D J Greenblatt

Summary

Affiliation: Tufts University
Country: USA

Publications

  1. ncbi In vitro biotransformation of sildenafil (Viagra) in the male rat: the role of CYP2C11
    Jill 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
  2. ncbi Age and gender effects on the pharmacokinetics and pharmacodynamics of triazolam, a cytochrome P450 3A substrate
    David J Greenblatt
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
    Clin Pharmacol Ther 76:467-79. 2004
  3. doi Mechanism-based inhibition of human cytochrome P450-3A activity by grapefruit hybrids having low furanocoumarin content
    David J Greenblatt
    Sackler 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
    Xenobiotica 42:1163-9. 2012
  4. doi Comparison of pharmacokinetic profiles of zolpidem buffered sublingual tablet and zolpidem oral immediate-release tablet: results from a single-center, single-dose, randomized, open-label crossover study in healthy adults
    David J Greenblatt
    Department of Molecular Physiology and Pharmacology, Tufts University School of Medicine, Boston, MA 02111, USA
    Clin Ther 35:604-11. 2013
  5. doi Pharmacokinetic evaluation of eszopiclone: clinical and therapeutic implications
    David J Greenblatt
    Tufts University School of Medicine, Tufts Medical Center, Department of Molecular Physiology and Pharmacology, Sackler Program in Pharmacology and Experimental Therapeutics, 136 Harrison Avenue, Boston, MA 02111, USA
    Expert Opin Drug Metab Toxicol 8:1609-18. 2012
  6. pmc Pharmacokinetics of high-dose oral thiamine hydrochloride in healthy subjects
    Howard A Smithline
    Department of Emergency Medicine, Tufts University School of Medicine and Baystate Medical Center, Springfield, MA, USA
    BMC Clin Pharmacol 12:4. 2012
  7. doi Zolpidem for insomnia
    David J Greenblatt
    Tufts University School of Medicine, Department of Molecular Physiology and Pharmacology, 136 Harrison Avenue, Boston, MA 02111, USA
    Expert Opin Pharmacother 13:879-93. 2012
  8. doi Sources of variability in ketoconazole inhibition of human cytochrome P450 3A in vitro
    David 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
  9. doi Gender has a small but statistically significant effect on clearance of CYP3A substrate drugs
    David 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
  10. ncbi Time course of recovery of cytochrome p450 3A function after single doses of grapefruit juice
    David J Greenblatt
    Department of Pharmaacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
    Clin Pharmacol Ther 74:121-9. 2003

Research Grants

  1. GARLIC PREPARATIONS AND ANTIRETROVIRAL DRUGS
    David Greenblatt; Fiscal Year: 2002
  2. CYP3A Function in Aging AfricanAmericans
    David Greenblatt; Fiscal Year: 2003
  3. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 2003
  4. Metabolic Consequences of HAART: CYP3A and P-gp
    David Greenblatt; Fiscal Year: 2003
  5. HAART Regimens in Substance Abusers
    David Greenblatt; Fiscal Year: 2003
  6. GARLIC PREPARATIONS AND ANTIRETROVIRAL DRUGS
    David Greenblatt; Fiscal Year: 2003
  7. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 2004
  8. CYP3A Function in Aging AfricanAmericans
    David Greenblatt; Fiscal Year: 2004
  9. GARLIC PREPARATIONS AND ANTIRETROVIRAL DRUGS
    David Greenblatt; Fiscal Year: 2004
  10. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 2005

Detail Information

Publications137 found, 100 shown here

  1. ncbi In vitro biotransformation of sildenafil (Viagra) in the male rat: the role of CYP2C11
    Jill 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...
  2. ncbi Age and gender effects on the pharmacokinetics and pharmacodynamics of triazolam, a cytochrome P450 3A substrate
    David 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...
  3. doi Mechanism-based inhibition of human cytochrome P450-3A activity by grapefruit hybrids having low furanocoumarin content
    David J Greenblatt
    Sackler 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
    Xenobiotica 42:1163-9. 2012
    ..Further study is needed to determine how low the FC content needs to be (or how high the IC(50) needs to be) to assure minimal risk of clinical interactions involving GFJ and CYP3A substrate drugs...
  4. doi Comparison of pharmacokinetic profiles of zolpidem buffered sublingual tablet and zolpidem oral immediate-release tablet: results from a single-center, single-dose, randomized, open-label crossover study in healthy adults
    David J Greenblatt
    Department of Molecular Physiology and Pharmacology, Tufts University School of Medicine, Boston, MA 02111, USA
    Clin Ther 35:604-11. 2013
    ..A zolpidem sublingual tablet (ZST) formulation was recently approved by the US Food and Drug Administration to treat middle-of-the-night (MOTN) awakening with difficulty returning to sleep...
