Literature DB >> 19833841

Delta9-tetrahydrocannabinol (THC), 11-hydroxy-THC, and 11-nor-9-carboxy-THC plasma pharmacokinetics during and after continuous high-dose oral THC.

Eugene W Schwilke1, David M Schwope, Erin L Karschner, Ross H Lowe, William D Darwin, Deanna L Kelly, Robert S Goodwin, David A Gorelick, Marilyn A Huestis.   

Abstract

BACKGROUND: Delta(9)-tetrahydrocannabinol (THC) is the primary psychoactive constituent of cannabis and an active cannabinoid pharmacotherapy component. No plasma pharmacokinetic data after repeated oral THC administration are available.
METHODS: Six adult male daily cannabis smokers resided on a closed clinical research unit. Oral THC capsules (20 mg) were administered every 4-8 h in escalating total daily doses (40-120 mg) for 7 days. Free and glucuronidated plasma THC, 11-hydroxy-THC (11-OH-THC), and 11-nor-9-carboxy-THC (THCCOOH) were quantified by 2-dimensional GC-MS during and after dosing.
RESULTS: Free plasma THC, 11-OH-THC, and THCCOOH concentrations 19.5 h after admission (before controlled oral THC dosing) were mean 4.3 (SE 1.1), 1.3 (0.5), and 34.0 (8.4) microg/L, respectively. During oral dosing, free 11-OH-THC and THCCOOH increased steadily, whereas THC did not. Mean peak plasma free THC, 11-OH-THC, and THCCOOH concentrations were 3.8 (0.5), 3.0 (0.7), and 196.9 (39.9) mug/L, respectively, 22.5 h after the last dose. Escherichia coli beta-glucuronidase hydrolysis of 264 cannabinoid specimens yielded statistically significant increases in THC, 11-OH-THC, and THCCOOH concentrations (P < 0.001), but conjugated concentrations were underestimated owing to incomplete enzymatic hydrolysis.
CONCLUSIONS: Plasma THC concentrations remained >1 mug/L for at least 1 day after daily cannabis smoking and also after cessation of multiple oral THC doses. We report for the first time free plasma THC concentrations after multiple high-dose oral THC throughout the day and night, and after Escherichia coli beta-glucuronidase hydrolysis. These data will aid in the interpretation of plasma THC concentrations after multiple oral doses.

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Year:  2009        PMID: 19833841      PMCID: PMC3196989          DOI: 10.1373/clinchem.2008.122119

Source DB:  PubMed          Journal:  Clin Chem        ISSN: 0009-9147            Impact factor:   8.327


  37 in total

1.  Stability of 11-nor-delta(9)-carboxy-tetrahydrocannabinol glucuronide in plasma and urine assessed by liquid chromatography-tandem mass spectrometry.

Authors:  Gisela Skopp; Lucia Pötsch
Journal:  Clin Chem       Date:  2002-02       Impact factor: 8.327

Review 2.  Hepatic disposition of electrophilic acyl glucuronide conjugates.

Authors:  B C Sallustio; L Sabordo; A M Evans; R L Nation
Journal:  Curr Drug Metab       Date:  2000-09       Impact factor: 3.731

3.  Partition coefficient, blood to plasma ratio, protein binding and short-term stability of 11-nor-Delta(9)-carboxy tetrahydrocannabinol glucuronide.

Authors:  Gisela Skopp; Lucia Pötsch; Martin Mauden; Barbara Richter
Journal:  Forensic Sci Int       Date:  2002-03-28       Impact factor: 2.395

4.  Simultaneous GC-EI-MS determination of Delta9-tetrahydrocannabinol, 11-hydroxy-Delta9-tetrahydrocannabinol, and 11-nor-9-carboxy-Delta9-tetrahydrocannabinol in human urine following tandem enzyme-alkaline hydrolysis.

Authors:  Tsadik T Abraham; Ross H Lowe; Stephane O Pirnay; William D Darwin; Marilyn A Huestis
Journal:  J Anal Toxicol       Date:  2007-10       Impact factor: 3.367

5.  Effects of THC and lofexidine in a human laboratory model of marijuana withdrawal and relapse.

Authors:  Margaret Haney; Carl L Hart; Suzanne K Vosburg; Sandra D Comer; Stephanie Collins Reed; Richard W Foltin
Journal:  Psychopharmacology (Berl)       Date:  2007-12-27       Impact factor: 4.530

6.  Validated method for the simultaneous determination of Delta 9-tetrahydrocannabinol (THC), 11-hydroxy-THC and 11-nor-9-carboxy-THC in human plasma using solid phase extraction and gas chromatography-mass spectrometry with positive chemical ionization.

