Formulary
Teriflunomide: Indications, Dosing, Side Effects and Interactions
Teriflunomide is a metabolite of leflunomide which has immunomodulating and anti-inflammatory properties.
MedNext Academy | 3 min read
Teriflunomide: Indications, Dosing, Side Effects and Interactions
Teriflunomide is a metabolite of leflunomide which has immunomodulating and anti-inflammatory properties.
Drug action
Teriflunomide is a metabolite of leflunomide which has immunomodulating and anti-inflammatory properties.
Indications and dose
**Multiple sclerosis (initiated by a specialist)**
- **Adult** (By Mouth): 14 mg once daily.
**Multiple sclerosis (initiated by a specialist) for teriflunomide**
- **Child 10-17 years (body-weight up to 40 kg)** (By mouth): 7 mg once daily.
- **Child 10-17 years (body-weight 40 kg and above)** (By mouth): 14 mg once daily.
Cautions
Adult over 65 years (limited information available); anaemia; dyspnoea-assess for interstitial lung disease and consider suspending treatment; hypoproteinaemia (avoid if severe); impaired bone-marrow function (avoid if severe); latent tuberculosis; leucopenia; persistent cough-assess for interstitial lung disease and consider suspending treatment; severe infection-delay or suspend treatment until resolved; significant alcohol consumption; signs or symptoms of serious skin reactions (including ulcerative stomatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis)-discontinue treatment; switching between other immunomodulating drugs; thrombocytopenia
Contraindications
Anaemia; leucopenia; neutropenia; serious infection; severe hypoproteinaemia; severe immunodeficiency; significantly impaired bone-marrow function; thrombocytopenia
Side effects
Common or very common Alopecia; anaemia; anxiety; arthralgia; cystitis; diarrhoea; gastrointestinal discomfort; headache; hypersensitivity; hypertension; increased risk of infection; menorrhagia; myalgia; nausea; nerve disorders; neutropenia; oral disorders; pain; palpitations; sensation abnormal; skin reactions; urinary frequency increased; vomiting; weight decreased Uncommon Dyslipidaemia; gastrointestinal disorders; interstitial lung disease; nail disorder; pancreatitis; sepsis; severe cutaneous adverse reactions (SCARs); thrombocytopenia Rare or very rare Hepatic disorders Frequency not known Pancreatic pseudocyst; pulmonary hypertension Side-effects, further information Hepatic injury Discontinue treatment if signs or symptoms of hepatic injury, or if liver enzymes exceed 3 times the upper limit of reference range. Important : accelerated elimination procedure recommended following discontinuation due to serious adverse effects (consult product literature).
Interactions
**Severe interactions:**
- Cholestyramine or activated charcoal It is recommended that patients receiving teriflunomide are not treated with cholestyramine or activated charcoal because this leads to a rapid and significant...
**Other interactions (18):**
- Pharmacokinetic interactions of other substances on teriflunomide The primary biotransformation pathway for teriflunomide is hydrolysis, with oxidation being a minor pathway.
- Potent cytochrome P450 (CYP) and transporter inducers Co-administration of repeated doses (600 mg once daily for 22 days) of rifampicin (a CYP2B6, 2C8, 2C9, 2C19, 3A inducer), as well as an inducer...
- Rifampicin and other known potent CYP and transporter inducers such as carbamazepine, phenobarbital, phenytoin and St John's Wort should be used with caution during the treatment with teriflunomide.
- The mechanism is thought to be by interruption of enterohepatic recycling and/or gastrointestinal dialysis of teriflunomide.
- Pharmacokinetic interactions of teriflunomide on other substances Effect of teriflunomide on CYP2C8 substrate: repaglinide There was an increase in mean repaglinide Cmax and AUC (1.7- and 2.4-fold,...
- Therefore, medicinal products metabolised by CYP2C8, such as repaglinide, paclitaxel, pioglitazone or rosiglitazone, should be used with caution during treatment with teriflunomide.
Pregnancy
Avoid-toxicity in animal studies.
Breast feeding
Present in milk in animal studies-manufacturer advises avoid.
Hepatic impairment
Avoid in severe impairment. M Monitoring In patients with pre-existing liver disease, monitor liver function every 2 weeks for the first 6 months during treatment, then every 8 weeks thereafter for at least 2 years. Increase to weekly monitoring if alanine aminotransferase (ALT) is 2-3 times the upper limit of normal; discontinue treatment if signs or symptoms of hepatic injury occur, or if liver enzymes exceed 3 times the upper limit of normal. M
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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