Azelaic acid 5%
Proven to inhibit up to
100% of DHT where applied
Description: Azelaic acid is a naturally
occurring saturated dicarboxylic acid with the chemical name of
1,7-heptanedicarboxylic acid and a molecular weight of 188.22. Azelaic acid is
a dietary component of whole grain cereals and animal products.
Clinical Pharmacology: The exact mechanism of action of azelaic acid is not
known. The antimicrobial action may be attributable to inhibition of microbial
cellular protein synthesis. Azelaic acid at high concentrations is bactericidal
against Propionibacterium acnes and Staphylococcus epidermis and possesses
bacteriostatic properties against a variety of aerobic microorganisms,
including Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa and
Candida albicans. In vitro, azelaic acid acted as a scavenger of oxy radicals
and inhibits a variety of oxidoreductive enzymes including 5-alpha reductase,
the enzyme responsible for converting testosterone to DHT. Azelaic acid (0.1 to
3.0 mmol/l) has been shown to produce a competitive concentration dependent
inhibition of 5-alpha reductase activity in homogenates of human foreskin.
Azelaic acid is being studied for potential antimycotic and antiviral
properties. The multiple actions of azelaic acid cause a normalization of
keratinization and a decrease in the free fatty acid content of skin surface
lipids.
Pharmacodynamics: Following a single application to human skin, 3 to 5% of the
azelaic acid penetrates into the strateum corneum (up to 10% is present in the
dermis and epidermis). There is negligible cutaneous metabolism after topical
application. Approximately 4% of topically applied azelaic acid is systemically
absorbed and mainly excreted unchanged in the urine. The half-life is approximately
12 hours after topical dosing, indicating percutaneous absorption rate-limited
kinetics. After topical treatment with azelaic acid, plasma concentration and
urinary excretion are not significantly different from baseline levels.
Contraindications: Azelaic acid solutions or lotions are contraindicated in
individuals who have shown hypersensitivity to any of their components.
Warnings: There have been isolated reports of hypopigmentation after use of
azelaic acid, although there is no depigmenting effect on normal melanocytes.
Precautions: If sensitivity or severe irritation develops with the use of
Azelaic Acid treatment should be discontinued. The most common adverse
reactions occurring in approximately 1-5% of patients were pruritis, burning,
stinging and tingling, usually at the start of treatment and may last 5 to 20
minutes, especially if the skin is inflamed or broken. The adverse effects
commonly subside if treatment is continued. Other adverse reactions such as
erythema, dryness, rash, peeling, irritation and dermatitis were reported in
less than 1% of patients. The following additional adverse experiences have
been rarely reported: worsening of asthma, vitilago pigmentation,
hypertrichosis and reddening (signs of keratosis pilaris). Note: azelaic acid
will consistently lighten hyperpigmented skin (skin that is daker than normal
for a given individual) but will not typically lighten skin beyond its normal
color. Rarely, patients with dark complexions may notice hypopigmentation of
skin. There are no systemic adverse effects.
Considerations: Azelaic acid is normally found in the human diet and is not
considered to be a carcinogenic substance. Mutagenicity studies are negative
and animal studies have shown no adverse effects on fertility or reproduction.
Human problems have not been reported during pregnancy.
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