Xeljanz: 7 things you should know

Medically reviewed by Carmen Fookes, BPharm. Last updated on Feb 27, 2023.

1. How it works

• Xeljanz is a brand (trade) name for tofacitinib citrate which may be used to treat several conditions such as rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, ulcerative colitis, and polyarticular juvenile idiopathic arthritis.
• Xeljanz works by inhibiting the Janus kinase (JAK) enzyme. JAKs transmit signals that originate from cytokine or growth factor-receptor interactions on cell membranes that influence the formation of blood cells and immune cell function. JAKs activate Signal Transducers and Activators of Transcription (STATs) which are involved in cell development, proliferation, and survival as well as the immune response. Xeljanz inhibits the in vitro activities of numerous JAK enzymes (JAK1, JAK2, JAK3, TYK2) inside the cell to help block the release of chemicals that lead to inflammation (swelling and pain).
• Xeljanz belongs to the class of medicines known as JAK inhibitors. It may also be called a non-biologic disease-modifying anti-rheumatic drug (DMARD).

2. Upsides

• Xeljanz may be used to treat patients with moderate to severe rheumatoid arthritis who have had an inadequate response to or cannot tolerate methotrexate. It can be used alone or with methotrexate or other nonbiologic disease-modifying antirheumatic drugs (DMARDs). Not recommended with biologic DMARDs or potent immunosuppressants such as azathioprine or cyclosporine.
• May also be used to reduce joint pain and joint swelling, and help to improve physical functioning in adults with psoriatic arthritis in those adults who have tried methotrexate or other medicines without success. Not recommended with biologic DMARDs or potent immunosuppressants such as azathioprine or cyclosporine.
• May also be used for moderate to severe ulcerative colitis in adults who have had an inadequate response or who are intolerant to TNF blockers. An initial induction dose is recommended before transitioning to a maintenance dose depending on the therapeutic response. The dosage will need to be reduced with CYP3A4 inhibitors or in those with kidney or liver disease.
• Consider using Xeljanz to treat polyarticular juvenile idiopathic arthritis in children aged 2 years of age and older. Do not use it with biologics or severe immunosuppressants.
• Can be used to treat adults with active ankylosing spondylitis who have had an inadequate response or intolerance to one or more tumor necrosis factor (TNF) blockers.
• Xeljanz is taken orally (by mouth).
• Available as Xeljanz and Xeljanz XR. Xeljanz is taken twice daily and is available in two strengths: 5mg and 10mg. Xeljanz is taken once a day and is available in two strengths: 11mg and 22mg.
• Xeljanz and Xeljanz XR is available as an oral tablet and a clear, colorless, oral solution. The strength of Xeljanz oral solution is 1 mg/mL.
• Weight gain and weight loss have not been identified as side effects during clinical trials of Xeljanz.
• May be taken with or without food.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• Upper respiratory tract infections, nasopharyngitis, diarrhea, and headache are the most common side effects. Diverticulitis, dehydration, insomnia, paresthesia, gastrointestinal effects (such as nausea, vomiting, abdominal pain, dyspepsia), dyspnea, rash, pain, and cough have also been reported.
• May cause high blood pressure (hypertension), high lipid levels, or elevations in liver enzymes or blood creatine phosphokinase.
• Xeljanz XR is not interchangeable with Xeljanz oral solution.
• Xeljanz should not be started in people with absolute lymphocyte counts less than 500 cells/mm³, absolute neutrophil counts of less than 1000 cells/mm³, or with hemoglobin levels of less than 9 g/dL. May not be suitable for people with a previous history of gastrointestinal perforation or with pre-existing severe gastrointestinal narrowing.
• The dosage of Xeljanz will need to be discontinued or reduced in people who develop lymphopenia, neutropenia, or anemia. Discontinue dosing in those with lymphocyte counts fewer than 500 cells/mm3 confirmed by repeat testing; interrupt dosing of Xeljanz with absolute neutrophil counts (ANC) of 500 to 1000 cells/mm3, but discontinue Xeljanz if ANC is less than 500 cells/mm3. In those with hemoglobin levels less than 8g/dL or a decrease of greater than 2 g/dL interrupt dosing until hemoglobin values have normalized.
