section name header

Pronunciation

toe-fa-SYE-ti-nib

Classifications

Therapeutic Classification: antirheumatics

Pharmacologic Classification: kinase inhibitors

Indications

REMS


Action

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

Pharmacokinetics

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.

Time/Action Profile

(clinical improvement)

ROUTEONSETPEAKDURATION
POwithin 2 wk3 mounknown
PO-ERunknownunknownunknown





Contraind./Precautions

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects

Interactions

Drug-drug:

Route/Dosage

Rheumatoid Arthritis, Psoriatic Arthritis, and Ankylosing Spondylitis

Hepatic Impairment

Renal Impairment

Ulcerative Colitis

Hepatic Impairment

Renal Impairment

Active Polyarticular Course Juvenile Idiopathic Arthritis

Hepatic Impairment

Renal Impairment

Availability

(Generic available)

Assessment

Lab Test Considerations:

Implementation

Patient/Family Teaching

Evaluation/Desired Outcomes

US Brand Names

Xeljanz, Xeljanz XR