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Genomes and Genes | David J GreenblattSummaryAffiliation: Tufts University Country: USA Publications
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Interaction of flurbiprofen with cranberry juice, grape juice, tea, and fluconazole: in vitro and clinical studiesDavid J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and Tufts New England Medical Center, Boston, Mass, USA
Clin Pharmacol Ther 79:125-33. 2006..To address this question, the effect of cranberry juice and other beverages on CYP2C9 activity was evaluated in vitro and in vivo...- Time course of recovery of cytochrome p450 3A function after single doses of grapefruit juiceDavid J Greenblatt
Department of Pharmaacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
Clin Pharmacol Ther 74:121-9. 2003..The time course of recovery from CYP3A inhibition after a single exposure to grapefruit juice is not clearly established... - Pomegranate juice does not impair clearance of oral or intravenous midazolam, a probe for cytochrome P450-3A activity: comparison with grapefruit juiceDora Farkas
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
J Clin Pharmacol 47:286-94. 2007..3 and 1.5, respectively, and reduced oral clearance to 72% of control values. Thus, PJ does not alter clearance of intravenous or oral midazolam, whereas GFJ impairs clearance and elevates plasma levels of oral midazolam... 
Pharmacokinetic properties of zolpidem in elderly and young adults: possible modulation by testosterone in menJoel O Olubodun
Department of Pharmacology and Experimental Therapeutics and the Jean Mayer USDA Human Nutrition Research Center on Ageing, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
Br J Clin Pharmacol 56:297-304. 2003..Our clinical and in vitro data both suggest that reduced free serum testosterone may have a modulatory role in age-dependent changes in zolpidem pharmacokinetics in men...- Age and gender effects on the pharmacokinetics and pharmacodynamics of triazolam, a cytochrome P450 3A substrateDavid J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
Clin Pharmacol Ther 76:467-79. 2004..Although the findings are consistent with reduced clearance of triazolam in elderly men, individual variability was large and was not explained by identifiable demographic or environmental factors... - Ginkgo biloba does not alter clearance of flurbiprofen, a cytochrome P450-2C9 substrateDavid J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
J Clin Pharmacol 46:214-21. 2006..These amounts were apparently too low to inhibit CYP2C9 function in vivo. The results confirm previous controlled clinical studies showing no effect of ginkgo on the kinetics or dynamics of warfarin... - Effect of extended exposure to grapefruit juice on cytochrome P450 3A activity in humans: comparison with ritonavirKerry E Culm-Merdek
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, and Tufts-New England Medical Center, Boston, Mass 02111, USA
Clin Pharmacol Ther 79:243-54. 2006..Ritonavir greatly inhibits both enteric and hepatic CYP3A. With extended exposure to ritonavir, inhibition is the predominant effect, and recovery to baseline is nearly complete 3 days after ritonavir discontinuation... - Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavirJames L Weemhoff
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
J Pharm Pharmacol 55:381-6. 2003..Although lopinavir is less potent than ritonavir as an inhibitor of CYP3A, lopinavir is nonetheless likely to contribute to net CYP3A inhibition in-vivo during treatment with the lopinavir-ritonavir combination... - Effect of age on in vitro triazolam biotransformation in male human liver microsomesKiran C Patki
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
J Pharmacol Exp Ther 308:874-9. 2004..Reduced V(max) and Cl(int) for TRZ hydroxylation and CYP3A protein in livers from elderly men suggest reduced CYP3A gene expression in this group... - UDP glucuronosyltransferase (UGT) 1A6 pharmacogenetics: I. Identification of polymorphisms in the 5'-regulatory and exon 1 regions, and association with human liver UGT1A6 gene expression and glucuronidationSoundararajan Krishnaswamy