• People taking Xeljanz and Xeljanz XR are at increased risk for developing serious infections that may lead to hospitalization or death. Most patients were already taking other immunosuppressants such as methotrexate or corticosteroids. Infections included active tuberculosis, invasive fungal infections, such as cryptococcosis and pneumocystosis as well as bacterial, viral (eg, herpes zoster, hepatitis B or C), and other infections. Review all other immune-suppressing medications before initiating Xeljanz and Xeljanz XR, and be aware of those immune-suppressing agents with a long half-life whose effects may persist for weeks after discontinuation, such as natalizumab, teriflunomide, or mitoxantrone. Life-threatening and fatal infections have occurred in association with Xeljanz and Xeljanz XR. Discontinue Xeljanz until the infection is controlled. People with diabetes and seniors are at higher risk for infection so monitor these populations carefully.
• Xeljanz and Xeljanz XR will also reduce the immune response to live vaccines, such as MMR and varicella vaccines. All vaccines should be up to date before Xeljanz and Xeljanz XR are even started. All pediatric patients should complete all immunizations per current immunization guidelines before initiating Xeljanz or Xeljanz XR therapy, if possible.
• Children taking Xeljanz for polyarticular course juvenile idiopathic arthritis will need their dosage adjusted if they weigh less than 40kg. Xeljanz 5mg twice a day is recommended for those weighing 40kg or more, which can be given in the form of a tablet or oral solution. A 4ml (4mg) dose of the Xeljanz oral solution given twice daily is recommended for patients weighing ≥20kg and ﹤40kg, while a 3.2ml dose given twice a day is recommended for patients weighing ≥10kg and ﹤20kg.
• Higher dosages of Xeljanz (for example 10mg twice a day compared to 5mg twice a day) are associated with a higher rate of mortality, including sudden cardiovascular death, in people with rheumatoid arthritis aged 50 years of age and older with at least one cardiovascular risk factor.
• People taking Xeljanz have an increased risk of developing cancer, such as lymphoma.
• Epstein Barr Virus-associated post-transplant lymphoproliferative disorder has been reported in renal transplant patients prescribed Xeljanz and other immunosuppressant medications. Severe allergic reactions and urticaria have also been reported.
• Xeljanz is associated with thrombosis (blood clotting) and an increased incidence of events such as pulmonary embolism, deep venous thrombosis, and arterial thrombosis. Many of these events were serious and some were fatal. In people with ulcerative colitis, always use the lowest effective dose of Xeljanz for the shortest possible time.
• Reduce the dosage of Xeljanz to 5mg once daily in those with moderate or severe kidney disease or moderate liver disease. Administer Xeljanz post-hemodialysis in those undergoing hemodialysis. Do not administer to people with severe liver disease.
• There is not enough data to establish if Xeljanz is associated with major birth defects, miscarriage, or other adverse maternal or fetal outcomes when it is given to pregnant women. weigh up the risks versus benefits because there is evidence that increased disease activity in conditions such as rheumatoid arthritis or ulcerative colitis is associated with preterm delivery (before 37 weeks of gestation), low birth weight (less than 2500 g) infants, and small for gestational age at birth. If a woman becomes pregnant while taking Xeljanz encourage her to enroll in the Xeljanz pregnancy registry by calling the toll-free number 1-877-311-8972. Breastfeeding is not recommended during Xeljanz treatment and for at least 18 hours after the last dose of Xeljanz/Xeljanz Oral Solution or 36 hours after the last dose of Xeljanz XR.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

• Xeljanz is a Janus kinase (JAK) inhibitor that may be used to reduce inflammation associated with several conditions such as rheumatoid arthritis, psoriatic arthritis, ulcerative colitis, or polyarticular juvenile idiopathic arthritis. Infections, nasopharyngitis, diarrhea, and headache are the main side effects reported and the dosage of Xeljanz needs to be reduced in people with liver or kidney disease or who take some interacting medicines.

