Eflornithine

Eflornithine
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alberto Plate [2]

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Overview

Eflornithine is a hair growth retardant, ornithine decarboxylase inhibitor that is FDA approved for the treatment of reduction of unwanted facial hair in women.. Common adverse reactions include acne and stinging of skin.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Apply a thin layer of VANIQA® (eflornithine hydrochloride) 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 VANIQA®. (VANIQA® should be applied at least 5 minutes after hair removal.) Cosmetics or sunscreens may be applied over treated areas after cream has dried.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Eflornithine in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Eflornithine in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding Eflornithine FDA-Labeled Indications and Dosage (Pediatric) in the drug label.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Eflornithine in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Eflornithine in pediatric patients.

Contraindications

contraindicated in patients with a history of sensitivity to any components of the preparation.

Warnings

Discontinue use if hypersensitivity occurs.

Precautions

General

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

Information for Patients

Patients using VANIQA® should receive the following information and instructions:

• This medication is not a depilatory, but rather appears to retard hair growth to improve the condition and the patient's appearance. Patients will likely need to continue using a hair removal method (e.g., shaving, plucking, etc.) in conjunction with VANIQA® (eflornithine hydrochloride) cream, 13.9%.
• Onset of improvement was seen after as little as 4-8 weeks of treatment in the 24-week clinical trials. The condition may return to pretreatment levels 8 weeks after discontinuing treatment.
• If skin irritation or intolerance develops, direct the patient to temporarily reduce the frequency of application (e.g., once a day). If irritation continues, the patient should discontinue use of the product.
• Refer to the Patient Information Leaflet for additional important information and instructions.

Adverse Reactions

Clinical Trials Experience

Adverse events reported for most body systems occurred at similar frequencies in VANIQA® (eflornithine hydrochloride) cream, 13.9% and vehicle control groups. The most frequent adverse events related to treatment with VANIQA® were skin-related. The following table notes the percentage of adverse events associated with the use of VANIQA® or its vehicle that occurred at greater than 1% in both the vehicle-controlled studies and the open-label safety studies up to 1 year of continuous use.

Treatment-related skin adverse events that occurred in less than 1% of the subjects treated with VANIQA® are: bleeding skin, cheilitis, contact dermatitis, swelling of lips, herpes simplex, numbness, and rosacea.

Adverse events were primarily mild in intensity and generally resolved without medical treatment or discontinuation of VANIQA®. Only 2% of subjects discontinued studies due to an adverse event related to use of VANIQA®.

Laboratory Test Abnormalities

No laboratory test abnormalities have been consistently found to be associated with VANIQA®. In an open-label study, some patients showed an increase in their transaminases; however, the clinical significance of these findings is not known.

Postmarketing Experience

There is limited information regarding Eflornithine Postmarketing Experience in the drug label.

Drug Interactions

There is limited information regarding Eflornithine Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): There is no FDA guidance on usage of Eflornithine in women who are pregnant.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Eflornithine in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Eflornithine during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Eflornithine in women who are nursing.

Pediatric Use

There is no FDA guidance on the use of Eflornithine in pediatric settings.

Geriatic Use

There is no FDA guidance on the use of Eflornithine in geriatric settings.

Gender

There is no FDA guidance on the use of Eflornithine with respect to specific gender populations.

Race

There is no FDA guidance on the use of Eflornithine with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Eflornithine in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Eflornithine in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Eflornithine in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Eflornithine in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding Eflornithine Administration in the drug label.

Monitoring

There is limited information regarding Eflornithine Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Eflornithine and IV administrations.

Overdosage

There is limited information regarding Eflornithine overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.

Pharmacology

There is limited information regarding Eflornithine Pharmacology in the drug label.

Mechanism of Action

There is limited information regarding Eflornithine Mechanism of Action in the drug label.

Structure

There is limited information regarding Eflornithine Structure in the drug label.

Pharmacodynamics

There is limited information regarding Eflornithine Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Eflornithine Pharmacokinetics in the drug label.

Nonclinical Toxicology

There is limited information regarding Eflornithine Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Eflornithine Clinical Studies in the drug label.

How Supplied

There is limited information regarding Eflornithine How Supplied in the drug label.

