Pharmacokinetics and organ distribution of intravenous and oral methylene blue.

Peter C, Hongwan D, Küpfer A, Lauterburg BH

European journal of clinical pharmacology1 Jun 2000Cited by 267 (Europe PMC)

PMID10952480DOI10.1007/s002280000124PepBankPUB-10952480

Publisher page PubMedAsk about this study

Summary

The text of this summary is not shown here, because the article license does not allow reuse. Read it at the source (opens in a new tab)

Text rights: Publisher copyright. Results still quote short attributed sentences.

Results from this study8

7 results from studies that gave the peptide. 3 results from people.

01HumanNon-randomized trialPharmacokinetics
In volunteers, intravenous methylene blue had a multiphasic blood time course and an estimated terminal half-life of 5.25 h.
In plain wordsIn volunteers, intravenous methylene blue had an estimated terminal half-life of 5.25 h.
Peptide
Methylene blue
Outcome
Not applicableTerminal half-life
Study
n = 7
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
100 mg · intravenousAs given in this study (human).
Measurements
Terminal half-life
5.25 h
intravenous methylene blue, whole blood, estimated
Source sentences
Summary
The time course of methylene blue in whole blood after i.v. administration showed a multiphasic time course with an estimated terminal half-life of 5.25 h.
1 context sentence(design, population, supporting numbers)
Summary · context
The concentration of methylene blue in whole blood was measured using high-performance liquid chromatography in seven volunteers after i.v. and oral administration of 100 mg methylene blue with and without mesna.
Report a problemFND-1095248001
02HumanNon-randomized trialPharmacokinetics
In volunteers, oral methylene blue produced lower blood exposure than intravenous dosing, with AUC 9 versus 137 nmol/min/ml.
In plain wordsIn volunteers, oral methylene blue produced less blood exposure than intravenous methylene blue.
Peptide
Methylene blue
Outcome
DecreaseBlood AUC after oral versus intravenous dosing
Study
n = 7
Comparator
Intravenous methylene blue
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
100 mg · oralAs given in this study (human).
Measurements
Blood AUC
9 nmol/min/ml
oral methylene blue
Blood AUC
137 nmol/min/ml
intravenous methylene blue
Source sentences
Summary
Following oral administration, the area under the concentration-time curve was much lower (9 nmol/min/ml vs 137 nmol/min/ml).
1 context sentence(design, population, supporting numbers)
Summary · context
The concentration of methylene blue in whole blood was measured using high-performance liquid chromatography in seven volunteers after i.v. and oral administration of 100 mg methylene blue with and without mesna.
Report a problemFND-1095248002
03HumanNon-randomized trialPharmacokinetics
In volunteers, urinary excretion of methylene blue and its leucoform was moderately higher after intravenous than oral administration.
In plain wordsIn volunteers, urine excretion of methylene blue and its leucoform was moderately higher after intravenous than oral dosing.
Peptide
Methylene blue
Outcome
IncreaseUrinary excretion of methylene blue and leucoform
Study
n = 7
Comparator
Oral methylene blue
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
100 mg · intravenous and oralAs given in this study (human).
Measurements
Urinary excretion of methylene blue and leucoform
18 % dose
first of two values in '18% vs 28% dose'; source does not label which route
Urinary excretion of methylene blue and leucoform
28 % dose
second of two values in '18% vs 28% dose'; source does not label which route
Source sentences
Summary
The urinary excretion of methylene blue and its leucoform was only moderately higher after i.v. administration (18% vs 28% dose).
1 context sentence(design, population, supporting numbers)
Summary · context
The concentration of methylene blue in whole blood was measured using high-performance liquid chromatography in seven volunteers after i.v. and oral administration of 100 mg methylene blue with and without mesna.
Report a problemFND-1095248004
04AnimalAnimal study (in vivo)Pharmacokinetics
In rats, intraduodenal methylene blue produced higher intestinal wall concentrations than intravenous methylene blue.
In plain wordsIn rats, methylene blue given into the duodenum produced higher intestinal wall levels than intravenous methylene blue.
Peptide
Methylene blue
Outcome
IncreaseIntestinal wall concentration
Study
ratn: not reported in source
rats
Comparator
Intravenous methylene blue
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · intraduodenalAs given in this study (rat).
Source sentences
Summary
Intraduodenal administration to rats resulted in higher concentrations in intestinal wall and liver but lower concentrations in whole blood and brain than i.v. methylene blue.
1 context sentence(design, population, supporting numbers)
Summary · context
The distribution of methylene blue in different tissues was measured in rats after intraduodenal and i.v. application.
Report a problemFND-1095248005
05AnimalAnimal study (in vivo)Pharmacokinetics
In rats, intraduodenal methylene blue produced higher liver concentrations than intravenous methylene blue.
In plain wordsIn rats, methylene blue given into the duodenum produced higher liver levels than intravenous methylene blue.
Peptide
Methylene blue
Outcome
IncreaseLiver concentration
Study
ratn: not reported in source
rats
Comparator
Intravenous methylene blue
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · intraduodenalAs given in this study (rat).
Source sentences
Summary
Intraduodenal administration to rats resulted in higher concentrations in intestinal wall and liver but lower concentrations in whole blood and brain than i.v. methylene blue.
1 context sentence(design, population, supporting numbers)
Summary · context
The distribution of methylene blue in different tissues was measured in rats after intraduodenal and i.v. application.
Report a problemFND-1095248006
06AnimalAnimal study (in vivo)Pharmacokinetics
In rats, intraduodenal methylene blue produced lower whole blood concentrations than intravenous methylene blue.
In plain wordsIn rats, methylene blue given into the duodenum produced lower blood levels than intravenous methylene blue.
Peptide
Methylene blue
Outcome
DecreaseWhole blood concentration
Study
ratn: not reported in source
rats
Comparator
Intravenous methylene blue
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · intraduodenalAs given in this study (rat).
Source sentences
Summary
Intraduodenal administration to rats resulted in higher concentrations in intestinal wall and liver but lower concentrations in whole blood and brain than i.v. methylene blue.
1 context sentence(design, population, supporting numbers)
Summary · context
The distribution of methylene blue in different tissues was measured in rats after intraduodenal and i.v. application.
Report a problemFND-1095248007
07AnimalAnimal study (in vivo)Pharmacokinetics
In rats, intraduodenal methylene blue produced lower brain concentrations than intravenous methylene blue.
In plain wordsIn rats, methylene blue given into the duodenum produced lower brain levels than intravenous methylene blue.
Peptide
Methylene blue
Outcome
DecreaseBrain concentration
Study
ratn: not reported in source
rats
Comparator
Intravenous methylene blue
Outcome group
Pharmacokinetics · Pharmacology
Studied dose
Dose not stated · intraduodenalAs given in this study (rat).
Source sentences
Summary
Intraduodenal administration to rats resulted in higher concentrations in intestinal wall and liver but lower concentrations in whole blood and brain than i.v. methylene blue.
1 context sentence(design, population, supporting numbers)
Summary · context
The distribution of methylene blue in different tissues was measured in rats after intraduodenal and i.v. application.
Report a problemFND-1095248008

