Description

TOFAXEN tablets: Each film-coated tablet contains Tofacitinib Citrate INN equivalent to Tofacitinib 5 mg.

Mechanism of Action 

Tofacitinib is a Janus Kinase (JAK) inhibitor. JAKs are intracell­ular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function. Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs

Indication and Usage

Tofacitinib is indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis, psoriatic arthritis, ulcerative colitis (UC) who have had an inadequate response or intolerance to methotrexate. It may be used as monotherapy or in combination with methotrexate or other nonbiologic disease-modifying antirheumatic drugs (DMARDs).

Dosage and Administration

Administration Instructions: Do not initiate TOFAXEN if absolute lymphocyte count <500 cells/mm3, an absolute neutrophil count (ANC) <1000 cells/mm3 or hemoglobin <9 g/dL.

Recommended Dosage

Rheumatoid Arthritis and Psoriatic Arthritis (in combination with nonbiologic DMARDs)

• Tofacitinib (Tofaxen) 5 mg twice daily. Tofaxen can be taken with or without food.
• Recommended dosage in patients with moderate and severe renal impairment or moderate hepatic impairment is Tofacitinib 5 mg (TOFAXEN) once daily.

Ulcerative Colitis

• The recommended dose is 10 mg Tofacitinib (Tofaxen) given orally twice daily for induction for 8 weeks and 5 mg given twice daily for maintenance.
• For patients who do not achieve adequate therapeutic benefit by week 8, the induction dose of 10 mg twice daily can be extended for an additional 8 weeks (16 weeks total), followed by 5 mg twice daily for maintenance. Tofacitinib induction therapy should be discontinued in any patient who shows no evidence of therapeutic benefit by week 16.
• Recommended dosage in patients with moderate and severe renal impairment or moderate hepatic impairment is half the total daily dose.

Overdose

There is no specific antidote for overdose with Tofacitinib. In case of an overdose, it is recommended that the patient be monitored for signs and symptoms of adverse reactions.

Side effects

Most common adverse reactions are: upper respiratory tract infection, nasopharyngitis, diarrhea, headache, elevated choles­terol levels, increased blood creatine phosphokinase, rash and herpes zoster.

Drug interactions

With medicine: Tofacitinib exposure is increased when Tofacitinib is co-administered with potent inhibitors of cytochrome P450 (CYP) 3A4 (e.g., ketoconazole) and CYP2C19 (e.g., fluconazole). Use of Tofacitinib in combination with biologic DMARDs or potent immune suppressants such as azathioprine and cyclosporine is not recommended.

With food and others: It is best to avoid taking Tofacitinib with grapefruit juice and to avoid grapefruit juice completely during

Pregnancy and Lactation

Pregnancy Category C. There are no adequate and well­ controlled studies in pregnant women. Tofacitinib should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is not known whether this medicine is excreted in human milk. Caution should be exercised when this product is administered to a nursing woman.

Storage Condition

Store Tofaxen below 25°C. Do not remove desiccant. Keep out of the reach and sight of children.

Reference: Everest Pharmaceuticals Limited