rituximab

REMS

Riabni, Rituxan, Ruxience, and Truxima:

Treatment of the following conditions:
- Relapsed or refractory, low-grade or follicular, CD20-positive, B-cell non-Hodgkin’s lymphoma (NHL) (as monotherapy).
- Previously untreated follicular, CD20-positive, B-cell NHL in combination with first-line chemotherapy and, in patients achieving a complete or partial response to rituximab in combination with chemotherapy, as single-agent maintenance therapy.
- Non-progressing, low-grade, CD20-positive, B-cell NHL following treatment with cyclophosphamide, vincristine, and prednisone (as monotherapy).
- Previously untreated diffuse large B-cell, CD20-positive, NHL (in combination with CHOP or another anthracycline-based chemotherapy regimen).
- CD-20 positive chronic lymphocytic leukemia (CLL) (in combination with fludarabine and cyclophosphamide).
- Moderately to severely active rheumatoid arthritis in patients who have had an inadequate response to ≥1 TNF antagonist therapies (with methotrexate).
- Granulomatosis with polyangiitis (Wegener's granulomatosis) and microscopic polyangiitis (in combination with glucocorticoids).

Rituxan only:

Treatment of the following condition:
- Moderate to severe pemphigus vulgaris.
Previously untreated, advanced stage, CD20-positive diffuse large B-cell lymphoma, Burkitt lymphoma, Burkitt-like lymphoma, or mature B-cell acute leukemia (in combination with chemotherapy).

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity to murine (mouse) proteins
OB: Can pass placental barrier potentially causing fetal B-cell depletion. Use during pregnancy only if clearly needed
Lactation: Lactation.

Use Cautiously in:

Pre-existing bone marrow depression
Hepatitis B virus (HBV) infection (may reactivate infection during and for several mo after treatment)
Systemic lupus erythematosus (may cause fatal progressive multifocal leukoencephalopathy [PML])
HIV infection (may ↑ risk of HIV-associated lymphoma)
Rep: Women of reproductive potential
Pedi: Safety and effectiveness not established for children <6 mo (mature B-cell lymphomas and B-cell acute leukemia), <2 yr (granulomatosis with polyangiitis and microscopic polyangiitis), and <18 yr (all other indications).

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension, ARRHYTHMIAS, peripheral edema.

Derm: flushing, STEVENS-JOHNSON SYNDROME (SJS), TOXIC EPIDERMAL NECROLYSIS (TEN), urticaria.

Endo: hyperglycemia.

F and E: hypocalcemia.

GI: abdominal pain, altered taste, dyspepsia, HBV REACTIVATION.

GU: renal failure.

Hemat: ANEMIA, NEUTROPENIA, THROMBOCYTOPENIA.

MS: arthralgia, back pain.

Neuro: PML, headache.

Resp: bronchospasm, cough, dyspnea.

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS AND ANGIOEDEMA), infection, INFUSION REACTIONS, TUMOR LYSIS SYNDROME.

Interactions ⬆ ⬇

Drug-Drug:

May ↓ antibody response to or ↑ risk of adverse reactions to live vaccines; avoid use during treatment; inactive vaccines should be administered ≥4 wk prior to start of therapy.

Availability ⬆ ⬇

Solution for injection: 10 mg/mL;

Route/Dosage ⬆ ⬇

Relapsed or Refractory, Low-Grade or Follicular, CD20-Positive, B-Cell Non-Hodgkin’s Lymphoma

IV (Adults): 375 mg/m² once weekly for 4 or 8 doses; may retreat with 375 mg/m² once weekly for 4 doses.

Previously Untreated Follicular, CD20–Positive, B-Cell Non-Hodgkin’s Lymphoma

IV (Adults): 375 mg/m² given on Day 1 of each cycle of chemotherapy with cyclophosphamide, vincristine, and prednisone for up to 8 doses; if patients experience complete or partial response, give 375 mg/m² (as monotherapy) every 8 wk for 12 doses (initiate this maintenance therapy 8 wk after completion of rituximab + cyclophosphamide/vincristine/prednisone regimen).

Non-Progressing Low-Grade, CD20-Positive, B-Cell Non-Hodgkin’s Lymphoma

IV (Adults): For patients who have not progressed following 6–8 cycles of chemotherapy with cyclophosphamide, vincristine, and prednisone, 375 mg/m² given once weekly for 4 doses given every 6 mo for up to 16 doses.

