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Psychopharm > Antipsychotics > Flashcards

Antipsychotics Flashcards

1
Q

lurasidone (Latuda)

A

Indication: Schizophrenia (+13+); Bipolar Depression (10+)

Dose: 20mg WITH FOOD (>350cal for a 2-3-fold increase); range 20-80mg daily; typical effective dose is 160mg+

Mechanism: 5HT2A; 5HT7; partial 5HT1

Monitoring: typical antipsychotic monitoring

Advantages: low-mod metabolic profile; low QTc

ADEs: sedation, orthostatic hypotension, syncope, EPS

Off-Label: Mixed Depression; TRD; impulse control d/o; mania

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2
Q

Antipsychotics and Weight Gain

A

Best: aripiprazole; lurasidone; ziprasidone

Worst: clozapine; olanzapine

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3
Q

Antipsychotics and Sedation

A

Best: aripiprazole; brexpiprazole

Worst: clozapine; olanzapine; quetiapine

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4
Q

Antipsychotics and Cardiac Issues

A

Best: aripiprazole; asenapine; brexipiprazole; cariprazine; clozapine; loxapine; lurasidone; olanzapine; risperidone

Worst: iloperidone; thioridazine; ziprasidone

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5
Q

Antipsychotics and EPS

A

Best: chlorpromazine; clozapine; iloperidone; olanzapine; quetiapine; ziprasidone

Worst EPS: haloperidol; paliperidone; risperidone

Worst Akathisia: aripiprazole; brexpiprazole

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6
Q

Antipsychotic Monitoring

A

BMI: baseline; monthly x 3 months; quarterly

Waist Circumference: baseline; annually

Blood Pressure/Pulse: baseline; 3rd month; annually

Fasting Glucose/A1C: baseline; 3rd month; annually

Lipids: baseline; 3rd month; annually

AIMS: baseline; quarterly

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7
Q

aripiprazole (Abilify)

A

Indication: Schizophrenia (13+); acute and maintenance treatment of manic and mixed episodes (10+); Bipolar Disorder (maintenance); MDD augmentation; irritability in autism (6+); Tourette’s Disorder (6+)

Dose: Schizophrenia/Bipolar Disorder: Start 10mg/d; MAX=30mg/d (12mg most effective)
Depression Augmentation: Start 2-5mg/d; increase in 5mg weekly increments; MAX=15mg/d
Autism Irritability: Start 2-5mg/d; increase in 5mg/d weekly increments; MAX=15mg/d
Tourette’s: Start 2mg/d, increase my 5mg/d weekly; MAX=10mg (<50kg) and 20mg (>50kg)

Dose Equivalent (10mg olan./5mg halo.): 15mg

Monitoring: typical antipsychotic monitoring

Mechanism: D2 receptor antagonist and 5HT-1A partial agonist; 5HT-2A receptor antagonist

Advantages: low weight gain; has an ODT and a liquid formulation (and LAI); also, an embedded ingestible sensor to track compliance (Abilify MyCite)

ADEs: akathisia; sedation; anxiety; insomnia; tremors; rare reports of pathologic gambling (reversible) and other impulse control disorders

Off-Label: counteracts antipsychotic-induced prolactinemia

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8
Q

asenapine (Saphris)

A

Indication: Schizophrenia; acute and maintenance treatment of manic and mixed episodes (10+)

Dose: Sublingual; Start 5mg BID (2.5mg in children); increase as needed to 10mg – DO NOT SWALLOW PILL; AVOID FOOD/WATER FOR TEN (10) MINUTES (15mg most effective)
Patch: Start 3.8mg/24hr; increase weekly (5.7mg, then 7.6mg as needed)

Dose Equivalent (10mg olan./5mg halo.): 9mg

Monitoring: LFTs (contraindicated in hepatic impairment); typical antipsychotic monitoring

Mechanism: D2 and 5HT-2A receptor antagonist

Advantages: sublingual, for those who cannot swallow pills; little anticholinergic activity

ADEs: tongue numbing (oral hypoesthesia); akathisia; somnolence; dizziness; EPS; weight gain (+); hypersensitivity reaction (including serious anaphylaxis); additive hypotension with antihypertensives

Off-Label: Bipolar maintenance; bipolar depression; behavioral disturbances; impulse control disorders

Fun Facts: black cherry flavor

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9
Q

brexpiprazole (Rexulti)