Authors:  Richard A Gustafson; Eric T Moolchan; Allan Barnes; Barry Levine; Marilyn A Huestis
Journal:  J Chromatogr B Analyt Technol Biomed Life Sci       Date:  2003-12-05       Impact factor: 3.205

7.  Do Delta9-tetrahydrocannabinol concentrations indicate recent use in chronic cannabis users?

Authors:  Erin L Karschner; Eugene W Schwilke; Ross H Lowe; W David Darwin; Harrison G Pope; Ronald Herning; Jean L Cadet; Marilyn A Huestis
Journal:  Addiction       Date:  2009-10-05       Impact factor: 6.526

Review 8.  Use of dronabinol for cannabis dependence: two case reports and review.

Authors:  Frances R Levin; Herbert D Kleber
Journal:  Am J Addict       Date:  2008 Mar-Apr

Review 9.  Cannabinoids for the treatment of neuropathic pain: clinical evidence.

Authors:  John C Ashton; Erin D Milligan
Journal:  Curr Opin Investig Drugs       Date:  2008-01

10.  The involvement of drugs in drivers of motor vehicles killed in Australian road traffic crashes.

Authors:  Olaf H Drummer; Jim Gerostamoulos; Helen Batziris; Mark Chu; John Caplehorn; Michael D Robertson; Philip Swann
Journal:  Accid Anal Prev       Date:  2004-03
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  33 in total

1.  Disposition of cannabinoids in oral fluid after controlled around-the-clock oral THC administration.

Authors:  Garry Milman; Allan J Barnes; David M Schwope; Eugene W Schwilke; William D Darwin; Robert S Goodwin; Deanna L Kelly; David A Gorelick; Marilyn A Huestis
Journal:  Clin Chem       Date:  2010-06-08       Impact factor: 8.327

2.  Identification of recent cannabis use: whole-blood and plasma free and glucuronidated cannabinoid pharmacokinetics following controlled smoked cannabis administration.

Authors:  David M Schwope; Erin L Karschner; David A Gorelick; Marilyn A Huestis
Journal:  Clin Chem       Date:  2011-08-11       Impact factor: 8.327

3.  Δ9-Tetrahydrocannabinol changes the brain lipidome and transcriptome differentially in the adolescent and the adult.

Authors:  Emma Leishman; Michelle Murphy; Ken Mackie; Heather B Bradshaw
Journal:  Biochim Biophys Acta Mol Cell Biol Lipids       Date:  2018-02-08       Impact factor: 4.698

4.  Direct quantification of cannabinoids and cannabinoid glucuronides in whole blood by liquid chromatography-tandem mass spectrometry.

Authors:  David M Schwope; Karl B Scheidweiler; Marilyn A Huestis
Journal:  Anal Bioanal Chem       Date:  2011-07-05       Impact factor: 4.142

Review 5.  Cannabis use during pregnancy: Pharmacokinetics and effects on child development.

Authors:  Kimberly S Grant; Rebekah Petroff; Nina Isoherranen; Nephi Stella; Thomas M Burbacher
Journal:  Pharmacol Ther       Date:  2017-08-25       Impact factor: 12.310

6.  Validation of an enzyme immunoassay for detection and semiquantification of cannabinoids in oral fluid.

Authors:  David M Schwope; Garry Milman; Marilyn A Huestis
Journal:  Clin Chem       Date:  2010-04-01       Impact factor: 8.327

7.  Antagonist-elicited cannabis withdrawal in humans.

Authors:  David A Gorelick; Robert S Goodwin; Eugene Schwilke; David M Schwope; William D Darwin; Deanna L Kelly; Robert P McMahon; Fang Liu; Catherine Ortemann-Renon; Denis Bonnet; Marilyn A Huestis
Journal:  J Clin Psychopharmacol       Date:  2011-10       Impact factor: 3.153

8.  Oral fluid/plasma cannabinoid ratios following controlled oral THC and smoked cannabis administration.

Authors:  Dayong Lee; Ryan Vandrey; Garry Milman; Mateus Bergamaschi; Damodara R Mendu; Jeannie A Murray; Allan J Barnes; Marilyn A Huestis
Journal:  Anal Bioanal Chem       Date:  2013-07-06       Impact factor: 4.142

9.  Around-the-clock oral THC effects on sleep in male chronic daily cannabis smokers.

Authors:  David A Gorelick; Robert S Goodwin; Eugene Schwilke; Jennifer R Schroeder; David M Schwope; Deanna L Kelly; Catherine Ortemann-Renon; Denis Bonnet; Marilyn A Huestis
Journal:  Am J Addict       Date:  2013 Sep-Oct

10.  Impact of dronabinol on quantitative electroencephalogram (qEEG) measures of sleep in obstructive sleep apnea syndrome.

Authors:  Sarah S Farabi; Bharati Prasad; Lauretta Quinn; David W Carley
Journal:  J Clin Sleep Med       Date:  2014-01-15       Impact factor: 4.062

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