Tocilizumab

Generic Details

Generic Name

Tocilizumab

Other Names

  • Actemra

Drug Class

  • Interleukin-6 (IL-6) receptor antagonist

Chemical Formula

C6428H9978N1722O2018S42

Molecular Weight

145476.9 g/mol

Mechanism of Action

  • Blocks the interleukin-6 (IL-6) receptor, inhibiting IL-6 mediated signaling

Indications

  • Rheumatoid arthritis
  • Juvenile idiopathic arthritis
  • Systemic juvenile idiopathic arthritis
  • Giant cell arteritis
  • Cytokine release syndrome
  • Severe or life-threatening cytokine storm syndrome
  • COVID-19 pneumonia

Common Dosage Forms

  • Injection

Typical Dosage

  • 4-8 mg/kg every 4 weeks for rheumatoid arthritis
  • 8-12 mg/kg every 2 weeks for systemic juvenile idiopathic arthritis

Pediatric Dosage

  • <30 kg: dose based on weight, ≥30 kg: adult dosage may be used

Geriatric Dosage

  • Dose adjustments based on renal function

Side Effects

  • Upper respiratory tract infections
  • Increased liver enzymes
  • Elevated cholesterol levels
  • Headache
  • Hypertension
  • Nasopharyngitis

Contraindications

  • Hypersensitivity to tocilizumab or any component of the formulation

Pregnancy Category

  • Category C

Lactation Safety

  • Limited data available, use with caution

Drug Interactions

  • Avoid use with live vaccines
  • May increase risk of infection when used with other immunosuppressive agents

Overdose Symptoms

  • Not well-defined, monitor for signs of infection or adverse effects

Antidote for Overdose

  • No specific antidote, provide supportive care

Storage Conditions

  • Refrigerate at 2-8°C (36-46°F), do not freeze

Pharmacokinetics

  • Absorption: Bioavailability: ~80%
  • Distribution: Distributed into the systemic circulation
  • Metabolism: Primarily hepatic metabolism
  • Excretion: Mainly excreted in the feces

Precautions

  • Monitor for signs of infection during treatment
  • Risk of gastrointestinal perforations
  • Hepatotoxicity potential

Warnings

  • Increased risk of serious infections
  • Risk of gastrointestinal perforations
  • Hepatotoxicity
  • Hypersensitivity reactions

Others