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Rituximab

RITUXAN

Pronunciation: ri-TUX-i-mab (ri-TUK-san)

Rituximab ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Rituximab ballicule
Rituximab RITUXAN mascot mnemonic cartoon
Visual mnemonic: Rituximab mascot
“The Right tux”

What it isCD20-directed monoclonal antibody depleting B cells; B-cell malignancies, rheumatoid arthritis, and ANCA vasculitis.

Why this oneIt remains a backbone of B-cell lymphoma therapy while also treating antibody-mediated autoimmune disease.

What limits it⚑ Hepatitis B reactivation can be fatal, so screen before treatment; infusion reactions, PML, and hypogammaglobulinemia also matter.

Rituximab molecular structure (skeletal formula)
Molecular structure: Rituximab

FDA label

BOXED WARNING Fatal infusion-related reactions (~80% with first infusion); severe mucocutaneous reactions (some fatal); hepatitis B virus reactivation (fulminant hepatitis, hepatic failure, death); progressive multifocal leukoencephalopathy (PML), including fatal PML.
FDA dosingPopulationStartTargetMax
Non-Hodgkin's lymphoma (CD20+ B-cell)Adult375 mg/m² IVweekly ×4–8 or on day 1 of each chemo cycle (per regimen)
Mature B-cell NHL / mature B-cell acute leukemia (with chemotherapy)Peds ≥6 mo375 mg/m² IV6 infusions with LMB chemotherapy
Chronic lymphocytic leukemia (CD20+, with fludarabine/cyclophosphamide)Adult375 mg/m² IV cycle 1500 mg/m² IV cycles 2–6 (every 28 days)
Rheumatoid arthritis (with methotrexate)Adult1,000 mg IV ×2 separated by 2 weeksrepeat every 24 weeks (no sooner than every 16 weeks)
Granulomatosis with polyangiitis / microscopic polyangiitis (with glucocorticoids)Adult375 mg/m² IV weekly ×4 (induction)follow-up two 500 mg IV 2 weeks apart, then 500 mg every 6 months
Granulomatosis with polyangiitis / microscopic polyangiitis (with glucocorticoids)Peds ≥2 yr375 mg/m² IV weekly ×4 (induction)follow-up two 250 mg/m² IV 2 weeks apart, then 250 mg/m² every 6 months
Pemphigus vulgaris (moderate to severe)Adult1,000 mg IV ×2 separated by 2 weeks (with tapering glucocorticoids)500 mg IV at Month 12 and every 6 months thereafter

Renal Undefined

Hepatic Undefined

Dose and frequency are indication-specific (see indications).

Instructions

Available strengths

Cautions

Adverse reactions

Pregnancy Can cause fetal harm — B-cell lymphocytopenia in infants exposed in utero (human data). Advise of risk; effective contraception for 12 months after the last dose.

Lactation Limited data; low levels reported in human milk. Advise not to breastfeed during treatment and for 6 months after the last dose.

Cost

Rituximab (RITUXAN)
Strength#/mogeneric $/unitCostPlus
10 mg/mLinjper unitnot offered
NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Rituximab is administered under clinical supervision and dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

⚠ BOXED WARNINGS

Classes and tags

Clinical profile

Therapeutic safety burden4 / 4
Overdose danger2 / 4
Weight-gain liability1 / 4
Sedation liability1 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk3 / 4

Legacy pregnancy categoryC

Defining liabilityFatal infusion reactions, infection and prolonged B-cell depletion

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Memory aids: interaction avatars

Rituximab no kinetic interactions avatar mnemonic
no kinetic interactions

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