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 |
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.IL-1RA Drug Interaction
Unknown: charcoal, charcoal, amoxicillin / clavulanate, amoxicillin / clavulanate, duloxetine, duloxetine, sodium iodide, sodium iodide, acetaminophen, acetaminophen, bioflavonoids, bioflavonoids, cyanocobalamin, cyanocobalamin, pyridoxine, pyridoxine, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
IL-1RA Disease Interaction
Major: infections, renal deficiency, tuberculosisModerate: liver disease, neutropenia
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
