D11AX16 - Eflornithine |
Propably not porphyrinogenic |
PNP |
Rationale
Eflornithine is administered topically and hepatic exposure is insignificant. Eflornithine is excreted in urine as unchanged drug and no metabolism is recognized.
Chemical description
Ornithine decarboxylase inhibitor, alpha-difluoromethylornitine
Therapeutic characteristics
Eflornithine is used in the treatment of facial hirsutism in women. It is applied topically.
Hepatic exposure
Cmax of efornithine is approximately 10 ng/mL (Malhotra 2001). This is equivalent to 0.05 µM and hepatic exposure is insignificant.
Metabolism and pharmacokinetics
Eflornithine is not known to be metabolized and is eliminated in the urine as unchanged drug (SPC).
Less than 1 % of the drug is absorbed following topical application (Martindale).
References
- Scientific articles
- Malhotra B, Noveck Rm, et al. Percutaneous absorption and pharmacokinetics of eflornithine HCl 13.9% cream in women with unwanted facial hair. J Clin Pharmacol. 2001 Sep;41(9):972-8. PMID 11549102. #4438
- Drug reference publications
- Martindale in Micromedex® 2.0 (electronic version). Eflornithine. (12.05.2015). #1390
- Summary of Product Characteristics
- The electronic Medicines Compendium (emc). Summary of Product Characteristics (SPC). (Vaniqa). #1391
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