Psychiatry pharmacology

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jknell
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226219
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Psychiatry pharmacology
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2013-07-31 19:42:43
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Psych drugs
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  1. Conventional (typical, first gen) antipsychotics
    Agents:
    Mechanism:
    Side effects:
    • Agents:
    • - Chlorpromazine (Thorazine) *low potency
    • - Thioridazine (Mellaril) *low potency
    • - Haloperidol (Haldol)
    • - Fluphenazine (Prolixin)
    • - Trifluoperazine (Stelazine)
    • - Perphenazine (Trilafon)
    • - Pimozide (Orap)

    Mechanism: bind strongly to post-synaptic D2 receptors in the mesolimbic pathway

    • Side effects:
    • 1. Extrapyramidal symptoms (Acute dystonia, Akathisia, Parkinsonian effects, Tardive dyskinesia); hyperprolactinemia (decreased libido...)
    • 2. Anti-HAM effects (histaminic, adrenergic, and muscarinic receptors): sedation, orthostatic hypotension, anticholinergic effects
    • 3. Weight gain
    • 4. Elevated liver enzymes
    • 5. Dermatologic
    • 6. Seizures: lower seizure thresholds (low potency > high potency)
    • 7. Tardive dyskinesia: choreoathetoid movements of mouth and tongue (50% of cases spontaneously remit)
    • 8. Neuroleptic malignant syndrome
  2. Neuroleptic malignant syndrome
    FALTER
    • rare, occurs most often in males in early treatment with neuroleptics
    • Medical emergency: 20% mortality rate if untreated
    • Often preceded by a catatonic state
    • Fever (most common presenting symptom)
    • Autonomic instability (tachycardia, labile hypertension, diaphoresis)
    • Leukocytosis
    • Tremor
    • Elevated creatine phosphokinase (CPK)
    • Rigidity (lead pipe rigidity is considered almost universal)
    • Treatment: d/c meds, supportive care
  3. Haldol
    Haloperidol
  4. Trilafon
    Perphenazine
  5. Prolixin
    Fluphenazine
  6. Stelazine
    Trifluoperazine
  7. Thorazine
    • Chlorpromazine: low potency (higher dose required for effecacy)
    • deposits in lens and cornea may occur
  8. Mellaril
    • Thioridazine: low potency
    • may cause irreversible retinal pigmentation at high doses
  9. Atypical Antipsychotics
    Agents
    Mechanism:
    Side effects:
    • Agents:
    • - Aripiprazole (Abilify)
    • - Asenapine (Saphris)
    • - Clozapine (Clozaril)
    • - Iloperidone (Fanapt)
    • - Lurasidone (Latuda)
    • - Olanzapine (Zyprexa)
    • - Paliperidone (Invega)
    • - Quetiapine (Seroquel)
    • - Risperidone (Risperdal)
    • - Ziprasidone (Geodon)

    • Mechanism: Vary in binding to D2/D4, 5-HT2, α1-adrenergic, and muscarinic receptors
    • - More effective at treating the negative symtpoms of schizophrenia

