1. Clinical & Scientific Overview
Tofacitinib & Baricitinib (Oral JAK Inhibitors) (TIP-MED-000127, Reference Code [7.25]) is classified under
Pain, Inflammation, Rheumatology & Gout Medicines (Ch 07) as a Targeted Synthetic Janus Kinase (JAK1/JAK3 & JAK1/JAK2) Inhibitors (Schedule H | HIGH-ALERT).
Within the Indian regulatory and compendial framework, it is governed under Schedule H Prescription Drug (To be sold by retail on the prescription of a Registered Medical Practitioner only — Drugs Rules 1945).
Representative Indian Market Examples (Edition 2.7 Ch 07 [7.25], p. 91): Tofacitinib: Tofajak (Cipla), Xeljanz (Pfizer), Tofatas (Intas). Baricitinib: Olumiant (Eli Lilly), Barinat (Natco) — Strengths & Dosage Forms: Tofacitinib Tablets: 5 mg IR, 11 mg XR. Baricitinib Tablets: 2 mg, 4 mg
Tofacitinib Tablets: 5 mg IR, 11 mg XR. Baricitinib Tablets: 2 mg, 4 mg
3. Mechanism of Action & Pharmacodynamics
Targeted Synthetic Janus Kinase (JAK1/JAK3 & JAK1/JAK2) Inhibitors (Schedule H | HIGH-ALERT) acting on target receptor/enzyme pathways in Pain, Inflammation, Rheumatology & Gout Medicines (Ch 07): clinical efficacy is mediated via Targeted Synthetic Janus Kinase (JAK1/JAK3 & JAK1/JAK2) Inhibitors (Schedule H | HIGH-ALERT) for Moderate-to-severe active Rheumatoid Arthritis, Psoriatic Arthritis, Ankylosing Spondylitis, and Ulcerative Colitis after inadequate response or intolerance to conventional DMARDs (Methotrexate).
4. Therapeutic Indications & Evidence-Supported Uses
- Moderate-to-severe active Rheumatoid Arthritis, Psoriatic Arthritis, Ankylosing Spondylitis, and Ulcerative Colitis after inadequate response or intolerance to conventional DMARDs (Methotrexate)
🇮🇳 Jurisdiction & Indication Note: Indications and schedules reflect Indian compendial and regulatory records (CDSCO / Indian Pharmacopoeia & NFI / NLEM 2022). Where international reference labels (US FDA DailyMed / NCBI StatPearls) are cited for pharmacokinetic or mechanistic parameters, international approvals do not automatically imply CDSCO approval in India.
5. Educational Dosage Context, Formulations & Administration
Educational Dosing & Regimen Summary: Tofacitinib (RA/PsA/AS): 5 mg IR PO BD (or 11 mg XR OD). Baricitinib (RA): 2–4 mg PO OD
Administration & Meal Timing: May be taken with or without food (swallow 11 mg XR whole) | Morning & Evening (Tofacitinib 5 mg BD) or Morning (11 mg XR / Baricitinib OD)
6. Pharmacokinetics, Metabolism & Renal/Hepatic Adjustment
Absorption, distribution, metabolism, and excretion follow class pharmacokinetic profile; verify patient renal/hepatic function.
