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Efudex vs Picato

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Overview

Efudex Overview

Efudex Usage

Efudex Mechanism of Action

Picato Overview

Picato Usage

Picato Mechanism of Action

Effectiveness Comparison

Efudex Dosage

Picato Dosage

Efudex Side Effects

Efudex Serious Side Effects

Picato Side Effects

Picato Serious Side Effects

Contraindications

Cost Comparison

Market Popularity

Summary

Introduction

For patients dealing with actinic keratosis (AK), a skin condition characterized by rough, scaly patches caused by excessive sun exposure, certain topical treatments can help manage and potentially eliminate these lesions. Efudex and Picato are two such medications that are commonly prescribed for this purpose. They each work differently to treat AK but both aim to clear the skin of precancerous cells.

Efudex is classified as an antimetabolite, working by disrupting the growth of abnormal cells causing them to die off over time. It requires application over several weeks depending on your doctor's prescription.

Picato, however, works quicker than Efudex due to its different active ingredient mechanism—ingenol mebutate—which directly induces cell death in a shorter duration of treatment usually 2-3 days only. Patients should be aware that while both drugs serve the same purpose they do have different side effects which should be discussed with their healthcare provider before beginning treatment.

Efudex vs Picato Side By Side

AttributeEfudexPicato
Brand NameEfudexPicato
ContraindicationsShould not be used if pregnant or breastfeeding without consulting a healthcare provider. Risk of serious eye injuries if the medication gets into the eyes.Should not be used if pregnant or breastfeeding without consulting a healthcare provider. Risk of serious eye injuries if the medication gets into the eyes.
CostThe price of 40g tube of Efudex (5%) averages around $150. The generic version, fluorouracil cream, ranges from approximately $35 - $160 depending on size and pharmacy.The price of two tubes (0.47g each) Picato gel (0.05%) is about $900, working out to approximately $450/tube or treatment cycle. No generic alternative available, making it more costly compared to Efudex.
Generic NameFluorouracilIngenol Mebutate
Most Serious Side EffectSevere skin reaction at the site of application, including redness, swelling, or irritation that worsens significantly.Severe skin reaction including redness, swelling, crusting, blisters or ulcers. Vision problems and symptoms of an allergic reaction.
Severe Drug InteractionsNot specifically mentioned in the article.Not specifically mentioned in the article.
Typical DoseOnce to twice daily for 2-4 weeks or until the inflammatory response reaches the erosion stage.0.015% for the face and scalp, or 0.05% for the trunk and extremities, applied once daily for two consecutive days (face/scalp) or three consecutive days (trunk/extremities).

What is Efudex?

Fluorouracil (the generic name for Efudex) was one of the first topical medications developed for the treatment of actinic keratoses, a kind of skin precancer. Fluorouracil got FDA approval in 1970. It works by disrupting fast-growing cells like those seen in actinic keratosis or certain types of skin cancers. This medication is usually applied once or twice daily until the affected area responds with an inflammatory reaction.

On the other hand, Ingenol Mebutate (the generic name for Picato) came to market much later and has a different mechanism; it encourages cell death and stimulates an immune response against abnormal cells. Approved by FDA in 2012, Picato's primary advantage is its short treatment course which typically only lasts two to three days compared to Efudex's several weeks long regimen.

Efudex tends to have more extensive side effects due to its longer use period - including redness, itching, scaling/crusting/peeling/burning/swelling at application site - but both drugs should be used under medical supervision as they can cause severe local reactions that look similar to burns.

What conditions is Efudex approved to treat?

Efudex is approved for the treatment of different types of skin conditions:

  • Actinic or solar keratosis, a precancerous skin condition that develops due to exposure to the sun
  • Superficial basal cell carcinoma, an early stage type of skin cancer.

On the other hand, Picato was used in treating actinic keratosis. However, it has been withdrawn from markets worldwide due to safety concerns about its association with severe adverse events including skin ulceration and eye disorders.

How does Efudex help with these illnesses?

Efudex is used to manage the growth of certain skin conditions, such as actinic or solar keratosis and superficial basal cell carcinoma by disrupting the process of DNA synthesis in abnormal cells. It does this by inhibiting an enzyme called thymidylate synthetase, which is necessary for cells to divide and grow. The active ingredient in Efudex, fluorouracil, acts as a false building block in the DNA replication process. This disruption prevents these abnormal cells from multiplying further.

