PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 14651727-1 2003 AIMS: To characterize the in vitro and in vivo inhibitory effect of stiripentol, a new anticonvulsant, on the metabolism of carbamazepine and saquinavir, which are substrates of CYP3A4. Carbamazepine 124-137 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 178-184 14522368-7 2003 Cytochrome P450 3A4 inducing anti-epileptic drugs like phenytoin, carbamazepine and phenobarbital may significantly increase the metabolism of many chemotherapeutic agents like CPT11 and paclitaxel (but also of newer biological agents like many tyrosine kinase inhibitors). Carbamazepine 66-79 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-19 12606595-4 2003 Felbamate heteroactivates CYP3A4-mediated formation of carbamazepine-10,11-epoxide (carbamazepine-ep), the major metabolite of carbamazepine, in human liver microsomes and recombinant CYP3A4 at relevant in vivo concentrations of both drugs (maximum activation 98% at 10 microM carbamazepine, 1 mM felbamate). Carbamazepine 84-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-32 14512885-8 2003 The influence of drug treatment on expression was examined from patient drug histories, and strong induction of CYP3A4 by carbamazepine and St. John"s wort was found. Carbamazepine 122-135 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 112-118 12606595-4 2003 Felbamate heteroactivates CYP3A4-mediated formation of carbamazepine-10,11-epoxide (carbamazepine-ep), the major metabolite of carbamazepine, in human liver microsomes and recombinant CYP3A4 at relevant in vivo concentrations of both drugs (maximum activation 98% at 10 microM carbamazepine, 1 mM felbamate). Carbamazepine 84-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 184-190 12606595-4 2003 Felbamate heteroactivates CYP3A4-mediated formation of carbamazepine-10,11-epoxide (carbamazepine-ep), the major metabolite of carbamazepine, in human liver microsomes and recombinant CYP3A4 at relevant in vivo concentrations of both drugs (maximum activation 98% at 10 microM carbamazepine, 1 mM felbamate). Carbamazepine 55-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-32 12606595-4 2003 Felbamate heteroactivates CYP3A4-mediated formation of carbamazepine-10,11-epoxide (carbamazepine-ep), the major metabolite of carbamazepine, in human liver microsomes and recombinant CYP3A4 at relevant in vivo concentrations of both drugs (maximum activation 98% at 10 microM carbamazepine, 1 mM felbamate). Carbamazepine 55-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 184-190 12606595-0 2003 In vivo CYP3A4 heteroactivation is a possible mechanism for the drug interaction between felbamate and carbamazepine. Carbamazepine 103-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 8-14 12606595-4 2003 Felbamate heteroactivates CYP3A4-mediated formation of carbamazepine-10,11-epoxide (carbamazepine-ep), the major metabolite of carbamazepine, in human liver microsomes and recombinant CYP3A4 at relevant in vivo concentrations of both drugs (maximum activation 98% at 10 microM carbamazepine, 1 mM felbamate). Carbamazepine 84-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-32 12606595-4 2003 Felbamate heteroactivates CYP3A4-mediated formation of carbamazepine-10,11-epoxide (carbamazepine-ep), the major metabolite of carbamazepine, in human liver microsomes and recombinant CYP3A4 at relevant in vivo concentrations of both drugs (maximum activation 98% at 10 microM carbamazepine, 1 mM felbamate). Carbamazepine 84-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 184-190 12606595-11 2003 Our results strongly suggest that in vivo heteroactivation of CYP3A4 is a possible mechanism of the clinically observed drug interaction between felbamate and carbamazepine. Carbamazepine 159-172 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-68 12673034-3 2003 In this study, we demonstrated the inductive effects of phenobarbital, rifampicin, carbamazepine, phenytoin, prednisolone, ciclosporin and clotrimazole on CYP3A4, CYP3A5 and CYP3A7 mRNA expression, and established the relationship between the expression of human glucocorticoid receptor alpha (hGR) mRNA and the induction of CYP3A4 mRNA in cultured HepG2 cells by reverse transcription polymerase chain reaction (RT-PCR). Carbamazepine 83-96 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 155-161 12673034-3 2003 In this study, we demonstrated the inductive effects of phenobarbital, rifampicin, carbamazepine, phenytoin, prednisolone, ciclosporin and clotrimazole on CYP3A4, CYP3A5 and CYP3A7 mRNA expression, and established the relationship between the expression of human glucocorticoid receptor alpha (hGR) mRNA and the induction of CYP3A4 mRNA in cultured HepG2 cells by reverse transcription polymerase chain reaction (RT-PCR). Carbamazepine 83-96 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 325-331 12673034-4 2003 Treatment with prednisolone, rifampicin and carbamazepine rapidly induced the level of CYP3A4 mRNA expression by 3- to 6-fold. Carbamazepine 44-57 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-93 12642469-0 2003 CYP3A4 and CYP3A7-mediated carbamazepine 10,11-epoxidation are activated by differential endogenous steroids. Carbamazepine 27-40 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 12642469-3 2003 In the present studies, we investigated the effects of endogenous steroids on the activity of CBZ 10,11-epoxidation by expressed CYP3A4 and CYP3A7. Carbamazepine 94-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 129-135 12405865-13 2002 Rifampicin (rifampin), phenobarbital, phenytoin, carbamazepine, nevirapine, and efavirenz decrease methadone blood concentrations, probably by induction of CYP3A4 activity, which can result in severe withdrawal symptoms. Carbamazepine 49-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 156-162 12008131-2 2002 This 10-ketoanalogue of carbamazepine seems to be a weaker inducer of cytochrome P450 3A4. Carbamazepine 24-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 70-89 12007677-6 2002 Apparently, the probable induction of CYP3A4 by carbamazepine results in a nonstereoselective increase in N-demethylation of citalopram. Carbamazepine 48-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-44 11950784-5 2002 To understand the mechanisms of these effects of androgens on CYP3A4 activities, we performed a kinetic analysis of the metabolism of CBZ and ZNS in the presence or absence of AND using the modified two-site equation model. Carbamazepine 134-137 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-68 11513246-14 2001 The 10,11-epoxidation of CBZ by the recombinant CYP3A4 was enhanced by the addition of exogenous cytochrome-b5, leading to a considerable over-prediction. Carbamazepine 25-28 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-54 12397847-3 2002 CBZ also has a low therapeutic index and is metabolized primarily by a single isoform (CYP3A3/4). Carbamazepine 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-93 11808819-6 2002 The clinical course and laboratory findings suggest that carbamazepine decreased the plasma concentration and hence the antihypertensive effect of nilvadipine probably via CYP3A induction. Carbamazepine 57-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 172-177 11318771-1 2001 AIMS: To determine whether the anticonvulsant carbamazepine (CBZ), a known CYP3A4 substrate, is also a substrate for the multidrug efflux transporter P-glycoprotein (Pgp). Carbamazepine 46-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-81 11318771-1 2001 AIMS: To determine whether the anticonvulsant carbamazepine (CBZ), a known CYP3A4 substrate, is also a substrate for the multidrug efflux transporter P-glycoprotein (Pgp). Carbamazepine 61-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-81 11318771-8 2001 Furthermore, the interaction of CBZ with drugs that modulate both CYP3A4 and Pgp function such as verapamil is probably due to inhibition of CYP3A4 and not Pgp. Carbamazepine 32-35 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-72 11318771-8 2001 Furthermore, the interaction of CBZ with drugs that modulate both CYP3A4 and Pgp function such as verapamil is probably due to inhibition of CYP3A4 and not Pgp. Carbamazepine 32-35 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 141-147 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. Carbamazepine 32-45 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 159-165 11158730-14 2001 Inhibition of one or both CYP2C19 and CYP3A isoforms is the likely mechanism by which INH slows the elimination of coadministered drugs, including phenytoin, carbamazepine, diazepam, triazolam, and primidone. Carbamazepine 158-171 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-43 10907977-4 2000 Carbamazepine is metabolized in the liver to a large extent by the cytochrome P450 (CYP) system, especially CYP3A4, 2C8, and 1A2, whereas RTV is metabolized primarily by CYP3A and is a potent inhibitor of this enzyme. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 108-113 9753209-3 1998 Known inducers of CYP3A, such as rifampin, phenytoin, carbamazepine, and phenobarbital, increase the urinary excretion of 6beta-hydroxycortisol and the ratio of 6beta-hydroxycortisol to cortisol. Carbamazepine 54-67 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 18-23 11020127-11 2000 Ritonavir acted as a CYP3A4 inhibitor, diminishing carbamazepine metabolism and provoking an increase in serum levels and clinical toxicity. Carbamazepine 51-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-27 10772431-11 2000 Carbamazepine is a potent enzyme inducer, predominantly of the CYP3A enzyme system, while HIV-protease inhibitors such as indinavir are substrates for and inhibitors of CYP3A. