Chemical formula: C₁₆H₁₈ClN₃S Molecular mass: 319.85 g/mol PubChem compound: 6099
In vivo, in low concentration, methylthioninium chloride speeds up the conversion of methaemoglobin to haemoglobin. Methylthioninium chloride has been observed to stain tissues selectively. Its use in parathyroid surgery (not indicated) has induced adverse CNS effects when administered concomitantly with serotonergic medicinal products.
The efficacy of methylthioninium chloride for the treatment of methaemoglobinaemia in peadiatric population was demonstrated in two retrospective studies and one open randomised clinical trial. Case reports of efficacy are also available in literature.
After intravenous administration Methylthioninium chloride is rapidly taken up by the tissues. It is also well absorbed by the oral route. The majority of the dose is excreted in the urine, usually in the form of leucomethylthioninium chloride.
The estimated terminal half-life of methylthioninium chloride after intravenous administration is 26.7h.
Methylthioninium chloride is not an in vitro inducer of CYP2B6 and CYP3A4.
Methylthioninium chloride is an in vitro inhibitor of P-gp.
Methylthioninium chloride is not an in vitro substrate for BCRP or OCT2 and is not an in vitro inhibitor of BCRP, OAT1 or OAT3.
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