    • Side effects:  fewer side effects
    • - some anti-HAM (antihistaminic, antiadrenergic, antimuscarinic)
    • - 1% incidence of agranulocytosis
    • - Seizures (2 to 5% incidence with clozapine)
  10. Abilify:
    Indications
    Weight gain/metabolic effects
    EPS/Akathisia
    QT prolongation
    Notes
    • Aripiprazole: Atypical antipsychotic
    • Mood stabilizer: ++ Mania; + Depression
    • Indications: Schizophrenia; Bipolar mania, monotherapy and adjunctive; bipolar maintenance; Depression adjunct; Agitation in bipolar or schizophrenia (IM only)
    • Weight gain/metabolic effects: Low
    • EPS/Akathisia: High, mainly akathisia (restless legs)
    • QT prolongation: low
    • Notes: probably most "activating"; low rates of side effects; can cause switching into mania
  11. Saphris
    Indications
    Weight gain/metabolic effects
    EPS/Akathisia
    QT prolongation
    Notes
    • Asenapine: Atypical antipsychotic
    • Indications: schizophrenia; Bipolar mania, monotherapy and adjunctive
    • Weight gain/metabolic effects: Moderate
    • EPS/Akathisia: Moderate
    • QT prolongation: Low
    • Notes: Avoid food or drinks for 10 minutes after taking; sedating
  12. Clozaril
    Indications
    Weight gain/metabolic effects
    EPS/Akathisia
    QT prolongation
    Notes
    • Clozapine: atypical antipsychotic, benzodiazepine
    • Mood stabilizer: ++ Mania, + Depression
    • Indications: Treatment-resistant schizophrenia; possibly useful for refractory bipolar disorder
    • Weight gain/metabolic effects: High
    • EPS/Akathisia: low
    • QT prolongation: low
    • Notes: Probably most effective AP; sedation; 1% risk of agranulocytosis (requires weekly blood test)
  13. Fanapt
    Indications
    Weight gain/metabolic effects
    EPS/Akathisia
    QT prolongation
    Notes
    • Iloperidone: Atypical antipsychotic
    • Indications: Schizophrenia
    • Weight gain/metabolic effects: Moderate
    • EPS/Akathisia: Low
    • QT prolongation: Moderate/High
    • Notes: Orthostatic dizziness
  14. Latuda
    Indications
    Weight gain/metabolic effects
    EPS/Akathisia
    QT prolongation
    Notes
    • Lurasidone: Atypical antipsychotic
    • Indications: Schizophrenia
    • Weight gain/metabolic effects: Low/moderate
    • EPS/Akathisia: Moderate
    • QT prolongation: Low
    • Notes: Sedating, take with food
  15. Zyprexa
    Indications
    Weight gain/metabolic effects
    EPS/Akathisia
    QT prolongation
    Notes
    • Olanzapine: Atypical antipsychotic
    • Mood stabilizer: ++ Mania, + Depression
    • Indications: Schizophrenia; Bipolar mania, monotherapy and adjunctive; Bipolar maintenance, monotherapy; Agitation in schizophrenia or bipolar (IM only)
    • Weight gain/metabolic effects: High severe in 15%; elevated lipids, new onset diabetes;  liver toxicity
    • EPS/Akathisia: Low/moderate
    • QT prolongation: Low
    • Notes: robust antimanic agent; comparable to VPA; monitor liver function tests
  16. Invega
    Indications
    Weight gain/metabolic effects
    EPS/Akathisia
    QT prolongation
    Notes
    • Paliperidone: Atypical antipsychotic
    • Indications: Schizophrenia; Schizoaffective disorder
    • Weight gain/metabolic effects: Moderate
    • EPS/Akathisia: High
    • QT prolongation: Moderate
    • Notes: Good for hepatically impaired; increases prolactin
  17. Seroquel
    Indications
    Weight gain/metabolic effects
    EPS/Akathisia
    QT prolongation
    Notes
    • Quetiapine: Atypical antipsychotic
    • Mood stabilizer: ++ Mania, ++ Depression
    • Indications: Schizophrenia; Bipolar mania, monotherapy and adjunctive; Bipolar depression
    • Weight gain/metabolic effects: Moderate
    • EPS/Akathisia: Low
    • QT prolongation: Low
    • Notes: Sedation (transient); low side effect burden; tardive dyskinesia
    • Cataracts in dogs, so monitor with slit lamp exam
  18. Risperdal
    Indications
    Weight gain/metabolic effects
    EPS/Akathisia
    QT prolongation
    Notes
    • Risperidone: Atypical antipsychotic
    • Mood stabilizer: ++ Mania; + Depression
    • Indications: Schizophrenia; Bipolar mania, monotherapy and adjunctive; Irritability in autism
    • Weight gain/metabolic effects: Moderate; less than most atypical anti-psychotics
    • EPS/Akathisia: High (tremor, muscle stiffness,  restless legs)
    • QT prolongation: Low
    • Notes: increases prolactin; menstrual irregularity; tardive dyskinesia
  19. Geodon
    Indications
    Weight gain/metabolic effects
    EPS/Akathisia
    QT prolongation
    Notes
    • Ziprasidone: Atypical antipsychotic
    • Mood stabilizer: ++ Mania, + Depression
    • Indications: Schizophrenia; Bipolar mania, monotherapy; Bipolar maintenance adjunctive; Agitation in schizophrenia (IM injection)
    • Weight gain/metabolic effects: Low
    • EPS/Akathisia: Low
    • QT prolongation: High
    • Notes: Take with food; sedation (transient); antidepressant-liked chemistry
  20. Mood Stabilizing Medications
    • Anti-epileptic Drugs:
    • - Lithium (Eskalith; Lithobid)
    • - Valproate (Depakote)
    • - Carbamazepine (Tegretol)
    • - Lamotrigine (Lamictal)
    • - Oxcarbazepine (Trileptal)