  5. doi Pharmacokinetic evaluation of eszopiclone: clinical and therapeutic implications
    David J Greenblatt
    Tufts University School of Medicine, Tufts Medical Center, Department of Molecular Physiology and Pharmacology, Sackler Program in Pharmacology and Experimental Therapeutics, 136 Harrison Avenue, Boston, MA 02111, USA
    Expert Opin Drug Metab Toxicol 8:1609-18. 2012
    ..Eszopiclone is the active S-enantiomer of R,S-zopiclone, and is a cyclopyrrolone hypnotic acting via the GABA-benzodiazepine receptor system. Nearly 6 million prescriptions for eszopiclone are written yearly in the United States...
  6. pmc Pharmacokinetics of high-dose oral thiamine hydrochloride in healthy subjects
    Howard A Smithline
    Department of Emergency Medicine, Tufts University School of Medicine and Baystate Medical Center, Springfield, MA, USA
    BMC Clin Pharmacol 12:4. 2012
    ..The purpose of this study was to determine the pharmacokinetic profile of oral thiamine hydrochloride at 100 mg, 500 mg and 1500 mg doses in healthy subjects...
  7. doi Zolpidem for insomnia
    David J Greenblatt
    Tufts University School of Medicine, Department of Molecular Physiology and Pharmacology, 136 Harrison Avenue, Boston, MA 02111, USA
    Expert Opin Pharmacother 13:879-93. 2012
    ..The imidazopyridine derivative zolpidem , which acts as a benzodiazepine (BZ) receptor agonist, is the most widely prescribed hypnotic drug in the US...
  8. doi Sources of variability in ketoconazole inhibition of human cytochrome P450 3A in vitro
    David 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
    ....
  9. doi Gender has a small but statistically significant effect on clearance of CYP3A substrate drugs
    David 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...
  10. ncbi Time course of recovery of cytochrome p450 3A function after single doses of grapefruit juice
    David 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...
  11. ncbi In vitro metabolism of midazolam, triazolam, nifedipine, and testosterone by human liver microsomes and recombinant cytochromes p450: role of cyp3a4 and cyp3a5
    Kiran 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...
  12. ncbi Alprazolam-ritonavir interaction: implications for product labeling
    D J Greenblatt
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and New England Medical Center, Boston, MA 02111, USA
    Clin Pharmacol Ther 67:335-41. 2000
    ..The viral protease inhibitor ritonavir is of particular concern since it both inhibits and induces the activity of cytochrome P450 3A (CYP3A) isoforms...
  13. ncbi Differential impairment of triazolam and zolpidem clearance by ritonavir
    D J Greenblatt
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, New England Medical Center, Boston, Massachusetts 02111, USA
    J Acquir Immune Defic Syndr 24:129-36. 2000
    ....
  14. ncbi Kinetics and dynamics of lorazepam during and after continuous intravenous infusion
    D J Greenblatt
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
    Crit Care Med 28:2750-7. 2000
    ..To evaluate the kinetics and dynamics of lorazepam during administration as a bolus plus an infusion, using electroencephalography as a pharmacodynamic end point...
  15. doi Mechanism of cytochrome P450-3A inhibition by ketoconazole
    David 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...
  16. doi Analysis of drug interactions involving fruit beverages and organic anion-transporting polypeptides
    David 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...
  17. pmc 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 oxidase
    David 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...
  18. doi Pharmacokinetic profile of SKP-1041, a modified release formulation of zaleplon
    David 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)...
  19. ncbi Comparative kinetics and response to the benzodiazepine agonists triazolam and zolpidem: evaluation of sex-dependent differences
    D J Greenblatt
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and New England Medical Center, Boston, Massachusetts 02111, USA
    J Pharmacol Exp Ther 293:435-43. 2000
    ..The complete dependence of triazolam clearance on CYP3A activity, as opposed to the mixed CYP participation in zolpidem clearance, may explain the differing sex effects on clearance of the two compounds...
  20. pmc Pharmocokinetics and pharmacodynamics of single-dose triazolam: electroencephalography compared with the Digit-Symbol Substitution Test
    David 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
    ....
  21. ncbi In vitro interactions of water-soluble garlic components with human cytochromes p450
    David 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...
  22. ncbi Age and gender effects on the pharmacokinetics and pharmacodynamics of ramelteon, a hypnotic agent acting via melatonin receptors MT1 and MT2
    David 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...
  23. ncbi Dynamics and kinetics of a modified-release formulation of zolpidem: comparison with immediate-release standard zolpidem and placebo
    David 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...
  24. ncbi Ritonavir and dexamethasone induce expression of CYP3A and P-glycoprotein in rats
    M D Perloff
    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
    Xenobiotica 34:133-50. 2004
    ..Qualitatively similar changes occur in human cell culture models and in clinical studies, and might contribute to drug interactions involving RIT (and other antiretroviral agents) in humans...
