Tofacitinib citrate (Xeljanz)

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GENERIC NAME: Tofacitinib citrate


DRUG CLASS AND MECHANISM: Tofacitinib is an oral drug used for treating rheumatoid arthritis. It belongs to a class of drugs called Janus kinase (JAK) inhibitors. JAKs are enzymes (proteins) that regulate chemical signaling pathways that control biologic processes such as blood formation and the immune response response that causes the pain, tenderness and swelling of inflammation. JAKs are found in many cells, especially stem cells in bones and joints. Inhibition of JAKs by tofacitinib prevents inflammation and tissue destruction that is associated with the inflammation of rheumatoid arthritis. Tofacitinib was approved in November 2012.



PREPARATIONS: Tofacitinib is available as film-coated, immediate-release, 5 mg tablets.

STORAGE: Tofacitinib should be stored at room temperature between 20 C to 25 C (68 F to 77 F).

PRESCRIBED FOR: Tofacitinib is used for moderate-to-severely active rheumatoid arthritis in adults who have had an insufficient response or cannot tolerate methotrexate (Rheumatrex, Trexall).

Tofacitinib may be used by itself or in combination with methotrexate or other non-biologic disease-modifying anti-rheumatic drugs (DMARDs).

DOSING: 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.

DRUG INTERACTIONS: 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.

PREGNANCY: There are no adequate studies of tofacitinib to determine safe and effective use in pregnant women.

NURSING MOTHERS: It is not known whether tofacitinib enters breast milk; therefore, it is best to be cautious before using it in nursing mothers.

SIDE EFFECTS: Side effects of tofacitinib are increased cholesterol levels (for example, HDL and LDL levels), headache, diarrhea, sore throat, runny nose, and infections such as 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.

REFERENCE: Xeljanz Prescribing Information.

Medically Reviewed by a Doctor on 5/15/2014

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