2008
DOI: 10.1016/s0924-977x(08)70669-2
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P.3.d.008 Asenapine pharmacokinetics: influence of cytochrome p450 modulators and udp-glucuronyltransferase inhibition

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Cited by 6 publications
(12 citation statements)
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“…Peak asenapine plasma concentrations of approximately 4 ng/mL are reached approximately 1 hour after sublingual dosing. 10 The administration of a strong CYP1A2 inhibitor, such as fluvoxamine, or severe hepatic impairment has been reported to increase asenapine exposure 11,12 ; exposure to asenapine is not altered in a clinically relevant manner by renal impairment or by mild to moderate hepatic impairment. 11 The asenapine schizophrenia clinical trials program has compared asenapine to placebo, with different agents being used as active comparators (ie, olanzapine, risperidone, and haloperidol).…”
mentioning
confidence: 99%
“…Peak asenapine plasma concentrations of approximately 4 ng/mL are reached approximately 1 hour after sublingual dosing. 10 The administration of a strong CYP1A2 inhibitor, such as fluvoxamine, or severe hepatic impairment has been reported to increase asenapine exposure 11,12 ; exposure to asenapine is not altered in a clinically relevant manner by renal impairment or by mild to moderate hepatic impairment. 11 The asenapine schizophrenia clinical trials program has compared asenapine to placebo, with different agents being used as active comparators (ie, olanzapine, risperidone, and haloperidol).…”
mentioning
confidence: 99%
“…Data on the pharmacokinetic properties of asenapine are available from several studies in healthy volunteers, [22][23][24][25] or patients with hepatic or renal impairment; [26] all of which are published as abstracts.…”
Section: Pharmacokinetic Profilementioning
confidence: 99%
“…[22,24] Asenapine is extensively metabolized, predominantly by uridine diphosphate-glucuronyltransferase (UGT) and cytochrome P450 (CYP) isoenzymes, with asenapine N-glucuronide and N-desmethylasenapine being two major metabolites. [22,25] Both of these metabolites are largely inactive. [22,25] Following administration of single-dose sublingual asenapine 5 mg in healthy volunteers, the C max values for asenapine N-glucuronide and N-desmethylasenapine were 5.34 and 0.39 ng/mL, respectively.…”
Section: Pharmacokinetic Profilementioning
confidence: 99%
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