  25. ncbi Ketoconazole inhibition of triazolam and alprazolam clearance: differential kinetic and dynamic consequences
    D J Greenblatt
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
    Clin Pharmacol Ther 64:237-47. 1998
    ..Kinetic and dynamic consequences of metabolic inhibition were evaluated in a study of the interaction of ketoconazole, a P4503A inhibitor, with alprazolam and triazolam, two 3A substrate drugs with different kinetic profiles...
  26. ncbi Relative contribution of CYP3A to amitriptyline clearance in humans: in vitro and in vivo studies
    K Venkatakrishnan
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and New England Medical Center, Boston, MA 02111, USA
    J Clin Pharmacol 41:1043-54. 2001
    ..In conclusion, CYP3A plays a relatively minor role in amitriptyline clearance in vivo, which is consistent with in vitro predictions using the RAF approach...
  27. ncbi Nefazodone, meta-chlorophenylpiperazine, and their metabolites in vitro: cytochromes mediating transformation, and P450-3A4 inhibitory actions
    L L von Moltke
    Division of Clinical Pharmacology, New England Medical Center Hospital, Boston, Massachusetts, USA
    Psychopharmacology (Berl) 145:113-22. 1999
    ..Understanding of the mechanisms of biotransformation of antidepressant drugs, and of their capacity to interact with other medications, is of direct relevance to rational clinical psychopharmacology...
  28. ncbi Comparative kinetics and dynamics of zaleplon, zolpidem, and placebo
    D J Greenblatt
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, New England Medical Center Hospital, Boston 02111, USA
    Clin Pharmacol Ther 64:553-61. 1998
    ..This study evaluated the relationship of dose, plasma concentration, and time to the pharmacodynamics of zaleplon and zolpidem, 2 structurally distinct benzodiazepine receptor agonists...
  29. ncbi In vitro approaches to predicting drug interactions in vivo
    L L von Moltke
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
    Biochem Pharmacol 55:113-22. 1998
    ..Such predictive models deserve further evaluation, since they may ultimately yield more cost-effective and expeditious screening for drug interactions, with reduced human drug exposure and risk...
  30. ncbi Biotransformation of chlorzoxazone by hepatic microsomes from humans and ten other mammalian species
    M H Court
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
    Biopharm Drug Dispos 18:213-26. 1997
    ..These data indicate a species-conserved mechanism for the oxidative biotransformation of chlorzoxazone...
  31. ncbi Kinetic and dynamic interaction study of zolpidem with ketoconazole, itraconazole, and fluconazole
    D J Greenblatt
    Department of Pharmacology, and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
    Clin Pharmacol Ther 64:661-71. 1998
    ..Potential interactions of zolpidem with 3 commonly prescribed azole derivatives were evaluated in a controlled clinical study...
  32. ncbi Differential metabolism of midazolam in mouse liver and intestine microsomes: a comparison of cytochrome P450 activity and expression
    M D Perloff
    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
    Xenobiotica 33:365-77. 2003
    ..5. MDZ hydroxylation is predominately CYP3A dependent in mouse intestine (compared with mouse liver) since CYP2C is not expressed in the intestine. The importance of CYP3A in the mouse intestine appears to mirror that in humans...
  33. ncbi Inhibition of desipramine hydroxylation (Cytochrome P450-2D6) in vitro by quinidine and by viral protease inhibitors: relation to drug interactions in vivo
    L L von Moltke
    Department of Pharmacology and Experimental Therapeutics, Division of Clinical Pharmacology, Tufts University School of Medicine Boston, Massachusetts 02111, USA
    J Pharm Sci 87:1184-9. 1998
    ..Thus the in vitro model correctly identifies ritonavir as a potent and clinically important inhibitor of human P450-2D6. Other protease inhibitors may also inhibit 2D6 activity in humans, but with lower potency than ritonavir...
  34. ncbi Role of CYP3A enzymes in the biotransformation of triazolam in rat liver
    J S Warrington
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA, USA
    Xenobiotica 34:463-71. 2004
    ..This finding was further supported by the use of rat cDNA-expressed CYPs. 7. The male rat might serve as a useful model for evaluating mechanisms regulating TRZ metabolism in vivo...
  35. ncbi Differentiation of intestinal and hepatic cytochrome P450 3A activity with use of midazolam as an in vivo probe: effect of ketoconazole
    S M Tsunoda
    School of Pharmacy, Bouve College of Health Sciences, Northeastern University, Boston, Mass 02115, USA
    Clin Pharmacol Ther 66:461-71. 1999
    ..CYP3A activity is highly variable, causing difficulty in the therapeutic use of CYP3A substrates. A practical in vivo probe method that characterizes both intestinal and hepatic CYP3A activity would be useful...
