Formulary
Tocilizumab: Indications, Dosing, Side Effects and Interactions
Tocilizumab is a recombinant humanised monoclonal antibody that binds to interleukin-6 receptors thereby blocking the activity of pro-inflammatory cytokines.
MedNext Academy | 7 min read
Tocilizumab: Indications, Dosing, Side Effects and Interactions
Tocilizumab is a recombinant humanised monoclonal antibody that binds to interleukin-6 receptors thereby blocking the activity of pro-inflammatory cytokines.
Drug action
Tocilizumab is a recombinant humanised monoclonal antibody that binds to interleukin-6 receptors thereby blocking the activity of pro-inflammatory cytokines.
Indications and dose
**Rheumatoid arthritis (initiated by a specialist)**
- **Adult** (By Intravenous Infusion): 8 mg/kg every 4 weeks (max. per dose 800 mg), for dose adjustments in patients with liver enzyme abnormalities, or low absolute neutrophil or platelet count-consult product literature.
- **Adult** (By Subcutaneous Injection): 162 mg once weekly, administer to abdomen, thigh or upper arm, for dose adjustments in patients with liver enzyme abnormalities, or low absolute neutrophil or platelet count-consult product literature.
**Giant cell arteritis (initiated by a specialist)**
- **Adult** (By Subcutaneous Injection): 162 mg once weekly, administer to abdomen, thigh or upper arm, for dose adjustments in patients with liver enzyme abnormalities, or low absolute neutrophil or platelet count-consult product literature, not to be used alone for acute relapses; review need for treatment beyond 52 weeks.
**COVID-19 in hospitalised patients who are receiving systemic corticosteroids and require oxygen supplementation or mechanical ventilation (initiated by a specialist)**
- **Adult** (By Intravenous Infusion): 8 mg/kg (max. per dose 800 mg) for 1 dose.
**Cytokine release syndrome (initiated by a specialist)**
- **Adult** (By Intravenous Infusion): (body-weight 30 kg and above) 8 mg/kg (max. per dose 800 mg), if no improvement in symptoms after the first dose, up to 3 additional doses may be administered. The interval between the infusions should be at least 8 hours.
**Systemic juvenile idiopathic arthritis (initiated by a specialist) for tocilizumab**
- **Child 2-17 years (body-weight up to 30 kg)** (By intravenous infusion): 12 mg/kg every 2 weeks, for dose adjustments in patients with liver enzyme abnormalities, or low absolute neutrophil or platelet count-consult product literature, review treatment if no improvement within 6 weeks.
- **Child 2-17 years (body-weight 30 kg and above)** (By intravenous infusion): 8 mg/kg every 2 weeks, for dose adjustments in patients with liver enzyme abnormalities, or low absolute neutrophil or platelet count- consult product literature, review treatment if no improvement within 6 weeks.
- **Child 1-17 years (body-weight 10-30 kg)** (By subcutaneous injection): 162 mg every 2 weeks, administer to abdomen, thigh or upper arm, for dose adjustments in patients with liver enzyme abnormalities, or low absolute neutrophil or platelet count-consult product literature, review treatment if no improvement within 12 weeks.
- **Child 1-17 years (body-weight 30 kg and above)** (By subcutaneous injection): 162 mg once weekly, administer to abdomen, thigh or upper arm, for dose adjustments in patients with liver enzyme abnormalities, or low absolute neutrophil or platelet count-consult product literature, review treatment if no improvement within 12 weeks.
**Polyarticular juvenile idiopathic arthritis (initiated by a specialist) for tocilizumab**
- **Child 2-17 years (body-weight up to 30 kg)** (By intravenous infusion): 10 mg/kg every 4 weeks, for dose adjustments in patients with liver enzyme abnormalities, or low absolute neutrophil or platelet count- consult product literature, review treatment if no improvement within 12 weeks.
- **Child 2-17 years (body-weight 30 kg and above)** (By intravenous infusion): 8 mg/kg every 4 weeks, for dose adjustments in patients with liver enzyme abnormalities, or low absolute neutrophil or platelet count-consult product literature, review treatment if no improvement within 12 weeks.
- **Child 2-17 years (body-weight up to 30 kg)** (By subcutaneous injection): 162 mg every 3 weeks, administer to abdomen, thigh or upper arm, for dose adjustments in patients with liver enzyme abnormalities, or low absolute neutrophil or platelet count-consult product literature, review treatment if no improvement within 12 weeks.
- **Child 2-17 years (body-weight 30 kg and above)** (By subcutaneous injection): 162 mg every 2 weeks, administer to abdomen, thigh or upper arm, for dose adjustments in patients with liver enzyme abnormalities, or low absolute neutrophil or platelet count-consult product literature, review treatment if no improvement within 12 weeks.
