Leah Wonderful, PharmD 2016

EFFICACY AND SAFETY OF ANTIPSYCHOTIC AGENTS BY RECEPTOR BINDING AFFINITY

RECEPTOR ANTOGONIZED

DOPAMINE SEROTONIN ADRENGIC MUSCARINIC HISTAMINE

D2 D3 5HT1a 5HT2a 5HT2c 5HT7 a1 M1 M3 H1

THERAPEUTIC EFFECTS

Reduced positive

symptoms

Reduced positive

and negative

symptoms

Reduced EPS & decreased

hyper prolactinemia, antidepressant

anxiolytic

Reduced EPS & decreased

hyper prolactinemia

Antidepressant improved

sleep

Reduced circadian rhythm

dysfunction and

negative symptoms, increased cognitive function

Reduced nightmares

Reduced EPS

Hypnotic

ADVERSE EFFECTS

EPS, increased

hyper prolactinemia,

negative symptoms, cognitive

deficits and sedation

Unknown Unknown Metabolic Metabolic Unknown Dizziness, sedation,

hypotension

Constipation, dry mouth,

blurred vision

Metabolic, sedation

Aripiprazole (Abilify®)

3PA* 3 3 2 2 3 2 0 0 2

Ziprasidone (Geodon®)

3 3 2PA* 4 4 3 2 0 0 2

Lurasidone (Latuda®)

3 0 3 2 1 2 3 0 0 0

Brexpiprazole (Rexulti®)

4PA* 3PA* 4PA* 4 1 1 4 0 0 2

Perphenazine 3 3 2 4 4 4 3 1 0 3

Asenapine (Saphris®)

4 4 1 3 1 2 1 0 0 3

Haloperidol (Haldol®)

3 2 0 1 0 0 2 0 0 0

Paliperidone (Invega®)

3 3 1 4 2 3 3 2 0 2

Iloperidone (Fanapt™)

3 2 2 3 1 2 3 0 0 2

Quetiapine (Seroquel®,

Seroquel XR®) 1 1 1 2 1 2 3 2 2 3

Risperidone (Risperdal® )

3 3 1 4 2 3 3 0 0 2

Olanzapine (Zyprexa®)

2 2 0 3 2 1 2 2 2 3

Clozapine (Clozaril®, FazaClo®)

1 1 1 2 2 2 3 3 2 3

BINDING AFFINITY

0 Ki>1,000 Very weak/none

1 1,000>Ki>100 Weak

2 100>Ki>10 Moderate

3 10>Ki>1 Strong

4 1>Ki Very strong *Denotes partial agonism