Eflornithine is a medication primarily used to treat excessive facial hair growth in women. It is available as a topical cream under the brand name Vaniqa. Eflornithine works by inhibiting the enzyme ornithine decarboxylase, which is involved in the production of polyamines necessary for cell division and hair growth. By inhibiting this enzyme, eflornithine can slow down the growth of facial hair.

Excessive facial hair growth in women, a condition known as hirsutism, can be caused by various factors including hormonal imbalances, medications, or certain medical conditions such as polycystic ovary syndrome (PCOS). Eflornithine is often used in combination with other treatments such as hormonal therapy to manage hirsutism effectively.

Eflornithine (Vaniqa) inhibits the enzyme Ornithine decarboxylase that is required for cellular replication and differentiation. The topical cream is used in the treatment of excessive unwanted facial hair. The injection formulation is used as an off-label medicine for the treatment of sleeping sickness.

Eflornithine (Vaniqa) Uses:

• Facial hair reduction:
  • It is indicated in female patients with excessive facial and chin hair. It is applied as a topical cream to reduce unwanted hair in females.
• Off Label Use of Eflornithine in Adults:
  • The intravenous formulation is used as an off-label drug for the treatment of sleeping sickness (meningoencephalitic stage of Trypanosoma brucei gambiense infection)

Eflornithine (Vaniqa) Dose in Adults

Eflornithine (Vaniqa) Dose in the treatment of Facial hair reduction in females:

• To reduce facial hair in women, you apply a thin layer of eflornithine cream to the affected areas of your face and under your chin two times a day.
• Make sure there's at least an 8-hour gap between each application.

Eflornithine (Vaniqa) Dose in the Treatment of Sleeping sickness (caused by Trypanosoma brucei gambiense infection (off-label):

• For treating infections caused by Trypanosoma brucei gambiense, commonly known as sleeping sickness, eflornithine is administered intravenously (IV).
• The typical dosage is 100 milligrams per kilogram of body weight per dose, given every 6 hours for a total of 14 days.

Eflornithine (Vaniqa) Dose in Childrens

Eflornithine (Vaniqa) Dose in the treatment of unwanted facial hair: Topical:

• For reducing unwanted facial hair, particularly in female children aged 12 years and above as well as adolescents, eflornithine is applied topically as a cream.
• The recommended dosage involves applying a thin layer of the cream to the affected areas of the face and adjacent chin two times a day.
• Ensure there is at least an 8-hour gap between each application.

Eflornithine (Vaniqa) Dose in the Treatment of Sleeping sickness (caused by Trypanosoma brucei gambiense infection:

For the treatment of infections caused by Trypanosoma brucei gambiense infection, commonly known as sleeping sickness, the recommended dosages of eflornithine vary depending on the treatment regimen:

• NECT regimen (Nifurtimox-Eflornithine Combination Therapy):
  • Children and Adolescents: Intravenously (IV) administered at a dosage of 200 milligrams per kilogram (mg/kg) per dose every 12 hours for a duration of 7 days. This is typically administered in combination with nifurtimox.
• Monotherapy:
  • For children under 12 years: IV administration at a dosage of 150 mg/kg per dose every 6 hours for a total duration of 14 days.
  • For children aged 12 years and older, as well as adolescents: IV administration at a dosage of 100 mg/kg per dose every 6 hours for a total duration of 14 days.

It's important to note that these dosages are based on the limited data available and recommendations provided by the World Health Organization (WHO) in 2013.

Eflornithine (Vaniqa) Pregnancy Risk Factor C

• When eflornithine is applied topically, there haven't been any harmful effects observed in animal studies regarding pregnancy.
• However, because there isn't enough information about its topical use during pregnancy, it's advised to think about stopping or not starting the treatment to avoid any potential risks.
• Eflornithine has been classified as Pregnancy Risk Factor C.

Use of eflornithine during lactation

• It's uncertain whether eflornithine passes into breast milk.
• As a precaution, the manufacturer advises being cautious when giving eflornithine to nursing mothers.

Eflornithine (Vaniqa) Dose in Kidney disease:

• The manufacturer's labeling does not provide specific dosage adjustments for eflornithine in cases of renal impairment.
• However, when administering eflornithine by injection, dose adjustments may be necessary for individuals with renal impairment, although there are no specific guidelines available for this adjustment.

