Baricitinib


Concise Prescribing Info
Indications/Uses
Moderate to severe active rheumatoid arthritis.
Dosage/Direction for Use
Adult : PO Monotherapy or combined with methotrexate or other non-biologic DMARDs: 4 mg once daily, may reduce to 2 mg once daily when sustained control is achieved. In patient with history of chronic or recurrent infections: 2 mg once daily
Dosage Details
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.
Contraindications
Patient with active, serious infections including localised infections. Concomitant use with biologic DMARDs, live vaccines. Lactation.
Special Precautions
Patient with risk factors for of gastrointestinal perforations (e.g. history of diverticulitis), thrombosis. Renal and hepatic impairment. Elderly. Pregnancy.
Adverse Reactions
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).
MonitoringParameters
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.
Drug Interactions
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.
Action
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.
Chemical Structure

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Storage
Store between 20-25°C.
MIMS Class
ATC Classification
L04AA37 - baricitinib ; Belongs to the class of selective immunosuppressive agents. Used to induce immunosuppression.
Disclaimer: This information is independently developed by MIMS based on Baricitinib from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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