Eflornithine

Author: Prof. Dr. med. Peter Altmeyer

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Last updated on: 29.10.2020

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Synonym(s)

DFMO; Difluoromethylornithine; Eflornithines

Definition
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Inhibitors of ornithine decarboxylase (alpha-difluoro-methylornithine).

Pharmacodynamics (Effect)
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Eflornithine irreversibly inhibits ornithine carboxylase, a key enzyme in cell proliferation and function. When applied twice daily for one week (in registration studies an average of 0.5 g/day) < 1% is absorbed and excreted renally unchanged. In parenteral application, hearing disorders, seizures, headaches, dizziness, loss of appetite, disturbed liver function as well as thrombopenia and leukopenia have been described.

Indication
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Hirsutism of the woman in the face.

Pregnancy/nursing period
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Eflornithine penetrates the blood-brain barrier and should therefore not be prescribed to pregnant women or while breastfeeding. Data from clinical studies on a limited number of exposed pregnancies suggest that there is no clinical evidence of side effects from local application of an eflornithine cream (Vaniqua) to the mother or fetus.

Dosage and method of use
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Hirsutism: Apply a thin layer of 15% cream 2 times/day on the affected areas (shave hair smooth before use). Warning: The preparation is not a "depilatory". After discontinuation, the effect will disappear within 8 weeks.

Undesirable effects
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With topical application acne-like skin changes (approx. 20% of patients), pseudofolliculitis barbae (approx. 15% of patients), burning, tingling or stinging pain (approx. 10-15% of patients). Besides 7-Eflornithine, Vaniqua® contains cetylstearyl alcohol, macrogolcetylstearyl ether, dimethicone, glycerol stearate, polyethylene glycol stearate, methyl 4-hydroxybenzoate (E218), paraffin oil, phenoxyethanol, propyl 4-hydroxybenzoate (E216), purified water, stearyl alcohol, sodium hydroxide (E524) (for pH adjustment).

Preparations
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Vaniqua Cream

Note(s)
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  • preparation was primarily synthesized as a cytostatic drug and is still being tested for the therapy and prevention of various tumors. It gained importance in the treatment of African sleeping sickness (trypanosomiasis), for which it has been approved as an i.v. preparation, for example in the USA (ORNIDYL) as an "orphan drug" since 1990. The observation that some patients who use eflornithine for sleeping sickness suffer from hair loss as a disruptive effect has led to the development of an external preparation against hirsutism.
  • The safety and effectiveness of Vaniqa in children and adolescents aged 0 to 18 years has not yet been proven. There are no data available to justify use in this age group!
  • Treatment success with topical application usually occurs at the earliest 6-8 weeks after the start of therapy and is reversible after discontinuation of therapy.
  • The treatment costs are covered if hirsutism is diagnosed.

Literature
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  1. Balfour JA et al (2001) Topical eflornithine. At J Clin Dermatol 2: 197-201
  2. Burri C, Brun R (2003) Eflornithine for the treatment of human African trypanosomiasis. Parasitol Res 90(Suppl1): S49-52
  3. Kunte C, Wolff H (2001) Current treatment of hypertrichosis. dermatologist 52: 993-997
  4. Trueb RM (2002) Causes and management of hypertrichosis. At J Clin Dermatol 3: 617-627
  5. Wolf JE Jr et al (2007) Eflornithine HCl Study Group. Randomized, double-blind clinical evaluation of the efficacy and safety of topical eflornithine HCl 13.9% cream in the treatment of women with facial hair. Int J Dermatol 46:94-98

Incoming links (2)

Hirsutism; Sleeping sickness;

Outgoing links (1)

Hirsutism;

Authors

Last updated on: 29.10.2020