Dosing and uses of Picato (ingenol mebutate topical)
Adult dosage forms and strengths
topical geL
- 0.015% (3 unit dose tubes/carton)
- 0.05% (2 unit dose tubes/carton)
Actinic Keratosis
Indicated for topical treatment of actinic keratosis
Face or scalp: Apply 0.015% gel to affected area qDay for 3 consecutive days; avoid application in, near, and around the eyes, in the mouth, and on the lips
Trunk or extremities: Apply 0.05% gel to affected area qDay for 2 consecutive days
Do not apply gel to more than 1 area simultaneously
Only be used on 1 contiguous skin area not exceeding ~25 cm² (5 cm × 5 cm)
Not for spot treatment of actinic keratosis on multiple application sites simultaneously that exceeds 25 cm²
Pediatric dosage forms and strengths
Actinic keratosis is not a condition generally seen within the pediatric population
<18 years: Safety and efficacy not established
Geriatric dosage forms and strengths
In clinical trials, 56% of participants were 65 years or older, and 21% were 75 years or older
No differences in safety or effectiveness were observed between elderly and younger participants
Picato (ingenol mebutate topical) adverse (side) effects
>10%
Face/scalp application
- Erythema (94%)
- Flaking/scaling (85%)
- Crusting (80%)
- Swelling (79%)
- Vesiculation/pustulation (56%)
- Erosion/ulceration (32%)
- Application site pain (15%)
Trunk/extremities application
- Erythema (92%)
- Flaking/scaling (90%)
- Crusting (74%)
- Swelling (64%)
- Vesiculation/pustulation (44%)
- Erosion/ulceration (26%)
1-10%
Face/scalp application
- Application site pruritus (8%)
- Application site infection (3%)
- Periorbital edema (3%)
- Headache (2%)
Trunk/extremities application
- Application site pruritus (8%)
- Application site irritation (4%)
- Nasopharyngitis (2%)
- Application site pain (2%)
Frequency not defined
Eyelid edema
Eye pain
Chemical conjunctivitis
Postmarketing Reports
Allergic contact dermatitis
Herpes Zoster
Corneal burn
Eye injuries
Application site pigmentation changes
Application site scarring
Warnings
Contraindications
Known hypersensitivity to drug or component of formulation
Cautions
Avoid treatment of periocular area; eye disorders, including severe eye pain, eyelid edema, eyelid ptosis, periorbital edema can occur after exposure; caution patients to wash hands well after application and avoid transfer of the drug to other areas of the body; if accidental exposure occurs, flush eyes with water and seek medical care
Severe skin reactions in the treated area, including erythema, crusting, swelling, vesiculation/postulation, and erosion/ulceration occurs after topical application
Severe allergic reactions and herpes zoster infection reported; cases describe severe eye injuries and skin reactions, of which some were associated with the gel not being used according to the instructions
Not recommended until skin is healed from any previous drug or surgical treatment
Pregnancy and lactation
Pregnancy category: C
Lactation: Unknown whether distributed in breast milk
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Picato (ingenol mebutate topical)
Mechanism of action
The mechanism by which ingenol mebutate induces cell death is unknown
Absorption
Systemic exposure is negligible; blood levels and 2 of its metabolites were below the lower limit of quantification (ie, <0.1 ng/mL)
Metabolism
Ex vivo studies showed extensive metabolism in human hepatocytes
Administration
Instructions
Only be used on 1 contiguous skin area not exceeding ~25 cm² (5 cm × 5 cm)
Not for spot treatment of actinic keratosis on multiple application sites simultaneously that exceeds 25 cm²
1 unit dose tube covers up to one contiguous skin area of approximately 25 cm² (eg, 5 cm x 5 cm)
Face or scalp: Apply 0.015% gel topically to the treatment area qDay for 3 consecutive days; avoid application in, near, and around the eyes, in the mouth, and on the lips
On the trunk or extremities: Apply 0.05% gel topically to the treatment area qDay for 2 consecutive days
Do not apply gel to more than 1 area simultaneously
After spreading evenly over the treatment area, allow gel to dry for 15 minutes
Patients should wash their hands immediately after application and take care not to transfer the applied drug to other areas, including the eye
Patients should avoid washing and touching the treated area for 6 hr after; following this time, patients may wash the area with a mild soap
