5. 1st generation (“typical”) antipsychotic agents Flashcards
1st generation (“typical”) antipsychotic agents
D2 antagonists
AE: EPS
types... Phenothiazines Thioxanthenes Butyrophenones Prochlorperazine
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
Phenothiazines
Chlorpromazine
Fluphenazine
Chlorpromazine
Aliphatic side chain
receptor affinity: D2»_space; M, H1,α1
High sedative and hypotensive actions
Fluphenazine
Piperazine side chain
receptor affinity: D2»_space; M, H1,α1
Thioxanthenes
Thiothixene
Flupenthixol
Thiothixene
In acute case IM injection
high clinical potency
Flupenthixol
depot inj. IM
Butyrophenones
Haloperidol
Droperidol
Prochlorperazine
antiemetic
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
Droperidol
receptor affinity: D2 > H1, α1
