azelaic acid

Action and Spectrum

Actions and Spectrum: 

azelaic acid is a naturally occurring dicarboxylic acid commonly used to treat acne, rosacea, and hyperpigmentation. Here are some of the actions and spectrum of azelaic acid: 

• Anti-inflammatory: azelaic acid has anti-inflammatory properties that help to reduce inflammation and redness associated with acne and rosacea. 
• Anti-bacterial: azelaic acid is effective against many bacteria, including Propionibacterium acnes, one of the main bacteria responsible for acne. 
• Keratolytic: azelaic acid is a keratolytic agent, which means it helps to exfoliate the skin by breaking down dead skin cells, unclogging pores, and preventing the formation of new comedones (clogged pores). 
• Depigmenting: azelaic acid is effective in treating hyperpigmentation, such as melasma and post-inflammatory hyperpigmentation. 
• Moisturizing: azelaic acid has humectant properties, which means it helps to draw moisture into the skin and can help to hydrate dry skin. 

Drug Interaction

Adverse Reaction

Frequency Defined 

>10% 

Burning 

Tingling 

1-10% 

Pruritis 

Xerosis 

Erythema 

Scaling  

Dry skin 

Irritation 

<1% 

Contact dermatitis 

Acne 

Edema 

Black Box Warning

Contraindication / Caution

Contraindication/Caution: 

azelaic acid is generally considered safe and well-tolerated by most people; there are some contraindications and cautions to keep in mind: 

• Allergies: If you have a known allergy to azelaic acid or any other ingredients in the product, you should avoid using it. 
• Sensitivity: Some people may experience skin sensitivity or irritation when using azelaic acid. If you have sensitive skin, starting with a lower concentration and patch-test the product before using it all over your face is essential. 
• Pregnancy and breastfeeding: The safety of azelaic acid during pregnancy and breastfeeding has not been established, so it’s best to avoid using it during these times. 
• Sun sensitivity: azelaic acid can make your skin more sensitive to the sun, so it’s essential to use sunscreen and avoid prolonged sun exposure while using it. 
• Other topical medications: azelaic acid can interact with other topical medications, such as retinoids and benzoyl peroxide. It’s essential to check with your healthcare provider before using azelaic acid with other topical medications. 

Pregnancy / Lactation

Pregnancy consideration:  

azelaic acid should not be used during pregnancy.  

Breastfeeding warnings:  

azelaic acid does not affect breastfeeding. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data for the drug under this category is available. 

Pharmacology

Pharmacology: 

azelaic acid has several pharmacological properties, including: 

• Anti-inflammatory activity: azelaic acid reduces inflammation by inhibiting the production of pro-inflammatory cytokines and chemokines involved in acne and rosacea. 
• Antibacterial activity: azelaic acid is active against Propionibacterium acnes, a bacterium that contributes to the development of acne. It also has antimicrobial properties against other bacteria and fungi. 
• Keratolytic activity: azelaic acid reduces hyperkeratosis (thickening of the skin) and promotes desquamation (shedding of dead skin cells), which helps to unclog pores and prevent the formation of comedones (blackheads and whiteheads). 
• Antioxidant activity: azelaic acid has antioxidant properties that help neutralize free radicals and protect the skin from oxidative stress, leading to premature aging. 
• Depigmenting activity: azelaic acid inhibits the activity of tyrosinase, which is an enzyme that is involved in the production of melanin. This results in a reduction in hyperpigmentation, such as melasma and post-inflammatory hyperpigmentation. 

Pharmacodynamics: 

The pharmacodynamics of azelaic acid involves its interaction with various biological targets in the skin, which results in its therapeutic effects. Some of the critical pharmacodynamic properties of azelaic acid include the following: 

• Inhibition of tyrosinase activity: azelaic acid inhibits the activity of tyrosinase, which is involved in melanin production. This results in a reduction in hyperpigmentation, such as melasma and post-inflammatory hyperpigmentation. 
• Antibacterial activity: azelaic acid is active against Propionibacterium acnes, a bacterium that contributes to the development of acne. It also has antimicrobial properties against other bacteria and fungi. 
• Anti-inflammatory activity: azelaic acid reduces inflammation by inhibiting the production of pro-inflammatory cytokines and chemokines involved in developing acne and rosacea. 
• Keratolytic activity: azelaic acid reduces hyperkeratosis (thickening of the skin) and promotes desquamation (shedding of dead skin cells), which helps to unclog pores and prevent the formation of comedones (blackheads and whiteheads). 
• Antioxidant activity: azelaic acid has antioxidant properties that help neutralize free radicals and protect the skin from oxidative stress, leading to premature aging. 

Pharmacokinetics: 

Absorption 

4% of the drug is systemically absorbed 

Distribution 

The half-life is 12 hours 

Metabolism 

Negligible cutaneous metabolites are formed 

Elimination and Excretion 

The drug is excreted unchanged in the urine  

Adminstartion

Administration: 

azelaic acid is available in topical formulations and is usually applied directly to the affected skin area. It is commonly used to treat acne, rosacea, and hyperpigmentation. 

The recommended dose and frequency of use may vary depending on the treated condition and the specific product used. Typically, azelaic acid is applied once or twice a day, and following the instructions provided by the healthcare provider or the product label is essential. 

Before applying azelaic acid, cleaning and drying the affected area thoroughly is essential. The medication is then applied thinly and gently rubbed into the skin. It should be allowed to dry completely before applying any other skincare products or makeup. 

It is essential to use azelaic acid regularly to see the best results, and it may take several weeks or months before the full benefits are observed. If there is no improvement after a few months of treatment, the healthcare provider may recommend a different treatment approach. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: azelaic acid 

Pronounced: ay-ze-LAY-ik AS-id 

Why do we use azelaic acid? 

azelaic acid is used for a variety of skin conditions, including: 

• Acne: azelaic acid has antibacterial and anti-inflammatory properties that can help reduce the number of acne-causing bacteria and inflammation in the skin. 
• Rosacea: azelaic acid has anti-inflammatory properties that can help reduce the redness and inflammation associated with rosacea. 
• Hyperpigmentation: azelaic acid has been shown to inhibit the production of melanin, which can help reduce the appearance of hyperpigmentation, such as melasma and post-inflammatory hyperpigmentation. 
• Folliculitis: azelaic acid can help reduce the inflammation and irritation associated with folliculitis, an infection of the hair follicles.