Interleukin-1 receptor antagonist(see also CD121a). Recombinant variant of the endogenous interleukin-1 receptor antagonist(IL-1Ra) obtained by genetic engineering from E. coli.
Anakinra
DefinitionThis section has been translated automatically.
Pharmacodynamics (Effect)This section has been translated automatically.
Anakinra causes a shift in the balance of endogenous IL-1 antagonists and IL-1 receptors, which is disturbed in inflammatory diseases, in favour of endogenous IL-1 antagonists.
IL-1 physiologically binds to the membrane-bound IL-1 receptor type 1, which then forms a heterodimeric complex with the accessory protein IL-1RacP. This complex triggers an intracellular signalling cascade during inflammation. In case of excess of IL-1 antagonists by application of anakinra, the inflammation cascade is inhibited.
Thus, Anakinra inhibits the recruitment of neutrophil granulocytes in joints mediated by interleukin-1, the activation of macrophages and the differentiation of T and B lymphocytes. Secondarily, this reduces the destruction of bone and cartilage as well as swelling and intra-articular pain.
IndicationThis section has been translated automatically.
Chronic polyarthritis (rheumatoid arthritis) (combination therapies with methotrexate in patients with an inadequate response to MTX alone). Good response has been described in Muckle-Wells Syndrome and Schnitzler Syndrome (100 mg/day s.c. every 2nd day) ( off-label use). According to individual case reports, good effectiveness in systemic lupus erythematosus (with lupus arthritis) ( off-label use).
Pregnancy/nursing periodThis section has been translated automatically.
Contraindicated (insufficient data available).
Dosage and method of useThis section has been translated automatically.
once/day 100 mg s.c.
Undesirable effectsThis section has been translated automatically.
Very frequent: headache, reactions at the injection site ( erythema, local oedema). This seems to be caused by a vehicle-associated effect such as a low pH or the citrate buffer itself.
Common: neutropenia, bacterial infections.
InteractionsThis section has been translated automatically.
TNFα antagonists, e.g. Infliximab, Etanercept (insufficient experience).
ContraindicationThis section has been translated automatically.
Hypersensitivity to proteins derived from E. coli, severe renal dysfunction (creatinine clearance < 30 ml/min), simultaneous vaccination with live vaccines.
PreparationsThis section has been translated automatically.
Kineret®
Note(s)This section has been translated automatically.
Remember! Women of childbearing age should use effective contraception during treatment (insufficient data available!)
LiteratureThis section has been translated automatically.
- Bresnihan B (2002) Anakinra as a new therapeutic option in rheumatoid arthritis: clinical results and perspectives. Clin Exp Rheumatol 20: S32-34
- Calabrese LH (2002) Anakinra treatment of patients with rheumatoid arthritis. Ann Pharmacother 36: 1204-1209
- Hawkins PN et al (2004) Spectrum of clinical features in Muckle-Wells syndrome and response to anakinra. Arthritis Rheum 50: 607-612