5. Tips

• Do not crush or chew Xeljanz XR tablets. Swallow them whole. Xeljanz may be taken with or without food.
• Xeljanz oral solution does not need to be shaken before use.
• There are three forms of Xeljanz: Xeljanz immediate-release tablets, Xeljanz XR tablets, and Xeljanz solution. Make sure your pharmacy has correctly dispensed the formulation that you have been prescribed.
• You may notice an inert tablet shell in your feces if you have been prescribed Xeljanz XR. This is not of concern as the active medication has already been absorbed.
• The dosage of Xeljanz may need to be reduced if you have liver or kidney disease, rheumatoid arthritis, or psoriatic arthritis, or if with certain other medications. Always take Xeljanz exactly as prescribed by your doctor. Do not take more or less than recommended.
• While you are taking Xeljanz you are at an increased risk of infections, because Xeljanz lowers your immune response. Some vaccinations may need to be avoided during treatment with Xeljanz and for two months after stopping it. Take care to avoid people who are unwell and protect yourself from injury. See your doctor immediately if you develop any signs of an infection which may include fever, pain, swelling, redness, or a discharge.
• See your doctor if you experience any unusual or worrying side effects, such as unusual bleeding or bruising, yellow eyes or skin, clay-colored stools, chest pain worsened with breathing, swelling, abdominal pain, allergic reactions, persistent fatigue, weight loss, or an infection (signs may include red or discolored skin, pain, swelling, burning when urinating). Xeljanz can increase your risk of serious infections, such as herpes zoster, or activate previously latent tuberculosis, hepatitis B or C.
• Tell your doctor if you have ever had any type of cancer as Xeljanz may increase your risk of developing other cancers such as lymphoma. Xeljanz may also not be suitable for you if you have chronic lung disease, diabetes, HIV, hepatitis B or C, an organ transplant, diverticulitis, stomach ulcers, or a weakened immune system.
• Tell your doctor if you live, have lived, or have traveled to certain parts of the country (such as the Ohio and Mississippi River valleys and the Southwest) because you may be at increased risk for certain kinds of fungal infections such as histoplasmosis, coccidioidomycosis, or blastomycosis.
• You should use adequate contraception to ensure that you do not become pregnant while taking Xeljanz, although it is unknown if Xeljanz is associated with major birth defects or other adverse pregnancy outcomes. If you do inadvertently become pregnant then you should enroll in the Xeljanz pregnancy registry by calling the toll-free number 1-877-311-8972. Breastfeeding is not recommended during Xeljanz treatment and for at least 18 hours after the last dose of Xeljanz/Xeljanz Oral Solution or 36 hours after the last dose of Xeljanz XR. There is evidence that Xeljanz may reduce female fertility.
• Xeljanz may affect the results of some laboratory tests. Tell all health professionals that you are taking Xeljanz.
• Store Xeljanz oral solution at room temperature between 68°F to 77°F (20°C to 25°C). Use Xeljanz oral solution within 60 days of opening the bottle. Throw away any remaining solution after this date.
• Xeljanz oral solution comes with a press-in bottle adapter and an oral dosing syringe (remove from plastic packaging before use). The first time you open the bottle, push on the child-resistant cap (keep this) and turn it to the left (counter-clockwise). Remove the seal off the top of the bottle and with the bottle on a flat surface push the ribbed end of the press-in bottle adapter into the neck of the bottle with your thumbs while holding the bottle firmly. When you need to give a dose of Xeljanz insert the oral dosing syringe tip into the upright bottle through the opening of the press-in bottle adapter until it is firmly in place. With the oral dosing syringe in place, turn the bottle upside down and pull down on the plunger until the bottom of the plunger is even with the markings on the oral dosing syringe for your prescribed dose of oral solution. If you see air bubbles in the oral dosing syringe, fully push the plunger in so that the oral solution flows back into the bottle. Then withdraw your prescribed dose of oral solution. Once you have filled up the dosing syringe turn the bottle upright and place the bottle on a flat surface. Remove the oral dosing syringe from the press-in bottle adapter and bottle by pulling straight up on the oral dosing syringe barrel. Check the dose and repeat the steps above if the dose is not correct. Administer the dose by placing the tip of the oral dosing syringe into the inside of the cheek and slowly pushing the plunger down. Swallow the medicine. Leave the press-in bottle adapter in place and replace the child-resistant cap. Clean the oral dosing syringe after use by removing the plunger and running it under water, then allow it to air dry. Reassemble the oral dosing syringe and keep it until the next use.

