First-Generation Antipsychotics

Question 1

Just in terms of names, what are the first-generation antipsychotics?

Answer 1

Haldol (haloperidol) –think of Van Gogh’s halos

Drugs that end in -azine: trifluoperazine, chlorpromazine, thioridazine, and fluphenazine (think of Starry Gazing)

Question 2

All first-generation antipsychotics work by _______________.

Answer 2

blocking postsynaptic D2 receptors in the CNS (think of the two cuts ropes held by Van Gogh) especially in the striatal and mesolimbic systems

Question 3

Which of the first-generation antipsychotics are high potency?

Answer 3

Haldol (the halos floating “high”) and the drugs with -flu- in them (“fluing” high with trifluperazine and fluphenazine)

Question 4

In terms of gross categories, how do the side effects of high and low potency first-generation antipsychotics compare?

Answer 4

High: more specific binding to D2 receptors leads to a greater chance of extrapyramidal effects (motor)
Low: less specific binding to D2 receptors leads to greater chance of antimuscarinic effects, anti-alpha-1 effects (specifically orthostatic hypotension), and antimuscarinic effects (specifically sedation) –think of the Alice party, the extinguished alpha candle held by the nurse, and the sunflowers with bees being swatted

Question 5

FGAs are better at blocking the __________ effects of schizophrenia.

Answer 5

positive (e.g., hallucinations)

Question 6

In addition to treating acute psychosis, FGAs also treat ______________.

Answer 6

acute agitation/aggression and Tourette’s

Question 7

Pharmacokinetically, most FGAs are _____________.

Answer 7

lipid-soluble with high protein binding –leads to a long, tapering half life

Question 8

Describe the side effects of high-potency FGAs.

Answer 8

Torticollis and other forms of acute dystonia (including oculomotor symptoms)

Question 9

What is akathisia?

Answer 9

Subjective restlessness with the inability to sit still (“Aye KAn’t THIt”)

Question 10

Other than acute dystonia, what other side effects do high-potency FGAs cause?

Answer 10

Akathisia (restlessness) and Parkinson’s – think of the guy jumping out of his chair (unable to sit) and the guy getting into the carriage with cog wheels

Question 11

Tardive dyskinesia presents after ______________.

Answer 11

months to years of treatment with high-potency FGAs

Question 12

True or false: patients with drug-induced Parkinson’s should be treated with L-dopa.

Answer 12

False! Giving a dopamine agonist will likely trigger psychotic symptoms. Instead, give an antimuscarinic for the motor symptoms – such as trihexyphenidyl or benztropine

Question 13

High-potency FGAs can also cause __________ in women.

Answer 13

symptoms of prolactinemia (breast soreness and galactorrhea)

Question 14

All FGAs –and especially the high potency ones –can cause a life-threatening condition characterized by lead-pipe rigidity, agitation, fever, and tachycardia (dysautonomic regulation). What is it?

Answer 14

Neuroleptic malignant syndrome (“Now More Spicy”)

Question 15

Sliding down the banner, the escaping asylee represents the side effects of _____________.

Answer 15

Torsades (the twisting banner) and seizure (because he’s shaking)

Question 16

Of the low-potency first-generation antipsychotics, what do chlorpromazine and thioridazine cause?

Answer 16

Chlorpromazine: corneal deposits (Corn Yellow painting)
Thioridazine: retinal deposits (retinal pallet)