Olumiant Baricitinib Tablets

1. Indications and Usage
Rheumatoid Arthritis (RA):
Indicated for adult patients with moderate to severe active rheumatoid arthritis, usually in combination with methotrexate or other non-biologic DMARDs.
Atopic Dermatitis (AD):
Indicated for adult patients with moderate to severe atopic dermatitis that is inadequately controlled with topical prescription therapies or when those therapies are not advisable.
Alopecia Areata:
Indicated for the treatment of severe alopecia areata.
2. Dosage and Administration
Route of Administration:
For Oral Use ONLY.
Recommended Dosage:
RA: The recommended dose is 4 mg once daily.
AD: The recommended dose is 4 mg once daily. (May be reduced to 2 mg once daily based on efficacy and safety).
Alopecia Areata: The recommended dose is 4 mg once daily.
Administration Instructions:
Swallow tablets whole with water.
Can be taken with or without food.
Missed Dose: Take as soon as possible on the same day and resume the normal schedule the following day. Do not take a double dose.
Dose Adjustments:
Renal Impairment: Reduce dose to 2 mg once daily for patients with moderate renal impairment (Creatinine Clearance 30–60 mL/min). Not recommended for severe impairment (CrCl <30 mL/min).
Hepatic Impairment: Reduce dose to 2 mg once daily for patients with moderate hepatic impairment (Child-Pugh Class B). Not recommended for severe impairment (Child-Pugh Class C).
3. Mechanism of Action
JAK Inhibition:
Baricitinib is a small molecule that reversibly binds to the intracellular region of JAK1 and JAK2 (purified JAK1 IC50 = 5.
9 nM; JAK2 IC50 = 5.7 nM).
Blocking Signaling Pathways:
It inhibits the JAK-STAT signaling pathway, which is used by multiple cytokine receptors (such as IL-6, IFN-γ, and IL-23). By blocking this pathway, baricitinib reduces inflammation and immune system activity associated with autoimmune diseases.
4. Safety and Warnings
Serious Infections:
Can cause serious infections (e.g., Tuberculosis, Herpes Zoster, Candidiasis, Pneumococcal Pneumonia). Screen for tuberculosis (TB) prior to initiation.
Malignancy:
Increased risk of malignancies (e.g., lymphoma, lung cancer), particularly in patients with RA or those with a history of smoking.
Major Adverse Cardiovascular Events (MACE):
Increased risk of MACE (myocardial infarction, stroke, cardiovascular death) in patients with RA and cardiovascular risk factors.
Thrombosis:
Risk of Deep Vein Thrombosis (DVT), Pulmonary Embolism (PE), and Arterial Thrombosis. Monitor for signs of clotting.
Laboratory Abnormalities:
May cause neutropenia, anemia, and increased liver enzymes (ALT/AST). Monitor complete blood count (CBC) and liver function tests periodically.
5. Adverse Reactions
Most Common (Incidence ≥2%):
Upper respiratory tract infections, nasopharyngitis, headache, diarrhea, nausea, increased creatine phosphokinase (CPK), and acne.
6. Drug Interactions
Strong CYP3A4 Inhibitors:
Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin) may increase baricitinib exposure. Dose reduction may be necessary.
Immunosuppressants:
Combination with biologic DMARDs or potent immunosuppressants (e.g., azathioprine, cyclosporine) is generally not recommended due to increased infection risk.
7. Pharmaceutical Information
Chemical Composition:
Active Ingredient: Baricitinib.
Available Strength: 1 mg, 2 mg, and 4 mg tablets.
Appearance:
1 mg: White, round, biconvex.
2 mg: Yellow, round, biconvex.
4 mg: Pink, round, biconvex.
Storage: Store at 25°C (77°F); excursions permitted to 15°C–30°C (59°F–86°F).