Psychiatry Pharmacology

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jknell
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270294
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Psychiatry Pharmacology
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2014-05-05 01:29:40
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Psychiatry Pharamacology
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Psychiatry Pharmacology
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  1. First Generation ("typical") Antipsychotics
      -Mechanism
      -Indications
      -Adverse Effects
      -Drugs
    • MECHANISM:
    • - block dopamine receptors (potency correlates to D2R affinity)
    • *typical antipsychotics block D2R more strongly than atypical (except risperdone)
    • - side effects due to blockage of 5HT2R
    • * takes several days to weeks to have effect

    • INDICATIONS:
    • - schizophrenia
    • - tourette's
    • - bipolar
    • - Huntington's
    • - acute mania
    • - psychotic depression
    • - acute delerium
    • - drug induced psychosis

    • ADVERSE EFFECTS:
    • - EPS (dose-dependent)
    • - Hyperprolactinemia
    • - QTc prolongation
    • - NMS
    • - akathisia
    • - lower seizure threshold
    • - sedation
    • - anticholinergic side effects
    • - orthostatic hypotension

    • DRUGS:
    • - Thioridazine (Mellaril)
    • - Chlorpromazine (Thorazine)
    • - Perphenazine (Trilafon)
    • - Thiothixene (Navane)
    • - Haloperidol (Haldol)
    • - Fluphenazine (Prolixin)
  2. Mellaril
    Thioridazine

    • - EPS: low
    • - Sedation: high
    • - Hypotension: high
    • - Anticholinergic: high

    - higher incidence of cardiotoxicity
  3. Thorazine
    Chlorpromazine

    • - low potency
    • - t1/2 = 10-40hrs

    • - EPS: low
    • - Sedation: high
    • - Hypotension: high
    • - Anticholinergic: med

    • - high incidence of metabolic effects (wt gain, lipids, gluc)
    • - agranulocytosis
    • - skin discoloration/photosensitivity
    • * also indicated for n/v
  4. Trilafon
    Perphenazine

    • - Mid potency
    • - t1/2 10-20hrs

    • - EPS: medium
    • - Sedative: low
    • - Hypotensive: low
    • - Anticholinergic: low
  5. Navane
    Thiothixene

    • - high potency
    • - t1/2 10-20hrs

    • - EPS: high
    • - Sedative: low
    • - Hypotensive: low
    • - Anticholinergic: low

    • - akithisia is common
    • - ocular pigment changes
  6. Haldol
    Haloperidol

    • - high potency
    • - t1/2 12-36hrs

    • - EPS: high
    • - Sedative: low
    • - Hypotensive: low
    • - Anticholinergic: low

    • - "gold standard" of D2 blockade
    • - decanoate: depot shot (qmonth)
    • - available in all routes
  7. Prolixin
    Fluphenazine

    • - potency high
    • - t1/2 10-20hrs

    • - EPS: high
    • - Sedative: med
    • - Hypotensive: low
    • - Anticholinergic: low

    - decanoate available
  8. Second Generation ("atypical") Antipsychotics
      -Mechanism
      -Indications
      -Adverse Effects
      -Drugs
    • MECHANISM:
    • - potent 5HT2 antagonists
    • - weaker D2 affinity that FGAs
    • - serotonin blockade protects against movement side effects

    • INDICATIONS:
    • - same as typical but with different approvals
    • - acute mania (but not yet studied in maintenance)
    • - augmentation of SSRI in MDD
    • - PTSD
    • - bulimia

    • ADVERSE EFFECTS:
    • - weight gain/metabolic syndrome (DM, DKA)

    • DRUGS:
    • - Risperidone (Risperdal)
    • - Quetiapine (Seroquel)
    • - Olanzapine (Zyprexa)
    • - Ziprasidone (Geodon)
    • - Clozapine (Clozaril)
    • - Aripiprazole (Abilify)
    • - Iloperidone (Fanapt)
    • - Paliperidone (invega)
  9. Risperdol
    Risperidone

    - strong D2 and 5HT2 antagonist

    • Side Effects:
    • - low EPS if < 6mg
    • - orthostatic hypoTN, c reflex tachycardia
    • - insomnia
    • - hyperprolactinemia
    • - weight gain

    • Misc:
    • - decanoate form available
  10. Seroquel
    Quetiapine

    • - low D2 and 5HT2 affinity
    • - high histamine affinity

    • Side Effects:
    • - orthostatic hypoTN
    • - somnolence
    • - weight gain (fewer metabolic sxs than olanzapine)
    • - dyspesia
  11. Zyprexa
    Olanzapine

    - high D2, 5HT2, muscarinic and histaminergic affinity

    • Side Effects:
    • - drowsiness
    • - dry mouth
    • - akithisia
    • - insomnia
    • - +++ wt gain (avg > 20lbs/yr)
    • - HLD
    • - DM, DKA

    • Misc:
    • - twice as costly as other atypicals
  12. Geodon
    Ziprasidone

    • Side Effects:
    • - dizziness, postural hypoTN
    • - prolactin elevation
    • - nausea
    • - QTc prolongation

