4/5/2018 Actinic keratosis - Topical agents

Actinic keratosis (topical therapy)

Actinic keratoses (AKs) are premalignant lesions that develop only on sun-damaged skin.

Aminolevulinic acid HCL-

AMELUZ ® gel 10% for topical diclofenac (Solaraze ®)
use

imiquimod - ZYCLARA™ cream

fluorouracil (Efudex ®,TOLAK™)
3.75%

ingenol mebutate - PICATO® gel Other

--® --®

Please see package insert for additional information and possible updates. The authors make no claims of
the accuracy of the information contained herein; and these suggested doses are not a substitute for clinical
judgment. Neither GlobalRPh Inc. nor any other party involved in the preparation of this program shall be liable for
any special, consequential, or exemplary damages resulting in whole or part from any user's use of or reliance
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Aminolevulinic acid hydrochloride - AMELUZ ® gel 10% for topical use

Drug UPDATES : AMELUZ ® (aminolevulinic acid hydrochloride) gel, 10%, for topical use
[Drug information / PDF]
Package insert - Dosing: Click (+) next to Dosage and Administration section (drug info link)

Initial U.S. Approval: 2016

Mechanism of Action:
Photoactivation following topical application of AMELUZ occurs when aminolevulinic acid (prodrug) is
metabolized to protoporphyrin IX (PpIX), a photoactive compound which accumulates in the skin.
When exposed to red light of a suitable wavelength and energy, PpIX is activated resulting in an
excited state of porphyrin molecules. In the presence of oxygen, reactive oxygen species are formed
which causes damage to cellular components, and eventually destroys the cells. AMELUZ
photodynamic therapy of AK lesions utilizes photoactivation of topically applied AMELUZ resulting from
BF-RhodoLED illumination, which provides a red light of narrow spectrum and a light dose of
approximately 37 J/cm2.

INDICATIONS AND USAGE:

AMELUZ gel, a porphyrin precursor, in combination with photodynamic therapy using BF-RhodoLED
lamp, is indicated for the lesion-directed and field-directed treatment of actinic keratoses of mild-to-
moderate severity on the face and scalp (1).

DOSAGE AND ADMINISTRATION

-Administer AMELUZ only by a health care provider (2.1).
-AMELUZ is for topical use only (2.1).
-Photodynamic therapy with AMELUZ involves preparation of lesions, application of the product,
occlusion and illumination with BF-RhodoLED (2.2).
-Retreat lesions that have not completely resolved 3 months after the initial treatment (2.2).
-See BF-RhodoLED user manual for detailed lamp safety and operating instructions (2).

HOW SUPPLIED:
DOSAGE FORMS AND STRENGTHS
Gel: 10%

diclofenac (Solaraze ®)
The mechanism of action of diclofenac sodium in the treatment of actinic keratoses (AK) is unknown.
The contribution to efficacy of individual components of the vehicle has not been established.

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INDICATIONS AND USAGE

Solaraze® (diclofenac sodium) Gel is indicated for the topical treatment of actinic keratoses (AK). Sun
avoidance is indicated during therapy.

WARNINGS
As with other NSAIDs, anaphylactoid reactions may occur in patients without prior exposure to
diclofenac. Diclofenac sodium should be given with caution to patients with the aspirin triad. The triad
typically occurs in asthmatic patients who experience rhinitis with or without nasal polyps, or who
exhibit severe, potentially fatal bronchospasm after taking aspirin or other NSAIDs.

DOSAGE AND ADMINISTRATION

Solaraze® Gel is applied to lesion areas twice daily. It is to be smoothed onto the affected skin gently.
The amount needed depends upon the size of the lesion site. Assure that enough Solaraze® Gel is
applied to adequately cover each lesion. Normally 0.5 g of gel is used on each 5 cm x 5 cm lesion site.
The recommended duration of therapy is from 60 days to 90 days. Complete healing of the lesion(s) or
optimal therapeutic effect may not be evident for up to 30 days following cessation of therapy. Lesions
that do not respond to therapy should be carefully re-evaluated and management reconsidered.

HOW SUPPLIED
Available in tubes of 100 g (NDC 10337-803-01). Each gram of gel contains 30 mg of diclofenac
sodium.

Storage: Store at controlled room temperature 20-25°C (68-77°F); excursions permitted between 15-
30°C (59-86°F). Protect from heat. Avoid freezing.

†Voltaren® is a registered trademark of Novartis.

Manufactured by:
Almirall Hermal GmbH
D-21465 Reinbek, Germany
Made in Germany
Manufactured for:
PharmaDerm® A division of Fougera Pharmaceuticals Inc.

fluorouracil (Efudex ®):

Superficial basal cell carcinomas: apply 5% cream/solution twice daily.

Actinic keratoses:
Carac™: Apply thin film to lesions once daily for up to 4 weeks, as tolerated.
Efudex®: Apply to lesions twice daily for 2-4 weeks; complete healing may not be evident for 1-2
months following treatment.
Fluoroplex®: Apply to lesions twice daily for 2-6 weeks
Supplied: Cream, topical:
Carac™: 0.5% (30 g). Efudex®: 5% (25 g, 40 g). Fluoroplex®: 1% (30 g).

