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White plastic supplement bottle labeled "Methylene Blue 10mg, Batch No.002, 10-05-2025" with two blue capsules beside it on a neutral beige background — pharmaceutical product packaging for nootropic or research chemical
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Methylene blue USP grade 100x10mg

Methylene blue USP grade 100x10mg

€60,00 EUR
Taxes included.

                                          NOT FOR HUMAN CONSUMPTION

Methylene blue is a phenothiazine redox dye with multiple pharmacologies. Clinically it’s FDA-approved for acquired methemoglobinemia (it accepts electrons from NADPH-methemoglobin reductase as leucomethylene blueand reduces Fe³⁺→Fe²⁺ to restore O₂ carriage). Beyond this, MB inhibits nitric-oxide synthase and soluble guanylyl cyclase (sGC) (countering pathologic vasodilation), acts as a photosensitizer for antimicrobial photodynamic therapy (aPDT), shuttles electrons in mitochondria, and is a potent reversible MAO-A inhibitor (important for drug interactions).

Additional Benefits of Methylene Blue Now Under Investigation

Benefit Key take-aways
1 Vasoplegic shock rescue (sepsis/post-CPB) IV MB can raise MAP and reduce catecholamine dose by blocking NO–sGC–cGMP signalling; early use in vasoplegia (post-cardiac surgery, septic shock) shows hemodynamic benefit in RCTs/series; mortality data remain mixed. <br/><em>Critical Care; Anesthesiology</em>
2 Ifosfamide-induced encephalopathy Case series and protocols support 1–2 mg/kg IV q4–8 h to reverse neurotoxicity, likely via redox re-routing (NAD⁺/NADH) and monoamine oxidase modulation. <br/><em>Journal of Clinical Oncology; Supportive Care in Cancer</em>
3 Tau aggregation & neurodegeneration MB/LMTM (leuco-methylthioninium) inhibits tau aggregation and supports mitochondria; Alzheimer’s trials show mixed outcomes (signals in monotherapy subsets), with dosing/formulation under refinement. <br/><em>Journal of Alzheimer’s Disease; The Lancet Neurology</em>
4 Mitochondrial rescue & neuroprotection At low doses, MB bypasses complex I/III blocks, improves ATP generation, reduces ROS, and shows retinal/optic-nerve protection in models and small studies. <br/><em>PNAS; Investigative Ophthalmology & Visual Science</em>
5 Antimicrobial photodynamic therapy (aPDT) MB + 630–670 nm light produces singlet oxygen, killing planktonic and biofilm bacteria (including MRSA/P. aeruginosa) and fungi; used in chronic wounds, dentistry, ENT pilots. <br/><em>Antimicrobial Agents & Chemotherapy; Journal of Clinical Periodontology</em>
6 Antimalarial partner & transmission-blocking Added to artemisinin regimens, MB lowers gametocytemia and may reduce transmission; GI/urine discoloration and G6PD-related hemolysis risk require screening. <br/><em>The Lancet Infectious Diseases; Malaria Journal</em>
7 Dermatologic/anti-photoaging (topical) MB creams show fibroblast rejuvenation, ↑ collagen genes, ↓ senescence markers, and improved hydration/wrinkles in small trials. <br/><em>Redox Biology; Dermatologic Therapy</em>
8 Refractory ischemic priapism Intracavernosal MB inhibits NO–sGC, offering rescue when alpha-agonists fail before shunting. <br/><em>Urology; BJU International</em>
9 Peri-anaphylaxis vasoplegia As adjunct in refractory hypotension after anaphylaxis or spinal anesthesia, MB can restore vascular tone via sGC blockade; evidence largely from series. <br/><em>Annals of Allergy, Asthma & Immunology; British Journal of Anaesthesia</em>

2. Molecular Mechanism of Action

2.1 Target Pharmacodynamics

  • RBC redox cycling: MB ⇄ leucomethylene blue accepts electrons from NADPH-MetHb reductase, reducing MetHb → Hb.

  • Vascular tone: NOS and sGC inhibition ↓ cGMP → reverses pathologic vasodilation in vasoplegia.

  • MAO-A inhibition: Potent, reversible inhibition → serotonin-syndrome risk with serotonergic drugs.

  • Mitochondrial electron shuttle: Accepts/donates electrons between NADH ↔ cytochrome c, bypassing ETC blocks.

  • Photosensitizer: Upon red-light activation, generates singlet oxygen/ROS for aPDT.

2.2 Down-stream Biology

Pathway Functional outcome Context
NADPH-MetHb reductase Restores O₂ carriage Methemoglobinemia
NO–sGC–cGMP axis ↑ MAP, vasoconstrictive tone Vasoplegic shock, priapism
MAO-A inhibition ↑ synaptic monoamines; DDI risk CNS/pharmacology
ETC bypass (redox) ↑ ATP, ↓ ROS Neuro/retina, ischemia–reperfusion
aPDT (ROS burst) Rapid microbicidal & anti-biofilm Wounds, dental/ENT

3. Pharmacokinetics

  • Routes: IV (methemoglobinemia, vasoplegia), oral (historical/adjunct), topical, intracavernosal (rescue), intranasal/neb (investigational aPDT).

  • Onset: IV minutes for MetHb/MAP effects.

  • Half-life: Biphasic; reports ~5–24 h (formulation-dependent).

  • Distribution/biotransformation: Rapid tissue distribution; reduced to leuco-MB intracellularly; renal excretion(blue-green urine), some biliary.

