PMID- 22673010
OWN - NLM
STAT- MEDLINE
DCOM- 20130903
LR  - 20191112
IS  - 1880-0920 (Electronic)
IS  - 1347-4367 (Linking)
VI  - 27
IP  - 6
DP  - 2012
TI  - Changes in CYP1A2 activity in humans after 3,4-methylenedioxymethamphetamine 
      (MDMA, ecstasy) administration using caffeine as a probe drug.
PG  - 605-13
AB  - 3,4-Methylenedioxymethamphetamine (MDMA; ecstasy) is a ring-substituted 
      amphetamine widely used for recreational purposes. MDMA is predominantly 
      O-demethylenated in humans by cytochrome P450 (CYP) 2D6, and is also a potent 
      mechanism-based inhibitor of the enzyme. After assessing the inhibition and 
      recovery of CYP2D6 in a previous study, the aim of this work was to study in 
      humans the activity of CYP1A2 in vivo after CYP2D6 had been inhibited by MDMA, 
      using caffeine as a probe drug. Twelve male and nine female recreational MDMA 
      users were included. In session 1, 100 mg of caffeine was given at 0 h. In 
      session 2, a 1.5 mg/kg MDMA dose (range 75-100 mg) was given at 0 h followed by a 
      100 mg dose of caffeine 4 h later. Aliquots of plasma were assayed for caffeine 
      (137X) and paraxanthine (17X) and statistically significant differences were 
      assessed with a one-way ANOVA. There were significant gender differences at basal 
      condition, which persisted after MDMA administration. CYP1A2 activity was higher 
      in both genders after drug administration, with an increase in 40% in females and 
      20% in males. Results show an increase in CYP1A2 activity when CYP2D6 is 
      inhibited by MDMA in both genders, being more pronounced in females.
FAU - Yubero-Lahoz, Samanta
AU  - Yubero-Lahoz S
AD  - Human Pharmacology and Clinical Neurosciences Research Group, Neurosciences 
      Research Program, IMIM-Hospital del Mar Medical Research Institute, Barcelona, 
      Spain.
FAU - Pardo, Ricardo
AU  - Pardo R
FAU - Farre, Magi
AU  - Farre M
FAU - Mathuna, Brian O
AU  - Mathuna BO
FAU - Torrens, Marta
AU  - Torrens M
FAU - Mustata, Cristina
AU  - Mustata C
FAU - Perez-Mana, Clara
AU  - Perez-Mana C
FAU - Langohr, Klaus
AU  - Langohr K
FAU - Carbo, Marcel Li
AU  - Carbo ML
FAU - de la Torre, Rafael
AU  - de la Torre R
LA  - eng
GR  - 5R01BA017987-01/BA/FDA HHS/United States
PT  - Journal Article
PT  - Research Support, N.I.H., Extramural
PT  - Research Support, Non-U.S. Gov't
DEP - 20120522
PL  - England
TA  - Drug Metab Pharmacokinet
JT  - Drug metabolism and pharmacokinetics
JID - 101164773
RN  - 0 (Cytochrome P-450 CYP2D6 Inhibitors)
RN  - 3G6A5W338E (Caffeine)
RN  - C137DTR5RG (Theophylline)
RN  - EC 1.14.14.1 (CYP1A2 protein, human)
RN  - EC 1.14.14.1 (Cytochrome P-450 CYP1A2)
RN  - EC 1.14.14.1 (Cytochrome P-450 CYP2D6)
RN  - KE1SEN21RM (N-Methyl-3,4-methylenedioxyamphetamine)
RN  - Q3565Y41V7 (1,7-dimethylxanthine)
SB  - IM
MH  - Adult
MH  - Area Under Curve
MH  - Caffeine/*administration & dosage/blood
MH  - Cytochrome P-450 CYP1A2/*metabolism
MH  - Cytochrome P-450 CYP2D6/metabolism
MH  - Cytochrome P-450 CYP2D6 Inhibitors
MH  - Female
MH  - Half-Life
MH  - Humans
MH  - Male
MH  - N-Methyl-3,4-methylenedioxyamphetamine/*pharmacology
MH  - Sex Factors
MH  - Theophylline/administration & dosage/blood
EDAT- 2012/06/08 06:00
MHDA- 2013/09/04 06:00
CRDT- 2012/06/08 06:00
PHST- 2012/06/08 06:00 [entrez]
PHST- 2012/06/08 06:00 [pubmed]
PHST- 2013/09/04 06:00 [medline]
AID - DN/JST.JSTAGE/dmpk/DMPK-12-RG-032 [pii]
AID - 10.2133/dmpk.dmpk-12-rg-032 [doi]
PST - ppublish
SO  - Drug Metab Pharmacokinet. 2012;27(6):605-13. doi: 10.2133/dmpk.dmpk-12-rg-032. 
      Epub 2012 May 22.