PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 18537577-3 2008 Risperidone is metabolized primarily by CYP2D6 and to a lesser extent by CYP3A4; the 9-hydroxy metabolite of risperidone (paliperidone) is now marketed as an antipsychotic in its own right. Risperidone 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-79 19395426-0 2010 Relationship between response to risperidone, plasma concentrations of risperidone and CYP3A4 polymorphisms in schizophrenia patients. Risperidone 33-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-93 19395426-1 2010 In this study, we examined the relationships between plasma concentrations of risperidone and 9-hydroxyrisperidone and polymorphisms of CYP3A4. Risperidone 78-89 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 136-142 19395426-5 2010 Our study has, for the first time, conducted a genetic association study of the CYP3A4 gene with risperidone response. Risperidone 97-108 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-86 21518375-0 2012 Effect of cytochrome P450 3A4 inhibitor ketoconazole on risperidone pharmacokinetics in healthy volunteers. Risperidone 56-67 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 10-29 21518375-16 2012 Ketoconazole significantly inhibited the metabolism of risperidone through the inhibition of hepatic CYP3A4. Risperidone 55-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 101-107 21518375-17 2012 our results suggest that besides CYP2D6, CYP3A4 contributes significantly to the metabolism of risperidone. Risperidone 95-106 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-47 21518375-19 2012 If a CYP3A4 inhibitor is used concomitantly with risperidone, it is necessary for the clinicians to monitor their patients for signs of adverse drug reactions. Risperidone 49-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 5-11 18691984-15 2008 CONCLUSION: In this study, use of medications that are potential inhibitors of CYP2D6 and CYP3A4 appeared to be associated with an increased risk of nonpersistence with risperidone, particularly while patients were still new to treatment. Risperidone 169-180 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-96 16321618-1 2005 BACKGROUND AND OBJECTIVE: Despite the belief that cytochrome P450 (CYP) 2D6 alone is responsible for the metabolism of risperidone, several studies suggest that CYP3A may be involved. Risperidone 119-130 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 161-166 18094221-0 2008 Effect of rifampin, an inducer of CYP3A and P-glycoprotein, on the pharmacokinetics of risperidone. Risperidone 87-98 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-39 18094221-8 2008 Thus, rifampin reduced the exposure to risperidone, probably because of a decrease in its bioavailability through the induction of CYP3A and probably P-glycoprotein. Risperidone 39-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 131-136 17381666-1 2007 BACKGROUND: Although cytochrome P450 (CYP) 2D6 is often thought to be the only CYP responsible for the metabolism of risperidone, many reports suggest that CYP3A may be involved too. Risperidone 117-128 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 156-161 17381666-10 2007 Our results provide in vivo evidence of the involvement of CYP3A in the metabolism of risperidone, in addition to CYP2D6. Risperidone 86-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 59-64 16321618-10 2005 CONCLUSIONS: Our results provide in vivo evidence of the involvement of CYP3A in the disposition of risperidone and 9-hydroxyrisperidone. Risperidone 100-111 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-77 17214606-5 2007 Risperidone is metabolized primarily by CYP2D6 and, to a lesser extent, CYP3A4. Risperidone 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-78 16226034-8 2005 However, higher doses of fluvoxamine may elevate plasma risperidone levels, presumably as a result of a dose-dependent inhibitory effect of fluvoxamine on CYP2D6-and/or CYP3A4-mediated 9-hydroxylation of risperidone. Risperidone 56-67 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 169-175 16321618-2 2005 The aim of this study was to evaluate the effect of itraconazole, a CYP3A inhibitor, on the plasma concentrations of risperidone and 9-hydroxyrisperidone in schizophrenic patients in relation to CYP2D6 genotype. Risperidone 117-128 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-73 16321618-11 2005 In addition to CYP2D6, treatment with CYP3A inhibitor(s) including itraconazole may influence clinical symptoms and risperidone side effects. Risperidone 116-127 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-43 12670127-3 2003 Risperidone is metabolized primarily by CYP2D6 and to a lesser extent by CYP3A4. Risperidone 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-79 15910772-9 2005 Furthermore, ketoconazole, an imidazole-based CYP 3A4 inhibitor, significantly augmented risperidone-induced catalepsy. Risperidone 89-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 46-53 15270204-9 2004 CYP3A4 is the most abundant drug metabolizing enzyme in humans, and in vitro and in vivo results suggest also a role for the enzyme in risperidone metabolism. Risperidone 135-146 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 15883149-5 2005 Genetic variations of cytochrome