tofacitinib citrate: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
tofacitinib citrate: clinical details
Prescribing considerations
- Initiation and supervision should be by a specialist experienced in the licensed condition.
- Use only when no suitable alternative is available in people aged 65 years or older, current or long-term former smokers, and those with cardiovascular or malignancy risk factors.
- Assess infection, tuberculosis, cardiovascular, malignancy and venous-thromboembolism risks before treatment and periodically thereafter.
- Review immunisation status before treatment and avoid concurrent live vaccines.
- Consider renal and hepatic function and interacting CYP inhibitors or inducers.
Contraindications and cautions
- Hypersensitivity to tofacitinib or formulation excipients
- Active tuberculosis, serious infection such as sepsis, or opportunistic infection
- Severe hepatic impairment
- Pregnancy
- Breastfeeding
Monitoring
- Full blood count, including lymphocytes, neutrophils and haemoglobin, before and during treatment
- Liver function tests
- Lipid profile after treatment begins
- Clinical surveillance for infection, tuberculosis, shingles, thrombosis, cardiovascular events and malignancy
- Periodic skin examination, particularly where skin-cancer risk is increased
Clinical pharmacology
An oral small-molecule JAK inhibitor that modulates cytokine signalling. It is metabolised mainly through CYP3A4, with a smaller CYP2C19 contribution; prolonged-release tablets produce later peak concentrations than film-coated tablets.
Formulation and product differences
- Film-coated tablets can be taken with or without food and may be crushed in water when necessary.
- Prolonged-release tablets must be taken whole and are not licensed for children.
- The oral solution is intended for paediatric administration using the supplied adapter and oral syringe and contains propylene glycol and sodium benzoate.
- The prolonged-release formulation contains sorbitol; the selected film-coated tablet contains lactose.
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
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.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.