  36. ncbi Human cytochromes mediating N-demethylation of fluoxetine in vitro
    L L von Moltke
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
    Psychopharmacology (Berl) 132:402-7. 1997
    ..Cytochrome P450-2C9 appears to be the principal human cytochrome mediating fluoxetine N-demethylation. P450-2C19 and -3A may make a further small contribution, but P450-2D6 is unlikely to make an important contribution...
  37. ncbi Inhibition of human cytochrome P450 isoforms by nonnucleoside reverse transcriptase inhibitors
    L L von Moltke
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
    J Clin Pharmacol 41:85-91. 2001
    ..However, the model does not incorporate interactions attributable to enzyme induction...
  38. ncbi Pomegranate juice does not impair clearance of oral or intravenous midazolam, a probe for cytochrome P450-3A activity: comparison with grapefruit juice
    Dora 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...
  39. ncbi Pharmacokinetic and pharmacodynamic interactions between zolpidem and caffeine
    R M Cysneiros
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and Tufts New England Medical Center, Boston, MA, USA
    Clin Pharmacol Ther 82:54-62. 2007
    ..Thus, caffeine only incompletely reverses zolpidem's sedative and performance-impairing effects, and cannot be considered as an antidote to benzodiazepine agonists...
  40. ncbi Cytochrome P-450 2B6 is responsible for interindividual variability of propofol hydroxylation by human liver microsomes
    M H Court
    Department of Pharmacology and Experimental Therapeutics, Tufts University, Boston, Massachusetts 02111, USA
    Anesthesiology 94:110-9. 2001
    ..The aim of this study was to identify the principal cytochrome P-450 (CYP) isoforms mediating this biotransformation...
  41. ncbi Potent mechanism-based inhibition of human CYP3A in vitro by amprenavir and ritonavir: comparison with ketoconazole
    L L von Moltke
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
    Eur J Clin Pharmacol 56:259-61. 2000
    ..Biotransformation of triazolam to its alpha-hydroxy and 4-hydroxy metabolites by human liver microsomes in vitro was used as an index of human cytochrome P450 3A (CYP3A) activity...
  42. ncbi Biotransformation of mestranol to ethinyl estradiol in vitro: the role of cytochrome P-450 2C9 and metabolic inhibitors
    J Schmider
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts 02111, USA
    J Clin Pharmacol 37:193-200. 1997
    ..Itraconazole produced no meaningful inhibition. Strong inhibition of ethinyl estradiol formation by sulfaphenazole suggests a major contribution of CYP2C9 to this reaction...
  43. doi Short-term clarithromycin administration impairs clearance and enhances pharmacodynamic effects of trazodone but not of zolpidem
    D Farkas
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and Tufts Medical Center, Boston, Massachusetts, USA
    Clin Pharmacol Ther 85:644-50. 2009
    ..However, clarithromycin has no significant kinetic or dynamic interaction with zolpidem...
  44. ncbi Relative contributions of CYP2C9 and 2C19 to phenytoin 4-hydroxylation in vitro: inhibition by sulfaphenazole, omeprazole, and ticlopidine
    G M Giancarlo
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Ave, Boston, MA 02111, USA
    Eur J Clin Pharmacol 57:31-6. 2001
    ..CONCLUSIONS: Formation of HPPH from PPH is mediated exclusively by CYP2C9 and 2C19, with CYP2C9 playing the major role...
  45. ncbi Molecular and pharmacokinetic evaluation of rat hepatic and gastrointestinal cytochrome p450 induction by tamoxifen
    M M Cotreau
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, MA 02111, USA
    Pharmacology 63:210-9. 2001
    ..These combined investigations suggest that TAM is an inducer of rat hepatic CYP 3A and 2B isoforms, and this agent has the potential of influencing the PK of coadministered 3A substrates...
  46. ncbi Drug interactions with newer antidepressants: role of human cytochromes P450
    D J Greenblatt
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and New England Medical Center, Boston, Mass 02111, USA
    J Clin Psychiatry 59:19-27. 1998
    ....
  47. ncbi Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate
    K Venkatakrishnan
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Ave, Boston, MA 02111, USA
    J Pharmacol Exp Ther 297:326-37. 2001
    ....
  48. ncbi Benzodiazepine receptor binding of triazolobenzodiazepines in vivo: increased receptor number with low-dose alprazolam
    L G Miller
    Department of Psychiatry and Medicine, Tufts New England Medical Center, Boston, MA 02111
    J Neurochem 49:1595-601. 1987
    ..05 mg/kg) was unchanged from that in untreated control mice, an observation suggesting that low doses of alprazolam increased receptor number.(ABSTRACT TRUNCATED AT 250 WORDS)..
  49. ncbi Human drug metabolism and the cytochromes P450: application and relevance of in vitro models
    K Venkatakrishnan
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, New England Medical Center Hospital, Boston, MA 02111, USA
    J Clin Pharmacol 41:1149-79. 2001
    ....
