Tofacitinib citrate

Name: Tofacitinib citrate

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

Tablets

20–25°C.1 Store in original container; do not repackage.1

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