Eflornithine (Vaniqa) Dose in Liver disease:

• The manufacturer's labeling does not include specific dosage adjustments for eflornithine in cases of hepatic impairment.
• However, when administering eflornithine by injection, dose adjustments may be necessary for individuals with hepatic impairment, although there are no specific guidelines available for this adjustment.

Injection:

Common Side Effects of Eflornithine Injection:

• Cardiovascular:
  • Cardiac Arrhythmia
  • Hypertension
  • Chest Pain
• Central Nervous System:
  • Headache
  • Dizziness
• Dermatologic:
  • Pruritus
  • Skin Rash
• Gastrointestinal:
  • Abdominal Pain
  • Diarrhea
  • Nausea
  • Vomiting
  • Anorexia
• Hematologic & Oncologic:
  • Neutropenia
• Infection:
  • Infection
• Local:
  • Injection Site Reaction
• Neuromuscular & Skeletal:
  • Arthralgia
  • Myalgia
  • Weakness
• Miscellaneous:
  • Fever

Less Common Side Effects Of Eflornithine Injection:

• Cardiovascular:
  • Edema
  • Hypotension
  • Shock
• Central Nervous System:
  • Insomnia
  • Seizure
  • Anxiety
  • Peripheral Neuropathy
  • Coma
  • Amnesia
  • Ataxia
  • Confusion
  • Depression
  • Hallucination
  • Lethargy
• Endocrine & Metabolic:
  • Dehydration
• Gastrointestinal:
  • Dysphagia
  • Xerostomia
  • Constipation
  • Dysgeusia
  • Hiccups
• Genitourinary:
  • Urinary Frequency
  • Urinary Urgency
  • Urinary Incontinence
  • Change In Creatinine
• Hematologic & Oncologic:
  • Anemia
  • Leukopenia
  • Thrombocytopenia
• Hepatic:
  • Abnormal Bilirubin Levels
  • Increased Serum Transaminases
• Local:
  • Extravasation
• Neuromuscular & Skeletal:
  • Tremor
• Otic:
  • Inner Ear Disturbance
• Respiratory:
  • Cough
  • Epistaxis
  • Dyspnea
  • Respiratory Distress

---

Topical application:

Common Side Effects Of Eflornithine (Vaniqa):

• Dermatologic:
  • Acne Vulgaris
  • Pseudofolliculitis Barbae

Less Common Side Effects Of Eflornithine (Vaniqa):

• Central Nervous System:
  • Headache
  • Tingling Of Skin
  • Dizziness
• Dermatologic:
  • Stinging Of The Skin
  • Burning Sensation Of Skin
  • Pruritus
  • Skin Rash
  • Xeroderma
  • Erythema
  • Alopecia
  • Skin Irritation
  • Folliculitis
  • Ingrown Hair
• Gastrointestinal:
  • Dyspepsia
  • Anorexia

Contraindications to Eflornithine (Vaniqa):

• If an individual has a known hypersensitivity or allergic reaction to eflornithine or any component of the formulation, they should not use eflornithine products.

• It's crucial to avoid using eflornithine if you have experienced any allergic reactions to it in the past or if you are allergic to any of the ingredients in the formulation.

Monitoring parameters:

• Monitor CBC with platelet counts

How to administer Eflornithine (Topical and Injection)?

Cream Application:

• For external use only: Only apply the cream on the outside of your skin.
• How to apply: Put a thin layer of the cream on the parts of your face and chin where you want to reduce hair. Rub it in well.
• Continuing hair removal: Keep using your usual hair removal methods. Wait at least 5 minutes after removing hair before applying the cream.
• Wait after application: Don't wash the areas where you applied the cream for at least 4 hours.
• Makeup and sunscreen: You can use makeup and sunscreen on the treated areas once the cream has dried.

IV Administration:

• Only IV administration: Eflornithine is only given through an intravenous (IV) line.
• Dilution required: Before using, it needs to be mixed with a liquid (diluted).
• Infusion time: It should be slowly infused over 45 to 120 minutes.
• Not for IM administration: Don't inject it into muscle (intramuscularly).

Mechanism of action of Eflornithine:

Cream:

• Mechanism of action: Eflornithine works by blocking the activity of an enzyme called ornithine decarboxylase (ODC). This enzyme is involved in cell division and the production of certain substances needed for cell growth.
• Effect on hair growth: By inhibiting ODC, eflornithine slows down the rate of hair growth on the treated areas of the skin.