    • Misc:
    • - must give with food, 300 cal (slow down gastric emptying to allow for absorption)
    • - mandatory pre-tx EKG
  13. Clozaril
    Clozapine

    - strong histamine affinity, low D2

    • * ONLY AGENT EFFECTIVE IN REFRACTORY SCHIZOPHRENIA
    • * some evidence for reversing TD

    • Side Effects:
    • - orthostatic hypoTN
    • - sedation
    • - tachycardia
    • - constipation
    • - hypersalivation
    • - +++ wt gain
    • - +++ HLD, hyperglycemia (w DKA)
    • * Agranulocytosis

    • Misc:
    • - mandatory EKG prior to use
    • - weekly CBC x6months, then biweekly after
    • - register in national database
  14. Abilify
    Aripiprazole

    - strong dopaminergic antagonist, also partial agonist (may get stimulation at high doses)

    * no QTc prolongation or increased prolactin

    • Side Effects:
    • - headache
    • - n/v
    • - sedation with high doses
    • - anxiety
  15. Fanapt
    Iloperidone

    - dopaminergic, strong serotonergic, low histamine

    • Side Effects:
    • - orthostasis
    • - weight gain
  16. Invega
    Paliperidone
  17. Medications for EPS or Parkinsonism
    • - Amantadine
    • - Benztropine
    • - Diphenhydramine
  18. Symmetrel
    Amantadine

    MOA: augments dopaminergic transmission

    Indications: EPS

    • Side Effects:
    • - insomnia
    • - dizziness
    • - impaired concentration
  19. Cogentin
    Benztropine

    • MOA:
    • - muscarinic/acetylcholine antagonist
    • - antihistamine

    • Indications:
    • - Parkinsonism
    • - EPS
    • - acute dystonia
    • - akithisia

    • Side Effects:
    • - anticholinergic (dry mouth, constipation, urinary retention)
  20. SSRI Antidepressants
      - mechanism
      - choice of SSRI
      - adverse effects
      - drugs
    • MECHANISM:
    • - inhibit 5HT reuptake (increased 5HT in cleft)
    • - no difference in efficacy but may have difference in tolerability

    • CHOICE OF SSRI:
    • - based on half-life and drug-drug interactions

    • ADVERSE EFFECTS:
    • - withdrawal if d/c'd too quickly
    • - Serotonin Syndrome with MAOIs
    • - Suicidality
    • - GI effects
    • - Insomnia
    • - Sedation
    • - Sexual dysfunction
    • - can cause mania
    • - antiplatelet effects
    • - rare hyponatremia in elderly

    • DRUGS:
    • - Citalopram
    • - Escitalopram
    • - Fluoxetine
    • - Fluvoxamine
    • - Paroxetine
    • - Sertraline
  21. Celexa
    Citalopram

    t1/2: 33hrs

    • Notes:
    • - SSRI of choice to minimize interactions with other meds
  22. Lexapro
    Escitalopram

    t1/2: 30hrs

    • Notes:
    • - enantiomer of citalopram
    • - somewhat fewer side effects that citalopram
  23. Prozac
    Fluoxetine

    t1/2: 15days

    • Notes:
    • - can be activating
    • - metabolites are activating (self tapers) --> OD is relatively safe
    • - best choice for pregnancy
    • - also approved for eating disorders
  24. Paxil
    Paroxetine

    t1/2: 21hrs

    • Notes:
    • - can be sedating
    • - shortest half life
    • - taper off to avoid withdrawal
  25. Zoloft
    Sertraline

    t1/2: 26hrs

    • Notes:
    • - moderately activating and sedating
  26. SNRIs
      - mechanism
      - adverse effects
      - notes
      - drugs
    • MECHANISM:
    • - inhibit reuptake of 5HT and NE

    • ADVERSE EFFECTS:
    • - less sexual side effects than SSRIs (10%)

    • NOTES:
    • - better at treating physical sxs (anergia, focus)
    • - "activating"

    • DRUGS:
    • - venlafaxine
    • - duloxetine
  27. Effexor
    Venlafaxine

    • MOA:
    • - blocks 5HT and NE reuptake (much more 5HT)
    • - very little anticholinergic or H1

    • ADVERSE EFFECTS:
    • - dose dependent HTN
    • - insomnia
    • - n/v
    • - anxiety
    • - dizziness

    • NOTES:
    • - avoid with MAOIs
  28. Cymbalta
    Duloxetine

    • MOA:
    • - blocks serotonin and NE reuptake

    • ADVERSE EFFECTS:
    • - n/v
    • - anorexia
    • - dry mouth, dizziness, constipation
    • - fatigue/insomnia
    • - sexual SEs
  29. MAOIs
      - mechanism
      - adverse effects
      - indications
      - drugs
    • MECHANISM:
    • - irreversibly inhibits MAO (tyramine accumulates when MAO-A is inhibited)

    • ADVERSE EFFECTS:
    • - 2 wks after d/c to replenish
    • - food interactions: aged cheese, wine, chinese food, tofu, aspartame)

    • INDICATIONS:
    • - MDD (esp with atypical features)
    • - anxiety
    • - panic disorder
    • - social phobia
    • - OCD

