Thioguanine

The Basics

What is Thioguanine?

Used to treat acute myeloid leukemia.

Brand names for Thioguanine

Tabloid

How Thioguanine is classified

Antimetabolites, Antineoplastic Agents

Thioguanine During Pregnancy

Thioguanine pregnancy category

Category DNote that the FDA has deprecated the use of pregnancy categories, so for some medications, this information isn’t available. We still think it’s useful to list historical info, however, given what a common proxy this has been in the past.

What we know about taking Thioguanine while pregnant

Drugs such as thioguanine are potential mutagens and teratogens. Thioguanine may cause fetal harm when administered to a pregnant woman. Thioguanine has been shown to be teratogenic in rats when given in doses 5 times the human dose. When given to the rat on the 4th and 5th days of gestation, 13% of surviving placentas did not contain fetuses, and 19% of offspring were malformed or stunted. The malformations noted included generalized edema, cranial defects, and general skeletal hypoplasia, hydrocephalus, ventral hernia, situs inversus, and incomplete development of the limbs. There are no adequate and well-controlled studies in pregnant women. 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. Precautions PRECAUTIONS General: Although the primary toxicity of thioguanine is myelosuppression, other toxicities have occasionally been observed, particularly when thioguanine is used in combination with other cancer chemotherapeutic agents. A few cases of jaundice have been reported in patients with leukemia receiving thioguanine. Among these were 2 adult male patients and 4 pediatric patients with acute myelogenous leukemia and an adult male with acute lymphocytic leukemia who developed hepatic veno-occlusive disease while receiving chemotherapy for their leukemia. Six patients had received cytarabine prior to treatment with thioguanine, and some were receiving other chemotherapy in addition to thioguanine when they became symptomatic. While hepatic veno-occlusive disease has not been reported in patients treated with thioguanine alone, it is recommended that thioguanine be withheld if there is evidence of toxic hepatitis or biliary stasis, and that appropriate clinical and laboratory investigations be initiated to establish the etiology of the hepatic dysfunction. Deterioration in liver function studies during thioguanine therapy should prompt discontinuation of treatment and a search for an explanation of the hepatotoxicity. Administration of live vaccines to immunocompromised patients should be avoided. Laboratory Tests: Prescribers should be aware that some laboratories offer testing for TPMT deficiency (see WARNINGS). 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. It may be advisable to perform liver function tests more frequently in patients with known pre-existing liver disease or in patients who are receiving thioguanine and other hepatotoxic drugs. Patients should be instructed to discontinue thioguanine immediately if clinical jaundice is detected (see WARNINGS).

Taking Thioguanine While Breastfeeding

What are recommendations for lactation if you're taking Thioguanine?

Most sources consider breastfeeding to be contraindicated during maternal antineoplastic drug therapy, although antimetabolites such as thioguanine appear to pose the least risk to breastfed infants.[1] Thioguanine levels in milk are reportedly low. Thioguanine nucleosides are active intracellular metabolites of azathioprine and have been measured in breastmilk and in infant serum following maternal use of azathioprine as an immunosuppressant. Although amounts in milk were low in breastmilk and mostly undetectable in infant serum, relatively low dosages of azathioprine were used. After high-dose chemotherapy, it might be possible to breastfeed safely during intermittent therapy with an appropriate period of breastfeeding abstinence. Although no data are available to determine an appropriate period to withhold breastfeeding, the drug’s terminal half-life suggests that withholding breastfeeding for 4 days may be sufficient. Chemotherapy may adversely affect the normal microbiome and chemical makeup of breastmilk.[2]

Maternal / infant drug levels

Most sources consider breastfeeding to be contraindicated during maternal antineoplastic drug therapy, although antimetabolites such as thioguanine appear to pose the least risk to breastfed infants.[1] Thioguanine levels in milk are reportedly low. Thioguanine nucleosides are active intracellular metabolites of azathioprine and have been measured in breastmilk and in infant serum following maternal use of azathioprine as an immunosuppressant. Although amounts in milk were low in breastmilk and mostly undetectable in infant serum, relatively low dosages of azathioprine were used. After high-dose chemotherapy, it might be possible to breastfeed safely during intermittent therapy with an appropriate period of breastfeeding abstinence. Although no data are available to determine an appropriate period to withhold breastfeeding, the drug’s terminal half-life suggests that withholding breastfeeding for 4 days may be sufficient. Chemotherapy may adversely affect the normal microbiome and chemical makeup of breastmilk.[2]

Possible effects of Thioguanine on milk supply

Relevant published information was not found as of the revision date.

Possible alternatives to Thioguanine

None listed