• Moderately to severely active rheumatoid arthritis in patients who have had an inadequate response/intolerance to ≥1 tumor necrosis factor (TNF) blocker (as monotherapy or in combination with nonbiologic disease-modifying antirheumatic drugs [DMARDs]) (not to be used with biologic DMARDs or potent immunosuppressants including azathioprine and cyclosporine) (immediate-release and extended-release tablets only).
• Active psoriatic arthritis in patients who have had an inadequate response/intolerance to ≥1 TNF blocker (in combination with other nonbiologic DMARDs) (not to be used with biologic DMARDs or potent immunosuppressants including azathioprine and cyclosporine) (immediate-release and extended-release tablets only).
• Active ankylosing spondylitis in patients who have had an inadequate response/intolerance to ≥1 TNF blocker (not to be used with biologic DMARDs or potent immunosuppressants including azathioprine and cyclosporine) (immediate-release and extended-release tablets only).
• Moderately to severely active ulcerative colitis in patients who have had an inadequate response/intolerance to ≥1 TNF blocker (not to be used with biologic therapies or potent immunosuppressants including azathioprine and cyclosporine) (immediate-release and extended-release tablets only).
• Active polyarticular course juvenile idiopathic arthritis in patients who have had an inadequate response/intolerance to ≥1 TNF blocker (not to be used with biologic DMARDs or potent immunosuppressants including azathioprine and cyclosporine) (immediate-release tablets and oral solution only).

Contraindicated in:

• Active infection
• Administration of live vaccines
• Severe hepatic impairment
• Increased risk for thrombosis
• History of MI or stroke
• Lymphocyte count <500 cells/mm³, absolute neutrophil count (ANC) <1000 cells/mm³, or Hgb <9 g/dL
• Lactation: Lactation.

Use Cautiously in:

• Patients with rheumatoid arthritis who are >50 yr old and have ≥1 cardiovascular risk factor (↑ risk of all-cause mortality, cardiovascular death, MI, stroke, and thrombosis)
• Current or past history of smoking (↑ risk of malignancy, cardiovascular death, MI, or stroke)
• Known malignancy
• Risk of GI perforation
• Chronic lung disease (↑ risk of infection)
• Japanese patients (↑ risk of herpes zoster)
• OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk
• Pedi: Safety and effectiveness not established in children <18 yr (rheumatoid arthritis, psoriatic arthritis, and ulcerative colitis) or <2 yr (active polyarticular course juvenile idiopathic arthritis)
• Geri: Infection risk may be ↑ in older adults.

CV: ARTERIAL THROMBOSIS, CARDIOVASCULAR DEATH, DEEP VEIN THROMBOSIS, MI, peripheral edema.

Derm: erythema, pruritus, rash.

F and E: dehydration.

GI: ↑ liver enzymes, abdominal pain, diarrhea, dyspepsia, gastritis, GI PERFORATION, vomiting.

GU: ↑ serum creatinine.

Hemat: anemia, neutropenia.

Metab: hyperlipidemia.

MS: arthralgia, joint swelling, musculoskeletal pain, tendonitis.

Neuro: fatigue, headache, insomnia, paresthesia, STROKE.

Resp: PULMONARY EMBOLISM.

Misc: DEATH, fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA AND URTICARIA), INFECTION (INCLUDING TUBERCULOSIS [TB], BACTERIAL, INVASIVE FUNGAL INFECTIONS, VIRAL, AND OTHER INFECTIONS DUE TO OPPORTUNISTIC PATHOGENS), MALIGNANCY.

Drug-Drug:

• May ↑ risk of adverse reactions and ↓ antibody response to live vaccines; avoid concurrent use.
• Strong CYP3A4 inhibitors, including ketoconazole, or moderate CYP3A4 inhibitors/strong CYP2C19 inhibitors, including fluconazole, may ↑ levels and the risk of toxicity; dose ↓ recommended.
• Strong CYP3A4 inducers, including rifampin, may ↓ levels and effectiveness; avoid concurrent use.
• ↑ risk of immunosuppression when used concurrently with other potent immunosuppressants, including azathioprine, cyclosporine, tacrolimus, antineoplastics, or radiation therapy.