  50. ncbi Escitalopram (S-citalopram) and its metabolites in vitro: cytochromes mediating biotransformation, inhibitory effects, and comparison to R-citalopram
    L L von Moltke
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Ave, Boston, MA 02111, USA
    Drug Metab Dispos 29:1102-9. 2001
    ..Thus S-CT, biotransformed by three CYP isoforms in parallel, is unlikely to be affected by drug interactions or genetic polymorphisms. S-CT and S-DCT are also unlikely to cause clinically important drug interactions via CYP inhibition...
  51. ncbi Methadone inhibits rhodamine123 transport in Caco-2 cells
    E Stormer
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts 02111, USA
    Drug Metab Dispos 29:954-6. 2001
    ..However, MET can inhibit P-gp activity at intraluminal concentrations that might be achieved clinically. This may lead to increased bioavailability of coadministered compounds...
  52. ncbi Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir
    James 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...
  53. ncbi In vitro, pharmacokinetic, and pharmacodynamic interactions of ketoconazole and midazolam in the rat
    Tsutomu 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...
  54. doi Pomegranate juice and pomegranate extract do not impair oral clearance of flurbiprofen in human volunteers: divergence from in vitro results
    M J Hanley
    Program in Pharmacology and Experimental Therapeutics, Sackler School of Graduate Biomedical Sciences, Tufts University School of Medicine, Boston, Massachusetts, USA
    Clin Pharmacol Ther 92:651-7. 2012
    ..Despite inhibition of CYP2C9 in vitro, pomegranate juice and extract had no effect on CYP2C9 activity in human subjects, and can be consumed by patients taking CYP2C9 substrate drugs with negligible risk of a pharmacokinetic interaction...
  55. ncbi P-glycoprotein interactions of nefazodone and trazodone in cell culture
    E Stormer
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
    J Clin Pharmacol 41:708-14. 2001
    ..Concentrations of NFZ and TZD achieved in the intestine after chronic oral dosing may induce P-gp expression and reduce absorption of coadministered drugs...
  56. ncbi Extrapolating in vitro data on drug metabolism to in vivo pharmacokinetics: evaluation of the pharmacokinetic interaction between amitriptyline and fluoxetine
    J Schmider
    Department of Clinical Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts, USA
    Drug Metab Rev 31:545-60. 1999
    ..The concept of in vitro-in vivo scaling is promising and might ultimately yield a fast and more cost-effective screening for drug interactions with reduced human drug exposure and risk...
  57. ncbi Appetite suppressant drugs as inhibitors of human cytochromes P450: in vitro inhibition of P450-2D6 by D- and L-fenfluramine, but not phentermine
    L L von Moltke
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, New England Medical Center Hospital, Boston, Massachusetts 02111, USA
    J Clin Psychopharmacol 18:338-41. 1998
    ..7 microM). Findings from the in vitro assay are consistent with clinical studies showing significant inhibition of desipramine clearance by coadministration of fenfluramine...
  58. ncbi Desmethyldiazepam pharmacokinetics: studies following intravenous and oral desmethyldiazepam, oral clorazepate, and intravenous diazepam
    D J Greenblatt
    Department of Psychiatry, Tufts University School of Medicine, Boston, Massachusetts
    J Clin Pharmacol 28:853-9. 1988
    ..After oral administration of DMDZ in tablet form (10 mg), or of clorazepate dipotassium in capsule form (15 mg), systemic availability of DMDZ from each of the oral dosage forms was not significantly different from 100%...
  59. ncbi Ritonavir induces P-glycoprotein expression, multidrug resistance-associated protein (MRP1) expression, and drug transporter-mediated activity in a human intestinal cell line
    M D Perloff
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts 02111, USA
    J Pharm Sci 90:1829-37. 2001
    ..Similar in vivo phenomena may occur during anti-HIV drug therapy, explaining potential decrements in therapeutic efficacy due to decreases in bioavailability or alterations in drug distribution...
  60. ncbi Interindividual variability in acetaminophen glucuronidation by human liver microsomes: identification of relevant acetaminophen UDP-glucuronosyltransferase isoforms
    M H Court
    Molecular Pharmacogenetics, Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts 02111, USA
    J Pharmacol Exp Ther 299:998-1006. 2001
    ..UGT1A1 was also predicted to contribute substantially at toxic concentrations (>1 mM; >28% activity), whereas UGT1A6 was most active at relatively low concentrations (<50 microM; >29% activity)...
  61. ncbi Unchanged cytochrome P450 3A (CYP3A) expression and metabolism of midazolam, triazolam, and dexamethasone in mdr(-/-) mouse liver microsomes
    M D Perloff
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, New England Medical Center Hospital, Boston, MA 02111, USA
    Biochem Pharmacol 57:1227-32. 1999
    ..68+/-0.09 pmol/microg protein. Although CYP3A and P-gp share aspects of activity and expression, disruption of the mdrl genes does not affect CYP3A-mediated metabolism or protein expression in the mouse...
