Allopurinol

Drug Levels and Effects:




Summary of Use during Lactation:


Limited information indicates that a maternal dose of allopurinol 300 mg daily provides near-therapeutic dose and plasma levels in an exclusively breastfed infant. If allopurinol is required by the mother, it is not a reason to discontinue breastfeeding, but exclusively breastfed infants should be monitored if this drug is used, including observation for allergic reactions (such as rash) and periodic CBC and differential blood counts.


Drug Levels:


Allopurinolis metabolized to oxypurinol which has xanthine oxidase inhibitory activity equal to allopurinol 's. Oxypurinol is well absorbed from the gastrointestinal tract.[1]

Maternal Levels.

A woman who was 5 weeks postpartum had been taking allopurinol 300 mg orally for 4 weeks. Two hours after a dose her breastmilk contained 0.9 mg/L of allopurinol and 53.7 mg/L of its active metabolite oxypurinol. Four hours after the dose, her breastmilk contained 1.4 mg/L of allopurinol and 48 mg/L of oxypurinol. The authors calculated that the exclusively breastfed infant would receive between 0.14 and 0.2 mg/kg of allopurinol and between 7.2 to 8 mg/kg of oxypurinol daily. This dose of oxypurinol is slightly less than the infant allopurinol dose of 10 mg/kg daily.[2][3]

Infant Levels.

A 5-week-old infant whose mother had been taking allopurinol 300 mg daily for 4 weeks had plasma levels of allopurinol that was undetectable (<0.5 mg/L) and of oxypurinol that was 6.6 mg/L 2 hours after nursing and 4 hours after the mother's dose of allopurinol . This plasma level was 33 to 48% of the measured maternal plasma oxypurinol levels.[2][3]


Effects in Breastfed Infants:


One infant breastfed from age 1 week to age 7 weeks during maternal allopurinol therapy with 300 mg or allopurinol daily. The infant had no observable side effects and no changes in clinical chemistry and hematology values.[3]


Possible Effects on Lactation:


Relevant published information was not found as of the revision date.


References:


1. Walter-Sack I , de Vries JX, Ernst B et al. Uric acid lowering effect of oxipurinol sodium in hyperuricemic patients - therapeutic equivalence to allopurinol . J Rheumatol. 1996;23:498-501. PMID:8832991
2. Kamilli I, Gresser U, Schaefer C et al.Allopurinolin breast milk. Adv Exp Med Biol. 1991;309A:143-5. PMID:1789194
3. Kamilli I, Gresser U.Allopurinoland oxypurinol in human breast milk. Clin Investig. 1993;71:161-4. PMID:8461629



Substance Identification:




Substance Name:

Allopurinol

CAS Registry Number:

315-30-0

Drug Class:


  • Antigout Agents

  • Enzyme Inhibitors

  • Gout Suppressants


  • Administrative Information:




    LactMed Record Number:


    334


    Last Revision Date:


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