6. Response and effectiveness

• Some reduction in symptoms may be noticed within two weeks of taking; however, it may take up to three or four months to notice an improvement in other symptoms.
• Xeljanz starts to work within two weeks for some patients with rheumatoid arthritis and psoriatic arthritis, with improvements noted in physical function and a reduction in the number of joints that are painful, tender, and swollen.
• For polyarticular juvenile idiopathic arthritis, a phase III trial reported 45.11% of patients achieving an American College of Rheumatology (ACR) 30 response within two weeks. ACR scores look for improvements across a range of paraments and provide a composite score. Parameters include tender and painful joints, inflammation, pain, physical function, and more. The number of patients who responded to treatment continued to increase with 92.21% achieving an ACR30 by 18 weeks.
• Xeljanz provides a significant improvement in ulcerative colitis symptoms (such as rectal bleeding and stool frequency) within three days. Xeljanz can lead to the remission of ulcerative colitis without the use of corticosteroids.
• In studies, disease flares of JIA were shown to be significantly less in patients receiving Xeljanz than those receiving a placebo. Patients can use an oral tablet or oral solution for their dose, which is based on weight.

7. Interactions

Medicines that interact with Xeljanz and Xeljanz XR may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with Xeljanz and Xeljanz XR. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

Xeljanz and Xeljanz XR interact with over 470 medications; at least half of these interactions are considered major. Common medications that may interact with Xeljanz and Xeljanz XR include:

• antibiotics such as azithromycin, ciprofloxacin, or norfloxacin
• anticonvulsants, such as carbamazepine or phenobarbital
• antifungals, such as itraconazole or ketoconazole
• antineoplastics, such as capecitabine, carboplatin, cyclophosphamide, or mitoxantrone
• antipsychotics, such as clozapine
• biologics, such as adalimumab, etanercept, golimumab, or infliximab
• busulfan
• corticosteroids (such as betamethasone, prednisone, or dexamethasone)
• digoxin
• fingolimod
• griseofulvin
• heart medications, such as beta-blockers (eg, atenolol, sotalol), digoxin, diltiazem, amiodarone, or flecainide
• herbals, such as echinacea or St. John's wort
• HIV medications, such as atazanavir or zidovudine
• hydroxyurea
• immunosuppressants such as azathioprine, cyclosporine, or tacrolimus
• interferon or peginterferon
• leflunomide
• live vaccines and some other vaccines, such as BCG, cholera, measles, hepatitis b vaccines, yellow fever, or live influenza vaccines
• methotrexate
• mifepristone
• NSAIDs such as diclofenac or ibuprofen
• omeprazole
• opioids, such as alfentanyl, buprenorphine, fentanyl, or morphine
• probiotics, such as lactobacillus
• quinidine
• rifampin
• tramadol.

Xeljanz and Xeljanz XR should not be given with other strong immunosuppressants, particularly those with prolonged immune-suppressing effects, such as natalizumab, teriflunomide, or mitoxantrone.

The dosage of Xeljanz should be reduced to 5mg once daily in people receiving a strong CYP3A4 inhibitor (such as clarithromycin, erythromycin, diltiazem, itraconazole, ketoconazole, ritonavir, verapamil, goldenseal, or grapefruit) or a moderate CYP3A4 inhibitor with a strong CYP2C19 inhibitor (such as fluconazole).

Note that this list is not all-inclusive and includes only common medications that may interact with Xeljanz. You should refer to the prescribing information for Xeljanz for a complete list of interactions.

References

• Xeljanz (tofacitinib citrate). Updated 11/2022. Pfizer Laboratories Div Pfizer Inc. https://www.drugs.com/pro/xeljanz.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use Xeljanz only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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