Tofacitinib citrate
Name: Tofacitinib citrate
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Do I need a prescription for Tofacitinib citrate (Xeljanz)?
Yes
What are the side effects of Tofacitinib citrate (Xeljanz)?
Side effects of tofacitinib are:
- increased cholesterol levels (for example, HDL and LDL levels),
- headache,
- diarrhea,
- sore throat,
- runny nose,
- urinary tract infection,
- nasopharyngitis, and
- upper respiratory infections.
Tofacitinib carries a boxed warning of risk of developing infections that may lead to hospitalization or death.
Patients must be carefully monitored for the development of signs and symptoms of infection before and during the treatment of tofacitinib.
What is the dosage for Tofacitinib citrate (Xeljanz)?
The recommended dose in adults is: One tablet (5 mg) by mouth twice daily with or without food.
Safe and effective use of tofacitinib is not established in pediatric patients.
Which drugs or supplements interact with Tofacitinib citrate (Xeljanz)?
Ketoconazole (Nizoral, Extina, Xolegel, Kuric) and fluconazole (Diflucan) slow down the metabolism (elimination) of tofacitinib, increasing tofacitinib levels in the body.
Rifampin accelerates tofacitinib metabolism, which can reduce the beneficial effects of tofacitinib.
Combining tofacitinib with other medications like azathioprine (Imuran, Azasan), cyclosporine, tacrolimus (Prograf), or oral steroids may cause further suppression of the immune system.
Interactions for Tofacitinib Citrate
Metabolized mainly by CYP3A4, with minor contribution from CYP2C19.1 Does not substantially inhibit or induce CYP isoenzymes 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, or 3A4 in vitro.1 10
Does not appear to normalize CYP enzyme activity over time in patients with rheumatoid arthritis.1
Unlikely to inhibit P-glycoprotein or organic anionic or cationic transport proteins at clinically relevant concentrations.1
Drugs Affecting Hepatic Microsomal Enzymes
Potent CYP3A4 inhibitors: Pharmacokinetic interaction (increased tofacitinib concentrations).1 Reduce tofacitinib dosage to 5 mg once daily.1
Drugs (or drug combinations) that result in both moderate CYP3A4 inhibition and potent CYP2C19 inhibition: Pharmacokinetic interaction (increased tofacitinib concentrations).1 Reduce tofacitinib dosage to 5 mg once daily.1
Drugs that inhibit only CYP2C19: Pharmacokinetic interaction unlikely.1
Potent CYP3A4 inducers: Pharmacokinetic interaction (decreased tofacitinib concentrations); possible decreased tofacitinib efficacy.1
Drugs Metabolized by Hepatic Microsomal Enzymes
Pharmacokinetic interaction unlikely.1 13
Drugs Affecting P-Glycoprotein Transport
P-glycoprotein inhibitors: Pharmacokinetic interaction unlikely.1
Biologic Antirheumatic Agents
Concomitant use with biologic DMARDS not recommended.1
Immunosuppressive Agents
Pharmacologic interaction (increased risk of immunosuppression).1 Concomitant use with potent immunosuppressive agents not recommended.1
Vaccines
Avoid live vaccines.1
No data available on response to vaccination.1 (See Immunizations under Cautions.)
No data available on secondary transmission of infection from individuals receiving live vaccines to tofacitinib-treated patients.1
Specific Drugs
Drug | Interaction | Comments |
---|---|---|
Azathioprine | Increased risk of immunosuppression1 | Concomitant use in rheumatoid arthritis not studied to date1 Concomitant use not recommended1 |
Cyclosporine | Increased risk of immunosuppression1 Decreased clearance and increased AUC of cyclosporine1 13 | Concomitant use in rheumatoid arthritis not studied to date1 Concomitant use not recommended1 |
Fluconazole | Increased tofacitinib concentrations1 13 | Reduce tofacitinib dosage to 5 mg once daily1 |
Ketoconazole | Increased tofacitinib concentrations1 13 | Reduce tofacitinib dosage to 5 mg once daily1 |
Metformin | No substantial effect on tofacitinib concentrations1 | No dosage adjustment required1 |
Methotrexate | No clinically important effect on pharmacokinetics of either drug1 9 | No dosage adjustment required1 9 |
Midazolam | No substantial effect on midazolam pharmacokinetics1 10 | No dosage adjustment required1 |
Oral contraceptives | No substantial effect on ethinyl estradiol or levonorgestrel concentrations1 13 | No dosage adjustment required1 |
Rifampin | Decreased tofacitinib concentrations1 13 | May reduce tofacitinib efficacy1 |
Tacrolimus | Increased risk of immunosuppression1 Slight decrease in clearance and increase in AUC of tacrolimus1 13 | Concomitant use in rheumatoid arthritis not studied to date1 Concomitant use not recommended1 |
Stability
Storage
Oral
Tablets20–25°C.1 Store in original container; do not repackage.1