Drug UPDATES : TOLAK™- fluorouracil cream

[Drug information / PDF] Click link for the latest monograph
Dosing: Click (+) next to Dosage and Administration section (drug info link)

Initial U.S. Approval: 2015

Mechanism of Action: There is evidence that the metabolism of fluorouracil in the anabolic pathway
blocks the methylation reaction of deoxyuridylic acid to thymidylic acid. In this manner, fluorouracil
interferes with the synthesis of DNA and to a lesser extent inhibits the formation of RNA. Since DNA
and RNA are essential for cell division and growth, the effect of fluorouracil may be to create a thymine
deficiency that provokes unbalanced growth and death of the cell. The effects of DNA and RNA
deprivation are most marked on those cells that grow more rapidly and take up fluorouracil at a more
rapid rate.

INDICATIONS AND USAGE: Tolak (fluorouracil) Cream, 4%, is a nucleoside metabolic inhibitor
indicated for the topical treatment of actinic keratosis lesions of the face, ears, and scalp

HOW SUPPLIED: Cream: 40 mg of fluorouracil per gram of cream (4%)

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imiquimod - ZYCLARA™:
INDICATIONS AND USAGE:
ZYCLARA Cream, 2.5% and 3.75% are indicated for the topical treatment of clinically typical, visible or
palpable actinic keratoses (AK) of the full face or balding scalp in immunocompetent adults.
ZYCLARA Cream, 3.75% is also indicated for the topical treatment of external genital and perianal
warts/condyloma acuminata (EGW) in patients 12 years or older.

Limitations of Use: Efficacy of imiquimod cream was not demonstrated for molluscum contagiosum in
children 2 to 12 years of age.

DOSAGE AND ADMINISTRATION:

For topical use only; not for oral, ophthalmic, intra-anal or intravaginal use.

Actinic Keratosis: Once daily to the skin of the affected area (either the entire face or balding scalp) for
two 2-week treatment cycles separated by a 2-week no-treatment period.

External Genital Warts: Once daily to the external genital/perianal warts until total clearance or up to 8
weeks.

DOSAGE FORMS AND STRENGTHS:

Cream: 2.5% packets; 3.75% packets or pump.

CONTRAINDICATIONS:
None

WARNINGS AND PRECAUTIONS

Intense local inflammatory reactions can occur (e.g., skin weeping, erosion). Dosing interruption may
be required.

Severe local inflammatory reactions of the female external genitalia can lead to severe vulvar swelling.
Severe vulvar swelling can lead to urinary retention; dosing should be interrupted or discontinued.

Flu-like systemic signs and symptoms including fatigue, nausea, fever, myalgias, arthralgias, and chills
can occur. Dosing interruption may be required.

Avoid concomitant use of ZYCLARA Cream and any other imiquimod cream because of increased risk
for adverse reactions.

ADVERSE REACTIONS
Most common adverse reactions (>4%) are local skin reactions (erythema, edema, erosion/ulceration,
exudate, scabbing/crusting), headache, application site pain, application site irritation, application site
pruritus, fatigue, influenza-like illness, and nausea.

ingenol mebutate - PICATO® gel:

Drug: PICATO® (ingenol mebutate) gel, 0.015% for topical use

[Drug information / PDF]
Dosing: Click (+) next to Dosage and Administration section (drug info link)
ABBREVIATED MONOGRAPH - SEE PACKAGE INSERT.

Initial U.S. Approval: 2012

Mechanism of Action: The mechanism of action by which Picato® gel induces cell death in treating
AK lesions is unknown.

INDICATIONS AND USAGE: Picato ® gel is an inducer of cell death indicated for the topical
treatment of actinic keratosis.

DOSAGE AND ADMINISTRATION

ABBREVIATED MONOGRAPH - SEE PACKAGE INSERT
For topical use only; not for oral, ophthalmic, or intravaginal use. (2)
Avoid transfer of Picato® to periocular area. (2)

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Avoid application near and around the mouth and lips. (2)

For application of up to one contiguous skin area of approximately 25 cm2 (5 cm x 5 cm) using one
unit dose tube. (2)
Actinic keratosis on the face or scalp: Apply Picato® gel, 0.015% to the affected area once daily for 3
consecutive days. (2)

Actinic keratosis on the trunk or extremities: Apply Picato® gel, 0.05% to the affected area once daily
for 2 consecutive days. (2)

DOSAGE FORMS AND STRENGTHS

Gel containing ingenol mebutate, 0.015% or 0.05%

CONTRAINDICATIONS
Known hypersensitivity to ingenol mebutate or any component of the formulation.

WARNINGS AND PRECAUTIONS:

Eye disorders, including severe eye pain, eyelid edema, eyelid ptosis, periorbital edema can occur
after exposure. Avoid contact with the periocular area. If accidental exposure occurs, flush eyes with
water and seek medical care.

Local skin reactions can occur including severe reactions (e.g., vesiculation/pustulation,
erosion/ulceration). Administration of Picato® gel is not recommended until skin is healed from any
previous drug or surgical treatment.

Other:
1) Liquid nitrogen cryotherapy - widely utilized.
2) Chemical peels.
3) Dermabrasion.
4) Surgical (curettage) therapy.

Reference(s)
National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA).
Please review the latest applicable package insert for additional information and possible updates. A
local search option of this data can be found here.
Disclaimer
Listed dosages are for - Adult patients ONLY. PLEASE READ THE DISCLAIMER CAREFULLY
BEFORE ACCESSING OR USING THIS SITE. BY ACCESSING OR USING THIS SITE, YOU AGREE
TO BE BOUND BY THE TERMS AND CONDITIONS SET FORTH IN THE DISCLAIMER. GlobalRPH
does not directly or indirectly practice medicine or provide medical services and therefore assumes no
liability whatsoever of any kind for the information and data accessed through the Service or for any
diagnosis or treatment made in reliance thereon.

David F. McAuley, Pharm.D., R.Ph. GlobalRPh Inc.

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