Antipsychotics Flashcards

1
Q
Carbamazepine 
Divalproex 
Lamotrigine 
Lithium 
Valporoic Acid 
→General Use 
→Which are ONLY for mania?
A

General use:
MOOD STABILIZERS

Only mania:
Divalproex
Valproic acid
(*others are mania w/ maintenance)

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2
Q

Lithium

MOA

A

→Not well defined
→Recycles phosphoinositides
Affects the 2nd messengers

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3
Q
Lithium
→Absorption: 
→Distribution: 
→Metabolism: 
→Excretion:
A
Lithium
→Absorption: 
    PO (rapid & complete) 
→Distribution: 
    All of a person's total body water 
→Metabolism: 
    NOT metabolized 
→Excretion: 
    Urine (100% unchanged)
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4
Q
Reversible ECG changes
Thirst (nephrogenic diabetes)
Polyuria
Elevated WBC
Edema
Acneiform skin eruptions
Tremor 
Thyroid enlargement
Nausea
Weight gain
Cognitive impairment
A

Lithium

ADR

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5
Q

Lithium

CI

A
→Severe cardiovascular disease
→Severe renal disease
→Severe debilitation
→Dehydration
→Sodium depletion
→Concurrent use w/diuretics
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6
Q
Lithium
Interactions
1. Thiazides/loops
2. NSAIDs
3. ACE-I/ARB
4. ↓ Salt 
5. Sodium bicarb
6. Theophylline/caffeine 
7. ↑ Salt
A
  1. Thiazides/loops – ↑ [lithium]
  2. NSAIDs – ↑ [lithium]
  3. ACEIs/ARBs – ↑ [lithium]
  4. Severe salt-restricted diet – ↑ [lithium]
  5. Sodium bicarbonate – ↓ [lithium]
  6. Theophylline/caffeine – ↓ [lithium] b/c increased secretion of lithium
  7. Increased intake of sodium – ↓ [lithium]
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7
Q

Lithium

Warnings

A
  1. NARROW Therapeutic Index
  2. Target [ ] → 0.8-1.2 mEq/L in Acute Mania
  3. Target [ ] → 0.6 -0.8 mEq/L
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8
Q

Lithium Target [ ] in Acute Mania

A

0.8-1.2 mEq/L in Acute Mania

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9
Q

Lithium Target [ ] in Bipolar Maintenance

A

Target [ ] → 0.6 -0.8 mEq/L in Bipolar Maintenance

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10
Q

Lithium Pregnancy Category

A

Category D

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11
Q

Lithium

→How do you make sure the pts taking the right dose?

A

MONITOR LEVELS ALWAYS

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12
Q

Monitoring levels of Lithium
→When you just changed the dose?
→When you are just now considering an ↑ dose (w/o a level recently)?
→When a patient is on a steady dose?
→Best practice when drawing a Lithium level?

A

→5-7 days after the change
→Draw a Lithium level
→6-12 mo
→Draw 12 hrs after last dose (before the next one)

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13
Q

P(ee) T(he) BEER

→What does this stand for?

A
Things to monitor when pt is on Lithium
P: pregnancy (need 2 types of birth control) 
T: thyroid (risk of hypothyroid)
B: blood levels
E: ecg
E: electrolytes 
R: renal function
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14
Q

Pt is on lithium for bipolar, finds out she’s pregnant, what med should she be switched to?

A

Lamotrigine

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15
Q
Hallucinations
Delusions
Disorganized thinking
Agitation
→What is the only med that tx these sx?
A

Positive Schizophrenia Sx

→Typical (1st Gen) only cover positive sx

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16
Q

Lack of drive or initiation
Social withdrawal/depression
Apathy
Lack of emotional response

A

Negative Schizophrenia Sx

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17
Q

Chlorpromazine
Haloperidol
Prochlorperazine

→Which one has the worse anticholinergic SE & should be avoided in elderly?
→Order of MOST potent to LEAST potent?

A

Typical (1st Gen) Antipsychotics

Worse anticholinergic:
Chlorpromazine

MOST potent → Haloperidol
LEAST potent → Chlorpromazine

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18
Q
Aripiprazole
Asenapine
Brexpiprazole
Clozapine
Iloperidone
Lurasidone
Olanzapine
Paliperidone
Quetiapine
Risperidone
Ziprasidone
A

Atypical (2nd Gen)

Antipsychotics

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19
Q
Affect/inhibit these receptors: 
-Cholinergic
-Adrenergic
-Dopamine
-Serotonin
-Histamine
→Which one is most related to the clinical effect?
A

Antipsychotics

→Dopamine Antagonism most relates to antipsychotic effect

Typicals: focus is on dopamine effects
Atypicals: focus is on serotonin, dopamine effects

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20
Q

Which hormone does dopamine antagonism affect?

