II. Indications
- FDA Approved
- Rheumatoid Arthritis (Severe active, refractory to DMARDs)
- Neonatal-Onset Multisystem Inflammatory Disease (NOMID)
- Other Off-Label Uses
- Still's Disease
- Juvenile Idiopathic Arthritis (JIA)
- Familial Mediterranean Fever
- Familial Cold Autoinflammatory Syndrome
- Muckle Wells Syndrome
III. Contraindications
- Chronic or acute infection
- Live Vaccination
- Concurrent use of TNF Antagonists (infection risk)
IV. Mechanism
-
Interleukin-1
- Interleukin-1 is primarly synthesized by Monocytes and Macrophages
- Subtypes include IL-1a and IL-1b
- Triggers IL-2 release from activated T Cells (via Antigens or mitogens)
- Pro-inflammatory Cytokine (mediates the acute phase host response)
- Triggeres COX2 induction, prostanoid release
- Sensitizes peripheral Nociceptor terminals and increases local pain sensitivity
- Other effects
- Fever (endogenous pyrogen)
- Myalgias and Arthralgias
- Anorexia
- Interleukin-1 is primarly synthesized by Monocytes and Macrophages
- Interleukin-1 Receptor Antagonist
- Binds to Interleukin-1 Receptors without activating them, thereby inhibiting other agents from binding
V. Medications
- Store in refrigerator (until 30 minutes before injection)
- Protect from light
VI. Dosing: Rheumatoid Arthritis
- Rotate injection sites (thigh, Abdomen, upper outer arm, upper outer buttock)
- Adults: 100 mg SQ daily
- Renal Adjustment
- Consider every other day dosing in GFR <30 ml/min
VII. Dosing: Neonatal-Onset Multisystem Inflammatory Disease (NOMID)
- Rotate injection sites (thigh, Abdomen, upper outer arm, upper outer buttock)
- Adult or Child
- Start: 1 to 2 mg/kg SQ daily
- Titrate in 0.5 to 1 mg/kg increments up to maximum of 8 mg/kg SQ daily
- Renal Adjustment
- Consider every other day dosing in GFR <30 ml/min
VIII. Adverse Effects
-
Immunosuppression
- Use caution in any patient prone to infection
- Headache
- Injection site inflammation
- Gastrointestinal upset
- Leukopenia (including Neutropenia)
IX. Safety
- Pregnancy Category B
- Unknown safety in Lactation
- Monitoring
- Serum Creatinine
- Complete Blood Count with Neutrophil Count
- Baseline, then
- Monthly for 3 months, then
- Quarterly
X. Resources
XI. References
- (2003) Lexicomp Drug Database