Baricitinib


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Rheumatoid arthritis
Adult: In patient with moderate to severe active cases: As monotherapy or in combination with methotrexate or other non-biologic disease modifying antirheumatic drugs (DMARDs): 4 mg once daily, may reduce dose to 2 mg once daily when sustained control is achieved. Do not initiate in patients with absolute lymphocyte count (ALC) <500 cells/mm3, absolute neutrophil count (ANC) <1,000 cells/mm3, or haemoglobin <8 g/dL. In patient with history of chronic or recurrent infections: 2 mg once daily.
Elderly: ≥75 years 2 mg once daily.
Special Patient Group
Patient taking potent organic anion transporter-3 inhibitor (e.g. probenecid): 2 mg once daily.
Renal Impairment
 CrCl (mL/min)  Dosage
 <30  Not recommended.
30-60
 2 mg once daily.
Hepatic Impairment
Severe: Not recommended.
Chống chỉ định
Patient with active, serious infections including localised infections. Concomitant use with biologic DMARDs, live vaccines. Lactation.
Thận trọng
Patient with risk factors for of gastrointestinal perforations (e.g. history of diverticulitis), thrombosis. Renal and hepatic impairment. Elderly. Pregnancy.
Phản ứng phụ
Significant: Haematologic toxicity (e.g. neutropenia, lymphopenia, anaemia), increased ALT/AST, increased LDL, HDL cholesterol, malignancies (e.g. lymphoma), herpes virus reactivation.
Gastrointestinal disorders: Nausea.
Respiratory, thoracic and mediastinal disorders: Upper respiratory tract infection.
Potentially Fatal: Serious infections (e.g. active tuberculosis, candidiasis, pneumocystosis); thrombosis (e.g. deep venous thrombosis, arterial thrombosis, pulmonary embolism).
Monitoring Parameters
Monitor CBC with differential and platelets, LFT at baseline and periodically thereafter, lipid parameters after 12 weeks of therapy and periodically thereafter. Monitor for signs and symptoms of infection (e.g. tuberculosis) during and after therapy; abdominal symptoms. Perform skin examinations periodically in patient at risk of skin cancer; viral hepatitis screening before initiation of therapy.
Tương tác
Increased risk of additive immunosuppression with potent immunosuppressive agents (e.g. azathioprine, ciclosporin, tacrolimus). Increased exposure with strong organic anion transporter-3 inhibitors (e.g. probenecid).
Potentially Fatal: May diminish therapeutic effect of live vaccines. May enhance the adverse effect of biologic DMARDs.
Tác dụng
Description: Baricitinib selectively and reversibly inhibits Janus kinase (particularly JAK1 and JAK2), an enzyme involved in the initiation of signal transduction pathway in stimulating haematopoiesis and immune function. JAKs phosphorylate and activate signal transducers and activators of transcription (STATs), which activate gene expression within the cell. Inhibition of JAKs leads to reduced phosphorylation and activation of STATs and decreased in serum IgG, IgM, IgA, and C-reactive protein.
Pharmacokinetics:
Absorption: Time to peak plasma concentration: Approx 1 hour. Bioavailability: Approx 80%.
Distribution: Volume of distribution: 76 L. Plasma protein binding: Approx 50%.
Metabolism: Metabolised in the liver by CYP3A4 enzyme.
Excretion: Via urine (approx 75%; 69% as unchanged drug); faeces (approx 20%; 15% as unchanged drug). Elimination half-life: Approx 12 hours.
Đặc tính

Chemical Structure Image
Baricitinib

Source: National Center for Biotechnology Information. PubChem Database. Baricitinib, CID=44205240, https://pubchem.ncbi.nlm.nih.gov/compound/Baricitinib (accessed on Jan. 21, 2020)

Bảo quản
Store between 20-25°C.
Phân loại MIMS
Phân loại ATC
L04AA37 - baricitinib ; Belongs to the class of selective immunosuppressive agents. Used to induce immunosuppression.
References
Anon. Baricitinib. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 14/03/2019.

Buckingham R (ed). Baricitinib. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/03/2019.

Joint Formulary Committee. Baricitinib. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 14/03/2019.

Olumiant Tablet, Film Coated (Eli Lilly and Company). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 14/03/2019.

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