Anakinra

Anakinra Uses, Dosage, Side Effects, Food Interaction and all others data.

Anakinra 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. Anakinra is composed of 153 amino acid residues. FDA approved on November 14, 2001.

Used to treat rheumatoid arthritis, Anakinra 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.

Anakinra
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Anakinra
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
Weight	100mg/0.67ml,
Type	Subcutaneous Solution, Subcutaneous
Formula	C₇₅₉H₁₁₈₆N₂₀₈O₂₃₂S₁₀
Weight	17257.6 Da
Groups	Approved
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Anakinra 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).

Anakinra 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 Anakinra works

Anakinra 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.

Anakinra 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.