rituximab (Rx)

Brand and Other Names:Rituxan, Truxima, more...rituximab-abbs
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

solution for IV

  • 10mg/mL (100mg/10mL or 500mg/50mL single-dose vials)
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Non-Hodgkin Lymphoma

Indications

  • Rituxan or Truxima
    • Relapsed or refractory, low-grade or follicular, CD20-positive, B-cell NHL as a single agent
    • 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
    • Nonprogressing (including stable disease), low-grade, CD20-positive, B-cell NHL as a single agent after first-line cyclophosphamide, vincristine, and prednisone (CVP) chemotherapy
  • Rituxan only
    • Previously untreated diffuse large B-cell, CD20-positive NHL in combination with CHOP or other anthracycline-based chemotherapy regimens

Dosage

  • 375 mg/m² IV infusion according to the following schedules 
  • Relapsed or refractory low-grade or follicular, CD20-positive, B-cell NHL: Once weekly x4-8 doses
  • Retreatment for relapsed or refractory, low-grade or follicular, CD20-positive, B-cell NHL: Once weekly x4 doses
  • Previously untreated, follicular, CD20-positive, B-cell NHL: Administer on Day 1 of each chemotherapy cycle for up to 8 doses; with complete or partial response, initiate maintenance 8 weeks following completion of combination chemotherapy as a single-agent q8weeks for 12 doses
  • Nonprogressing, low-grade, CD20-positive, B-cell NHL, after first-line CVP chemotherapy: Following completion of 6-8 cycles of CVP chemotherapy, administer once weekly for 4 doses at 6-month intervals to a maximum of 16 doses
  • Diffuse large B-cell NHL: Administer on Day 1 of each cycle of chemotherapy for up to 8 infusions

Chronic Lymphocytic Leukemia

Rituxan only

Indicated for untreated and previously treated CD20-positive CLL; combined therapy with fludarabine and cyclophosphamide (FC)

375 mg/m² IV infusion on day 1 of 1st cycle (for 1st cycle, administer 1 day before chemotherapy with FC), THEN  

500 mg/m² IV on day 1 of subsequent cycles (administer on same day as chemotherapy with FC)

Repeat q28 days x6 cycles

Fludarabine & cyclophosphamide dosage

  • Fludarabine: 25 mg/m² IV qDay x 3 days
  • Cyclophosphamide: 250 mg/m² IV qDay x3 days
  • Repeat q28 days x 6 cycles

Rheumatoid Arthritis

Rituxan only

1000 mg IV infusion, repeat after 2 week (2 infusions separated by 2 week is 1 course)

Repeat course q24weeks or based on clinical evaluation (but no sooner than 16 weeks)

Use in combination with methotrexate

Premedicate with glucocorticoids 30 minutes before infusion to reduce infusion rxn

Not to exceed 1000 mg/dose

Wegener Granulomatosis

Rituxan only

Indicated for adults with granulomatosis with polyangiitis (GPA; Wegener granulomatosis) in combination with glucocorticoids

Induction: 375 mg/m² IV qWeek x4 weeks 

Follow up treatment

  • If disease control achieved with induction treatment, initiate follow up treatment
  • Induction treatment with rituximab: Initiate follow up treatment within 24 after last rituximab induction dose or based on clinical evaluation, but no sooner than 16 weeks after last induction dose
  • Induction treatment with other standard of care immunosuppressants: Initiate follow up treatment within 4 weeks following achievement of disease control
  • 500 mg IV on Days 1 and 15, THEN 100 mg IV q6months thereafter

Glucocorticoid regimen

  • Also see premedication
  • Induction
    • Methylprednisolone 1000 mg IV qDay x 1 to 3 days followed by prednisone PO 1 mg/kg/day (not to exceed 80 mg/day and tapered per clinical need) are recommended to treat severe vasculitis symptoms
    • This regimen should begin within 14 days before or with initiation of rituximab and may continue during and after the 4 week induction course
  • Follow up treatment
    • Methylprednisolone 100 mg IV to be completed 30 minutes before each rituximab IV infusion

Microscopic Polyangiitis

Rituxan only

Indicated for adults with microscopic polyangiitis (MPA) in combination with glucocorticoids

Induction: 375 mg/m² IV qWeek x4 weeks 

Follow up treatment

  • If disease control achieved with induction treatment, initiate follow up treatment
  • Induction treatment with rituximab: Initiate follow up treatment within 24 after last rituximab induction dose or based on clinical evaluation, but no sooner than 16 weeks after last induction dose
  • Induction treatment with other standard of care immunosuppressants: Initiate follow up treatment within 4 weeks following achievement of disease control
  • 500 mg IV on Days 1 and 15, THEN 100 mg IV q6months thereafter

