Provayblue Uses, Dosage, Side Effects and more

Provayblue is an oxidation-reduction agent. The intravenous form of methylene blue is approved by the FDA for the treatment of pediatric and adult patients with acquired methemoglobinemia. Historically, it has been widely used in Africa to treat malaria, but now it disappeared when chloroquine (CQ) and other drugs entered the market. Its use as an urinary tract antiseptic has also been investigated.

Methylthioninium chloride (INN, or methylene blue, proposed trade name Rember) is an investigational drug being developed by the University of Aberdeen and TauRx Therapeutics that has been shown in early clinical trials to be an inhibitor of Tau protein aggregation. The drug is of potential interest for the treatment of patients with Alzheimer's disease.

Trade Name	Provayblue
Generic	Methylene blue
Methylene blue Other Names	Azul de metileno, Basic Blue 9, C.I. basic blue 9, Chlorure de méthylthioninium, Cloruro de metiltioninio, Methylene blue, Methylenium ceruleum, Methylthioninii chloridum, Methylthioninium chloride
Weight	10mg/ml, 5mg/ml,
Type	Injectable Solution, Intravenous Solution, Injection, Intravenous
Formula	C₁₆H₁₈ClN₃S
Weight	Average: 319.85 Monoisotopic: 319.0909965
Protein binding	Methylene blue was reported to bind strongly to rabbit plasma (71–77% of bound drug).
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country	United States,
Last Updated:	January 7, 2025 at 1:49 am

Uses

Provayblue is an oxidation-reduction agent used for the treatment of pediatric and adult patients with acquired methemoglobinemia.

Indicated for the treatment of pediatric and adult patients with acquired methemoglobinemia.

Other clinical applications of methylene blue include improvement of hypotension associated with various clinical states, an antiseptic in urinary tract infections, treatment of hypoxia and hyperdynamic circulation in cirrhosis of liver and severe hepatopulmonary syndrome, and treatment of ifofosamide induced neurotoxicity.

Provayblue is also used to associated treatment for these conditions: Cystitis, Methaemoglobinaemia, Nephritis, Urethritis, Urinary tract inflammation, Diuresis

How Provayblue works

Main mechanism of action involves inhibition of nitric oxide synthase and guanylate cyclase.
In Alzheimers Disease: a mechanistic study found that methylene blue oxidizes cysteine sulfhydryl groups on tau to keep tau monomeric. One preclinical treatment study in tauopathy mice reported anti-inflammatory or neuroprotective effects mediated by the Nrf2/antioxidant response element (ARE); another reported insoluble tau reduction and a learning and memory benefit when given early.
In Methemoglobinemia: Methylene Blue acts by reacting within RBC to form leukomethylene blue, which is a reducing agent of oxidized hemoglobin converting the ferric ion (fe+++) back to its oxygen-carrying ferrous state(fe++).
As antimalarial agent: Methylene Blue, a specific inhibitor of P.falciparum glutathione reductase has the potential to reverse CQ resistance and it prevents the polymerization of haem into haemozoin similar to 4-amino-quinoline antimalarials.
For ifosfamide induced neurotoxicity: Provayblue functions as an alternate electron acceptor. It acts to reverse the NADH inhibition caused by gluconeogenesis in the liver while blocking the transformation of chloroethylamine into chloroacetaldehyde. In addition, it inhibits various amine oxidase activities, which also prevents the formation of chloroacetaldehyde.

Toxicity

LD50 = 1180 mg/kg ( Rat ).

Food Interaction

No interactions found.

Volume of Distribution

10 mg/kg (in rats).

Half Life

5–6.5 hours (after IV dose).

Clearance

3.0 ± 0.7 L/min.

Elimination Route

Excreted in urine and bile. About 75% of an oral dose excreted in urine, primarily as stabilized colorless leukomethylene blue.