Genetic Implications:
Pronunciation:
toe-fa-sye-ti-nib
Trade Name(s)
Ther. Class.
Pharm. Class.
kinase inhibitors
Acts as a Janus kinase (JAK) inhibitor. Some results of inhibition include decreased hematopoiesis and immune cell function. Decreases circulating killer cells, increases in B cell count and decreases serum C-reactive protein (CRP).
Therapeutic Effect(s):
Improvement in clinical and symptomatic parameters of RA, psoriatic arthritis, and ulcerative colitis.
Absorption: Well absorbed following oral administration (74%).
Distribution: Distributes equally between red blood cells and plasma.
Metabolism and Excretion: 70% metabolized by the liver (primarily CYP3A4 with some contribution from CYP2C19). 30% renal excretion of the parent drug.
Half-life: 3 hr.
TIME/ACTION PROFILE (clinical improvement)
ROUTE | ONSET | PEAK | DURATION |
---|---|---|---|
PO | within 2 wk | 3 mo | unknown |
PO-ER | unknown | unknown | unknown |
Contraindicated in:
Use Cautiously in:
CV: ARTERIAL THROMBOSIS, DEEP VEIN THROMBOSIS, peripheral edema
Derm: erythema, pruritus, rash
F and E: dehydration
GI: GI PERFORATION, abdominal pain, diarrhea, dyspepsia, gastritis, ↑ liver enzymes, vomiting
GU: ↑ serum creatinine
Hemat: anemia, neutropenia
Metabolic: ↑ lipids
MS: arthralgia, joint swelling, musculoskeletal pain, tendonitis
Neuro: paresthesia, fatigue, headache, insomnia
Resp: PULMONARY EMBOLISM
Misc: DEATH, HYPERSENSITIVITY REACTIONS (including angioedema and urticaria), INFECTION (including tuberculosis, bacterial, invasive fungal infections, viral, and other infections due to opportunistic pathogens), MALIGNANCY, fever
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
Drug-Drug
RA and Psoriatic Arthritis
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).
Renal Impairment
PO (Adults): Moderate or severe renal impairment– 5 mg once daily (immediate-release); if taking 11 mg once daily (extended-release tablets), then switch to 5 mg once daily (immediate-release tablets). For patients undergoing hemodialysis, administer dose after dialysis session.
Hepatic Impairment
PO (Adults): Moderate hepatic impairment– 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).
Renal Impairment
PO (Adults): Moderate or severe renal impairment– if taking 10 mg twice daily (immediate-release tablets), ↓ to 5 mg twice daily (immediate-release tablets); if taking 5 mg twice daily (immedate-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). For patients undergoing hemodialysis, administer dose after dialysis session.
Hepatic Impairment
PO (Adults): Moderate hepatic impairment– 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).
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).
Renal Impairment
PO (Children ≥ 2 yr): Moderate or severe renal impairment– ≥40 kg: 5 mg once daily (immediate-release tablets or oral solution); 20–<40 kg: 4 mg once daily (oral solution). 10–<20 kg: 3.2 mg once daily (oral solution). For patients undergoing hemodialysis, administer dose after dialysis session.
Hepatic Impairment
PO (Children ≥2 yr): Moderate hepatic impairment– ≥40 kg: 5 mg once daily (immediate-release tablets or oral solution); 20–<40 kg: 4 mg once daily (oral solution). 10–<20 kg: 3.2 mg once daily (oral solution).
Immediate-release tablets: 5 mg, 10 mg
Extended-release tablets: 11 mg, 22 mg
Oral solution (grape flavor): 1 mg/mL
Lab Test Considerations:
Monitor CBC prior to and periodically during therapy. Do not initiate tofacitinib in patients with lymphocyte count <500 cells/mm3 , an ANC <1000 cells/mm3 , or who have hemoglobin level <9 g/dL.
Administer a tuberculin skin test prior to administration of tofacitinib. Patients with active latent TB should be treated for TB prior to therapy.
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