Storage

There is limited information regarding Eflornithine Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Eflornithine Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Eflornithine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Eflornithine Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Eflornithine Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

Eflornithine

File:Eflornithine-2D-skeletal.png
Clinical data
[[Regulation of therapeutic goods |Template:Engvar data]]	US FDA: Eflornithine
Pregnancy category	Category C for dermal cream
Routes of administration	Intravenous (discontinued) Dermal
ATC code	D11AX16 (WHO) P01CX03 (WHO)
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	100% (Intravenous) 13% (Dermal)
Metabolism	Not metabolised
Elimination half-life	8 hours
Excretion	Renal
Identifiers
IUPAC name 2,5-diamino-2-(difluoromethyl)pentanoic acid
CAS Number	70052-12-9
PubChem CID	3009
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C6H12F2N2O2
Molar mass	182.2 g/mol

Overview

Eflornithine (α-difluoromethylornithine or DFMO) is a drug manufactured by Sanofi-Aventis which has various uses. It was initially developed for cancer treatment, but while having little use in treating malignancies, it was found to be highly effective in African trypanosomiasis (sleeping sickness), especially the West African form (Trypanosoma brucei gambiense). In the United States it is known by the brand name Ornidyl®.

Sleeping sickness treatment

Function

Eflornithine appears to kill trypanosomes by acting as a suicide inhibitor of the enzyme ornithine decarboxylase (EC 4.1.1.17), this enzyme regulates cell division by catalysing the first step in polyamine biosynthesis.

Eflornithine's effects against Trypanosoma brucei gambiense were discovered by chance and because of its ability to bring patients back from coma, it became known as "Resurrection Drug".

It is hoped that eflornithine will replace the relatively toxic melarsoprol.

Production

Supplies of eflornithine are limited as its manufacturer does not consider it cost effective.

Its production was halted by its manufacturer, Aventis, in 1995 because the company did not consider it a profitable drug. The disease mainly affects poor people unable to pay for any sort of treatment.

In 2001, after lobbying at the WHO World Health Organization by Médecins Sans Frontières ("Doctors Without Borders"), the manufacturer resumed production of eflornithine, melarsoprol and pentamidine in sufficient amounts to cover existing needs. This 5-year agreement with the WHO also envisaged MSF working on the distribution of the drugs. The yearly value of the drugs donated by Aventis under this agreement is US$5 million. In addition, under the agreement, Bristol-Myers Squibb, the manufacturer of Vaniqa, will pay for part of the eflornithine. The 5-year agreement expired in 2006. The trade name of eflornithine as manufactured for the treatment of sleeping sickness is Ornidyl®.

Once the five years period is over, Sanofi-Aventis (its new name after merging with another drugs company, Sanofi-Synthélabo) would start transferring technology and giving technical assistance to any possible manufacturer willing to continue production on their own.

As of September 2005, the World Health Organization reports that the India Institute of Chemical Technology in Hyderabad, India and ILEX Oncology in Texas, United States are both working on new ways of making eflornithine more cheaply. The WHO goes on to say that ILEX is experimenting with an oral formulation of the drug as a treatment for cancer and that trials of the new oral formulation for efficacy against sleeping sickness are underway.

Dosing

When used for sleeping sickness, eflornithine is given intravenously, 50 mg/kg every six hours for 14 days.

Hair growth inhibitor cream

Eflornithine is also an effective hair growth inhibiting agent. As a topical application, the drug has been shown to be an effective hair growth retardant in some patients, and is sold under the brand name Vaniqa® (eflornithine hydrochloride 13.9%). Efficacy data submitted to Food and Drug Administration (FDA) observed about 58% of women using it on facial hair had improvement. This study suggested it may be particularly effective in postmenopausal women. One large published study on safety found the product rarely caused significant side effects such as acne, follicle irritation, itching or dryness. This corroborates unpublished data submitted to FDA showing about 2% of subjects discontinued use due to adverse reactions.

It is partly the development of the hair removal market that encouraged Aventis to re-start the manufacture of eflornithine, and which allowed it to once again become available for use in sleeping sickness.

External links

• HairFacts: Vaniqa overview and medical data
• WHO Eflornithine page