What is Aubagio (teriflunomide)?
Aubagio (teriflunomide) is a pyrimidine synthesis inhibitor used to treat relapsing forms of multiple sclerosis (MS). Aubagio can decrease the number of MS flare-ups (relapses). Aubagio does not cure MS, but it can help slow down the physical problems that MS causes.
Common side effects of Aubagio include:
- liver problems,
- hair loss or thinning hair,
- burning or prickly feeling in the skin, and
- numbness or tingling in the hands or feet that is different from MS symptoms.
Serious side effects of Aubagio include:
- body aches,
- flu symptoms,
- sores in the mouth and throat,
- tired feeling,
- loss of appetite,
- dark urine,
- clay-colored stools,
- yellowing of the skin or eyes,
- fast or racing heartbeats,
- little or no urinating,
- chest pain,
- dry cough,
- feeling short of breath,
- skin redness or peeling,
- rapid weight gain, and
- severe skin reactions (fever, sore throat, swelling in the face or tongue)
- burning in the eyes,
- skin pain, followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.
Coadministration of Aubagio with warfarin requires close monitoring of the international normalized ratio (INR).
Aubagio may increase the systemic exposures of oral contraceptives.
When taking Aubagio, the dose of rosuvastatin should not exceed 10 mg once daily.
For other substrates of BCRP (e.g., mitoxantrone) and drugs in the OATP family (e.g., methotrexate, rifampin), especially HMG-Co reductase inhibitors, patients should be monitored closely for signs and symptoms of increased exposures to those drugs.
Aubagio is contraindicated for use in pregnant women and females of reproductive potential not using effective contraception because it may harm a fetus. There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to Aubagio during pregnancy.
It is unknown if Aubagio is excreted in human milk. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for Aubagio and any potential adverse effects on the breastfed infant from Aubagio or from the underlying maternal condition.
What are the important side effects of Aubagio (teriflunomide)?
The most common side effects associated with teriflunomide treatment are:
- alopecia (hair thinning or loss),
- paresthesia (tingling, burning, prickling or pricking sensations of the skin),
- and increase in liver enzymes.
Serious liver injury, kidney problems, decrease in white blood cell counts, risk for serious infections such as:
Aubagio (teriflunomide) side effects list for healthcare professionals
The following serious adverse reactions are described elsewhere in the prescribing information:
- Bone Marrow Effects/Immunosuppression Potential/Infections
- Hypersensitivity and Serious Skin Reactions
- Peripheral Neuropathy
- Increased Blood Pressure
- Respiratory Effects
Clinical Trials Experience
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
A total of 2047 patients receiving Aubagio (7 mg or 14 mg once daily) constituted the safety population in the pooled analysis of placebo controlled studies in patients with relapsing forms of multiple sclerosis; of these, 71% were female. The average age was 37 years.
Table 1 lists adverse reactions in placebo-controlled trials with rates that were at least 2% for Aubagio patients and also at least 2% above the rate in placebo patients. The most common were headache, an increase in ALT, diarrhea, alopecia, and nausea. The adverse reaction most commonly associated with discontinuation was an increase in ALT (3.3%, 2.6%, and 2.3% of all patients in the Aubagio 7 mg, Aubagio 14 mg, and placebo treatment arms, respectively).
Table 1: Adverse Reactions in Pooled Placebo-Controlled Studies in Patients with Relapsing Forms of Multiple Sclerosis
|Increase in Alanine aminotransferase||13%||15%||9%|
Four cardiovascular deaths, including three sudden deaths, and one myocardial infarction in a patient with a history of hyperlipidemia and hypertension were reported among approximately 2600 patients exposed to Aubagio in the premarketing database. These cardiovascular deaths occurred during uncontrolled extension studies, one to nine years after initiation of treatment. A relationship between Aubagio and cardiovascular death has not been established.
Acute Renal Failure
In placebo-controlled studies, creatinine values increased more than 100% over baseline in 8/1045 (0.8%) patients in the 7 mg Aubagio group and 6/1002 (0.6%) patients in the 14 mg Aubagio group versus 4/997 (0.4%) patients in the placebo group. These elevations were transient. Some elevations were accompanied by hyperkalemia. Aubagio may cause acute uric acid nephropathy with transient acute renal failure because Aubagio increases renal uric acid clearance.