Injection:

• Mechanism of action: Eflornithine acts by specifically and irreversibly inhibiting the enzyme ornithine decarboxylase (ODC). This enzyme is crucial for the production of certain substances called polyamines, which are necessary for cell growth and function.
• Antitumor and antiprotozoal effects: By inhibiting ODC, eflornithine reduces the production of polyamines in cells, which are essential for cell growth and replication. This effect makes it useful in treating certain tumors and parasitic infections.
• Effect on cell growth: Eflornithine depletes cells of important polyamines like putrescine and spermidine, which are needed for cell growth and DNA synthesis. This depletion affects rapidly dividing cells the most, making them more susceptible to the drug's effects.

Onset of Action (Decreased Hair Growth):

• Timeframe: It typically takes about 4 to 8 weeks to notice a decrease in hair growth after starting treatment.

Duration of Action (Decreased Hair Growth):

• Continued Effect: The reduction in hair growth continues until around 8 weeks after stopping the treatment.

Absorption (Topical):

• Rate: Less than 1% of the applied cream is absorbed through the skin into the bloodstream.

Half-life Elimination:

• Intravenous (IV): The half-life of elimination is approximately 3 to 3.5 hours when administered intravenously.
• Topical: The half-life of elimination is around 8 hours when applied topically to the skin.

Excretion:

• Primary Route: Eflornithine is primarily excreted in the urine without undergoing significant changes (as the unchanged drug).

International Brand Names of Eflornithine:

• Vaniqa
• Clearoswab
• Florexa
• Flornith
• Malsa
• Vanihair

Eflornithine Brand Names in Pakistan:

Eflornithine Cream 11.5 % w/w in Pakistan
Depilus	Atco Laboratories Limited
Eflogen	Zam Zam Corporation

 

Eflornithine Cream 11.5 % w/w in Pakistan
Epila	Valor Pharmaceuticals

 

Eflornithine Cream 13.9 % w/w in Pakistan
Epila	Valor Pharmaceuticals

Eflornithine is a medication primarily used to treat excessive facial hair growth in women. It is available as a topical cream under the brand name Vaniqa. Eflornithine works by inhibiting the enzyme ornithine decarboxylase, which is involved in the production of polyamines necessary for cell division and hair growth. By inhibiting this enzyme, eflornithine can slow down the growth of facial hair.

Excessive facial hair growth in women, a condition known as hirsutism, can be caused by various factors including hormonal imbalances, medications, or certain medical conditions such as polycystic ovary syndrome (PCOS). Eflornithine is often used in combination with other treatments such as hormonal therapy to manage hirsutism effectively.

Eflornithine (Vaniqa) inhibits the enzyme Ornithine decarboxylase that is required for cellular replication and differentiation. The topical cream is used in the treatment of excessive unwanted facial hair. The injection formulation is used as an off-label medicine for the treatment of sleeping sickness.

Eflornithine (Vaniqa) Uses:

• Facial hair reduction:
  • It is indicated in female patients with excessive facial and chin hair. It is applied as a topical cream to reduce unwanted hair in females.
• Off Label Use of Eflornithine in Adults:
  • The intravenous formulation is used as an off-label drug for the treatment of sleeping sickness (meningoencephalitic stage of Trypanosoma brucei gambiense infection)

Eflornithine (Vaniqa) Dose in Adults

Eflornithine (Vaniqa) Dose in the treatment of Facial hair reduction in females:

• To reduce facial hair in women, you apply a thin layer of eflornithine cream to the affected areas of your face and under your chin two times a day.
• Make sure there's at least an 8-hour gap between each application.

Eflornithine (Vaniqa) Dose in the Treatment of Sleeping sickness (caused by Trypanosoma brucei gambiense infection (off-label):

• For treating infections caused by Trypanosoma brucei gambiense, commonly known as sleeping sickness, eflornithine is administered intravenously (IV).
• The typical dosage is 100 milligrams per kilogram of body weight per dose, given every 6 hours for a total of 14 days.

