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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.