Molecular Pharmacogenetics Laboratory, Department of Pharmacology and Experimental Therapeutics, Tufts University, Boston, MA 02111, USA
J Pharmacol Exp Ther 313:1331-9. 2005..In conclusion, although the identified UGT1A6 polymorphisms did not explain the observed glucuronidation variability, there does seem to be a significant role for environmental factors associated with alcohol consumption... - The effect of chronic lorazepam administration in aging miceJeanne M Fahey
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and the Division of Clinical Pharmacology, Tufts New England Medical Center, Boston, MA 02111, USA
Brain Res 1118:13-24. 2006.... - Age-related differences in CYP3A expression and activity in the rat liver, intestine, and kidneyJill S Warrington
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
J Pharmacol Exp Ther 309:720-9. 2004..In addition, changes in testosterone levels and NADPH reductase expression may contribute to age-related differences in hepatic CYP3A activity... - Pharmacogenetic determinants of interindividual variability in bupropion hydroxylation by cytochrome P450 2B6 in human liver microsomesLeah M Hesse
Clinical Pharmacology Laboratory, Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
Pharmacogenetics 14:225-38. 2004..In conclusion, the results of this study indicate that interindividual variability in bupropion hydroxylation is a consequence of interactions between environmental and genetic influences on CYP2B6 gene function... - Short-term exposure to low-dose ritonavir impairs clearance and enhances adverse effects of trazodoneDavid J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Tufts-New England Medical Center, Boston MA, 02111, USA
J Clin Pharmacol 43:414-22. 2003..Thus short-term low-dose administration of ritonavir impairs oral clearance of trazodone and increases the occurrence of adverse reactions. The findings are consistent with impairment of CYP3A-mediated trazodone metabolism by ritonavir... - Ethanol inhibits in-vitro metabolism of nifedipine, triazolam and testosterone in human liver microsomesKiran C Patki
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Tufts-New England Medical Center, Boston, MA 02111, USA
J Pharm Pharmacol 56:963-6. 2004..The IC50 values obtained were lower than clinically relevant blood alcohol concentrations. In conclusion, ethanol is an inhibitor of human CYP3A metabolism and may contribute to clinically important interactions... - Kinetics and dynamics of intravenous adinazolam, N-desmethyl adinazolam, and alprazolam in healthy volunteersKarthik Venkatakrishnan
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
J Clin Pharmacol 45:529-37. 2005..Collectively, these results indicate that the benzodiazepine-like effects occurring after adinazolam administration are mediated by mainly NDMAD... - Factors influencing midazolam hydroxylation activity in human liver microsomesPing He
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
Drug Metab Dispos 34:1198-207. 2006..In conclusion, the investigated genetic factors did not contribute substantially to the large interindividual variability in midazolam hydroxylation, although alcohol consumption has a discernable but modest influence... 
Mechanism of cytochrome P450-3A inhibition by ketoconazoleDavid J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and Tufts Medical Center, 136 Harrison Ave, Boston, MA 02111, USA
J Pharm Pharmacol 63:214-21. 2011..Ketoconazole is extensively used as an index inhibitor of cytochrome P450-3A (CYP3A) activity in vitro and in vivo, but the mechanism of ketoconazole inhibition of CYP3A still is not clearly established...- Genotype-phenotype associations of cytochrome P450 3A4 and 3A5 polymorphism with midazolam clearance in vivoPing He
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Ave, Boston, MA 02111, USA
Clin Pharmacol Ther 77:373-87. 2005..012). In conclusion, these results indicate that the genetic variants identified so far in the CYP3A4 and CYP3A5 genes have only a limited impact on CYP3A-mediated drug metabolism in vivo... - UDP glucuronosyltransferase (UGT) 1A6 pharmacogenetics: II. Functional impact of the three most common nonsynonymous UGT1A6 polymorphisms (S7A, T181A, and R184S)Soundararajan Krishnaswamy