A

Indication: Schizophrenia; Depression augmentation

Dose: Schizophrenia: 1mg/d for 4d, then 2mg x 3d; increase as needed; MAX=4mg/d
(3mg most effective)
Depression augmentation: 0.5mg daily; increase by 0.5mg weekly;
MAX=3mg/d

Monitoring: standard antipsychotic monitoring

Mechanism: D2 receptor antagonist; 5HT-1A partial agonist; 5HT-2A receptor antagonist

Advantages: once daily option

Disadvantages: lower doses no better than placebo in clinical trials

ADEs: weight gain; akathisia (worst); somnolence; rare reports of pathologic gambling (reversible) and other impulse control disorders

Fun Facts: structurally resembles aripiprazole

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10
Q

cariprazine (Vraylar)

A

Indication: Psychosis

Dose: Start at 1mg BID; adjust by 1mg BID weekly to effective dose; Dose range usually 2.5-20mg; MAX=40mg/d

Monitoring: typical antipsychotic monitoring

Mechanism: D2 receptor antagonist; HIGH POTENCY

Advantages: liquid and injectable forms give flexibility

ADEs: EPS (high); headache, drowsiness; dry mouth, prolactin elevation (with associated amenorrhea; sexual ADEs; galactorrhea); usual serious antipsychotic ADEs

Off-Label: Bipolar Disorder; behavioral disturbances; impulse control disorders

Fun Facts: there was also a branded Permitil (not just Prolixin)

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11
Q

chlorpromazine (Thorazine)

A

Indication: psychosis; mania; nausea/vomiting; intractable hiccups

Dose: Start at 10mg TID; increase by 20-50mg/d every four days; range 200mg-600mg;
MAX=1000mg/d

Dose Equivalent (10mg olan./5mg halo.): 300-389mg

Monitoring: EKG; typical antipsychotic monitoring

Mechanism: D2 receptor antagonist; LOW POTENCY

ADEs: sedation; orthostasis; tachycardia; drowsiness; dry mouth, constipation; blurred vision; prolactin elevation (with associated amenorrhea; sexual ADEs; galactorrhea); usual serious antipsychotic ADEs; injection site infections; skin pigmentation (dose-related); ocular changes (dose-related); jaundice

Off-Label: Bipolar Disorder; behavioral disturbances; impulse control disorders

Fun Facts: initially developed to induce relaxation and indifference in surgical patients

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12
Q

fluphenazine (Prolixin)

A

Indication: Schizophrenia; acute and maintenance treatment of manic and mixed episodes; bipolar depression

Dose: Start 1.5mg daily; increase to 3mg on the 3nd day; adjust by 1.5-3mg/d; usual dose 6mg/d (MAX=3mg in bipolar depression)

Monitoring: usual antipsychotic monitoring

Mechanism: D2 and D3 receptor antagonist; 5HT-1A partial agonist; 5HT-2A receptor antagonist

Advantages: supposed focus on negative symptoms (not really supported in literature)

ADEs: EPS (high); akathisia; weight gain; sedation; usual serious antipsychotic ADEs

Off-Label: negative symptoms of schizophrenia; major depression

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13
Q

haloperidol (Haldol)

A

Indication: psychosis; Tourette’s Disorder

Dose: Start at 1mg BID; adjust q3-4d; range 5-20mg/d; MAX=100mg, but doses >20mg rarely used

Monitoring: EKG; typical antipsychotic monitoring

Mechanism: D2 receptor antagonist; HIGH POTENCY

ADEs: EPS; headache; drowsiness; dry mouth; prolactin elevation (with associated amenorrhea; sexual ADEs; galactorrhea); usual serious antipsychotic ADEs

Off-Label: Bipolar Disorder; behavioral disturbances; impulse control disorders; delirium

Fun Facts: 1958 discovery

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14
Q

iloperidone (Fanapt)

A

Indication: schizophrenia; acute agitation associated with schizophrenia or mania

Dose: Start at 1mg BID; increase to 2mg BID on d2; then by 4mg weekly; range 6-12mg BID; MAX=12mg BID (most effective found to be >20mg)

Monitoring: typical antipsychotic monitoring (esp. fasting glucose and lipds); Mg; K

