* Upadacitinib ('''RINVOQ''') is a '''[[Janus kinase]] (JAK) inhibitor''' used to treat adults with moderate to severe [[rheumatoid arthritis]].
[[File:Upadacitinib.svg|thumb|Chemical structure of Upadacitinib]]
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'''Upadacitinib''' is a medication used in the treatment of several inflammatory conditions, including [[rheumatoid arthritis]], [[psoriatic arthritis]], and [[atopic dermatitis]]. It is classified as a [[Janus kinase inhibitor]], specifically targeting the JAK1 enzyme.
Upadacitinib is primarily prescribed for adults with moderate to severe [[rheumatoid arthritis]] who have had an inadequate response or intolerance to one or more [[disease-modifying antirheumatic drugs]] (DMARDs). It is also approved for the treatment of active [[psoriatic arthritis]] and moderate to severe [[atopic dermatitis]].
* RINVOQ is used to treat adults with moderate to severe [[rheumatoid arthritis]] in whom [[methotrexate]] did not work well or could not be tolerated.
== Mechanism of Action ==
Upadacitinib works by inhibiting the activity of the [[Janus kinase 1]] (JAK1) enzyme, which plays a crucial role in the signaling pathways of various inflammatory cytokines. By blocking JAK1, upadacitinib reduces the inflammatory response that contributes to the symptoms of autoimmune diseases.
== '''How does this medicine work?''' ==
== Side Effects ==
Common side effects of upadacitinib include upper respiratory tract infections, nausea, cough, and fever. Serious side effects may include increased risk of infections, [[thrombosis]], and [[gastrointestinal perforation]]. Patients are advised to undergo regular monitoring for these potential adverse effects.
* Upadacitinib is a '''[[Janus kinase]] (JAK) inhibitor'''.
== Approval and Regulation ==
* 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.
Upadacitinib was approved by the [[United States Food and Drug Administration]] (FDA) in 2019 for the treatment of rheumatoid arthritis. It has since received approval for additional indications, including psoriatic arthritis and atopic dermatitis, in various countries.
* 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.
== '''Who Should Not Use this medicine ?''' ==
== Related Pages ==
* [[Rheumatoid arthritis]]
* [[Psoriatic arthritis]]
* [[Atopic dermatitis]]
* [[Janus kinase inhibitor]]
* This medicine have no usage limitations.
== References ==
{{Reflist}}
== '''What drug interactions can this medicine cause?''' ==
[[Category:Janus kinase inhibitors]]
[[Category:Immunosuppressants]]
* RINVOQ should be used with caution in patients receiving chronic treatment with strong CYP3A4 inhibitors (e.g., [[ketoconazole]]).
[[Category:Drugs approved by the United States Food and Drug Administration]]
* Coadministration of RINVOQ with strong CYP3A4 inducers (e.g., [[rifampin]]) is not recommended.
== '''Is this medicine FDA approved?''' ==
* It was approved for use in the United States in 2019.
== '''How should this medicine be used?''' ==
'''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.
== '''What are the dosage forms and brand names of this medicine?''' ==
This medicine is available in fallowing doasage form:
* '''As Extended-release tablets:''' 15 mg
This medicine is available in fallowing brand namesː
*'''RINVOQ'''
=='''What side effects can this medication cause?'''==
The most common side effects of this medicine include:
* upper respiratory tract infections
* nausea
* cough
* [[pyrexia]]
RINVOQ may cause serious side effects, including:
* Serious Infections
* Cancer
* Blood Clots ([[thrombosis]])
* Tears (perforation) in the stomach or intestines
* Changes in certain laboratory test results
==''' What special precautions should I follow?''' ==
* 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.
== '''What to do in case of emergency/overdose?''' ==
* 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.
== '''Can this medicine be used in pregnancy?''' ==
* 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.
=='''Can this medicine be used in children?'''==
* 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.
== '''What are the active and inactive ingredients in this medicine?''' ==
Upadacitinib works by inhibiting the activity of the Janus kinase 1 (JAK1) enzyme, which plays a crucial role in the signaling pathways of various inflammatory cytokines. By blocking JAK1, upadacitinib reduces the inflammatory response that contributes to the symptoms of autoimmune diseases.
Side Effects
Common side effects of upadacitinib include upper respiratory tract infections, nausea, cough, and fever. Serious side effects may include increased risk of infections, thrombosis, and gastrointestinal perforation. Patients are advised to undergo regular monitoring for these potential adverse effects.
Approval and Regulation
Upadacitinib was approved by the United States Food and Drug Administration (FDA) in 2019 for the treatment of rheumatoid arthritis. It has since received approval for additional indications, including psoriatic arthritis and atopic dermatitis, in various countries.
