10-31 Anti-Psychotics

Question 1

*Typical Antipsychotics?
—examples by potency?
—effect?
—side effects?

Answer 1

(C)linical (P)sych is (F)ucking (H)ard
LOW POTENCY
—Chlorpromazine
MID RANGE
—Perphenazine
HIGH POTENCY
—Fluphenazine
—Haloperidol

EFFECT: Antagonize D2-R’s
ADRs: EPS’s (worse w/ ↑ potency), ↑ prolcatin

Question 2

Akathisia

Answer 2

motor restlessness

Question 3

Tardive Dyskinesia

Answer 3

—Oral-facial dyskinesia

—choreoathetosis [combination of chorea (irregular migrating contractions) and athetosis (twisting and writhing)]

Question 4

“Rabbit syndrome”

Answer 4

Perioral tremor

Question 5

Why EPS’s?

Answer 5

Dopaminergic signals in Nigrostriatal pathway altered

Question 6

Neuroleptic Malignant Syndrome

Answer 6

ALL MAJOR: fever, rigidity, ↑↑ CPK

2+ MINOR: tachy, BP∆, altered, tachypneic, diaphoretic

Question 7

Atypical antipsychotics

Answer 7

NEWER, fewer SE's
*Clozapine
Risperidone
*Olanzapine
Quetiapine
*Aripiprazole
(See clozapine) Weight gain!

Question 8

Clozpaine

Answer 8

-atypical antipsychotic
—weak D2 antagonism; potent antagonism at 5-HT2 and NE α2 receptors (↑s NE release)

—fewer EPS's
ADRs
—have to monitor CBC for agranulocytosis
—big wt gain
—myocarditis, szs, sedation, drooling, liver

Question 9

Risperidone

Answer 9

• First post-clozapine atypical antipsychotic
• 5HT2/D2 ratio similar to clozapine
• Side effects: EPS (higher doses), prolactin elevation.

Question 10

*Olanzapine

Answer 10

• Second post clozapine novel antipsychotic
• 5HT/D2 receptor blockade similar to clozapine
• Low EPS, low prolactin elevation
• Side effects: weight gain, gluc/lipid dysreg?, sedation

Question 11

Quetiapine (seroquel)

Answer 11

• 5HT/D2 ratio receptor blockade similar to clozapine
• Few serious side effects
• Minimal EPS
• Minimal prolactin elevation
• Cataract warning (animal studies)

Question 12

*Aripiprazole (Abilify)

Answer 12

• Aripiprazole is a high-affinity D2 PARTIAL agonist
– Functional antagonist under conditions of dopamine hyperactivity (ie, control of positive symptoms)
– Functional agonist in conditions of dopamine hypoactivity (ie, control of negative symptoms, cognitive improvement, minimal motor effects)
• Minimal EPS, no prolactin elevation, low
weight gain.
• Early activation, insomnia