tofacitinib citrate at a glance
Medicine class
Targeted synthetic disease-modifying treatment; Janus kinase inhibitor.
Licensed conditions
Includes rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, ulcerative colitis and specified forms of juvenile idiopathic arthritis.
Food
May be taken with or without food.
Infection precautions
Screening, vaccination review and ongoing monitoring are needed because treatment can increase infection risk.
What is tofacitinib citrate used for?
Selected UK products are licensed for:
Moderate to severe active rheumatoid arthritis in adults after an inadequate response or intolerance to disease-modifying treatment; usually with methotrexate, or alone when methotrexate is unsuitable.
Active psoriatic arthritis in adults after an inadequate response or intolerance to previous disease-modifying treatment, with methotrexate.
Active ankylosing spondylitis in adults after an inadequate response to conventional treatment.
Moderately to severely active ulcerative colitis in adults after an inadequate response, loss of response or intolerance to conventional or biological treatment.
Active polyarticular juvenile idiopathic arthritis and juvenile psoriatic arthritis in children aged 2 years and older after an inadequate response to previous disease-modifying treatment.
How does tofacitinib citrate work?
Tofacitinib enters cells and inhibits JAK enzymes, particularly pathways involving JAK1 and JAK3. This reduces the action of several cytokines that drive immune activation and inflammation.
tofacitinib citrate preparations and strengths
Modified-release tablet
Route: Oral
Strengths: 11 mg
Oral solution
Route: Oral
Strengths: 1 mg/mL
Tablet
Route: Oral
Strengths: 5 mg, 10 mg
How to take tofacitinib citrate
Take the prescribed formulation exactly as directed by the specialist. It may be taken with or without food.
Film-coated tablets may be crushed and taken with water if swallowing is difficult.
Prolonged-release tablets must be swallowed whole.
Measure oral solution using the supplied bottle adapter and oral syringe.
Keep oral solution in its original bottle and packaging, protected from light, and discard it 60 days after first opening.
tofacitinib citrate side effects
Common or expected effects
- Upper respiratory tract or viral infections
- Headache
- Diarrhoea or nausea
- Raised blood pressure
- Abdominal discomfort
- Rash or acne
- Raised blood cholesterol or liver enzymes
Get urgent medical advice
- Serious or opportunistic infection, including tuberculosis, pneumonia or shingles
- Blood clot in a leg or lung
- Heart attack or stroke symptoms
- Severe allergic reaction
- New severe abdominal pain, which may indicate gastrointestinal perforation
- Possible malignancy, including lymphoma, lung cancer or non-melanoma skin cancer
tofacitinib citrate in pregnancy
Tofacitinib is contraindicated during pregnancy. People who could become pregnant should use effective contraception during treatment and for at least 4 weeks afterwards. Discuss pregnancy plans or suspected pregnancy promptly with the specialist prescriber.
tofacitinib citrate while breastfeeding
Tofacitinib passes into human milk, and its effects on a breastfed child remain uncertain. UK product information contraindicates its use during breastfeeding, so discuss feeding and treatment options with the specialist.
tofacitinib citrate interactions
Check all prescribed, over-the-counter and herbal products with the specialist or pharmacist. Important interactions include:
Potent CYP3A4 inhibitors, such as ketoconazole
They increase tofacitinib exposure, so the prescription may require adjustment.
Fluconazole and similar combined CYP3A4/CYP2C19 inhibitors
They can increase tofacitinib exposure and may require prescription adjustment.
Potent CYP3A4 inducers, such as rifampicin
They can reduce tofacitinib exposure and clinical response; combined use is not recommended.
Common questions about tofacitinib citrate
Answers are fully visible for fast scanning and source review.
Is tofacitinib citrate an immunosuppressant?
It reduces selected immune-signalling pathways and can increase susceptibility to infections, including serious and opportunistic infections.
Can tofacitinib citrate tablets be crushed?
Film-coated tablets may be crushed and taken with water. Prolonged-release tablets must be swallowed whole.
Why are blood tests needed?
Treatment can lower lymphocytes, neutrophils or haemoglobin and alter liver enzymes and blood lipids, so laboratory monitoring supports safe prescribing.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.