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XELJANZ

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Overview

What is XELJANZ?

XELJANZ/XELJANZ XR are formulated with the citrate salt of tofacitinib, a JAK inhibitor.

Tofacitinib citrate is a white to off-white powder with the following chemical name: (3R,4R)-4-methyl-3-(methyl-7H-pyrrolo [2,3-d]pyrimidin-4-ylamino)-ß-oxo-1-piperidinepropanenitrile, 2-hydroxy-1,2,3-propanetricarboxylate (1:1).

The solubility of tofacitinib citrate in water is 2.9 mg/mL.

Tofacitinib citrate has a molecular weight of 504.5 Daltons (or 312.4 Daltons as the tofacitinib free base) and a molecular formula of CHNO∙CHO. The chemical structure of tofacitinib citrate is:

XELJANZ is supplied for oral administration as 5 mg tofacitinib (equivalent to 8 mg tofacitinib citrate) white round, immediate-release film-coated tablet. Each tablet of XELJANZ contains the appropriate amount of tofacitinib as a citrate salt and the following inactive ingredients: microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate, HPMC 2910/Hypromellose 6cP, titanium dioxide, macrogol/PEG3350, and triacetin.

XELJANZ XR is supplied for oral administration as 11 mg tofacitinib (equivalent to 17.77 mg tofacitinib citrate) pink, oval, extended release film-coated tablet with a drilled hole at one end of the tablet band. Each tablet of XELJANZ XR contains the appropriate amount of tofacitinib as a citrate salt and the following inactive ingredients: sorbitol, hydroxyethyl cellulose, copovidone, magnesium stearate, cellulose acetate, hydroxypropyl cellulose, HPMC 2910/Hypromellose, titanium dioxide, triacetin, and red iron oxide. Printing ink contains shellac glaze, ammonium hydroxide, propylene glycol, and ferrosoferric oxide/black iron oxide.



What does XELJANZ look like?



What are the available doses of XELJANZ?

XELJANZ Tablets: 5 mg ()

XELJANZ XR Tablets: 11 mg ()

What should I talk to my health care provider before I take XELJANZ?

All information provided in this section is applicable to XELJANZ and XELJANZ XR as they contain the same active ingredient (tofacitinib).

How should I use XELJANZ?

Switching from XELJANZ Tablets to XELJANZ XR Tablets

Patients treated with XELJANZ 5 mg twice daily may be switched to XELJANZ XR 11 mg once daily the day following the last dose of XELJANZ 5 mg.


What interacts with XELJANZ?

Sorry No Records found


What are the warnings of XELJANZ?

Sorry No Records found


What are the precautions of XELJANZ?

Sorry No Records found


What are the side effects of XELJANZ?

Sorry No records found


What should I look out for while using XELJANZ?

None


What might happen if I take too much XELJANZ?


How should I store and handle XELJANZ?

Storage and HandlingStore XELJANZ/XELJANZ XR at 20°C to 25°C (68°F to 77°F). [See USP Controlled Room Temperature].Storage and HandlingStore XELJANZ/XELJANZ XR at 20°C to 25°C (68°F to 77°F). [See USP Controlled Room Temperature].XELJANZ is provided as 5 mg tofacitinib (equivalent to 8 mg tofacitinib citrate) tablets: White, round, immediate-release film-coated tablets, debossed with "Pfizer" on one side, and "JKI 5" on the other side, and available in:XELJANZXELJANZ XR is provided as 11 mg tofacitinib (equivalent to 17.77 mg tofacitinib citrate) tablets: Pink, oval, extended release tablet with a drilled hole at one end of the tablet band and "JKI 11" printed on one side of the tablet:XELJANZ XRXELJANZ is provided as 5 mg tofacitinib (equivalent to 8 mg tofacitinib citrate) tablets: White, round, immediate-release film-coated tablets, debossed with "Pfizer" on one side, and "JKI 5" on the other side, and available in:XELJANZXELJANZ XR is provided as 11 mg tofacitinib (equivalent to 17.77 mg tofacitinib citrate) tablets: Pink, oval, extended release tablet with a drilled hole at one end of the tablet band and "JKI 11" printed on one side of the tablet:XELJANZ XRXELJANZ is provided as 5 mg tofacitinib (equivalent to 8 mg tofacitinib citrate) tablets: White, round, immediate-release film-coated tablets, debossed with "Pfizer" on one side, and "JKI 5" on the other side, and available in:XELJANZXELJANZ XR is provided as 11 mg tofacitinib (equivalent to 17.77 mg tofacitinib citrate) tablets: Pink, oval, extended release tablet with a drilled hole at one end of the tablet band and "JKI 11" printed on one side of the tablet:XELJANZ XRXELJANZ is provided as 5 mg tofacitinib (equivalent to 8 mg tofacitinib citrate) tablets: White, round, immediate-release film-coated tablets, debossed with "Pfizer" on one side, and "JKI 5" on the other side, and available in:XELJANZXELJANZ XR is provided as 11 mg tofacitinib (equivalent to 17.77 mg tofacitinib citrate) tablets: Pink, oval, extended release tablet with a drilled hole at one end of the tablet band and "JKI 11" printed on one side of the tablet:XELJANZ XR