Renal: Tofacitinib: Halve dose to 5 mg OD in moderate-to-severe CKD (CrCl <50 mL/min). Baricitinib: 2 mg OD if eGFR 30–60 mL/min; AVOID if eGFR <30 mL/min! Hepatic: Tofacitinib 5 mg OD in Child–Pugh B; contraindicated in Child–Pugh C
Renal: Tofacitinib: Halve dose to 5 mg OD in moderate-to-severe CKD (CrCl <50 mL/min). Baricitinib: 2 mg OD if eGFR 30–60 mL/min; AVOID if eGFR <30 mL/min! Hepatic: Tofacitinib 5 mg OD in Child–Pugh B; contraindicated in Child–Pugh C
Renal: Tofacitinib: Halve dose to 5 mg OD in moderate-to-severe CKD (CrCl <50 mL/min). Baricitinib: 2 mg OD if eGFR 30–60 mL/min; AVOID if eGFR <30 mL/min! Hepatic: Tofacitinib 5 mg OD in Child–Pugh B; contraindicated in Child–Pugh C
7. Contraindications, Precautions & High-Risk Warnings
- BOXED WARNINGS (ORAL SURVEILLANCE TRIAL): Increased risk of (1) Serious Infections — especially Tuberculosis (mandatory Mantoux/IGRA + Chest X-ray before starting in India!) and Herpes Zoster; (2) Major Adverse Cardiovascular Events (MACE: MI/stroke) in patients >=50 yr with CV risk factors; (3) Venous Thromboembolism (DVT/PE); and (4) Malignancies! Contraindicated if ALC <500/mm3, ANC <1000/mm3, Hb <9 g/dL, pregnancy, lactation, or Child–Pugh C cirrhosis
Key Clinical Precautions: Renal: Tofacitinib: Halve dose to 5 mg OD in moderate-to-severe CKD (CrCl <50 mL/min). Baricitinib: 2 mg OD if eGFR 30–60 mL/min; AVOID if eGFR <30 mL/min! Hepatic: Tofacitinib 5 mg OD in Child–Pugh B; contraindicated in Child–Pugh C
8. Adverse Effects Profile
- Upper respiratory tract infection, nasopharyngitis, herpes zoster (shingles), headache, diarrhoea, dose-dependent LDL/HDL cholesterol elevation
- Disseminated tuberculosis, invasive fungal/opportunistic infections, DVT/pulmonary embolism, GI perforation, neutropenia/lymphopenia/anaemia
- Monitor for severe hypersensitivity, organ toxicity, or dose-limiting adverse events.
9. Major Drug–Drug, Drug–Food & Drug–Herb Interactions
- Tofacitinib: Strong CYP3A4 inhibitors (Clarithromycin, Itraconazole, Ketoconazole) or Fluconazole double exposure -> reduce Tofacitinib from 5 mg BD to 5 mg OD! Rifampicin causes loss of Tofacitinib efficacy! Baricitinib: Probenecid doubles Baricitinib exposure -> halve to 2 mg OD! Never combine with biologic DMARDs, Azathioprine, or Cyclosporine; avoid live vaccines!
10. Clinical Monitoring, Patient Counselling & Storage
Clinical & Laboratory Monitoring: Monitor clinical response, baseline renal/hepatic parameters, and relevant serum biomarkers.
Pharmacist Patient Counselling Points:
- Patient Counselling Checklist: Confirm TB chest test was done before starting; report fever, night sweats, persistent cough, painful blistering skin rash (shingles), chest pain, or unilateral leg swelling immediately; blood count and cholesterol check needed at 1–2 months
- Meal & Clock Timing Instruction: May be taken with or without food (swallow 11 mg XR whole) (Morning & Evening (Tofacitinib 5 mg BD) or Morning (11 mg XR / Baricitinib OD))
- Missed Dose Protocol: Take same day if remembered; never double dose
- Geriatric Dispensing Pearl: Use with extreme caution in patients >=65 years, current/past smokers, or those with ASCVD/VTE history (halve Baricitinib to 2 mg OD in >=75 yr)
Storage, Stability & Dispensing Safeguards: Store below 25°C–30°C in original moisture- and light-resistant packaging out of reach of children. Available forms: Tofacitinib Tablets: 5 mg IR, 11 mg XR. Baricitinib Tablets: 2 mg, 4 mg
11. Visual Pharmacology & Mechanism Diagram (svg-v339-01-adme-12-step-journey)
12. Authoritative References, Regulatory Sources & Editorial Disclaimer
Primary Compendial & Guideline Reference: Indian Pharmacist Desk Reference — Professional Edition 2.7 (2026–27) • Ch 07 [7.25] (p. 91)
Official Verification Portals: Indian Pharmacopoeia Commission (IPC) & National Formulary of India (NFI) • Central Drugs Standard Control Organization (CDSCO) • Ministry of Health & Family Welfare — NLEM 2022 • NCBI Bookshelf / StatPearls Pharmacology Reference • DailyMed (US FDA Official Prescribing Reference)
Last Medically & Pharmaceutically Reviewed: 2026-11-10 • Verification Status: HANDBOOK_SOURCE_CONTENT
Educational & Clinical Disclaimer: This reference profile is published solely for pharmacy education, academic study, and professional clinical reference. It does not substitute for patient-specific clinical judgement, qualified specialist oncology/medical supervision, or official CDSCO/IP prescribing information. Never self-medicate with prescription, Schedule H/H1/X, NDPS, or oncology medicines.
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