PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 31885304-4 2020 Literature data on decreases in the area under the curve (AUC) of alfentanil, a CYP3A substrate, caused by CYP3A inducers were also collected. Alfentanil 66-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 80-85 31885304-4 2020 Literature data on decreases in the area under the curve (AUC) of alfentanil, a CYP3A substrate, caused by CYP3A inducers were also collected. Alfentanil 66-76 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 107-112 21562488-1 2011 Systemic and oral clearances of alfentanil (ALF) are in vivo probes for hepatic and first-pass cytochrome P450 (CYP) 3A. Alfentanil 32-42 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-119 31853755-11 2020 When the model was integrated with independently developed CYP3A4 substrate models (midazolam and alfentanil), the observed AUC change of substrates by voriconazole was inside the 90% confidence interval of the predicted AUC change, indicating that CYP3A4 inhibition was appropriately incorporated into the voriconazole model. Alfentanil 98-108 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 59-65 31853755-11 2020 When the model was integrated with independently developed CYP3A4 substrate models (midazolam and alfentanil), the observed AUC change of substrates by voriconazole was inside the 90% confidence interval of the predicted AUC change, indicating that CYP3A4 inhibition was appropriately incorporated into the voriconazole model. Alfentanil 98-108 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 249-255 29926893-3 2018 The cytochrome P-450 3A4 (CYP3A4) gene has been reported to contribute significantly to human liver microsomal oxidation of sufentanil and alfentanil. Alfentanil 139-149 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 4-24 29926893-3 2018 The cytochrome P-450 3A4 (CYP3A4) gene has been reported to contribute significantly to human liver microsomal oxidation of sufentanil and alfentanil. Alfentanil 139-149 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-32 24671884-5 2014 The new models were validated by showing improved predictions of the systemic clearances of ropivacaine (major CYP1A2 substrate; minor CYP3A4 substrate) and alfentanil (major CYP3A4 substrate) compared with those using a previous ontogeny function based on in vitro data (alfentanil: mean squared prediction error 3.0 vs. 6.8; ropivacaine: mean squared prediction error 2.3 vs.14.2). Alfentanil 157-167 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 175-181 21562488-1 2011 Systemic and oral clearances of alfentanil (ALF) are in vivo probes for hepatic and first-pass cytochrome P450 (CYP) 3A. Alfentanil 44-47 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 95-119 21562488-3 2011 This investigation determined ALF sensitivity for detecting graded CYP3A induction and compared it with that of midazolam (MDZ). Alfentanil 30-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 67-72 19232844-4 2009 CYP3A4/5 and transporters were assessed using alfentanil and fexofenadine, respectively. Alfentanil 46-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-6 17112806-1 2006 OBJECTIVE: Alfentanil is a short-acting synthetic opioid analgesic, which is extensively metabolized, mainly by hepatic cytochrome P450 (CYP) 3A enzymes. Alfentanil 11-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 120-144 17554244-0 2007 Influence of CYP3A5 genotype on the pharmacokinetics and pharmacodynamics of the cytochrome P4503A probes alfentanil and midazolam. Alfentanil 106-116 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 81-87 17554244-1 2007 The hepatic and first-pass cytochrome P4503A (CYP3A) probe alfentanil (ALF) is also metabolized in vitro by CYP3A5. Alfentanil 59-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 27-33 17554244-1 2007 The hepatic and first-pass cytochrome P4503A (CYP3A) probe alfentanil (ALF) is also metabolized in vitro by CYP3A5. Alfentanil 59-69 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 46-51 16172184-1 2005 This investigation determined the ability of alfentanil miosis and single-point concentrations to detect various degrees of CYP3A inhibition. Alfentanil 45-55 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 124-129 16291719-0 2005 Alfentanil-induced miosis clearance as a liver CYP3A4 and 3A5 activity measure in healthy volunteers: improvement of experimental conditions. Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 47-53 16291719-1 2005 The aims of this study were to demonstrate the correlation between alfentanil-induced miosis evaluation and alfentanil pharmacokinetics (PK) as a CYP3A4 and 3A5 activity probe in volunteers and to explain the variability in pupilar response and in alfentanil PK. Alfentanil 67-77 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 146-152 16291719-1 2005 The aims of this study were to demonstrate the correlation between alfentanil-induced miosis evaluation and alfentanil pharmacokinetics (PK) as a CYP3A4 and 3A5 activity probe in volunteers and to explain the variability in pupilar response and in alfentanil PK. Alfentanil 108-118 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 146-152 16291719-1 2005 The aims of this study were to demonstrate the correlation between alfentanil-induced miosis evaluation and alfentanil pharmacokinetics (PK) as a CYP3A4 and 3A5 activity probe in volunteers and to explain the variability in pupilar response and in alfentanil PK. Alfentanil 108-118 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 146-152 16291719-7 2005 Alfentanil-induced miosis clearance as a noninvasive CYP3A4 and 3A5 activity measure can be done in both ambient and dark conditions. Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 53-59 16172184-13 2005 Alfentanil miosis could detect 50% to 70% inhibition of CYP3A activity, but was less sensitive than plasma AUCs. Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 56-61 16172184-14 2005 Further refinements are needed to increase the sensitivity of alfentanil miosis for detecting small CYP3A changes. Alfentanil 62-72 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 100-105 15731592-2 2005 Alfentanil undergoes extensive metabolism by cytochrome P4503A4 (CYP3A4). Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 45-63 15731592-2 2005 Alfentanil undergoes extensive metabolism by cytochrome P4503A4 (CYP3A4). Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 65-71 15731592-6 2005 METHODS: Alfentanil metabolism to noralfentanil and N-phenylpropionamide was determined in microsomes from two groups of human livers, characterized for CYP3A4 and CYP3A5 protein content: low CYP3A5 (2.0-5.2% of total CYP3A, n = 10) and high CYP3A5 (46-76% of total CYP3A, n = 10). Alfentanil 9-19 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 153-159 15731592-8 2005 The effects of the CYP3A inhibitors troleandomycin and ketoconazole, the latter being more potent toward CYP3A4, on alfentanil metabolism were also determined. Alfentanil 116-126 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 105-111 15731592-17 2005 Therefore, alfentanil is metabolized by human liver microsomal CYP3A5 in addition to CYP3A4, and pharmacogenetic variability in CYP3A5 expression significantly influences human liver alfentanil metabolism in vitro. Alfentanil 11-21 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 85-91 15557344-0 2005 Metabolism of alfentanil by cytochrome p4503a (cyp3a) enzymes. Alfentanil 14-24 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 47-52 15557344-1 2005 The synthetic opioid alfentanil is an analgesic and an in vivo probe for hepatic and first-pass CYP3A activity. Alfentanil 21-31 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 96-101 15557344-2 2005 Alfentanil is a particularly useful CYP3A probe because pupil diameter change is a surrogate for plasma concentrations, thereby affording noninvasive assessment of CYP3A. Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 36-41 15557344-2 2005 Alfentanil is a particularly useful CYP3A probe because pupil diameter change is a surrogate for plasma concentrations, thereby affording noninvasive assessment of CYP3A. Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 164-169 15557344-3 2005 Alfentanil undergoes extensive CYP3A4 metabolism via two major pathways, forming noralfentanil and N-phenylpropionamide. Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-37 15557344-10 2005 These results demonstrate that alfentanil is a substrate for CYP3A5 in addition to CYP3A4, and the effects of the CYP3A inhibitors troleandomycin and ketoconazole are CYP3A enzyme-selective. Alfentanil 31-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-89 15557344-10 2005 These results demonstrate that alfentanil is a substrate for CYP3A5 in addition to CYP3A4, and the effects of the CYP3A inhibitors troleandomycin and ketoconazole are CYP3A enzyme-selective. Alfentanil 31-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 61-66 15557344-10 2005 These results demonstrate that alfentanil is a substrate for CYP3A5 in addition to CYP3A4, and the effects of the CYP3A inhibitors troleandomycin and ketoconazole are CYP3A enzyme-selective. Alfentanil 31-41 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-88 15557344-11 2005 Alfentanil is one of the few CYP3A substrates that is metabolized in vitro as avidly by both CYP3A4 and 3A5. Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 29-34 15557344-11 2005 Alfentanil is one of the few CYP3A substrates that is metabolized in vitro as avidly by both CYP3A4 and 3A5. Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 93-99 15601808-0 2005 Evaluation of first-pass cytochrome P4503A (CYP3A) and P-glycoprotein activities using alfentanil and fexofenadine in combination. Alfentanil 87-97 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-49 15601808-4 2005 Alfentanil is a selective CYP3A probe but not a P-gp substrate. Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 26-31 15601808-6 2005 This investigation tested the hypothesis that alfentanil and fexofenadine could be administered in combination to probe first-pass CYP3A and P-gp activities in humans. Alfentanil 46-56 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 131-136 15601808-17 2005 Alfentanil and fexofenadine in combination appear to be a useful probe for evaluating both first-pass CYP3A and P-gp activities in humans. Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 102-107 12657846-20 2003 CYP3A inhibition decreases alfentanil clearance more than fentanyl clearance, confirming that the extraction ratio influences the consequence of altered hepatic drug metabolism. Alfentanil 27-37 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 12621385-0 2003 Disposition and miotic effects of oral alfentanil: a potential noninvasive probe for first-pass cytochrome P4503A activity. Alfentanil 39-49 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 96-102 12621385-1 2003 BACKGROUND AND OBJECTIVES: Systemic clearance of the opioid alfentanil after intravenous administration is an excellent in vivo probe for hepatic cytochrome P4503A (CYP3A) activity and drug interactions. Alfentanil 60-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 146-152 12621385-1 2003 BACKGROUND AND OBJECTIVES: Systemic clearance of the opioid alfentanil after intravenous administration is an excellent in vivo probe for hepatic cytochrome P4503A (CYP3A) activity and drug interactions. Alfentanil 60-70 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 165-170 12621385-2 2003 Alfentanil effect (miosis) is a surrogate for plasma alfentanil concentrations, and alfentanil effect kinetics may be a suitable noninvasive probe for hepatic CYP3A. Alfentanil 84-94 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 159-164 12621385-3 2003 Oral alfentanil might be a probe for first-pass CYP3A activity; however, it is not used clinically, and oral alfentanil disposition is unknown. Alfentanil 5-15 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 48-53 12621385-16 2003 Oral alfentanil may be a suitable probe for first-pass CYP3A activity. Alfentanil 5-15 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 55-60 12621385-19 2003 Further studies are warranted to determine whether oral alfentanil and alfentanil effect kinetics may be a suitable noninvasive in vivo probe for first-pass CYP3A activity. Alfentanil 56-66 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 157-162 12621385-19 2003 Further studies are warranted to determine whether oral alfentanil and alfentanil effect kinetics may be a suitable noninvasive in vivo probe for first-pass CYP3A activity. Alfentanil 71-81 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 157-162 11753266-0 2001 A pilot evaluation of alfentanil-induced miosis as a noninvasive probe for hepatic cytochrome P450 3A4 (CYP3A4) activity in humans. Alfentanil 22-32 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 83-102 11753266-0 2001 A pilot evaluation of alfentanil-induced miosis as a noninvasive probe for hepatic cytochrome P450 3A4 (CYP3A4) activity in humans. Alfentanil 22-32 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 104-110 11753266-1 2001 OBJECTIVE: The opioid alfentanil is a CYP3A4 substrate whose plasma clearance depends exclusively on hepatic CYP3A4 activity. Alfentanil 22-32 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-44 11753266-1 2001 OBJECTIVE: The opioid alfentanil is a CYP3A4 substrate whose plasma clearance depends exclusively on hepatic CYP3A4 activity. Alfentanil 22-32 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 109-115 11753266-2 2001 Alfentanil clearance is an excellent in vivo probe for hepatic CYP3A4 activity and drug interactions in humans. Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 63-69 11753266-11 2001 RESULTS: Compared with control, CYP3A4 induction and inhibition significantly altered the clearances of alfentanil (2.8 +/- 1.4, 5.3 +/- 1.0, and 0.42 +/- 0.1 ml/kg/min, respectively; P <.05 versus control) and midazolam. Alfentanil 104-114 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 32-38 11753266-13 2001 Alfentanil-dependent miosis was significantly altered by CYP3A4 modulation, and log(diameter(0) - diameter(t)) versus time curves resembled alfentanil plasma disposition. Alfentanil 0-10 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 57-63 7995002-4 1994 To overcome the variable of route of administration, the aim of this study was to determine whether the elimination of two intravenously administered CYP3A4 substrates (alfentanil and erythromycin) correlate. Alfentanil 169-179 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 150-156 10392320-0 1999 Intraindividual variability in male hepatic CYP3A4 activity assessed by alfentanil and midazolam clearance. Alfentanil 72-82 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 44-50 8968170-14 1996 CYP3A-mediated drug interactions should be considered as confounders when recovery from anesthesia with midazolam and alfentanil infusions is assessed. Alfentanil 118-128 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-5 8712396-2 1996 We have previously shown that cytochrome P-450 3A4 (CYP3A4) contributes significantly to human liver microsomal alfentanil oxidation. Alfentanil 112-122 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 30-50 8712396-2 1996 We have previously shown that cytochrome P-450 3A4 (CYP3A4) contributes significantly to human liver microsomal alfentanil oxidation. Alfentanil 112-122 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 52-58 9232131-0 1997 Assessment of cytochrome P450 3A4 activity during the menstrual cycle using alfentanil as a noninvasive probe. Alfentanil 76-86 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 14-33 9232132-0 1997 The role of cytochrome P450 3A4 in alfentanil clearance. Alfentanil 35-45 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 12-31 9232132-4 1997 Cytochrome P450 3A4 was previously shown to be the predominant P450 isoform responsible for human liver microsomal alfentanil metabolism in vitro. Alfentanil 115-125 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 0-19 9264313-3 1997 Differences in pharmacokinetic parameters of alfentanil have previously been associated with the wide distribution of CYP3A4, the only known hepatic cytochrome P450 monooxygenase (CYP) involved in the conversion of alfentanil to noralfentanil. Alfentanil 45-55 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 118-124 9264313-3 1997 Differences in pharmacokinetic parameters of alfentanil have previously been associated with the wide distribution of CYP3A4, the only known hepatic cytochrome P450 monooxygenase (CYP) involved in the conversion of alfentanil to noralfentanil. Alfentanil 215-225 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 118-124 9264313-5 1997 Microsomes prepared from different human liver samples were compared for their abilities to metabolize fentanyl, sufentanil and alfentanil, and it was found that disappearance of the three substrates was well correlated with immunoreactive CYP3A4 contents but not with other CYPs, including CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2D6 and CYP2E1. Alfentanil 128-138 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 240-246 8484504-0 1993 Human alfentanil metabolism by cytochrome P450 3A3/4. Alfentanil 6-16 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 31-52 8484504-6 1993 Human liver microsomal alfentanil metabolism was correlated strongly with the content of cytochrome P450 3A3/4 (r = 0.85, P < 0.005), measured by Western blot analysis with a rabbit anti-human P450 3A3/4 probe. Alfentanil 23-33 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 89-110 1519785-0 1992 Identification of the pharmacogenetic determinants of alfentanil metabolism: cytochrome P-450 3A4. Alfentanil 54-64 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 77-97