upadacitinib (Rx)

Brand and Other Names:Rinvoq
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet, extended-release

  • 15mg

Rheumatoid Arthritis

Indicated for moderately to severely active rheumatoid arthritis in adults who have had an inadequate response or intolerance to methotrexate

15 mg PO qDay

May be used as monotherapy or in combination with methotrexate or other nonbiological DMARDs

Dosage Modifications

Dose interruption for laboratory abnormalities

  • Absolute neutrophil count (ANC) <1000 cells/mm3: Interrupt; may restart once ANC >1000 cells/mm3
  • Absolute lymphocyte count (ALC) <500 cells/mm3: Interrupt; may restart once ALC >500 cells/mm3
  • Hemoglobin (Hb) <8 g/dL: Interrupt; may restart once Hb >8 g/dL
  • Hepatic transaminases: Interrupt if drug-induced liver injury suspected

Renal impairment

  • Mild, moderate, or severe: No dose adjustment required
  • ESRD: Not studied

Hepatic impairment

  • Mild or moderate (Child-Pugh A or B): No dose adjustment required
  • Severe (Child-Pugh C): Not recommended

Dosing Considerations

ALC <500 cells/mm3, ANC <1000 cell/mm3, or Hb <8 g/dL: Do not initiate

Test for tuberculosis (TB) before initiating; initiate antitubercular treatment for previously untreated latent TB or active TB before initiating treatment

Verify pregnancy status in women of reproductive potential before initiating upadacitinib

Limitation of use: Do not use in combination with other JAK inhibitors, biologic DMARDs, or potent immunosuppressants (eg, azathioprine, cyclosporine)

Safety and efficacy not established

Ulcerative Colitis (Orphan)

Orphan designation for treatment of pediatric ulcerative colitis

Sponsor

  • AbbVie; 1 North Waukegan Road; North Chicago, Illinois 60044
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Interactions

Interaction Checker

and upadacitinib

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      Serious - Use Alternative

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            Contraindicated (0)

              Serious - Use Alternative (45)

              • abametapir

                abametapir will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.

              • adenovirus types 4 and 7 live, oral

                upadacitinib decreases effects of adenovirus types 4 and 7 live, oral by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • amobarbital

                amobarbital will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • apalutamide

                apalutamide will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • BCG vaccine live

                upadacitinib decreases effects of BCG vaccine live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • bosentan

                bosentan will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • butabarbital

                butabarbital will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • butalbital

                butalbital will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • carbamazepine

                carbamazepine will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • cholera vaccine

                upadacitinib decreases effects of cholera vaccine by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • dabrafenib

                dabrafenib will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • dengue vaccine

                upadacitinib decreases effects of dengue vaccine by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • efavirenz

                efavirenz will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • enzalutamide

                enzalutamide will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • etravirine

                etravirine will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • fosphenytoin

                fosphenytoin will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • influenza virus vaccine quadrivalent, intranasal

                upadacitinib decreases effects of influenza virus vaccine quadrivalent, intranasal by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • ivosidenib

                ivosidenib will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • lonafarnib

                lonafarnib will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration with sensitive CYP3A substrates. If coadministration unavoidable, monitor for adverse reactions and reduce CYP3A substrate dose in accordance with product labeling.

              • lorlatinib

                lorlatinib will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • lumacaftor/ivacaftor

                lumacaftor/ivacaftor will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • measles (rubeola) vaccine

                upadacitinib decreases effects of measles (rubeola) vaccine by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • measles mumps and rubella vaccine, live

                upadacitinib decreases effects of measles mumps and rubella vaccine, live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • measles, mumps, rubella and varicella vaccine, live

                upadacitinib decreases effects of measles, mumps, rubella and varicella vaccine, live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • mitotane

                mitotane will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • nafcillin

                nafcillin will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • pentobarbital

                pentobarbital will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • phenobarbital

                phenobarbital will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • phenytoin

                phenytoin will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • primidone

                primidone will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • rifabutin

                rifabutin will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • rifampin

                rifampin will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • rifapentine

                rifapentine will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • rotavirus oral vaccine, live

                upadacitinib decreases effects of rotavirus oral vaccine, live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • rubella vaccine

                upadacitinib decreases effects of rubella vaccine by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • secobarbital

                secobarbital will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • smallpox (vaccinia) vaccine, live

                upadacitinib decreases effects of smallpox (vaccinia) vaccine, live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • St John's Wort

                St John's Wort will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid upadacitinib coadministration with strong CYP3A4 inducers.

