Eflornithine

Eflornithine: Mechanism of Action, Uses, Side effects, and Contraindications

Difluoromethylornithine DFMO which is now commonly known as Eflornithine shows clinical efficacy against Pneumocystis pneumonia (PCP) and West African trypanosomiasis. The drug was initially designed to be used as an anticancer agent, but it proved to be unproductive later.

African sleeping sickness, which is also known as Human African trypanosomiasis, is a parasite infection transmitted by the tsetse fly that has a near-100 percent fatality rate if not treated. When life years lost are taken into account, it is the world’s third most important parasitic illness. An estimated 450,000 people were affected in 1997. Despite the fact that the number has reduced in recent years as a result of integrated efforts, it remained an overlooked disease, with many people unable to receive treatment.

Human African trypanosomiasis is caused by two parasite subspecies:

  1. Trypanosoma brucei rhodesiense
  2. Trypanosoma brucei gambiense

A vast majority of the reported cases are said to be caused by the subspecies Trypanosoma brucei gambiense.

There are two stages of the disease African sleeping sickness

  1. Initial hemolytic phase
  2. Later encephalopathy phase

There are just a few therapy choices for the later phase, such as melarsoprol and eflornithine. It is given either alone or in combination with nifurtimox, which is taken orally. Considering the side effects and resistance shown by Nifurtimox, Eflornithine is more commonly used as first-line therapy to treat later stages of the African sleeping sickness.

Topical Eflornithine preparations are used to treat hirsutism in women. It is approved for the treatment of face hirsutism in women aged 18 and up.

Eflornithine Mechanism of Action

As an irreversible inhibitor of ornithine decarboxylase, eflornithine inhibits the biosynthesis of the polyamine. Polyamines are necessary for trypanosome cell proliferation, differentiation, and replication.

Eflornithine Pharmacokinetics

Routes of Administration

It can be administered into the body via

  • Oral route
  • Intravenous (IV) route

Bioavailability

Upon oral administration of the drug, Eflornithine shows a bioavailability of 50%.

Distribution

The drug is not bound to plasma proteins and penetrates the central nervous system quite well, achieving 6–51 percent of plasma levels.

Metabolism

The drug shows no significant metabolism in the human body.

Excretion

It is primarily excreted by the kidneys.

Eflornithine Uses

It is used to treat the following diseases

  • African sleeping sickness
  • Pneumocystis carinii (Pneumonia in patients with AIDS)
  • Prevention of growth of untoward hair on women’s face due to PCOS or other hormonal conditions

Eflornithine Contraindications

Some contraindications of Eflornithine include

  • Cardiac diseases
  • Epilepsy
  • Anemia
  • Hypersensitivity

Eflornithine Side Effects

  • Osmotic diarrhea
  • Bone marrow suppression
  • Leukopenia
  • Anemia
  • Thrombocytopenia

How does Eflornithine hydrochloride cream work?

The anagen phase of hair formation is inhibited by eflornithine, which prevents hair growth. This is accomplished by binding irreversibly to ornithine decarboxylase and physically blocking the natural substrate ornithine from reaching the active site. Eflornithine is a drug that is used to prevent undesirable facial hair from growing around the lips or beneath the chin in women. It acts by preventing a natural chemical found in your hair follicle that is required for hair growth.

Is eflornithine cream over the counter?

No, the cream is a prescription medication.

Eflornithine cream side effects

  • Skin irritation
  • Itching
  • Dryness
  • Acne
  • Redness
  • Pruritus
  • Tingling skin

Can you get Vaniqa on the NHS?

Due to a lack of data, prescribing Vaniqa / eflornithine 11.5 percent cream is not suggested.

Vaniqa cream contains eflornithine 11.5%. The cream is approved by NHS Scotland for the treatment of face hirsutism in women on a limited basis.

Due to constraints in the Herefordshire and Worcestershire health budget, the Medicines Prescribing Committee does not believe the cream to be suitable for use within the Herefordshire and Worcestershire health economy because of current clinical trial data and weight of information of cost-benefit analysis for the usage of NHS grants.

References

https://medlineplus.gov/druginfo/meds/a604031.html
https://go.drugbank.com/drugs/DB06243
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4335853/
https://patient.info/medicine/eflornithine-cream-vaniqa
https://www.rxlist.com/vaniqa-drug.htm
https://herefordshireandworcestershireccg.nhs.uk/policies/clinical-medicines-commissioning/clinical-policies-and-guidance/skin/293-eflornithine-vaniqa-cream-for-facial-hirsutism-position-statement/file

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