5-HT2A antagonist

5-HT2A serotonin receptor antagonist

5-HT2A serotonin receptor antagonist — mechanism peg (Ballicules) — 5-HT2A antagonist — mechanism card

If BBB-crossing:
Antipsychotic and sleep-promoting effects
May improve negative symptoms
Can offset D2-blockade EPS and prolactin elevation

5-HT2A antagonist (1/2)

An effect of most antipsychotics 2A for 2nd gen Antipsychotic
High 5-HT2A/D2 blocking ratio defines the "atypical" profile—antipsychotic efficacy with reduced motor side effects
By ↓ DA release in the limbic striatum, less D2 receptor blockade is required for antipsychotic effect
↑ DA release in motor striatum → offsets EPS risk
↑ DA release in prefrontal cortex → may improve negative symptoms
↑ DA release in pituitary → offsets prolactin elevation
Decreased propensity for serotonin toxicity
May improve sleep
<a href="/drug/serotonin/">Serotonicity</a> — how much a drug raises synaptic serotonin, and why "serotonergic" is not the same thing

5-HT2A antagonist (2/2)

Not directly associated with weight gain, but may contribute to insulin resistance
Possible antidepressant or mood stabilizing effect

Drugs with this mechanism (91)

7-OH loxapine 8-OH-Amoxapine Loxapine inhaled Amitriptyline Amoxapine Aripiprazole Aripiprazole lauroxil LAI Aripiprazole lauroxil LAI Aripiprazole monohydrate LAI Aripiprazole monohydrate LAI Asenapine Asenapine transdermal Brexpiprazole Buspirone Cariprazine Chlorpromazine Chlorpromazine injection Clomipramine Clozapine Cyclobenzaprine Cyproheptadine Dehydroaripiprazole Desipramine Desmethylcariprazine Desmethylclomipramine (Desmethyl-) mirtazapine Didesmethylcariprazine Diphenhydramine Diphenhydramine injection Domperidone Doxepin Droperidol Clozapine ODT Flibanserin Flupentixol Fluphenazine Fluphenazine decanoate LAI Haloperidol Haloperidol decanoate LAI Haloperidol injection Hydroxynefazodone Hydroxyzine HCl Hydroxyzine IM Hydroxyzine pamoate Iloperidone Imipramine Loxapine Lumateperone Lurasidone Melperone Mianserin Milsaperidone Mirtazapine Molindone Nefazodone Nordoxepin Norquetiapine Nortriptyline Olanzapine Olanzapine IM Olanzapine pamoate LAI Olanzapine SubQ LAI Paliperidone Paliperidone palmitate LAI Paliperidone palmitate LAI Paliperidone palmitate LAI Paliperidone palmitate LAI Perphenazine Pimozide Prochlorperazine Promethazine Promethazine injection Protriptyline Quetiapine Risperidone Risperidone LAI Risperidone LAI Risperidone LAI Risperidone LAI Risperidone LAI Quetiapine XR Doxepin low-dose (insomnia) Thioridazine Thiothixene Trazodone Trifluoperazine Trimipramine Clozapine oral suspension Vilazodone Ziprasidone Ziprasidone IM

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