Transcript Evalulation of Azelaic Acid for Non

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
TM
• RCS Methodology
– Research
– Collaborate
– Synthesize
Search Strategy
• Relied primarily on MedLine search
• Used tertiary resources at the discretion of
the author
• One dermatologist interview
Disease State
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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
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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:
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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
Name
Manufacturer
Quantity/Price
Quantity/Price
AW Price
Retail Price
Azelaic Acid
Gallipot
500 gm
($156.00)
Azelex cream 20%
Allergan
30 gm
($48.53)
benzoyl peroxide
(aqueous) gel 2.5%
Glades
60 gm
($17.82)
benzoyl peroxide
(aqueous) gel 5%
Glades
60 gm
($18.22)
90 gm
($23.91)
$0.27-0.3
$0.170.32/gm
benzoyl peroxide
(aqueous) gel 10%
Glades
60 gm
($18.68)
90 gm
($25.06)
$0.280.31
$0.260.32/gm
$0.31
50 gm
($84.88)
$1.62$1.70
$1.84 2.26/gm
$0.30
erythromycin 2%
gel
$0.70/gm
clindamycin Pi 1%
gel
$0.95/gm
sulfacetamide
sodium and sulfur
10% ointment
Allscripts
2.5 gm
($19.31)
tretinoin 0.025%
Alpharma/USP
D
20 gm
($35.50)
45 gm
($67.20)
$7.72
$0.38/gm
$1.49$1.78
$1.011.06/gm
Conclusions
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Effective
Safe
Low Interactions
Low Pregnancy Risk
Elevated Cost
Recommended for OTC Use
References
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Facts and Comparisons 4.0 Available from URL:Online http://online.factsandcomparisons.com/
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