Classes
DEA Class; Rx
Common Brand Names; Aubagio
- Multiple Sclerosis Treatments;
- Pyrimidine Synthesis Inhibitors
Description
Oral pyrimidine synthesis inhibitor; an active metabolite of leflunomide
Used in adults with relapsing forms of multiple sclerosis, including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease
Boxed warnings regarding risk for hepatotoxicity and for teratogenicity
Indications
Indicated for the treatment of relapsing forms of multiple sclerosis (MS), including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease.
Contraindications
History of hypersensitivity reaction to teriflunomide, leflunomide, or excipients
Severe hepatic impairment
Pregnancy
Current leflunomide treatment
Adverse Effects
- Headache (19-22%)
- Diarrhea (15-18%)
- Increased ALT (12-14%)
- Alopecia (10-13%)
- Influenza (9-12%)
- Nausea (9-14%)
- Paresthesia (9-10%)
- Phosphatemia (5-18%)
- URTI (9%)
- Bronchitis (5-8%)
- Upper abdominal pain (5-6%)
- Sinusitis (4-6%)
- Musculoskeletal pain (4-5%)
- Hypertension (4%)
- Toothache (4%)
- Increased GGT (3-5%)
- Anxiety (3-4%)
- Myalgia (3-4%)
- Pruritus (3-4%)
- Blurred vision (3%)
- Cystitis (2-4%)
- Viral gastroenteritis (2-4%)
- Oral herpes (2-4%)
- Neutropenia (2-4%)
- Increased AST (2-3%)
- Seasonal allergy (2-3%)
- Burning sensation (2-3%)
- Palpitations (2-3%)
- Decreased weight (2-3%)
- Decreased neutrophil count (2-3%)
- Sciatica (1-3%)
- Conjunctivitis (1-3%)
- Increased WBC (1-3%)
- Acne (1-3%)
- Carpal tunnel syndrome (1-3%)
- Leukopenia (1-2%)
- Abdominal distention (1-2%)
- Cardiovascular death (0.25%)
- Hypersensitivity reactions
Warnings
Risk of malignancy, particularly lymphoproliferative disorders, is increased with use of some immunosuppressive medications; there is potential for immunosuppression with this drug; no apparent increase in the incidence of malignancies and lymphoproliferative disorders reported in clinical trials, but larger and longer-term studies would be needed to determine whether there is an increased risk of malignancy or lymphoproliferative disorders with therapy
No clinical data available on efficacy and safety of live vaccinations in patients receiving therapy; vaccination with live vaccines is not recommended; the long half-life of the drug should be considered when contemplating administration of a live vaccine after stopping therapy
May take an average of 8 months to clear drug from plasma; consider accelerated elimination with cholestyramine or activated charcoal
Decreases in white blood cell count and platelet count have been observed; a recent CBC should be available before starting teriflunomide; monitor for signs and symptoms of infection; consider suspending treatment with teriflunomide in case of serious infection; do not start teriflunomide in patients with active infections
Pregnancy and Lactation
Contraindicated for use in pregnant women and females of reproductive potential not using effective contraception because of potential for fetal harm based on animal data
Not known whether drug is excreted in human milk; detected in rat milk following a single oral dose; because of potential for adverse reactions in a breastfed infant from therapy, women should not breastfeed during treatment
Maximum Dosage
14 mg/day PO.
14 mg/day PO.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
Safety and efficacy have not been established.
How supplied
Teriflunomide
tablet
- 7mg
- 14mg
