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词条 Anakinra
释义

  1. Medical use

  2. Adverse effects

  3. Chemistry

  4. History

  5. References

{{Drugbox
| Verifiedfields = changed
| verifiedrevid = 457810558
| IUPAC_name = Recombinant human Interleukin-1 receptor antagonist protein; syn. N2-l-methionyl-interleukin 1 receptor antagonist (human isoform x reduced)
| image = Anakinra.png
| width = 220
| tradename = Kineret
| Drugs.com = {{drugs.com|monograph|anakinra}}
| MedlinePlus = a602001
| pregnancy_AU = B1
| pregnancy_US = B
| licence_EU = yes
| legal_AU = S4
| legal_CA = Rx-only
| legal_UK = POM
| legal_US = Rx-only
| routes_of_administration = Subcutaneous
| bioavailability = 95%
| protein_bound =
| metabolism = predominantly renal
| elimination_half-life = 4-6 hrs
| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
| ChemSpiderID = none
| CAS_number_Ref = {{cascite|correct|??}}
| CAS_number = 143090-92-0
| ATC_prefix = L04
| ATC_suffix = AC03
| ATC_supplemental =
| PubChem =
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB00026
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 9013DUQ28K
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D02934
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 1201570
| C=759 | H=1186 | N=208 | O=232 | S=10
| molecular_weight = 17,257.6 g/mol
}}Anakinra (brand name Kineret) is a biopharmaceutical drug used to treat rheumatoid arthritis. It is a recombinant and slightly modified version of the human interleukin 1 receptor antagonist protein. It is marketed by Swedish Orphan Biovitrum.[1]

Medical use

Anakinra is administered at home by subcutaneous injection.[2]

It is used as a second line treatment to manage symptoms of rheumatoid arthritis after treatment with a disease-modifying antirheumatic drug (DMARD) has failed.[1][2] It can be used in combination with some DMARDs.[1][2][3]

It is used to treat anyone from infants to adults with a cryopyrin-associated periodic syndrome, including neonatal-onset multisystem inflammatory disease.[1][2]

It is used off label to treat Schnitzler's syndrome.[4]

It was not tested in pregnant women, but appeared to be safe in animal studies.[2]

It should not be used in people who have active infections or latent tuberculosis, who have low white blood cells counts, or who are taking TNF inhibitors.[2]

Adverse effects

More than ten percent of people taking anakinra have injection site reactions, headaches, and have increased levels of cholesterol in their blood.[1]

Between one and ten percent of people have severe infections, decreased white blood cells, or decreased platelets.[1]

It is unclear if taking anakinra increases the risk of getting cancer; studies are complicated by the fact that people with rheumatoid arthritis are already at higher risk of getting cancer.[1][3]

Chemistry

Anakinra is a protein that differs from the sequence of Interleukin 1 receptor antagonist by one methionine added to its N-terminus; it also differs from the human protein in that it is not glycosylated, as it is manufactured in Escherichia coli.[2]

History

It was first approved in the US in 2001[2] and Europe in March 2002.[1]

In June 2018 NHS England published a Clinical Commissioning Policy: Anakinra to treat periodic fevers and autoinflammatory disorders (all ages) allowing Anakinra to be commissioned as a first-line treatment for Schnitzler's syndrome and in cases where the first-line treatment is not effective for Familial Mediterranean fever, Hyper-IgD syndrome also known as Mevalonate kinase deficiency, and TNF receptor associated periodic syndrome (TRAPS),[5] and a Clinical Commissioning Policy: Anakinra/tocilizumab for the treatment of Adult-Onset Still's Disease refractory to second-line therapy (adults), allowing Anakinra to be commissioned for Adult-onset Still's disease "as a third line treatment where patients are refractory to steroid-sparing effect DMARDs".[6] Anakira effectively treated meningitis caused by a rare genetic mutation in the gene NALP3 in a 67-year-old man enrolled in the Undiagnosed Diseases Network.[7]

References

1. ^{{cite web|title=UK Anakinra label|url=https://www.medicines.org.uk/emc/product/559|publisher=UK Electronic Medicines Compendium|accessdate=23 March 2018|language=en|date=5 October 2017}}
2. ^{{cite web|title=US Anakinra label|url=https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/103950s5175lbl.pdf|publisher=FDA|accessdate=23 March 2018|date=May 2016}} For label updates see [https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=overview.process&ApplNo=103950 FDA index page for BLA 103950]
3. ^{{cite journal|last1=Singh|first1=JA|last2=Hossain|first2=A|last3=Tanjong Ghogomu|first3=E|last4=Kotb|first4=A|last5=Christensen|first5=R|last6=Mudano|first6=AS|last7=Maxwell|first7=LJ|last8=Shah|first8=NP|last9=Tugwell|first9=P|last10=Wells|first10=GA|title=Biologics or tofacitinib for rheumatoid arthritis in incomplete responders to methotrexate or other traditional disease-modifying anti-rheumatic drugs: a systematic review and network meta-analysis|journal=The Cochrane Database of Systematic Reviews|date=13 May 2016|issue=5|pages=CD012183|doi=10.1002/14651858.CD012183|pmid=27175934}}
4. ^{{cite journal|last1=Gusdorf|first1=L|last2=Lipsker|first2=D|title=Schnitzler Syndrome: a Review|journal=Current Rheumatology Reports|date=August 2017|volume=19|issue=8|pages=46|doi=10.1007/s11926-017-0673-5|pmid=28718061}}
5. ^{{cite book |last1=NHS England |title=Clinical Commissioning Policy: Anakinra to treat periodic fevers and autoinflammatory disorders (all ages) |date=29 June 2018 |url=https://www.england.nhs.uk/wp-content/uploads/2018/07/1713-anakinra-for-periodic-fever.pdf |accessdate=9 July 2018}}
6. ^{{cite book |last1=NHS England |title=Clinical Commissioning Policy: Anakinra/tocilizumab for the treatment of Adult-Onset Still's Disease refractory to second-line therapy (adults) |date=29 June 2018 |url=https://www.england.nhs.uk/wp-content/uploads/2018/07/1609-anakinra-and-tocilizumab-for-aosd.pdf |accessdate=13 July 2018}}
7. ^{{Cite news|url=https://www.nytimes.com/2019/01/07/health/patients-medical-mysteries.html|title=When the Illness Is a Mystery, Patients Turn to These Detectives|last=Kolata|first=Gina|date=2019-01-07|work=The New York Times|access-date=2019-01-09|language=en-US|issn=0362-4331}}
{{Immunosuppressants}}{{Interleukin receptor modulators}}

1 : Immunosuppressants

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