Molecular Pharmacogenetics Laboratory, Department of Pharmacology and Experimental Therapeutics, Tufts University, Boston, MA 02111, USA
J Pharmacol Exp Ther 313:1340-6. 2005.... - Fluvoxamine impairs single-dose caffeine clearance without altering caffeine pharmacodynamicsKerry E Culm-Merdek
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and Tufts-New England Medical Center, 136 Harrison Avenue, Boston, MA 02111, USA
Br J Clin Pharmacol 60:486-93. 2005..However, this study does not rule out possible adverse effects due to extensive accumulation of caffeine with daily ingestion in fluvoxamine-treated individuals... - Inhibition of oral midazolam clearance by boosting doses of ritonavir, and by 4,4-dimethyl-benziso-(2H)-selenazine (ALT-2074), an experimental catalytic mimic of glutathione oxidaseDavid J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
Br J Clin Pharmacol 68:920-7. 2009..The viral protease inhibitor ritonavir is known to inhibit clearance of intravenous midazolam. * ALT-2074, a catalytic mimic of glutathione oxidase, inhibits human cytochrome P450 3A (CYP3A) isoforms in vitro... - In vitro, pharmacokinetic, and pharmacodynamic interactions of ketoconazole and midazolam in the ratTsutomu Kotegawa
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Tufts-New England Medical Center, 136 Harrison Avenue, Boston, MA 02111, USA
J Pharmacol Exp Ther 302:1228-37. 2002..Although the in vitro and in vivo characteristics of midazolam in rats incompletely parallel those in humans, the experimental model can be used to assess aspects of drug interactions having potential clinical importance... - Role of NADPH-cytochrome P450 reductase and cytochrome-b5/NADH-b5 reductase in variability of CYP3A activity in human liver microsomesLu Gan
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, Massachusetts 02111, USA
Drug Metab Dispos 37:90-6. 2009..Consequently, while aging is associated with decreased CPR and b(5) expression in human livers, this effect does not contribute to CYP3A variability... - Ritonavir greatly impairs CYP3A activity in HIV infection with chronic viral hepatitisTamsin A Knox
Nutrition Infection Division, Department of Public Health and Family Medicine, Tufts University School of Medicine, Boston, MA 02111, USA
J Acquir Immune Defic Syndr 49:358-68. 2008..Ritonavir is a powerful inhibitor of cytochrome P450 3A (CYP3A) that metabolizes many antiretrovirals. We examined the effect of ritonavir and of chronic viral hepatitis (CVH) status on CYP3A activity... - Phenacetin and chlorzoxazone biotransformation in aging male Fischer 344 ratsJill S Warrington
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
J Pharm Pharmacol 56:819-25. 2004..Also, the relative specificity of the index substrates phenacetin (for CYP1A2) and chlorzoxazone (for CYP2E1) in man appears not to be applicable in rats... - UDP-glucuronosyltransferase (UGT) 2B15 pharmacogenetics: UGT2B15 D85Y genotype and gender are major determinants of oxazepam glucuronidation by human liverMichael H Court
Comparative and Molecular Pharmacogenetics Laboratory, Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts, USA
J Pharmacol Exp Ther 310:656-65. 2004..05). In conclusion, gender and D85Y genotype are identified as major determinants of S-oxazepam glucuronidation by human liver and may explain in part polymorphic oxazepam glucuronidation by human subjects... - Rapid assessment of P-glycoprotein inhibition and induction in vitroMichael D Perloff
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, Massachusetts 02111, USA
Pharm Res 20:1177-83. 2003..This assay has the potential to predict P-gp-mediated alterations in intestinal absorption of drugs... - The effect of age on sildenafil biotransformation in rat and mouse liver microsomesJill S Warrington
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
Drug Metab Dispos 31:1306-9. 2003..Although the role of specific CYP enzymes and the clearance values for this reaction may differ among species, age-related changes in these rodent models are consistent with the reduced clearance of SIL observed in human studies... - Dynamics and kinetics of a modified-release formulation of zolpidem: comparison with immediate-release standard zolpidem and placeboDavid J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