(Generic available)

• Immediate-release tablets: 5 mg; 10 mg;
• Extended-release tablets: 11 mg; 22 mg;
• Oral solution (grape flavor): 1 mg/mL;

Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis

• PO (Adults): Immediate-release tablets: 5 mg twice daily; Extended-release tablets: 11 mg once daily; Concurrent use of strong CYP3A4 inhibitors or concurrent use of moderate CYP3A4 inhibitor with a strong CYP2C19 inhibitor: 5 mg once daily (immediate-release tablets); if taking 11 mg once daily (extended-release tablets), then switch to 5 mg once daily (immediate-release tablets).

Ulcerative Colitis

• PO (Adults): Immediate-release tablets: Induction: 10 mg twice daily for ≥8 wk; based on therapeutic response, may transition to maintenance dose or continue 10 mg twice daily for an additional 8 wk. Discontinue therapy if inadequate response achieved after 16 wk using 10 mg twice daily. Maintenance: 5 mg twice daily; if patient experiences loss of response on 5 mg twice daily, then use 10 mg twice daily after assessing the benefits and risks and use for the shortest duration; use lowest effective dose to maintain response; Extended-release tablets: Induction: 22 mg once daily for ≥8 wk; based on therapeutic response, may transition to maintenance dose or continue 22 mg once daily for an additional 8 wk. Discontinue therapy if inadequate response achieved after 16 wk using 22 mg once daily. Maintenance: 11 mg once daily; if patient experiences loss of response on 11 mg once daily, then use 22 mg once daily after assessing the benefits and risks and use for the shortest duration; use lowest effective dose to maintain response; Concurrent use of strong CYP3A4 inhibitors or concurrent use of moderate CYP3A4 inhibitor with a strong CYP2C19 inhibitor: if taking 10 mg twice daily (immediate-release tablets), ↓ to 5 mg twice daily (immediate-release tablets); if taking 5 mg twice daily (immediate-release tablets), ↓ to 5 mg once daily (immediate-release tablets). If taking 22 mg once daily (extended-release tablets), then ↓ to 11 mg once daily (extended-release tablets); if taking 11 mg once daily (extended-release tablets), then switch to 5 mg once daily (immediate-release tablets).

Active Polyarticular Course Juvenile Idiopathic Arthritis

• PO (Children ≥ 2 yr and ≥40 kg): Immediate-release tablets or oral solution: 5 mg twice daily. Concurrent use of strong CYP3A4 inhibitors or concurrent use of moderate CYP3A4 inhibitor with a strong CYP2C19 inhibitor: 5 mg once daily (immediate-release tablets or oral solution).
• PO (Children ≥ 2 yr and 20–<40 kg): Oral solution: 4 mg twice daily. Concurrent use of strong CYP3A4 inhibitors or concurrent use of moderate CYP3A4 inhibitor with a strong CYP2C19 inhibitor: 4 mg once daily (oral solution).
• PO (Children ≥ 2 yr and 10–<20 kg): Oral solution: 3.2 mg twice daily. Concurrent use of strong CYP3A4 inhibitors or concurrent use of moderate CYP3A4 inhibitor with a strong CYP2C19 inhibitor: 3.2 mg once daily (oral solution).

Xeljanz, Xeljanz XR

• Acts as a Janus kinase inhibitor. Some results of inhibition include decreased hematopoiesis and immune cell function. Decreases circulating killer cells, increases B cell count, and decreases serum C-reactive protein.

• Improvement in clinical and symptomatic parameters of rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, ulcerative colitis, and polyarticular course juvenile idiopathic arthritis.

