Rheumatoid arthritis (Moderate to Severe), In patients who had an inadequate response to disease modifying antirheumatic therapy.
藥理
Antagonist of the interleukin-6 (IL-6) receptor. Endogenous IL-6 is induced by inflammatory stimuli and mediates a variety of immunological responses. Inhibition of IL-6 receptors by tocilizumab leads to a reduction in cytokine and acute phase reactant production. (UTD)
藥動學
Absorption:
Bioavailability, subQ: 80%
Distribution:
Vd, rheumatoid arthritis: 6.4 L
Elimination Half Life:
Rheumatoid arthritis: Up to 11 days (multiple-dose, 4 mg/kg IV), up to 13 days (multiple-dose, 8 mg/kg IV), 6.3 days (single-dose, 10 mg/kg IV) ; up to 13 days (multiple-dose, 162 mg subQ every week); up to 5 days (multiple-dose, 162 mg subQ every other week) .(UTD)
禁忌症
Known hypersensitivity to tocilizumab or any component of the formulation.(UTD)
懷孕分類
Fetal risk cannot be ruled out. (TH)
哺乳分類
Infant risk cannot be ruled out.(MDX)
副作用
Common:
Cardiovascular: Hypertension (Adult, 4% to 6% )
Dermatologic: Injection site reaction ( Rheumatoid arthritis, 2.4% to 10.1% ), Rash (Rheumatoid arthritis, 2% to 4% )
Gastrointestinal: Diarrhea (Pediatric, greater than 5% ), Upper abdominal pain (Adult, 2% to 3% )
Hepatic: ALT/SGPT level raised (Rheumatoid arthritis, 0.7% to 48%; polyarticular or systemic juvenile idiopathic arthritis, 4% to 13% ), AST/SGOT level raised (Rheumatoid arthritis, 0.1% to 41%; polyarticular or systemic juvenile idiopathic arthritis, less than 1% to 5% )
Neurologic: Dizziness (Adult, 2% to 3% ), Headache (Adults, 5% to 7%; pediatric, greater than 5% )
Respiratory: Nasopharyngitis (Rheumatoid arthritis, 4% to 7%; systemic juvenile idiopathic arthritis, 5% or higher )
Other: Infusion reaction (Rheumatoid arthritis, 7% to 8%; polyarticular juvenile idiopathic arthritis, 16% to 20.2% )
Serious:
Gastrointestinal: Gastrointestinal perforation, Pancreatitis
Hematologic: Decreased platelet count (1% to 4% ), Neutropenia (Rheumatoid arthritis, 1.8% to 3.7% ; polyarticular or systemic juvenile idiopathic arthritis, 3.7% to 17% )
Immunologic: Anaphylaxis, Hypersensitivity reaction (Up to 0.9% ), Opportunistic infection, Tuberculosis
Respiratory: Upper respiratory infection (Rheumatoid arthritis, 6% to 8%; systemic juvenile idiopathic arthritis, 5% or higher )
Other: Cancer, Severe infectious disease.(UTD)
劑量和給藥方法
Rheumatoid arthritis (RA):
<100 kg: 162 mg once every other week; increase to 162 mg once every week based on clinical response
?100 kg: 162 mg once every week.
Transitioning from IV therapy to SubQ therapy: Administer the first SubQ dose instead of the next scheduled IV dose.(UTD)
小兒調整劑量
腎功能調整劑量
肝功能調整劑量
For patients receiving SubQ therapy with persistent increases >1 to 3 x ULN, reduce injection frequency to every other week or interrupt until ALT/AST have normalized; increase frequency to every week as clinically appropriate.(UTD)