XELJANZ / XELJANZ XR (tofacitinib) Dosage And Administration

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Dosing Considerations

There is a risk of added immunosuppression when XELJANZ/ XELJANZ XR is coadministered with potent immunosuppressive drugs (e.g. azathioprine, tacrolimus, cyclosporine). Combined use of XELJANZ/ XELJANZ XR with potent immunosuppressants or biologic DMARDS (tumor necrosis factor (TNF) antagonists, interleukin 1 receptor (IL-1R) antagonists, IL-6R antagonists, anti-CD20 monoclonal antibodies, IL-17 antagonists, IL-12/IL-23 antagonists and selective co-stimulation modulators) has not been studied in RA, PsA and UC patients and its use should be avoided.

Recommended Dose and Dosage Adjustment

Rheumatoid Arthritis XELJANZ/ XELJANZ XR Posology

Adults :

XELJANZ / XELJANZ XR is to be used in combination with methotrexate.

XELJANZ / XELJANZ XR, monotherapy may be considered in cases of intolerance to methotrexate.

The recommended dose of XELJANZ is 5 mg administered twice daily. The recommended dose of XELJANZ XR is 11 mg once daily

XELJANZ / XELJANZ XR is given orally with or without food.

Swallow XELJANZ XR tablets whole and intact. Do not crush, split, or chew.

Switching between XELJANZ Tablets and XELJANZ XR Tablets
Where appropriate, patients treated with XELJANZ 5 mg twice daily may be switched to XELJANZ XR 11 mg once daily the day following the last dose of XELJANZ 5 mg.

Where appropriate, patients treated with XELJANZ XR 11 mg once daily may be switched to XELJANZ 5 mg twice daily 24 hours following the last dose of XELJANZ XR 11 mg.

Patients treated with XELJANZ XR 11 mg once daily who require a dose reduction due to renal or hepatic impairment or drug interactions may be switched to XELJANZ 5 mg once daily, 24 hours following the last dose of XELJANZ XR 11 mg once daily (see WARNINGS AND PRECAUTIONS and DRUG INTERACTIONS).

Psoriatic Arthritis XELJANZ Posology

Adults :
The recommended dose of XELJANZ is 5 mg administered twice daily in combination with MTX or another csDMARD.

Ulcerative Colitis XELJANZ Posology

Adults :
The recommended dose is 10 mg given orally twice daily for induction for at least 8 weeks and 5 mg given twice daily for maintenance.

Depending on therapeutic response; 10 mg twice daily may also be used for maintenance in some patients. However, the lowest effective dose possible should be used for maintenance therapy to minimize adverse effects (see WARNINGS AND PRECAUTIONS).

XELJANZ induction therapy should be discontinued in patients who show no evidence of adequate therapeutic benefit by Week 16.

In patients who have responded to treatment with XELJANZ, corticosteroids may be cautiously reduced and/or discontinued in accordance with standard of care.

Dose Modification due to Serious Infections and Cytopenias (see Tables 5-7 below)

  • It is recommended that XELJANZ/XELJANZ XR not be initiated in patients with an absolute neutrophil count (ANC) less than 1000/mm3, hemoglobin (Hgb) levels < 9 g/d, or with a lymphocyte count less than 500 cells/mm3 (see WARNINGS AND PRECAUTIONS).
  • Dose interruption is recommended for management of lymphopenia, neutropenia and anemia (see WARNINGS AND PRECAUTIONS and ADVERSE REACTIONS).
  • Avoid use of XELJANZ/XELJANZ XR if a patient develops a serious infection until the infections is controlled
Table 5: Dose Adjustments for Neutropenia

Low ANC

Lab Value

(cells/mm3)

Recommendation

ANC >1000

Maintain dose

ANC 500-1000

For persistent decreases in this range, interrupt or reduce administration with XELJANZ/XELJANZ XR until ANC is >1000 cells/mm3

  • For patients receiving XELJANZ 5 mg twice daily, interrupt XELJANZ dosing. When ANC is > 1000, resume XELJANZ 5 mg twice daily.

RA patients:

  • When ANC is > 1000 cells/mm3, resume XELJANZ XR 11 mg once daily.

UC patients:

  • For patients receiving XELJANZ 10 mg twice daily, reduce dose to XELJANZ 5 mg twice daily. When ANC is > 1000, increase to XELJANZ 10 mg twice daily based on clinical response.