Eflornithine (Vaniqa) Dose in Childrens

Eflornithine (Vaniqa) Dose in the treatment of unwanted facial hair: Topical:

• For reducing unwanted facial hair, particularly in female children aged 12 years and above as well as adolescents, eflornithine is applied topically as a cream.
• The recommended dosage involves applying a thin layer of the cream to the affected areas of the face and adjacent chin two times a day.
• Ensure there is at least an 8-hour gap between each application.

Eflornithine (Vaniqa) Dose in the Treatment of Sleeping sickness (caused by Trypanosoma brucei gambiense infection:

For the treatment of infections caused by Trypanosoma brucei gambiense infection, commonly known as sleeping sickness, the recommended dosages of eflornithine vary depending on the treatment regimen:

• NECT regimen (Nifurtimox-Eflornithine Combination Therapy):
  • Children and Adolescents: Intravenously (IV) administered at a dosage of 200 milligrams per kilogram (mg/kg) per dose every 12 hours for a duration of 7 days. This is typically administered in combination with nifurtimox.
• Monotherapy:
  • For children under 12 years: IV administration at a dosage of 150 mg/kg per dose every 6 hours for a total duration of 14 days.
  • For children aged 12 years and older, as well as adolescents: IV administration at a dosage of 100 mg/kg per dose every 6 hours for a total duration of 14 days.

It's important to note that these dosages are based on the limited data available and recommendations provided by the World Health Organization (WHO) in 2013.

Eflornithine (Vaniqa) Pregnancy Risk Factor C

• When eflornithine is applied topically, there haven't been any harmful effects observed in animal studies regarding pregnancy.
• However, because there isn't enough information about its topical use during pregnancy, it's advised to think about stopping or not starting the treatment to avoid any potential risks.
• Eflornithine has been classified as Pregnancy Risk Factor C.

Use of eflornithine during lactation

• It's uncertain whether eflornithine passes into breast milk.
• As a precaution, the manufacturer advises being cautious when giving eflornithine to nursing mothers.

Eflornithine (Vaniqa) Dose in Kidney disease:

• The manufacturer's labeling does not provide specific dosage adjustments for eflornithine in cases of renal impairment.
• However, when administering eflornithine by injection, dose adjustments may be necessary for individuals with renal impairment, although there are no specific guidelines available for this adjustment.

Eflornithine (Vaniqa) Dose in Liver disease:

• The manufacturer's labeling does not include specific dosage adjustments for eflornithine in cases of hepatic impairment.
• However, when administering eflornithine by injection, dose adjustments may be necessary for individuals with hepatic impairment, although there are no specific guidelines available for this adjustment.

Injection:

Common Side Effects of Eflornithine Injection:

• Cardiovascular:
  • Cardiac Arrhythmia
  • Hypertension
  • Chest Pain
• Central Nervous System:
  • Headache
  • Dizziness
• Dermatologic:
  • Pruritus
  • Skin Rash
• Gastrointestinal:
  • Abdominal Pain
  • Diarrhea
  • Nausea
  • Vomiting
  • Anorexia
• Hematologic & Oncologic:
  • Neutropenia
• Infection:
  • Infection
• Local:
  • Injection Site Reaction
• Neuromuscular & Skeletal:
  • Arthralgia
  • Myalgia
  • Weakness
• Miscellaneous:
  • Fever

Less Common Side Effects Of Eflornithine Injection:

• Cardiovascular:
  • Edema
  • Hypotension
  • Shock
• Central Nervous System:
  • Insomnia
  • Seizure
  • Anxiety
  • Peripheral Neuropathy
  • Coma
  • Amnesia
  • Ataxia
  • Confusion
  • Depression
  • Hallucination
  • Lethargy
• Endocrine & Metabolic:
  • Dehydration
• Gastrointestinal:
  • Dysphagia
  • Xerostomia
  • Constipation
  • Dysgeusia
  • Hiccups
• Genitourinary:
  • Urinary Frequency
  • Urinary Urgency
  • Urinary Incontinence
  • Change In Creatinine
• Hematologic & Oncologic:
  • Anemia
  • Leukopenia
  • Thrombocytopenia
• Hepatic:
  • Abnormal Bilirubin Levels
  • Increased Serum Transaminases
• Local:
  • Extravasation
• Neuromuscular & Skeletal:
  • Tremor
• Otic:
  • Inner Ear Disturbance
• Respiratory:
  • Cough
  • Epistaxis
  • Dyspnea
  • Respiratory Distress

