|
Receptor
|
Paliperidone[25],[26]
|
Risperidone
|
Olanzapine
|
Quetiapinea
|
Ziprasidone
|
Clozapine
|
Aripiprazole
|
Haloperidol
|
|---|
|
Receptor binding affinity expressed as equilibrium constant (Ki)b
|
|
D2
|
1.6 [25]
|
4 [27]
|
11 [27]
|
160 [27]
|
5 [27]
|
126 [27]
|
0.45 [27]
|
0.7 [27]
|
|
5-HT2A
|
1.1 [25]
|
0.5 [27]
|
4 [27]
|
295 [27]
|
0.4 [27]
|
16 [27]
|
3.4 [27]
|
45 [27]
|
|
α1
|
2.5c[25]
|
0.7 [27]
|
19 [27]
|
7 [27]
|
10 [27]
|
7 [27]
|
57 [27]
|
6 [27]
|
|
α2d
|
3.9e[25]
|
3 [27]
|
230 [27]
|
87 [27]
|
– [27]
|
8 [27]
|
– [27]
|
360 [27]
|
|
H1
|
19 [25]
|
20 [27]
|
7 [27]
|
11 [27]
|
47 [27]
|
6 [27]
|
61 [27]
|
440 [27]
|
|
M1
|
>10,000 [25]
|
>10,000 [27]
|
1.9 [27]
|
120 [27]
|
>1,000 [27]
|
1.9 [27]
|
>10,000 [27]
|
>1,500 [27]
|
|
Pharmacokinetic profiles, half-life
|
|
t1/2, h
|
23f[28]
|
3 [29]
|
20–70 [30]
|
5–8 [30]
|
4–10 [30]
|
6–33 [30]
|
48–68 [30]
|
20 [31]
|
|
Tmax, h
|
24 [28]
|
1–2 [29]
|
5–8 [32]
|
1–2 [33, 34]
|
4–6 [35]
|
0.4–4.2 [36]
|
3–5 [37]
|
4.9 [38]
|
|
Bioavailability, %
|
28 [28]
|
70 [29]
|
60–80 [30]
|
9 [39]
|
60 [30]
|
12–81 [30]
|
87 [30, 37]
|
44–74 [31]
|
- aData refer to the quetiapine immediate release formulation; bdata represented as nanomolar concentration required to block 50% of receptors in vitro (Ki [nM]); cthis value relates specifically to affinity for the α1A receptor; dpaliperidone may have higher receptor affinity for the α2A receptor than risperidone [26]; ethis value relates specifically to affinity for the α2A receptor; fdata refer to paliperidone extended release formulation. D2, dopamine type 2 receptor; 5-HT2A, serotonin type 2A receptor; α, alpha-adrenergic receptor; H, histaminergic receptor; M, muscarinic receptor; t1/2, half-life; Tmax, time at which maximum plasma drug concentration is achieved.
