IL-1RA

IL-1RA Uses, Dosage, Side Effects, Food Interaction and all others data.

IL-1RA is a recombinant, nonglycosylated human interleukin-1 receptor antagonist (IL-1Ra). The difference between anakinra and the native human IL-1Ra is that anakinra has an extra methionine residue at the amino terminus. It is manufactured by using the E. coli expression system. IL-1RA is composed of 153 amino acid residues. FDA approved on November 14, 2001.

Used to treat rheumatoid arthritis, IL-1RA blocks the biologic activity of IL-1 by competitively inhibiting IL-1 binding to the interleukin-1 type I receptor (IL-1RI), which is expressed in a wide variety of tissues and organs. IL-1 production is induced in response to inflammatory stimuli and mediates various physiologic responses including inflammatory and immunological responses. Patients with rheumatoid arthritis have elevated levels of IL-1. The levels of the naturally occurring IL-1Ra in synovium and synovial fluid from rheumatoid arthritis (RA) patients are not sufficient to compete with the elevated amount of locally produced IL-1. Increasing the levels of IL-1Ra by artificial means reduces the negative effects (cartilage degradation, bone resorption) of IL-1.

Trade Name IL-1RA
Availability Prescription only
Generic Anakinra
Anakinra Other Names Anakinra, IL-1RA, Interleukin-1 receptor antagonist anakinra
Related Drugs Actemra, Kineret, Ilaris, Humira, hydroxychloroquine, Enbrel, Remicade, Rituxan, Orencia, Arcalyst
Type
Formula C759H1186N208O232S10
Weight 17257.6 Da
Groups Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
IL-1RA
IL-1RA

Uses

IL-1RA is a recombinant form of human interleukin-1 receptor antagonist used in the treatment of rheumatoid arthritis and neonatal-onset multisystem inflammatory disease.

For the treatment of adult rheumatoid arthritis and treatment of Neonatal-Onset Multisystem Inflammatory Disease (NOMID).

IL-1RA is also used to associated treatment for these conditions: Juvenile Idiopathic Arthritis (JIA), Neonatal-Onset Multisystem Inflammatory Disease (NOMID), Moderate Rheumatoid arthritis, Recurrent Pericarditis, Severe Rheumatoid arthritis

How IL-1RA works

IL-1RA binds competitively to the Interleukin-1 type I receptor (IL-1RI), thereby inhibiting the action of elevated levels IL-1 which normally can lead to cartilage degradation and bone resorption.

Toxicity

Most common adverse reactions (incidence ≥ 5%) are injection site reaction, worsening of rheumatoid arthritis, upper respiratory tract infection, headache, nausea, diarrhea, sinusitis, arthralgia, flu like-symptoms, and abdominal pain when anakinra is used in RA patients. In NOMID patients, the most common AEs during the first 6 months of treatment (incidence >10%) are injection site reaction, headache, vomiting, arthralgia, pyrexia, and nasopharyngitis.

Food Interaction

No interactions found.

Elimination Route

When a 70 mg subcutaneous bolus injection is given to healthy subjects, the absolute bioavailability is 95%. Accumulation does not occur following daily subcutaneous doses. Tmax, SubQ, 1-2 mg/kg, healthy subjects = 3-7 hours; Cmax, SubQ, 3 mg/kg once daily, NOMID patients = 3628 ng/mL.

Half Life

Healthy subjects = 4 - 6 hours; NOMID patients = 5.7 hours (range of 3.1 - 28.2 hours).

Clearance

Clearance is variable and increases with increasing creatinine clearance and body weight. However, gender and age were not significant factors.

Innovators Monograph

You find simplified version here IL-1RA

*** Taking medicines without doctor's advice can cause long-term problems.
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