1st gen antipsychotics

Question 1

What are the High potency FGAs

Answer 1

HaloPeridol

FluPhenazine

TriFluPeraZine

Question 2

Low potency FGAs

Answer 2

Thioridazine

Chlorpromazine

Question 3

Difference between high and low potency

Answer 3

High potency:
Stronger and more specific D2 binding and blocking
Higher risk for Extrapyramidal symptoms
Higher risk for Neuroleptic Malign Syn
Higher prolactin release and antiandrenergic effects.
But, much fewer antiadrenergic, antihistamine, and antimuscarinic effects.

-Haloperidol is the only AP that has NO effect on histamine receptors at all, and only weak alpha1 blocking

Low potency:
Less EPS
More alpha1, H1, 5HT2, and M4 blocking.

Question 4

What are the phenothiazine drugs

Answer 4

Chlorpromazine
Thioridazine
Fluphenazine

Question 5

What are the butyrophenones

Answer 5

Haloperidol

Question 6

What are the thioxanthenes

Answer 6

Thiothixene

Question 7

Haloperidol actions

Answer 7

Blocks D2 and alpha1 only.

Question 8

Thioridzine actions

Answer 8

Blocks D2, a1, 5HT2, and H1, and very strong antimuscarinic.

Question 9

What are the extrpyramidal symptoms, in order of their development

Answer 9

Acute dystonia,

• within hours,
• especially of the eyes, also head and neck

Akathesia

• in a few days,
• restlessness, inability to remain still,

Parkinsonism

• after days to weeks
• Bradykinesia
• Cogwheel rigidity
• Masked facies

Tardive dyskinesia

• after months or years
• tremor, especially of face, tongue, mouth
• is often irreversible!

Question 10

What are the other side effects of the FGAs

Answer 10

Antihistamine, Antimuscarinic, Anti-androgenic.

• Orthostatic hypo
• Sedation
• Antimuscarinic effects, hot, blind, red, mad, dry, full, and constipated.

Prolactin disinhibition - strongest with high potency
- galactorrhea, amenorrhea, gynecomastia, impotence

Neuroleptic Malignant Syndrome
Rhabdomyolysis

Long QT syndrome and possible Torsades.

ALL antipsychotics, 1st and 2nd gen Lower the Seizure threshold. Increase seizures.

Question 11

What are the kinetics of the FGAs

Answer 11

They are all lipophilic and given orally

All metabolized by the liver and are increased by CYP inhibitors

They have half lives of 20-40 hours

Question 12

Unique eye effect of chlorpromazine

Answer 12

Corneal deposits

Question 13

Unique eye effect of Thioridazine

Answer 13

Retinal deposits.

Question 14

Indications for the FGAs

Answer 14

Acute psychotic episodes
Controls positive symptoms of schizophrenia, bipolar disorders

Tourettes

Sometimes used in panic disorder

2nd line for tourettes after clonidine