Anakinra

Author: Prof. Dr. med. Peter Altmeyer

Last updated on: 13.01.2024

Definition
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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.

Pharmacodynamics (Effect)
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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.

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Indication
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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 period
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Contraindicated (insufficient data available).

Dosage and method of use
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once/day 100 mg s.c.

Undesirable effects
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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.

Interactions
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TNFα antagonists, e.g. Infliximab, Etanercept (insufficient experience).

Contraindication
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Hypersensitivity to proteins derived from E. coli, severe renal dysfunction (creatinine clearance < 30 ml/min), simultaneous vaccination with live vaccines.

Preparations
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Kineret®

Note(s)
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Remember! Women of childbearing age should use effective contraception during treatment (insufficient data available!)

Literature
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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