Evaluation of Azelaic Acid for NonPrescription Use

1
Evaluation of Azelaic Acid for Non-Prescription
Use

• Michelle Brown
• Andy Reynolds
• Ted Williams
• Pharm. D candidates
• OSU College of Pharmacy

2
Project Methodology

• Divide and Conquer
• RCS Methodology
• Research
• Collaborate
• Synthesize

TM
3
Search Strategy

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

4
Disease State

• Definition
• Causes
• Progression
• Classification

5
Diseases

• Mild to Moderate Acne Vulgaris
• Rosacea
• Melasma

6
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

7
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

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Disease State Progression

• Normal Follicle

9
Disease State Progression

• Microcomedo

10
Disease State Progression

• Open Comedo
• Blackhead

11
Disease State Progression

• Closed Comedo
• Whitehead

12
Disease State Progression

• Papule
• Enflamed lesion

13
Disease State Progression

• Pustule
• Enlarged papule
• Pus filled
• Raised
• Reddened

14
Disease State Progression

• Nodule (or Cyst)
• Inflammation penetrates
• deeper into skin
• May lead to scarring
• or pitting

15
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

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Drug Information

• Drug Requested/Indications
• Pharmacokinetics
• Pharmacology
• Dose
• Adverse Effects

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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

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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

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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

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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 . . .

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Adverse Effects

• Common Effects
• Itching
• Burning
• Stinging
• Tingling
• Scaling
• Dry skin
• Irritation at application site
• Depigmentation of skin

22
Adverse Effects

• Rare Effects (lt1)
• Worsening of asthma
• Hypertrichosis
• Reddening of skin
• Exacerbation of recurrent herpes labialis

23
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

24
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)

25
Cost
26
Conclusions

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

27
References

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  URLOnline http//online.factsandcomparisons.com/
  
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  Newton G, Oszko M, Popovich N, Rollims C, et al.
  Handbook of Nonprescription Drugs 2004913-927.
• The Red Book, (2003).
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