AZELEX- azelaic acid cream

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

azelaic acid (UNII: F2VW3D43YT) (azelaic acid - UNII:F2VW3D43YT)

Available from:

Physicians Total Care, Inc.

INN (International Name):

azelaic acid

Composition:

azelaic acid 0.2 g in 1 g

Administration route:

CUTANEOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

AZELEX® Cream is indicated for the topical treatment of mild-to-moderate inflammatory acne vulgaris. AZELEX® Cream is contraindicated in individuals who have shown hypersensitivity to any of its components.

Product summary:

AZELEX® Cream is supplied in a closed orifice tube with a white, spiked screwcap in the following sizes: 30 g - NDC 54868-4442-0 Note: Protect from freezing. Store product on its side. Store between 15° - 30° C (59° - 86° F). Rx Only. Distributed by: Irvine, California 92612, U.S.A. ©2004 Allergan, Inc. Made in Italy 8466X Distributed under license. ® Mark of Allergan, Inc. Revised May 2004 70896US15P Additional barcode labeling by: Physicians Total Care, Inc. Tulsa, Oklahoma        74146

Authorization status:

New Drug Application

Summary of Product characteristics

AZELEX - AZELAIC ACID CREAM
PHYSICIANS TOTAL CARE, INC.
----------
AZELEX®
(AZELAIC ACID CREAM) 20%
FOR DERMATOLOGIC USE ONLY
NOT FOR OPHTHALMIC USE
DESCRIPTION
AZELEX (azelaic acid cream) 20% contains azelaic acid, a naturally
occurring saturated dicarboxylic
acid.
Structural Formula: HOOC-(CH ) -COOH
Chemical Name: 1,7-heptanedicarboxylic acid
Empirical Formula: C H O
Molecular Weight: 188.22
ACTIVE INGREDIENT: Each gram of AZELEX contains azelaic acid.........
0.2 gm (20% w/w).
INACTIVE INGREDIENTS: cetearyl octanoate; glycerin; glyceryl stearate
and cetearyl alcohol and cetyl
palmitate and cocoglycerides; PEG-5 glyceryl stearate; propylene
glycol; and purified water. Benzoic
acid is present as a preservative.
CLINICAL PHARMACOLOGY
The exact mechanism of action of azelaic acid is not known. The
following _in vitro_ data are available,
but their clinical significance is unknown. Azelaic acid has been
shown to possess antimicrobial activity
against _Propionibacterium acnes and Staphylococcus epidermidis._ The
antimicrobial action may be
attributable to inhibition of microbial cellular protein synthesis.
A normalization of keratinization leading to an anticomedonal effect
of azelaic acid may also contribute
to its clinical activity. Electron microscopic and immunohistochemical
evaluation of skin biopsies from
human subjects treated with AZELEX Cream demonstrated a reduction in
the thickness of the stratum
corneum, a reduction in number and size of keratohyalin granules, and
a reduction in the amount and
distribution of filaggrin (a protein component of keratohyalin) in
epidermal layers. This is suggestive of
the ability to decrease microcomedo formation.
PHARMACOKINETICS: Following a single application of AZELEX Cream to
human skin _in vitro_, azelaic
acid penetrates into the stratum corneum (approximately 3 to 5% of the
applied dose) and other viable
skin layers (up to 10% of the dose is found in the epidermis and
dermis). Negligible cutaneous
metabolism occurs after topical application. Approximately 4% of the