  62. pmc Pharmacokinetic properties of zolpidem in elderly and young adults: possible modulation by testosterone in men
    Joel 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
    ..The influence of ageing on the pharmacokinetics of zolpidem, an extensively prescribed hypnotic medication, was evaluated in healthy human volunteers...
  63. ncbi Ethanol inhibits in-vitro metabolism of nifedipine, triazolam and testosterone in human liver microsomes
    Kiran 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...
  64. pmc Saint John's wort: an in vitro analysis of P-glycoprotein induction due to extended exposure
    M D Perloff
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, Massachusetts, MA 02111, USA
    Br J Pharmacol 134:1601-8. 2001
    ..4. SJW and HYP significantly induced P-gp expression at low, clinically relevant concentrations. Similar effects occurring in vivo may explain the decreased bioavailability of P-gp substrate drugs when co-administered with SJW...
  65. ncbi Propofol hydroxylation by dog liver microsomes: assay development and dog breed differences
    M H Court
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts 02111, USA
    Drug Metab Dispos 27:1293-9. 1999
    ....
  66. ncbi Comparative single-dose kinetics and dynamics of lorazepam, alprazolam, prazepam, and placebo
    D J Greenblatt
    Department of Psychiatry, Tufts University School of Medicine, Boston, MA
    Clin Pharmacol Ther 44:326-34. 1988
    ....
  67. ncbi Human cytochromes and some newer antidepressants: kinetics, metabolism, and drug interactions
    D J Greenblatt
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine and New England Medical Center, Boston, Massachusetts 02111, USA
    J Clin Psychopharmacol 19:23S-35S. 1999
    ..Also reviewed are the relative activities of various new antidepressants as inhibitors of CYPs, and the benefits and drawbacks of in vivo and in vitro methodologies for identification and quantitation of drug interactions...
  68. ncbi Serotonin (5-hydroxytryptamine) glucuronidation in vitro: assay development, human liver microsome activities and species differences
    S Krishnaswamy
    Comparative and Molecular Pharmacogenetics Laboratory, Tufts University School of Medicine, Boston, MA 02111, USA
    Xenobiotica 33:169-80. 2003
    ..6. This assay provides a novel sensitive and specific technique for the measurement of serotonin-UGT activity in vitro...
  69. ncbi A large-sample study of diazepam pharmacokinetics
    D J Greenblatt
    Department of Psychiatry, Tufts University School of Medicine, Boston, Massachusetts
    Ther Drug Monit 11:652-7. 1989
    ..Parametric statistical testing procedures and pharmacokinetic forecasting schemes may be improved by more precise delineation of the underlying distributions for pharmacokinetic variables...
  70. ncbi Clearance of the antihistamine doxylamine. Reduced in elderly men but not in elderly women
    H Friedman
    Department of Psychiatry, Tufts University School of Medicine, Boston, Massachusetts
    Clin Pharmacokinet 16:312-6. 1989
    ..5 vs 10.2 h, p less than 0.05). The reduced doxylamine clearance and prolonged half-life in elderly men, but not in elderly women, is similar to results for many other drugs which are transformed by oxidation...
  71. pmc Fluvoxamine impairs single-dose caffeine clearance without altering caffeine pharmacodynamics
    Kerry 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
    ..Coadministration of fluvoxamine impairs the clearance of caffeine and prolongs its elimination half-life, which is attributable to inhibition of CYP1A2 by fluvoxamine. The clinical importance of this interaction is not established...
  72. ncbi The influence of age and sex on the clearance of cytochrome P450 3A substrates
    Monette 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...
  73. ncbi Short-term exposure to low-dose ritonavir impairs clearance and enhances adverse effects of trazodone
    David 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...
  74. ncbi Pharmacodynamic and receptor binding changes during chronic lorazepam administration
    J M Fahey
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
    Pharmacol Biochem Behav 69:1-8. 2001
    ..These observed changes in binding are not necessarily associated with robust changes in receptor function...
  75. ncbi Doxylamine and diphenhydramine pharmacokinetics in women on low-dose estrogen oral contraceptives
    B G Luna
    Department of Psychiatry, Tufts University School of Medicine, Boston, MA
    J Clin Pharmacol 29:257-60. 1989
    ..8 vs 25.5 ml/min/kg. None of these differences were statistically significant. Thus, low-dose estrogen-containing oral contraceptives do not significantly influence the pharmacokinetics of the antihistamines doxylamine or diphenhydramine...
