Xaluprine

Xaluprine is the trade name for the oral suspension form of mercaptopurine, a medication used primarily in the treatment of acute lymphoblastic leukemia (ALL). It is an antimetabolite and a purine analog that interferes with the synthesis of nucleic acids, thereby inhibiting the proliferation of rapidly dividing cells.

Pharmacology

Mechanism of Action

Xaluprine, as a form of mercaptopurine, acts as an antimetabolite. It is a purine analog that mimics the structure of adenine and guanine, which are essential components of DNA and RNA. Once inside the cell, mercaptopurine is converted into thioinosinic acid, which inhibits the enzyme amidophosphoribosyltransferase, a key enzyme in the de novo synthesis of purine nucleotides. This inhibition leads to a reduction in the synthesis of DNA and RNA, thereby preventing cell division and proliferation, particularly in rapidly dividing cells such as cancer cells.

Pharmacokinetics

Xaluprine is administered orally. Its bioavailability is variable, ranging from 5% to 37%, due to extensive first-pass metabolism in the liver. The drug is metabolized primarily by the enzyme thiopurine S-methyltransferase (TPMT) and to a lesser extent by xanthine oxidase. The half-life of mercaptopurine is approximately 1.3 hours. It is excreted primarily through the kidneys.

Clinical Use

Indications

Xaluprine is indicated for the treatment of acute lymphoblastic leukemia (ALL) in both pediatric and adult patients. It is often used as part of a combination chemotherapy regimen.

Dosage and Administration

The dosage of Xaluprine is individualized based on the patient's body surface area and response to therapy. It is typically administered once daily. Regular monitoring of blood counts and liver function tests is essential during treatment.

Adverse Effects

Common Adverse Effects

- Myelosuppression: This is the most significant adverse effect, leading to leukopenia, thrombocytopenia, and anemia. - Hepatotoxicity: Elevated liver enzymes and jaundice may occur. - Gastrointestinal disturbances: Nausea, vomiting, and diarrhea are common.

Serious Adverse Effects

- Infections: Due to myelosuppression, patients are at increased risk of infections. - Hepatic necrosis: Severe liver damage can occur, necessitating regular monitoring.

Contraindications and Precautions

Xaluprine is contraindicated in patients with known hypersensitivity to mercaptopurine. Caution is advised in patients with impaired liver function or those with a history of thiopurine S-methyltransferase deficiency, as they are at increased risk of toxicity.

Drug Interactions

- Allopurinol: Concomitant use with allopurinol, a xanthine oxidase inhibitor, can increase the risk of mercaptopurine toxicity. Dose adjustment of Xaluprine is necessary. - Warfarin: Mercaptopurine may affect the anticoagulant effect of warfarin.

Monitoring

Regular monitoring of complete blood counts and liver function tests is essential during treatment with Xaluprine. Patients should be monitored for signs of infection and liver toxicity.

Conclusion

Xaluprine is a critical component in the treatment of acute lymphoblastic leukemia, offering a targeted approach to inhibiting cancer cell proliferation. Its use requires careful monitoring and management of potential adverse effects and drug interactions.

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