              • tucatinib

                tucatinib will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

              • typhoid polysaccharide vaccine

                upadacitinib decreases effects of typhoid polysaccharide vaccine by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • typhoid vaccine live

                upadacitinib decreases effects of typhoid vaccine live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • varicella virus vaccine live

                upadacitinib decreases effects of varicella virus vaccine live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • voxelotor

                voxelotor will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

              • yellow fever vaccine

                upadacitinib decreases effects of yellow fever vaccine by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              • zoster vaccine live

                upadacitinib decreases effects of zoster vaccine live by immunosuppressive effects; risk of infection. Avoid or Use Alternate Drug.

              Monitor Closely (26)

              • atazanavir

                atazanavir will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • chloramphenicol

                chloramphenicol will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • clarithromycin

                clarithromycin will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • cobicistat

                cobicistat will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • conivaptan

                conivaptan will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • darunavir

                darunavir will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • elagolix

                elagolix decreases levels of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

              • idelalisib

                idelalisib will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • indinavir

                indinavir will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • isoniazid

                isoniazid will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • istradefylline

                istradefylline will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

              • itraconazole

                itraconazole will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • ketoconazole

                ketoconazole will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • lopinavir

                lopinavir will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • mifepristone

                mifepristone will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • nefazodone

                nefazodone will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • nelfinavir

                nelfinavir will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • posaconazole

                posaconazole will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • ribociclib

                ribociclib will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • ritonavir

                ritonavir will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • rucaparib

                rucaparib will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Adjust dosage of CYP3A4 substrates, if clinically indicated.

              • saquinavir

                saquinavir will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • stiripentol

                stiripentol will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • tazemetostat

                tazemetostat will decrease the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              • tipranavir

                tipranavir will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Caution if upadacitinib is coadministered with strong CYP3A4 inhibitors.

              • voriconazole

                voriconazole will increase the level or effect of upadacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              Minor (0)

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                Adverse Effects

                >10%

                Upper respiratory tract infection (13.5%)

                1-10%

                Nausea (3.5%)

                Neutropenia (1.1-2.4%)

                Lymphopenia (0.3-2.4%)

                Cough (2.2%)

                Elevated ALT (0.8-2.1%)

                Increased creatine phosphokinase (0.3-1.6%)

                Elevated AST (1-1.5%)

                Pyrexia (1.2%)

                <1%

                Pneumonia

                Herpes zoster

                Herpes simplex (includes oral herpes)

                Oral candidiasis

                Anemia (<0.1%)

                Frequency Not Defined

                Tuberculosis

                Malignancies, excluding nonmelanoma skin cancer

                Venous thrombosis

                Elevated LDL

                Elevated HDL

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                Warnings

                Black Box Warnings

                Serious infection

                • Increases risk for developing serious infections that may lead to hospitalization or death
                • Most patients with severe infections were also taking concomitant immunosuppressants (eg, methotrexate, corticosteroids)
                • Interrupt upadacitinib treatment if serious infection develops; may resume once infection controlled
                • Carefully consider risks and benefits before initiating upadacitinib in patients with chronic or recurrent infection
                • Closely monitor for signs and symptoms of infection during and after treatment, including possible development of TB in patients who tested negative for latent TB infection before initiating therapy
                • Reported infections include
                  • Active TB, which may present with pulmonary or extrapulmonary disease; test for latent TB before use and during therapy; consider treating latent infection before upadacitinib use
                  • Invasive fungal infections, including cryptococcosis and pneumocystosis
                  • Bacterial, viral ( including herpes zoster), and other infections due to opportunistic pathogens

                Malignancies

                • Lymphoma and other malignancies reported in patients treated with upadacitinib

                Thrombosis

                • Thrombosis, including DVT, PE, and arterial thrombosis have occurred in patients treated with JAK inhibitors used to treat inflammatory conditions
                • Many of these adverse events were serious and some resulted in death
                • Consider risks and benefits prior to treating patients who may be at increased risk
                • Promptly evaluate and treat patients with symptoms of thrombosis

                Contraindications

                None

                Cautions

                Malignancies reported; consider risks and benefits of treatment before initiating in patients with known malignancy, other than previously treated nonmelanoma skin cancer; screen for malignancies during treatment according to guidelines

                Thrombosis reported, including DVT, PE, and arterial thrombosis

                Gastrointestinal perforation reported; unknown if JAK inhibition is implicated in these events; many patients were also receiving NSAIDs