Mechanism: D2 and 5HT-2A receptor antagonist

Disadvantages: decrease dose by 50% when with 2D6 or 3A4 inhibitors

ADEs: dizziness (dose-related); dry mouth; fatigue; nasal congestion; orthostatic hypotension (reduced with more gradual titration); somnolence; tachycardia (dose-related); weight gain; SERIOUS: QTc prolongation (avoid in patient with bradycardia, hypokalemia, or hypomagnesemia); priapism

Off-Label: Bipolar Disorder; major depression; behavioral disturbances; impulse control disorders

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15
Q

loxapine (Loxitane/Adasuve)

A

Indication: schizophrenia; acute agitation associated with schizophrenia or mania

Dose: Start at 10mg BID; increase by 10mg q3-4d; range 60mg-100mg BID-TID
MAX=250mg/d, but rarely is >100mg used
ACUTE: 10mg oral inhalation (Adasuve): Contraindicated in asthma or COPD

Monitoring: typical antipsychotic monitoring

Mechanism: D2 and 5HT-2A receptor antagonist; INTERMEDIATE POTENCY

ADEs: EPS; headache; drowsiness; dry mouth, prolactin elevation (with associated amenorrhea; sexual ADEs; galactorrhea); usual serious antipsychotic ADEs; throat irritation (Adasuve); bronchospasm (Adasuve)

Off-Label: Bipolar Disorder; behavioral disturbances; impulse control disorders

Fun Facts: metabolized into amoxapine

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16
Q

molindone (Moban)

A

Indication: Schizophrenia

Dose: Start at 75mg daily in divided doses; increase to 100mg/d in 4d; MAX=225mg/d

Monitoring: typical antipsychotic monitoring

Mechanism: D2 receptor antagonist; INTERMEDIATE POTENCY

Advantages: inexpensive (recently re-introduced); shown to reduce weight in patients

ADEs: EPS; sedation; agitation; headache; usual serious antipsychotic ADEs; SERIOUS: leukocytosis and leukopenia

Off-Label: bipolar disorder; behavioral disturbances; impulse control disorders

17
Q

olanzapine (Zyprexa)

A

Indication: schizophrenia (13+); acute treatment of manic episodes; maintenance treatment of bipolar disorder; bipolar depression (as Symbyax (10+)); treatment-resistant depression (with fluoxetine); acute agitation

Dose: Start 5-10mg daily; increase by 5mg weekly; range 10-20mg/d; MAX=20mg/d (but up to 40mg used); typical therapeutic response at 15mg/d
Symbax: Start 6/25; MAX=12/50

Monitoring: BMI; typical antipsychotic monitoring (esp. lipids and fasting glucose)

Mechanism: D2 and 5HT-2A receptor antagonist

ADEs: somnolence (dose-related); dry mouth (dose-related); constipation; weight gain (40%; substantial gains of 10-30#); increased appetite; EPS (at high doses); usual serious antipsychotic ADEs; SERIOUS: fatal DRESS drug reaction

Off-Label: behavioral disturbances; impulse control disorders

18
Q

paliperidone (Invega)

A

Indication: schizophrenia (12+); schizoaffective disorder (first one with this indication)

Dose: (Adults): 6mg in AM (3mg in adolescents) may be effective dose); increase by 3mg weekly; MAX=12mg/d (adults) or 6mg (<51kg); typical therapeutic dose is 13mg+

Dose Equivalent (10mg olan./5mg halo.): 4.5mg

Monitoring: prolactin; typical antipsychotic monitoring (esp. lipids and fasting glucose)

Mechanism: D2 and 5HT-2A receptor antagonist

ADEs: EPS; tremor; tachycardia; insomnia; somnolence (esp. seen in adolescents); weight gain; orthostatic hypotension; headache; prolactin elevation (with associated amenorrhea; sexual ADEs; galactorrhea); usual serious antipsychotic ADEs; SERIOUS: QTc elevations; bowel obstructions in patients with strictures; esophageal dysmotility and aspiration (which may result in pneumonia)

Off-Label: Bipolar Disorder; behavioral disturbances; impulse control disorders; delirium

Fun Facts: controlled release capsule like Concerta (capsules may be in stool)

19
Q

perphenazine (Trilafon)

A

Indication: psychosis; severe nausea and vomiting (similar in efficacy to other antipsychotics in CATIE trials)

Dose: Start at 4-8mg TID; adjust q3-4d; range 8mg-16mg BID-QID; MAX=24mg, but doses >64mg in hospitalized patients common