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-68 10772431-11 2000 Carbamazepine is a potent enzyme inducer, predominantly of the CYP3A enzyme system, while HIV-protease inhibitors such as indinavir are substrates for and inhibitors of CYP3A. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 169-174 10771457-13 2000 CONCLUSIONS: Induction of CYP3A4 with carbamazepine led to a modest reduction (<36%) in steady-state exposure to ziprasidone that is believed to be clinically insignificant. Carbamazepine 38-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-32 10486655-9 1999 Following explanation can be hypothesis: several antihypertensive drugs are liver-metabolised by microsomal cytochrome P450 3A4 isoform that could explain a significantly decreased half-life in association with enzymatic inducers, such as rifampicine or antiepileptic drugs (phenobarbital, phenytoin or carbamazepine). Carbamazepine 303-316 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 108-127 10379423-5 1999 CBZ has multiple problematic drug-drug interactions due to its low therapeutic index, metabolism primarily by a single isoform (CYP3A3/4), active epoxide metabolite, susceptibility to CYP3A3/4 or epoxide hydrolase inhibitors, and ability to induce drug metabolism (via both cytochrome P450 oxidation and conjugation). Carbamazepine 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 128-134 10379423-5 1999 CBZ has multiple problematic drug-drug interactions due to its low therapeutic index, metabolism primarily by a single isoform (CYP3A3/4), active epoxide metabolite, susceptibility to CYP3A3/4 or epoxide hydrolase inhibitors, and ability to induce drug metabolism (via both cytochrome P450 oxidation and conjugation). Carbamazepine 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 184-190 10466905-8 1999 Carbamazepine is metabolized by the cytochrome P450 3A4 isoenzyme. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-55 10466905-11 1999 CONCLUSIONS: Fluconazole may cause carbamazepine toxicity presumably by inhibiting the cytochrome P450 3A4 isoenzyme. Carbamazepine 35-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-106 10354960-9 1999 The identification of CYP3A4 as a low-affinity nortriptyline E-10-hydroxylase explains the ability of poor metabolizers of debrisoquin to hydroxylate nortriptyline, as well as the increased in vivo clearance via this pathway caused by CYP3A4-inducing drugs such as pentobarbital, carbamazepine, and rifampin. Carbamazepine 280-293 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 22-28 10354960-9 1999 The identification of CYP3A4 as a low-affinity nortriptyline E-10-hydroxylase explains the ability of poor metabolizers of debrisoquin to hydroxylate nortriptyline, as well as the increased in vivo clearance via this pathway caused by CYP3A4-inducing drugs such as pentobarbital, carbamazepine, and rifampin. Carbamazepine 280-293 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 235-241 10219967-9 1999 Induction of CYP3A4-dependent reporter gene expression and enhancement of the induction by the glucocorticoid receptor was also observed with pregnenolone-16alpha-carbonitrile (PCN), rifampicin, phenytoin, carbamazepine, phenylbutazone and phenobarbitone, all known in vivo inducers of CYP3A4 in man. Carbamazepine 206-219 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 13-19 10613614-2 1999 We have studied the possible effect of the CYP3A4-inducing antiepileptic agents carbamazepine and phenytoin on the pharmacokinetics of vincristine. Carbamazepine 80-93 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-49 10463320-1 1999 RATIONALE: A previously reported pharmacokinetic interaction between bromperidol and carbamazepine, an inducer of cytochrome P450 (CYP) 3A4, suggests possible involvement of CYP3A4 in the metabolism of bromperidol. Carbamazepine 85-98 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-139 10463320-1 1999 RATIONALE: A previously reported pharmacokinetic interaction between bromperidol and carbamazepine, an inducer of cytochrome P450 (CYP) 3A4, suggests possible involvement of CYP3A4 in the metabolism of bromperidol. Carbamazepine 85-98 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 174-180 10217335-5 1999 These results strongly suggest the involvement of CYP3A4, the major CYP enzyme induced by carbamazepine, in the metabolism of both enantiomers of mianserin. Carbamazepine 90-103 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-56 10096433-3 1999 In humans, CYP3A4, CYP2C8 and CYP1A2 have been shown to be implicated in CBZ biotransformation. Carbamazepine 73-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 11-17 9390105-9 1997 With use of carbamazepine, in vivo inhibition constants for CYP3A4 ranged between 12 and 35 mumol/L, whereas the corresponding in vitro value was 80 mumol/L. Carbamazepine 12-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-66 9860152-5 1998 Measurement of urinary 6beta-hydroxycortisol/cortisol excretion was used as an endogenous marker to confirm that induction of CYP3A4 by carbamazepine had occurred. Carbamazepine 136-149 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 126-132 9860152-8 1998 CONCLUSION: Carbamazepine has been shown to induce several P450 cytochromes including CYP3A4 and CYP1A2. Carbamazepine 12-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 86-92 9521735-3 1998 Sigmoidal kinetic characteristics were observed for carbamazepine metabolism by CYP3A4 and naphthalene metabolism by CYPs 2B6, 2C8, 2C9, and 3A5 as well as dapsone metabolism by CYP2C9. Carbamazepine 52-65 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-86 9390105-4 1997 In vivo inhibition constants for CYP3A4 were calculated with use of data that previously documented the interaction between stripentol and carbamazepine. Carbamazepine 139-152 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 33-39 9357097-4 1997 This interaction was probably mediated by an inhibiting action of ketoconazole on cytochrome CYP3A4, the main enzyme responsible for CBZ metabolism. Carbamazepine 133-136 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-99 9314612-4 1997 Compounds which induce CYP3A4 (e.g. carbamazepine, phenytoin and phenobarbital) increase felbamate clearance. Carbamazepine 36-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 23-29 9314612-7 1997 Although not yet examined in vitro, felbamate appears to induce the activity of CYP3A4, which would account for it reducing plasma concentrations of carbamazepine or the progestin gestodene. Carbamazepine 149-162 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-86 9536449-1 1998 The effect of carbamazepine, an inducer of cytochrome P450 (CYP) 3A4, on the single oral dose pharmacokinetics of alprazolam was examined in a double-blind, randomized crossover study with two phases. Carbamazepine 14-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-68 9278208-0 1997 Carbamazepine treatment induces the CYP3A4 catalysed sulphoxidation of omeprazole, but has no or less effect on hydroxylation via CYP2C19. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-42 9278208-7 1997 CONCLUSIONS: CBZ induces CYP3A4, but not, or to a lesser extent, CYP2C19. Carbamazepine 13-16 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 25-31 8968657-16 1996 Interactions observed between fluoxetine and alprazolam, midazolam and carbamazepine seem to occur on the level of CYP3A. Carbamazepine 71-84 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-120 9084959-20 1997 Recognised enzyme inducers of CYP3A, which are likely to be prescribed for patients with HIV disease, include rifampicin (rifampin) [treatment of pulmonary tuberculosis], rifabutin (treatment and prophylaxis of Mycobacterium avium complex), phenobarbital (phenobarbitone), phenytoin and carbamazepine (treatment of seizures secondary to cerebral toxoplasmosis or cerebral lymphoma). Carbamazepine 287-300 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-35 8877250-8 1996 Carbamazepine is a potent inducer of CYP3A4 and other oxidative enzyme system in the liver, and it may also increase glucuronyltransferase activity. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 8930576-4 1996 The substrates and inhibitors of CYP2C19 and CYP3A4 and the known genetic polymorphism of CYP2C19 explain some but not all of the interactions of lansoprazole, and particularly the interactions of omeprazole with carbamazepine, diazepam, phenytoin and theophylline or caffeine. Carbamazepine 213-226 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-51 8817061-6 1996 Microsomal preparations from hCYP3A4/OR cells converted CBZ into its principal oxidative metabolite, carbamazepine-10,11-epoxide (CBZ-E), at a rate of 630 pmol/min per mg protein, confirming a major role of CYP3A4 in this reaction. Carbamazepine 56-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-36 8598183-7 1996 Induction of CYP3A (cytochrome P-450IIIA) enzymes by CBZ and PHT is the most likely explanation of the great difference in the pharmacokinetic and pharmacodynamic profiles of oral midazolam in the two groups. Carbamazepine 53-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 13-18 8817061-6 1996 Microsomal preparations from hCYP3A4/OR cells converted CBZ into its principal oxidative metabolite, carbamazepine-10,11-epoxide (CBZ-E), at a rate of 630 pmol/min per mg protein, confirming a major role of CYP3A4 in this reaction. Carbamazepine 56-59 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-36 8610817-8 1996 Cytochrome P450 3A4 metabolizes terfenadine, astemizole, carbamazepine, alprazolam, triazolam, and other benzodiazepines. Carbamazepine 57-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-19 8806399-6 1995 For CBZ, studies utilizing chemical inhibitors, immunoinhibition, liver bank correlations, and expressed enzymes established that CYP3A4 is the main enzyme catalyzing formation