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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)
-
Mellaril
Thioridazine
- - EPS: low
- - Sedation: high
- - Hypotension: high
- - Anticholinergic: high
- higher incidence of cardiotoxicity
-
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
-
Trilafon
Perphenazine
- - Mid potency
- - t1/2 10-20hrs
- - EPS: medium
- - Sedative: low
- - Hypotensive: low
- - Anticholinergic: low
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Navane
Thiothixene
- - high potency
- - t1/2 10-20hrs
- - EPS: high
- - Sedative: low
- - Hypotensive: low
- - Anticholinergic: low
- - akithisia is common
- - ocular pigment changes
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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
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Prolixin
Fluphenazine
- - potency high
- - t1/2 10-20hrs
- - EPS: high
- - Sedative: med
- - Hypotensive: low
- - Anticholinergic: low
- decanoate available
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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)
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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
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Seroquel
Quetiapine
- - low D2 and 5HT2 affinity
- - high histamine affinity
- Side Effects:
- - orthostatic hypoTN
- - somnolence
- - weight gain (fewer metabolic sxs than olanzapine)
- - dyspesia
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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
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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
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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
-
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
-
Fanapt
Iloperidone
- dopaminergic, strong serotonergic, low histamine
- Side Effects:
- - orthostasis
- - weight gain
-
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Medications for EPS or Parkinsonism
- - Amantadine
- - Benztropine
- - Diphenhydramine
-
Symmetrel
Amantadine
MOA: augments dopaminergic transmission
Indications: EPS
- Side Effects:
- - insomnia
- - dizziness
- - impaired concentration
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Cogentin
Benztropine
- MOA:
- - muscarinic/acetylcholine antagonist
- - antihistamine
- Indications:
- - Parkinsonism
- - EPS
- - acute dystonia
- - akithisia
- Side Effects:
- - anticholinergic (dry mouth, constipation, urinary retention)
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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
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Celexa
Citalopram
t1/2: 33hrs
- Notes:
- - SSRI of choice to minimize interactions with other meds
-
Lexapro
Escitalopram
t1/2: 30hrs
- Notes:
- - enantiomer of citalopram
- - somewhat fewer side effects that citalopram
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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
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Paxil
Paroxetine
t1/2: 21hrs
- Notes:
- - can be sedating
- - shortest half life
- - taper off to avoid withdrawal
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Zoloft
Sertraline
t1/2: 26hrs
- Notes:
- - moderately activating and sedating
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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
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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
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Cymbalta
Duloxetine
- MOA:
- - blocks serotonin and NE reuptake
- ADVERSE EFFECTS:
- - n/v
- - anorexia
- - dry mouth, dizziness, constipation
- - fatigue/insomnia
- - sexual SEs
-
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
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ATYPICAL ANTIDEPRESSANTS
- drugs
- - Bupropion
- - Mirtazapine
- - Trazodone
-
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
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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
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Trazodone
- MOA:
- - inhibits presynaptic 5HT reuptake
- - antagonizes at alpha and H
- ADVERSE EFFECTS:
- - sedation
- - orthostatic hypotension
- - priapism
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Mood Stabilizers
- drugs
- - Lithium
- - Valproic Acid
- - Lamotrigine
- - Carbamazepine
- - Oxcarbazepine
-
Lithium
- 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
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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!
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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
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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
-
Vistaril
Hydroxyzine
- ADVERSE EFFECTS:
- - sedation
- - hypotension
- - paradoxical excitement and agitation
-
Buspar
Buspirone
- MOA:
- - partial agonist at 5HT, D2
- ADVERSE EFFECT:
- - restlessness
- - nervousness
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Zolpidem
Ambien
- ADVERSE EFFECTS:
- - dizziness
- - GI upset
- - anterograde amnesia
- NOTES:
- - rapid onset
- - avoid with benzos/EtOH
- - can be habit forming
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Lunesta
Eszopiolone
- ADVERSE EFFECTS:
- - HA
- - somnolence
- - dizziness
- - n/v
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