Dosing in PsA
Dosing
XELJANZ 5 mg film-coated tablets twice daily and 11 mg prolonged release once daily are the only approved dosages for the treatment of Psoriatic Arthritis (PsA).1,2

Steady-state AUC and Cmax of XELJANZ for 11 mg prolonged-release tablet administered once daily are equivalent to those of 5 mg film-coated tablets administered twice daily.1-3

An alternative way to treat patients with PsA:1,2
Always refer to full SmPC before prescribing XELJANZ.
Tablets shown in the above image are not true to size.
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  • XELJANZ 5 mg film-coated or 11mg prolonged release tablets can be given with or without food.
  • For patients who have difficulties swallowing, XELJANZ 5 mg tablets may be crushed and taken with water. Whereas, XELJANZ 11 mg tablet must be taken whole in order to ensure the entire dose is delivered correctly. They must not be crushed, split or chewed.
  • No dose adjustment is required when used in combination with MTX.
  • XELJANZ treatment should be interrupted if a patient develops a serious infection until the infection is controlled.
  • Rapid absorption in healthy human subjects with plasma concentrations peaking approximately 1 hour after administration of 5 mg tablets. Following oral administration of tofacitinib 11 mg tablet, peak plasma concentrations are reached at 4 hours.
  • Terminal half-life of approximately 3 hours for XELJANZ 5 mg tablets and approximately 6 hours for XELJANZ 11 mg tablet.
  • XELJANZ 5 mg tablets is available in a 28-day treatment pack. 
  • XELJANZ 11 mg tablets is available in HDPE (High Density Polyethylene) bottles with 2 silica gel desiccants and child-resistant, polypropylene closure containing 30 or 90 prolonged-release tablets. Or availble as aluminium foil/PVC backed aluminium foil blisters containing 7 prolonged-release tablets. Each pack contains 28 or 91 prolonged-release tablets.
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​​​​​​​Packs and tablets shown not true to size.
Contraindications and special populations1,2
Contraindications for use:
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  • Hypersensitivity to the active substance of XELJANZ or to any of its excipients*
  • Active tuberculosis (TB), serious infections such as sepsis, or opportunistic infections
  • Severe hepatic impairment
  • Pregnancy and lactation
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  • *XELJANZ 5 mg contains lactose. Patients with rare hereditary problems of galactose intolerance, total lactase deficiency or glucose-galactose malabsorption should not take this medicinal product. 
  • XELJANZ 11mg contains sorbitol. The additive effect of concomitantly administered products containing sorbitol (or fructose) and dietary intake of sorbitol (or fructose) should be taken into account. The content of sorbitol in medicinal products for oral use may affect the bioavailability of other medicinal products for oral use administered concomitantly.
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Special populations:
XELJANZ should only be used in patients over 65 years of age, in patients who are current or past smokers, patients with other cardiovascular risk factors, and patients with other malignancy risk factors if no suitable treatment alternatives are available.

Renal Impairment
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  • XELJANZ dose should be reduced to 5 mg once-daily in patients with severe renal impairment (creatinine clearance <30 mL/min).
  • For severe renal impairment (including patients undergoing haemodialysis) (creatinine clearance < 30 mL/min), XELJANZ dose should be reduced to 5 mg film-coated tablet once daily when the indicated dose in the presence of normal renal function is 11 mg prolonged-release tablet once daily
  • Patients with severe renal impairment should remain on a reduced dose of 5 mg once-daily even after haemodialysis.

Hepatic impairment

  • XELJANZ dose should be reduced to 5 mg once daily in patients with moderate hepatic impairment (Child Pugh B).
  • XELJANZ should not be used in patients with severe hepatic impairment (Child Pugh C).
  • For moderate hepatic impairment, XELJANZ dose should be reduced to 5 mg film-coated tablets once daily when the indicated dose in the presence of normal hepatic function is 11 mg prolonged-release tablet once daily

Elderly
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  • No dose adjustment is required in patients aged ≥65 years based on age alone (see other special populations). There are limited data in patients aged 75 years and older.
  • Considering the increased risk of serious infections in patients over 65 years of age, XELJANZ should only be used in these patients if no suitable treatment alternatives are available.
Drug-drug interactions
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  • XELJANZ dose should be reduced to 5 mg once daily in patients receiving potent inhibitors of CYP3A4 (e.g., ketoconazole).†
  • XELJANZ dose should also be reduced to 5 mg once daily in patients receiving one or more concomitant medicines that result in both moderate inhibition of CYP3A4 and potent inhibition of CYP2C19 (e.g., fluconazole).†
  • Co-administration of XELJANZ with potent CYP inducers (e.g., rifampicin) may result in a loss of, or reduced, clinical response.
  • Co-administration of potent inducers of CYP3A4 with XELJANZ is not recommended.
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Support & Resources
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†XELJANZ dose should be reduced to 5 mg once daily in patients receiving 11 mg once daily.

Note, the licensed dose of XELJANZ for the treatment of PsA in the UK is 5mg administered twice daily or one 11 mg prolonged-release tablet administered once daily, which should not be exceeded.

AUC - area under curve; Cmax - maximum concentration; MTX - methotrexate; TB - tuberculosis; RA - rheumatoid arthritis; PsA - psoriatic arthritis; OD - once daily
References
  1.  
  2. ​​​​​​​​​​​​​​XELJANZ (tofacitinib citrate) 5 mg film-coated tablets - Summary of Product Characteristics.
  3. XELJANZ (tofacitinib citrate) 11 mg prolonged release tablet - Summary of Product Chracteristics.
  4. Lamba M, et al. J Clin Pharmacol. 2016;56(11):1362-1371.
  5.  
PP-XEL-GBR-3220. October 2021
XELJANZ Risk Minimisation Programme (RMP) materials, including a Patient Alert Card, Prescriber Checklists and a Prescriber Brochure are available from https://www.medicines.org.uk/emc/. Patients treated with XELJANZ should be given the Patient Alert Card.

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