Monitoring: typical antipsychotic monitoring

Mechanism: D2 receptor antagonist; INTERMEDIATE POTENCY

ADEs: EPS; headache; drowsiness; dry mouth; prolactin elevation (with associated amenorrhea; sexual ADEs; galactorrhea); usual serious antipsychotic ADEs; tachycardia (especially when dose increased rapidly)

Off-Label: bipolar disorder; behavioral disturbances; impulse control disorders; delirium

Fun Facts: combination with amitriptyline is called Triavil (1965)

20
Q

pimavanserin (Nuplazid)

A

Indication: Hallucinations and delusions in Parkinson’s Disease

Dose: 34mg daily (10mg if on 3A4 inhibitors)

Monitoring: typical antipsychotic monitoring (esp. lipids and fasting glucose)

Mechanism: inverse agonist and antagonist activity at 5HT-2A and 5HT-2C receptors (NO dopamine receptor activity)

Disadvantages: no significant evidence of superiority over other agents; major controversy over safety (post-marketing deaths have occurred)

ADEs: nausea; peripheral edema; confusion; SERIOUS: QTc prolongation (5-8msec); increased mortality in elderly

21
Q

quetiapine (Seroquel)

A

Indication: schizophrenia (13+); maintenance treatment of bipolar disorder; manic or mixed episodes (10+); bipolar depression; major depression (as adjunct)

Dose: Start 25mg BID (or 300mg XR at bedtime); increase by 50-100mg/d q4d; range 400-800mg/d; MAX=800mg; XR is taken WITHOUT food (or <300cal)

Dose Equivalent (10mg olan./5mg halo.): 375mg

Monitoring: typical antipsychotic monitoring (esp. lipids and fasting glucose); slit-lamp examination q6mos (cataracts)

Mechanism: D2 and 5HT-2A receptor antagonist

ADEs: somnolence; hypotension (+orthostatic hypotension); dry mouth; dizziness; weight gain; constipation; fatigue; usual serious antipsychotic ADEs; cataracts (in beagles)

Off-Label: insomnia; anxiety disorders (better than most medications); behavioral disturbances; impulse control disorders

22
Q

risperidone (Risperidal)

A

Indication: schizophrenia (13+); manic or mixed episodes (10+); irritability symptoms of autism (5+)

Dose: Start 1mg BID; increase by 1mg/d every 2-3d; weight-based: <15kg, use with caution; 15-20kg, start with 0.25mg daily and increase by 0.5mg weekly; >20kg, start at 0.5mg daily and increase my 1mg/d weekly; MAX=6mg, but >4mg associated with significant EPS; typical therapeutic dose is 6mg/d

Dose Equivalent (10mg olan./5mg halo.): 3mg

Monitoring: typical antipsychotic monitoring (esp. lipids and fasting glucose); prolactin

Mechanism: D2 and 5HT-2A receptor antagonist

Advantages: has an ODT form

ADEs: EPS; somnolence; orthostatic hypotension; anxiety; constipation; nausea; dyspepsia; dizziness; rhinitis; prolactin elevation (with associated amenorrhea; sexual ADEs; galactorrhea); weight gain; usual serious antipsychotic ADEs

Off-Label: insomnia; anxiety disorders (better than most medications); behavioral disturbances; impulse control disorders

23
Q

thioridazine (Mellaril)

A

Indication: Schizophrenia (considered last-line)

Dose: Start at 50-100mg TID; adjust q3-4d; range 200-800mg/d; MAX=800mg/d.

Monitoring: EKG; ophthalmology examinations; typical antipsychotic monitoring

Mechanism: D2 receptor antagonist; LOW POTENCY

ADEs: EPS; headache; sedation; dry mouth; constipation; blurred vision; prolactin elevation (with associated amenorrhea; sexual ADEs; galactorrhea); usual serious antipsychotic ADEs; SERIOUS: QT prolongation (highest of all antipsychotics); ocular pigmentation; degenerative retinopathies; retrograde ejaculation

Off-Label: anxiety; insomnia

Fun Facts: can kill antibiotic-resistant bacteria (like MRSA and drug-resistant Mycobacterium tuberculosis by weakening the bacterial cell walls.

24
Q

thiothixene (Navane)

A

Indication: Schizophrenia

Dose: Start at 2mg TID – 5mg BID; adjust q3-4d; range 20-30mg/d; MAX=60mg/d, but doses >40mg rarely used.