Studies that did not test the peptide alone1

In this study, Methylene blue was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking Methylene blue.

08HumanNot a test of Methylene blue aloneNon-randomized trialPharmacokinetics
In volunteers, mesna co-administration did not alter methylene blue pharmacokinetics.
In plain wordsIn volunteers, adding mesna did not change methylene blue pharmacokinetics compared with methylene blue alone.
Peptide
Methylene blue
Outcome
No significant changeEffect of mesna on pharmacokinetics
Study
n = 7
Comparator
Methylene blue without mesna
Outcome group
Pharmacokinetics · Pharmacology
Source sentences
Summary
Co-administration of mesna, which could influence distribution by ion-pairing, did not alter the pharmacokinetics.
1 context sentence(design, population, supporting numbers)
Summary · context
The concentration of methylene blue in whole blood was measured using high-performance liquid chromatography in seven volunteers after i.v. and oral administration of 100 mg methylene blue with and without mesna.
In this study, Methylene blue was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Methylene blue.
Report a problemFND-1095248003

AI wrote and checked these results. AI can make mistakes, so check important results against the source.

Registered trials1

Trials this study reports on, or that list this study as a reference. Registry data from ClinicalTrials.gov.

1 trial · 1 completed · 1 with posted results · source ClinicalTrials.gov (opens in a new tab)

CompletedPhase 2Results postedNCT02380573

Effects of Methylene Blue in Healthy Aging, Mild Cognitive Impairment and Alzheimer's Disease

The University of Texas Health Science Center at San Antonion = 117Jul 2015 to Jul 2023

Mild Cognitive Impairment · MCI · Aging · Alzheimer's Disease · AD

Trial page ClinicalTrials.govUpdated 19 Sept 2024

Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
14 Oct 2026, 05:02 UTC
Study results updated
Version 1
14 Oct 2026, 01:46 UTC
First added · source update from Europe PMC

Subjects

Terms as the source lists them.

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