Evaluation of Azelaic Acid for Non-Prescription Use Michelle Brown Andy Reynolds Ted Williams Pharm. D candidates OSU College of Pharmacy

Project Methodology Divide and Conquer RCS Methodology –Research –Collaborate –Synthesize TM

Search Strategy Relied primarily on MedLine search Used tertiary resources at the discretion of the author One dermatologist interview

Disease State Definition Causes Progression Classification

Diseases Mild to Moderate Acne Vulgaris Rosacea Melasma

Disease State Definition Acne –chronic inflammatory disease of the pilosebaceous units in the dermis –Pilosebaceous unit location –Mainly face, back and chest –Also neck and upper arms

Disease State Causes Causes of Acne –Exact causes unknown –4 factors involved Excessive Sebum produced Hyperkeratinization of the hair follicle –Prevents shedding of the follicular keratinocytes –Leads to the formation of microscopic lesions microcomedo Accumulation of lipids and cellular debris Colonization by Propionibacterium acnes

Disease State Progression Normal Follicle

Disease State Progression Microcomedo

Disease State Progression Open Comedo –“Blackhead”

Disease State Progression Closed Comedo –“Whitehead”

Disease State Progression Papule –Enflamed lesion

Disease State Progression Pustule –Enlarged papule Pus filled Raised Reddened

Disease State Progression Nodule (or Cyst) –Inflammation penetrates deeper into skin –May lead to scarring or pitting

Disease State Classification Defined by American Academy of Dermatology –Mild Acne A few to several papules or pustules –Moderate Acne Several to many papules and pustules along with several nodules –Severe Acne Numerous or extensive papules and pustules as well as many nodules

Drug Information Drug Requested/Indications Pharmacokinetics Pharmacology Dose Adverse Effects

Drug Requested Azelaic acid 20% Azelaic acid cream= Azelex (Allergan) Skin and Mucus Membrane Agent Acne Medication FDA approved for tx. Mild to moderate acne

Pharmacokinetics Chemical structure of Azelaic acid: straight chain, saturated dicarboxylic acid Some undergoes ß-oxidation Most excreted unchanged in urine 10% cream is found in dermis and epidermis 3-5% penetrates outermost layer of epidermis 4% systemically absorbed 12 hour half-life

Pharmacology Antimicrobial ex. tetracycline, clindamycin, erythromycin, benzoyl peroxide Anti-keratinizing agent ex. Retinol Antioxidant? (result = anti-inflammatory properties) ex. Retinol Reduces size of acne lesions, prevents recurrence

Dose Wash face with mild soap or soapless cleanser Pat dry Cover affected area with thin layer of Azelaic acid 20% cream Massage into skin Do this twice daily, once in morning and once in the evening In case of missed dose...

Adverse Effects Common Effects: –Itching –Burning –Stinging –Tingling –Scaling –Dry skin –Irritation at application site –Depigmentation of skin

Adverse Effects Rare Effects (<1%): Worsening of asthma Hypertrichosis Reddening of skin Exacerbation of recurrent herpes labialis

Safety Low systemic absorption –FDA Pregnancy category B –Not passed in lactation in above baseline levels –Good option for pregnant patients vs. oral treatments No known drug interactions

Efficacy Demonstrated effective vs. no treatment Demonstrated effective vs. other topicals (benzoyl peroxide) Demonstrated effective vs. oral treatments (tetracycline) Effective in combinations with other topicals (Glycolic Acid) and oral treatments (minocycline)

Cost NameManufacturerQuantity/Price AW PriceRetail Price Azelaic AcidGallipot500 gm ($156.00) $0.31 Azelex cream 20%Allergan30 gm ($48.53) 50 gm ($84.88) $1.62- $1.70 $ /gm benzoyl peroxide (aqueous) gel 2.5% Glades60 gm ($17.82) $0.30 benzoyl peroxide (aqueous) gel 5% Glades60 gm ($18.22) 90 gm ($23.91) $ $ /gm benzoyl peroxide (aqueous) gel 10% Glades60 gm ($18.68) 90 gm ($25.06) $ $ /gm erythromycin 2% gel $0.70/gm clindamycin Pi 1% gel $0.95/gm sulfacetamide sodium and sulfur 10% ointment Allscripts2.5 gm ($19.31) $7.72$0.38/gm tretinoin 0.025%Alpharma/USP D 20 gm ($35.50) 45 gm ($67.20) $1.49- $1.78 $ /gm

Conclusions Effective Safe Low Interactions Low Pregnancy Risk Elevated Cost Recommended for OTC Use

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