J Clin Pharmacol 46:1469-80. 2006..001). Thus, MR zolpidem produces sustained plasma levels compared to IR, with resulting enhancement of pharmacodynamic effects in the 3- to 6-hour post-dosage interval... - Effect of zolpidem on human cytochrome P450 activity, and on transport mediated by P-glycoproteinLisa L von Moltke
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
Biopharm Drug Dispos 23:361-7. 2002..The findings indicate that zolpidem is very unlikely to cause clinical drug interactions attributable to impairment of CYP activity or P-gp mediated transport... - In vitro interactions of water-soluble garlic components with human cytochromes p450David J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and Tufts New England Medical Center, Boston, MA, USA
J Nutr 136:806S-809S. 2006..However available clinical evidence does not indicate CYP3A inhibition in vivo. The findings suggest that drug interactions involving inhibition of CYP3A enzymes by aged garlic extract are very unlikely... - Interaction of triazolam and ketoconazole in P-glycoprotein-deficient miceLisa L von Moltke
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
Drug Metab Dispos 32:800-4. 2004..KET impairs clearance of TRZ but does not increase tissue uptake. However, KET itself may be a substrate for efflux transport at the blood-brain barrier... - The influence of age and sex on the clearance of cytochrome P450 3A substratesMonette M Cotreau
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
Clin Pharmacokinet 44:33-60. 2005..In such cases, women primarily have higher clearance than men... - Atazanavir: effects on P-glycoprotein transport and CYP3A metabolism in vitroElke S Perloff
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
Drug Metab Dispos 33:764-70. 2005..D. 0.13) and 5.7 microM (S.D. 4.1), respectively. Thus, atazanavir is an inhibitor and inducer of P-gp as well as a potent inhibitor of CYP3A in vitro, suggesting a potential for atazanavir to cause drug-drug interactions in vivo... - Evidence for oxazepam as an in vivo probe of UGT2B15: oxazepam clearance is reduced by UGT2B15 D85Y polymorphism but unaffected by UGT2B17 deletionXi He
Laboratory of Comparative and Molecular Pharmacogenomics and Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
Br J Clin Pharmacol 68:721-30. 2009..We also determined the possible influence of a common deletion polymorphism in the gene encoding UGT2B17, which shows substantial substrate specificity overlap with UGT2B15... - Pharmocokinetics and pharmacodynamics of single-dose triazolam: electroencephalography compared with the Digit-Symbol Substitution TestDavid J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and Tufts New England Medical Center, Boston, MA 02111, USA
Br J Clin Pharmacol 60:244-8. 2005.... - Gender has a small but statistically significant effect on clearance of CYP3A substrate drugsDavid J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Ave, Boston, MA 02111, USA
J Clin Pharmacol 48:1350-5. 2008..Thus gender has a small and statistically significant, although most likely clinically unimportant, influence on CYP3A phenotype for substrates not transported by P-gp... - Age and gender effects on the pharmacokinetics and pharmacodynamics of ramelteon, a hypnotic agent acting via melatonin receptors MT1 and MT2David J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and Tufts New England Medical Center, 136 Harrison Avenue, Boston, MA 02111, USA
J Clin Pharmacol 47:485-96. 2007..The usually recommended clinical dose of ramelteon (8 mg) does not require modification based on age or gender... - Human pregnane X receptor: genetic polymorphisms, alternative mRNA splice variants, and cytochrome P450 3A metabolic activityPing He
Division of Clinical Pharmacology, Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
J Clin Pharmacol 46:1356-69. 2006..In conclusion, several hPXR polymorphisms have been identified that may have predictive value for oral midazolam clearance, particularly in African Americans... - Ritonavir has minimal impact on the pharmacokinetic disposition of a single dose of bupropion administered to human volunteersLeah M Hesse
