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Rheumatoid arthritis (RA) Rheumatoid arthritis (RA) Dosage and Administration Dose Adjustments and Drug Interactions Efficacy Mechanism of Action Prescribing Information Safety Special Populations and Contraindications Special Warnings and Precautions Psoriatic arthritis (PsA) Psoriatic arthritis (PsA) Dosage and Administration Dose Adjustments and Drug Interactions Efficacy Mechanism of Action Prescribing Information Safety Special Populations and Contraindications Special Warnings and Precautions Ulcerative colitis (UC) Ulcerative colitis (UC) Dosage and Administration Dose Adjustments and Drug Interactions Efficacy Mechanism of Action Prescribing Information Safety Special Populations and Contraindications Special Warnings and Precautions
Dose Adjustments and Drug InteractionsDose adjustments1 Lipid monitoning1Treatment with XELJANZ® (tofacitinib) was associated with increases in lipid parameters such as total cholesterol, low-density lipoprotein (LDL) cholesterol, and high-density lipoprotein (HDL) cholesterol. Maximum effects were generally observed within 6 weeks. Assessment of lipid parameters should be performed after 8 weeks following initiation of XELJANZ® (tofacitinib) therapy. Patients should be managed according to clinical guidelines for the management of hyperlipidaemia Increases in total and LDL cholesterol associated with XELJANZ® (tofacitinib) may be decreased to pre-treatment levels with statin therapy.Vaccinations1Prior to initiating XELJANZ® (tofacitinib), it is recommended that all patients be brought up to date with all immunisations in agreement with current immunisation guidelines. It is recommended that live vaccines not be given concurrently with XELJANZ® (tofacitinib). The decision to use live vaccines prior to XELJANZ® (tofacitinib) treatment should take into account the pre-existing immunosuppression in a given patient.

Prophylactic zoster vaccination should be considered in accordance with vaccination guidelines. Particular consideration should be given to patients with longstanding RA who have previously received two or more biological DMARDs. If live zoster vaccine is administered, it should only be administered to patients with a known history of chickenpox or those that are seropositive for varicella zoster virus (VZV). If the history of chickenpox is considered doubtful or unreliable it is recommended to test for antibodies against VZV.
Drug interactions1

XELJANZ® (tofacitinib) total daily dose should be reduced by half in patients receiving potent inhibitors of cytochrome P450 (CYP) 3A4 (e.g., ketoconazole) and in patients receiving 1 or more concomitant medicines that result in both moderate inhibition of CYP3A4 as well as potent inhibition of CYP2C19 (e.g., fluconazole) as follows:

  • XELJANZ® (tofacitinib) dose should be reduced to 5 mg once daily in patients receiving 5 mg twice daily.
  • XELJANZ® (tofacitinib) dose should be reduced to 5 mg twice daily in patients receiving 10 mg twice daily.
Potential for other medicines to influence the pharmacokinetics (PK) of tofacitinib1

Since tofacitinib is metabolised by CYP3A4, interaction with medicines that inhibit or induce CYP3A4 is likely. Tofacitinib exposure is increased when co-administered with potent inhibitors of CYP3A4 (e.g., ketoconazole) or when administration of one or more concomitant medicines results in both moderate inhibition of CYP3A4 and potent inhibition of CYP2C19 (e.g., fluconazole).

Tofacitinib exposure is decreased when co-administered with potent CYP inducers (e.g., rifampicin). Inhibitors of CYP2C19 alone or P-glycoprotein are unlikely to significantly alter the PK of XELJANZ® (tofacitinib). 

Co-administration with ketoconazole (strong CYP3A4 inhibitor), fluconazole (moderate CYP3A4 and potent CYP2C19 inhibitor), tacrolimus (mild CYP3A4 inhibitor) and ciclosporin (moderate CYP3A4 inhibitor) increased tofacitinib AUC, while rifampicin (potent CYP inducer) decreased tofacitinib AUC. Coadministration of tofacitinib with potent CYP inducers (e.g., rifampicin) may result in a loss of or reduced clinical response (see Figure 1). Co-administration of potent inducers of CYP3A4 with tofacitinib is not recommended. Co-administration with ketoconazole and fluconazole increased tofacitinib Cmax while tacrolimus, ciclosporin and rifampicin decreased tofacitinib Cmax.

Concomitant administration with MTX 15-25 mg once weekly had no effect on the PK of tofacitinib in RA patients (see Figure 1)

Potential for tofacitinib to influence the PK of other medicine1

Co-administration of tofacitinib did not have an effect on the PK of oral contraceptives, levonorgestrel and ethinyl estradiol, in healthy female volunteers.

In RA patients, co-administration of tofacitinib with MTX 15 - 25 mg once weekly decreased the AUC and Cmax of MTX by 10% and 13%, respectively. The extent of decrease in MTX exposure does not warrant modifications to the individualised dosing of MTX.

XELJANZ® (tofacitinib) dose should be reduced to 5 mg twice daily in patients receiving 10 mg twice daily. XELJANZ® (tofacitinib) dose should be reduced to 5 mg once daily in patients receiving 5 mg twice daily.1

Note: Reference group is administration of tofacitinib alone.1

ReferencesPfizer Laboratories (Pty) Ltd. XELJANZ® 5mg and 10mg film-coated tablets. Final Approved Package Insert - 27 October 2020.
PP-XEL-ZAF-0083

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