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Clinical Information

Chemical Structure

No Image found
Clinical Pharmacology

Tofacitinib is a Janus kinase (JAK) inhibitor. JAKs are intracellular enzymes which transmit signals arising from cytokine or growth factor-receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function. Within the signaling pathway, JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs) which modulate intracellular activity including gene expression. Tofacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs. JAK enzymes transmit cytokine signaling through pairing of JAKs (e.g., JAK1/JAK3, JAK1/JAK2, JAK1/TyK2, JAK2/JAK2). Tofacitinib inhibited the activities of JAK1/JAK2, JAK1/JAK3, and JAK2/JAK2 combinations with IC of 406, 56, and 1377 nM, respectively. However, the relevance of specific JAK combinations to therapeutic effectiveness is not known.

Non-Clinical Toxicology
None

Aminoglutethimide:

Amphotericin B injection and potassium-depleting agents:

Antibiotics:

Anticholinesterases:

Anticoagulants, oral:

Antidiabetics:

Antitubercular drugs:

Cholestyramine:

Cyclosporine:

Digitalis glycosides:

Estrogens, including oral contraceptives:

Hepatic enzyme inducers (eg, barbiturates, phenytoin, carbamazepine, rifampin):

Ketoconazole:

Nonsteroidal anti-inflammatory drugs (NSAIDs):

Skin tests:





Serious and sometimes fatal infections due to bacterial, mycobacterial, invasive fungal, viral, or other opportunistic pathogens have been reported in patients receiving XELJANZ. The most common serious infections reported with XELJANZ included pneumonia, cellulitis, herpes zoster, urinary tract infection, diverticulitis, and appendicitis. Among opportunistic infections, tuberculosis and other mycobacterial infections, cryptococcosis, histoplasmosis, esophageal candidiasis, pneumocystosis, multidermatomal herpes zoster, cytomegalovirus infections, BK virus infection, and listeriosis were reported with XELJANZ. Some patients have presented with disseminated rather than localized disease, and were often taking concomitant immunomodulating agents such as methotrexate or corticosteroids.

Other serious infections that were not reported in clinical studies may also occur (e.g., coccidioidomycosis).

Avoid use of XELJANZ/XELJANZ XR in patients with an active, serious infection, including localized infections. The risks and benefits of treatment should be considered prior to initiating XELJANZ/XELJANZ XR in patients:

Patients should be closely monitored for the development of signs and symptoms of infection during and after treatment with XELJANZ/XELJANZ XR. XELJANZ/XELJANZ XR should be interrupted if a patient develops a serious infection, an opportunistic infection, or sepsis. A patient who develops a new infection during treatment with XELJANZ/XELJANZ XR should undergo prompt and complete diagnostic testing appropriate for an immunocompromised patient; appropriate antimicrobial therapy should be initiated, and the patient should be closely monitored.

Caution is also recommended in patients with a history of chronic lung disease, or in those who develop interstitial lung disease, as they may be more prone to infections.

Risk of infection may be higher with increasing degrees of lymphopenia and consideration should be given to lymphocyte counts when assessing individual patient risk of infection. Discontinuation and monitoring criteria for lymphopenia are discussed in Dosage Modifications due to Serious Infections and Cytopenias

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Professional

Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72
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Tips

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Interactions

Interactions

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