Tìm theo
Anakinra
Các tên gọi khác (6 ) :
  • ICIL-1RA
  • IL-1ra
  • IL-1RN
  • IL1 inhibitor
  • Interleukin-1 receptor antagonist protein precursor
  • IRAP
antirheumatic agents, immunosuppressive agents
Thuốc Gốc
Biotech
CAS: 143090-92-0
ATC: L04AC03
ĐG : Amgen Inc. , http://www.amgen.com
CTHH: C759H1186N208O232S10
PTK: 17257.6000
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C759H1186N208O232S10
Phân tử khối
17257.6000
Độ kỵ nước
-0.412
Điểm đẳng điện tích
5.46
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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. 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.
Dược Động Học :
▧ Absorption :
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.
Độc Tính : 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.
Chỉ Định : For the treatment of adult rheumatoid arthritis and treatment of Neonatal-Onset Multisystem Inflammatory Disease (NOMID).
Tương Tác Thuốc :
  • Abatacept Avoid combination due to enhanced adverse effects of abatacept
  • Canakinumab results in increased immunosuppressive effects; increases the risk of infection.
  • Certolizumab pegol Co-administration with other TNF-blocking agents may increase the risk of serious infections. Concomitant therapy is not recommended.
  • Etanercept Avoid combination due to increased adverse effects of anakinra and increased risk of infections.
  • golimumab Avoid combination with anakinra due to the increased chance of serious infection.
  • Infliximab Combination may enhance the toxic effect of Anakinra and should be avoided otherwise there may be an increased risk of infection
  • Rilonacept results in increased immunosuppressive effects; increases the risk of infection.
  • Thalidomide Thalidomide may increase the adverse effects of Anakinra. Increased risk of serious infection. Concomitant therapy should be avoided.
  • Tofacitinib Avoid combination due to the potential increase in tofacitinib related adverse effects.
  • Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Liều Lượng & Cách Dùng : Injection, solution - Subcutaneous - 10MIU/VIAL; 18MIU/VIAL; 25MIU/VIAL
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Amgen Inc
    Sản phẩm biệt dược : Kineret
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00026
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02934
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/66658-234-28
GenBank
http://www.ncbi.nlm.nih.gov/nuccore/M55646
PharmGKB
http://www.pharmgkb.org/drug/PA10799
Wikipedia
http://en.wikipedia.org/wiki/Anakinra
RxList
http://www.rxlist.com/cgi/generic/anakinra.htm
Drugs.com
http://www.drugs.com/cdi/anakinra.html
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