Week 13 - Antipsychotics (FGAs and SGAs)

Question 1

What was the first antipsychotic that was created?

Answer 1

Chlorpromazine (Thorazine)

Question 2

FGA: MOA

Answer 2

Reduces dopaminergic neurotransmission in the four dopamine pathways by blocking D2 receptors

• Too much dopamine blockade leads to symptoms of Parkinsonism

Question 3

True/False: Typical antipsychotics (FGAs) do not share the same primary MOA and differs in their therapeutic profiles

Answer 3

False - similar MOA and does not differ in therapeutic profile

But there are differences in secondary properties such as degree of muscarinic, histaminergic, and/or alpha adrenergic receptor antagonism

Question 4

Are FGAs more benefitial for positive or negative symptoms?

Answer 4

Positive

Question 5

Careful monitoring of what syndrome is necessary when taking a FGA?

Answer 5

Neuroleptic malignant syndrome (NMS)

• Extreme muscle rigidity, high fevers, coma, death

Question 6

FGA: examples

Answer 6

• Haloperidol (Haldol)
• Fluphenazine (Prolixin)
• Thioridazine (Mellaril)
• Trifluoperazine (Stelazine)

Question 7

FGAs differ in potency and side effects

• High potency

Answer 7

Examples: haloperidol, fluphenazine

• Carry increased risk of causing EPS

Question 8

FGAs differ in potency and side effects

• Low potency

Answer 8

Examples: chlorpromazine, thioridazine

• Lower risk of EPS, but…
  
  • Increased risk of anticholinergic side effects (dry mouth, constipation, urinary retention, blurred vision)
  • Increased risk of antiadrenergic effects (orthostatic hypotension)

Question 9

Acronym for undesirable effects seen with antipsychotics

Answer 9

STANCE

S: sedation, sunlight sensitivity skin effects, sexual side effects

T: tardive dyskinesia

A: anticholinergic effects and agranulocytosis

N: neuroleptic malignant syndrome

C: cardiac arrhythmias (orthostatic hypotension)

E: extrapyramidal symptoms, akathisia endocrine effects (increased prolactin eye effects)

Question 10

What medications could be prescribed if a patient develops EPS?

Answer 10

Benzotropine, trihexyphenidyl, diphenhydramine

Question 11

What medications could be prescribed if a patient develops tardive dyskinesia?

Answer 11

Diphenhydramine

Question 12

What medications could be prescribed if a patient develops pseudo-Parkinsonism?

Answer 12

Trihexyphenidyl or benztropine

Question 13

How soon will symptoms of EPS appear after administration?

Answer 13

Occurs soon after administration, remits after d/c of medication

• Acute dystonia* - occurs hours to 5 days
• Akathisia* (inner feeling of restlessness) - days to months
• Akinesia* (decrease in voluntary movements) - days to weeks
• Parkinsonism: thorazine shuffle

Question 14

How soon after administration will symptoms of tardive dyskinesia present?

Answer 14

• Late onset - occurs months after initation of therapy
• Commonly persists after d/c
• Can be irreversible

Question 15

How is there an increase in prolactin levels (associated with EPS effects)?

Answer 15

Blockade of dopamine receptors in the tuberoinfundibular tract results in the increased secretion of prolactin

• Results in breast enlargement, galactorrhea, amenorrhea, inhibited orgasm in women, impotence in men

Question 16

What classification of medication is not associated with an increase in prolactin levels?

Answer 16

• Serotonin dopamine antagonist (SDA)* - with the exception of risperidone (Risperdal)
• Drugs of choice for persons experiencing disturbing side effects from increased prolactin

Question 17

Do atypical antipsychotics (SGAs) have more of an effect on positive or negative symptoms?

Answer 17

Both positive and negative

• Low EPS and less hyperprolactinemia compared to FGAs
• Have an antidepressant action

Question 18

SGA: MOA

Answer 18

Blockade of D2 dopamine receptors

• Higher ratio interactions w/ serotonin receptor subtypes (e.g. 5-HT2A)

Question 19

Can atypical antipsychotics (SGAs) also be used for depression?

Answer 19

Yes - interacts w/ dopamine and serotonin receptors

• Serotonin and/or norepinephrine reuptake inhibition
• Alpha-2 antagonism
  
  • All the (-pines) and (-dones)

Question 20

Can antipsychotics be used to treat mania?

Answer 20

Yes - both FGAs and SGAs

• SGAs have greater efficacy for nonpsychotic mania

Question 21

Can antipsychotics be used to treat anxiety?

Answer 21

Controversial use of SGAs for anxiety and PTSD

Quetiapine (Seroquel) has clinical evidence for use in anxiety disorders

Question 22

Pros of the sedating actions of antipsychotics

Answer 22

With short term treatment, sedation is a desired therapeutic effect when patients are aggressive, agitated, or needing sleep induction

Question 23

Cons of the sedating actions of antipsychotics

Answer 23

With long term treatment, sedation is a side effect to be avoided because diminished arousal, sedation, and somnolence can lead to cognitive impairment

Question 24

Which antipsychotics are more sedating: (-pines) or (-dones)?

Answer 24

(-pines)

Question 25

Do antipsychotics (e.g. -pines) have antihistamine actions?

Answer 25

Yes - potent antihistamine actions

Question 26

What are the metabolic risks associated with SGAs?

Answer 26

Weight gain, obesity, dyslipidemia, DM, accelerated CVD, premature death * **High metabolic risk**: clozapine, olanzapine * **Moderate risk**: risperidone, paliperidone, quetiapine, iloperidone (moderate for weight) * **Low risk**: ziprasidone, ariprprazole, lurasidone, iloperidone (low for dyslipidemia)

Question 27

Which antipsychotic is most associated w/ weight gain and metabolic risk?

Answer 27

Olanzapine

Question 28

Which antipsychotic can lead to weight gain, increased triglyceride levels, and may be a second-line option if a primary concern is metabolic issues?

Answer 28

Quetiapine and risperidone

Question 29

Which antipsychotic is weight neutral and has been shown to lower TG levels?

Answer 29

Ziprasidone