Methylene Blue Injection 1%

(FOR SLOW INTRAVENOUS ADMINISTRATION)

Rx only

Methylene Blue Injection may cause serious or fatal serotonergic syndrome when used in combination with serotonergic drugs. Avoid concomitant use of Methylene Blue Injection with selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), and monoamine oxidase inhibitors (see WARNINGS and PRECAUTIONS, Drug Interactions).

Methylene Blue Injection is a sterile solution of Phenothiazin-5-ium, 3, 7-bis (dimethylamino)-, chloride, trihydrate. Each mL contains methylene blue, 10 mg in water for injection q.s. pH adjusted with hydrochloric acid and/or sodium hydroxide when necessary.

The structural formula is:

Structural Formula

The molecular formula is:

C₁₆H₁₈ClN₃S • 3H₂O       MW = 373.90

Methylene blue will produce two opposite actions on hemoglobin. Low concentrations will convert methemoglobin to hemoglobin. High concentrations convert the ferrous iron of reduced hemoglobin to ferric iron which results in the formation of methemoglobin.

Methylene blue is metabolized in the body to leukomethylene blue which is excreted primarily in the urine. Some unchanged drug is also excreted in the urine. (1)

Drug-induced methemoglobinemia.

Methylene blue can cause fetal harm when administered to a pregnant woman. An association exists between the use of methylene blue in amniocentesis and atresia of the ileum and jejunum, ileal occlusions and other adverse effects in the neonate. (2, 3) Methylene blue is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.

Intraspinal and subcutaneous injections are contraindicated.

Methylene blue is contraindicated in patients with a known hypersensitivity to the drug.

Methylene blue should not be given by subcutaneous or intrathecal injection.

0.1 to 0.2 mL per kg body weight (0.045 to 0.09 mL per pound body weight). Inject methylene blue intravenously very slowly over a period of several minutes.

Methylene blue must be injected intravenously very slowly over a period of several minutes to prevent local high concentration of the compound from producing additional methemoglobin. Do not exceed recommended dosage.

Parenteral drug products should be inspected visually for particulate matter and discoloration, whenever solution and container permit.

Methylene Blue Injection, 1% is supplied as follows:

NDC 17478-504-01

1 mL in 2 cc (partially filled) vials in packages of 10.

NDC 17478-504-10

10 mL vials in packages of 10.

The vials are packaged with a Flip Tear-Off Seal. The seal can either be flipped normally to reveal the rubber stopper or be totally removed so the rubber stopper can be taken out of the vial. The plastic button is attached to the metal seal, which when pulled, tears the seal at the score line allowing the metal portion to be removed.

Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].

Flip Tear-Off Seal: Directions for Use:

1. With the thumb, flip the plastic button up to reveal the rubber stopper.
2. Pull the button to tear the seal at the score line and twist to remove.

1. DiSanto AR, Wagner JG. Pharmacokinetics of highly ionized drugs II: methylene blue – absorption, metabolism, and excretion in man and dog after oral administration. J Pharm Sci. 1972; 61:1086-1090.
2. Cragan JD. Teratogen update: methylene blue. Teratology. 1999; 60:42-48.
3. Kidd SA, Lancaster PA, Anderson JC, Boogert A, Fisher CC, Robertson R, et al. Fetal death after exposure to methylene blue dye during mid-trimester amniocentesis in twin pregnancy. Prenat Diagn. 1996; 16:39-47.
4. Ramsay RR, Dunford C, Gillman PK. Methylene blue and serotonin toxicity: inhibition of monoamine oxidase A (MAOA) confirms a theoretical prediction. Br J Pharmacol. 2007; 152:946-51.
5. Beutler E. G6PD Deficiency. Blood. 1994; 84:3613-3636.
6. Youngster I, Arcavi L, Schechmaster R, Akayzen Y, Popliski H, Shimonov J, Beig S, Berkovitch M. Medications and glucose-6-phosphate dehydrogenase deficiency: an evidence-based review. Drug Saf. 2010; 33:713-726.

Methylene Blue and Methylene Blue Injection were in compliance with USP #39, but differs from the Current USP #40 with respect to active assay, Impurities: Azure A, Azure B, Azure C, and unknown impurities.

AKORN

Manufactured by: Akorn, Inc.
Lake Forest, IL 60045

MB00N        Rev. 11/17

NDC 17478-504-10

Methylene Blue

Injection

1% (10 mg/mL)

For slow Intravenous administration.

10 mL Single-dose Vial

Rx only Akorn Logo

NDC 17478-504-10

Methylene Blue Injection

1% (10 mg/mL)

For slow Intravenous administration

10 Vials (10 mL each)

Rx only Akorn Logo