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Pharm Exam 3 > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

Depression

A
  • > 5 sx present during same 2 week period
  • Represent a change from previous functioning
  • At least one of the sx has to be depressed mood or loss interest/pleasure (Anhedonia)

*Do not include sx that are due to a general medical condition, or mood incongruent delusions or hallucinations

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2
Q

Depression Sx

A
  • Need to cause clinically significant distress or impairment in social, occupational or other important areas of functioning
SIGECAPS
S= sleep
I= intrest
G= guilt
E= energy
C= concentration
A= appetite
P= psychomotor
S= suicidal
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3
Q

Antidepressant Classes

A
  • SSRIs
  • SNRIs
  • Serotonin Modulators
  • Tricyclics
  • MAOIs
  • Atypicals
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4
Q

All Antidepressants

A
  • Blackbox warning for suicidality in pts
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5
Q

Serotonin Syndrome

A
  • Too much serotonin (usually too many serotonin drugs, can happen with monotherapy)
  • RARE
  • Sx: mental status changes (agitation, hallucinations, coma); autonomic instability (tachycardia, HTN, hyperthermia); neuromuscular aberrations (hyperreflexia, incoordination, tremor); GI sx (N/V/D); Ocular clonus, mydriasis
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6
Q

Bleed risk

A
  • Increased bleed associated with SSRIs
  • Blocks 5-HT transport into platelet, interfering with platelet activation, aggregation
  • Intracranial hemorrhage, GI bleed
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7
Q

SSRIs

Fluvoxamine (Luvox)
Fluoxetine (Prozac)
Paroxetine (Paxil)
Citalopram (Celexa)
Escitalopram (Lexapro)
Sertraline (Zoloft)
Vortioxetine (Brintellix)
A
  • Selective serotonin reuptake inhibitors
  • MOA: Block presynaptic serotonin transporter (Leaves more serotonin available for us)
  • ADR: NAUSEA/VOMITING, INSOMNIA, wt gain, HA, bruxism (teeth grinding), erectile dysfunction/decreased libido, diaphoresis, orthostasis, akathisia, osteopenia, GI bleed, some anticholinergic effects
  • DRUG INTERACTIONS: other serotonin drugs, 2D6 inhibitors
  • PREGNANCY: 1st trimester (associated w/ cardiac defects); 3rd trimester (low birth wt, prematurity, neonatal withdrawal, persistent pulmonary HTN of newborn)
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8
Q

Fluoxetine (Prozac)

  • For Major Depressive Disorder, OCD, Panic Disorder, bulimia
  • Lease wt gain
A
  • Long t1/2
  • Can be activating– take in the morning
  • Potential for drug interactions (2D6 inhibitor)
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9
Q

Paroxetine (Paxil, Pexeva)

  • For MDD, OCD, Social Anxiety Disorder, General Anxiety Disorder
  • Most sedating, wt gain, sexual dysfunction, anticholindergic AEs
A
  • Shortest t1/2

- High risk of drug interaction (2D6 inhibition)

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10
Q

Sertraline (Zoloft)

- For MDD, OCD, Panic Disorder, PTSD, PreMenstrual Dysphoric Disorder, SAD

A
  • Few drug interactions (2D6 inhibition at higher doses)
  • Benefit in pts with depression and CVD
  • ADR: dry mouth, sedation, insomnia, tremor, dizziness, sexual dysfunction
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11
Q

Escitalopram (Lexapro)

- For MDD, GAD

A
  • Few drug interactions

- ADR: N, sedation, insomnia, sexual side effects

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12
Q

Citalopram (Celexa)

  • For depression
  • Lowest risk of sexual side effects
A
  • Few drug interactions

- Risk of QTC prolongation

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13
Q

SNRIs

Venlafaxine (Effexor)
Desvenlafaxine (Pristiq)
Trintellix (Vortioxetine)
Duloxetine (Cymbalta)
Milnacipran (Savella)
Levomilnacipran (Fetzima)
A
  • Serotonin-norepinephrine reuptake inhibitors
  • MOA: binds 5HT and NE receptor transporters
  • INDICATIONS: Depression, Anxiety disorder (GAD, PTSD, SAD, PD)
  • Neuropathic pain/chronic pain: Duloxetine, Venlafaxine
  • Fibromyalgia: Milnacipran
  • ADR: HTN, hyperlipidemia, dry mouth, HA, sexual dysfunction, insomnia, N/V, akathisia, diaphoresis, wt changes
  • DRUG INTERACTIONS: other serotonergic drugs, MAOIs, platelet inhibitors, strong 3A4 inhibitors (levomilnacipran), strong 2D6 inhibitors (vortioxetine, duloxetine)
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14
Q

Aytpical antidepressants

A

Mirtazapine (Remeron)

