PMID- 11352441
OWN - NLM
STAT- MEDLINE
DCOM- 20010920
LR  - 20181130
IS  - 0312-5963 (Print)
IS  - 0312-5963 (Linking)
VI  - 40 Suppl 1
DP  - 2001
TI  - Evaluation of the influence of antacids and H2 antagonists on the absorption of 
      moxifloxacin after oral administration of a 400mg dose to healthy volunteers.
PG  - 39-48
AB  - OBJECTIVE: To determine the effect of concomitant administration of the antacid 
      Maalox 70 or the histamine H2 receptor antagonist ranitidine on the 
      bioavailability of moxifloxacin. DESIGN: These were nonblinded, randomised, 
      crossover studies performed in healthy volunteers. PARTICIPANTS: 24 healthy males 
      aged 22 to 39 years (study 1; n = 12) and 24 to 43 years (study 2; n = 12) were 
      included in these studies. METHODS: In study 1, 12 participants received 
      ranitidine 150mg twice daily during a 3-day pretreatment phase and 1 tablet of 
      ranitidine together with a single 400mg dose of moxifloxacin on the profile day. 
      In study 2, 12 participants received a single 400mg dose of moxifloxacin alone 
      (treatment A), simultaneously with Maalox 70 10ml (treatment B), or with Maalox 
      70 10ml given 4 hours before (treatment C) or 2 hours after (treatment D) the 
      fluoroquinolone. In treatments B, C and D, administration of the antacid (10ml, 1 
      hour after each meal) was continued for 2 days. Plasma and urine samples were 
      obtained for determination of the pharmacokinetic parameters of moxifloxacin. 
      RESULTS: Coadministration of moxifloxacin with ranitidine showed lack of 
      interaction for area under the plasma concentration-time curve extrapolated to 
      infinity (AUCinfinity) [35.5 versus 34.3 mg/L x h with versus without ranitidine; 
      relative bioavailability 103%, 90% confidence interval (CI) 97.7 to 109.3%] and 
      maximum plasma concentration (Cmax) [2.98 versus 2.76 mg/L with versus without 
      ranitidine; ratio 107.9%, 90% CI 90.5 to 128.6%]. When moxifloxacin was given 
      simultaneously with Maalox 70, AUCinfinity ( 14.7 mg/L x h) and Cmax (1.00 mg/L) 
      were reduced by approximately 60%. When the antacid was given 4 hours before or 2 
      hours after the fluoroquinolone, AUCinfinity values (28.0 and 26.7 versus 34.3 
      mg/L x h) were moderately reduced (by <27%), terminal elimination half-life 
      values declined by approximately 24% (9.4 and 9.3 versus 12.3 hours) compared 
      with moxifloxacin alone and Cmax values were almost unchanged (2.55 and 2.38 
      versus 2.57 mg/L). The mean bioavailabilities corrected for the elimination rate 
      constants (lambdaz) were 101% (antacid given 4 hours before moxifloxacin) and 98% 
      (antacid given 2 hours after moxifloxacin), indicating that Maalox 70 may 
      interfere with the gastrointestinal recirculation of moxifloxacin. CONCLUSIONS: 
      The bioavailability of moxifloxacin is not affected by concurrent administration 
      of ranitidine. Absorption of moxifloxacin is impaired by concomitant 
      administration of aluminium- and magnesium-containing antacids and administration 
      of these agents should be staggered. An interval of 2 hours before or 4 hours 
      after taking the antacid ensures that the effect of the interaction is not 
      clinically relevant.
FAU - Stass, H
AU  - Stass H
AD  - Pharma Research Centre, Institute of Clinical Pharmacology, Bayer AG, Wuppertal, 
      Germany. Heino.Stass.hs@bayer-ag.de
FAU - Bottcher, M F
AU  - Bottcher MF
FAU - Ochmann, K
AU  - Ochmann K
LA  - eng
PT  - Clinical Trial
PT  - Journal Article
PT  - Randomized Controlled Trial
PL  - Switzerland
TA  - Clin Pharmacokinet
JT  - Clinical pharmacokinetics
JID - 7606849
RN  - 0 (Antacids)
RN  - 0 (Anti-Infective Agents)
RN  - 0 (Aza Compounds)
RN  - 0 (Drug Combinations)
RN  - 0 (Fluoroquinolones)
RN  - 0 (Histamine H2 Antagonists)
RN  - 0 (Quinolines)
RN  - 37317-08-1 (aluminum hydroxide, magnesium hydroxide, drug combination)
RN  - 5QB0T2IUN0 (Aluminum Hydroxide)
RN  - 884KT10YB7 (Ranitidine)
RN  - NBZ3QY004S (Magnesium Hydroxide)
RN  - U188XYD42P (Moxifloxacin)
SB  - IM
MH  - Administration, Oral
MH  - Adult
MH  - Aluminum Hydroxide/*pharmacology
MH  - Antacids/*pharmacology
MH  - Anti-Infective Agents/administration & dosage/blood/*pharmacokinetics/urine
MH  - Area Under Curve
MH  - *Aza Compounds
MH  - Biological Availability
MH  - Chromatography, High Pressure Liquid
MH  - Cross-Over Studies
MH  - Drug Combinations
MH  - Drug Interactions
MH  - *Fluoroquinolones
MH  - Half-Life
MH  - Histamine H2 Antagonists/*pharmacology
MH  - Humans
MH  - Hydrogen-Ion Concentration
MH  - Intestinal Absorption
MH  - Magnesium Hydroxide/*pharmacology
MH  - Male
MH  - Metabolic Clearance Rate
MH  - Moxifloxacin
MH  - *Quinolines
MH  - Ranitidine/*pharmacology
EDAT- 2001/05/16 10:00
MHDA- 2001/09/21 10:01
CRDT- 2001/05/16 10:00
PHST- 2001/05/16 10:00 [pubmed]
PHST- 2001/09/21 10:01 [medline]
PHST- 2001/05/16 10:00 [entrez]
AID - 10.2165/00003088-200140001-00006 [doi]
PST - ppublish
SO  - Clin Pharmacokinet. 2001;40 Suppl 1:39-48. doi: 10.2165/00003088-200140001-00006.