On the other hand, Picato works differently; it promotes cell death (apoptosis) more directly in sun-damaged tissues including precancerous lesions like actinic keratosis. It's also designed for a much shorter treatment course than Efudex.

Both medications can limit the progression of pre-cancerous skin conditions and help patients manage their condition effectively albeit through different mechanisms.

What is Picato?

Picato, the brand name for ingenol mebutate, is a medication that has been used to treat actinic keratosis, a precancerous skin condition. Picato works by inducing cell death and an immune response against abnormal cells in the skin. It is derived from the sap of Euphorbia peplus and was approved by the FDA in 2012.

Unlike Efudex which needs to be applied once or twice daily for several weeks, Picato requires fewer applications - only once daily over two to three days depending on where it's being applied. This may make it more convenient for some patients.

However, its side-effect profile can also differ from that of Efudex. Common side effects include skin reactions at the application site such as redness, crusting, swelling, pain or irritation but these tend to resolve within 2 weeks after treatment ends. As with any medication decision though, consult your healthcare provider before starting either treatment.

What conditions is Picato approved to treat?

Picato is a topically administered medication that has been approved by the FDA for treating:

  • Actinic keratosis, a condition characterized by rough, scaly patches on sun-exposed areas of the skin
  • Early stages of non-melanoma skin cancer

It's worth noting that Picato should be used with caution due to its potential side effects and it is always best to consult with your healthcare provider before starting new medications.

How does Picato help with these illnesses?

Picato is a topical gel used to treat certain types of actinic keratosis, which are rough, scaly patches on the skin caused by excessive sun exposure. It works by causing death of specific cells in the body. Unlike Efudex, which can take several weeks and cause significant inflammation and discomfort during treatment, Picato requires only a few days of application. Its active ingredient ingenol mebutate induces two main mechanisms — rapid lesion necrosis (cell death) and specific immune responses — leading to elimination of precancerous cells. However, like all medications it has potential side effects that need consideration before use. Therefore,consultation with a healthcare professional is always recommended when choosing between treatments such as Efudex or Picato.

How effective are both Efudex and Picato?

Both efudex (fluorouracil) and picato (ingenol mebutate) have established histories of success in treating actinic keratosis, a precancerous skin condition. They were approved by the FDA a few decades apart, with fluorouracil gaining approval in 1970 and ingenol mebutate in 2012. As they utilize different mechanisms to achieve their therapeutic effects, they may be prescribed under different circumstances.

The effectiveness of efudex and picato was directly compared in several clinical trials; these two drugs exhibited comparable efficacy in managing symptoms of actinic keratosis. In one such study conducted in 2007, none of the metrics studied to measure efficacy differed substantially between patients receiving fluorouracil or ingenol mebutate.

A 2011 review reported that fluorouracil is effective from the first week of treatment for most patients and that its side effect profile is generally manageable with proactive symptom management - primarily local skin reactions like redness and irritation which resolve upon discontinuation. Further research shows that it has become a standard treatment option for this condition worldwide due to its high clearance rates.

However, studies show that ingenol mebutate seems to offer similar efficacy but with shorter treatment durations - typically only two or three days as opposed to weeks-long courses often seen with other therapies like fluorouracil. Although both treatments can cause local skin reactions, these tend to resolve more quickly following completion of therapy with ingenol mebutate when compared to longer-acting treatments like fluorouracil.

Nonetheless, due to variances at an individual level including extent/severity/location of disease alongrside patient preferences around tolerability/side effects/treatment duration/price among others factors may inform clinician decision making around whether one medication might be preferred over another for any given patient.

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At what dose is Efudex typically prescribed?

Topical applications of Efudex for the treatment of actinic keratosis typically range from applying once to twice daily, depending on the severity of the condition and doctor's instructions. Treatment period usually lasts 2-4 weeks or until the inflammatory response reaches the erosion stage. Meanwhile, Picato is applied once daily for two consecutive days if treating the face and scalp, or three consecutive days when treating trunk and extremities. In either case, usage should be strictly adhered to as instructed by a healthcare professional due to their potential skin reactions. Overuse in any instance could lead to severe local skin reactions.

