Last update June 7, 2022

Leflunomide

Incompatible

Very unsafe. Contraindicated. Use of an alternative or cessation of breastfeeding. Read the Commentary.

An immunosuppressant with antiproliferative properties used as a disease-modifying antirheumatic drug (DMARD) in rheumatoid arthritis, psoriatic arthritis and in some neoplasms. Its main active metabolite is teriflunomide. Oral administration once or twice a day for months.

Since the last update we have not found published data on its excretion in breastmilk.

Its high binding to plasma proteins makes its transfer to milk in significant concentrations unlikely.

Its slow elimination (half-life of 15 days) and its potentially serious side effects means it is recommended that, until there is more published data on this drug in relation to breastfeeding, safer alternatives are used (Sammaritano 2020, Götestam 2016, Flint 2016, Sammaritano 2014, Weber 2008, Østensen 2006, Temprano 2005), especially during the neonatal period and in case of prematurity.


See below the information of this related product:

  • Teriflunomide (Very unsafe. Contraindicated. Use of an alternative or cessation of breastfeeding. Read the Commentary.)

Alternatives

Suggestions made at e-lactancia are done by APILAM team of health professionals, and are based on updated scientific publications. It is not intended to replace the relationship you have with your doctor but to compound it. The pharmaceutical industry contraindicates breastfeeding, mistakenly and without scientific reasons, in most of the drug data sheets.

Jose Maria Paricio, Founder & President of APILAM/e-Lactancia

Your contribution is essential for this service to continue to exist. We need the generosity of people like you who believe in the benefits of breastfeeding.

Thank you for helping to protect and promote breastfeeding.

José María Paricio, founder of e-lactancia.

Other names

Leflunomide in other languages or writings:

Group

Leflunomide belongs to this group or family:

Tradenames

Main tradenames from several countries containing Leflunomide in its composition:

Pharmacokinetics

Variable Value Unit
Oral Bioavail. 82 - 95 %
Molecular weight 270 daltons
Protein Binding 99.3 %
VD 0.13 l/Kg
pKa 10.41 -
Tmax 6 - 12 hours
360 hours

References

  1. Sammaritano LR, Bermas BL, Chakravarty EE, Chambers C, Clowse MEB, Lockshin MD, Marder W, Guyatt G, Branch DW, Buyon J, Christopher-Stine L, Crow-Hercher R, Cush J, Druzin M, Kavanaugh A, Laskin CA, Plante L, Salmon J, Simard J, Somers EC, Steen V, Tedeschi SK, et al. 2020 American College of Rheumatology Guideline for the Management of Reproductive Health in Rheumatic and Musculoskeletal Diseases. Arthritis Rheumatol. 2020 Apr;72(4):529-556. Abstract Full text (link to original source)
  2. Flint J, Panchal S, Hurrell A, van de Venne M, Gayed M, Schreiber K, Arthanari S, Cunningham J, Flanders L, Moore L, Crossley A, Purushotham N, Desai A, Piper M, Nisar M, Khamashta M, Williams D, Gordon C, Giles I; BSR and BHPR Standards, Guidelines and Audit Working Group. BSR and BHPR guideline on prescribing drugs in pregnancy and breastfeeding-Part I: standard and biologic disease modifying anti-rheumatic drugs and corticosteroids. Rheumatology (Oxford). 2016 Sep;55(9):1693-7. Abstract Full text (link to original source) Full text (in our servers)
  3. Götestam Skorpen C, Hoeltzenbein M, Tincani A, Fischer-Betz R, Elefant E, Chambers C, da Silva J, Nelson-Piercy C, Cetin I, Costedoat-Chalumeau N, Dolhain R, Förger F, Khamashta M, Ruiz-Irastorza G, Zink A, Vencovsky J, Cutolo M, Caeyers N, Zumbühl C, Østensen M. The EULAR points to consider for use of antirheumatic drugs before pregnancy, and during pregnancy and lactation. Ann Rheum Dis. 2016 May;75(5):795-810. Abstract Full text (link to original source) Full text (in our servers)
  4. Sammaritano LR, Bermas BL. Rheumatoid arthritis medications and lactation. Curr Opin Rheumatol. 2014 Abstract
  5. Weber JC, Kuhnert C. Traitements de fond des affections inflammatoires systémiques au cours de l’allaitement. [Breastfeeding and drug management in connective tissue and rheumatic diseases]. Rev Med Interne. 2008 Dec;29(12):1017-23. Abstract
  6. Østensen M, Khamashta M, Lockshin M, Parke A, Brucato A, Carp H, Doria A, Rai R, Meroni P, Cetin I, Derksen R, Branch W, Motta M, Gordon C, Ruiz-Irastorza G, Spinillo A, Friedman D, Cimaz R, Czeizel A, Piette JC, Cervera R, Levy RA, et al. Anti-inflammatory and immunosuppressive drugs and reproduction. Arthritis Res Ther. 2006 Abstract Full text (link to original source) Full text (in our servers)
  7. Temprano KK, Bandlamudi R, Moore TL. Antirheumatic drugs in pregnancy and lactation. Semin Arthritis Rheum. 2005 Abstract

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