Diffuse Large B-Cell Non-Hodgkin’s Lymphoma

IV (Adults): 375 mg/m² given on Day 1 of each cycle of chemotherapy for up to 8 infusions.

Previously Untreated Mature B-Cell Lymphomas and B-Cell Acute Leukemia

IV (Children ≥6 mo): 375 mg/m²/dose in combination with systemic Lymphome Malin B chemotherapy regimen; administer 2 doses during each of the two induction courses (Day −2 and Day 1), and one dose during each of the two consolidation cycles (Day 1) (6 doses total).

Chronic Lymphocytic Leukemia

IV (Adults): 375 mg/m² given on the day before initiating chemotherapy with fludarabine and cyclophosphamide, then 500 mg/m² on Day 1 of cycles 2–6 (every 28 days).

Rheumatoid Arthritis

IV (Adults): 1000 mg every 2 wk for 2 doses; subsequent courses should be administered every 24 wk (not sooner than every 16 wk).

Granulomatosis With Polyangiitis and Microscopic Polyangiitis

IV (Adults): Induction treatment: 375 mg/m² once weekly for 4 wk; Follow-up treatment in patients who have achieved disease control with induction treatment: 500 mg every 2 wk for 2 doses (should be started 16–24 wk after last rituximab induction dose; if achieved disease control with another agent, start follow-up treatment within 4 wk after last induction dose of that agent), then 500 mg every 6 mo thereafter.
IV (Children ≥2 yr): Induction treatment: 375 mg/m² once weekly for 4 wk; Follow-up treatment in patients who have achieved disease control with induction treatment: 250 mg/m² every 2 wk for 2 doses (should be started 16–24 wk after last rituximab induction dose; if achieved disease control with another agent, start follow-up treatment within 4 wk after last induction dose of that agent), then 250 mg/m² every 6 mo thereafter.

Pemphigus Vulgaris

IV (Adults): 1000 mg every 2 wk for 2 doses, then maintenance dose of 500 mg infusion at month 12 and then every 6 mo thereafter. Upon relapse, administer 1000 mg.

US Brand Names ⬆ ⬇

Riabni, Rituxan, Ruxience, Truxima

Action ⬆ ⬇

Binds to the CD20 antigen on the surface of lymphoma cells, preventing the activation process for cell cycle initiation and differentiation.

Therapeutic Effects:

Death of lymphoma cells.
Prolonged progression-free survival in CLL.
Reduced signs and symptoms of rheumatoid arthritis.
Achievement of complete remission in granulomatosis with polyangiitis, microscopic polyangiitis, and pemphigus vulgaris.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: monoclonal antibodies

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Binds specifically to CD20 binding sites on lymphoma cells.

Metabolism/Excretion: Unknown.

Half-life: 59.8–174 hr (depending on tumor burden).

Canadian Brand Names ⬆ ⬇

Time/Action Profile ⬆ ⬇

(B-cell depletion)

ROUTE	ONSET	PEAK	DURATION
IV	within 14 days	3–4 wk	6–9 mo†

†Duration of depletion after 4 wk of treatment.

Patient/Family Teaching ⬆ ⬇

Inform patient of the purpose of the medication. Advise patient to read the Medication Guide prior to starting therapy and before each infusion in case of changes.
Advise patient to report infusion-related events or symptoms of hypersensitivity reactions immediately.
Instruct patient to notify health care professional promptly if fever; chills; cough; hoarseness; sore throat; signs of infection; lower back or side pain; painful or difficult urination; bleeding gums; bruising; petechiae; blood in stools, urine, or emesis; increased fatigue; dyspnea; orthostatic hypotension; or painful ulcers or sores on your skin, lips, or in mouth, blisters, peeling skin, rash, pustule occurs. Caution patient to avoid crowds and persons with known infections. Instruct patient to use soft toothbrush and electric razor and to avoid falls. Caution patient not to drink alcoholic beverages or take medication containing aspirin or NSAIDs; may precipitate gastric bleeding.
Advise patient to consult health care professional prior to receiving any vaccinations.
Rep: May cause fetal harm. Advise females of reproductive potential to use effective contraception during and for 12 mo following therapy, and to avoid breast feeding during and for at least 6 mo after last dose. Observe newborns and infants of women taking rituximab during pregnancy for signs of infection.

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Indications ⬇