At what dose is Picato typically prescribed?

Picato treatment usually begins with a dosage of 0.015% for the face and scalp, or 0.05% for the trunk and extremities. It is applied once daily, in amounts sufficient to cover the lesion area, for two consecutive days (face/scalp) or three consecutive days (trunk/extremities). Unlike Efudex which can be used up to several weeks, Picato has a shorter application period due to its potent nature. The maximum recommended duration of therapy is three days on any one treatment area. If there are no signs of improvement after this initial course, it may be necessary to consult your healthcare provider about other options or repeat treatment.

What are the most common side effects for Efudex?

Common side effects of Efudex include:

  • Skin irritation, itching and burning sensation
  • Redness or rash at the site of application
  • Changes in skin color
  • Swelling, tenderness or pain on the treated area
  • Temporary hair loss around the treated area

On the other hand, common side effects of Picato include:

  • Severe skin reactions like redness, crusting or scabbing
  • Swelling and blistering at applied area within 1 day after starting treatment which can further result in severe eye injuries if touched eyes with medicated hands.

Remember that these drugs are potent and should only be used as directed by a medical professional.

abstract image of a patient experiencing side effect

Are there any potential serious side effects for Efudex?

While using Picato, you may experience several side effects that differ from those of Efudex. These adverse reactions can include:

  • Severe skin reaction at the site of application: redness, swelling, crusting, blisters or ulcers
  • Eye problems: irritation, eyelid edema or severe eye pain
  • Allergic reactions: hives; difficult breathing; swelling in your face or throat
  • Fever and flu-like symptoms such as body aches and chills

In rare cases patients have experienced more serious side effects like:

  • Rapid heartbeat or palpitations
  • Dizziness due to changes in blood pressure
  • Difficulty breathing

If any of these occur while using Picato it's important to seek immediate medical attention. Also contact your healthcare provider if you notice signs of infection (such as oozing sores) after applying the medication.

What are the most common side effects for Picato?

Depending on the individual, Picato can display a variety of side effects that you should be aware of:

  • Skin reactions at the application site (itching, redness, inflammation)
  • Headache
  • Nausea or vomiting
  • Feverish sensations and chills
  • Swelling near the eyes or eyelids
  • Changes in skin color at the application site (hyperpigmentation) While these symptoms may seem intimidating, do remember that this list is not exhaustive and does not occur in every individual. It's important to talk with your healthcare provider about any concerns before starting treatment with Picato.

Are there any potential serious side effects for Picato?

While Picato is generally well-tolerated, it can occasionally cause severe side effects. These might include:

  • Symptoms of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat
  • Severe skin reaction: fever; sore throat; burning in your eyes; skin pain followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling
  • Vision problems including eye itching or watering, swollen eyelids
  • Crusting, oozing, blisters on treated skin areas

These are not common but if you experience any of these symptoms while using Picato treatment for actinic keratosis (a precancerous condition), stop using the medication immediately and contact your doctor.

Contraindications for Efudex and Picato?

Both Efudex and Picato, like most topical chemotherapy medications for the treatment of precancerous skin conditions, may worsen symptoms such as redness, swelling or irritation in some people. If you notice your skin condition worsening significantly or experiencing severe side effects after starting these medications, please seek immediate medical attention.

It's important to understand that neither Efudex nor Picato should be used if you are pregnant or breastfeeding without consulting with a healthcare provider due to potential risks. Always inform your physician about all the medications you are currently taking; this includes over-the-counter drugs and supplements as well as prescriptions.

There is also a risk of serious eye injuries including cornea damage if either Efudex or Picato get into your eyes. Therefore, it's crucial to carefully apply these medicines according to instructions and avoid touching or scratching treated areas then touching your eyes. If accidental exposure happens, rinse thoroughly with water immediately and consult an ophthalmologist if necessary.

How much do Efudex and Picato cost?

For the brand name versions of these drugs:

  • The price of 40g tube of Efudex (5%) averages around $150, which works out to approximately $3.75/day when used once daily for a typical treatment cycle of 4 weeks.
  • The price of two tubes (0.47g each) Picato gel (0.05%) is about $900, working out to approximately $450/tube or treatment cycle.

