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Table 1 Approximate receptor binding profiles and half-lives of selected first-generation and second-generation antipsychotics

From: Dosing and switching of paliperidone ER in patients with schizophrenia: recommendations for clinical practice

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]

  1. 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.