  • Device interference: Transient SpO₂ under-reading (absorbs at 660 nm).

4. Pre-clinical and Translational Evidence

4.1 Vasoplegic Syndromes

In sepsis and post-cardiopulmonary-bypass vasoplegia, MB improves MAP and reduces vasopressor needs; timing (early vs rescue), dose, and patient selection are key determinants; outcome effects are under active study.

4.2 Oncology/Neurodegeneration

Tau-targeting LMTM programs show dose/formulation-dependent cognitive outcomes; mitochondrial support and anti-aggregation continue to be explored in AD/FTD.

4.3 Anti-infective aPDT

Topical/oral cavity MB-aPDT clears biofilms, reduces peri-implant mucositis/periodontitis indices, and accelerates chronic-wound granulation; standardized dosing and light fluence remain to be harmonized.

4.4 Ifosfamide Encephalopathy & Others

Observational cohorts report neurologic recovery after MB in IIE; additional uses include priapism rescue, sentinel-node mapping, and urologic staining.

Evidence quality note: Robust for methemoglobinemia; moderate/heterogeneous for vasoplegia and IIE (controlled but small); emerging for aPDT, dermatology, and neurodegeneration.

5. Emerging Clinical Interests

Field Rationale Current status
Vasoplegic shock (sepsis/post-CPB) sGC blockade complements vasopressors RCTs/series; practice heterogeneity
Ifosfamide encephalopathy Redox/MAO pathways Protocolized rescue in centers
Alzheimer’s/FTD (LMTM) Tau inhibition + mitochondrial support Mixed trials; next-gen formulations
Chronic wounds/dentistry (aPDT) Anti-biofilm + pro-healing Early clinical adoption
Retinal/optic neuroprotection ETC bypass, anti-ROS Small human/mechanistic
Antimalarial partner Gametocyte kill/transmission block Regional trials
Priapism (refractory) NO–sGC inhibition Salvage case series

6. Safety and Tolerability

  • Common: Blue/green urine, skin/scleral tint, nausea, dizziness, headache, dysgeusia.

  • Hematology: Hemolysis risk in G6PD deficiency; screen when feasible. High doses can worsen methemoglobinemia (paradoxical).

  • Neurologic/psychiatric: Serotonin syndrome possible with SSRIs/SNRIs/MAOIs/linezolid/tramadol, etc. (MB is a potent MAO-A inhibitor).

  • Cardiovascular: ↑ SVR/MAP desired in vasoplegia; watch for hypertension/ischemia in susceptible patients.

  • Pulmonary: Can transiently lower SpO₂ readings (optical artifact).

  • Pregnancy/Neonates: Avoid—risk of fetal/neonatal hemolysis and hyperbilirubinemia; crosses placenta.

  • Dosing considerations: Typical IV 1–2 mg/kg (slow push/infusion) with repeat dosing per protocol; monitor MetHb, ABG, hemodynamics.

Comparative safety matrix (vasoplegia context)

Concern Methylene blue Hydroxocobalamin Vasopressin
Primary mechanism NOS/sGC inhibition NO scavenger (cobalt) V1 receptor agonist
Effect on MAP Rapid ↑; catecholamine-sparing Rapid ↑; catecholamine-sparing ↑ SVR with low arrhythmia risk
Key risks MAO-A DDIs, G6PD hemolysis, SpO₂ artifact Chromaturia, potential oxalate, interference with labs Ischemia at high dose, hyponatremia
Special notes Can worsen MetHb at high dose Useful when MB contraindicated Synergizes with MB in rescue

7. Regulatory Landscape

  • Approved: Acquired methemoglobinemia (parenteral MB).

  • Common off-label: Vasoplegic shock, ifosfamide encephalopathy, priapism rescue, aPDT (topical/oral cavity).

  • Investigational: Tau-targeting LMTM, retinal neuroprotection, antimalarial partner.

  • Supply: Use GMP-grade MB (sterile, USP) for IV; compounded/non-sterile dyes are unsafe IV.

8. Future Directions

  • Precision use in vasoplegia: Timing (early vs rescue), dose–response, and phenotype selection (e.g., high NO/cGMP signatures).

  • Neurodegeneration: Optimize LMTM pharmacokinetics and identify tau-positive, monotherapy-responsivesubgroups.

  • Standardize aPDT: Dose, fluence, and outcomes for wounds/dentistry/ENT; head-to-head vs antibiotics.

  • Mitochondrial medicine: Define dose window for ETC support without MAO-A adverse effects.

  • Safety registries: Serotonin-syndrome pharmacovigilance; G6PD screening pathways; pregnancy/neonatal outcomes.

Selected References

  • Anesthesiology; Critical Care — Vasoplegic shock trials/series with MB (post-CPB, sepsis).

  • Journal of Clinical Oncology; Supportive Care in Cancer — Ifosfamide-induced encephalopathy reversal protocols.

  • The Lancet Neurology; Journal of Alzheimer’s Disease — LMTM (methylthioninium) in tauopathies.

  • PNAS; Redox Biology — Mitochondrial electron-shuttling and antioxidant properties.

  • Antimicrobial Agents & Chemotherapy; Journal of Clinical Periodontology — MB-mediated aPDT in wounds/dentistry.

  • The Lancet Infectious Diseases; Malaria Journal — MB as an antimalarial partner and transmission-blocking agent.

  • Investigative Ophthalmology & Visual Science — Retinal/optic neuroprotection studies.

  • Urology; BJU International — MB for refractory priapism via NO–sGC inhibition.