Antipsychotics Flashcards

1
Q

Which dopamine receptor do typicals antagonise?

A

D2

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2
Q

Which dopamine receptor do 2nd generation atypicals antagonize? What makes them different from typicals?

A

D2- Have fast dissociations

They are selective to the meso-limbic area

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3
Q

What other receprors do 2nd generation atypicals antagonize?

A

5-HT2

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4
Q

What receptors do 3rd generation atypicals antagonize?

A

Partial agonist-antagnoist of D2 and 5-HT1A

Antagonist of 5-HT2A

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5
Q

When are typical antipsychotics used?

A

Control active psychosis
Reduce assaultive behavior/agitation
Decanoate for maintenance in non-compliant patients

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6
Q

What is the potency level of haldol?

A

High

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7
Q

What are the worst side effects from haldol?

A

High:

  • EPS
  • Prolactin elevation

Low:

  • Anticholinergic
  • Orthostasis
  • Sedation
  • Wt gain
  • Cardiac arrythmias
  • Seizures
  • Hyperglycemia
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8
Q

What is the potency level of thorazine?

A

Medium

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9
Q

What are the side effects of thorazine?

A

High

  • Anticholinergic
  • Orthostasis
  • Sedation
  • Wt gain

Moderate

  • EPS
  • Cardiac arrythmias
  • Photosensitivity
  • Rashes
  • Pigmentation
  • Glucose intolerance
  • Elevated cholesterol

Low

  • Seizures
  • Blood dyscrasias
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10
Q

In what areas of treatment are atypicals more efficatious then typicals?

A

Negative symptoms

Cognitive symptoms

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11
Q

How is risperdal’s half life special?

A

It’s half life is 3 hrs, but it’s metabolite is 24 hrs

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12
Q

What are the side effects of risperdal?

A

High

  • EPS
  • Elevated prolactin

Moderate

  • Orthostatic hypotension
  • Sedation
  • Metabolic syndrome

Low

  • Anticholinergic
  • Seizures
  • Priapism
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13
Q

Which two atypicals are more effective than risperdal?

A

Clozaril

Zyprexa

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14
Q

What is paliperidone?

A

6-OH-risperidone (active metabolie)

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15
Q

How can you increase the absorptions of paliperidone?

A

Take it with a high calorie meal

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16
Q

What about paliperidone makes it ideal for patients with hepatic insufficency?

A

60% us excreted unchanged by the kidney

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17
Q

What are the side effects of paliperidone?

A

Similar to Risperdal except it may prolong QT

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18
Q

What are the side effects of ziprasidone?

A

Moderate
- Prolong QT

Low

  • Anticholinergic
  • Rash
  • Seizures
  • Elevated prolactin
  • EPS
  • Weight gain
  • Orthostatic hypotension
  • Sedation
  • Metabolic syndrome
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19
Q

What is a concerning disadvantage about ziprasidone (other than prolonged QT)?

A

May be activating

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20
Q

In what circumstances should ziprasidone not be prescribed because of the increased risk of prolonged QT?

A

Bradycardia
Hypokalemia or hypomagnesemia
Other drugs that prolong the QT interval
Congential prolonged QT interval

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21
Q

What is the cut off QT interval for using ziprasidone?

A

> 500 msec

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22
Q

What is the “gold standard” of antipsychotic pharmacology?

A

Clozapine

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23
Q

What about clozapine’s MOA makes it “special”?

A

Exclusive activity on the mesolimbic and mesocortical areas

- Works equally well on postive and negative symptoms

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24
Q

What are the side effects of Clozapine?

A

High

  • Anticholinergic
  • Sedation
  • Metabolic syndrome
  • Orthostasis

Medium

  • Agranulocytosis
  • Myocaarditis
  • Cardiac arrhythmias
  • Sialorrhea
  • Constipation

Low

  • Eosinophilia
  • PE
  • Hepatitis

Minimal

  • EPS
  • Prolactin elevation
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25
Q

What are some advantages of clozapine?

A

Effective for treatment resistant cases
Lowers suicide risk
Effective for treating TD

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26
Q

How many drugs should a patient fail before starting them on clozapine?

A

2 to 3

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27
Q

How often do you need to get a CBC for patients using clozapine?

A

1 wk X 6 months the q2wks

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28
Q

Side effects of olanzapine?

A

High
- Metabolic syndrome

Medium

  • Sedation
  • Orthostasis
  • Anticholinergic

Low

  • EPS
  • Elevated prolactin
  • Cardiac arrhythmias
  • Elevated LFTs
  • Seizures
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29
Q

What drugs are more efficatious then olanzapine?

A

Clozapine

Risperdal

30
Q

Why does quetiapine have a reduced risk for EPS?

A

Rapid dissociation from D2 receptors

31
Q

Side effects of quetiapine?

A

High

  • Sedation
  • Anxiolysis

Moderate

  • Metabolic syndrome
  • Orthostatic hypotension

Low

  • Cataracts
  • Seizures
  • Hypothyroidism
  • Elevated LFTs
  • Cognitive impairment
  • Priapism
  • Anticholinergic
  • Cardiac arrhythmias

Minimal

  • EPS
  • Elevated prolactin
32
Q

What are the side effects of aripipazole?