P450 2D6 (CYP2D6) and drug-drug interactions causing inhibition (CYP2D6 and/or CYP3A) or induction (CYP3A) may be important for risperidone, and perhaps for aripiprazole, dosing. Risperidone 161-172 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 112-117 15883149-5 2005 Genetic variations of cytochrome P450 2D6 (CYP2D6) and drug-drug interactions causing inhibition (CYP2D6 and/or CYP3A) or induction (CYP3A) may be important for risperidone, and perhaps for aripiprazole, dosing. Risperidone 161-172 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 133-138 12172343-8 2002 These findings indicate that fluoxetine, a potent inhibitor of the cytochrome P450 enzyme CYP2D6 and a less potent inhibitor of CYP3A4, reduces the clearance of risperidone by inhibiting its 9-hydroxylation or alternative metabolic pathways. Risperidone 161-172 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 128-134 12665390-6 2003 Atypical antipsychotics are metabolised predominantly by cytochrome p450 (CYP) isoenzymes, particularly CYP1A2 (clozapine and olanzapine), CYP3A4 (clozapine, quetiapine and ziprasidone) and CYP2D6 (olanzapine and risperidone). Risperidone 213-224 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 139-145 10942191-8 2000 These findings demonstrate that carbamazepine markedly decreases the plasma concentrations of risperidone and its active 9-OH-metabolite, probably by inducing CYP3A4-mediated metabolism. Risperidone 94-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 159-165 12186270-2 2002 Risperidone is oxidized by CYP2D6/CYP3A4 and iloperidone is reduced by cytosolic enzymes, although CYP1A2, CYP2E1 and CYP3A4 are involved as well. Risperidone 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 12186270-2 2002 Risperidone is oxidized by CYP2D6/CYP3A4 and iloperidone is reduced by cytosolic enzymes, although CYP1A2, CYP2E1 and CYP3A4 are involved as well. Risperidone 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 118-124 11978161-12 2002 Based on the pharmacokinetics of these medications, we hypothesize that inhibition of CYP2D6 and CYP3A4 by ritonavir and indinavir may have resulted in an accumulation of the active moiety of risperidone, which may explain the occurrence of EPS in this patient. Risperidone 192-203 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-103 11560868-0 2001 Different enantioselective 9-hydroxylation of risperidone by the two human CYP2D6 and CYP3A4 enzymes. Risperidone 46-57 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-92 11560868-8 2001 These findings clearly suggest that CYP2D6 plays a predominant role in (+)-9-hydroxylation of risperidone, the major metabolic pathway in clinical conditions, whereas CYP3A catalyzes the formation of the (-)-9-hydroxymetabolite. Risperidone 94-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 167-172 11476125-7 2001 Drugs that inhibit cytochrome P450 (CYP) 2D6 or induce or inhibit CYP3A4 may alter risperidone plasma concentrations, but the clinical significance of such interactions seems to be minimal. Risperidone 83-94 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-72 34335273-4 2021 Olanzapine is mainly metabolized by cytochrome P450 enzymes, CYP1A2 and CYP2D6, whereas aripiprazole and risperidone metabolism is mainly mediated by CYP2D6 and CYP3A4. Risperidone 105-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 161-167 10771452-5 2000 IC50 values for the inhibition of specific probe substrates for CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4, by ziprasidone, risperidone and 9-hydroxyrisperidone were also determined using human liver microsomes from three subjects. Risperidone 124-135 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-106 10771452-11 2000 Similar in vitro inhibition of CYP2D6 (Ki 6.9-16 microM) and CYP3A4 (Ki 64-80 microM) was obtained with ziprasidone, risperidone and 9-hydroxyrisperidone. Risperidone 117-128 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 61-67 9231305-5 1996 It is postulated that the addition of erythromycin, a known inhibitor of CYP3A and CYP1A2, resulted in alterations in the metabolism of clomipramine and risperidone. Risperidone 153-164 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 73-78 34903590-6 2022 For risperidone, estimated fm values for CYP3A4 and CYP2D6 ranged from 0.87-0.98 and 0.02-0.13, respectively, as compared to in vivo values of 0.36 (CYP3A4) and 0.63-0.88 (CYP2D6), showing that the importance of CYP3A4 was over-estimated and the importance of CYP2D6 under-estimated. Risperidone 4-15 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-47 34903590-6 2022 For risperidone, estimated fm values for CYP3A4 and CYP2D6 ranged from 0.87-0.98 and 0.02-0.13, respectively, as compared to in vivo values of 0.36 (CYP3A4) and 0.63-0.88 (CYP2D6), showing that the importance of CYP3A4 was over-estimated and the importance of CYP2D6 under-estimated. Risperidone 4-15 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 212-218 10843459-3 2000 Risperidone has metabolic routes in common with ziprasidone but shows differences in regard to other main pathways: the benzisoxazole moiety of risperidone is oxidised by cytochrome P450 (CYP) 2D6 to the active 9-hydroxyrisperidone, whereas the benzisothiazole of ziprasidone is primarily oxidised by CYP3A4, yielding sulfoxide