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.
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.
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.
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.
L04AA37 - baricitinib ; Belongs to the class of selective immunosuppressive agents. Used to induce immunosuppression.
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.