In clinical trials, 18% of Aubagio-treated patients had hypophosphatemia with serum phosphorus levels of at least 0.6 mmol/L, compared to 7% of placebo-treated patients; 4% of Aubagio-treated patients had hypophosphatemia with serum phosphorus levels at least 0.3 mmol/L but less than 0.6 mmol/L, compared to 0.8% of placebo-treated patients. No patient in any treatment group had a serum phosphorus below 0.3 mmol/L.
The following adverse reactions have been identified during postapproval use of Aubagio. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
What drugs interact with Aubagio (teriflunomide)?
Effect Of Aubagio On CYP2C8 Substrates
Teriflunomide is an inhibitor of CYP2C8 in vivo. In patients taking Aubagio, exposure of drugs metabolized by CYP2C8 (e.g., paclitaxel, pioglitazone, repaglinide, rosiglitazone) may be increased. Monitor these patients and adjust the dose of the concomitant drug(s) metabolized by CYP2C8 as required.
Effect Of Aubagio On Warfarin
Coadministration of Aubagio with warfarin requires close monitoring of the international normalized ratio (INR) because Aubagio may decrease peak INR by approximately 25%.
Effect Of Aubagio On Oral Contraceptives
Aubagio may increase the systemic exposures of ethinylestradiol and levonorgestrel. Consideration should be given to the type or dose of contraceptives used in combination with Aubagio.
Effect Of Aubagio On CYP1A2 Substrates
Teriflunomide may be a weak inducer of CYP1A2 in vivo. In patients taking Aubagio, exposure of drugs metabolized by CYP1A2 (e.g., alosetron, duloxetine, theophylline, tizanidine) may be reduced. Monitor these patients and adjust the dose of the concomitant drug(s) metabolized by CYP1A2 as required.
Effect Of Aubagio On Organic Anion Transporter 3 (OAT3) Substrates
Teriflunomide inhibits the activity of OAT3 in vivo. In patients taking Aubagio, exposure of drugs which are OAT3 substrates (e.g., cefaclor, cimetidine, ciprofloxacin, penicillin G, ketoprofen, furosemide, methotrexate, zidovudine) may be increased. Monitor these patients and adjust the dose of the concomitant drug(s) which are OAT3 substrates as required.
Effect Of Aubagio On BCRP And Organic Anion Transporting Polypeptide B1 And B3 (OATP1B1/1B3) Substrates
Teriflunomide inhibits the activity of BCRP and OATP1B1/1B3 in vivo. For a patient taking Aubagio, the dose of rosuvastatin should not exceed 10 mg once daily. For other substrates of BCRP (e.g., mitoxantrone) and drugs in the OATP family (e.g., methotrexate, rifampin), especially HMG-Co reductase inhibitors (e.g., atorvastatin, nateglinide, pravastatin, repaglinide, and simvastatin), consider reducing the dose of these drugs and monitor patients closely for signs and symptoms of increased exposures to the drugs while patients are taking Aubagio.
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Related Disease Conditions
Multiple Sclerosis (MS)
Multiple sclerosis or MS is an autoimmune disorder in which brain and spinal cord nerve cells become demyelinated. This damage results in symptoms that may include numbness, weakness, vertigo, paralysis, and involuntary muscle contractions. Different forms of MS can follow variable courses from relatively benign to life-threatening. MS is treated with disease-modifying therapies. Some MS symptoms can be treated with medications.
MS (Multiple Sclerosis) vs. ALS (Amyotrophic Lateral Sclerosis) Differences and Similarities
ALS (amyotrophic lateral sclerosis, Lou Gehrig's disease) and MS (multiple sclerosis) are both diseases of the nervous system (neurodegenerative). ALS is a disease in which the nerve cells in the body are attacked by the immune system, although it's not considered an autoimmune disease by some scientists. MS is an autoimmune disease in which the insulated covering of the nerves (myelin sheath) in the CNS (central nervous system) degenerate, or deteriorate. Scientists don't know the exact cause of either problem. However, they have discovered that mutations in the gene that produces the SOD1 enzyme were associated with some cases of familial ALS. Scientists also theorize that multiple sclerosis may be caused by infection or vitamin D deficiency. ALS occurs between 50-70 years of age (the average age of occurrence ALS is 55), and mostly affects men. While MS occurs between 20-60 years of age, and mostly affects women. About 30,000 people in the US have ALS, and an average of 5,000 new diagnoses per year (that's about 15 new cases per week). Worldwide, MS affects more than 2.3 million people, with about 10,000 new cases diagnosed each year (that's about 200 new diagnoses per week).Some of the signs and symptoms of both diseases include muscle weakness, muscle spasms, problems walking, fatigue, slurred speech, and problems swallowing. ALS signs and symptoms that are different from MS include problems holding the head upright, clumsiness, muscle cramps and twitches, problems holding objects, and uncontrollable periods of laughing or crying. MS signs and symptoms that are different from ALS include vision problems, vertigo and balance problems, sexual problems, memory problems, depression, mood swings, and digestive problems. There is no cure for either disease, however the prognosis and life expectancy are different. Multiple sclerosis is not a fatal condition, while ALS progresses rapidly and leads to death.
