5. 1st generation (“typical”) antipsychotic agents Flashcards Preview

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1

1st generation (“typical”) antipsychotic agents

D2 antagonists
AE: EPS

types...
Phenothiazines
Thioxanthenes
Butyrophenones
Prochlorperazine

2

extrapyramidal symptoms (EPS)

drug-induced movement disorders...

dystonia (continuous spasms and muscle contractions)
akathisia (motor restlessness)
parkinsonism (characteristic symptoms such as rigidity
bradykinesia (slowness of movement)
tremor
tardive dyskinesia (irregular, jerky movements)
neuroleptic malignent syndrome

3

Phenothiazines

Chlorpromazine
Fluphenazine

4

Chlorpromazine

Aliphatic side chain
receptor affinity: D2 >> M, H1,α1
High sedative and hypotensive actions

5

Fluphenazine

Piperazine side chain
receptor affinity: D2 >> M, H1,α1

6

Thioxanthenes

Thiothixene
Flupenthixol

7

Thiothixene

In acute case IM injection
high clinical potency

8

Flupenthixol

depot inj. IM

9

Butyrophenones

Haloperidol
Droperidol

10

Prochlorperazine

antiemetic

11

Haloperidol

AE: neuroleptic malignant syndrome and tardive dyskinesia (EPS toxicity)
used in acute case IM injections
depot inj. IM
High clinical potency
Very low hypotensive and anticholinergic actions

12

Droperidol

receptor affinity: D2 > H1, α1