Interleukin-1 Receptor Antagonist

Aka: Interleukin-1 Receptor Antagonist, Interleukin 1 Receptor Antagonist Protein, Anti-IL6 Monoclonal Antibody, Anakinra, Kineret

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II. Indications

  1. FDA Approved
    1. Rheumatoid Arthritis (Severe active, refractory to DMARDs)
    2. Neonatal-Onset Multisystem Inflammatory Disease (NOMID)
  2. Other Off-Label Uses
    1. Still's Disease
    2. Juvenile Idiopathic Arthritis (JIA)
    3. Familial Mediterranean Fever
    4. Familial Cold Autoinflammatory Syndrome
    5. Muckle Wells Syndrome

III. Contraindications

  1. Chronic or acute infection
  2. Live Vaccination
  3. Concurrent use of TNF Antagonists (infection risk)
    1. Adalimumab (Humira)
    2. Etanercept (Enbrel)
    3. Infliximab (Remicade)

IV. Mechanism

  1. Interleukin-1
    1. Interleukin-1 is primarly synthesized by Monocytes and Macrophages
      1. Subtypes include IL-1a and IL-1b
      2. Triggers IL-2 release from activated T Cells (via Antigens or mitogens)
    2. Pro-inflammatory Cytokine (mediates the acute phase host response)
      1. Triggeres COX2 induction, prostanoid release
      2. Sensitizes peripheral Nociceptor terminals and increases local pain sensitivity
    3. Other effects
      1. Fever (endogenous pyrogen)
      2. Myalgias and Arthralgias
      3. Anorexia
  2. Interleukin-1 Receptor Antagonist
    1. Binds to Interleukin-1 Receptors without activating them, thereby inhibiting other agents from binding

V. Medications

  1. Store in refrigerator (until 30 minutes before injection)
  2. Protect from light

VI. Dosing: Rheumatoid Arthritis

  1. Rotate injection sites (thigh, Abdomen, upper outer arm, upper outer buttock)
  2. Adults: 100 mg SQ daily
  3. Renal Adjustment
    1. Consider every other day dosing in GFR <30 ml/min

VII. Dosing: Neonatal-Onset Multisystem Inflammatory Disease (NOMID)

  1. Rotate injection sites (thigh, Abdomen, upper outer arm, upper outer buttock)
  2. Adult or Child
    1. Start: 1 to 2 mg/kg SQ daily
    2. Titrate in 0.5 to 1 mg/kg increments up to maximum of 8 mg/kg SQ daily
  3. Renal Adjustment
    1. Consider every other day dosing in GFR <30 ml/min

VIII. Adverse Effects

  1. Immunosuppression
    1. Use caution in any patient prone to infection
  2. Headache
  3. Injection site inflammation
  4. Gastrointestinal upset
  5. Leukopenia (including Neutropenia)

IX. Safety

  1. Pregnancy Category B
  2. Unknown safety in Lactation
  3. Monitoring
    1. Serum Creatinine
    2. Complete Blood Count with Neutrophil Count
      1. Baseline, then
      2. Monthly for 3 months, then
      3. Quarterly

X. Resources

  1. Anakinra (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d9d74915-6606-4570-9c52-c4001d3177de

XI. References

  1. (2003) Lexicomp Drug Database

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