Upadacitinib (Rinvoq) Mechanism of Action |Side effects |Nursing Implications |Patient Teachings

Introduction

In this article, you’ll learn about the Upadacitinib (Rinvoq) mechanism of action (MOA), side effects, and nursing considerations. Also, its dosage, indication, contraindications, interactions, nursing assessment, nursing interventions, and patient teachings.

Upadacitinib (Rinvoq) is a Janus kinase (JAK) inhibitor used to treat moderate to severe active rheumatoid arthritis in patients who have had an unsatisfactory response or intolerance to one or more tumor necrosis factor (TNF) blockers.

Upadacitinib pronunciation: juˌpædəˈsaɪtɪnɪb/ Ue-pad′ a-sye′ ti-nib

Generic Name: Upadacitinib

Brand Names: Rinvoq

Upadacitinib (Rinvoq) Class and Category

Pharmacologic class: Janus associated kinase (JAK) inhibitor

Therapeutic class: Immunomodulating agent

Pregnancy category: D

Upadacitinib (Rinvoq) Dosage

Rheumatoid Arthritis Dosage

  • Adults: PO: 15 mg, OD.

Rinvoq can be taken alone or in combination with other conventional synthetic disease-modifying antirheumatic drugs (csDMARDs) like methotrexate.

Psoriatic Arthritis Dosage

  • Adults: PO: 15 mg, OD.

Rinvoq can be taken alone or in combination with non-biologic disease-modifying antirheumatic drugs (DMARDs).

Ankylosing Spondylitis

  • Adults: PO: 15 mg, OD.

Upadacitinib (Rinvoq) Pharmacokinetics and Pharmacodynamics

Absorption: Upadacitinib is effectively absorbed in the GI tract when taken orally.

Distribution: Protein binding is 52 – 59 %.

Metabolism: Upadacitinib metabolism is primarily mediated by CYP3A4, with a little contribution from CYP2D6.

Half-life: 8 – 14 hours

Excretion: Upadacitinib is excreted unchanged via urine, feces, and as metabolites.

Upadacitinib (Rinvoq) Mechanism of Action

Upadacitinib is a Janus kinase inhibitor. Janus Kinases (JAKs) are intracellular enzymes that carry cytokine or growth factor signals that are involved in a variety of cellular activities such as inflammatory responses, hematopoiesis, and immunological surveillance. 

The JAK enzyme family consists of four members: JAK1, JAK2, JAK3, and TYK2, which work in pairs to phosphorylate and activate signal transducers and transcription activators (STATs). 

This, in turn, influences gene expression and cellular function. JAK1 signals are crucial in inflammatory cytokine signals, JAK2 signals are vital in red blood cell maturation, and JAK3 signals are important in immune surveillance and lymphocyte function.

In a cell-free isolated enzyme assay, Upadacitinib inhibited JAK1 and JAK2 more effectively than JAK3 and TYK2. Upadacitinib reduced cytokine-induced STAT phosphorylation mediated by JAK1 and JAK1/JAK3 more potently than JAK2/JAK2 mediated STAT phosphorylation in human leukocyte cellular tests.

What are the indications of Upadacitinib (Rinvoq)?

Upadacitinib (Rinvoq) indications are as follows.  

  • To treat Rheumatoid Arthritis.
  • To treat Psoriatic Arthritis.
  • To treat Ankylosing Spondylitis.

What are the contraindications of Upadacitinib (Rinvoq)?

The contraindications of Upadacitinib (Rinvoq) are:

  • Hypersensitivity to Upadacitinib and its components.
  • Should NOT take with biologic disease-modifying anti-rheumatic medications (bDMARDs).
  • Should NOT use live attenuated vaccines with or just prior to Upadacitinib therapy.

Caution: Chronic anemia, hepatic disease, dyslipidemia.

Upadacitinib (Rinvoq) Interactions

  • Co-administered with strong CYP3A4 inhibitors (such as ketoconazole, itraconazole, posaconazole, voriconazole and clarithromycin) increases Upadacitinib plasma levels.
  • Co-administered with strong CYP3A4 inducers (such as rifampicin and phenytoin) decreases Upadacitinib plasma levels. Which can reduce the therapeutic effectiveness of Rinvoq.
  • Upadacitinib increases blood creatine phosphokinase (CPK), ALT, and AST.
  • Upadacitinib decreases neutrophil counts, lymphocyte count, and hemoglobin levels.
  • Upadacitinib increases total cholesterol, low-density lipoprotein (LDL) cholesterol, triglycerides, and high-density lipoprotein (HDL) cholesterol levels.

Herbal/food interactions

  • Upadacitinib interactions with food or herbs is unknown.

What are the side-effects of Upadacitinib (Rinvoq)?