Molecular Pharmacogenetics Laboratory, Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
J Clin Pharmacol 46:567-76. 2006..These findings indicate that short-term ritonavir dosing has only minimal impact on the pharmacokinetic disposition of a single dose of bupropion in healthy volunteers... - Apparent active transport of MDMA is not mediated by P-glycoprotein: a comparison with MDCK and Caco-2 monolayersKirk M Bertelsen
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
Biopharm Drug Dispos 27:219-27. 2006.... - In vitro metabolism of midazolam, triazolam, nifedipine, and testosterone by human liver microsomes and recombinant cytochromes p450: role of cyp3a4 and cyp3a5Kiran C Patki
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Ave, Boston, MA 02111
Drug Metab Dispos 31:938-44. 2003..Because the inhibitory potency of ketoconazole in rCYP3A5 is substantially less than in rCYP3A4 and HLMs, CYP3A5 is probably less important than CYP3A4 in drug-drug interactions involving ketoconazole and CYP3A substrates... - Validation of serotonin (5-hydroxtryptamine) as an in vitro substrate probe for human UDP-glucuronosyltransferase (UGT) 1A6Soundararajan Krishnaswamy
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts 02111, USA
Drug Metab Dispos 31:133-9. 2003..769; P < 0.001) (n = 52). In conclusion, these results indicate that serotonin is a highly selective in vitro probe substrate for human UGT1A6... - Kinetics and EEG effects of midazolam during and after 1-minute, 1-hour, and 3-hour intravenous infusionsDavid J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
J Clin Pharmacol 44:605-11. 2004..Despite the delay in effect onset during the 1-minute midazolam infusion, midazolam infusions in duration of up to 3 hours produce CNS sedation without evidence of tolerance... - Effect of bupropion on CYP2B6 and CYP3A4 catalytic activity, immunoreactive protein and mRNA levels in primary human hepatocytes: comparison with rifampicinLeah M Hesse
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
J Pharm Pharmacol 55:1229-39. 2003..1 fold, while 10 microM bupropion minimally altered CYP2E1 protein (1.2 fold). Overall, results of this study suggest that multiple doses of bupropion are not likely to induce CYP2B6, 3A4 or 2E1 in-vivo in man... - Pharmacokinetic profile of SKP-1041, a modified release formulation of zaleplonDavid J Greenblatt
Program in Pharmacology and Experimental Therapeutics, Department of Molecular Physiology and Pharmacology, Tufts University School of Medicine and Tufts Medical Center, Boston, MA 02111, USA
Biopharm Drug Dispos 32:489-97. 2011..Two investigations aimed to define the pharmacokinetic profile of a modified-release preparation of zaleplon (SKP-1041)... - Inhibition of human cytochromes P450 by components of Ginkgo bilobaLisa L von Moltke
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
J Pharm Pharmacol 56:1039-44. 2004..The clinical importance of these potential inhibitors will depend on their amounts in ginkgo preparations sold to the public, and the extent to which their bioavailability allows them to reach the CYP enzymes in-situ... - Evaluation of 3'-azido-3'-deoxythymidine, morphine, and codeine as probe substrates for UDP-glucuronosyltransferase 2B7 (UGT2B7) in human liver microsomes: specificity and influence of the UGT2B7*2 polymorphismMichael H Court
Comparative and Molecular Pharmacogenetics Laboratory, Tufts University, Boston, MA 02111, USA
Drug Metab Dispos 31:1125-33. 2003..Codeine is not a useful UGT2B7 probe substrate because of significant glucuronidation by UGT2B4. The UGT2B7*2 polymorphism is not a determinant of glucuronidation of AZT, morphine, or codeine in HLMs... - Microsomal protein concentration modifies the apparent inhibitory potency of CYP3A inhibitorsThanh Huu Tran
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and New England Medical Center, Boston, Massachusetts 02111, USA
