Tocilizumab

Anti-rheumatic, Systemic · Cytokine modulator

Indications

Moderate to severe active rheumatoid arthritis in adults, in combination with methotrexate or as monotherapy if methotrexate not tolerated or inappropriate, when previous therapy with one or more DMARD or TNF antagonist was inadequate or not tolerated. Active systemic juvenile idiopathic arthritis (SJIA), in combination with methotrexate or as monotherapy if methotrexate not tolerated or inappropriate, when response to NSAID and systemic corticosteroid inadequate.

Dosage

Adults: Rheumatoid arthritis: By IV infusion initially 4 mg/kg, may be increased to 8 mg/kg (max 800 mg) once every 4 wk. Children: Active systemic juvenile idiopathic arthritis, in combination with methotrexate or alone if methotrexate inappropriate) who have had an inadequate response to NSAIDs and systemic corticosteroids: IV infusion: 2-18 yr body-weight less than 30 kg, 12 mg/kg once every 2 wk; review treatment if no improvement within 6 wk; body-weight over 30 kg, 8 mg/kg once every 2 wk; review treatment if no improvement within 6 wk. Polyarticular juvenile idiopathic arthritis, in combination with methotrexate or alone if methotrexate inappropriate who have had an inadequate response to methotrexate: IV infusion: 2-18 yr body-weight less than 30 kg, 10 mg/kg once every 4 wk; review treatment if no improvement within 12 wk; body-weight over 30 kg, 8 mg/kg once every 4 wk; review…

Administration

Dilute to 100 mL and give by IV infusion over 1 hour. For children, dilute to 100 mL (50 mL if <30 kg) and given by IV infusion over 1 hour. Stability: Refrigerate at 2°C-8°C (36°F-46°F). Do not freeze. Protect the vials from light by storage in the original package until time of use. The fully diluted solutions may be stored at 2°C-8°C or room temperature for up to 24 hours and should be protected from light. Unused product remaining in the vials should not be used.

Adverse Effects

Infections, headache, hypertension, raised liver enzymes and bilirubin, weight gain, GI upset, mouth ulceration, rash, pruritus, urticaria, dizziness, blood dyscrasias, hypercholesterolaemia, peripheral oedema, cough, dyspnoea.

Risk Factor (Pregnancy/Lactation)

Pregnancy: Contraindicated in pregnancy. Lactation: Contraindicated or not recommended. Contraindications: Active, severe infections. ALT/AST >5 x ULN. ANC <2 x 109/L before treatment. Patients who develop ANC <0.5 x 109/L or platelet count <50 x 10³/µL. Precautions: History of recurrent or chronic infections or underlying conditions (e.g. diverticulitis, diabetes, interstitial lung disease). If serious infection develops, interrupt therapy until controlled. Screen for latent TB before starting therapy. Monitor renal function. Active liver disease or hepatic impairment. Monitor ALT/AST, neutrophil and platelets at base line. Assess lipid parameters. Monitor for the symptoms of demyelinating disorders. Hypersensitivity reactions during infusions, discontinue if occur; ensure emergency treatment is available. Macrophage activation syndrome.

Interactions

Live vaccines, TNF antagonists, drugs metabolized by CYP450 enzymes (e.g. atorvastatin, calcium-channel blockers, theophylline, warfarin, phenytoin, cyclosporin, benzodiazepines), hepatotoxic drugs.

Advice to Patient

Contact prescriber if there is difficulty in breathing, swelling on face, rash, constant and severe abdominal pain. Avoid highly crowded places to prevent infection. Get all laboratory tests done as recommended by prescriber. Do not receive live-virus vaccines during therapy.

Pharmacokinetics

Metabolism: Via proteolytic enzymes. Half-life elimination: Rheumatoid arthritis: Up to 11-13 days. Systemic juvenile idiopathic arthritis: Up to 23 days. Juvenile Idiopathic Polyarthritis: Up to 16 days.

Compiled by Healify Pharmacy from published drug references. How we compile it →

Always consult a pharmacist or doctor.