of CBZ-10, 11-epoxide. Carbamazepine 4-7 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 130-136 8748427-4 1995 However, the cytochrome P450 3A subfamily and the 3A3 and 3A4 isoforms (CYP3A3/4) in particular are becoming increasingly important in psychopharmacology as a result of their central involvement in the metabolism of a wide range of steroids and medications, including antidepressants, benzodiazepines, calcium channel blockers, and carbamazepine. Carbamazepine 332-345 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-80 8748427-6 1995 The induction of CYP3A3/4 by medications such as carbamazepine can decrease the concentrations of CYP3A3/4 substrates, yielding inefficiency. Carbamazepine 49-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 17-23 8748427-6 1995 The induction of CYP3A3/4 by medications such as carbamazepine can decrease the concentrations of CYP3A3/4 substrates, yielding inefficiency. Carbamazepine 49-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-104 8535412-5 1995 Next, the P450 inducing potency of E 5110 was compared with those of phenobarbital, rifampicin, phenytoin and carbamazepine, which induce CYP 3A in human subjects and human hepatocyte cultures. Carbamazepine 110-123 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 138-144 8010982-4 1994 This study addressed the role of CYP3A4 in the formation of carbamazepine-10,11-epoxide, the major metabolite of carbamazepine. Carbamazepine 60-73 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 33-39 8010982-5 1994 Results of the study showed that: (1) purified CYP3A4 catalyzed 10,11-epoxidation; (2) cDNA-expressed CYP3A4 catalyzed 10,11-epoxidation (Vmax = 1730 pmol/min/nmol P450, Km = 442 microM); (3) the rate of 10,11-epoxidation correlated with CYP3A4 content in microsomes from sixteen human livers (r2 = 0.57, P < 0.001); (4) triacetyloleandomycin and anti-CYP3A4 IgG reduced 10,11-epoxidation to 31 +/- 6% (sixteen livers) and 43 +/- 2% (four livers) of control rates, respectively; and (5) microsomal 10,11-epoxidation but not phenol formation was activated 2- to 3-fold by alpha-naphthoflavone and progesterone and by carbamazepine itself (substrate activation). Carbamazepine 619-632 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 47-53 8010982-5 1994 Results of the study showed that: (1) purified CYP3A4 catalyzed 10,11-epoxidation; (2) cDNA-expressed CYP3A4 catalyzed 10,11-epoxidation (Vmax = 1730 pmol/min/nmol P450, Km = 442 microM); (3) the rate of 10,11-epoxidation correlated with CYP3A4 content in microsomes from sixteen human livers (r2 = 0.57, P < 0.001); (4) triacetyloleandomycin and anti-CYP3A4 IgG reduced 10,11-epoxidation to 31 +/- 6% (sixteen livers) and 43 +/- 2% (four livers) of control rates, respectively; and (5) microsomal 10,11-epoxidation but not phenol formation was activated 2- to 3-fold by alpha-naphthoflavone and progesterone and by carbamazepine itself (substrate activation). Carbamazepine 619-632 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-108 8010982-5 1994 Results of the study showed that: (1) purified CYP3A4 catalyzed 10,11-epoxidation; (2) cDNA-expressed CYP3A4 catalyzed 10,11-epoxidation (Vmax = 1730 pmol/min/nmol P450, Km = 442 microM); (3) the rate of 10,11-epoxidation correlated with CYP3A4 content in microsomes from sixteen human livers (r2 = 0.57, P < 0.001); (4) triacetyloleandomycin and anti-CYP3A4 IgG reduced 10,11-epoxidation to 31 +/- 6% (sixteen livers) and 43 +/- 2% (four livers) of control rates, respectively; and (5) microsomal 10,11-epoxidation but not phenol formation was activated 2- to 3-fold by alpha-naphthoflavone and progesterone and by carbamazepine itself (substrate activation). Carbamazepine 619-632 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-108 8010982-5 1994 Results of the study showed that: (1) purified CYP3A4 catalyzed 10,11-epoxidation; (2) cDNA-expressed CYP3A4 catalyzed 10,11-epoxidation (Vmax = 1730 pmol/min/nmol P450, Km = 442 microM); (3) the rate of 10,11-epoxidation correlated with CYP3A4 content in microsomes from sixteen human livers (r2 = 0.57, P < 0.001); (4) triacetyloleandomycin and anti-CYP3A4 IgG reduced 10,11-epoxidation to 31 +/- 6% (sixteen livers) and 43 +/- 2% (four livers) of control rates, respectively; and (5) microsomal 10,11-epoxidation but not phenol formation was activated 2- to 3-fold by alpha-naphthoflavone and progesterone and by carbamazepine itself (substrate activation). Carbamazepine 619-632 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-108 8010982-9 1994 The role of CYP3A4 in the major pathway of carbamazepine elimination is consistent with the number of inhibitory drug interactions associated with its clinical use, interactions that result from a perturbation of CYP3A4 catalytic activity. Carbamazepine 43-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 12-18 8010982-9 1994 The role of CYP3A4 in the major pathway of carbamazepine elimination is consistent with the number of inhibitory drug interactions associated with its clinical use, interactions that result from a perturbation of CYP3A4 catalytic activity. Carbamazepine 43-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 213-219 34671997-11 2022 Carbamazepine, a common anti-epileptic medication and known inducer of the CYP3A4 enzyme, may reduce levels of colchicine in the blood resulting in treatment failure. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-81 7917777-14 1994 The results indicate that at concentrations of carbamazepine which produce marked induction of hepatic CYP3A, an enzyme involved in the metabolism and bioactivation of carbamazepine, there is only a slight increase in lymphocyte microsomal epoxide hydrolase. Carbamazepine 47-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 103-108 7917777-14 1994 The results indicate that at concentrations of carbamazepine which produce marked induction of hepatic CYP3A, an enzyme involved in the metabolism and bioactivation of carbamazepine, there is only a slight increase in lymphocyte microsomal epoxide hydrolase. Carbamazepine 168-181 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 103-108 7974626-14 1994 The induction of clozapine metabolism by carbamazepine might be partly mediated by CYP3A4. Carbamazepine 41-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-89 33671323-0 2021 Pharmacokinetics of the CYP3A4 and CYP2B6 Inducer Carbamazepine and Its Drug-Drug Interaction Potential: A Physiologically Based Pharmacokinetic Modeling Approach. Carbamazepine 50-63 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 24-30 34495458-9 2021 Co-administration of moderate CYP3A4 inducers (efavirenz, carbamazepine, phenytoin) was predicted to result in an average decrease in entrectinib exposure between 45 and 79%, with corresponding average decreases for M5 of approximately 50%. Carbamazepine 58-71 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-36 33756436-0 2021 Associations between CYP3A4, CYP3A5 and SCN1A polymorphisms and carbamazepine metabolism in epilepsy: A meta-analysis. Carbamazepine 64-77 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-27 33756436-7 2021 We found that the G allele of CYP3A4 rs2242480 markedly decreased the plasma CBZ concentration in epilepsy. Carbamazepine 77-80 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-36 33756436-11 2021 CONCLUSION: The CYP3A4 rs2242480, CYP3A5 rs776746 and SCN1A rs3812718 polymorphisms may play important roles in CBZ metabolism and resistance, while SCN1A rs2298771 polymorphism is not associated with CBZ in epilepsy. Carbamazepine 112-115 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 16-22 33756436-11 2021 CONCLUSION: The CYP3A4 rs2242480, CYP3A5 rs776746 and SCN1A rs3812718 polymorphisms may play important roles in CBZ metabolism and resistance, while SCN1A rs2298771 polymorphism is not associated with CBZ in epilepsy. Carbamazepine 201-204 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 16-22 33671323-1 2021 The anticonvulsant carbamazepine is frequently used in the long-term therapy of epilepsy and is a known substrate and inducer of cytochrome P450 (CYP) 3A4 and CYP2B6. Carbamazepine 19-32 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 129-154 33671323-5 2021 The carbamazepine model applies metabolism by CYP3A4 and CYP2C8 to produce carbamazepine-10,11-epoxide, metabolism by CYP2B6 and UDP-glucuronosyltransferase (UGT) 2B7 and glomerular filtration. Carbamazepine 4-17 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 46-52 33671323-5 2021 The carbamazepine model applies metabolism by CYP3A4 and CYP2C8 to produce carbamazepine-10,11-epoxide, metabolism by CYP2B6 and UDP-glucuronosyltransferase (UGT) 2B7 and glomerular filtration. Carbamazepine 75-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 46-52 32082165-6 2019 The PBPK model described imatinib pharmacokinetics in adult and paediatric populations and predicted drug interaction with carbamazepine, a cytochrome P450 (CYP)3A4 and 2C8 inducer, with a good accuracy (evaluated by visual inspections of the simulation results and predicted pharmacokinetic parameters that were within 1.25-fold of the clinically observed values). Carbamazepine 123-136 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 140-172 33283769-1 2020 OBJECTIVES: The objectives of this study were to determine the relationship between genetic polymorphisms in gene encodings for CYP3A4 and carbamazepine (CBZ)-induced dose-related side effects in North Indian people with epilepsy. Carbamazepine 139-152 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 128-134 33283769-1 2020 OBJECTIVES: The objectives of this study were to determine the relationship between genetic polymorphisms in gene encodings for CYP3A4 and carbamazepine (CBZ)-induced dose-related side effects in North Indian people with epilepsy. Carbamazepine 