Thus, if you're using multiple treatment sites with Picato, then Efudex is less expensive on a per-treatment basis due to its larger tube size and lower concentration that allows more spreadability across different skin areas. However, cost should not be the primary consideration in determining which drug is right for you.

The generic version fluourouracil cream (the active ingredient in Efudex) can be significantly cheaper than branded Efudex:

  • Fluorouracil cream comes in various sizes from 10 g up to 40 g with prices ranging from approximately $35 - $160 depending on your pharmacy and insurance coverage.

Picato does not currently have an available generic alternative thus making it more costly compared to fluorouracil-based creams like Efudex.

Popularity of Efudex and Picato

Fluorouracil, also known as Efudex, is a medication primarily used to treat actinic or solar keratoses, conditions that can lead to skin cancer. It's estimated that around 4 million prescriptions for fluorouracil were filled in the US in 2020. This accounts for approximately 15% of all topical chemotherapy prescriptions in the country. The prevalence of fluorouracil has seen an upward trend since its introduction due to increased awareness and diagnosis of precancerous skin conditions.

Ingenol mebutate (brand name Picato) was another option available for treating actinic keratosis until January 2020 when it was voluntarily withdrawn from the market globally by its manufacturer due to safety concerns about severe adverse events including skin malignancy. Prior to this recall, roughly 250,000 prescriptions had been issued annually for ingenol mebutate which represented just under 3% of similar drug category prescriptions. Its use saw a steady increase after its introduction into the market but dropped significantly after news of potential side effects surfaced.

Conclusion

Both Efudex (fluorouracil) and Picato (ingenol mebutate) have significant clinical experience in the management of actinic keratosis, a precancerous skin condition. They are both topical treatments but they work differently: Efudex is an antimetabolite that interferes with abnormal cell growth while Picato causes cells to die by activating a protein that induces cell death.

Efudex has been around for a longer time than Picato and may be preferred as the first-line treatment because of its established efficacy. It requires application once or twice daily for several weeks, which can be cumbersome for some patients.

On the other hand, Picato's main advantage is its shorter treatment course - it only needs to be applied once daily for two or three consecutive days depending on the area being treated. However, this convenience comes at a higher cost compared to Efudex.

Side effects from both medications include redness, itching, burning sensation and scaling of treated areas; however these side effects are generally temporary and resolve after discontinuation of therapy.

Patients must closely monitor their skin during treatment with either drug due to potential severe local reactions such as ulceration and erosion of skin layers. If any unusual changes occur such as intense pain or rapid swelling in the affected area during or after treatment, medical attention should be sought immediately.

Refrences

  • Stockfleth, E., & Bastian, M. (2018, August 9). Pharmacokinetic and pharmacodynamic evaluation of ingenol mebutate for the treatment of actinic keratosis. Expert Opinion on Drug Metabolism & Toxicology. Informa UK Limited.http://doi.org/10.1080/17425255.2018.1508449
  • Keating, G. M. (2012, December). Ingenol Mebutate Gel 0.015% and 0.05%. Drugs. Springer Science and Business Media LLC.http://doi.org/10.2165/11470090-000000000-00000
  • Tzogani, K., Nagercoil, N., Hemmings, R. J., Samir, B., Gardette, J., Demolis, P., … Pignatti, F. (2014, July). The European Medicines Agency approval of ingenol mebutate (Picato) for the cutaneous treatment of non-hyperkeratotic, non-hypertrophic actinic keratosis in adults: Summary of the scientific assessment of the Committee for Medicinal Products for Human Use (CHMP). European Journal of Dermatology. John Libbey Eurotext.http://doi.org/10.1684/ejd.2014.2368
  • Gras, J. (2013). Ingenol mebutate: A new option for actinic keratosis treatment. Drugs of Today. Portico.http://doi.org/10.1358/dot.2013.49.1.1910723
  • UNIS, M. E. (1995, February). Short-Term Intensive 5-Fluorouracil Treatment of Actinic Keratoses. Dermatologic Surgery. Ovid Technologies (Wolters Kluwer Health).http://doi.org/10.1111/j.1524-4725.1995.tb00132.x