  76. ncbi Effect of extended exposure to grapefruit juice on cytochrome P450 3A activity in humans: comparison with ritonavir
    Kerry 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
    ..However, the effect of extended exposure to grapefruit juice on CYP3A activity is not established...
  77. ncbi Effect of age on in vitro triazolam biotransformation in male human liver microsomes
    Kiran 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...
  78. ncbi Age-related differences in CYP3A expression and activity in the rat liver, intestine, and kidney
    Jill 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...
  79. ncbi Phenacetin and chlorzoxazone biotransformation in aging male Fischer 344 rats
    Jill 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...
  80. ncbi Ginkgo biloba does not alter clearance of flurbiprofen, a cytochrome P450-2C9 substrate
    David 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...
  81. ncbi Influence of fruit juices on drug disposition: discrepancies between in vitro and clinical studies
    Dora 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...
  82. ncbi Evaluation of Supermix as an in vitro model of human liver microsomal drug metabolism
    Karthik 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...
  83. ncbi Atazanavir: effects on P-glycoprotein transport and CYP3A metabolism in vitro
    Elke 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...
  84. ncbi Kinetics and dynamics of intravenous adinazolam, N-desmethyl adinazolam, and alprazolam in healthy volunteers
    Karthik 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...
  85. ncbi Fexofenadine transport in Caco-2 cells: inhibition with verapamil and ritonavir
    Michael 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...
  86. ncbi Genotype-phenotype associations of cytochrome P450 3A4 and 3A5 polymorphism with midazolam clearance in vivo
    Ping 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...
  87. ncbi Kinetics and EEG effects of midazolam during and after 1-minute, 1-hour, and 3-hour intravenous infusions
    David 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...
  88. ncbi Bioinequivalence of a generic brand of diazepam
    A Locniskar
    Department of Psychiatry, Tufts University School of Medicine, Boston, Massachusetts
    Biopharm Drug Dispos 10:597-605. 1989
    ..Findings for desmethyldiazepam were similar. Thus, diazepam absorption from the generic brand of diazepam is significantly slower than from Valium, which in turn could lead to therapeutic inequivalence...
  89. pmc Identification of polymorphisms in the 3'-untranslated region of the human pregnane X receptor (PXR) gene associated with variability in cytochrome P450 3A (CYP3A) metabolism
    L Oleson
    Clinical Pharmacology, Tufts University School of Medicine, 136 Harrison Avenue, Boston, MA 02111, USA
    Xenobiotica 40:146-62. 2010
    ..036). The results identify rs3732359 and rs3732360 as PXR-3'UTR single nucleotide polymorphisms associated with higher CYP3A activity in vivo in African-Americans...
  90. ncbi Molecular genetic basis for deficient acetaminophen glucuronidation by cats: UGT1A6 is a pseudogene, and evidence for reduced diversity of expressed hepatic UGT1A isoforms
    M H Court
    Department of Pharmacology and Experimental Therapeutics, Tufts University School of Medicine, Boston, Massachusetts, USA
    Pharmacogenetics 10:355-69. 2000
    ..Such differences most likely reflect the highly carnivorous diet of Feliform species and resultant minimal exposure to phytoalexins...
  91. ncbi The effect of chronic lorazepam administration in aging mice
    Jeanne 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
    ....
  92. pmc Evidence for oxazepam as an in vivo probe of UGT2B15: oxazepam clearance is reduced by UGT2B15 D85Y polymorphism but unaffected by UGT2B17 deletion
    Xi 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...
  93. ncbi Factors influencing midazolam hydroxylation activity in human liver microsomes
    Ping 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...
  94. ncbi Acute zolpidem administration produces pharmacodynamic and receptor occupancy changes at similar doses
    Jeanne 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...
  95. ncbi Ritonavir greatly impairs CYP3A activity in HIV infection with chronic viral hepatitis
    Tamsin 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...
  96. pmc Role of NADPH-cytochrome P450 reductase and cytochrome-b5/NADH-b5 reductase in variability of CYP3A activity in human liver microsomes
    Lu 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...
  97. ncbi Interaction of flurbiprofen with cranberry juice, grape juice, tea, and fluconazole: in vitro and clinical studies
    David 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...
  98. ncbi Pharmacogenetic determinants of interindividual variability in bupropion hydroxylation by cytochrome P450 2B6 in human liver microsomes
    Leah 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...
  99. ncbi Human cytochromes mediating gepirone biotransformation at low substrate concentrations
    David 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...
  100. ncbi Effect of zolpidem on human cytochrome P450 activity, and on transport mediated by P-glycoprotein
    Lisa 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...
  101. ncbi Validation of serotonin (5-hydroxtryptamine) as an in vitro substrate probe for human UDP-glucuronosyltransferase (UGT) 1A6
    Soundararajan 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...