A

High

  • Activation
  • Akithisia

Moderate

  • Headache
  • GI distress
  • Tremor

Low

  • Anticholinergic
  • Sedation
  • EPS
  • Metabolic syndrome
  • Seizures
  • Orthostatic hypotension
  • Cardiac arrhythmias
33
Q

What drug would you give to a patient who is intolerant of weight gain, sedation, or EPS?

A

Aripipazole

34
Q

What enzyme is responsible for the metabolism of aripipazole?

A

CYP2D6

35
Q

What enzyme metabolizes Iloperidone?

A

CYP2D6

CYP3A4

36
Q

What are the side effects of Iloperidone?

A

High

  • Orthostasis: can be significant; titrate dose
  • Weight gain
  • Dizziness

Moderate

  • Prolong QT
  • Fatigue

Low

  • Akisthisa
  • Blurry vision
  • Ejaculatory failure
37
Q

What drug should be avoided in elderly patients?

A

Iloperidone

38
Q

What receptors does asenopine act on?

A

Adrenergic

Histaminergic

39
Q

What are the side effects of asenopine?

A

High

  • Sedation
  • Dizziness
  • Akithisia
  • Dyskesia

Moderate

  • Orthostasis
  • Syncope
  • Rash

Low

  • Elevated prolactin
  • Weight gain
  • QT prolongation
40
Q

What atypical antipsychotic should you avoid giving to patients with hepatic dysfunction?

A

asenopine

41
Q

What receptors does lurasidone antagonize?

A

5-HT7
5-HT1
5-HT2

42
Q

Side effects of Lurasidone?

A

High

  • Somnolence
  • Akithisia
  • Nausea
  • Agitation
  • EPS

Moderate
- Weight gain

Low
- QT changes

43
Q

What second generation antipsychotic should you avoid using in patients with severe hepatic dysfunction or renal dysfunction?

A

Lurasidone

44
Q

What enzyme metabolizes Lurasidone?

A

CYP3A4

45
Q

Which anxiety disorders can antipsychotics be used to treat?

A

Resistant OCD and PTSD

46
Q

Baseline measurements for cardiac patients?

A

Blood pressure
- Then annual
EKG
- Then once theraputic dose is acheived

47
Q

AIMS monitoring?

A

Baseline then q6 months (typical) or q1 year (atypical)

48
Q

What is a major contibutor for treatment non-adherence with antipsychotics?

A

Weight gain

49
Q

Monitoring for weight

A

Baseline then q1 month then q3 months

50
Q

When is the majority of the weight gained?

A

First 12 weeks

51
Q

What medication can be used to augment the weight gain?

A

Glucophage

52
Q

Lipid monitoring recomendations

A
Baseline screen for family and personel history
Fasting lipid panel
- Baseline
- 6 months
- Yearly
53
Q

Glucose monitoring recommnedations

A

Education

  • Especially if colzapine or olanzipine are used
  • Espeically if risk factors are present

Fasting glucose

  • Baseline
  • q6 months (until 1 year)
  • q1 year provided no changes are documented
54
Q

When will hyperglycemia typically present?

A

10 days to 18 months

55
Q

Effect of elevated prolactin on women? On men?

A
Women
- Galactorrhea
- Amenorrhea
Men
- Sexual dysfuction
- Gynecomastia
56
Q

At what prolactin level with sypmtoms start to occur?

A

80 ng/mL

57
Q

Monitoring recommendations for risperidone?

Prolactin; Cataracts

A

Prolactin
- Yearly
Cataracts
- Annual eye exam

58
Q

What is the first line treatment for Parkinsonism?

Akinesia, masked facies, cogwheel rigidity, tremor, hypersalivation

A
Minimize dose
Anticholinergic medications
- Cogentin (Benzatropine)
- Artane
- Benadryl
59
Q

What are the second line agents for Parkinsonism?

Akinesia, masked facies, cogwheel rigidity, tremor, hypersalivation

A

Dopaminergic medications

  • Amantadine
  • Switch to atypical with lower EPS profile
60
Q

What is the first line treatment for akathisia?

A

Minimize dose

Beta blockers or BZD

61
Q

What is the second line treatment for akathisia?

A

Anticholinergics

Switch to atypical with lower EPS profile

62
Q

Eyes rolling upward

A

Oculogyric crisis

63
Q

Cervical muscle spasm causing torsion of the neck

A

Torticollis

64
Q

Gagging, cyanosis, or asphyxia

Can be life threatening

A

Laryngeal-pharyngeal dystonia

65
Q

What is the recommended treatment for acute dystonic reactions?

A

Anticholinergics

  • Cogentin (Benzatropine)
  • Benadryl
  • Botulism toxin (for TD)
66
Q

Choreathetoid movements of face, trunk, and extremities:

  • Lip smacking
  • Grinding teeth
  • Grunting
  • Rolling of tonque
A

Tardive dyskinesia

67
Q

How often should AIMS be performed?

A

q6 months

68
Q

What is the treatment for TD?

A

Stop antipsychotic or lower dose

Switch to low EPS drug

69
Q

What are the first line antipsychotics to try in a patient with TD?

A

Quitiapine

Clonzapine

70
Q

Idiosyncratic dopamine blockade

  • Rigidity
  • Fever
  • Autonomic instability
  • Delirium
  • Elevated CPK
  • Elevated WBC
A

Neuroleptic malignant syndrome

71
Q

Treatment for NMS?

A
DC antipsychotics
Supportive care
Bromocriptine- DA agonist
Dantroline- Muscle relaxant
ECT