A

Can ↑ prolactin (maybe lactation)

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21
Q
Typical (1st Gen) Antipsychotics
→Absorption: 
→Distribution: 
→Metabolism: 
→Excretion:
A

→Absorption: ERRATIC
→Distribution: Brain > many tissues (lipophylic/highly protein bound)
→Metabolism: LIVER
→Excretion: URINE & BILE

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22
Q

Typical (1st Gen) Antipsychotics

→Phenothiazine metabolixm

A

Can be found in fatty tissues → effects produced up to 3 mo after

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23
Q

Typical (1st Gen) Antipsychotics
ADR
→What is it called when it is EXTREME?

A
  1. Akathesia (can’t sit still)
  2. Acute Dystonia
  3. Dyskinesia
  4. Tardive Dyskinesia
    * Extrapyramidal sx

EXTREME: Neuroleptic Malignant Syndrome

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24
Q

Typical (1st Gen) Antipsychotics
→Neuroleptic Malignant Syndrome
FALTER

A
*Can be fatal
→Muscle rigidity (↑ CPK)
→Extreme EPS 
→Severely ↑ body temp
→↑ HR 
→Death from Respiratory Failure & Cardiac Collapse 

F: fever A: AMS L: leukocytosis T: tremors E: elevated CPK R: rigidity

25
Q

Tx for Neuroleptic Malignant Syndrome

A
  1. Dantrolene
  2. Bromocriptine
  3. DISCONTINUE offending agent
26
Q

LEAST anticholinergic effects
MOST EPS
MOST antipsychotic potency

A

Haloperidol

27
Q

Seizures & antipsychotics

A

Antipsychotics ↓ seizure threshold

28
Q

ECG change w/ Haloperidol

A

↑ QT interval

29
Q

Typical (1st Gen) Antipsychotics

→Black Box Warning

A

Black Box Warning: increased risk for mortality when used in elderly patients with dementia-related behavioral disturbances and psychosis

30
Q

Typical (1st Gen) Antipsychotics

→CI: (3)

A
  1. Parkingson’s dz
  2. Severe CNS depression
  3. Coma
31
Q

Haloperidol

→Clinical Utility (4)

A
  1. N/V in advanced illness
  2. ICU delirium
  3. Psychosis w/ agitation
  4. Rapid tranquilizaiton
32
Q

Synergy with other CNS depressants
CNS depressants may reduce phenothiazine effectiveness, resulting in ↑ psychotic behavior or agitation
Synergy w/ other anticholinergics
May reduce the antiparkinsonian effects of levodopa.
Use with lithium ↑ risk of neurotoxicity
Use with droperidol ↑ risk of EPS
Threshold for seizures is lowered when phenothiazines are used with anticonvulsants
May increase the serum levels of TCAs and beta-blockers

A

Interactions of Chlorpromazine & Prochlorperazine

33
Q

DA-blocking activity can inhibit levodopa and may cause disorientation in patients on both meds
May boost effects of lithium, producing encephalopathy
Has the LEAST anticholinergic effects & MOST EPS and antipsychotic potency
Treat EPS with Benztropine (basically benadryl)

A

Interactions of Haloperidol

34
Q

Treat POSITIVE and NEGATIVE symptoms of schizophrenia

A

Typical (2nd Gen) Antipsychotics

35
Q

Typical (2nd Gen) Antipsychotics
MOA
→Why are Aripiprazole & Brexpiprazole unique?

