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Anakinra


Thông tin thuốc gốc
Chỉ định và Liều dùng
Subcutaneous
Cryopyrin associated periodic syndrome
Adult: For the treatment of cryopyrin associated periodic syndromes (CAPS), including neonatal-onset multisystem inflammatory disease (NOMID), familial cold autoinflammatory syndrome (FCAS) and Muckle-Wells syndrome (MWS): Initially, 1-2 mg/kg daily. Initial dose may be maintained in mild CAPS (FCAS and mild MWS). In severe CAPS (MWS and NOMID), dose may be adjusted in increments of 0.5-1 mg/kg after 1-2 months based on therapeutic response; usual maintenance dose is 3-4 mg/kg daily, may be adjusted up to a Max of 8 mg/kg daily. Doses may be administered once daily (preferred) or divided and administered bid. Treatment recommendations may vary among countries (refer to local or country-specific product guidelines).
Child: ≥8 months Patients weighing ≥10 kg: Same as adult dose.

Subcutaneous
Rheumatoid arthritis
Adult: For moderate to severely active cases when response to methotrexate or another DMARD alone has been inadequate: 100 mg once daily given at approx same time each day. Dose may be given alone or in combination with methotrexate or other DMARDs (excluding tumour necrosis factor [TNF] inhibitors). Treatment recommendations may vary among countries (refer to local or country-specific product guidelines).

Subcutaneous
Deficiency of interleukin-1 receptor antagonist
Adult: Initially, 1-2 mg/kg daily. Dose may be adjusted in increments of 0.5-1 mg/kg as necessary, up to a Max of 8 mg/kg daily. Treatment recommendations may vary among countries (refer to local or country-specific product guidelines).

Subcutaneous
Adult onset Still’s disease, Systemic juvenile idiopathic arthritis
Adult: As monotherapy or in combination with other anti-inflammatory agents and DMARDs in patients with active systemic features of moderate to high disease activity or with continued disease activity after NSAIDs or corticosteroids treatment: Patients weighing <50 kg: Initially, 1-2 mg/kg daily; ≥50 kg: 100 mg daily. Evaluate clinical response after 1 month of therapy. Dosage and treatment recommendations may vary among countries (refer to local or country-specific product guidelines).
Child: ≥8 months As monotherapy or in combination with other anti-inflammatory agents and DMARDs in patients with active systemic features of moderate to high disease activity or with continued disease activity after NSAIDs or corticosteroids treatment: Patients weighing 10-49 kg: Initially, 1-2 mg/kg daily; ≥50 kg: 100 mg daily. Dose may be adjusted up to 4 mg/kg daily if response is inadequate. Evaluate clinical response after 1 month of therapy. Dosage and treatment recommendations may vary among countries (refer to local or country-specific product guidelines).
Suy thận
ESRD (including dialysis): Consider reducing the dose frequency to every other day.
CrCl (mL/min) Dosage
<30 Consider reducing the dose frequency to every other day.
Chống chỉ định
Hypersensitivity to Escherichia coli-derived proteins or anakinra. Neutropenia (ANC <1.5 x 109/L).
Thận trọng
Patient with asthma, history of recurrent infections, underlying condition predisposing to infection (e.g. advanced or poorly controlled diabetes). Not recommended for use in patients with pre-existing malignancy. Concomitant use with TNF inhibitors (e.g. etanercept) is not recommended. Live vaccines must not be given concurrently during anakinra therapy. Treatment with anakinra must not be started in patients with active infections, including chronic or localised infections. Moderate to severe renal and severe hepatic impairment. Children and elderly. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Serious infections (e.g. pneumonia, cellulitis, bone and joint infections); increased risk of reactivation of TB infection (latent TB) or other atypical or opportunistic infections; neutropenia, hypersensitivity reactions (e.g. anaphylactic reactions, angioedema); increased risk of lymphoma; inj site reactions (e.g. erythema, swelling, pain, bruising); transient elevations of liver enzymes, non-infectious hepatitis.
Blood and lymphatic system disorders: Thrombocytopenia.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, abdominal pain, gastroenteritis.
General disorders and administration site conditions: Fever, flu-like symptoms.
Immune system disorders: Antibody development.
Investigations: Increased blood cholesterol.
Musculoskeletal and connective tissue disorders: Arthralgia.
Nervous system disorders: Headache.
Respiratory, thoracic and mediastinal disorders: Sinusitis, nasopharyngitis, URTI.
Skin and subcutaneous tissue disorders: Rash.
Potentially Fatal: Rarely, drug reaction with eosinophilia and systemic symptoms (mainly in patients with systemic juvenile idiopathic arthritis).
Chỉ số theo dõi
Perform screening for hepatitis B infection and latent TB prior to treatment initiation. Monitor ANC (at baseline, monthly for 6 months, then quarterly thereafter); serum creatinine; hepatic enzymes (during the 1st month, particularly in patients with pre-disposing factors or symptoms of hepatic dysfunction). Assess for signs and symptoms of infection and inj site reactions. For severe CAPS: Assess clinical symptoms, inflammatory markers, and CNS inflammation, including the inner ear and eyes after the initial 3 months of treatment and every 6 months thereafter until effective treatment doses are established. Once the patient is well-controlled, CNS and ophthalmological assessments may be done annually.
Tương tác
Increased risk of serious infections and neutropenia with etanercept.
Tác dụng
Description:
Mechanism of Action: Anakinra, a biological DMARD, is a recombinant receptor antagonist of interleukin-1 (IL-1). It competitively inhibits IL-1 from binding to the IL-1 type I receptor (IL-1RI), which is expressed in many tissues and organs, thereby blocking the biological activity of IL-1α and IL-1β, including inflammation and cartilage degradation (loss of proteoglycans).
Pharmacokinetics:
Absorption: Bioavailability: 95%. Time to peak plasma concentration: 3-7 hours.
Excretion: Mainly via urine. Terminal elimination half-life: Approx 4-6 hours.
Bảo quản
Store between 2-8°C. Do not freeze. Protect from light. Do not shake.
Phân loại MIMS
Thuốc chống thấp khớp có cải thiện bệnh trạng / Thuốc ức chế miễn dịch
Phân loại ATC
L04AC03 - anakinra ; Belongs to the class of interleukin inhibitors. Used as immunosuppressants.
Tài liệu tham khảo
Anakinra. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 12/04/2024.

Anon. Anakinra. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 12/04/2024.

Buckingham R (ed). Anakinra. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/04/2024.

Joint Formulary Committee. Anakinra. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 12/04/2024.

Kineret 100 mg/0.67 mL Solution for Injection in Pre-filled Syringe (Swedish Orphan Biovitrum AB [publ]). MHRA. https://products.mhra.gov.uk. Accessed 12/04/2024.

Kineret Injection, Solution (Swedish Orphan Biovitrum AB [publ]). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 12/04/2024.

Paediatric Formulary Committee. Anakinra. BNF for Children [online]. London. BMJ Group, Pharmaceutical Press, and RCPCH Publications . https://www.medicinescomplete.com. Accessed 13/06/2024.

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