Monitoring: typical antipsychotic monitoring

Mechanism: D2 receptor antagonist; HIGH POTENCY

ADEs: EPS; headache; drowsiness; dry mouth; prolactin elevation (with associated amenorrhea; sexual ADEs; galactorrhea); usual serious antipsychotic ADEs

Off-Label: bipolar disorder; behavioral disturbances; impulse control disorders

Fun Facts: was also found to be effective in depression, but Pfizer chose the psychosis indication.

25
Q

trifluoperazine (Stelazine)

A

Indication: Schizophrenia; non-psychotic anxiety

Dose: Start at 1-2mg BID; adjust q3-4d; range 5-10mg/d; MAX=40mg/d

Monitoring: typical antipsychotic monitoring

Mechanism: D2 receptor antagonist; HIGH POTENCY

ADEs: EPS; headache; drowsiness; dry mouth; prolactin elevation (with associated amenorrhea; sexual ADEs; galactorrhea); usual serious antipsychotic ADEs

Off-Label: bipolar disorder; behavioral disturbances; impulse control disorders

Fun Facts: tagline was “Calm, but still alert”

26
Q

ziprasidone (Geodon)

A

Indication: schizophrenia (13+); maintenance treatment of bipolar disorder; manic or mixed episodes (10+); acute agitation associated with schizophrenia (IM only)

Dose: Start at 20mg BID (or 40mg BID for mania) WITH MEALS (increases absorption two-fold); adjust q3-4d; range 60-80mg/d; MAX=160mg/d; safety data shows safety to 320mg/d; typical therapeutic dose is 200mg+
IM: 10mg q2hrs or 20mg q4hrs; MAX=40mg/d

Dose Equivalent (10mg olan./5mg halo.): 80mg

Monitoring: EKG; typical antipsychotic monitoring

Mechanism: D2 and 5HT-2A receptor antagonist

ADEs: somnolence; dizziness; akathisia; rash; usual serious antipsychotic ADEs; SERIOUS: QTc prolongation; fatal DRESS drug reaction

Off-Label: bipolar disorder; behavioral disturbances; impulse control disorders

Fun Facts: name suggested to bring to mind the phrase “bring down to earth.”

27
Q

clozapine (Clozaril)

A

Indication: Treatment-resistant schizophrenia (use after two failed antipsychotic trials); reduction of suicide risk in schizophrenia and schizoaffective disorder

Dose: Start at 12.5mg daily and increase to BID on d3; Increase by 25-50mg/d to a target of 300-450mg by the end of two weeks; increase by 50mg no more frequently than 50mg/d weekly; may require doses over 600mg/d for effect, but toxic effects may appear at doses >700mg/d; MAX=900mg/d (in divided doses – BID to TID); may take 4-6 weeks to 6 months for an effect; has an ODT formulation

Dose Equivalent (10mg olan./5mg halo.): 200mg

Monitoring: ANC; typical antipsychotic monitoring; serum monitoring may be helpful (therapeutic response usually seen at levels of 350-450ng/mL); requires REMS program certification to prescribe

Mechanism: D2 and 5HT-2A receptor antagonist

ADEs: sedation, orthostatic hypotension; hypersalivation (place towel on pillow); weight gain (30lb gain average at 1yr); constipation (with risk of toxic megacolon); tachycardia (best treated with propranolol); usual serious antipsychotic ADEs; SERIOUS: seizure risk increased; life-threatening neutropenia (1-2%) (avoid neutropenic agents like CBZ) – worse in the first six months

Off-Label: treatment-resistant bipolar disorder; treatment resistant aggression and violence

28
Q

ANC Guidelines for Clozapine

A

Initial: ANC needs to be >1500; in benign ethnic populations (BEN), two ANCs > 1000

  • Weekly ANCs x 6 months; THEN
  • Every-other-week ANCs x 6 months (to 12mos); THEN
  • Monthly ANCs

If level 1000-1500, continue clozapine, but increase ANC to 3x/week

If level 500-1000, hold clozapine, check ANC daily until level > 1000, then follow 3/x protocol

If level <500, discontinue clozapine, consult hematology, and decide on rechallenge if benefits outweigh risks

REPEAT LAB IF BELOW 1500 BEFORE MAKING NEXT CHOICE

Psychopharm (16 decks)

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