---

Topical application:

Common Side Effects Of Eflornithine (Vaniqa):

• Dermatologic:
  • Acne Vulgaris
  • Pseudofolliculitis Barbae

Less Common Side Effects Of Eflornithine (Vaniqa):

• Central Nervous System:
  • Headache
  • Tingling Of Skin
  • Dizziness
• Dermatologic:
  • Stinging Of The Skin
  • Burning Sensation Of Skin
  • Pruritus
  • Skin Rash
  • Xeroderma
  • Erythema
  • Alopecia
  • Skin Irritation
  • Folliculitis
  • Ingrown Hair
• Gastrointestinal:
  • Dyspepsia
  • Anorexia

Contraindications to Eflornithine (Vaniqa):

• If an individual has a known hypersensitivity or allergic reaction to eflornithine or any component of the formulation, they should not use eflornithine products.

• It's crucial to avoid using eflornithine if you have experienced any allergic reactions to it in the past or if you are allergic to any of the ingredients in the formulation.

Monitoring parameters:

• Monitor CBC with platelet counts

How to administer Eflornithine (Topical and Injection)?

Cream Application:

• For external use only: Only apply the cream on the outside of your skin.
• How to apply: Put a thin layer of the cream on the parts of your face and chin where you want to reduce hair. Rub it in well.
• Continuing hair removal: Keep using your usual hair removal methods. Wait at least 5 minutes after removing hair before applying the cream.
• Wait after application: Don't wash the areas where you applied the cream for at least 4 hours.
• Makeup and sunscreen: You can use makeup and sunscreen on the treated areas once the cream has dried.

IV Administration:

• Only IV administration: Eflornithine is only given through an intravenous (IV) line.
• Dilution required: Before using, it needs to be mixed with a liquid (diluted).
• Infusion time: It should be slowly infused over 45 to 120 minutes.
• Not for IM administration: Don't inject it into muscle (intramuscularly).

Mechanism of action of Eflornithine:

Cream:

• Mechanism of action: Eflornithine works by blocking the activity of an enzyme called ornithine decarboxylase (ODC). This enzyme is involved in cell division and the production of certain substances needed for cell growth.
• Effect on hair growth: By inhibiting ODC, eflornithine slows down the rate of hair growth on the treated areas of the skin.

Injection:

• Mechanism of action: Eflornithine acts by specifically and irreversibly inhibiting the enzyme ornithine decarboxylase (ODC). This enzyme is crucial for the production of certain substances called polyamines, which are necessary for cell growth and function.
• Antitumor and antiprotozoal effects: By inhibiting ODC, eflornithine reduces the production of polyamines in cells, which are essential for cell growth and replication. This effect makes it useful in treating certain tumors and parasitic infections.
• Effect on cell growth: Eflornithine depletes cells of important polyamines like putrescine and spermidine, which are needed for cell growth and DNA synthesis. This depletion affects rapidly dividing cells the most, making them more susceptible to the drug's effects.

Onset of Action (Decreased Hair Growth):

• Timeframe: It typically takes about 4 to 8 weeks to notice a decrease in hair growth after starting treatment.

Duration of Action (Decreased Hair Growth):

• Continued Effect: The reduction in hair growth continues until around 8 weeks after stopping the treatment.

Absorption (Topical):

• Rate: Less than 1% of the applied cream is absorbed through the skin into the bloodstream.

Half-life Elimination:

• Intravenous (IV): The half-life of elimination is approximately 3 to 3.5 hours when administered intravenously.
• Topical: The half-life of elimination is around 8 hours when applied topically to the skin.

Excretion:

• Primary Route: Eflornithine is primarily excreted in the urine without undergoing significant changes (as the unchanged drug).

International Brand Names of Eflornithine:

• Vaniqa
• Clearoswab
• Florexa
• Flornith
• Malsa
• Vanihair

Eflornithine Brand Names in Pakistan:

Eflornithine Cream 11.5 % w/w in Pakistan
Depilus	Atco Laboratories Limited
Eflogen	Zam Zam Corporation

 

Eflornithine Cream 11.5 % w/w in Pakistan
Epila	Valor Pharmaceuticals

 

Eflornithine Cream 13.9 % w/w in Pakistan
Epila	Valor Pharmaceuticals