Thioguanine

What is Thioguanine?

• Thioguanine (Tabloid) (also referred to as 6-thioguanine and as tioguanine) is a purine analogue that is used in the therapy of acute and chronic myelogenous leukemias.

Thioguanine synthesis

Tioguanine

6-Thioguanine 3D ball

What are the uses of this medicine?

Thioguanine is approved to be used as remission induction therapy and remission consolidation therapy to treat:

• Acute myeloid leukemia (AML)

• However, it is not recommended for use during maintenance therapy or similar long-term continuous treatments due to the high risk of liver toxicity.

How does this medicine work?

• Thioguanine (thye" oh gwa' neen) is a thiopurine, a purine analogue and antimetabolite.
• It is a derivative of mercaptopurine (2-amino-6-mercaptopurine) and, like its parent molecule, inhibits purine metabolism, thus blocking DNA, RNA and subsequent protein synthesis.
• Thioguanine also has antiinflammatory activity.

Who Should Not Use this medicine ?

This medicine cannot be used in patients:

• whose disease has demonstrated prior resistance to this drug.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.
• Be sure to mention any of the following:
• aminosalicylates such as mesalamine (Apriso, Asacol, Pentasa, others), olsalazine (Dipentum), and sulfasalazine (Azulfidine).
• Also tell your doctor and pharmacist about all the medications you are taking so they can check whether any of your medications may increase the risk that you will develop liver damage during your treatment with thioguanine.

Is this medicine FDA approved?

• Thioguanine was approved for use in the United States in 1966 and is commonly used in the therapy of acute and chronic myelogenous (nonlymphocytic) leukemias.
• Thioguanine has also been used off-label to treat autoimmune diseases as a steroid sparing agent.

How should this medicine be used?

Recommended dosage:

• The usual initial dosage for pediatric patients and adults is approximately 2 mg/kg of body weight per day.
• If, after 4 weeks on this dosage, there is no clinical improvement and no leukocyte or platelet depression, the dosage may be cautiously increased to 3 mg/kg/day.
• The total daily dose may be given at one time.

Administration:

• Thioguanine comes as a tablet to take by mouth usually once a day.
• The length of treatment depends on the types of drugs you are taking, how well your body responds to them, and the type of cancer you have.
• Take thioguanine at around the same time every day.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As tablets for oral administration

This medicine is available in fallowing brand namesː

• Tabloid

What side effects can this medication cause?

The most common side effects of this medicine include:

• myelosuppression
• pancytopenia
• Hyperuricemia
• nausea
• vomiting
• anorexia
• stomatitis
• Intestinal
• necrosis
• perforation
• Hepatic Effects

What special precautions should I follow?

• Patients should be informed that the major toxicities of thioguanine are related to myelosuppression, hepatotoxicity, and gastrointestinal toxicity.
• It is advisable to monitor liver function tests (serum transaminases, alkaline phosphatase, bilirubin) at weekly intervals when first beginning therapy and at monthly intervals thereafter.
• Do not have any vaccinations without talking to your doctor. Administration of live vaccines to immunocompromised patients should be avoided.
• Thioguanine therapy is associated with minor, usually transient and asymptomatic elevations in serum aminotransferase levels and has also been linked to rare instances of cholestatic acute liver injury and to chronic liver injury, resulting in portal hypertension due to nodular regenerative hyperplasia.
• It is not recommended for use during maintenance therapy or similar long-term continuous treatments due to the high risk of liver toxicity

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• nausea
• vomiting
• malaise
• hypertension,
• diaphoresis
• myelosuppression
• azotemia

Management of overdosage:

• It is not known whether thioguanine is dialyzable.
• Hemodialysis is thought to be of marginal use due to the rapid intracellular incorporation of thioguanine into active metabolites with long persistence.
• There is no known pharmacologic antagonist of thioguanine.
• The drug should be discontinued immediately if unintended toxicity occurs during treatment.
• Severe hematologic toxicity may require supportive therapy with platelet transfusions for bleeding, and granulocyte transfusions and antibiotics if sepsis is documented.
• If a patient is seen immediately following an accidental overdosage of the drug, it may be useful to induce emesis.

Can this medicine be used in pregnancy?

• Thioguanine may cause fetal harm when administered to a pregnant woman.
• If this drug is used during pregnancy, or if the patient becomes pregnant while taking the drug, the patient should be apprised of the potential hazard to the fetus.
• Women of childbearing potential should be advised to avoid becoming pregnant.

Can this medicine be used in children?

• The safety and effectiveness of Thioguanine in pediatric patients have been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• THIOGUANINE

Inactive ingredients:

• ACACIA
• LACTOSE MONOHYDRATE
• MAGNESIUM STEARATE
• STARCH, POTATO
• STEARIC ACID

Who manufactures and distributes this medicine?

Manufactured by:

• Excella GmbH & Co.KG, Feucht, Germany

Distributed by:

• Prasco Laboratories
• Mason, OH USA
• Made in Germany

What should I know about storage and disposal of this medication?

• Store at 15° to 25°C (59° to 77°F) in a dry place.

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• Dailymed label info on Thioguanine
• FDA Thioguanine

Thioguanine Resources
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