XELJANZ*
Manufacturer DetailsGENERIC*
USA AND CANADA
Compositions:
Tofacitinib- mg,
Tofacitinib- mg,
| Strength | Rate | Packing Style |
|---|---|---|
| mg | 0.00 | unit |
List of Related Indications:
- To treat adults with moderately severely active rheumatoid arthiritis (RA) who have had inadequate response to, or who are intolerant to methotrexate
List Of Drugs:
- Tofacitinib- Xeljanz- @- (Nov 2012)- Anti-rheumatic agent
Indication Type Description:
Drug Interaction
Indication
Adverse Reaction
Contra-Indications
Dosages/ Overdosage Etc
Patient Information
Pharmacology/ Pharmacokinetics
Pregnancy and lactation
Drug Interaction:
Potent inhibitors of Cytochrome P450 3A4 (CYP3A4) (e.g.,ketoconazole):
Reduce dose to 5 mg once daily.
One or more concomitant medications that result in both moderate
inhibition of CYP3A4 and potent inhibition of CYP2C19 (e.g.,fluconazole):
Reduce dose to 5 mg once daily.
Potent CYP inducers (e.g., rifampin): May result in loss of or reduced
clinical response.
Indication:
XELJANZ (tofacitinib) tablets, for oral use
Initial U.S. Approval: 2012
WARNING: SERIOUS INFECTIONS AND MALIGNANCY
See full prescribing information for complete boxed warning.
Serious infections leading to hospitalization or death, including tuberculosis
and bacterial, invasive fungal, viral, and other opportunistic infections,
have occurred in patients receiving XELJANZ.
If a serious infection develops, interrupt XELJANZ until the infection
is controlled.
Prior to starting XELJANZ, perform a test for latent tuberculosis; if it is positive,
start treatment for tuberculosis prior to starting XELJANZ.
Monitor all patients for active tuberculosis during treatment, even if the initial
latent tuberculosis test is negative.
Lymphoma and other malignancies have been observed in patients treated
with XELJANZ. Epstein Barr Virus-associated post-transplant lymphoproliferative
disorder has been observed at an increased rate in renal transplant patients
treated with XELJANZ and concomitant immunosuppressive medications.
RECENT MAJOR CHANGES
Indications and Usage (1) 02/2014
Dosage and Administration (2) 02/2014
Warnings and Precautions, Serious Infections (5.1) 06/2015
Warnings and Precautions, Malignancy and Lymphoproliferative
Disorders (5.2) 03/2014
Warnings and Precautions, Laboratory Abnormalities (5.4) 02/2014
Warnings and Precautions, Vaccinations (5.5) 02/2014
Drug Name- Xeljanz*
Active Ingredient - Tofacitinib
To treat adults with moderetely to severely active rheumatic arthoritis (RA)
who have had an inadequate response to, or who are intolerant of,
methotrexate
Indication-
To treat adults with moderetely to severely active rheumatic arthoritis (RA)
who have had an inadequate response to ,or who are intolerant of,
methotrexate
Approved by FDA on 6-11--2012 (Ref- FDA approved List- 2012)
LIST OF NEW DRUG APPROVED FROM 01-01-2016 To TILL DATE
BY NEW DRUG DIVISION - DRUG CONTROLLER GENERAL- INDIA
Sr.No Name of Drug Indication Date of Issue
4. Tofacitainib Tablets 5mg 01-04-2016
100/150mg
For the treatment of adult patients with moderately
to severe active rheumatoid arthritis who have had
an iadequate response or intolerance to Methotrexate.
It may be used as monotherapy or in combination
with Methotexate or other nonbiologic disease-
modifying antirheumatic drugs( DMARDs)
Approved by DCG INDIA (Ref- DCGI approved List- 01-01-2016 To Till Date)
Adverse Reaction:
The most commonly reported adverse reactions during the first 3 months in
controlled clinical trials (occurring in greater than or equal to 2% of patients
treated with XELJANZ monotherapy or in combination with DMARDs) were
upper respiratory tract infections, headache, diarrhea and nasopharyngitis.
Contra-Indications:
CONTRAINDICATIONS
None
WARNINGS AND PRECAUTIONS
Avoid use of XELJANZ during an active serious infection, including
localized infections.
Gastrointestinal Perforations- Use with caution in patients that may
be at increased risk.