Glucocorticoid regimen

  • Also see premedication
  • Induction
    • Methylprednisolone 1000 mg IV qDay x 1 to 3 days followed by prednisone PO 1 mg/kg/day (not to exceed 80 mg/day and tapered per clinical need) are recommended to treat severe vasculitis symptoms
    • This regimen should begin within 14 days before or with initiation of rituximab and may continue during and after the 4 week induction course
  • Follow up treatment
    • Methylprednisolone 100 mg IV to be completed 30 minutes before each rituximab IV infusion

Pemphigus Vulgaris

Rituxan only

Indicated for adults with moderate-to-severe pemphigus vulgaris (PV)

Initial: 1000 mg IV once, then repeat dose in 2 weeks (ie, two 1000-mg doses 2 weeks apart); use in combination with a tapering course of glucocorticoids

Maintenance: 500 mg IV at Month 12 and q6Months thereafter or based on clinical evaluation

Treatment relapse: 1000 mg IV and consider resuming or increasing the glucocorticoid dose based on clinical evaluation

Orphan Designations

Treatment of immune thrombocytopenic purpura (ITP)

Sponsor

  • Genentech, Inc; 1 DNA Way; South San Francisco, CA 94080-4990

Rasmussen Encephalitis (Orphan)

Orphan designation for treatment of Rasmussen encephalitis

Sponsor

  • Keck Graduate Institute of Applied Life Sciences; 535 Watson Drive; Claremont, California 91711

Safety and efficacy not established

Rheumatoid Arthritis: Safety and effectiveness not established; FDA has not required pediatric studies in polyarticular juvenile idiopathic arthritis (PJIA) patients <16 years due to concerns regarding the potential for prolonged immunosuppression as a result of B-cell depletion in the developing juvenile immune system

Wegener Granulomatosis: Safety and effectiveness not established

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Interactions

Interaction Checker

and rituximab

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            NHL

            • Angioedema (11%), hypotension (10%)
            • Asthenia (26%), chills (33%), dizziness (10%), fever (53%), headache (19%)
            • Pruritus (14%), rash (15%)
            • Abdominal pain (14%), diarrhea (10%), nausea (23%), vomiting (10%)
            • Leukopenia (14%), lymphopenia (48%), neutropenia (14%), thrombocytopenia (12%)
            • Back pain (10%), myalgia (10%)
            • Cough (13%), rhinitis (12%)
            • Infection (31%), night sweats (15%)

            GPA and MPA

            • Nausea (18%)
            • Diarrhea (17%)
            • Headache (17%)
            • Muscle spasms (17%)
            • Anemia (16%)
            • Peripheral edema (16%)
            • Insomnia (14%)
            • Arthralgia (13%)
            • Cough (13%)
            • Fatigue (13%)
            • Increased ALT (13%)
            • Hypertension (12%)
            • Epistaxis (11%)

            PV

            • Infusion reactions (58%)
            • Depression (18%)
            • Herpes simplex (13%)
            • Alopecia (13%)

            1-10%

            NHL

            • Edema
            • Flushing
            • Hypertension
            • Anxiety
            • Anemia
            • Elevated LDH
            • Hyperglycemia
            • Bronchospasm, dyspnea, sinusitis, throat irritation, urticaria

            RA (Rituximab+Methotrexate vs Methotrexate Alone)

            • Hypertension
            • Anxiety, asthenia, chills, migraine, paresthesia, pyrexia
            • Pruritus, urticaria
            • Dyspepsia, nausea, upper abd pain
            • Hypercholesterolemia
            • Arthralgia
            • Rhinitis, throat irritation, URI

            GPA and MPA

            • Dyspnea (10%)
            • Leukopenia (10%)
            • Rash (10%)

            PV

            • Fatigue (8%)
            • Upper abdominal pain (5%)
            • Conjunctivitis (5%)
            • Dizziness, headache (5%)
            • Herpes zoster (5%)
            • Irritability (5%)
            • Muscular pain (5%)
            • Pyrexia (5%)
            • Tachycardia (5%)
            • Pruritus, skin disorder, skin papilloma, urticaria (5%)

            Frequency Not Defined

            Tumor lysis syndrome

            Lymphoid malignancies

            Hypogammaglobulinemia

            Postmarketing Reports

            Hematologic: Prolonged pancytopenia, marrow hypoplasia, Grade 3-4 prolonged or late-onset neutropenia, hyperviscosity syndrome in Waldenstrom macroglobulinemia, prolonged hypogammaglobulinemia

            Cardiac: Fatal cardiac failure

            Immune/autoimmune events: Uveitis, optic neuritis, systemic vasculitis, pleuritis, lupus-like syndrome, serum sickness, polyarticular arthritis, and vasculitis with rash