A

SGAs typically block the dopamine receptors, but to a lesser extent than typical antipsychotics
Produces < EPS
Aripiprazole and brexpiprazole: partial D2 agonists
SGAs also block serotonin receptor activity to varying degrees

36
Q

Typical (2nd Gen) Antipsychotics

→Absorption ↑ w/ food

A

Ziprasidone and paliperidone: absorption increased with food

Take ziprasidone w/ food (increasing its absorption is desired)

37
Q

Typical (2nd Gen) Antipsychotics
→Distribution:
→Metabolism:
→Excretion:

A

→Distribution: large volume & highly protein bound
→Metabolism: usually P450 system in the liver – particularly CYP-2D6, CYP-1A2, and CYP-3A4 isoenzymes
→Excretion: Urine & Stool

38
Q
Weight gain
Muscle rigidity
Parkinsonism
Constipation
Dry mouth
Dizziness
Somnolence/ fatigue
A

Typical (2nd Gen) Antipsychotics
Common ADR

Other: 
EPS: Akathesia, Acute dystonia, Dyskinesia, Tardive dyskinesia
QTc Prolongation
Myocarditis
Hyperlipidemia
Sexual side effects
DM
Cataracts
39
Q

Necessary to enroll in REMS program to track wbc count (risk of agranulocytosis)
→Use

A

Clozapine

→Use: only for tx resistant psychosis

40
Q

→Known hypersensitivity
→CNS depression
→Blood dyscrasias in pts w/ parkingsons
→Liver, renal, cardiac insufficiency
→Caution in diabetics, elderly, or debilitated
→SSRI + antipsychotic → sudden EPS
→Cigarette smoking ↓ antipsychotic plasma [ ]
→Carbamazepine + antipsychotic → 50% reduction in antipsychotic level
→Fluvoxamine + antipsychotic →↑ haldol & clozaril
→BB + antipsych → severe HYPO tension
→Antidepressants + antipsych → ↑ antidepressant [ ]

A

CI for Atypical Antipsych

41
Q

Typical (2nd Gen) Antipsychotic w/ these SE:
Insomnia, agitation, prolactin ↑, EPS at higher doses
→Use

A

Risperidone

→Use: broad efficacy

42
Q

Typical (2nd Gen) Antipsychotic w/ these SE:
HA, sedation, weight ↑, hyperlipidemia, DM
→Use

A

Olanzapine

→ Use: very effective w/ positive/negative sx

43
Q

Typical (2nd Gen) Antipsychotic w/ these SE:

Sedation, postural HYPOtension, dizziness, constipation

A

Quetiapine

→Use: broad efficacy (less weight gain than risperidone)

44
Q

Typical (2nd Gen) Antipsychotic w/ these SE:
Insomnia, EPS at higher doses, QT prolongation
→Use

A

Ziprasidone

→Use: only for tx resistant psychosis (less weight gain than clozapine)

45
Q

Typical (2nd Gen) Antipsychotic w/ these SE:
Mild, dose related EPS
→Use

A

Aripiprazole

→Use: novel mechanism (less weight gain)

46
Q

Typical (2nd Gen) Antipsychotic w/ these SE:

Tachycardia, HA, somnolence, anxiety

A

Paliperidone

47
Q

Typical (2nd Gen) Antipsychotic w/ these SE:

Nausea, dry mouth, somnolence, weight gain, muscle stiffness, arthralgia

A

Iloperidone

48
Q

Typical (2nd Gen) Antipsychotic w/ these SE:

EPS, akathisia, hypoesthesia, dry mouth, ↑ appetite, abdominal pain

A

Asenapine

49
Q

Typical (2nd Gen) Antipsychotic w/ these SE:

N/V, parkinsonism, dyspepsia, akathisia, anxiety, weight gain

A

Lurasidone

50
Q

Typical (2nd Gen) Antipsychotic:

Used for tx of resistant schizophrenia & preventing suicide in schizophrenia

A

Clozapine

51
Q

Typical (2nd Gen) Antipsychotic:

Highest EPS

A

Risperidone

52
Q

Typical (2nd Gen) Antipsychotic:

Highest ↑ in prolactin

A

Risperidone

53
Q

Typical (2nd Gen) Antipsychotic:

Highest anticholinergic SE

A

Clozapine

54
Q

Typical (2nd Gen) Antipsychotic:

Highest sedation

A

Clozapine > Olanzapine > Quetiapine

55
Q

Typical (2nd Gen) Antipsychotic:

Highest weight gain

A

Clozapine > Olanzapine

56
Q

Typical (2nd Gen) Antipsychotic:

Highest risk of diabetes

A

Clozapine > Olanzapine

57
Q

Typical (2nd Gen) Antipsychotic:

Highest dyslipidemia

A

Clozapine > Olanzapine

58
Q

Typical (2nd Gen) Antipsychotic:

Used if concerned about QTc prolongation

A

Aripiprazole

59
Q

Risperidone vs haloperidol compared at high potency with maintenance of psychosis

A

Risperidone has fewer relapses