    • Anti-psychotics:
    • - Olanzapine (Zyprexa)
    • - Risperidone (Risperdal)
    • - Quetiapine (Seroquel)
    • - Ziprasidone (Geodon)
    • - Aripiprazole (Abilify)
    • - Clozapine (Clozaril)
  21. Eskalith; Lithobid
    Positives/negatives:
    Side effects: 
    Medical risks:
    • Lithium: mood stabilizer, anti-epileptic drug
    • Mood stabilizing effectiveness: ++ Mania; + Depression
    • Positives/negatives: long history of use' works best early in course of illness; best for "classic" pattern
    • Side effects: Tremor; weight gain; sedation; acne, hair loss
    • Medical risks: kidney damage (uncommon/only after prolonged use); reduced thyroid function
    • Onset: 5 to 7 days
    • Therapeutic range: 0.7 to 1.2
    • Toxic: >1.5
    • Lethal: >2.0
  22. Lithium side effects
    • hypothyroidism
    • nephrogenic diabetes insipidus
    • weight gain
    • tremor
    • GI disturbances
    • fatigue
    • arrhythmias
    • seizures
    • goiter/hypothyroidism
    • leukocytosis (benign)
    • Coma
    • Polyuria
    • Polydypsia
    • Alopecia
    • Metallic taste
  23. Depakote/Depakene
    Positives/negatives:
    Side effects: 
    Medical risks:
    • Valproate: mood stabilizer; anti-epileptic
    • Mood stabilizing effectiveness: ++ Mania; + Depression
    • Mechanism: increases levels of GABA
    • Positives/negatives: long history of use; broad spectrum (wide range of presentations)
    • Side effects: weight gain; tremor; sedation; nausea, diarrhea; hair loss
    • Medical risks: liver inflammation; low platelets
    • Notes: dose by weight, BID dosing is 20mg/kg, QD dosing is 30mg/kg
    • Pregnancy risk: neural tube defects
  24. Depakene
    side effects
    • sedation
    • weight gain
    • alopecia
    • hemorrhagic pancreatitis
    • hepatotoxicity
    • thrombocytopenia
    • Teratogenic: NT defects
  25. Tegretol
    Positives/negatives:
    Side effects: 
    Medical risks:
    • Carbamazepine: mood stabilizer; AED
    • Mood stabilizing effectiveness: ++ Mania; + Depression
    • Positives/negatives: long history of use; broad spectrum (wide range of presentations); good for rapid-cycling bipolar
    • Side effects: neurological (double vision, unsteady gait, vertigo)
    • Medical risks: rare bone marrow suppression; liver inflammation
    • Onset: 5 to 7 days
  26. Tegretol
    side effects
    • Skin rash
    • drowsiness
    • ataxia
    • slurred speech
    • leukopenia
    • hyponatremia
    • aplastic anemia
    • agranulocytosis
    • elevates liver enzymes
    • NT defects during pregnancy
    • monitor: CBC and LFT
  27. Lamictal
    Positives/negatives:
    Side effects:
    Medical risks:
    • Lamotrigine: mood stabilizer, AED
    • Mood stabilizing effectiveness: + Mania, ++ Depression
    • Positives/negatives: first line tx for bipolar depression; fewer side effects; less effective for mania
    • Side effects: headache; rash (10%); cognitive (memory, concentration, word finding)
    • Medical risks: 1/5000 to 1/10,000 chance of Stevens-Johnson Syndrome
  28. Trileptal
    Positives/negatives:
    Side effects:
    Medical risks:
    • Oxcarbazepine: mood stabilizer; AED
    • Mood stabilizing effectiveness: ++ Mania; + Depression
    • Positives/negatives: related to carbamazepine; fewer side effects; no bone marrow suppression
    • Side effects: GI; neurological
    • Medical risks: low sodium
  29. Antidepressant medications
    Medication classes, members
    • SSRI: serotonin reuptake inhibitors
    • - Fluoxetine (Prozac), Sertraline (Zoloft), Paroxetine (Paxil), Fluvoxamine (Luvox), Citalopram (Celexa), Escitalopram (Lexapro)