154-157 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 128-134 32737897-5 2021 Model-based analysis of carbamazepine-pharmacokinetics quantified significant time- and dose-dependent phenytoin-mediated CYP3A4 induction and carbamazepine-concentration-dependent auto-induction (apparent clearance increased up to 2.5/3-fold). Carbamazepine 24-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 122-128 29569712-2 2018 The objective of this study was to determine if these relationships could be utilized to predict transporter induction by other CYP3A inducers (rifabutin and carbamazepine) and of another P-gp substrate, sofosbuvir. Carbamazepine 158-171 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 128-133 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. Carbamazepine 90-103 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-40 30785734-1 2019 The role of Phe213 in the allosteric mechanism of human cytochrome P450 CYP3A4 was studied using a combination of progesterone (PGS) and carbamazepine (CBZ) as probe substrates. Carbamazepine 137-150 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-78 30785734-1 2019 The role of Phe213 in the allosteric mechanism of human cytochrome P450 CYP3A4 was studied using a combination of progesterone (PGS) and carbamazepine (CBZ) as probe substrates. Carbamazepine 152-155 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-78 30581412-7 2018 Older AEDs, acting on cytochrome P450 isoenzymes, and especially on CYP3A4, such as phenobarbital, phenytoin, and carbamazepine are more likely to significantly reduce the anticoagulant effect of DOACs (especially rivaroxaban, apixaban, and edoxaban). Carbamazepine 114-127 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-74 32910451-6 2020 It is striking that carbamazepine and quetiapine have a strong pharmacokinetic interaction via the metabolizing liver enzyme, CYP3A4. Carbamazepine 20-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 126-132 27690733-2 2017 Carbamazepine (CBZ) is an antiepileptic drug with narrow therapeutic window and administration in humans receiving long-term therapy with diosmin (DSN) may occur, which leads to CYP3A4-mediated drug interactions. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 178-184 29649093-2 2018 The aim of this study was to estimate CYP3A4-inductive potency of EIAEDs by comparing CYP3A4 activity in patients treated with carbamazepine, phenobarbital, or phenytoin. Carbamazepine 127-140 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-44 29649093-10 2018 CONCLUSIONS: This study shows that phenytoin and carbamazepine have approximately twice the CYP3A4-inducing potency of phenobarbital. Carbamazepine 49-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 92-98 29649093-11 2018 The results indicate that 2-fold higher doses of CYP3A4-metabolized drugs may generally be required during concurrent treatment with phenytoin or carbamazepine compared with phenobarbital. Carbamazepine 146-159 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 49-55 29369597-2 2017 A series of studies has shown that concurrent use of carbamazepine decreases quetiapine serum level due to induction of CYP3A enzymes by carbamazepine. Carbamazepine 53-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 120-125 29369597-2 2017 A series of studies has shown that concurrent use of carbamazepine decreases quetiapine serum level due to induction of CYP3A enzymes by carbamazepine. Carbamazepine 137-150 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 120-125 29369597-7 2017 CONCLUSION: We hypothesize that induction of CYP3A lasts even after carbamazepine withdrawal. Carbamazepine 68-81 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-50 29369597-10 2017 The influence of carbamazepine on CYP3A enzymes lasted at least 3 weeks after carbamazepine withdrawal which is in accordance with CYP3A de-induction lasting 3 weeks. Carbamazepine 17-30 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-39 29369597-10 2017 The influence of carbamazepine on CYP3A enzymes lasted at least 3 weeks after carbamazepine withdrawal which is in accordance with CYP3A de-induction lasting 3 weeks. Carbamazepine 17-30 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 131-136 29369597-10 2017 The influence of carbamazepine on CYP3A enzymes lasted at least 3 weeks after carbamazepine withdrawal which is in accordance with CYP3A de-induction lasting 3 weeks. Carbamazepine 78-91 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 34-39 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. Carbamazepine 11-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 106-112 29384591-7 2018 MECHANISM: Induction of CYP3A and potentially phase I metabolism (SULT2A1) by carbamazepine. Carbamazepine 78-91 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 24-29 27690733-2 2017 Carbamazepine (CBZ) is an antiepileptic drug with narrow therapeutic window and administration in humans receiving long-term therapy with diosmin (DSN) may occur, which leads to CYP3A4-mediated drug interactions. Carbamazepine 15-18 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 178-184 27690733-14 2017 The results suggest that the altered CYP3A4 enzyme activity and pharmacokinetics of CBZ might be attributed to DSN-mediated inhibition of CYP3A4 enzyme, which indicates pharmacokinetic interaction present between DSN and CBZ. Carbamazepine 84-87 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 27690733-14 2017 The results suggest that the altered CYP3A4 enzyme activity and pharmacokinetics of CBZ might be attributed to DSN-mediated inhibition of CYP3A4 enzyme, which indicates pharmacokinetic interaction present between DSN and CBZ. Carbamazepine 84-87 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 138-144 27690733-14 2017 The results suggest that the altered CYP3A4 enzyme activity and pharmacokinetics of CBZ might be attributed to DSN-mediated inhibition of CYP3A4 enzyme, which indicates pharmacokinetic interaction present between DSN and CBZ. Carbamazepine 221-224 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 27690733-14 2017 The results suggest that the altered CYP3A4 enzyme activity and pharmacokinetics of CBZ might be attributed to DSN-mediated inhibition of CYP3A4 enzyme, which indicates pharmacokinetic interaction present between DSN and CBZ. Carbamazepine 221-224 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 138-144 27417180-5 2016 The CYP3A4 assay was evaluated using two long t1/2 compounds, carbamazepine and antipyrine (t1/2 > 30 minutes); one moderate t1/2 compound, ketoconazole (10 < t1/2 < 30 minutes); and two short t1/2 compounds, loperamide and buspirone (t1/2 < 10 minutes). Carbamazepine 62-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-10 27776366-10 2017 The results suggest that the altered CYP3A4 enzyme activity and pharmacokinetics of CBZ might be attributed to PIP mediated inhibition of CYP3A4 enzyme. Carbamazepine 84-87 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 27776366-10 2017 The results suggest that the altered CYP3A4 enzyme activity and pharmacokinetics of CBZ might be attributed to PIP mediated inhibition of CYP3A4 enzyme. Carbamazepine 84-87 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 138-144 27821711-3 2017 A further study using the CYP3A4 inducer carbamazepine resulted in an AUCi/AUC ratio of 0.69. Carbamazepine 41-54 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-32 28215696-4 2017 Several antiepileptic drugs like carbamazepine are known to affect P-gp and CYP3A4-activity. Carbamazepine 33-46 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-82 26936324-2 2016 Carbamazepine is an antiepileptic drug which is metabolized by CYP3A4 into carbamazepine-10,11-epoxide. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-69 28215696-11 2017 CONCLUSION: The combination of DOACs with carbamazepine, an inducer of P-gp and CYP3A4-activity, should be avoided since the anticoagulant effect is decreased. Carbamazepine 42-55 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-86 27402728-9 2016 The potential utility of 1beta-hydroxylation of DCA as a urinary CYP3A biomarker was illustrated by comparing the ratio of 1beta-OH-DCA:DCA in a pooled spot urine sample from six healthy control subjects to a sample from one patient treated with carbamazepine, a potent CYP3A inducer; 1beta-OH-DCA:DCA was considerably higher in the patient versus controls (ratio 2.8 vs. 0.4). Carbamazepine 246-259 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 65-70 27450623-7 2016 Carbamazepine, oxcarbazepine, phenytoin, phenobarbital and topiramate might decrease the effect of NOACs by inducing CYP3A4 activity. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 117-123 27650703-0 2016 Correction to Concurrent Cooperativity and Substrate Inhibition in the Epoxidation of Carbamazepine by Cytochrome P450 3A4 Active Site Mutants Inspired by Molecular Dynamics Simulations. Carbamazepine 86-99 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 103-122 27274257-6 2016 Carbamazepine and other antiepileptic drugs can enhance its metabolism via induction of CYP3A4. