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

Question 1

2nd generation (“atypical”) antipsychotic agents

Answer 1

tricyclic compounds
heterocyclic compounds
Benzamides

Question 2

tricyclic compounds

Answer 2

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

drugs …
Clozapine
Olanzapine
Quetiapine

Question 3

heterocyclic compounds

Answer 3

Mixed (DA2 / 5-HT2A) antagonist

drugs ...
Risperidone 
Paliperidone 
Ziprasidone 
Sertindole
Aripiprazole

Question 4

Benzamides

Answer 4

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

drugs …
Sulpiride
Tiapride

Question 5

Sulpiride

Answer 5

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

Question 6

Tiapride

Answer 6

used in acute case IM injection

Question 7

Clozapine

Answer 7

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

Question 8

Olanzapine

Answer 8

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

Question 9

Quetiapine

Answer 9

blocks DA2 > 5-HT2A/C

for bipolar depression

Question 10

Risperidone

Answer 10

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

Question 11

Paliperidone

Answer 11

also H1 , α1, 5-HT1A receptors (partial agonists?)

depot inj. IM

Question 12

Ziprasidone

Answer 12

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

Question 13

Aripiprazole

Answer 13

also partial agonist at D2 and 5-HT1A receptors

In acute case IM injections