    • SNRI: serotonin and norepinephrine reuptake inhibitors
    • - Venlafaxine (Effexor), Cymbalta

    • TCA: Trycyclic antidepressants; Norepinephrine Reuptake inhibitors
    • - Nortriptyline (Pamelor), Desipramine (Norpramin), Imipramine (Tofranil), Amitriptyline (Elavil), Trimipramine (Surmontil), Clomipramine (Anafranil), Doxepin (Sinequan)

    • MAOI: Monoamine oxidase inhibitors
    • -Tranylcypromine (Parnate), Phenelzine (Nardil), Deprenyl, Isocarboxazid (Marplan)

    • Miscellaneous agents:
    • - Remeron, Wellbutrin
  30. SSRI
    Positives
    Negatives
    • SSRIs: Fluoxetine (Prozac), Sertraline (Zoloft), Paroxetine (Paxil), Fluvoxamine (Luvox), Citalopram (Celexa), Escitalopram (Lexapro)
    • Positives: Relatively low side effects; good for atypical depression; good for anxiety, safe in overdose
    • Side effects: sexual dysfunction (25 to 30%); headache, GI disturbance, insomnia, anorexia, weight loss, Serotonin syndrome
  31. Prozac
    • Fluoxetine: SSRI
    • Longest half-life with active metabolites
    • Do not need to taper
  32. Zoloft
    • Sertraline: SSRI
    • Highest risk for gastrointestinal (GI) disturbances
  33. Paxil
    • Paroxetine: SSRI
    • Most serotonin specific, most activating (stimulant)
  34. Luvox
    • Fluvoxamine: SSRI
    • Currently approved only for use in OCD
  35. Celexa
    • Citalopram: SSRI
    • Used in Europe for 12 years prior to FDA approval in the US
  36. Lexapro
    • Escitalopram: SSRI
    • Levo enantiomer of citalopram
    • similar side efficacy, fewer side effects, much more expensive
  37. SNRI
    Positives
    Negatives
    • SNRI: Venlafaxine (Effexor), Cymbalta
    • Positives: Broader activity; may be better than SSRIs for melancholic depression
    • Negatives: Side effects similar to both SSRIs and TCAs
  38. Effexor
    • Venlafaxine: SNRI
    • Low drug interaction potential
    • Potential withdrawal symptoms can be seen with 1-3 missed doses; not life threatening
  39. Cymbalta
    Duloxetine: SNRI
  40. TCA
    Positives
    Side effects
    • TCA: Nortriptyline (Pamelor), Desipramine (Norpramin), Imipramine (Tofranil), Amitriptyline (Elavil), Trimipramine (Surmontil), Clomipramine (Anafranil), Doxepin (Sinequan)
    • Positives: Best for melancholic depression
    • Side effects: lethal in overdose (1 week supply can be lethal)
    • 1. Antihistaminic properties - Sedation
    • 2. Antiadrenergic properites - orthostatic hypotension, tachycardia, arrhythmias
    • 3. Antimuscarinic effects - dry mouth, constipation, urinary retention, blurred vision, tachycardia
    • 4. Weight gain
    • 5. Major complications: 3 C's Convulsions, coma, cardiotoxicity
  41. Pamelor
    • Nortriptyline: TCA
    • Least likely to cause orthostatic hypotension
  42. Norpramin
    • Desipramine: TCA
    • Least sedating, least anticholinergic side effects
  43. Tofranil
    Imipramine: TCA
  44. Elavil
    Amytriptyline: TCA
  45. Anafranil
    • Clomipramine: TCA
    • most serotonin specific, useful in treatment of OCD
  46. Sinequan
    Doxepin: TCA
  47. MAOI
    Mechanism
    Positives
    Negatives
    • MAOI: Tranylcypromine (Parnate), Phenelzine (Nardil), Deprenyl, Isocarboxazid (Marplan)
    • Mechanism: irreversibly inhibit the enzymes MAO-A and -B increase amount of norepinephrine, serotonin, dopamine, and tyramine
    • Positives: Frequently works with tx refractory depression; best for atypical depression
