Arsenic Trioxide (arsenic trioxide)

Antineoplastics - Arsenic Compounds Intravenous Vial (ML)

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Last reviewed · Source: First Databank (FDB) drug data

Overview

Arsenic trioxide, a proapoptotic agent, is an antineoplastic agent.

Arsenic trioxide is an antineoplastic agent. The mechanism of action of arsenic trioxide is not fully understood, but it appears to induce apoptosis and promote degradation of the promyelocytic leukemia retinoic acid receptor alpha (PML-RARalpha) fusion protein.

The pharmacokinetics of trivalent arsenic have not been fully characterized. After dilution in the syringe, arsenic trioxide converts to arsenious acid, the active form. Exposure appears proportional to dosage, and peak plasma concentrations occur by the end of the 2-hour infusion, followed by a biphasic decline and modest accumulation with repeated dosing.

Arsenic distributes widely throughout body tissues, and the volume of distribution increases with body weight. The liver extensively metabolizes arsenious acid through methyltransferases rather than cytochrome P-450 isoenzymes, producing monomethylarsonic acid (MMAV) and dimethylarsinic acid (DMAV), with smaller amounts of arsenic acid, which remain at low plasma concentrations. Compared with the active form, the metabolites reach measurable plasma concentrations later, have longer half-lives, and accumulate to a greater extent with repeated dosing.

About 15% of arsenic trioxide is excreted unchanged in the urine. The half-life is 10 to 14 hours for arsenious acid, 32 hours for MMAV, and 72 hours for DMAV. Exposure increases by about 50% in patients with severe renal impairment (creatinine clearance less than 30 mL/minute); in one patient with severe hepatic impairment (Child-Pugh class C), arsenic exposure increased by 40-70%.

Arsenic trioxide does not inhibit the metabolism of substrates of major CYP isoenzymes, including 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, 3A4/5, and 4A9/11.

USES: Arsenic trioxide is used to treat a type of leukemia (acute promyelocytic leukemia-APL).

Generic name: arsenic trioxide
Pronunciation: (AR-se-nik trye-OX-ide)
Drug class: Antineoplastics - Arsenic Compounds
Therapeutic class: Antineoplastics

Reference product & biosimilars

No reference, biosimilar or interchangeable associated with this drug.

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Indications

The following indications are listed for Arsenic Trioxide:

  • Acute Myelomonocytic Leukemia
  • Acute Promyelocytic Leukemia

Also known as: Acute Naegeli Type Of Monocytic Leukemia, Acute Naegeli's Leukemia, Myelomonocytic Leukemia, Promyelocytic Leukemia.

Dosing

Table 1. Dose Reduction Levels for Hematologic and Nonhematologic Toxicities

Dose Level Arsenic trioxide Tretinoin (rounded to the nearest 10 mg) Starting Dose 0.15 mg/kg IV once daily 22.5 mg/m2orally twice daily First Dose Reduction 0.11 mg/kg IV once daily 18.75 mg/m2orally twice daily Second Dose Reduction 0.10 mg/kg IV once daily 12.5 mg/m2orally twice daily Third Dose Reduction 0.075 mg/kg IV once 10 mg/m2orally twice daily daily

Drug interactions

No formal drug interaction studies have been conducted to date with arsenic trioxide.

Contraindications

*Known hypersensitivity to arsenic.

Adverse reactions

The most common adverse reactions reported in more than 30% of patients receiving arsenic trioxide in clinical studies were nausea, cough, fatigue, pyrexia, headache, abdominal pain, vomiting, tachycardia, diarrhea, dyspnea, hypokalemia, leukocytosis, hyperglycemia, hypomagnesemia, insomnia, dermatitis, edema, QTc prolongation, rigors, sore throat, arthralgia, paresthesia, and pruritus.

Precautions

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ICD codes

CodeTypeDescription
Acute myelomonocytic leukemia
C92.5ICD10CMAcute myelomonocytic leukemia
C92.50ICD10CMAcute myelomonocytic leukemia, not having achieved remission
C92.52ICD10CMAcute myelomonocytic leukemia, in relapse
Acute promyelocytic leukemia
C92.4ICD10CMAcute promyelocytic leukemia
C92.40ICD10CMAcute promyelocytic leukemia, not having achieved remission
C92.42ICD10CMAcute promyelocytic leukemia, in relapse

ICD code information from First Databank (FDB).

Formulary status

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Last reviewed · Source: First Databank (FDB) drug data