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-94 26711482-5 2016 The fold change for CYP3A4 induction level by oxcarbazepine, 10-hydroxyoxcarbazepine and carbamazepine was 3.5 (1.2-7.4), 2.7 (0.8-5.7) and 8.3 (3.5-14.5), respectively. Carbamazepine 89-102 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 20-26 26574235-1 2016 AIM: 4beta-hydroxycholesterol (4betaOHC) is an endogenous CYP3A(4) biomarker, which is elevated by use of the CYP3A4 inducer carbamazepine. Carbamazepine 125-138 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 58-63 27276192-0 2016 Effects of EPHX1 and CYP3A4*22 genetic polymorphisms on carbamazepine metabolism and drug response among Tunisian epileptic patients. Carbamazepine 56-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-27 27276192-1 2016 The aim of this study was to evaluate the impact of polymorphisms in the EPHX1 (c.416A > G, c.337T > C) and CYP3A4*22 genes involved in carbamazepine (CBZ) metabolism and pharmacoresistance among 118 Tunisian patients with epilepsy under maintenance dose of CBZ. Carbamazepine 142-155 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-120 26574235-1 2016 AIM: 4beta-hydroxycholesterol (4betaOHC) is an endogenous CYP3A(4) biomarker, which is elevated by use of the CYP3A4 inducer carbamazepine. Carbamazepine 125-138 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-116 26574235-12 2016 This suggests a stronger inductive effect of carbamazepine on presystemic than systemic CYP3A4 phenotype and might indicate a role of the intestine in 4betaOHC formation. Carbamazepine 45-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-94 26651976-2 2016 METHODS: We herein discuss all published data on the contribution of CYP3A5 and its polymorphisms to the metabolism of antipsychotics and antidepressants that are known to be metabolized by CYP3A enzymes, as well as of carbamazepine, an antiepileptic drug used as mood stabilizer. Carbamazepine 219-232 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-74 30085479-0 2016 EFFECT OF CARBAMAZEPINE ON THE ACTIVITY OF CYP3A4 ISOENZYME IN PATIENTS WITH ALCOHOL ADDICTION. Carbamazepine 10-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-49 30085479-1 2016 According to literature data, isoenzyme CYP3A4 of cytochrome P450 is involved in biotransformation of drugs.,At the same time, there is evidence that carbamazepine induces CYP3A4 activity. Carbamazepine 150-163 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 40-46 30085479-1 2016 According to literature data, isoenzyme CYP3A4 of cytochrome P450 is involved in biotransformation of drugs.,At the same time, there is evidence that carbamazepine induces CYP3A4 activity. Carbamazepine 150-163 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 172-178 30085479-2 2016 The purpose of the study was to evaluate the effect of carbamazepine on the CYP3A4 activity in patients with alcohol addiction. Carbamazepine 55-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-82 30085479-5 2016 The results were used to construct a plot and derive an equation of logarithmic regression reflecting the dependence of CYP3A4 activity on the dose of carbamazepine: y = (5.5 - 9.1) x 10-5 - DeltaDeltax2. Carbamazepine 151-164 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 120-126 30085479-6 2016 These data demonstrate a statistically significant effect of carbamazepine on the activity of CYP3A4 isoenzyme in patients with alcohol addiction treated by haloperidol. Carbamazepine 61-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 94-100 25438721-3 2015 Armodafinil and the mood stabilizer carbamazepine are both inducers of and substrates for cytochrome P450 (CYP3A4). Carbamazepine 36-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 107-113 26421491-0 2015 Effects of CYP3A4/5 and ABCB1 genetic polymorphisms on carbamazepine metabolism and transport in Chinese patients with epilepsy treated with carbamazepine in monotherapy and bitherapy. Carbamazepine 55-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 11-17 26315684-0 2015 Evaluation of Cytochrome P450 (CYP) 3A4-Based Interactions of Levomilnacipran with Ketoconazole, Carbamazepine or Alprazolam in Healthy Subjects. Carbamazepine 97-110 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-39 25624269-8 2015 The results suggest that the altered CYP3A4 enzyme activity and pharmacokinetics of CBZ might be attributed to RSV-mediated inhibition of CYP3A4 enzyme. Carbamazepine 84-87 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 25624269-8 2015 The results suggest that the altered CYP3A4 enzyme activity and pharmacokinetics of CBZ might be attributed to RSV-mediated inhibition of CYP3A4 enzyme. Carbamazepine 84-87 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 138-144 25656284-0 2015 Sertraline-induced potentiation of the CYP3A4-dependent neurotoxicity of carbamazepine: an in vitro study. Carbamazepine 73-86 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-45 25656284-13 2015 SIGNIFICANCE: These results demonstrate an unexpected neurotoxic interaction between CBZ and SRT, apparently related to increased CYP3A4-mediated production of reactive CBZ metabolites. Carbamazepine 85-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 130-136 25656284-13 2015 SIGNIFICANCE: These results demonstrate an unexpected neurotoxic interaction between CBZ and SRT, apparently related to increased CYP3A4-mediated production of reactive CBZ metabolites. Carbamazepine 169-172 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 130-136 26516577-7 2015 In addition, PXR (rifampicin) and CAR-selective (carbamazepine and phenytoin) inducers of CYP3A4 and CYP2B6 induction, respectively, were demonstrated. Carbamazepine 49-62 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-96 24691829-1 2014 Carbamazepine (CBZ), an antiepileptic with narrow therapeutic window, is a substrate of CYP 3A4 which metabolizes CBZ to carbamazepine-10,11-epoxide (CBZE). Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-95 25545162-0 2015 Concurrent cooperativity and substrate inhibition in the epoxidation of carbamazepine by cytochrome P450 3A4 active site mutants inspired by molecular dynamics simulations. Carbamazepine 72-85 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-108 25545162-1 2015 Cytochrome P450 3A4 (CYP3A4) is the major human P450 responsible for the metabolism of carbamazepine (CBZ). Carbamazepine 87-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-19 25545162-1 2015 Cytochrome P450 3A4 (CYP3A4) is the major human P450 responsible for the metabolism of carbamazepine (CBZ). Carbamazepine 87-100 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-27 25545162-1 2015 Cytochrome P450 3A4 (CYP3A4) is the major human P450 responsible for the metabolism of carbamazepine (CBZ). Carbamazepine 102-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-19 25545162-1 2015 Cytochrome P450 3A4 (CYP3A4) is the major human P450 responsible for the metabolism of carbamazepine (CBZ). Carbamazepine 102-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-27 25545162-2 2015 To explore the mechanisms of interactions of CYP3A4 with this anticonvulsive drug, we carried out multiple molecular dynamics (MD) simulations, starting with the complex of CYP3A4 manually docked with CBZ. Carbamazepine 201-204 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-51 25545162-3 2015 On the basis of these simulations, we engineered CYP3A4 mutants I369F, I369L, A370V, and A370L, in which the productive binding orientation was expected to be stabilized, thus leading to increased turnover of CBZ to the 10,11-epoxide product. Carbamazepine 209-212 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 49-55 25545162-5 2015 Evaluation of the kinetics profiles of CBZ epoxidation demonstrate that CYP3A4-containing bacterial membranes (bactosomes) as well as purified CYP3A4 (wild-type and mutants I369L/F) exhibit substrate inhibition in reconstituted systems. Carbamazepine 39-42 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 72-78 25545162-7 2015 MD simulations with two to four CBZ molecules provide evidence that the substrate-binding pocket of CYP3A4 can accommodate more than one molecule of CBZ. Carbamazepine 32-35 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-106 25545162-7 2015 MD simulations with two to four CBZ molecules provide evidence that the substrate-binding pocket of CYP3A4 can accommodate more than one molecule of CBZ. Carbamazepine 149-152 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-106 25545162-8 2015 Analysis of the kinetics profiles of CBZ metabolism with a model that combines the formalism of the Hill equation with an allowance for substrate inhibition demonstrates that the mechanism of interactions of CBZ with CYP3A4 involves multiple substrate-binding events (most likely three). Carbamazepine 37-40 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 217-223 25545162-8 2015 Analysis of the kinetics profiles of CBZ metabolism with a model that combines the formalism of the Hill equation with an allowance for substrate inhibition demonstrates that the mechanism of interactions of CBZ with CYP3A4 involves multiple substrate-binding events (most likely three). Carbamazepine 208-211 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 217-223 24898833-2 2015 Data are scarce for this subgroup of patients; however, data for the interaction of antiepileptic drugs with the pituitary axis have shown that chronic use of many antiepileptic drugs, such as carbamazepine, oxcarbazepine, and topiramate, enhances hepatic cytochrome P450 3A4 (CYP3A4) activity, and can decrease serum concentrations of sex hormones. Carbamazepine 193-206 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 256-275 24898833-2 2015 Data are scarce for this subgroup of patients; however, data for the interaction of antiepileptic drugs with the pituitary axis have shown that chronic use of many antiepileptic drugs, such as carbamazepine, oxcarbazepine, and topiramate, enhances hepatic cytochrome P450 3A4 (CYP3A4) activity, and can decrease serum concentrations of sex hormones. Carbamazepine 193-206 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 277-283 24691829-1 2014 Carbamazepine (CBZ), an antiepileptic with narrow therapeutic window, is a substrate of CYP 3A4 which metabolizes CBZ to carbamazepine-10,11-epoxide (CBZE). Carbamazepine 15-18 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-95 24691829-1 2014 Carbamazepine (CBZ), an antiepileptic with narrow therapeutic window, is