            Infection: Viral infections, including progressive multifocal leukoencephalopathy (PML), increase in fatal infections in HIV-associated lymphoma, and a reported increased incidence of Grade 3 and 4 infections

            Neoplasia: Disease progression of Kaposi sarcoma

            Skin: Severe mucocutaneous reactions

            Gastrointestinal: Bowel obstruction and perforation

            Pulmonary: Fatal bronchiolitis obliterans and fatal interstitial lung disease

            Nervous system: Posterior reversible encephalopathy syndrome (PRES)/reversible posterior leukoencephalopathy syndrome (RPLS)

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            Warnings

            Black Box Warnings

            Fatal infusion reaction

            • Can result in serious, including fatal reactions
            • Deaths within 24 hours of infusion have occurred
            • Approximately 80% of fatal infusion reactions occurred in association with the first infusion
            • Carefully monitor patients during infusion
            • In patients with Non-Hodgkin’s Lymphoma (NHL) receiving rituximab monotherapy, NCI-CTC Grade 3 and 4 cytopenias reported; reactions included lymphopenia, neutropenia, leukopenia, anemia, and thrombocytopenia; discontinue infusion and provide medical treatment for grade 3 or 4 reactions

            Mucocutaneous reactions (severe)

            • Severe, including fatal, mucocutaneous reactions reported including paraneoplastic pemphigus, Stevens-Johnson syndrome, lichenoid dermatitis, vesiculobullous dermatitis, and toxic epidermal necrolysis

            Progressive multifocal leukoencephalopathy

            • John Cunningham virus infection resulting in progressive multifocal leukoencephalopathy and death has been reported in patients treated with rituximab

            Reactivation of hepatitis B

            • Reactivation of hepatitis B virus (HBV) infection reported, including deaths
            • Screen all patients for HBV infection before initiating drug by measuring hepatitis B surface antigen (HBsAg) and hepatitis B core antibody (anti-HBc)
            • Consult with hepatitis experts regarding monitoring and use of HBV antiviral therapy when screening identifies patients at risk of HBV reactivation due to evidence of prior HBV infection
            • Monitor patients with evidence of prior HBV infection for clinical and laboratory signs of hepatitis B or HBV reactivation during therapy and for several months thereafter, since reactivations have occurred several months following completion of therapy
            • In patients who develop reactivation of HBV, immediately discontinue the drug and start appropriate HBV treatment, also discontinue any chemotherapy until the HBV infection is controlled or resolved
            • Because of insufficient data, no recommendation can be made regarding the resumption of the drug in patients who develop HBV reactivation hepatitis

            Contraindications

            None

            Cautions

            Can cause severe, including fatal, infusion-related reactions; severe reactions typically occurred during the first infusion with time to onset of 30-120 minutes; premedicate as recommended according to indication; have appropriate medical management available if reaction occurs (eg, glucocorticoids, epinephrine, bronchodilators, oxygen) (see Black Box Warnings and Administration)

            Risk of potentially fatal mucocutaneous reactions (see Black Box Warnings)

            Increased risk of potentially fatal hepatitis B virus reactivation (see Black Box Warnings)

            Potential risk of progressive multifocal leukoencephalopathy (see Black Box Warnings)

            Risk of potentially fatal tumor lysis syndrome

            Serious, including fatal, bacterial, fungal, and new or reactivated viral infections can occur during and following the completion of therapy; not recommended for patients with severe, active infections

            Cardiac adverse reactions (eg, ventricular fibrillation, myocardial infarction, cardiogenic shock) may occur; discontinue infusions for serious or life-threatening cardiac arrhythmias; cardiac monitoring needed during and after all infusions patients who develop clinically significant arrhythmias, or who have a history of arrhythmia or angina

            Severe, including fatal, renal toxicity can occur after administration in patients with non-Hodgkin lymphoma (NHL); renal toxicity has occurred in patients who experience tumor lysis syndrome and in patients with NHL administered concomitant cisplatin therapy during clinical trials; the combination of cisplatin and rituximab is not an approved treatment regimen

            Abdominal pain, bowel obstruction and perforation reported, including cases leading to death

            Based on human data, rituximab can cause fetal harm owing to B-cell lymphocytopenia in infants exposed in utero (see Pregnancy)

            Use in patients with rheumatoid arthritis who have not had prior inadequate response to more than 1 TNF antagonists is not recommended

            Drug interaction overview

            • Safety of immunization with live viral vaccines following rituximab has not been studied and vaccination with live virus vaccines is not recommended before or during treatment; for patients with rheumatoid arthritis, physicians should follow current immunization guidelines and administer non-live vaccines at least 4 weeks prior to treatment
            • Limited data are available on the safety of the use of biologic agents or disease modifying antirheumatic drugs (DMARDs) other than methotrexate in RA patients exhibiting peripheral B-cell depletion following treatment with rituximab; observe patients closely for signs of infection if biologic agents and/or DMARDs are used concomitantly
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            Pregnancy & Lactation