ANC <500

(Confirmed by repeat testing)

Discontinue treatment with XELJANZ/XELJANZ XR

Table 6: Dose Adjustments for Anemia

Low Hemoglobin Value

Lab Value

(g/dL)

Recommendation

< 2 g/dL decrease and ≥ 9.0 g/dL

Maintain dose

≥ 2 g/dL decrease or < 8.0 g/dL

(Confirmed by repeat testing)

Interrupt the administration of XELJANZ/XELJANZ XR until hemoglobin values have normalized

Table 7: Dose Adjustments for Lymphopenia Low Lymphocyte Count

Low Lymphocyte Count

Lab Value

(cells/mm3)

Recommendation

Lymphocyte count greater than or equal to 500

Maintain dose

Lymphocyte count less than 500

(Confirmed by repeat testing)

Discontinue XELJANZ/XELJANZ XR

Dose Modification in Patients with Renal or Hepatic Impairment

XELJANZ

  • XELJANZ is contraindicated in patients with severe hepatic impairment
    In patients with moderate (CLcr ≥30 and <60 mL/min) or severe (CLcr ≥15 and <30 mL/min) renal insufficiency - (including patients with ESRD but not limited to those undergoing
    • The recommended dose is XELJANZ 5 mg once daily when the indicated dose in the presence of normal renal function is XELJANZ 5 mg twice daily.
    • The recommended dose is XELJANZ 5 mg twice daily when the indicated dose in the presence of normal renal function is XELJANZ 10 mg twice daily.
    • Use XELJANZ with caution in this patient population
    • For patients undergoing hemodialysis, dose should be administered after the dialysis session on dialysis days. If a dose was taken before the dialysis procedure, supplemental doses are not recommended in patients after dialysis.
    • Patients with severe renal insufficiency should remain on a reduced dose even after hemodialysis.
  • In patients with moderate hepatic impairment:
    • The recommended dose is XELJANZ 5 mg once daily when the indicated dose in the presence of normal hepatic function is XELJANZ 5 mg twice daily.
    • The recommended dose is XELJANZ 5 mg twice daily when the indicated dose in the presence of normal hepatic function is XELJANZ 10 mg twice daily.
    • Use XELJANZ with caution in this patient population.

XELJANZ XR

  • XELJANZ XR is contraindicated in patients with severe hepatic impairment and should not be used in patients with moderate hepatic impairment.
  • XELJANZ XR is not recommended in patients with moderate (CLcr ≥30 and <60 mL/min), or severe (CLcr ≥15 and <30 mL/min), renal insufficiency (including patients with ESRD but not limited to those undergoing hemodialysis).

In patients with moderate hepatic impairment or moderate to severe renal insufficiency, XELJANZ 5 mg once daily may be considered.

Dose Modification Due to Drug Interactions

Coadministration of potent inducers of CYP3A4 (e.g. rifampin) with XELJANZ/XELJANZ XR may result in loss of efficacy or reduced clinical response to XELJANZ/XELJANZ XR. Coadministration of potent inducers of CYP3A4 with XELJANZ/XELJANZ XR is not recommended.

XELJANZ

  • In patients receiving potent inhibitors of Cytochrome P450 3A4 (CYP3A4) (e.g ketoconazole) or one or more concomitant medications that result in both moderate inhibition of CYP3A4 and potent inhibition of CYP2C19 (e.g. fluconazole),
    • Reduce XELJANZ dose to 5 mg twice daily in patients taking 10 mg twice daily
    • Reduce XELJANZ dose to 5 mg once daily in patients taking 5 mg twice daily

XELJANZ XR
  • XELJANZ XR is not recommended in patients
    • Receiving potent inhibitors of Cytochrome P450 3A4 (CYP3A4) (e.g ketoconazole).
    • Receiving one or more concomitant medications that result in both moderate inhibition of CYP3A4 and potent inhibition of CYP2C19 (e.g. fluconazole).

In patients with dose modifications due to drug interactions, XELJANZ 5 mg once daily may be considered.

Special Populations

Geriatrics (>65 years)

No dosage adjustment is required in patients aged 65 years and older (see WARNINGS AND PRECAUTIONS and ACTION AND CLINICAL PHARMACOLOGY).

Pediatrics (<18 years of age)

The safety and efficacy of XELJANZ/XELJANZ XR in children aged from neonates to less than 18 years of age has not yet been established. Therefore XELJANZ/XELJANZ XR should not be used in this patient population (see WARNINGS AND PRECAUTIONS and ACTION AND CLINICAL PHARMACOLOGY).

Missed Dose

For a missed dose, resume at the next scheduled dose.