Rituximab

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Mabthera; Belgium: Mabthera; Bulgaria: Mabthera; Czech Republic: Mabthera; Denmark: Mabthera; Estonia: Mabthera; Finland: Mabthera; France: Mabthera;Germany: Mabthera; Greece: Mabthera; Hungary: Mabthera; Ireland: Mabthera; Italy: Mabthera; Latvia: Mabthera; Lithuania: Mabthera; Luxembourg: Mabthera; Malta: Mabthera; Netherlands: Mabthera; Poland: Mabthera; Portugal: Mabthera; Romania: Mabthera; Slovakia: Mabthera; Slovenia: Mabthera; Spain: Mabthera; Sweden: Mabthera; UK: Mabthera.

North America

Canada: Rituxan; USA: Rituxan.

Latin America

Argentina: Mabthera; Brazil: Mabthera; Mexico: Mabthera.

Asia

Japan: Rituxan.

Drug combinations

Chemistry

Rituximab: Mw: approx. 144187.01. (1) Immunoglobulin G~1~ (human-mouse monoclonal IDEC-C2B8 γ~1~-chain anti-human antigen CD20), disulfide with human-mouse monoclonal IDEC-C2B8 κ-chain, dimer; (2) Immunoglobulin G~1~ (human-mouse monoclonal IDEC-C2B8 γ~1~-chain anti-human antigen CD20), disulfide with human-mouse monoclonal IDEC-C2B8 κ-chain, dimer. CAS-174722-31-7 (1997).

Pharmacologic Category

Other Antineoplastic Agents; Monoclonal Antibodies. Antirheumatic (Miscellaneous). (ATC-Code: L01XC02).

Mechanism of action

A monoclonal antibody directed against CD20 antigen on B lymphocytes. Rituximab binds to antigen on cell surface, activating complement-dependent B-cell cytotoxicity; and to human Fc receptors, mediating cell killing through antibody-dependent cellular toxicity. B cells are believed to play a role in development and progression of rheumatoid arthritis (RA). Signs and symptoms of RA reduced by targeting B cells and progression of structural damage is delayed.

Therapeutic use

Treatment of low-grade or follicular CD20-positive, B-cell non-Hodgkin lymphoma (NHL). Treatment of diffuse large B-cell CD20-positive NHL. Treatment of moderately- to severely-active rheumatoid arthritis in combination with methotrexate.

Pregnancy and lactiation implications

Use during pregnancy only if clearly needed. Not recommended in nursing women.

Unlabeled use

Treatment of autoimmune hemolytic anemia in children. Chronic immune thrombocytopenic purpura. Chronic lymphocytic leukemia. Small lymphocytic lymphoma. Pemphigus vulgaris, Waldenström’s macroglobulinemia. Treatment of systemic autoimmune diseases (other than rheumatoid arthritis). Treatment of refractory chronic graft vs host disease.

Contraindications

Warnings and precautions

Bowel obstruction/perforation reported. Severe (occasionally fatal) infusion-related reactions reported, usually with first infusion. Severe and sometimes fatal mucocutaneous reactions (lichenoid dermatitis, paraneoplastic pemphigus, Stevens-Johnson syndrome, toxic epidermal necrolysis and vesiculobullous dermatitis) reported, occurring from 1-13 weeks following exposure (discontinue in severe mucocutaneous skin reactions). Progressive multifocal leukoencephalopathy due to JC virus infection reported with rituximab use. Rituximab may cause renal toxicity in hematologic malignancies. Tumor lysis syndrome leading to acute renal failure requiring dialysis may occur 12-24 hours following first dose. Rarely, reactivation of hepatitis B (with fulminant hepatitis and hepatic failure) reported with use. Other serious and potentially fatal viral infections, either new or reactivated, associated with use include cytomegalovirus, herpes simplex virus, parvovirus B19, varicella zoster virus, West Nile virus, and hepatitis C. Viral infections may be delayed (occurring up to 1 year after discontinuation of therapy). Use with caution in pre-existing cardiovascular disease, pre-existing pulmonary disease, or prior cardiopulmonary events. Live vaccines should not be given concurrently with rituximab. Increased risk of cardiovascular events.

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