a substrate of CYP 3A4 which metabolizes CBZ to carbamazepine-10,11-epoxide (CBZE). Carbamazepine 114-117 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-95 25561870-9 2014 Therefore, using Ferula asafetida with CYP3A4 drug substrates should be cautioned especially those with narrow therapeutic index such as cyclosporine, tacrolimus and carbamazepine. Carbamazepine 166-179 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-45 25495409-6 2014 CYP3A4*1G and CYP3A5*3 could influence CBZ metabolism, while POR*28 had no effect on it. Carbamazepine 39-42 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 24817818-0 2014 Effects of EPHX1 and CYP3A4 polymorphisms on carbamazepine metabolism in epileptic patients. Carbamazepine 45-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-27 24817818-2 2014 Moreover, we reported the genotype frequencies of the CYP3A4*22 (rs 35599367, C>T) variant and its influence on the metabolism of CBZ. Carbamazepine 133-136 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 54-60 24861996-0 2014 Association of ABCB1, CYP3A4, EPHX1, FAS, SCN1A, MICA, and BAG6 polymorphisms with the risk of carbamazepine-induced Stevens-Johnson syndrome/toxic epidermal necrolysis in Chinese Han patients with epilepsy. Carbamazepine 95-108 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 22-28 24695353-0 2014 Reduction of nevirapine-driven HIV mutations by carbamazepine is modulated by CYP3A activity. Carbamazepine 48-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 78-83 24695353-6 2014 In contrast, the reduction in HIV-1 mutations by single-dose carbamazepine reached statistical significance at P = 0.04 with an OR of 0.1 (95% CI 0.01-0.90) upon consideration of CYP3A activity, defined as the ratio of 4beta-hydroxycholesterol to cholesterol, and it was more likely in women with higher CYP3A activity. Carbamazepine 61-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 179-184 24695353-6 2014 In contrast, the reduction in HIV-1 mutations by single-dose carbamazepine reached statistical significance at P = 0.04 with an OR of 0.1 (95% CI 0.01-0.90) upon consideration of CYP3A activity, defined as the ratio of 4beta-hydroxycholesterol to cholesterol, and it was more likely in women with higher CYP3A activity. Carbamazepine 61-74 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 304-309 24695353-7 2014 These findings were in agreement with CYP3A induction in carbamazepine-treated patients. Carbamazepine 57-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-43 24695353-8 2014 Likewise, carbamazepine induced CYP3A4, but not CYP2B6, in vitro when combined with nevirapine. Carbamazepine 10-23 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-38 24406279-5 2014 On the other hand, in order to explain the differences in the clinical response to CBZ, genetic polymorphisms in phase I (CYP3A4, CYP3A5 and EPHX1) and phase II (UGT2B7) metabolising enzymes have been assessed; additionally, the influence of transporters (ABCB1 and ABCC2), receptors (PXR) and other drug targets (voltage- gated Na+ channels) in CBZ clinical response has been evaluated. Carbamazepine 83-86 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 122-128 23480152-8 2013 The terminal half-life (t1/2 ) in humans is 105 h; however, in the presence of a strong CYP3A4 inducer (such as carbamazepine), the t1/2 can be reduced. Carbamazepine 112-125 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 88-94 23212742-4 2013 With human hepatocytes, treatment with phenobarbital, hyperforin, carbamazepine, and rifampin significantly increased the levels of CYP3A4, but not CYP24A1 or CYP27B1 mRNA. Carbamazepine 66-79 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 132-138 23716885-6 2013 The coadministration of aripiprazole with carbamazepine leads to significant decrease in blood concentration of aripiprazole possibly due to induction of enzyme CYP3A4 resulting in loss or reduction of clinical efficacy. Carbamazepine 42-55 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 161-167 24292054-3 2013 In our study, the kinetics of CYP3A4-catalyzed carbamazepine 10,11-epoxidation in human liver microsomes was sigmoidal and fitted to the Hill equation, revealing the S50 value of 358 microM, n of 2.0, and the Vmax value of 463 pmol/min/mg. Carbamazepine 47-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-36 23252947-2 2013 MATERIALS & METHODS: Twenty-five SNPs within seven CBZ pathway genes, namely CYP3A4, CYP3A5, EPHX1, NR1I2, UGT2B7, ABCB1 and ABCC2, were analyzed for association with CBZ pharmacokinetics in 90 epilepsy patients. Carbamazepine 55-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-87 23252947-3 2013 RESULTS: The CYP3A4*1B SNP was significantly associated with CBZ clearance. Carbamazepine 61-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 13-19 21996064-0 2012 Histone deacetylase 1 is required for Carbamazepine-induced CYP3A4 expression. Carbamazepine 38-51 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 60-66 24382036-7 2013 Use of carbamazepine, a CYP3A4 inducer, probably led to an increased clearance of rivaroxaban resulting in pulmonary embolisms. Carbamazepine 7-20 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 24-30 22197672-0 2012 Prediction of sites of metabolism in a substrate molecule, instanced by carbamazepine oxidation by CYP3A4. Carbamazepine 72-85 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 99-105 22197672-10 2012 The experimentally known epoxidized sites of CBZ by CYP3A4 were successfully predicted as the most accessible sites to the heme iron that was judged from a numerical analysis of calculated DeltaG(binding) and the frequency of appearance. Carbamazepine 45-48 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-58 21996064-7 2012 In addition, both dominant negative form and siRNA of HDAC1 could repress the CBZ-induced CYP3A4 expression. Carbamazepine 78-81 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 90-96 21996064-3 2012 CBZ is mainly metabolized by cytochrome P450 (CYP) 3A4, a strong inducer of CYP3A4 as well, which in turn influences the pharmaceutical profiles of the co-administrated drugs. Carbamazepine 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-54 21996064-3 2012 CBZ is mainly metabolized by cytochrome P450 (CYP) 3A4, a strong inducer of CYP3A4 as well, which in turn influences the pharmaceutical profiles of the co-administrated drugs. Carbamazepine 0-3 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-82 21996064-8 2012 These data, for the first time indicate that HDAC1, is required for the CBZ-induced CYP3A4 expression. Carbamazepine 72-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-90 21996064-4 2012 To date, little is known about the mechanisms underlying CBZ-induced CYP3A4 expression. Carbamazepine 57-60 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 69-75 21996064-5 2012 In this study, we explored the possible roles of Pregnane X receptor (PXR) and the histone deacetylase 1 (HDAC1) on the CBZ-induced CYP3A4 expression. Carbamazepine 120-123 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 132-138 21992114-4 2011 To unravel the structural basis of MDZ cooperativity, we probed MDZ and CBZ bound to CYP3A4 using longitudinal T(1) nuclear magnetic resonance (NMR) relaxation and molecular docking with AutoDock 4.2. Carbamazepine 72-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-91 21992114-6 2011 These simulations revealed that either two MDZ molecules or an MDZ molecule and a CBZ molecule assume a stacked configuration within the CYP3A4 active site. Carbamazepine 82-85 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 137-143 21832258-5 2011 In the 96-well plate induction assay, the CYP3A4 inducers rifampin, phenobarbital, carbamazepine, phenytoin, troglitazone, rosiglitazone, and pioglitazone yielded dose-dependent induction of LIPA metabolism, whereas the CYP1A2 inducers omeprazole and 3-methylcholanthrene did not display any induction in the CYP3A4 activity. Carbamazepine 83-96 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 42-48 21441468-1 2011 Rifampin and carbamazepine have been recommended in the U.S. Food and Drug Administration draft drug interaction guidance as CYP3A4 inducers for clinical drug-drug interaction (DDI) studies. Carbamazepine 13-26 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-131 21190921-1 2011 Carbamazepine is a (CYP1A2 and CYP3A4 enzyme inducer) medicine which is used by epileptic patients for a long time. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 21294720-14 2011 CYP3A4 overexpression in HEK cells conferred resistance to cytotoxic levels of carbamazepine. Carbamazepine 79-92 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 21294720-15 2011 CYP3A4 levels positively correlated with the amount of CBZ metabolized. Carbamazepine 55-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 20847137-3 2010 In this study, catalytic activities of the two alleles found in East Asians, CYP3A4*16 (T185S) and CYP3A4*18 (L293P), were assessed using the following seven substrates: midazolam, carbamazepine, atorvastatin, paclitaxel, docetaxel, irinotecan, and terfenadine. Carbamazepine 181-194 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 77-83 20847137-3 2010 In this study, catalytic activities of the two alleles found in East Asians, CYP3A4*16 (T185S) and CYP3A4*18 (L293P), were assessed using the following seven substrates: midazolam, carbamazepine, atorvastatin, paclitaxel, docetaxel, irinotecan, and terfenadine. Carbamazepine 181-194 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 99-105 20847137-5 2010 CYP3A4.16 exhibited intrinsic clearances (V(max)/K(m)) that were lowered considerably (by 84-60%) for metabolism of midazolam, carbamazepine, atorvastatin, paclitaxel, and irinotecan compared with CYP3A4.1 due to increased K(m) with or without decreased V(max) values, whereas no apparent decrease in intrinsic clearance was observed for docetaxel. Carbamazepine 127-140 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 20847137-5 2010 CYP3A4.16 exhibited intrinsic clearances (V(max)/K(m)) that were lowered considerably (by 84-60%) for metabolism of midazolam, carbamazepine, atorvastatin, paclitaxel, and irinotecan compared with CYP3A4.1 due to increased K(m) with or without decreased V(max) values, whereas no apparent decrease in intrinsic clearance was observed for docetaxel. Carbamazepine 127-140 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 197-203 21190921-17 2011 This is probably due to the inhibition of CYP3A4 isoenzyme by ciprofloxacin which is responsible for metabolism of CBZ. Carbamazepine 115-118 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 42-48 19255940-0 2009 Functional characterization of CYP3A4.16: catalytic activities toward midazolam and carbamazepine. Carbamazepine 84-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 20699409-6 2010 Cotreatment of avasimibe or efavirenz with 10 muM rifampicin was found to reduce CYP3A activities induced by rifampicin at a lower rate than treatment with rifampicin alone, whereas treatment with phenobarbital and carbamazepine had no effect. Carbamazepine 215-228 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-86 19744012-1 2009 BACKGROUND AND OBJECTIVE: Carbamazepine (CBZ) is metabolized mainly by the CYP3A family of enzymes, which includes CYP3A4 and CYP3A5. Carbamazepine 26-39 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-121 19744012-1 2009 BACKGROUND AND OBJECTIVE: Carbamazepine (CBZ) is metabolized mainly by the CYP3A family of enzymes, which includes CYP3A4 and CYP3A5. Carbamazepine 41-44 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 115-121 19451401-7 2009 LIPA metabolism in human hepatocytes was found to be induced by the treatment of human hepatocytes with the prototypical CYP3A4 inducers rifampin, carbamazepine, omeprazole, phenobarbital, and phenytoin but not by the CYP1A2 inducer 3-methylcholanthrene. Carbamazepine 147-160 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 121-127 20369030-7 2010 AEDs, such as phenytoin, phenobarbital, carbamazepine, felbamate, topiramate, oxcarbazepine and primidone, induce cytochrome P450 3A4, leading to enhanced metabolism of either or both the estrogenic and progestogenic component of OCs, thereby reducing their efficacy in preventing pregnancy. Carbamazepine 40-53 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 114-133 17971810-1 2008 The aim of this study was to develop a model describing the carbamazepine autoinduction and the carbamazepine-mediated induction of CYP3A4, CYP1A2, and P-glycoprotein. Carbamazepine 96-109 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 132-138 19182847-2 2009 Moreover, the 1 mg overnight dexamethasone suppression test was positive and the midnight serum cortisol level was slightly increased, probably as a result of carbamazepine-induced activity of CYP3A4 and increased levels of cortisol binding globulin. Carbamazepine 159-172 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 193-199 18463198-9 2008 The results of this study suggest that CYP3A4-dependent secondary oxidation of 3-OHCBZ represents a potential carbamazepine bioactivation pathway via formation of reactive metabolites capable of inactivating CYP3A4, potentially generating a neoantigen that may play a role in the etiology of carbamazepine-induced idiosyncratic toxicity. Carbamazepine 110-123 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-45 18463198-9 2008 The results of this study suggest that CYP3A4-dependent secondary oxidation of 3-OHCBZ represents a potential carbamazepine bioactivation pathway via formation of reactive metabolites capable of inactivating CYP3A4, potentially generating a neoantigen that may play a role in the etiology of carbamazepine-induced idiosyncratic toxicity. Carbamazepine 110-123 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 208-214 18463198-9 2008 The results of this study suggest that CYP3A4-dependent secondary oxidation of 3-OHCBZ represents a potential carbamazepine bioactivation pathway via formation of reactive metabolites capable of inactivating CYP3A4, potentially generating a neoantigen that may play a role in the etiology of carbamazepine-induced idiosyncratic toxicity. Carbamazepine 292-305 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 39-45 18463198-9 2008 The results of this study suggest that CYP3A4-dependent secondary oxidation of 3-OHCBZ represents a potential carbamazepine bioactivation pathway via formation of reactive metabolites capable of inactivating CYP3A4, potentially generating a neoantigen that may play a role in the etiology of carbamazepine-induced idiosyncratic toxicity. Carbamazepine 292-305 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 208-214 18420779-1 2008 A systematic analysis of the heteroactivation of CYP3A-mediated carbamazepine 10,11-epoxidation has been investigated in three different in vitro systems, namely recombinant CYP3A4 and CYP3A5, human liver microsomes (HLMs) and cryopreserved human hepatocytes. Carbamazepine 64-77 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 49-54 19006545-3 2009 We have previously shown that plasma 4beta-hydroxycholesterol continues to increase for several weeks after maximal induction of CYP3A4/5 by carbamazepine at the dose given. Carbamazepine 141-154 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 129-135 18781906-2 2008 CYP3A4 enzyme-inducing antiepileptic drugs (EIAEDs) like carbamazepine, phenytoin, and oxcarbazepine--as well as non-EIAEDs like valproic acid, levetiracetam, and lamotrigine--are frequently used in patients with GBM. Carbamazepine 57-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 17971810-0 2008 Pharmacodynamics of carbamazepine-mediated induction of CYP3A4, CYP1A2, and Pgp as assessed by probe substrates midazolam, caffeine, and digoxin. Carbamazepine 20-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-62 18372180-3 2008 To clarify the reason why CYP3A4 produces such an energetically unfavorable compound, the mechanism of epoxidation of CBZ by CYP3A4 was investigated by theoretical calculations. Carbamazepine 118-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-32 18279471-5 2008 Whereas induction of CYP3A4/5 was apparently complete within 1-2 weeks of carbamazepine treatment, plasma 4beta-hydroxycholesterol levels continued to increase until at least 8 weeks of treatment. Carbamazepine 74-87 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 21-29 18279471-14 2008 CONCLUSIONS: Carbamazepine treatment of paediatric patients with epilepsy resulted in an induction of CYP3A4/5 and a concomitant increase in plasma 4beta-hydroxycholesterol. Carbamazepine 13-26 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-108 18372180-0 2008 An epoxidation mechanism of carbamazepine by CYP3A4. Carbamazepine 28-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-51 18372180-3 2008 To clarify the reason why CYP3A4 produces such an energetically unfavorable compound, the mechanism of epoxidation of CBZ by CYP3A4 was investigated by theoretical calculations. Carbamazepine 118-121 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 125-131 18372180-1 2008 Human CYP3A4 catalyzes the 10,11-epoxidation of carbamazepine (CBZ). Carbamazepine 48-61 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 6-12 18372180-1 2008 Human CYP3A4 catalyzes the 10,11-epoxidation of carbamazepine (CBZ). Carbamazepine 63-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 6-12 18033049-8 2007 As clarithromycin is also metabolized by CYP3A4, this drug has the propensity to inhibit the metabolism of carbamazepine. Carbamazepine 107-120 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 41-47 18096676-9 2008 The CBZ-modified CYP3A4 retained its functional activity albeit at a reduced level, but its testosterone 6beta-hydroxylase kinetics were altered from sigmoidal (a characteristic profile of substrate cooperativity) to near-hyperbolic (Michaelis-Menten) type, suggesting that CBZ may have modified CYP3A4 within its active site. Carbamazepine 4-7 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 17-23 18096676-9 2008 The CBZ-modified CYP3A4 retained its functional activity albeit at a reduced level, but its testosterone 6beta-hydroxylase kinetics were altered from sigmoidal (a characteristic profile of substrate cooperativity) to near-hyperbolic (Michaelis-Menten) type, suggesting that CBZ may have modified CYP3A4 within its active site. Carbamazepine 4-7 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 296-302 18096676-9 2008 The CBZ-modified CYP3A4 retained its functional activity albeit at a reduced level, but its testosterone 6beta-hydroxylase kinetics were altered from sigmoidal (a characteristic profile of substrate cooperativity) to near-hyperbolic (Michaelis-Menten) type, suggesting that CBZ may have modified CYP3A4 within its active site. Carbamazepine 274-277 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 17-23 18096676-0 2008 CYP3A4-Mediated carbamazepine (CBZ) metabolism: formation of a covalent CBZ-CYP3A4 adduct and alteration of the enzyme kinetic profile. Carbamazepine 16-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 18096676-0 2008 CYP3A4-Mediated carbamazepine (CBZ) metabolism: formation of a covalent CBZ-CYP3A4 adduct and alteration of the enzyme kinetic profile. Carbamazepine 16-29 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-82 18096676-0 2008 CYP3A4-Mediated carbamazepine (CBZ) metabolism: formation of a covalent CBZ-CYP3A4 adduct and alteration of the enzyme kinetic profile. Carbamazepine 31-34 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 