            Pregnancy

            Based on human data, can cause adverse developmental outcomes including B-cell lymphocytopenia in infants exposed to rituximab in-utero

            Observe newborns and infants for signs of infection and manage accordingly

            Contraception

            • Females of childbearing potential should use effective contraception while receiving rituximab and for 12 months following treatment

            Lactation

            Data are not available on the presence of rituximab in human milk, the effect on the breastfed child, or the effect on milk production

            However, rituximab is detected in the milk of lactating cynomolgus monkeys, and IgG is present in human milk

            Since many drugs, including antibodies, are present in human milk, advise lactating women not to breastfeed during treatment and for at least 6 months after the last rituximab dose owing to the potential for serious adverse reactions in breastfed infants

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

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            Pharmacology

            Mechanism of Action

            Humanized monoclonal antibody, binds to CD20 antigen, inducing complement- or antibody-mediated cytolysis

            Elimination

            Half-life: 59.8 hr (1st dose); 174 hr (4th dose)

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            Administration

            IV Compatibilities

            0.9% NaCl

            D5W

            IV Preparation

            Withdraw necessary amount of rituximab and dilute to a final concentration of 1-4 mg/mL into an infusion bag containing either 0.9% NaCl or D5W

            Visually inspect vials, solution should appear clear and colorless, do not use vial if particular is present

            Gently invert the bag to mix the solution

            Do not mix with other drugs

            Discard any unused portion left in the vial

            IV Administration

            Premedication

            • Premedicate with acetaminophen and an antihistamine before each infusion 90-minute infusion rate regimen
            • For patients administered rituximab according to the 90-minute IV infusion regimen, administer the glucocorticoid component of their chemotherapy regimen prior to rituximab infusion
            • RA and PV: Methylprednisolone 100 mg IV (or equivalent glucocorticoid) recommended 30 minutes before each infusion
            • GPA and MPA: Glucocorticoids are given in combination with rituximab (see Adult Dosing)
            • Provide prophylaxis treatment for Pneumocystis jirovecii pneumonia (PCP) prophylaxis and herpes virus infections for patients with CLL during treatment and for up to 12 months following treatment as appropriate
            • PCP prophylaxis is also recommended for patients with GPA and MPA during treatment and for at least 6 months following the last rituximab infusion
            • Consider PCP prophylaxis for patients with PV during and following rituximab treatment

            IV infusion rate

            • Because transient hypotension may occur during infusion, consider withholding antihypertensive medications 12 hr prior to infusion
            • Administer by slow IV infusion only; do not administer as an IV push or bolus
            • First IV infusion rate: Start 50 mg/hr; increase by 50 mg/hr q30min, not to exceed 400 mg/hr
            • Drug is associated with hypersensitivity reactions which may respond to adjustments in infusion rate
            • Subsequent IV infusions
              • Standard IV infusions: Start 100 mg/hr, increase by 100 mg/hr q30min, not to exceed 400 mg/hr; institutional protocols may allow faster increments
              • Previously untreated patients with follicular NHL or diffuse large B-cell lymphoma: If patients did not experience a Grade 3 or 4 infusion related adverse event during Cycle 1, a 90-minute infusion can be administered in Cycle 2 with a glucocorticoid-containing chemotherapy regimen
              • Initiate at a rate of 20% of the total dose given in the first 30 minutes and the remaining 80% of the total dose given over the next 60 minutes
              • If tolerated in Cycle 2, the same rate can be used when administering the remainder of the treatment regimen (through Cycle 6 or 8)
              • Patients who have clinically significant cardiovascular disease or who have a circulating lymphocyte count ≥5000/mm³ before Cycle 2 should not be administered the 90-minute infusion

            Infusion-related adverse effects

            • Hypotension, bronchospasm, and angioedema have occurred as part of an infusion-related symptom complex
            • Interrupt infusion for severe reactions and resume at a 50% reduction in rate (eg, from 100 to 50 mg/hr) when symptoms have completely resolved
            • Treatment of these symptoms with diphenhydramine and acetaminophen is recommended
            • Additional treatment with bronchodilators or IV saline may be indicated
            • Discontinue infusions if serious or life-threatening cardiac arrhythmias

            Storage

            IV

            • Unused vials: Refrigerate at 2-8°C (36-46°F); protect vials from direct sunlight
            • Solutions for infusion are stable at 2-8°C (36-46°F) for 24 hr
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            Images

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
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