PMID- 22722651
OWN - NLM
STAT- MEDLINE
DCOM- 20121227
LR  - 20181201
IS  - 1423-0313 (Electronic)
IS  - 0031-7012 (Linking)
VI  - 90
IP  - 1-2
DP  - 2012
TI  - Bioequivalence of intravenous and oral formulations of the antiepileptic drug 
      lacosamide.
PG  - 40-6
LID - 10.1159/000339077 [doi]
AB  - BACKGROUND/AIMS: To evaluate the bioequivalence of intravenous and oral 
      lacosamide (tablet), an antiepileptic drug. METHODS: Two randomized, single-dose 
      (200 mg) trials were conducted: a 2-way trial (study A, 15-min infusion, oral 
      tablet) and a 3-way crossover trial (study B, 30- and 60-min infusions, oral 
      tablet). Twenty four healthy men participated in study A and 27 in study B. 
      Eighteen blood samples were taken before to 72 h after lacosamide administration 
      during each treatment period, followed by a 1-week washout. Safety and the ratio 
      of intravenous/oral lacosamide for AUC(0-tz) (area under the concentration-time 
      curve from zero up to the last measurable plasma concentration) and C(max) 
      (maximum plasma concentration) were evaluated. RESULTS: For AUC(0-tz) and C(max), 
      90% confidence intervals for the ratio of intravenous/oral lacosamide fell within 
      the predetermined bioequivalence range (80-125%) for 30- and 60-min infusions. In 
      study A, all adverse events (AEs) were mild, with no discontinuations. In study 
      B, 3 volunteers discontinued due to AEs; one serious AE (epiglottitis) was 
      reported. No clinically relevant effects on vital signs, electrocardiograms or 
      laboratory parameters and no AEs relating to infusion site were reported. 
      CONCLUSION: Intravenous infusions (15, 30 and 60 min) of 200 mg lacosamide are as 
      well tolerated as the oral tablet. Bioequivalence was demonstrated for 30- and 
      60-min infusions; therefore, direct conversion from oral to intravenous 
      lacosamide, or vice versa, is possible.
CI  - Copyright (c) 2012 S. Karger AG, Basel.
FAU - Cawello, Willi
AU  - Cawello W
AD  - UCB Pharma, Monheim, Germany. Willi.Cawello@ucb.com
FAU - Bonn, Rainer
AU  - Bonn R
FAU - Boekens, Hilmar
AU  - Boekens H
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
DEP - 20120621
PL  - Switzerland
TA  - Pharmacology
JT  - Pharmacology
JID - 0152016
RN  - 0 (Acetamides)
RN  - 0 (Anticonvulsants)
RN  - 563KS2PQY5 (Lacosamide)
SB  - IM
MH  - Acetamides/administration & dosage/adverse effects/*pharmacokinetics
MH  - Administration, Oral
MH  - Adolescent
MH  - Adult
MH  - Anticonvulsants/administration & dosage/adverse effects/*pharmacokinetics
MH  - Area Under Curve
MH  - Cross-Over Studies
MH  - Humans
MH  - Infusions, Intravenous
MH  - Lacosamide
MH  - Male
MH  - Middle Aged
MH  - Therapeutic Equivalency
MH  - Young Adult
EDAT- 2012/06/23 06:00
MHDA- 2012/12/28 06:00
CRDT- 2012/06/23 06:00
PHST- 2012/03/16 00:00 [received]
PHST- 2012/03/30 00:00 [accepted]
PHST- 2012/06/23 06:00 [entrez]
PHST- 2012/06/23 06:00 [pubmed]
PHST- 2012/12/28 06:00 [medline]
AID - 000339077 [pii]
AID - 10.1159/000339077 [doi]
PST - ppublish
SO  - Pharmacology. 2012;90(1-2):40-6. doi: 10.1159/000339077. Epub 2012 Jun 21.