18096676-0 2008 CYP3A4-Mediated carbamazepine (CBZ) metabolism: formation of a covalent CBZ-CYP3A4 adduct and alteration of the enzyme kinetic profile. Carbamazepine 31-34 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-82 18096676-0 2008 CYP3A4-Mediated carbamazepine (CBZ) metabolism: formation of a covalent CBZ-CYP3A4 adduct and alteration of the enzyme kinetic profile. Carbamazepine 72-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 18096676-0 2008 CYP3A4-Mediated carbamazepine (CBZ) metabolism: formation of a covalent CBZ-CYP3A4 adduct and alteration of the enzyme kinetic profile. Carbamazepine 72-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 76-82 18096676-2 2008 Sera of CBZ-hypersensitive patients often contain anti-CYP3A antibodies, including those to a CYP3A23 K-helix peptide that is also modified during peroxidative CYP3A4 heme-fragmentation. Carbamazepine 8-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-60 18096676-2 2008 Sera of CBZ-hypersensitive patients often contain anti-CYP3A antibodies, including those to a CYP3A23 K-helix peptide that is also modified during peroxidative CYP3A4 heme-fragmentation. Carbamazepine 8-11 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 160-166 18096676-3 2008 We explored the possibility that cytochromes P450 (P450s) such as CYP3A4 bioactivate CBZ to reactive metabolite(s) that irreversibly modify the P450 protein. Carbamazepine 85-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 66-72 18783297-9 2008 Using this equation, the ICCYP3A4 was calculated for seven inducers (bosentan, carbamazepine, efavirenz, phenytoin, pioglitazone, rifampicin [rifampin], and St John"s wort [hypericum]) on the basis of the reduction in the AUC of a coadministered standard substrate of CYP3A4, such as simvastatin, in ten DDI studies. Carbamazepine 79-92 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-33 18783297-17 2008 It was indicated that coadministration of rifampicin, phenytoin and carbamazepine may reduce plasma AUCs to less than half for a broad range of CYP3A4 substrate drugs, with CRCYP3A4 values greater than 0.13, 0.21 and 0.33, respectively. Carbamazepine 68-81 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 144-150 17502775-9 2007 Both aripiprazole and dehydroaripiprazole are substrates for the cytochrome P-450 3A4 enzyme which is known to be induced by carbamazepine dosed to steady state. Carbamazepine 125-138 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 65-85 17541885-4 2007 Comedication with the CYP3A4 inducer carbamazepine lowered the dose-adjusted aripiprazole concentration by 88%. Carbamazepine 37-50 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 22-28 16600452-6 2006 The concentrations of perospirone and ID-15036 were influenced significantly by the treatment with carbamazepine, and this was probably attributable to the induction of CYP3A4. Carbamazepine 99-112 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 169-175 17346248-0 2007 A comparative pharmacokinetic study in healthy volunteers of the effect of carbamazepine and oxcarbazepine on cyp3a4. Carbamazepine 75-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 110-116 17346248-1 2007 PURPOSE: Carbamazepine (CBZ) and oxcarbazepine (OXCZ) are well-known inducers of drug metabolism via CYP3A4. Carbamazepine 9-22 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 101-107 17346248-1 2007 PURPOSE: Carbamazepine (CBZ) and oxcarbazepine (OXCZ) are well-known inducers of drug metabolism via CYP3A4. Carbamazepine 24-27 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 101-107 17346248-4 2007 We performed a study in healthy volunteers to investigate the relative inductive effect of CBZ and OXCZ on CYP3A4 activity using the metabolism of quinidine as a biomarker reaction. Carbamazepine 91-94 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 107-113 17190925-2 2006 One concern, however, is the increased risk for OC failure with the use of cytochrome P450 3A4 enzyme-inducing AEDs, such as phenobarbital, carbamazepine, phenytoin, felbamate, topiramate, and oxcarbazepine. Carbamazepine 140-153 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 75-94 17374625-8 2007 DATA SYNTHESIS: Elevated plasma concentrations and toxicities have been reported for a number of CYP3A substrates including amiodarone, carbamazepine, quinidine, tacrolimus, and cyclosporine when administered with metronidazole. Carbamazepine 136-149 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 97-102 16135660-12 2005 Thus, CYP3A4-dependent secondary oxidation of 2-hydroxycarbamazepine represents a potential carbamazepine bioactivation pathway leading to the formation of thiol-reactive metabolites, intermediates that may play a role in the etiology of idiosyncratic toxicity attributed to carbamazepine. Carbamazepine 55-68 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 6-12 16720703-10 2006 The major metabolic pathway involves oxidation of carbamazepine via CYP3A4 to an active metabolite, carbamazepine-10,11-epoxide. Carbamazepine 50-63 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 68-74 16390352-10 2006 Quetiapine pharmacokinetics were affected by concomitant administration of ketoconazole and carbamazepine, and therefore other drugs and ingested natural products that strongly modulate the activity or expression of CYP3A4 would be predicted to change exposure to quetiapine. Carbamazepine 92-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 216-222 16135660-12 2005 Thus, CYP3A4-dependent secondary oxidation of 2-hydroxycarbamazepine represents a potential carbamazepine bioactivation pathway leading to the formation of thiol-reactive metabolites, intermediates that may play a role in the etiology of idiosyncratic toxicity attributed to carbamazepine. Carbamazepine 92-105 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 6-12 15829439-5 2005 The induction property of carbamazepine on CYP3A4 was observed through significant increase (p=0.01) in 6 beta-OHC/FC ratio among epileptic patients in comparison with control subjects. Carbamazepine 26-39 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-49 16318439-6 2005 Pharmacokinetic considerations (cytochrome P450 3A3/4 metabolism, active epoxide metabolite and catabolic enzyme induction) can influence the clinical use of CBZ. Carbamazepine 158-161 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-51 15829439-7 2005 Also, measurement of urinary 6 beta-OHC/FC ratio provides a simple non-invasive method to monitor CYP3A4 enzyme induction during administration of carbamazepine antiepileptic drug. Carbamazepine 147-160 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 98-104 15383492-6 2004 CYP3A5 exhibited comparable metabolic activity as CYP3A4 (90-110%) toward dextromethorphan N-demethylation and carbamazepine epoxidation. Carbamazepine 111-124 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 50-56 15673597-2 2005 The ability of pomegranate to inhibit the carbamazepine 10,11-epoxidase activity of CYP3A was examined using human liver microsomes, and pomegranate juice was shown to be a potent inhibitor of human CYP3A. Carbamazepine 42-55 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 84-89 15673597-3 2005 Addition of 25 microl (5.0% v/v) of pomegranate juice resulted in almost complete inhibition of the carbamazepine 10,11-epoxidase activity of human CYP3A (1.8%). Carbamazepine 100-113 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 148-153 15673597-9 2005 Thus, we discovered that a component(s) of pomegranate inhibits the human CYP3A-mediated metabolism of carbamazepine. Carbamazepine 103-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 74-79 15572649-2 2005 It has been previously shown that in vitro CYP3A4 heteroactivation of carbamazepine (CBZ)-epoxide (ep) formation can be associated with the clinical drug interaction between felbatame and CBZ. Carbamazepine 85-88 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-49 15708356-6 2005 Patients treated with the antiepileptic drug carbamazepine, a CYP3A4 inducer, had markedly elevated urinary excretion of 1beta-hydroxydeoxycholic acid compared to healthy controls. Carbamazepine 45-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 62-68 15572649-2 2005 It has been previously shown that in vitro CYP3A4 heteroactivation of carbamazepine (CBZ)-epoxide (ep) formation can be associated with the clinical drug interaction between felbatame and CBZ. Carbamazepine 70-83 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 43-49 15519127-1 2004 Carbamazepine is metabolized by CYP3A4 and several other cytochrome P450 enzymes. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-38 15747502-9 2005 Some drugs such as anticonvulsants (phenobarbital, phenytoin, and carbamazepine) and halothane are suggested to induce hepatitis with anti-CYP3A and anti-CYP2E1, respectively. Carbamazepine 66-79 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 139-144 15519127-11 2004 The observed mean zonisamide t1/2 (36.3h), relative to approximately 65 h reported in subjects on zonisamide monotherapy, reflects known CYP3A4 induction by carbamazepine. Carbamazepine 157-170 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 137-143 15298747-5 2004 DISCUSSION: Carbamazepine is well known as a potent inducer and a substrate of hepatic CYP3A4. Carbamazepine 12-25 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 87-93 15371980-10 2004 CONCLUSIONS: Aside from induction of CYP3A4, carbamazepine acts as an inducer of intestinal MDR1 mRNA, MRP2 mRNA, and MRP2 protein content. Carbamazepine 45-58 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 37-43 15024831-4 2004 Carbamazepine is known to induce hepatic enzyme CYP3A4 and alter metabolism of other drugs. Carbamazepine 0-13 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-54