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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
What are some advantages of clozapine?
Effective for treatment resistant cases Lowers suicide risk Effective for treating TD
26
How many drugs should a patient fail before starting them on clozapine?
2 to 3
27
How often do you need to get a CBC for patients using clozapine?
1 wk X 6 months the q2wks
28
Side effects of olanzapine?
High - Metabolic syndrome Medium - Sedation - Orthostasis - Anticholinergic Low - EPS - Elevated prolactin - Cardiac arrhythmias - Elevated LFTs - Seizures
29
What drugs are more efficatious then olanzapine?
Clozapine | Risperdal
30
Why does quetiapine have a reduced risk for EPS?
Rapid dissociation from D2 receptors
31
Side effects of quetiapine?
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
What are the side effects of aripipazole?
High - Activation - Akithisia Moderate - Headache - GI distress - Tremor Low - Anticholinergic - Sedation - EPS - Metabolic syndrome - Seizures - Orthostatic hypotension - Cardiac arrhythmias
33
What drug would you give to a patient who is intolerant of weight gain, sedation, or EPS?
Aripipazole
34
What enzyme is responsible for the metabolism of aripipazole?
CYP2D6
35
What enzyme metabolizes Iloperidone?
CYP2D6 | CYP3A4
36
What are the side effects of Iloperidone?
High - Orthostasis: can be significant; titrate dose - Weight gain - Dizziness Moderate - Prolong QT - Fatigue Low - Akisthisa - Blurry vision - Ejaculatory failure
37
What drug should be avoided in elderly patients?
Iloperidone
38
What receptors does asenopine act on?
Adrenergic | Histaminergic
39
What are the side effects of asenopine?
High - Sedation - Dizziness - Akithisia - Dyskesia Moderate - Orthostasis - Syncope - Rash Low - Elevated prolactin - Weight gain - QT prolongation
40
What atypical antipsychotic should you avoid giving to patients with hepatic dysfunction?
asenopine
41
What receptors does lurasidone antagonize?
5-HT7 5-HT1 5-HT2
42
Side effects of Lurasidone?
High - Somnolence - Akithisia - Nausea - Agitation - EPS Moderate - Weight gain Low - QT changes
43
What second generation antipsychotic should you avoid using in patients with severe hepatic dysfunction or renal dysfunction?
Lurasidone
44
What enzyme metabolizes Lurasidone?
CYP3A4
45
Which anxiety disorders can antipsychotics be used to treat?
Resistant OCD and PTSD
46
Baseline measurements for cardiac patients?
Blood pressure - Then annual EKG - Then once theraputic dose is acheived
47
AIMS monitoring?
Baseline then q6 months (typical) or q1 year (atypical)
48
What is a major contibutor for treatment non-adherence with antipsychotics?
Weight gain
49
Monitoring for weight
Baseline then q1 month then q3 months
50
When is the majority of the weight gained?
First 12 weeks
51
What medication can be used to augment the weight gain?
Glucophage
52
Lipid monitoring recomendations
``` Baseline screen for family and personel history Fasting lipid panel - Baseline - 6 months - Yearly ```
53
Glucose monitoring recommnedations
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
When will hyperglycemia typically present?
10 days to 18 months
55
Effect of elevated prolactin on women? On men?
``` Women - Galactorrhea - Amenorrhea Men - Sexual dysfuction - Gynecomastia ```
56
At what prolactin level with sypmtoms start to occur?
80 ng/mL
57
Monitoring recommendations for risperidone? | Prolactin; Cataracts
Prolactin - Yearly Cataracts - Annual eye exam
58
What is the first line treatment for Parkinsonism? | Akinesia, masked facies, cogwheel rigidity, tremor, hypersalivation
``` Minimize dose Anticholinergic medications - Cogentin (Benzatropine) - Artane - Benadryl ```
59
What are the second line agents for Parkinsonism? | Akinesia, masked facies, cogwheel rigidity, tremor, hypersalivation
Dopaminergic medications - Amantadine - Switch to atypical with lower EPS profile
60
What is the first line treatment for akathisia?
Minimize dose | Beta blockers or BZD
61
What is the second line treatment for akathisia?
Anticholinergics | Switch to atypical with lower EPS profile
62
Eyes rolling upward
Oculogyric crisis
63
Cervical muscle spasm causing torsion of the neck
Torticollis
64
Gagging, cyanosis, or asphyxia | Can be life threatening
Laryngeal-pharyngeal dystonia
65
What is the recommended treatment for acute dystonic reactions?
Anticholinergics - Cogentin (Benzatropine) - Benadryl - Botulism toxin (for TD)
66
Choreathetoid movements of face, trunk, and extremities: - Lip smacking - Grinding teeth - Grunting - Rolling of tonque
Tardive dyskinesia
67
How often should AIMS be performed?
q6 months
68
What is the treatment for TD?
Stop antipsychotic or lower dose | Switch to low EPS drug
69
What are the first line antipsychotics to try in a patient with TD?
Quitiapine | Clonzapine
70
Idiosyncratic dopamine blockade - Rigidity - Fever - Autonomic instability - Delirium - Elevated CPK - Elevated WBC
Neuroleptic malignant syndrome
71
Treatment for NMS?
``` DC antipsychotics Supportive care Bromocriptine- DA agonist Dantroline- Muscle relaxant ECT ```

Psychopharmacotherapy (8 decks)

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