and sulfone derivatives with low affinity for target receptors in vitro. Risperidone 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 301-307 10843459-3 2000 Risperidone has metabolic routes in common with ziprasidone but shows differences in regard to other main pathways: the benzisoxazole moiety of risperidone is oxidised by cytochrome P450 (CYP) 2D6 to the active 9-hydroxyrisperidone, whereas the benzisothiazole of ziprasidone is primarily oxidised by CYP3A4, yielding sulfoxide and sulfone derivatives with low affinity for target receptors in vitro. Risperidone 144-155 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 301-307 10453802-4 1999 One case report suggests that CYP3A participates in the metabolism of risperidone. Risperidone 70-81 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-35 10453802-7 1999 Drugs affecting CYP3A, in particular powerful inducers and inhibitors, resulted in at least a 2-fold decrease or increase in plasma risperidone levels. Risperidone 132-143 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 16-21 10453802-9 1999 Drugs influencing CYP3A and CYP2D6 metabolic activity may significantly affect risperidone levels. Risperidone 79-90 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 18-23 10422890-5 1999 Risperidone is metabolized by CYP2D6, and possibly CYP3A4. Risperidone 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 51-57 10048600-3 1999 In the present study, in vitro metabolism of risperidone (100 microM) was investigated using the recombinant human cytochrome P450 (CYP) enzymes CYP1A1, CYP1A2, CYP2C8, CYP2C9-arg144, CYP2C9-cys144, CYP2C19, CYP2D6, CYP3A4 and CYP3A5 supplemented with an NADPH-generating system. Risperidone 45-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 216-222 28520384-2 2012 Risperidone is metabolized to the active metabolite 9-hydroxyrisperidone by the enzyme CYP2D6 and to a lesser extent by CYP3A4. Risperidone 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 120-126 32519344-1 2020 BACKGROUND: Risperidone is a second-generation antipsychotic drug metabolized to an active metabolite, 9-hydroxyrisperidone, primarily by cytochrome P4502D6 (CYP2D6) and to a lesser extent by CYP3A4. Risperidone 12-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 192-198 32276526-8 2020 Risperidone commonly caused (85.7%) potential DDIs with donepezil, lamotrigine and trazodone via the CYP3A4 isoform. Risperidone 0-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 101-107 31359271-3 2020 The goal of this study was to develop a physiologically based pharmacokinetic (PBPK) model considering the CYP2D6 genetic polymorphism for risperidone and 9-hydroxyrisperidone (9-OH-RIS) taking CYP3A4 into account. Risperidone 139-150 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 194-200 32446424-5 2020 Case 2 was also very sensitive to CYP3A4 inducers as indicated by very low C/D ratios for carbamazepine, risperidone and paliperidone. Risperidone 105-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 29055041-3 2018 It was hypothesized that cytochrome P450 (CYP)3A inhibition of the small intestine by voriconazole and P-glycoprotein (P-gp) inhibition of the small intestine by risperidone exerted a synergistic effect on the bioavailability of tacrolimus. Risperidone 162-173 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 25-48 27993531-8 2017 A possible interpretation proposes a slight inducing effect of smoking on risperidone metabolism most likely via CYP3A4. Risperidone 74-85 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 113-119 31359271-12 2020 CONCLUSION: PBPK modelling can provide a valuable tool to predict the pharmacokinetics of risperidone and 9-OH-RIS in healthy volunteers, according to the different CYP2D6 phenotypes taking CYP3A4 into account. Risperidone 90-101 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 190-196 29869546-0 2018 The Use of Carbamazepine to Expedite Metabolism of Risperidone Long-Acting Injection Through Induction of CYP3A4 in a Patient With Extrapyramidal Symptoms. Risperidone 51-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-112 28160505-12 2017 We suggest that the mechanism underlying the effect of perazine on RIS metabolism is based on an inhibition of CYP2D6 and CYP3A4 activity. Risperidone 67-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 122-128 27251417-10 2016 CONCLUSIONS AND LIMITATIONS: Our data show a potential pharmacokinetic interaction, most likely via CYP3A4 between amlodipine and RIS, reflected in significantly different C/Ds for RIS, 9-OH-RIS and AM. Risperidone 130-133 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-106 26387027-4 2015 Pharmacokinetic parameters were derived from plasma concentrations of risperidone and its active metabolite, 9-hydroxyrisperidone (formed via CYP2D6 and CYP3A4), collected before and over 4 days after risperidone administration, and from steady-state plasma concentrations of armodafinil and its circulating metabolites, R-modafinil acid and modafinil sulfone. Risperidone 118-129 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 153-159 25868121-4 2015 Aripiprazole, haloperidol, pimozide, and risperidone are antipsychotics that are metabolized by CYP3A4 and CYP2D6. Risperidone 41-52 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 96-102