Drug Metab Dispos 30:1441-5. 2002..The effect can be minimized by use of the lowest possible microsomal protein concentration for in vitro studies of metabolic inhibition... - Induction of P-glycoprotein expression and activity by ritonavir in bovine brain microvessel endothelial cellsMichael D Perloff
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
J Pharm Pharmacol 59:947-53. 2007..Similar findings may occur at the clinical level with prolonged HIV protease inhibitor use, giving insight into the central nervous system as an HIV sanctuary site and eventual development of HIV dementia... - Influence of fruit juices on drug disposition: discrepancies between in vitro and clinical studiesDora Farkas
Tufts University School of Medicine, Department of Pharmacology and Experimental Therapeutics, Boston, MA 02111, USA
Expert Opin Drug Metab Toxicol 4:381-93. 2008..After the discovery of this interaction almost 20 years ago, there have been many reports investigating the effects of fruit juices on drug disposition... - Fexofenadine transport in Caco-2 cells: inhibition with verapamil and ritonavirMichael D Perloff
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
J Clin Pharmacol 42:1269-74. 2002..Thefindings support the use of FXD as an index or probe compound to reflect P-gp activity in vivo... - The effect of age on P-glycoprotein expression and function in the Fischer-344 ratJill S Warrington
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
J Pharmacol Exp Ther 309:730-6. 2004..The converse pattern was observed in the kidney. Thus, age-related changes in P-gp expression and function are likely to be tissue-specific, and these changes may be inversely related to differences in CYP3A expression... - The absence of an interaction between warfarin and cranberry juice: a randomized, double-blind trialJack Ansell
Department of Medicine, Boston Medical Center, Boston University School of Medicine, Boston, MA, USA
J Clin Pharmacol 49:824-30. 2009..Enhanced warfarin anticoagulation attributed to CJ in anecdotal reports may represent a chance temporal association... - Evaluation of 5-hydroxytryptophol and other endogenous serotonin (5-hydroxytryptamine) analogs as substrates for UDP-glucuronosyltransferase 1A6Soundararajan Krishnaswamy
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
Drug Metab Dispos 32:862-9. 2004..In conclusion, these results indicate that human UGT1A6 plays a predominant role in the glucuronidation of 5-hydroxytryptophol and N-acetylserotonin, whereas 6-hydroxymelatonin is not a substrate for this enzyme... - Evaluation of Supermix as an in vitro model of human liver microsomal drug metabolismKarthik Venkatakrishnan
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
Biopharm Drug Dispos 23:183-90. 2002..These factors should be considered when this formulation is used as an in vitro model in human liver microsomal drug metabolism studies... - Sources of variability in ketoconazole inhibition of human cytochrome P450 3A in vitroDavid J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and Tufts Medical Center, Boston, MA, USA
Xenobiotica 40:713-20. 2010.... - Interactions of tamoxifen, N-desmethyltamoxifen and 4-hydroxytamoxifen with P-glycoprotein and CYP3ATanios S Bekaii-Saab
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
Biopharm Drug Dispos 25:283-9. 2004..Tamoxifen, and possibly its metabolites, may have the potential to cause drug interactions by inhibiting both drug transport and metabolism. This possibility requires further evaluation in clinical studies... - Stereoselective conjugation of oxazepam by human UDP-glucuronosyltransferases (UGTs): S-oxazepam is glucuronidated by UGT2B15, while R-oxazepam is glucuronidated by UGT2B7 and UGT1A9Michael H Court
Comparative and Molecular Pharmacogenetics Laboratory, Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts 02111, USA
Drug Metab Dispos 30:1257-65. 2002..Allelic variation associated with the UGT2B15 gene may explain polymorphic S-oxazepam glucuronidation in humans... - Apparent mechanism-based inhibition of human CYP2D6 in vitro by paroxetine: comparison with fluoxetine and quinidineKirk M Bertelsen
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts 02111, USA
