Upadacitinib

What is Upadacitinib?[edit | edit source]

Upadacitinib (RINVOQ) is a Janus kinase (JAK) inhibitor used to treat adults with moderate to severe rheumatoid arthritis.

RINVOQ is used to treat adults with moderate to severe rheumatoid arthritis in whom methotrexate did not work well or could not be tolerated.

Upadacitinib is a Janus kinase (JAK) inhibitor.
JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function.
Within the signaling pathway, JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs) which modulate intracellular activity including gene expression.
Upadacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs.
In human leukocyte cellular assays, upadacitinib inhibited cytokine-induced STAT phosphorylation mediated by JAK1 and JAK1/JAK3 more potently than JAK2/JAK2 mediated STAT phosphorylation.
However, the relevance of inhibition of specific JAK enzymes to therapeutic effectiveness is not currently known.

RINVOQ should be used with caution in patients receiving chronic treatment with strong CYP3A4 inhibitors (e.g., ketoconazole).
Coadministration of RINVOQ with strong CYP3A4 inducers (e.g., rifampin) is not recommended.

Recommended Dosage

The recommended oral dose of RINVOQ is 15 mg once daily with or without food.
RINVOQ may be used as monotherapy or in combination with methotrexate or other nonbiologic DMARDs.
Avoid initiation or interrupt RINVOQ if absolute lymphocyte count is less than 500 cells/mm3, absolute neutrophil count is less than 1000 cells/mm3, or hemoglobin level is less than 8 g/dL.

Administration

Take RINVOQ exactly as your healthcare provider tells you to use it.
Take RINVOQ 1 time a day with or without food.
Swallow RINVOQ whole with water at about the same time each day. Do not split or break, crush, or chew the tablets.

This medicine is available in fallowing doasage form:

This medicine is available in fallowing brand namesː

The most common side effects of this medicine include:

RINVOQ may cause serious side effects, including:

Avoid use of RINVOQ in patients with active, serious infection, including localized infections.
Consider the risks and benefits of RINVOQ treatment prior to initiating therapy in patients with a known malignancy.
Consider the risks and benefits prior to treating patients who may be at increased risk of thrombosis. Promptly evaluate patients with symptoms of thrombosis and treat appropriately.
Events of gastrointestinal perforation have been reported in clinical studies with RINVOQ. Use with caution in patients who may be at increased risk.
Laboratory monitoring is recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids.
RINVOQ may cause fetal harm based on animal studies. Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception.
Avoid use of RINVOQ with live vaccines.

In case of an overdose, it is recommended that the patient be monitored for signs and symptoms of adverse reactions. Patients who develop adverse reactions should receive appropriate treatment.

The limited human data on use of RINVOQ in pregnant women are not sufficient to evaluate a drug-associated risk for major birth defects or miscarriage.

The safety and efficacy of RINVOQ in children and adolescents aged 0 to less than 18 years have not yet been established. No data are available.

Active ingredient: upadacitinib
Inactive ingredients: microcrystalline cellulose, hypromellose, mannitol, tartaric acid, colloidal silicon dioxide, magnesium stearate, polyvinyl alcohol, polyethylene glycol, talc, titanium dioxide, ferrosoferric oxide, and iron oxide red.

Store RINVOQ in original container at 36°F to 77°F (2°C to 25°C) to protect it from moisture.
Keep RINVOQ and all medicines out of the reach of children.

Upadacitinib Resources
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