Bupropion (Wellbutrin)

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15
Q

Mirtazapine (Remeron)

- Major depressive disorder

A
  • MOA: increases central NE and 5HT activity; 5HT receptor antagonist/ H1 receptor antagonist/ peripheral alpha 1 antagonist
  • ADR: SEDATION/SOMNOLENCE (caution abt driving, avoid EtOH and other CNS depressants), dizziness, orthostasis, WT GAIN, elevated cholesterol/elevated LFTs, agranulocytosis
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16
Q

Bupropion (Wellbutrin)

  • For MDD, smoking cessation
  • Can make anxiety worse for anxiety disorders
A
  • MOA: weak NE/DA reuptake inhibitor (does not inhibit 5HT reuptake or MAO)
  • ADR: agitation/anxiety/insomnia, wt loss, psychosis/delusions/hallucinations/confusion, HTN, N/V, HA, dry mouth
  • CONTRAINDICATION: seizure disorder (eating disorder, withdrawal of EtOH or sedatives)
17
Q

TCAs
- More likely to cause suicide effects compared with SSRI/SNRI

Amitriptyline (Elavil)
Doxepin (Sinequan)
Clomipramine
Imipramine (Tofranil)
Desipramine (Norpramin)
A
  • MOA: SNRI/anticholinergic action/ direct alpha-adrenergic blockade/ membrane stabilizing effect on the myocardium (block the cardiac myocyte fast Na channels)
  • INDICATIONS: depression, anxiety, bipolar disorder, OCD, neuropathic pain, migraine prophylaxis
  • ADR: anticholinergic effects (dry mouth, urinary retention, sedation), arrhythmia, sexual dysfunction, fall risk, diaphoresis
  • CYP 2D6 substrate: potential for toxicity– 2D6 inhibitors (SSRIs); MAOI; anticholinergics; Sympathomimetics; Cimetidine
18
Q

TCA overdose

- 10 day supply taken all at once can be fatal

A
  • Seizures
  • Decreased contractility, alpha adrenergic effects (Hypotension)
  • CV sx: palpitation, chest pain, hypotension
  • CNS sx: convulsion, decreased mental status, respiratory depression, drowsiness, coma
  • Peripheral sx: dry mouth, dry skin, urinary retention, blurred vision
19
Q

5HT modulators

A

Trazodone (Desyrel, Olepto)

20
Q

Trazodone (Desyrel, Olepto)

  • Indicated for depression
  • OFF LABEL: FOR SLEEP
A
  • MOA: 5HT receptor antagonist and reuptake inhibitor

- ADR: sedation/somnolence, HA/dizziness/dry mouth, Orthostasis/long QT/arrhythmia, priapsism

21
Q

Vilazodone (Viibryd)

- For depression

A
  • MOA: 5HT receptor partial agonist and reuptake
  • ADR: sedation/somnolence, HA/dizziness/dry mouth, Orthostasis/long QT/arrhythmia, priapsism
  • P450 3A4 substrate
22
Q

MAOIs

- Last line for depression (for those who failed or not responded to other antidepressants)

A
  • MOA: nonselective monoamine oxidase inhibitors (increases level of 5HT, NE, DA)
  • ADR: serotonin syndrome, sexual dysfunction, myoclonus, orthostasis, HTN crisis, dizziness/drowsiness, C/dry mouth, wt gain
  • CONTRAINDICATION: HTN, CVD, other MAOIs/sympathomimetics/CNS depressants; antihypertensive, diuretics, antihistamine, sedative or anesthetic drugs; bupropion????
23
Q

Supplements

A

St John’s Wort

24
Q

St John’s Wort

- Likely effective for depression

A
  • Contain hyperforin, hypericin (melatonin, adhyperforin)
  • Modulates 5HT, NE, DA (may inhibit reuptake)
  • ADR: INSOMNIA (Take in morning); vivid dreams; restlessness, anxiety, agitation; D, dry mouth; dizziness; HA; rash; hypoglycemia; paresthesias
  • Potent P450 inducer (3A4, 2C19, 1A2): increases OCP estrogen metabolism; reduces digoxin, imatinib, irinotecan levels
  • Potential for serotonin syndrome
25
Q

Guidelines depression treatment

A
  • First line: SSRI, SNRI, bupropion, mirtazapine
  • Choose based on: pt preference; nature of prior response to medication; safety, tolerability, and anticipate SE; co-occuring psychiatric or general medical conditions; pharmacological properties of the medication; cost
  • At lease 4 weeks for full effects of medication
  • Treatment for adults with major depressive disorder (either Cognitive Behavior Therapy or Second Generation Antidepressants– SSRI/SNRI)

Pharm Exam 3 (5 decks)

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