Multiple Sclerosis (MS) Symptoms and Treatments
Multiple sclerosis (MS) symptoms vary from person to person, and can last for days to months without periods of remission. Symptoms of MS include sexual problems and problems with the bowel, bladder, eyes, muscles, speech, swallowing, brain, and nervous system. The early symptoms and signs of multiple sclerosis usually start between age 20 and 40. MS in children, teens, and those over age 40 is rare. Treatment options for multiple sclerosis vary depending on the type and severity of symptoms. Medications may be prescribed to manage MS symptoms.
Multiple Sclerosis (MS) Early Warning Signs and Types
Multiple sclerosis (MS) can be thought of as an immune-mediated inflammatory process involving different areas of the central nervous system (CNS) at various points in time. Early warning signs and symptoms of MS in children, teens, and adults are similar; however, children and teens with pediatric also may have seizures and a complete lack of energy. Adults with MS do not have these signs and symptoms. Other signs and symptoms of MS include inflammation of the optic nerve (optic neuritis), changes in vision, Wiping or having tissues around the eye and moving the eye may be painful, and double vision. There are four types of MS, relapsing remitting MS (RRMS), secondary progressive MS (SPMS), primary progressive MS (PPMS), and progressive relapsing MD (PRMS).
Is MS Contagious? (Multiple Sclerosis)
Multiple sclerosis, or MS, is a degenerative disease of the covering around the nerves in the central nervous system (CNS). Researchers and doctors don't know the exact cause, but many theorize that it may be due to environmental triggers, an autoimmune disease, and viruses (infections). Symptoms of MS include vision changes, paralysis, vertigo, heat intolerance, slurred speech, sexual dysfunction, and urinary incontinence (the inability to urinate). There's no vaccine or cure for MS, but the progression and symptoms of the disease can be treated.
Multiple Sclerosis (MS) and Pregnancy
Multiple sclerosis or MS is a central nervous system disease in which the immune system attacks the myelin sheath (the protective coating around nerves). Symptoms of MS include pain, sexual problems, fatigue, numbness and tingling, emotional changes, and depression.Women who are pregnant and have multiple sclerosis may have more difficulty carrying a pregnancy. Multiple sclerosis does not affect ability to conceive, and does not seem to affect fertility. MS symptoms during pregnancy may stay the same or get better; however, they may worsen after giving birth. Pregnancy decreases the number of relapses, but flares increase in the first 3-6 months after delivery. Pregnant women with MS may carrying a pregnancy more difficult to tell when labor starts, and there is an increased need to use forceps or vacuum to assist with delivery or b7 C-section (Cesarean birth) increases. Some treatment MS drugs may be safe to use during pregnancy; however, some drugs should not be taken, for example, baclofen (Gablofen, Lioresal), fluoxetine (Prozac, Sarafem), or solifenacin succinate (VESIcare), and most disease-modifying therapies (DMTs). Talk with your healthcare team about vitamins, supplements, and medications that you are taking if you are pregnant and have MS.
Alternative Treatment for MS (CAM for MS)
The term alternative therapy, in general, is used to describe any medical treatment or intervention that has not been scientifically documented or identified as safe or effective for a specific condition. Alternative therapy encompasses a variety of disciplines that range from diet and exercise to mental conditioning to lifestyle changes.
Treatment & Diagnosis
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Professional side effects and drug interactions sections courtesy of the U.S. Food and Drug Administration.