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: Anakinra (Kineret) 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)
- Anakinra (Kineret): 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. Drug Interactions
-
Live Vaccines
- Hold for 1 dosing interval before and 4 weeks after Live Vaccines
XI. Resources
XII. References
- (2003) Lexicomp Drug Database
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Related Studies
| Definition (NCI) | A recombinant human nonglycosylated interleukin-1 (IL-1) receptor antagonist with potential antineoplastic activity. Anakinra binds to the IL-1 receptor, thereby blocking the binding of the IL-1 to and activation of its receptor. Blockade of IL-1 activity may inhibit the cascade of downstream pro-angiogenic factors such as vascular endothelial cell growth factor, tumor necrosis factor-alpha, and IL-6, resulting in inhibition of tumor angiogenesis. (NCI04) |
| Definition (NCI_NCI-GLOSS) | A substance that is used to treat rheumatoid arthritis, and is being studied in the treatment of cancer. Anakinra blocks the action of interleukin 1 (IL-1). It is a type of interleukin receptor antagonist. |
| Definition (MSH) | A synthetic form of native human IL-1Ra that has an additional methionine residue at its amino terminus. |
| Definition (PDQ) | A recombinant human nonglycosylated interleukin-1 (IL-1) receptor antagonist with potential antineoplastic activity. Anakinra binds to the IL-1 receptor, thereby blocking the binding of the IL-1 to and activation of its receptor. Blockade of IL-1 activity may inhibit the cascade of downstream pro-angiogenic factors such as vascular endothelial cell growth factor, tumor necrosis factor-alpha, and IL-6, resulting in inhibition of tumor angiogenesis. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43007&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43007&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C38717" NCI Thesaurus) |
| Concepts | Amino Acid, Peptide, or Protein (T116) , Pharmacologic Substance (T121) |
| MSH | D053590 |
| SnomedCT | 395279009, 385549000 |
| English | Anakinra, anakinra (medication), Anakinra (obsolete), Anakinra [Chemical/Ingredient], rIL-1ra, rIL1RN, Kinaret, anakinra, Anakinra (product), Anakinra (substance), ANAKINRA |
| French | Anakinra |
| German | Anakinra |
| Czech | anakinra |
| Japanese | アナキンラ |
| Spanish | anakinra (producto), anakinra (sustancia), anakinra |
Ontology: Kineret (C1170364)
| Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
| MSH | D053590 |
| English | Kineret, Amgen Brand of Anakinra, Anakinra Amgen Brand, kineret |
| French | Kineret |
| German | Kineret |
| Czech | Kineret |
Ontology: Interleukin 1 Receptor Antagonist Protein (C1704264)
| Definition (MSH) | A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA. |
| Definition (NCI) | Interleukin-1 receptor antagonist protein (177 aa, ~20 kDa) is encoded by the human IL1RN gene. This protein is involved in the inhibition of the interaction between interleukin-1 and its receptor. |
| Concepts | Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116) |
| MSH | D053590 |
| English | Febrile Inhibitor, IL1, IL 1 Inhibitor, Urine, IL-1 Inhibitor, Urine, IL-1Ra, IL1 Febrile Inhibitor, IL1 Inhibitor, Urine-Derived, Interleukin 1 Inhibitor, Urine, Urine Derived IL1 Inhibitor, Urine IL-1 Inhibitor, Urine-Derived IL1 Inhibitor, Interleukin 1 Receptor Antagonist Protein, INTERLEUKIN 001 RECEPTOR ANTAGONIST PROTEIN, Interleukin 1 Receptor Antagonist Protein [Chemical/Ingredient], il-1ra, IRAP, IL-1RN, IL1 Inhibitor, Intracellular Interleukin-1 Receptor Antagonist, ICIL-1RA, Interleukin-1 Receptor Antagonist Protein, Intracellular IL-1 Receptor Antagonist Type II, IL-1ra, interleukin-1 receptor antagonist |
| Portuguese | Proteína Antagonista do Receptor de Interleucina 1, Proteína Antagonista do Receptor da Interleucina 1 |
| Spanish | Proteína Antagonista del Receptor de Interleucina 1, Proteína Antagonista del Receptor de la Interleucina 1 |
| Russian | ИНТЕРЛЕЙКИНА-1 РЕЦЕПТОРА БЕЛОК-АНТАГОНИСТ, INTERLEIKINA-1 RETSEPTORA BELOK-ANTAGONIST |
| German | Interleukin-1-Rezeptor-Antagonist, Urine-Derived-IL1-Inhibitor, Interleukin-1-Rezeptor-Antagonist-Protein, IL-1-Inhibitor, Harn, IL-1-Inhibitor, Urin, IL1-Febrile-Inhibitor, Interleukin-1-Rezeptorantagonist, IL-1Ra |
| French | Antagoniste du récepteur à IL1, Antagoniste du récepteur à la cytokine proinflammatoire IL-1, Antagoniste du récepteur de l'interleukine-1, Antagoniste du récepteur à la cytokine pyrogène IL1, Antagoniste du récepteur IL1-R, Antagoniste du récepteur à la cytokine pro-inflammatoire IL-1, IL-1Ra, Antagoniste du récepteur à IL-1, Antagoniste du récepteur à l'interleukine-1, Antagoniste du récepteur à la cytokine IL1, Inhibiteur de la cytokine pro-inflammatoire IL-1 |
| Finnish | Interleukiini 1 -reseptorin antagonistiproteiini |
| Czech | receptor interleukinu 1 - antagonista, receptor pro interleukin 1 - antagonista, IL-1Ra, antagonista receptoru pro interleukin 1 |
| Japanese | インターロイキン1受容体アンタゴニスト, インターロイキン1レセプターアンタゴニスト, IL-1受容体アンタゴニスト, IL-1レセプターアンタゴニスト, インターロイキン1受容体アンタゴニスト蛋白質 |
| Italian | Proteina antagonista del recettore dell'interleuchina-1 |
| Swedish | Interleukin 1 Receptor Antagonist Protein |
| Polish | Białko antagonistyczne receptora interleukiny 1 |