Research Grants29

  1. GARLIC PREPARATIONS AND ANTIRETROVIRAL DRUGS
    David Greenblatt; Fiscal Year: 2002
    ..The work will provide immediately applicable clinical data on garlic interactions with antiretrovirals, as well as mechanistic data identifying the interaction process and its predictability from in vitro models. ..
  2. CYP3A Function in Aging AfricanAmericans
    David Greenblatt; Fiscal Year: 2003
    ..This study should provide important mechanistic information on the role of age, gender, and ethnicity as sources of variability in CYP3A-mediated drug metabolism and response. ..
  3. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 2003
    ....
  4. Metabolic Consequences of HAART: CYP3A and P-gp
    David Greenblatt; Fiscal Year: 2003
    ..This multidisciplinary proposal provides a clinical and scientific basis to assess the effects of currently available as well as experimental HAART medications on human CYP3A and P-gp. ..
  5. HAART Regimens in Substance Abusers
    David Greenblatt; Fiscal Year: 2003
    ....
  6. GARLIC PREPARATIONS AND ANTIRETROVIRAL DRUGS
    David Greenblatt; Fiscal Year: 2003
    ..The work will provide immediately applicable clinical data on garlic interactions with antiretrovirals, as well as mechanistic data identifying the interaction process and its predictability from in vitro models. ..
  7. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 2004
    ....
  8. CYP3A Function in Aging AfricanAmericans
    David Greenblatt; Fiscal Year: 2004
    ..This study should provide important mechanistic information on the role of age, gender, and ethnicity as sources of variability in CYP3A-mediated drug metabolism and response. ..
  9. GARLIC PREPARATIONS AND ANTIRETROVIRAL DRUGS
    David Greenblatt; Fiscal Year: 2004
    ..The work will provide immediately applicable clinical data on garlic interactions with antiretrovirals, as well as mechanistic data identifying the interaction process and its predictability from in vitro models. ..
  10. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 2005
    ....
  11. CYP3A Function in Aging AfricanAmericans
    David Greenblatt; Fiscal Year: 2005
    ..This study should provide important mechanistic information on the role of age, gender, and ethnicity as sources of variability in CYP3A-mediated drug metabolism and response. ..
  12. MDR1 and Related Proteins during HIV PI Exposure
    David Greenblatt; Fiscal Year: 2005
    ..The findings will be of importance in understanding lipid disorders related to PIs as well as the kinetics of drugs used to treat HIV and related disorders. ..
  13. HAART Regimens in Substance Abusers
    David Greenblatt; Fiscal Year: 2002
    ....
  14. ANTIRETROVIRAL THERAPIES AND SUBSTANCE ABUSE
    David Greenblatt; Fiscal Year: 2002
    ..The in vitro model, if validated, has the potential to provide clinically important information on interactions involving HIV treatments and abusable drugs, at relatively low cost and with no human drug exposure. ..
  15. Metabolic Consequences of HAART: CYP3A and P-gp
    David Greenblatt; Fiscal Year: 2002
    ..This multidisciplinary proposal provides a clinical and scientific basis to assess the effects of currently available as well as experimental HAART medications on human CYP3A and P-gp. ..
  16. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 1992
    ..The proposed studies will provide a broad picture of effects of chronic benzodiazepines at the molecular level, together with evaluation of interventions that have direct relevance to prevention of benzodiazepine withdrawal...
  17. CHRONIC BENZODIAZEPINES--BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 1999
    ..Age-dependent differences in response to chronic benzodiazepine administration and withdrawal, and the possible role of EAA coregulation, studied using matched cohorts of young and old animals. ..
  18. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 1991
    ..The proposed studies will provide a broad picture of effects of chronic benzodiazepines at the molecular level, together with evaluation of interventions that have direct relevance to prevention of benzodiazepine withdrawal...
  19. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 2001
    ....
  20. Metabolic Consequences of HAART: CYP3A and P-gp
    David Greenblatt; Fiscal Year: 2001
    ..This multidisciplinary proposal provides a clinical and scientific basis to assess the effects of currently available as well as experimental HAART medications on human CYP3A and P-gp. ..
  21. HAART Regimens in Substance Abusers
    David Greenblatt; Fiscal Year: 2001
    ....
  22. CYP3A Function in Aging AfricanAmericans
    David Greenblatt; Fiscal Year: 2002
    ..This study should provide important mechanistic information on the role of age, gender, and ethnicity as sources of variability in CYP3A-mediated drug metabolism and response. ..
  23. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 2001
    ....
  24. CHRONIC BENZODIAZEPINES: BEHAVIOR AND NEUROCHEMISTRY
    David Greenblatt; Fiscal Year: 2002
    ....
  25. CYP3A Function in Aging AfricanAmericans
    David Greenblatt; Fiscal Year: 2006
    ..This study should provide important mechanistic information on the role of age, gender, and ethnicity as sources of variability in CYP3A-mediated drug metabolism and response. ..