Irrevesible blocking monoamine oxidase, the enzyme responsible for the oxidative deamination of neurotramsitters such as serotonin, norepinephrine, and dopamine
30
Q

MAOI Fun Facts: History, Restrictions, Use

A
  • The first class of antidepressants used clincally
  • No longer first line anti-depressants
    • Many SE (hypotensive effects)
    • Dietary Restrictions: cheese or tyramine reaction
      • MAOs is blocked in intestinal tract (where tyramine is normally broken down) allowing tyramine to build up in the systemic circulation and cause HTN crisis
      • ​Ex of food with tyramine: aged meats/cheeses, improperly stored food, beer and wine
    • DDI’s: potential for serotinin syndrome
  • Useful for “Atypical” Dpression as well as treatment-resistant depressed patients
31
Q

MAOI Drugs (FYI)

A
  • Tranylcypromine (Parnate)
  • Phenelzine (Nardil)
  • Selegiline (Eldepryl or Emsam-patch)
32
Q

Bupropion

A
  • Wellbutrin
  • MOA:
    • Dual DA/NE reuptake inhibitor with NO serotonin activity
  • SE
    • Insomina, dry mouth, seizures (with high doses)
    • C/I in paitents with hx of seizures, bulimia and anorexia
  • Admin
    • w or w/o food, Lacks 5HT activity therefore no sex dysf, weight gain, excessive sedation. Avoid EtOH
33
Q

Mirtazipine: MOA, SE, Admin

A
  • Remeron
  • MOA:
    • Antagonizes alpha-2 receptors centrally which increases release of 5HT and NE
  • SE
    • increased appetite leading to weight gain
    • dry mouth
    • constipation
    • drowsiness
  • Admin/Notes
    • At bedtime
    • Potential for less sexual SE than SSRIs
34
Q

Trazodone: MOA, SE, Admin

A
  • ​Desyrel
  • MOA:
    • Probably a serotonin reuptake inhibitor
  • SE
    • Drowsiness
    • Dizziness
    • Headache
    • Anti-cholingeric (high doses)
    • Rare-priapism
  • Admin/notes
    • At bedtime
    • Commonly used as a non-habit forming sleep aid. Take with food
35
Q

Anxiety: What is it, Nonpharmacologic/Pharm Treatments

A
  • Generalized Anxiety Disorder (GAD)
    • Excessive worry and tension
      • hard for patient to control
      • Interferes with day to day activities
      • Symptoms on most days (for at least 6 months)
  • ​Non-Pharmacological Treatments
    • CBT
    • Relaxation Techniques
  • Pharmacological Treatments
    • SSRIs and SNRIs first line
36
Q

Benzodiazepines: MOA

A
  • Binds to a separate site on the GABA receptor
  • Causes increased effectiveness of GABA
  • Less excitable neuronal state (less anxiety, more sedation)
37
Q

Benzodiazepines: Primary Indications, Onset, Admin

A
  • Primary Indications:
    • Anti-anxiety
    • Anti-convulsant
    • Hypnotic
  • Onset: 1 hour
  • Administration:
    • before anxiety promoting activity (flight, dentist, etc)
    • If used long term, do not abruptly D/C, withdrawl effects likely
38
Q

Benzodiazepines: SE, Monitoring

A
  • SE
    • drowsiness, memory impairment, coordination problems, dizziness, CNS depressive effects
  • Monitoring:
    • Alcohol and other CNS depresseants intensifies effects and may lead to respiratory depression
    • Caution with falls in elderly
    • All are schedule (C-IV) drugs-may be habit forming
39
Q

Alprazolam

A
  • Xanax
  • Half-life: Short (~11 hours)
  • Onset: 1 hour
  • Max: 10mg/day
  • Short half-life increase abuse potential and increases likelihood for withdrawl sx
40
Q

Clonazepam

A
  • Klonopin
  • Half Life: Long (~19-50 hours)
  • Onset: 20-60 min
  • Max 20mg/day
  • Once daily dosing at bedtime sometimes used
41
Q

Diazepam

A
  • Valium
  • Half-Life: Long (20-50 hours-active metabolite: 50-100 hours)
  • Used with caution in elderly: long half-life
42
Q

Lorazepam

A
  • Ativan
  • Half-Life: 13 hours
43
Q

Buspirone: MOA

A
  • Not well understood. Though to not interact with the GABA receptor, but instead act as an agonist for a serotonin receptor
44
Q

Buspirone: Pros and Cons

A
  • Buspar
    • Not scheduled
  • Cons:
    • Less clinical utility
    • Not for seizure or sedation…only for anxiety
  • Pros:
    • Less sedating
    • Higher threshold of interaction with other CNS depressants and EtOH
  • Good Option for the following patients:
    • Unable to tolerate BZDs
    • Patients with a history of drug or alcohol abuse
    • elderly
45
Q

Buspirone: Onset, Admin

A
  • Onset: a week or more
  • Admin:
    • Generally dosed twice daily
    • Avoid taking concurrently with grapefruit juice
    • Do not d/c abruptly
46
Q

Busprione: SE, monitoring

A
  • SE:
    • drowsiness, dizziness, lightheadedness, nervousneses, excitement
  • Monitoring:
    • Alcohol and other CNS depressant intensifies effects and may lead to respiratory despression (lesser extent than BZDs)
47
Q

Insomina

A
  • Difficulty falling asleep
  • Difficulty staying asleep
  • Sleep that is not restorative
  • Poor sleep, difficulty function during the daytime
48
Q

Sleep Hygiene

A
  • Avoid naps
  • Avoid stimulants such as caffeine
  • Exercise. But vigourous exercise should be done in the morning
  • Stay away from large meals at bedtime
  • Ensure adequate exposure to natural light
  • Bedtime routine
  • Don’t bring problems to bed
  • Associate bed with sleep
  • Pleasant and relaxing sleep environmen t
49
Q

Temazepam

A
  • Restoril
  • Specifically for sleep
  • Half life: 10-12 hours
  • Take just before going to sleep
  • Only use for very short term duration (7-10d)
  • Additional SE to watch out for with sedative-hypnotic Benzos in complex behavior, such as sleep driving
50
Q

Non-Benzo Sedative Hypnotics: Drugs and MOA

A
  • Zolpidem (Ambien, Ambien CR)
  • Eszopiclone (Lunesta)
  • MOA:
    • may bind to a different site on the GABA receptor, eliciting only sedation effects
51
Q

Non-Benzo Sedative Hypnotics: Onset, Admin, Dosing

A
  • Onset: ~30 min
  • Admin:
    • Take just before going to sleep or once having trouble falling asleep
    • Use only when needed and for short-term duration
    • Don’t take unless you can dedication 8 hours to sleeping
  • Dosing: Watch for differential dosing for males and females
52
Q

Non-Benzo Sedative Hypnotics: SE, Monitoring

A
  • SE:
    • Droswinss
    • CNS dpressive effects
    • Complex behavior (sleep driving)
  • Monitoring:
    • Alcohol and other CNS depressants intensify effects
      • EtOH should be avoided
    • Do no d/c abruptly
    • All are scheduled C-IV drugs and may be habit forming
    • Elderly patients most suseptible to SE

Pharm 585 (13 decks)

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