Moderately to severely active rheumatoid arthritis (RA) in patients who have had an inadequate response/intolerance to methotrexate (as monotherapy or in combination with methotrexate) (not to be used with other Janus kinase [JAK] inhibitors, biologic disease-modifying antirheumatic drugs [DMARDs] or potent immunosuppressants [including azathioprine or cyclosporine]).
Inhibits JAK enzymes which prevents the activation of signal transducers and activators of transcription (STATs), which ultimately results in decreased hematopoiesis and immune cell function.
Improvement in clinical and symptomatic parameters of RA.
Absorption: Well absorbed following oral administration.
Distribution: Distributes equally between red blood cells and plasma.
Metabolism and Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme (with some contribution from CYP2D6); 38% excreted in feces and 24% excreted in urine as unchanged drug.
Assess pain and range of motion before and periodically during therapy.
Assess for signs of infection (fever, dyspnea, flu-like symptoms, frequent or painful urination, redness or swelling at the site of a wound), including tuberculosis and Hepatitis B virus (HBV), prior to and periodically during therapy. Upadacitinib is contraindicated in patients with active infection. Monitor new infections closely; most common are upper respiratory tract infections, bronchitis, and urinary tract infections. Infections may be fatal, especially in patients taking immunosuppressive therapy.
Assess patient for latent tuberculosis with a tuberculin skin test prior to initiation of therapy. Treatment of latent tuberculosis should be started before therapy with upadacitinib.
Assess skin for new lesions periodically during therapy; risk of skin cancer is increased.
Monitor for signs and symptoms of thrombosis (swelling, pain or tenderness in the leg, sudden unexplained chest pain, shortness of breath) during therapy.
Lab Test Considerations:
Verify negative pregnancy test before starting therapy.
Monitor neutrophil count at baseline and periodically during therapy. Do not start therapy and interrupt therapy if ANC <1000 cells/mm3 and restart therapy once ANC returns above this value.
Monitor lymphocyte count at baseline and periodically during therapy. Do not start therapy and interrupt therapy if absolute lymphocyte count (ALC) <500 cells/mm3 and restart therapy once ALC returns above this value.
May cause anemia. Monitor hemoglobin at baseline and periodically during therapy. Do not start therapy and interrupt therapy if hemoglobin level <8 g/dL.
May cause increases in total cholesterol, low-density lipoprotein (LDL) cholesterol, and high-density lipoprotein (HDL) cholesterol. Monitor levels 12 wk after starting therapy and periodically thereafter for hyperlipidemia.
Monitor liver enzymes at baseline and periodically thereafter. If AST or ALT are increased and drug-induced liver injury is suspected, hold upadacitinib.
Immunizations, prophylactic zoster vaccinations, should be current before starting therapy. Patients on upadacitinib may receive concurrent vaccinations, except for live vaccines.
Administer a tuberculin skin test prior to administration of upadacitinib. Patients with active latent TB should be treated for TB prior to therapy.
Screen patient for viral hepatitis before starting therapy.
PO Administer once daily without regard to food. DNC: Swallow tablets whole; do not split, crush, or chew.
Instruct patient to take upadacitinib as directed. Advise patient to read Patient Information before starting therapy and with each Rx refill in case of changes.
Advise patient to avoid live vaccines during therapy.
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), blood clots, 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: May cause fetal harm. Advise females of reproductive potential to use effective contraception during and for 4 wk after final dose and to avoid breastfeeding during and for 6 days (10 half-lives) after last dose. Advise patient to notify health care professional immediately if pregnancy is suspected.
Emphasize the importance of regular lab tests to monitor for adverse drug reactions.
Improved physical function and decreased fatigue.
upadacitinib is a sample topic from the Davis's Drug Guide.
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