PMID- 18971181
OWN - NLM
STAT- MEDLINE
DCOM- 20091005
LR  - 20131121
IS  - 1673-4254 (Print)
IS  - 1673-4254 (Linking)
VI  - 28
IP  - 10
DP  - 2008 Oct
TI  - [Pharmacokinetics of nalmefene after a single or multiple intravenous doses in 
      Chinese healthy volunteers].
PG  - 1816-9
AB  - OBJECTIVE: To investigate the pharmacokinetics of nalmefene after intravenous 
      administration at a single or multiple doses in Chinese healthy volunteers. 
      METHODS: This open, randomized clinical trial involved 12 healthy volunteers, who 
      received a single-dose (2 mg) nalmefene injection. Before and at different time 
      points after the injection, blood sample were obtained from the subjects. After 
      the single intravenous dose trial, 8 healthy volunteers received intravenous 
      nalmefene at 2 mg once daily for 6 consecutive days, and the plasma drug 
      concentrations were determined on the morning of days 4, 5 and 6 using liquid 
      chromatography/tandem mass spectrometry and the pharmacokinetic parameters were 
      calculated using PKS program. RESULTS: The main pharmacokinetic parameters of 
      nalmefene (Cmax, Tmax, T1/2, AUC0-48, and AUC0-infinity) after the single 
      intravenous dose were 7.34-/+1.56 microg/L, 0.08 h, 12.01-/+2.20 h, 30.29-/+9.84 
      microg.L(-1).h, and 32.23-/+9.94 microg.L(-1).h, respectively; the parameters 
      after multiple doses were 8.04-/+1.09 microg/L, 0.08 h, 12.43-/+1.44 h, 
      33.64-/+9.15 microg.L(-1).h and 35.98-/+9.23 microg.L(-1).h, respectively. The 
      steady-state pharmacokinetic parameters including the degree of fluctuation (DF), 
      AUCss and Cav were 4.69-/+1.29, 19.64-/+6.20 microg.L(-1).h and 1.64-/+0.52 
      microg/L, respectively. CONCLUSION: Nalmefene showed similar pharmacokinetics in 
      Chinese healthy volunteers with those in the foreign testees, and can be safely 
      administered in healthy volunteers without producing unmanageable pain.
FAU - Liao, Ri-fang
AU  - Liao RF
AD  - Department of Clinical Pharmacy, Second Affiliated Hospital of Sun Yat-sen 
      University, Guangzhou 510120, China. liaorf@mail.sysu.edu.cn
FAU - Zeng, Zhuan-ping
AU  - Zeng ZP
FAU - Wen, Yu-guan
AU  - Wen YG
LA  - chi
PT  - Clinical Trial, Phase I
PT  - English Abstract
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
PL  - China
TA  - Nan Fang Yi Ke Da Xue Xue Bao
JT  - Nan fang yi ke da xue xue bao = Journal of Southern Medical University
JID - 101266132
RN  - 0 (Narcotic Antagonists)
RN  - 5S6W795CQM (Naltrexone)
RN  - TOV02TDP9I (nalmefene)
SB  - IM
MH  - Adult
MH  - China
MH  - Female
MH  - Humans
MH  - Injections, Intravenous
MH  - Male
MH  - Naltrexone/administration & dosage/*analogs & derivatives/pharmacokinetics
MH  - Narcotic Antagonists/administration & dosage/*pharmacokinetics
EDAT- 2008/10/31 09:00
MHDA- 2009/10/06 06:00
CRDT- 2008/10/31 09:00
PHST- 2008/10/31 09:00 [pubmed]
PHST- 2009/10/06 06:00 [medline]
PHST- 2008/10/31 09:00 [entrez]
PST - ppublish
SO  - Nan Fang Yi Ke Da Xue Xue Bao. 2008 Oct;28(10):1816-9.