**Cytokine release syndrome (initiated by a specialist) for tocilizumab**
- **Child 2-17 years (body-weight up to 30 kg)** (By intravenous infusion): 12 mg/kg (max. per dose 800 mg), if no improvement in symptoms after the first dose, up to 3 additional doses may be administered. The interval between the infusions should be at least 8 hours.
- **Child 2-17 years (body-weight 30 kg and above)** (By intravenous infusion): 8 mg/kg (max. per dose 800 mg), if no improvement in symptoms after the first dose, up to 3 additional doses may be administered. The interval between the infusions should be at least 8 hours.
Cautions
When used for COVID-19 History of recurrent or chronic infection (interrupt treatment if serious infection occurs); predisposition to infection (interrupt treatment if serious infection occurs) When used for Giant cell arteritis Hepatic enzymes more than 1.5 times the upper limit of normal; history of diverticulitis; history of intestinal ulceration; history of recurrent or chronic infection (interrupt treatment if serious infection occurs); low absolute neutrophil count (discontinue treatment if neutrophil count less than 0.5 x 10 9 /litre); platelet count less than 100 x 10 3 /microlitre (discontinue treatment if platelet count less than 50 x 10 3 /microlitre); predisposition to infection (interrupt treatment if serious infection occurs) When used for Rheumatoid arthritis Hepatic enzymes more than 1.5 times the upper limit of normal; history of diverticulitis; history of intestinal ulceration; history of recurrent or chronic infection (interrupt treatment if serious infection occurs); low absolute neutrophil count (discontinue treatment if neutrophil count less than 0.5 x 10 9 /litre); platelet count less than 100 x 10 3 /microlitre (discontinue treatment if platelet count less than 50 x 10 3 /microlitre); predisposition to infection (interrupt treatment if serious infection occurs) Cautions, further information Tuberculosis When used for Rheumatoid arthritis or Giant cell arteritis: Patients with latent tuberculosis should be treated with standard therapy before starting tocilizumab. M
Contraindications
General contra-indications: Severe active infection (unless used for the treatment of COVID-19) Specific contra-indications: When used for COVID-19 Do not initiate if absolute neutrophil count less than 1 x 10 9 /litre; do not initiate if hepatic enzymes more than 10 times the upper limit of normal; do not initiate if platelet count less than 50 x 10 3 /microlitre When used for giant cell arteritis Do not initiate if hepatic enzymes more than 5 times the upper limit of normal; do not initiate in patients not previously treated with RoActemra if absolute neutrophil count less than 2 x 10 9 /litre When used for rheumatoid arthritis Do not initiate if hepatic enzymes more than 5 times the upper limit of normal; do not initiate in patients not previously treated with RoActemra if absolute neutrophil count less than 2 x 10 9 /litre
Side effects
Common or very common With parenteral use Abdominal pain; anxiety; conjunctivitis; constipation; cough; diarrhoea; dizziness; dyslipidaemia; dyspnoea; gastrointestinal disorders; headache; hypersensitivity; hypertension; hypofibrinogenaemia; hypokalaemia; increased risk of infection; insomnia; leucopenia; nausea; neutropenia; oral disorders; peripheral oedema; skin reactions; weight increased Uncommon With parenteral use Hypothyroidism; nephrolithiasis Rare or very rare With parenteral use Hepatic disorders; Stevens-Johnson syndrome Frequency not known With parenteral use Infusion related reaction; interstitial lung disease; pancytopenia; pulmonary fibrosis; sepsis
Interactions
**Other interactions (6):**
- Population pharmacokinetic analyses did not detect any effect of MTX, non-steroidal anti-inflammatory drugs (NSAIDs) or corticosteroids on tocilizumab clearance in RA patients.
- In GCA patients, no effect of cumulative corticosteroid dose on tocilizumab exposure was observed.
- In vitro studies with cultured human hepatocytes demonstrated that IL-6 caused a reduction in CYP1A2, CYP2C9, CYP2C19, and CYP3A4 enzyme expression.
- In a study in RA patients, levels of simvastatin (CYP3A4) were decreased by 57% one week following a single dose of tocilizumab, to the level similar to, or slightly higher than, those observed in...
- When starting or stopping therapy with tocilizumab, patients taking medicinal products which are individually adjusted and are metabolised via CYP450 3A4, 1A2 or 2C9 (e.g.
- Given its long elimination half-life (t 1/2 ), the effect of tocilizumab on CYP450 enzyme activity may persist for several weeks after stopping therapy.
Pregnancy
Manufacturer advises avoid unless essential-toxicity in animal studies.
Breast feeding
Specialist sources indicate use with caution. Monitor breast-fed infants for adequate feeding, fever, frequent infections, diarrhoea, or unusual behaviour.
Hepatic impairment
Manufacturer advises caution-consult product literature.
Renal impairment
With intravenous use: Manufacturer advises monitor renal function closely in moderate-to-severe impairment-no information available. With subcutaneous use: Manufacturer advises monitor renal function closely in severe impairment-no information available.
Medicinal forms
Solution,Solution
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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