6. 2nd generation (“atypical”) antipsychotic agents Flashcards Preview

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1

2nd generation (“atypical”) antipsychotic agents

tricyclic compounds
heterocyclic compounds
Benzamides

2

tricyclic compounds

Mixed (DA2 / 5-HT2A/C) antagonists also H1, α1, and M blockage

drugs ...
Clozapine
Olanzapine
Quetiapine

3

heterocyclic compounds

Mixed (DA2 / 5-HT2A) antagonist

drugs ...
Risperidone
Paliperidone
Ziprasidone
Sertindole
Aripiprazole

4

Benzamides

Selective D2 / (D3) antagonists
eliminated via the kidney in active form

drugs ...
Sulpiride
Tiapride

5

Sulpiride

has very low EPS toxicity, Sedative, hypotensive and anticholinergic actions

6

Tiapride

used in acute case IM injection

7

Clozapine

AE: granulocytopenia
also high affinity for D1, D4
low affinity for D2 (very low EPS toxicity)

8

Olanzapine

blocks 5-HT2A/C > DA2 (very low EPS toxicity)
high clinical potency
medium anticholinergic actions

9

Quetiapine

blocks DA2 > 5-HT2A/C
for bipolar depression

10

Risperidone

blocks 5-HT2A > DA2 (+ H1 and α1 binding)
depot inj. IM
high clinical potency
very low anticholinergic actions

11

Paliperidone

also H1 , α1, 5-HT1A receptors (partial agonists?)
depot inj. IM

12

Ziprasidone

blocks 5-HT2A > DA2and on 5-HT1A receptors (partial agonists?))

13

Aripiprazole

also partial agonist at D2 and 5-HT1A receptors
In acute case IM injections