Common Upadacitinib (Rinvoq) side effects include:

  • Upper respiratory tract infections (URTIs)
  • Bronchitis
  • Nausea
  • Cough
  • Fever
  • Acne
  • Gastroenteritis
  • Anemia
  • Leukopenia
  • Lymphopenia
  • Neutropenia
  • Hypercholesterolemia
  • Headache
  • Dizziness
  • Hypertension
  • Constipation or diarrhea
  • Weight gain
  • Cellulitis
  • Herpes zoster
  • Herpes simplex

Life-threatening adverse effects Upadacitinib (Rinvoq)

  • Pneumonia
  • Gastrointestinal Perforations
  • Thrombosis
  • Sepsis
  • Neoplastic disease (such as lymphomas/leukemia) and skin cancer

Upadacitinib (Rinvoq) Nursing Implications [Nursing Considerations]

Upadacitinib (Rinvoq) nursing implications are divided into nursing assessment, nursing diagnosis, nursing interventions, and evaluation. 

Upadacitinib (Rinvoq) nursing assessment

  • Obtain detailed clinical history including hypersensitivity, tuberculosis, chronic or recurrent infection, vaccination, malignancies, pregnancy, and lactation.
  • Obtain travel history for regions with prevalent tuberculosis or endemic mycoses.
  • Assess and document baseline vital signs and weight.
  • Assess the pain, stiffness, ROM, swelling of joints.
  • Assess for underlying conditions that may predispose patient to infection.
  • Obtain baseline CBC, LFTs, Lipids.

Upadacitinib (Rinvoq) nursing diagnosis

Upadacitinib (Rinvoq) nursing interventions/ actions

  • Monitor patient for any sign or symptoms of infection (such as chills, fever, flulike symptoms). Possibility of viral reactivation is increased with Upadacitinib.
  • Monitor CBCs. Do Not initiate or continue Rinvoq therapy 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.
  • Monitor patient’s LFTs during Rinvoq therapy. Because Rinvoq increase liver enzymes and cholesterol levels which can lead to serious hepatic and cardiac adverse events.
  • Monitor patient’s lipid profile. Rinvoq therapy is associated with increased risk of elevated total cholesterol, LDL, HDL, and triglycerides.
  • Observe for any signs or symptoms of major cardiac events. Rinvoq therapy increases risk of major cardiac events such as MI, Stroke, and cardiovascular death.

Evaluation

Evaluate the effectiveness of the Upadacitinib (Rinvoq):

  • For decreased arthritic pain, inflammation, and improved ROM.
  • For decreased joint destruction.
  • Remained free of adverse effects related to Upadacitinib therapy.
  • Adherence to treatment regimen.

Pregnancy/breastfeeding considerations for Upadacitinib (Rinvoq)

  • Upadacitinib has the potential to be fatal to the fetus.
  • Advise the patients of reproductive age to use an effective contraception during and for 4 weeks after the last dose.
  • It is unknown whether Upadacitinib is excreted in breastmilk. Animal studies shows Upadacitinib is excreted in lactating rats. Therefore, Rinvoq therapy is NOT recommended during lactation.

What is the nurse patient teachings for Upadacitinib (Rinvoq)?

The nursing patient teaching for Upadacitinib (Rinvoq) should include the following points.

  • Instruct the patient that he or she should take the missed dose as soon as possible. The next dose should be taken at the regularly scheduled time.
  • Advise the patient to take Rinvoq dose regularly on time with or without food.
  • Inform the patient that Rinvoq extended-release tablets should be taken as a whole. It should NOT be split, crushed, or chewed.
  • Teach the patient about the adverse effects of Upadacitinib and advise to seek medical attention if any sign or symptom occurs.
  • Inform the patient that they are more prone to infections while of Upadacitinib therapy. Advise to contact healthcare provider immediately if they develop any signs or symptoms of an infection (such as fever, shortness of breath).
  • Inform the patient that Upadacitinib therapy increases risk of certain cancers such as lymphomas and skin cancer.
  • Explain to the patient that Rinvoq therapy increases risk of major cardiac events such as MI, Stroke, and cardiovascular death. Teach the patient signs and symptoms of cardiovascular events and advice to be on alert for those symptoms.
  • Inform the patient about the risk of thrombosis such as DVT and pulmonary embolism. Teach the patient signs and symptoms of DVT and PE, and advise to seek immediate medical attention if any of those signs or symptoms occurs.
  • Explain to the patient that Rinvoq therapy affects certain blood tests and importance of doing routine blood test as advised.
  • Advise the patients of reproductive age to avoid pregnancy and use an effective contraception during and for 4 weeks after the last dose.

Treatment for Upadacitinib (Rinvoq) Overdose

Upadacitinib (Rinvoq) overdosage does not have a specific treatment. Symptomatic treatment should be given to the patient.  Also, closely observe for adverse effects.

Conclusion

You’ve learned about the Upadacitinib (Rinvoq) mechanism of action (MOA), side effects, and nursing considerations in this article.

In addition, you’ve learned about Upadacitinib’s pharmacokinetics, dosage and administration, indications, contraindications, nursing assessment, nursing diagnoses, nursing interventions, and patient teaching.

Recommended Readings & Reference

Australian TGA Pembrolizumab (Keytruda) Information

FDA Pembrolizumab (Keytruda) Information

Herdman, T., Kamitsuru, S. & Lopes, C. (2021). NURSING DIAGNOSES: Definitions and Classifications 2021-2023 (12th ed.). Thieme.

Skidmore-Roth, L. (2021). MOSBY’S 2021 NURSING DRUG REFERENCE (34th ed.). Elsevier Inc.

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