Drug Metab Dispos 31:289-93. 2003..These data are consistent with mechanism-based inhibition of CYP2D6 by paroxetine but not by quinidine or fluoxetine... - Clinically important drug interactions with zopiclone, zolpidem and zaleplonLeah M Hesse
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts 02111, USA
CNS Drugs 17:513-32. 2003.... - Analysis of drug interactions involving fruit beverages and organic anion-transporting polypeptidesDavid J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Ave, Boston, MA 02111, USA
J Clin Pharmacol 49:1403-7. 2009..Beyond these two examples, other meaningful drug interactions with fruit beverages via OATP inhibition are not established at the present time... - In vitro biotransformation of sildenafil (Viagra) in the male rat: the role of CYP2C11Jill S Warrington
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and Tufts-New England Medical Center, Boston, MA 02111, USA
Drug Metab Dispos 30:655-7. 2002..P450 isoforms mediating sildenafil biotransformation differ substantially between humans and the male rat, thereby limiting the applicability of this species as a model for sildenafil metabolism and drug interactions in humans... - Zolpidem pharmacokinetic properties in young females: influence of smoking and oral contraceptive useJoel O Olubodun
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Tufts-New England Medical Center, Boston, MA 02111
J Clin Pharmacol 42:1142-6. 2002..In any case, the differences were quantitatively small and not likely to be of clinical importance... - Human cytochromes mediating gepirone biotransformation at low substrate concentrationsDavid J Greenblatt
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Tufts New England Medical Center, Boston MA 02111, USA
Biopharm Drug Dispos 24:87-94. 2003..CYP2D6 would account for less than 5% of net clearance. The findings are consistent with previous in vitro studies of gepirone using higher substrate concentrations... - The effect of grapefruit juice on drug dispositionMichael J Hanley
Tufts University School of Medicine, Program in Pharmacology and Experimental Therapeutics, 136 Harrison Avenue, Boston, MA 02111, USA
Expert Opin Drug Metab Toxicol 7:267-86. 2011..The number of drugs shown to interact with GFJ in vitro is far greater than the number of clinically relevant GFJ-drug interactions. For the majority of patients, complete avoidance of GFJ is unwarranted... - Acute zolpidem administration produces pharmacodynamic and receptor occupancy changes at similar dosesJeanne M Fahey
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and the Division of Clinical Pharmacology, Tufts New England Medical Center, 136 Harrison Avenue, Boston, MA 02111, USA
Pharmacol Biochem Behav 83:21-7. 2006..In addition, zolpidem had no significant effect on the affinity of the benzodiazepine receptor for [3H]flunitrazepam, but did decrease the density of receptor binding sites... - Effect of 7-day exposure to midazolam on electroencephalogram pharmacodynamics in rats: a model to study multiple pharmacokinetic-pharmacodynamic relationships in individual animalsBart E Laurijssens
Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
J Pharm Pharmacol 54:77-86. 2002..A modest degree of tolerance to midazolam was found with this paradigm, the effect only being evident after correction for the fraction unbound of midazolam... - UGT1A1 polymorphisms are important determinants of dietary carcinogen detoxification in the liverHugo Girard
Laboratory of Pharmacogenomics, Oncology and Molecular Endocrinology Research Center, CHUL Research Center and Faculty of Pharmacy, Laval University, 2705 Boulevard Laurier, , Canada
Hepatology 42:448-57. 2005..In conclusion, UGT1A1 polymorphisms modulate the hepatic metabolism of the carcinogenic intermediate of PhIP and may determine the level of its exposure and potentially influence the risk of cancer through dietary exposure to HCAs... - Identification of common polymorphisms in the promoter of the UGT1A9 gene: evidence that UGT1A9 protein and activity levels are strongly genetically controlled in the liverHugo Girard
Canada Research Chair in Pharmacogenomics, Laboratory of Pharmacogenomics, Oncology and Molecular Endocrinology Research Center, CHUL Research Center and Faculty of Pharmacy, Laval University, Quebec, Canada
