Tocilizumab


Concise Prescribing Info
Indications/Uses
Rheumatoid arthritis.
Dosage/Direction for Use
Adult : IV Initial: 4 mg/kg once every 4 wk, may increase to a usual dose of 8 mg/kg once every 4 wk. Max: 800 mg. SC 162 mg once wkly.
Dosage Details
Intravenous
Rheumatoid arthritis
Adult: As monotherapy or in combination w/ methotrexate or other non-biologic disease-modifying drugs (DMARDs): Initially, 4 mg/kg once every 4 wk, may be increased to a usual dose of 8 mg/kg once every 4 wk via infusion over 1 hr. Max: 800 mg. Do not initiate in patients w/ absolute neutrophil count (ANC) <2 x 109/L, platelet count <100 x 109/L, or ALT/AST >1.5 x ULN (upper limit of normal). Interrupt dosing if ANC 0.5-1 x 109/L, platelet count 50-100 x 109/L, or ALT/AST >3-5 ULN. Discontinue if ANC <0.5 x 109/L, platelet count <50 x 109/L, or ALT/AST >5 x ULN.
Child: ≥2 yr Systemic juvenile idiopathic arthritis: <30 kg: 12 mg/kg; ≥30 kg: 8 mg/kg. Doses are given once every 2 wk via infusion over 1 hr. Juvenile idiopathic polyarthritis: <30 kg: 10 mg/kg; ≥30 kg: 8 mg/kg. Doses are given once every 4 wk via infusion over 1 hr.

Subcutaneous
Rheumatoid arthritis
Adult: As monotherapy or in combination w/ methotrexate or other non-biologic DMARDs: 162 mg once wkly. Do not initiate in patients w/ absolute neutrophil count (ANC) <2 x 109/L, platelet count <100 x 109/L, or ALT/AST >1.5 x ULN (upper limit of normal). Interrupt dosing if ANC 0.5-1 x 109/L, platelet count 50-100 x 109/L, or ALT/AST >3-5 ULN. Discontinue if ANC <0.5 x 109/L, platelet count <50 x 109/L, or ALT/AST >5 x ULN.
Reconstitution
IV infusion: Dilute w/ NaCl 0.45% or 0.9% to a final volume of 50 mL (for childn <30 kg) or 100 mL (for adult and childn ≥30 kg). Withdraw equal volume of NaCl 0.9% or 0.45% to the volume of drug required for dose then slowly add tocilizumab dose into infusion bag or bottle.
Contraindications
Severe active infections (e.g. sepsis, abscess, hepatitis B, active TB). Concomitant use w/ other biologic DMARDs.
Special Precautions
Patient w/ history of recurrent or chronic infections, or conditions that may predispose to infections (e.g. diverticulitis, DM), pre-existing or recent CNS demyelinating disorders, and those at risk for GI perforation. Hepatic impairment or active hepatic disease. Childn. Pregnancy and lactation.
Adverse Reactions
Significant: GI perforation, elevated transaminases, hyperlipidaemia, neutropenia, thrombocytopenia, viral reactivation (e.g. hepatitis B virus, HZV), auto-immune effects, malignancies. Rarely, multiple sclerosis, chronic inflammatory demyelinating polyneuropathy.
Nervous: Headache, flu-like symptoms, dizziness.
CV: HTN, hypotension, peripheral oedema.
GI: Gastritis, mouth ulcers, diarrhoea, nausea, abdominal pain.
Resp: Nasopharyngitis, upper resp tract infection, bronchospasm.
Endocrine: Hypertryglyceridaemia, hypothryroidism.
Haematologic: Leucopenia.
Ophthalmologic: Conjunctivitis.
Others: Infusion-related (e.g. HTN, headache, rash, hypersensitivity) or SC inj site (e.g. haematoma, erythema, pain, pruritus) reactions.
Potentially Fatal: Serious infections (e.g. active TB, invasive fungal infections, bacterial, viral and other opportunistic infections, serious hypersensitivity reactions (e.g. anaphylaxis).
Patient Counseling Information
This drug may cause dizziness, if affected, do not drive or operate machinery.
MonitoringParameters
Measure neutrophil and platelet counts, lipids, and LFTs before and regularly during treatment. Perform screening test for latent TB prior to therapy. Monitor signs and symptoms of CNS demyelinating disorders.
Drug Interactions
Risk of secondary transmission of infection when given concurrently w/ live vaccines. May increase the metabolism of drugs that are metabolised by CYP enzymes.
Potentially Fatal: Increased risk of infection w/ other biologic DMARDs, including tumour necrosis factor (TNF) blocking agents (e.g. adalimumab, etanercept, infliximab), IL-1 receptor antagonists (e.g. anakinra), anti-CD20 monoclonal antibodies (e.g. rituximab), selective costimulation modulators (e.g. abatacept).
Action
Description: Tocilizumab, a recombinant humanised monoclonal antibody of the IgG1 subclass, inhibits the actions of interleukin-6 (sIL-6R and mIL- 6R), a pleiotropic pro-inflammatory cytokine that is involved in T-cell activation, induction of Ig secretion, initiation of hepatic acute phase protein synthesis, and stimulation of haematopoiesis. It binds specifically to both soluble and membrane-bound IL-6 receptors and inhibits IL-6-mediated signaling, thereby resulting in a reduction in inflammatory mediator production.
Pharmacokinetics:
Absorption: Bioavailability: 80% (SC).
Distribution: Volume of distribution: 6.4L (IV).
Excretion: Elimination half-life: IV: Concentration-dependent: 6.3 days (up to 11-13 days); SC: up to 13 days.
Storage
Store between 2-8°C. Do not freeze. Protect from light. 
ATC Classification
L04AC07 - tocilizumab ; Belongs to the class of interleukin inhibitors. Used as immunosuppressants.
Disclaimer: This information is independently developed by MIMS based on Tocilizumab from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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