                May cause neutropenia, lymphopenia, anemia, elevated lipids, or elevated liver enzymes; monitor for abnormal laboratory values and assess the need to interrupt dosing

                Based on findings in animal studies, may cause fetal harm when administered to pregnant women

                Serious and fatal infections

                • Serious and fatal infections reported
                • Most frequent infections reported included pneumonia and cellulitis
                • Opportunistic infections reported included TB, multidermatomal herpes zoster, oral/esophageal candidiasis, and cryptococcosis
                • Avoid in patients with an active, serious infection, including localized infections
                • Monitor for viral reactivation (eg, hepatitis B, herpes zoster) during treatment
                • Patients should be screen for opportunistic infections and treated according to guidelines

                Drug interaction overview

                • Upadacitinib is a substrate of CYP3A4 (major) and CYP2D6 (minor)
                • Strong CYP3A4 inhibitors
                  • Use caution
                  • Upadacitinib systemic exposure is increased when coadministered with strong CYP3A4 inhibitors
                • Strong CYP3A4 inducers
                  • Coadministration not recommended
                  • Upadacitinib systemic exposure is decreased when coadministered with strong CYP3A4 inducers
                • Vaccines
                  • Use of live, attenuated vaccines during or immediately before initiating upadacitinib is not recommended
                  • Before initiating, assess vaccination history, including prophylactic zoster vaccinations
                  • Ensure vaccinations are current before initiating upadacitinib
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                Pregnancy & Lactation

                Pregnancy

                Limited human data on use in pregnant women are not sufficient to evaluate a drug-associated risk for major birth defects or miscarriage

                Verify pregnancy status of females of reproductive potential before starting treatment

                Animal data

                • Based on animal studies, upadacitinib has the potential to adversely affect a developing fetus
                • In animal embryofetal development studies, oral upadacitinib administration to pregnant rats and rabbits at exposures greater or equal than ~1.6 and 15 times the maximum recommended human dose (MRHD), respectively, resulted in dose-related increases in skeletal malformations (rats only), an increased incidence of cardiovascular malformations (rabbits only), increased postimplantation loss (rabbits only), and decreased fetal body weights in both rats and rabbits

                Contraception

                • Females of reproductive potential: Use effective contraception during treatment and for 4 weeks after final dose

                Clinical considerations

                • Published data suggest that increased disease activity is associated with risk of developing adverse pregnancy outcomes in women with rheumatoid arthritis
                • Adverse pregnancy outcomes include preterm delivery (before 37 weeks of gestation), low birth weight (less than 2500 g) infants, and small for gestational age at birth

                Lactation

                No data available on the presence of upadacitinib in human milk, the effects on the breastfed infant, or the effects on milk production

                Available data in animals have shown upadacitinib excreted in milk

                If a drug is present in animal milk, it is likely the drug will be present in human milk

                Because of the potential for serious adverse reactions in the breastfed infant, advise patients that breastfeeding is not recommended during treatment with upadacitinib, and for 6 days (~10 half-lives) after the last dose

                Pregnancy Categories

                A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                NA: Information not available.

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                Pharmacology

                Mechanism of Action

                Janus kinase-1 (JAK1)-selective inhibitor; JAK1 is essential for certain cytokines to elicit signals from various interleukins, cardiotrophin, neurotrophin, and interferons

                These signals are crutial in maintaining the inflammatory condition in rheumatoid arthritis (RA); inhibition of JAK reduces production of and modulates proinflammatory cytokines central to RA

                Absorption

                Peak plasma time: 2-4 hr

                Steady-state reached within 4 days

                Distribution

                Protein bound: 52%

                Metabolism

                Metabolized by mainly CYP3A4 and potentially minor contribution from CYP2D6

                Elimination

                Half-life: 8-14 hr

                Excretion

                • Urine (24%); feces (38%)
                • ~34% of upadacitinib dose was metabolites
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                Administration

                Oral Administration

                Take orally with or without food

                Swallow tablet whole; do not split, crush, or chew

                Storage

                Store at 2-25ºC (36-77ºF)

                Store in original bottle to protect from moisture

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                Images

                No images available for this drug.
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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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                Formulary

                FormularyPatient Discounts

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                • Compare formulary status to other drugs in the same class.
                • Access your plan list on any device – mobile or desktop.

                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                OR Other Restrictions
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.