Laboratory Monitoring-Recommended due to potential changes in lymphocytes,
neutrophils, hemoglobin, liver enzymes and lipids.
Immunizations ¡V Live vaccines: Avoid use with XELJANZ.
Dosages/ Overdosage Etc:
Indication-
To treat adults with moderetely to severely active rheumatic arthoritis (RA)
who have had an inadequate response to ,or who are intolerant of,
methotrexate
Approved by FDA on 6-11--2012 (Ref- FDA approved List- 2012)
INDICATIONS AND USAGE
XELJANZ is an inhibitor of Janus kinases (JAKs) indicated for the treatment
of adult patients with moderately to severely active rheumatoid arthritis
who have had an inadequate response or intolerance to methotrexate.
It may be used as monotherapy or in combination with methotrexate
or other nonbiologic disease-modifying antirheumatic drugs (DMARDs).
Limitations of Use: Use of XELJANZ in combination with biologic
DMARDs or potent immunosuppressants such as azathioprine and
cyclosporine is not recommended.
DOSAGE AND ADMINISTRATION
Rheumatoid Arthritis
Recommended dose of XELJANZ is 5 mg twice daily.
Moderate and severe renal impairment and moderate hepatic impairment:
Reduce dose to 5 mg once daily.
DOSAGE FORMS AND STRENGTHS
Tablets: 5 mg
Patient Information:
PATIENT COUNSELING INFORMATION
See FDA-approved patient labeling (Medication Guide).
Advise the patient to read the FDA-approved patient labeling (Medication Guide).
Patient Counseling
Advise patients of the potential benefits and risks of XELJANZ.
Serious Infection
Inform patients that XELJANZ may lower the ability of their immune system
to fight infections. Advise patients not to start taking XELJANZ if they
have an active infection.
Instruct patients to contact their healthcare provider immediately during treatment
if symptoms suggesting infection appear in order to ensure rapid evaluation and
appropriate treatment
Advise patients that the risk of herpes zoster, some cases of which can be serious,
is increased in patients treated with XELJANZ
Malignancies and Lymphoproliferative Disorders
Inform patients that XELJANZ may increase their risk of certain cancers,
and that lymphoma and other cancers have been observed in patients
taking XELJANZ.
Instruct patients to inform their healthcare provider if they have ever had
any type of cancer
Important Information on Laboratory Abnormalities
Inform patients that XELJANZ may affect certain lab test results, and that
blood tests are required before and during XELJANZ treatment
Pregnancy
Inform patients that XELJANZ should not be used during pregnancy unless
clearly necessary, and advise patients to inform their doctors right away
if they become pregnant while taking XELJANZ. Inform patients that
Pfizer has a registry for pregnant women who have taken XELJANZ
during pregnancy. Advise patients to contact the registry at
1-877-311-8972 to enroll
Pharmacology/ Pharmacokinetics:
CLINICAL PHARMACOLOGY
1. Mechanism of Action
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.
2. Pharmacokinetics
Following oral administration of XELJANZ, peak plasma concentrations are
reached within 0.5-1 hour, elimination half-life is ~3 hours and a dose-proportional
increase in systemic exposure was observed in the therapeutic dose range.
Steady state concentrations are achieved in 24-48 hours with negligible
accumulation after twice daily administration.
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
1. Pregnancy
Pregnancy Category C. There are no adequate and well-controlled studies in pregnant
women. XELJANZ should be used during pregnancy only if the potential benefit
justifies the potential risk to the fetus.
2. Nursing Mothers
Tofacitinib was secreted in milk of lactating rats. It is not known whether tofacitinib
is excreted in human milk. Because many drugs are excreted in human milk and
because of the potential for serious adverse reactions in nursing infants from
tofacitinib, a decision should be made whether to discontinue nursing or to
discontinue the drug, taking into account the importance of the drug for the mother.
3. Pediatric Use
The safety and effectiveness of XELJANZ in pediatric patients have not been established.
4. Geriatric Use
Of the 3315 patients who enrolled in Studies I to V, a total of 505 rheumatoid arthritis
patients were 65 years of age and older, including 71 patients 75 years and older.
The frequency of serious infection among XELJANZ-treated subjects 65 years
of age and older was higher than among those under the age of 65.
As there is a higher incidence of infections in the elderly population in general,
caution should be used when treating the elderly.
