A-Z Drug Facts > Rituximab

Rituximab

Pronouncation: (ri-TUX-i-mab)
Class: Monoclonal antibody

Trade Names:
Rituxan
- Solution for injection 10 mg/mL

Pharmacology

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Rituximab is a monoclonal antibody directed against the CD20 antigen found on the surface of normal and malignant B lymphocytes. The CD20 antigen is also expressed on more than 90% of B-cell non-Hodgkin lymphomas (NHL).

Pharmacokinetics

Absorption

IV absorption is immediate and results in a rapid and sustained depletion of circulating and tissue-based cells.

Distribution

Binds to lymphoid cells in thymus, white pulp of spleen, and a majority of B lymphocytes in peripheral blood and lymph nodes.

Elimination

Mean serum t _1/2 is 59.8 h after first infusion and 174 h after fourth infusion. Wide range of half-lives reflect the variable tumor burden and changes in CD20-positive, B-cell populations.

Duration

Detectable in serum 3 to 6 mo after completion of treatment. B-cell recovery began at about 6 mo following completion of treatment. Median B-cell levels returned to normal by 12 mo after completion of treatment.

Indications and Usage

Treatment of relapsed or refractory, low-grade or follicular, CD20-postive, B-cell, NHL; first-line treatment of follicular, CD20-positive, B-cell NHL in combination with cyclophosphamide, vincristine, and prednisone (CVP) chemotherapy; treatment of low-grade, CD20-positive, B-cell NHL in patients with stable disease or who achieve partial or complete response following first-line treatment with CVP chemotherapy; first-line treatment of diffuse large B-cell, CD20-positive NHL in combination with cyclophosphamide, doxorubicin, vincristine, and prednisone (CHOP) or other anthracycline-based chemotherapy regimens; in combination with methotrexate to reduce signs and symptoms in moderately to severely active rheumatoid arthritis in patients who have an inadequate response to 1 or more tumor necrosis factor antagonist therapies.

Unlabeled Uses

Relapsed or refractory chronic lymphocytic leukemia; relapsed or refractory Waldenström macroglobulinemia; thrombocytopenic purpura.

Contraindications

None.

Dosage and Administration

Relapsed or Refractory, Low-Grade or Follicular, CD20-Positive, B-Cell NHL
Adults

IV 375 mg/m ² infused once weekly for 4 or 8 doses. Retreatment: 375 mg/m ² IV infusion once/wk for 4 doses in responding patients who develop progressive disease after previous rituximab therapy.

Previously Untreated, Follicular, CD20-Positive, B-Cell NHL
Adults

IV 375 mg/m ² infusion, given on day 1 of each cycle of CVP chemotherapy, for up to 8 doses.

Previously Untreated, Low-Grade, CD20-Positive, B-Cell NHL
Adults

IV In patients who have not progressed following 6 to 8 cycles of CVP chemotherapy, 375 mg/m ² infusion once weekly for 4 doses every 6 mo for up to 16 doses.

Diffuse Large B-Cell NHL
Adults

IV 375mg/m ² infused on day 1 of each chemotherapy cycle for up to 8 infusions.

Rheumatoid Arthritis
Adults

IV Two infusions of 1,000 mg separated by 2 wk.

Rituximab as a Component of Ibritumomab Tiuxetan Therapeutic Regimen
Adults

IV As a required component of the ibritumomab tiuxetan therapeutic regimen, infuse 250 mg/m ² within 4 h prior to administration of indium-111 (In-111) ibritumomab tiuxetan and within 4 h prior to administration of yttrium-90 (Y-90) ibritumomab tiuxetan. Rituximab and In-111 ibritumomab tiuxetan should precede rituximab and Y-90 ibritumomab tiuxetan by 7 to 9 days.

General Advice

• Do not administer as an IV push or bolus.
• Because infusion reactions may occur, consider premedication with acetaminophen and an antihistamine prior to each rituximab infusion.
• Because transient hypotension may occur during rituximab infusion, consider withholding antihypertensive medications 12 h prior to rituximab infusion.
• First infusion: Infuse rituximab solution at an initial rate of 50 mg/h. Do not mix or dilute with other drugs. If infusion reactions do not occur, escalate infusion rate in 50 mg/h increments every 30 min, to a max of 400 mg/h. If an infusion reaction develops, temporarily slow or interrupt infusion. Upon improvement of patient's symptoms, continue infusion at one half the previous rate.
• Subsequent infusions: If the first infusion is well tolerated, subsequent rituximab infusions can be given at an initial rate of 100 mg/h, and increased in 100 mg/h increments at 30-min intervals, to a max of 400 mg/h as tolerated. If the first infusion is not tolerated, follow the guidelines under First infusion.

