Upacit XR 15 mg

INDICATIONS

Upadacitinib is a Janus kinase (JAK) inhibitor indicated for the treatment of adults with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to one or more TNF blockers.
 
It is also indicated in atopic dermatitis (adult and pediatric patients 12 years of age and older) psoriatic arthritis, ulcerative colitis, Crohn's disease ankylosing spondylitis and non-radiographic axial spondyloarthritis.

PHARMACOLOGY

Upadacitinib is a Janus kinase (JAK) inhibitor. JAKs are intracellular enzymes that 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.

DOSAGE & ADMINISTRATION

Rheumatoid Arthritis: 15 mg once dailyPsoriatic Arthritis: 15 mg once dailyAnkylosing Spondylitis: 15 mg once dailyNon-radiographic Axial Spondyloarthritis: 15 mg once dailyPolyarticular Juvenile Idiopathic Arthritis: 15 mg once dailyEczema: 15 mg once dailyGiant Cell Arteritis: 15 mg once dailyCrohn's Disease: 

Starting- 45 mg daily for 12 weeks
Maintenance- 15 mg once daily

Ulcerative Colitis:

Starting- 45 mg once daily for 8 weeks
Maintenance- 15 mg once daily 

Upadacitinib may be used as monotherapy or in combination with methotrexate or other non-biologic DMARDs. Avoid initiation or interrupt Upadacitinib 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.
Pediatric Use: The safety and efficacy of Upadacitinib in children and adolescents aged 0 to 18 years have not yet been established. No data are available.Hepatic Impairment: Upadacitinib is not recommended in patients with severe hepatic impairment.

INTERACTION

Strong CYP3A4 Inhibitors: Upadacitinib exposure is increased when co-administered with strong CYP3A4 inhibitors (such as ketoconazole). Upadacitinib should be used with caution in patients receiving chronic treatment with strong CYP3A4 inhibitors.Strong CYP3A4 Inducers: Upadacitinib exposure is decreased when co-administered with strong CYP3A4 inducers (such as rifampin), which may lead to reduced therapeutic effect of Upadacitinib. Coadministration of Upadacitinib with strong CYP3A4 inducers is not recommended.

SIDE EFFECTS

Adverse reactions (greater than or equal to 1%) are: upper respiratory tract infections, nausea, cough, and pyrexia.

PREGNANCY & LACTATION

The limited human data on the use of Upadacitinib in pregnant women are not sufficient to evaluate a drug-associated risk for major birth defects or miscarriage. Based on animal studies, upadacitinib has the potential to adversely affect a developing fetus. Advise not to breastfeed.

PRECAUTIONS & WARNINGS

Serious Infections: Avoid use of Upadacitinib in patients with active, serious infection, including localized infections.Malignancy: Consider the risks and benefits of Upadacitinib treatment prior to initiating therapy in patients with a known malignancy.Thrombosis: 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.Gastrointestinal Perforations: Use with caution in patients who may be at increased risk.Laboratory Monitoring: Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids.Embryo-Fetal Toxicity: Upadacitinib 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.Vaccinations: Avoid use of Upadacitinib with live vaccines.

THERAPEUTIC CLASS

Drugs used for Rheumatoid Arthritis

STORAGE CONDITIONS

Do not store above 25°C. Protect from light. Keep out of reach of children.