Antipsychotics

on 17.9.07 with 0 comments



Typical Antipsychotics: Blockers of Dopamine D2 Post-synaptic Receptors

Phenothiazines – chlorpromazine, fluphenazine, trifluoperazine, thioridazine

Chlorpromazine α1 = 5-HT2 > D2 > D1

Thioxanthines – chlorprothixene, thiothixene

Butyrophenones – haloperidol, droperidol

Haloperidol: D2 > D1 = D4 > α1 > 5-HT2

Others – loxapine, molindone, pimozide



Atypical Antipsychotic Drugs: Lower relative blockade of D2 receptors, no or low EPS

Clozapine Antagonizes D4 = a1 > 5HT2 > D2 = D1; no EPS; agranulocytosis and seizure in 2% of patients

Risperidone D2 and 5HT2 antagonist; antipsychotic > EPS

Olanzapine Most like clozapine in receptor profile, S2 > D2, high M1 and D1 receptor blockage

Quetiapine Similar to clozapine, S2 > D2

Sertindole: Similar to resperidone (5HT and DA antagonist) also a1 antagonist.

Category: Pharmacology Notes

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