1. 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