    • Side effects: Orthostatic hypotension, drowsiness, weight gain, sexual dysfunction, dry mouth, sleep dysfunction
    • Hypertensive crisis: Risk with tyramine-rich foods or sympathomimetics (red Chianti wine, cheese, chicken liver, fava beans, cured meats)
    • Serotonin syndrome: when use SSRIs and MAOIs together - lethargy, restlessness, confusion, flushing, diaphoresis, tremor, myoclonic jerk
    • Wait at least 2 weeks before switching from SSRI to MAOI
  48. Parnate
    Tranylcypromine: MAOI
  49. Nardil
    Phenelzine: MAOI
  50. Deprenyl
    Selegiline: MAOI
  51. Remeron
    Positives
    Negatives
    • Mirtazapine: Antidepressant; antiemetic; Norepinephrine and serotonin antagonist (NASA)
    • Positives: used in tx refractory depression
    • Negatives: May cause sedation, weight gain, dizziness, somnolence, tremor, agranulocytosis
  52. Wellbutrin
    Positives
    Negatives
    • Bupropion: Norepinephrine/dopamine reuptake inhibitor
    • Positives: relatively low side effect burden; smoking cessation, seasonal affective disorder, adult ADHD; no sexual side effects
    • Negatives: May cause anxiety, low appetite, seizures, can exacerbate psychosis; not optimal for patients with anxiety
  53. Anxiolytics
    indications
    • Anxiolytics: benzodiazepines, barbiturates, buspirone
    • Mechanism: depreesing the CNS, sedation
    • Indications: Anxiety disorders, Muscle spasm, seizures, sleep disorders, alcohol withdrawal, anesthesia induction
  54. Benzodiazepines (BDZs)
    • first-line anxiolytic
    • safe at high doses
    • limitations: abuse potential, tolerance and dependence after prolonged use
    • Mechanism: potentiating the effects of GABA
  55. Benzodiazepines
    long acting (1 to 3 days)
    • Chlordiazepoxide (Librium): used in alcohol detoxification, presurgery anxiety
    • Diazepam (Valium): rapid onset, used in tx of anxiety and seizure control
    • Flurazepam (Dalmane): rapid onset, treatment of insomnia
  56. Benzodiazepines
    Intermediate acting (10 to 20 hours)
    • Alprazolam (Xanax): treatment of panic attacks
    • Clonazepam (Klonopin): treatment of panic attacks, anxiety
    • Lorazepam (Ativan): treatment of panic attacks, alcohol withdrawal
    • Temazepam (Restoril): treatment of insomnia
  57. Benzodiazepines
    Short acting (3 to 8 hours)
    • Oxazepam (Serax)
    • Triazolam (Halcion): rapid onset, treatment of insomnia
  58. Benzodiazepams
    which are cleared by the kidneys?
    • LOT
    • Lorazepam: Ativan
    • Oxazepam: Serax
    • T
    • ***
  59. Benzodiazepines
    side effects
    toxicities
    • side effects: cognitive impairment, reduced motor coordination
    • toxicity: respiratory depression, especially when combined with alcohol
  60. Zolpidem (Ambien)
    Zaleplon (Sonata)
    • NOT benzodiazepines, but functionally similar
    • Use: short-term treatment of insomnia
    • Minimal rebound insomnia
    • Sonata: shorter half-life than Ambien
  61. Buspirone (BuSpar)
    • Alternative to BDZ or venlafaxine for tx of generalized anxiety disorder
    • Slower onset of action: 1 to 2 weeks
    • Anxiolytic action is at 5HT-1A receptor (partial agonist)
    • Does not potentiate the CNS depression of alcohol!
    • Low potential for abuse/addiction
  62. Propranolol
    • Beta blocker
    • treats the autonomic effects of panic attacks
    • Performance anxiety

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