Pharmacogenetics 14:501-15. 2004..The great interindividual variability of UGT1A9-mediated glucuronidation remains poorly explained, while evidence for its genetic origin exists... - Limited sampling strategy to predict AUC of the CYP3A phenotyping probe midazolam in adults: application to various assay techniquesJooran S Kim
Clinical Pharmacology Research Center, Bassett Healthcare, Cooperstown, New York 13326-1394, USA
J Clin Pharmacol 42:376-82. 2002..A limited sampling strategy is more convenient and cost-effective than standard sampling strategies and is applicable to more than one assay technique... - The novel UGT1A9 intronic I399 polymorphism appears as a predictor of 7-ethyl-10-hydroxycamptothecin glucuronidation levels in the liverHugo Girard
Laboratory of Pharmacogenomics, , Quebec, QC, Canada G1V 4G2
Drug Metab Dispos 34:1220-8. 2006.... - Effects of acute lorazepam administration on aminergic activity in normal elderly subjects: relationship to performance effects and apolipoprotein genotypeNunzio Pomara
Geriatric Psychiatry Program, Nathan Kline Institute for Psychiatric Research, Orangeburg, New York 10962, USA
Neurochem Res 29:1391-8. 2004..The epsilon4 allele may modulate the effect of lorazepam on p5-HIAA, but further studies are needed to confirm this finding and elucidate its possible significance... - Interdose elevation in plasma cortisol during chronic treatment with alprazolam but not lorazepam in the elderlyNunzio Pomara
Geriatric Psychiatry Program, Nathan S Kline Institute for Psychiatric Research, Orangeburg, NY 10962, USA
Neuropsychopharmacology 29:605-11. 2004..If confirmed, this effect may contribute to an increased risk for drug escalation and dependence during chronic alprazolam treatment... - Cortisol response to diazepam: its relationship to age, dose, duration of treatment, and presence of generalized anxiety disorderNunzio Pomara
Nathan Kline Institute for Psychiatric Research, 140 Old Orangeburg Road, Building 35, Orangeburg, NY 10962, USA
Psychopharmacology (Berl) 178:1-8. 2005..However, the effects of chronic diazepam treatment on cortisol have been less studied, and the relationship to age, anxiety, duration of treatment, and dose are not well understood... - Drug metabolism and drug interactions: application and clinical value of in vitro modelsKarthik Venkatakrishnan
Department of Pharmacokinetics, Pharmacodynamics, and Drug Metabolism, Pfizer Global Research and Development, Groton, CT, USA
Curr Drug Metab 4:423-59. 2003.... - Role of CYP3A and CYP2E1 in alcohol-mediated increases in acetaminophen hepatotoxicity: comparison of wild-type and Cyp2e1(-/-) miceKristina K Wolf
Department of Pharmacology and Toxicology, Dartmouth Medical School, Hanover, New Hampshire, USA
Drug Metab Dispos 35:1223-31. 2007..In conclusion, these findings suggest that both CYP3A and CYP2E1 contribute to APAP hepatotoxicity in alcohol-treated mice... - Dose-dependent retrograde facilitation of verbal memory in healthy elderly after acute oral lorazepam administrationNunzio Pomara
Geriatric Psychiatry Program, Nathan S Kline Institute, 140 Old Orangeburg Rd Bldg 35, Orangeburg, NY 10962, USA
Psychopharmacology (Berl) 185:487-94. 2006.... - Apolipoprotein E epsilon4 allele and lorazepam effects on memory in high-functioning older adultsNunzio Pomara
Geriatric Psychiatry Program, Nathan S Kline Institute for Psychiatric Research, Orangeburg, NY 10962, USA
Arch Gen Psychiatry 62:209-16. 2005..The apolipoprotein E (APOE) epsilon4 allele has been implicated as a significant risk factor in the development of late-onset Alzheimer disease, but the evidence of cognitive sequelae in healthy individuals has been mixed... - Baseline plasma GABA: its relationship to the adverse effects of acute lorazepam administration on cognition in the elderlyNunzio Pomara
Nathan Kline Institute for Psychiatric Research, Orangeburg, NY 10962, USA
Neurochem Res 29:2311-5. 2004..Plasma GABA concentration does not appear to be a useful marker of susceptibility to benzodiazepine-induced cognitive toxicity in the elderly. Other approaches to estimating central GABA activity should be pursued...