Alpha-difluoromethylornithine

Alpha-difluoromethylornithine

Alpha-difluoromethylornithine prevents hair growth by inhibiting the anagen phase of hair production. This occurs by eflornithine irreversibly binding (also called suicide inhibition) to ornithine decarboxylase (ODC) and physically preventing the natural substrate ornithine from accessing the active site.

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Uses

Alpha-difluoromethylornithine Hydrochloride cream, 13.9% is used for the reduction of unwanted facial hair in women. Alpha-difluoromethylornithine Hydrochloride has only been studied on the face and adjacent involved areas under the chin of affected individuals. Usage should be limited to these areas of involvement.

Alpha-difluoromethylornithine is also used to associated treatment for these conditions: Meningoencephalitic stage Trypanosoma brucei gambiense infection, Hair removal therapy

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How Alpha-difluoromethylornithine works

Alpha-difluoromethylornithine prevents hair growth by inhibiting the anagen phase of hair production. This occurs by eflornithine irreversibly binding (also called suicide inhibition) to ornithine decarboxylase (ODC) and physically preventing the natural substrate ornithine from accessing the active site.

Alpha-difluoromethylornithine

Trade Name Alpha-difluoromethylornithine
Generic Eflornithine
Eflornithine Other Names alpha-difluoromethylornithine, DFMO, Eflornithine
Type
Formula C6H12F2N2O2
Weight Average: 182.171
Monoisotopic: 182.08668396
Groups Approved, Withdrawn
Therapeutic Class Hair Growth Inhibitor
Manufacturer
Available Country
Last Updated: June 7, 2022 at 8:58 pm

Structure

Alpha-difluoromethylornithine
Eflornithine Structure
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Dosage

Alpha-difluoromethylornithine dosage

Adults: Apply a thin layer of Alpha-difluoromethylornithine cream, 13.9% to affected areas of the face and adjacent involved areas under the chin and rub in thoroughly. Do not wash treated area for at least 4 hours. Use twice daily at least 8 hours apart or as directed by a physician. The patient should continue to use hair removal techniques as needed in conjunction with Alpha-difluoromethylornithine (Wonica should be applied at least 5 minutes after hair removal). Cosmetics or sunscreens may be applied over treated areas after cream has dried. 

.Elderly: No apparent differences in safety were observed between older patients and younger patients. 

Children: The safety and effectiveness of this product have not been established in pediatric patients less than 12 years of age.

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Side Effects

Adverse events were primarily mild in intensity and generally resolved without medical treatment or discontinuation of Alpha-difluoromethylornithine. Side effects can include acne, barbae, pseudofolliculitis, stinging skin, headache, burning skin, dry skin, erythema (redness), pruritus (itching), tingling skin, dyspepsia, skin irritation, rash, alopecia, dizziness, folliculitis, hair ingrown, facial edema, anorexia, nausea, asthenia, vertigo.

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Precaution

For external use only. Transient stinging or burning may occur when applied to abraded or broken skin.

Interaction

It is not known whether Alpha-difluoromethylornithine has any interaction with other topically applied drug products.

Food Interaction

No interactions found.
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Half Life

8 hours

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Elimination Route

Renal

Pregnancy & Breastfeeding use

Pregnancy Category C. It is not known whether or not Alpha-difluoromethylornithine Hydrochloride is excreted in human milk. Caution should be exercised when Alpha-difluoromethylornithine is administered to a nursing woman.

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Contraindication

Alpha-difluoromethylornithine is contraindicated in patients with a history of sensitivity to any components of the preparation.

Special Warning

Store at 25°C, excursions permitted to 15°C-30°C. Do not freeze.

Acute Overdose

Overdosage information with Alpha-difluoromethylornithine is unavailable. However, if very high topical doses (e.g., multiple tubes per day) or oral ingestion has been encountered (a 30 gm tube contains 4.2 gm of Alpha-difluoromethylornithine Hydrochloride), the patient should be monitored, and appropriate supportive measures should be administered as necessary.

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Storage Condition

Store at 25°C, excursions permitted to 15°C-30°C. Do not freeze.