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Tofacitinib

Tofacitinib

  • Pregnancy category C
  • Xeljanz
  • Topical, oral
  • JAK1/3 >>2

FDA

  • Psoriatic arthritis 
  • Rheumatoid arthritis 
  • Ulcerative colitis 

Off-label

  • Atopic dermatitis
  • Psoriasis (not approved yet due to side effects with the 10 mg twice daily dose)
  • Alopecia areata (recurrence of alopecia areata observed after discontinuation)
  • Vitiligo
  • Systemic lupus erythematosus

Reports

  • Discoid lupus 
  • Diffuse systemic sclerosis
  • Sjögren syndrome
  • Chronic actinic dermatitis
  • Hypereosinophilic syndrome
  • Idiopathic erythema multiforme
  • Cutaneous sarcoidosis
  • Dermatomyositis
  • Diffuse systemic sclerosis
  • SAPHO (synovitis, acne, pustulosis, hyperostosis & osteitis)

Boxed warning

  • Serious infections & malignancy

Infections

  • Nasopharyngitis & upper respiratory tract infections (most common), bacterial, fungal, viral & opportunistic infections

Cardiovascular

  • Bradycardia & prolonged PR- interval, thromboembolic events

Pulmonary

  • Interstitial lung disease (caution with methotrexate)

Gastrointestinal

  • Perforation (caution with nonsteroidal anti-inflammatory drugs)

Cutaneous

  • Non-melanoma skin cancers (report of aggressive cutaneous squamous cell carcinoma), Melanoma, Varicella zoster reactivation, pruritus, acne, aphthous ulcers, drug eruptions

Laboratory changes

  • Anemia
  • Lymphopenia 
  • Neutropenia
  • Transaminitis 
  • Hyperlipidemia
  • Increased creatinine
  • Strong CYP3A4 inhibitors increase toxicity 
  • Avoid combination with immunosuppressive agents due to increased risk of complications

Baseline

  • Complete blood count with differential
  • Electrolytes
  • Liver function tests
  • Lipid profile
  • Hepatitis B & C
  • Tuberculosis evaluation
  • Pregnancy test 

Follow up

  • Annual physical exam for skin cancers 
  • Monitor for signs/symptoms of infections including tuberculosis 
  • Complete blood count with differential
  • Liver function test
  • Lipid profile
  • Repeat labs every 4-8 weeks after initiation, then every 3 months

Notes

  • Discontinue if lymphocyte <500 or ANC <500
  • Interrupt dose if hemoglobin drop >2g or <8g/dl
  • Avoid live vaccines