    • DRUGS:
    • - Phenelzine
    • - Tranylcypromine
    • - Iscocarboxazid
    • - Selegiline
  30. ATYPICAL ANTIDEPRESSANTS
      - drugs
    • - Bupropion
    • - Mirtazapine
    • - Trazodone
  31. Wellbutrin
    Bupropion

    • MOA:
    • - inhibit NE reuptake and dopaminergic neurotransmission

    • INDICATIONS:
    • - MDD
    • - ADHD
    • - bipolar depression (with SSRI)
    • - smoking cessation

    • ADVERSE EFFECTS:
    • - insomnia
    • - HA
    • - constipation, dry mouth
    • - n/v
    • - tremor
    • - lowers seizure threshold

    • NOTES:
    • - no sexual, weight gain or sedation side effects
    • - do NOT use in pts with eating disorder
    • - do NOT use with MAOIs
  32. Remeron
    Mirtazapine

    • MOA:
    • - agonist at: 5HT2, 5HT3, alpha

    • INDICATIONS:
    • - MDD
    • - dysthymia
    • - anxiety
    • - bulimia
    • - chronic pain

    • ADVERSE EFFECTS:
    • - low sexual side effects
    • - increased appetite, dry mouth
    • - constipation
    • - fatigue
    • - orthostatic hypotension

    • NOTES:
    • - good choice for elderly with depression
    • - some risk for agranulocytosis
  33. Trazodone
    • MOA:
    • - inhibits presynaptic 5HT reuptake
    • - antagonizes at alpha and H

    • ADVERSE EFFECTS:
    • - sedation
    • - orthostatic hypotension
    • - priapism
  34. Mood Stabilizers
      - drugs
    • - Lithium
    • - Valproic Acid
    • - Lamotrigine
    • - Carbamazepine
    • - Oxcarbazepine
  35. Lithium
    • MOA:
    • - unknown

    • INDICATIONS:
    • - bipolar
    • - unipolar mood disorder
    • - impulse control

    • ADVERSE EFFECTS:
    • - GI distress
    • - weight gain
    • - tremor
    • - cognitive impairement
    • - diabetes insipidus
    • - thyroidtoxic
    • - leukocytosis

    • TOXICITY:
    • - n/v/d
    • - tremor
    • - increased DTR
    • - ataxia
    • - confusion
    • - arrhythmia

    • NOTES:
    • - Ebstein's anomaly in first trimester pregnancy
    • - affected by renal clearance
  36. Depakote
    Valproic Acid

    • MOA:
    • - acts on PKC and GABA
    • - blocks Na channel

    • INDICATIONS:
    • - Bipolar disorder (good for acute mania, rapid cycling)
    • - mood lability
    • - impulse behavior

    • ADVERSE EFFECTS:
    • - n/v
    • - sedation
    • - tremor
    • - low platelets
    • - pancreatic and hepatotoxic
    • - hair loss

    • NOTES:
    • - first line for acute mania
    • - follow CBC and LFTs
    • - birth defects!
  37. Lamictal
    Lamotrigine

    • MOA:
    • - effects Na channels that modulate glutamate and aspartate release

    • INDICATIONS:
    • - bipolar depression (not good for acute mania)

    • ADVERSE REACTIONS:
    • - dizziness
    • - sedation
    • - HA
    • - ataxia
    • - rash (SJS)

    • NOTES:
    • - multiple drug interactions
  38. Tegretol
    Carbamazepine

    • MOA:
    • - inactivation of voltage-dependent Na channels

    • INDICATIONS:
    • - Bipolar (good for rapid cycling)
    • - cyclothymia
    • - impulse control disorder

    • ADVERSE EFFECTS:
    • - GI sxs
    • - sedation
    • - dizziness
    • - ataxia
    • - confusion
    • - rash (SJS)
    • - fatal thrombocytopenia
    • - agranulocytosis
    • - aplastic anemia

    • NOTES:
    • - less efficacious for Li or VPA for acute mania or maintenance
    • - CI in BBB
  39. Vistaril
    Hydroxyzine

    • MOA:
    • - antihistamine

    • INDICATION:
    • - anxiety

    • ADVERSE EFFECTS:
    • - sedation
    • - hypotension
    • - paradoxical excitement and agitation
  40. Buspar
    Buspirone

    • MOA:
    • - partial agonist at 5HT, D2

    • INDICATION:
    • - anxiety

    • ADVERSE EFFECT:
    • - restlessness
    • - nervousness
  41. Zolpidem
    Ambien

    • MOA:
    • - binds GABA R

    • INDICATION:
    • - insomnia

    • ADVERSE EFFECTS:
    • - dizziness
    • - GI upset
    • - anterograde amnesia

    • NOTES:
    • - rapid onset
    • - avoid with benzos/EtOH
    • - can be habit forming
  42. Lunesta
    Eszopiolone

    • MOA:
    • - binds GABA R

    • INDICATIONS:
    • - insomnia

    • ADVERSE EFFECTS:
    • - HA
    • - somnolence
    • - dizziness
    • - n/v

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