Storage/Stability

Rituximab vials are stable at 36° to 46°F. Do not use beyond expiration date stamped on carton. Protect vials from direct sunlight. Do not freeze or shake. Rituximab solutions for infusion may be stored at 36° to 46°F for 24 h and are stable at room temperature for an additional 24 h. However, because rituximab solutions do not contain a preservative, store diluted solutions refrigerated at 36° to 46°F.

Drug Interactions

No specific drug interactions have been reported. Coadministration of drugs with similar pharmacologic effects may cause additive side effects, including toxicity. Renal toxicity was seen with this drug in combination with cisplatin in clinical trials.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension (10%); hypertension (6%); fatal cardiac failure, systemic vasculitis (postmarketing).

CNS

Headache (19%); dizziness (10%); anxiety (5%).

Dermatologic

Night sweats, rash (15%); pruritus (14%); urticaria (8%); flushing (5%); severe mucocutaneous reactions (postmarketing).

EENT

Throat irritation (9%); optic neuritis, uveitis (postmarketing).

GI

Nausea (23%); diarrhea, vomiting (10%); bowel obstruction and perforation (postmarketing).

Hematologic-Lymphatic

Lymphopenia (48%); leukopenia, neutropenia (14%); thrombocytopenia (12%); anemia (8%); hyperviscosity syndrome in Waldenström macroglobulinemia, late onset neutropenia, marrow hypoplasia, prolonged pancytopenia (postmarketing).

Metabolic-Nutritional

Angioedema (11%); hyperglycemia (9%); peripheral edema (8%); LDH increase (7%).

Musculoskeletal

Arthralgia, back pain, myalgia (10%).

Respiratory

Increased cough (13%); rhinitis (12%); bronchospasm (8%); dyspnea (7%); sinusitis (6%).

Miscellaneous

Fever (53%); chills (33%); infection (31%); infusion reactions including angioedema, bronchospasm (with or without hypotension or hypertension), chills, cough, fever, pruritus, rigors, sneezing, throat irritation, and urticaria/rash (27%); asthenia (26%); abdominal pain (14%); pain (12%); fatal infections in HIV-associated lymphoma, lupus-like syndrome, pleuritis, polyarticular arthritis, serum sickness, vasculitis with rash (postmarketing).

Precautions

Warnings Fatal infusion reaction Deaths within 24 h of infusion have been reported. Reaction complex consists of hypoxia, pulmonary infiltrates, acute respiratory distress syndrome, MI, ventricular fibrillation, or cardiogenic shock. Approximately 80% of fatal infusion reactions occur with first infusion. Interrupt the rituximab infusion for severe reactions and institute supportive care measures as medically indicated (eg, IV fluids, vasopressors, oxygen, bronchodilators, diphenhydramine, acetaminophen). Mucocutaneous reactions (severe) Reported with fatal outcomes. Tumor lysis syndrome Rapid reduction in tumor volume followed by acute renal failure, hyperkalemia, hypocalcemia, hyperuricemia, or hyperphosphatasemia has been reported within 12 to 24 h after the first rituximab infusion.

Monitor Obtain CBC and platelet counts at regular intervals and more frequently in patients developing cytopenias.

Pregnancy

Category C .

Lactation

Because human immunoglobulin (Ig) G is excreted in breast milk and the potential for absorption and immunosuppression in the infant is unknown, advise women to discontinue breast‐feeding until circulating drug levels are no longer detectable.

Children

Safety and efficacy have not been established.

Hypersensitivity

Rituximab is associated with hypersensitivity reactions (non-IgE-mediated reactions), which may respond to adjustments in the infusion rate and in medical management.

Bowel obstruction

Abdominal pain and bowel obstruction and perforation, sometimes leading to death, have been reported in patients concurrently receiving chemotherapy.

Cardiac arrhythmias

Discontinue infusions in the event of serious or life-threatening cardiac arrhythmias.

Hepatitis B reactivation

Hepatitis B reactivation with fulminant hepatitis, hepatic failure, and death has been reported in patients with hematologic malignancies.

Overdosage

Symptoms

No experience with overdosage in humans.

Patient Information

• Advise patient to read the patient information leaflet before using product the first time and with each refill.
• Advise patient, family, or caregiver that medication will be prepared and administered by health care provider in a health care setting.
• Review dosing schedule with patient, family, or caregiver.
• Advise patient, family, or caregiver to immediately report any of the following to health care provider: chest pain; decreased urine output; fever, chills, or other signs of infection; hives; itching; rash; shortness of breath or difficulty breathing; sores in mouth; unusual bleeding or bruising.
• Advise patient, family, or caregiver to report any of the following to health care provider: persistent nausea, vomiting, diarrhea, or appetite loss; persistent or worsening general body weakness.

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