A Janus kinase (JAK) inhibitor, tofacitinib is sold under the brand name Xeljanz and is used to treat a number of autoimmune conditions. The specifically designed 11 mg extended-release tablet has the convenience of a once-daily dosing. It is important in the treatment of long-term inflammatory diseases in which the immune system targets healthy tissues, causing damage, discomfort, and swelling.

Indications

The main indications for tofacitinib 11 mg (Xeljanz XR, extended release) are:

Those who have developed an intolerance to methotrexate or who have moderate to severe active rheumatoid arthritis (RA) and have not responded well to it.

For people with active psoriatic arthritis (PsA) who did not respond well to other disease-modifying antirheumatic medications (DMARDs).

When traditional treatments or TNF inhibitors are unsuccessful or poorly tolerated, persons with moderately to highly active ulcerative colitis (UC) may benefit from this treatment.

People with active ankylosing spondylitis (AS) can now receive treatment in some places.

Note: The 11 mg dosage form is not usually started at the beginning of treatment; rather, it is mostly used for maintenance therapy.

Mechanism of Action

Janus kinases (JAKs), specifically JAK1 and JAK3, and to a lesser degree JAK2, are selectively inhibited by tofacitinib. The signaling pathways of many cytokines involved in immune function depend on these enzymes. Tofacitinib reduces the symptoms and course of autoimmune disorders by blocking JAKs, which interferes with the mechanism that triggers immune cell activation, proliferation, and inflammation.

Dosage and Administration

The 11 mg extended-release tablet is intended to be taken orally once daily.

It should be swallowed whole, not crushed, split, or chewed.

Tofacitinib can be taken with or without food.

Dose adjustments may be necessary in patients with hepatic or renal impairment, or those taking strong CYP3A4 inhibitors.

Pharmacokinetics

Absorption: The 11 mg extended-release formulation allows for steady absorption over 24 hours.

Half-life: Approximately 3 hours (for immediate release), but the XR formulation maintains therapeutic levels longer.

Metabolism: Mainly through the liver enzyme CYP3A4, with CYP2C19 playing a small role.

Excretion: Mainly through feces and urine.

Efficacy

According to clinical research, tofacitinib considerably reduces RA, PsA, and UC symptoms. It has been discovered to:

Decrease edema and joint pain.

Improve your physical function and quality of life.

induce and sustain remission in people suffering from ulcerative colitis.

Safety and Side Effects

Tofacitinib 11 mg (Xeljanz) is susceptible to infections and other side effects, just like other immunomodulator. Typical and dangerous adverse effects include:

Typical adverse effects:

Infections of the upper respiratory tract

A headache

Having diarrhea

Nasopharyngitis

Serious adverse effects:

An elevated risk of severe infections, such as herpes zoster and TB

Clots of blood

Heart-related incidents

Some types of cancer (like lymphoma)

Increased lipid levels and liver enzymes

To keep an eye on lipid profiles, white blood cell counts, and liver function, routine blood tests are frequently necessary.

Warnings and Precautions

Infections: Patients should be screened for latent tuberculosis and other infections prior to starting therapy.

Thrombosis Risk: Caution in patients with a history of blood clots or cardiovascular disease.

Malignancy: Long-term use may increase the risk of malignancies; regular check-ups are recommended.

Immunizations: Live vaccines should be avoided during treatment; patients should be up to date on immunizations before starting Tofacitinib.

Drug Interactions

Interactions between tofacitinib and:

CYP3A4 inhibitors, like ketoconazole, have the potential to raise medication levels.

Inducers of CYP3A4, such as rifampin, may lessen efficacy.

The possibility of cumulative immunosuppression with other immunosuppressants.

To prevent negative interactions, medical professionals should go over the patient’s whole drug list.

Utilization in Particular Populations

Lactation and pregnancy: Not advised unless the possible advantages outweigh the risks. Studies on animals have revealed fetal damage.

Pediatric utilize: Children are not permitted to utilize the 11 mg extended-release formulation.

Elderly Patients: Close observation is recommended due to the increased risk of infections and side effects.

Conclusion

For individuals with long-term autoimmune diseases, tofacitinib 11 mg (Xeljanz XR) provides a practical and efficient once-daily solution. Despite its good efficacy profile, the possibility of severe adverse effects necessitates cautious monitoring when using it. Healthcare professionals must customize therapy according to the patient’s medical history, risk factors, and general health.

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1. What is Tofacitinib 11 mg (Xeljanz XR) used for?
Tofacitinib 11 mg is used to treat autoimmune diseases like:
Rheumatoid arthritis (RA)
Psoriatic arthritis (PsA)
Ulcerative colitis (UC)
Ankylosing spondylitis (AS)
It helps reduce inflammation and slow disease progression.

2. How does Tofacitinib work?
Tofacitinib is a Janus kinase (JAK) inhibitor. It blocks specific enzymes (JAK1 and JAK3) involved in the immune system’s inflammatory response, thereby reducing symptoms and tissue damage.

3. What distinguishes Tofacitinib 11 mg from different dosages?
Tofacitinib 11 mg is used once daily as an extended-release (XR) tablet. Other types are used twice a day, such as immediate-release pills containing 5 mg. The same daily dosage is convenient with the XR formulation.

4. How should I take 11 mg of tofacitinib?
One 11 mg tablet should be taken once daily, ideally at the same time every day. Do not chew, split, or crush; swallow whole. Taking it with or without food is possible.

5. What should I do if I forget to take a dose?
When you remember to take the missed dose, do so. Skip the missed dose and resume your regular schedule if the next one is coming up. To make up for a missed dose, never take two at once.