Therapeutic Classification: antirheumatics

Pharmacologic Classification: kinase inhibitors

Absorption: 74% absorbed following oral administration.

Distribution: Well distributed to tissues.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme, with some contribution from the CYP2C19 isoenzyme. 30% renal excretion of the parent drug.

Half-life: 3 hr.

(clinical improvement)

• Instruct patient to take tofacitinib as directed. Advise patient to read Medication Guide before starting and with each Rx refill in case of changes.
• Caution patient to notify health care professional immediately if signs of infection (fever, sweating, chills, muscle aches, cough, shortness of breath, blood in phlegm, weight loss, warm, red, or painful skin or sores, diarrhea or stomach pain, burning on urination or urinating more often than normal, feeling very tired) or stomach or intestinal perforation (fever, stomach-area pain that does not go away, change in bowel habits) occur.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• Instruct patient to notify health care professional of medication regimen prior to treatment or surgery.
• Inform patient of increased risk of lymphoma and other cancers. Advise patient to have periodic skin exams for new lesions of skin cancer.
• Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy and for at least 18 hr after the last dose of oral solution or 36 hr after the last dose of extended release tablets. Inform patient of pregnancy exposure registry that monitors pregnancy outcomes in women exposed to tofacitinib during pregnancy. Encourage patients who become pregnant during therapy to enroll in the pregnancy registry by calling 1-877-311-8972. May impair female fertility.
• Emphasize the importance of follow-up lab tests to monitor for adverse reactions.

toe-fa-SYE-ti-nib

NDC Code^*

• 0069- Pfizer Laboratories Div Pfizer Inc
  • 0069-0501- XELJANZ XR
    • 0069-0501-14- 14 TABLET, FILM COATED, EXTENDED RELEASE in 1 BOTTLE (0069-0501-14)

• 0069- Pfizer Laboratories Div Pfizer Inc
  • 0069-0501- XELJANZ XR
    • 0069-0501-30- 30 TABLET, FILM COATED, EXTENDED RELEASE in 1 BOTTLE (0069-0501-30)

• 0069- Pfizer Laboratories Div Pfizer Inc
  • 0069-1001- XELJANZ
    • 0069-1001-01- 60 TABLET, FILM COATED in 1 BOTTLE (0069-1001-01)

• 0069- Pfizer Laboratories Div Pfizer Inc
  • 0069-1001- XELJANZ
    • 0069-1001-03- 28 TABLET, FILM COATED in 1 BOTTLE (0069-1001-03)

• 0069- Pfizer Laboratories Div Pfizer Inc
  • 0069-1002- XELJANZ
    • 0069-1002-01- 60 TABLET, FILM COATED in 1 BOTTLE (0069-1002-01)

• 0069- Pfizer Laboratories Div Pfizer Inc
  • 0069-1002- XELJANZ
    • 0069-1002-02- 180 TABLET, FILM COATED in 1 BOTTLE (0069-1002-02)

• 0069- Pfizer Laboratories Div Pfizer Inc
  • 0069-1002- XELJANZ
    • 0069-1002-03- 28 TABLET, FILM COATED in 1 BOTTLE (0069-1002-03)

• 63539- U.S. Pharmaceuticals
  • 63539-012- XELJANZ
    • 63539-012-02- 60 TABLET, FILM COATED in 1 BOTTLE (63539-012-02)

• 63539- U.S. Pharmaceuticals
  • 63539-016- XELJANZ
    • 63539-016-02- 60 TABLET, FILM COATED in 1 BOTTLE (63539-016-02)

• 63539- U.S. Pharmaceuticals
  • 63539-501- XELJANZ XR
    • 63539-501-14- 14 TABLET, EXTENDED RELEASE in 1 BOTTLE (63539-501-14)

• 63539- U.S. Pharmaceuticals
  • 63539-501- XELJANZ XR
    • 63539-501-30- 30 TABLET, EXTENDED RELEASE in 1 BOTTLE (63539-501-30)