Azelaic acid is a skincare ingredient used to treat acne and rosacea. It works by unclogging pores and reducing inflammation. It can also help fade dark spots and even out skin tone. You can find it in various forms like creams, gels, and serums. It's generally safe for most people to use, but it's always a good idea to talk to a dermatologist before adding it to your routine, especially if you have sensitive skin.

Azelaic acid is a natural dietary constituent that is thought to have antimicrobial effects. It is used in the treatment of the following conditions:

• Azelaic acid Cream Formulation:
  • Treatment of mild to moderate acne vulgaris. 
  • Azelaic acid is recommended as an adjunctive treatment for acne and particularly for post-inflammatory pigmentation by the American Association of Dermatology).
• Foam and Gel formulation):
  • Treatment of mild to moderate rosacea with papules and pustules. (Use for erythema in the absence of papules or pustules has not been evaluated).

Azelaic acid Dose in Adults

Azelaic acid Dose in the treatment of Acne vulgaris:  

• It usually comes in a cream form with 20% concentration.
• To use it, simply put a thin layer on the areas of your skin affected by acne twice a day, once in the morning and once in the evening.
• If your skin gets irritated, you can switch to applying it just once a day.
• You'll likely start seeing improvements in your skin within about four weeks of consistent use.

Azelaic acid Dose in the treatment of Rosacea:  

• In gel and foam forms, usually at a concentration of 15%.
• To use it, apply a thin layer to the affected areas of your face twice a day, once in the morning and once in the evening.
• If you don't see any improvement after 12 weeks of using it regularly.

Azelaic acid Dose in Children

Azelaic acid Dose in the treatment of Acne vulgaris:  

In children aged 12 years and above, as well as adolescents:

• Azelaic acid is commonly available as a cream, such as Azelex 20%.
• Simply apply a thin layer of the cream to the affected areas of the skin twice a day, once in the morning and once in the evening.
• If the skin gets irritated, you can switch to applying it just once a day.

Pregnancy Risk Factor B

• Azelaic acid is categorized as Pregnancy Risk Factor B.
• This means that while animal studies have shown adverse effects when the acid is taken orally, the risk to pregnant individuals from using it topically is low.
• When applied to the skin, only a tiny amount of azelaic acid gets absorbed into the bloodstream, less than 4%.

Azelaic acid use during breastfeeding:

• It's unclear whether azelaic acid is excreted in breast milk.
• When applied topically, only a small amount of the acid enters the bloodstream, less than 4%, so it's unlikely to cause a significant change in breast milk composition.
• However, caution is advised when using azelaic acid while breastfeeding.
• The manufacturer of the cream suggests being cautious, while the manufacturers of the gel and foam recommend considering whether to stop nursing or discontinue the drug, weighing the importance of treatment to the mother.

Azelaic acid Dose in Renal Disease:

• The manufacturer's labeling does not provide dosage adjustments for renal impairment when using azelaic acid.
• This is likely because the low systemic absorption of the acid makes it unlikely that it would have a significant impact on kidney function.

Azelaic acid Dose in Liver Disease:

• The manufacturer's labeling does not typically offer dosage adjustments for hepatic impairment when using azelaic acid.
• This is because the low systemic absorption of the acid means it's unlikely to have a significant effect on liver function.

Common Side Effects of Azelaic acid Include:

• Dermatologic:
  • Burning sensation of skin
  • Stinging of skin
  • Tingling of skin

Less Common Side Effects of Azelaic acid Include:

• Dermatologic:
  • Pruritus
  • Erythema
  • Skin Irritation
  • Acne
  • Contact Dermatitis
  • Desquamation
  • Xeroderma
  • Xerosis
• Local:
  • Application Site Pain
  • Application Site Pruritus

Contraindication to Azelaic acid Include:

• Using azelaic acid cream is contraindicated if you have a known hypersensitivity to azelaic acid or any component in the cream formulation.
• There are no contraindications listed in the manufacturer's labeling for the foam or gel forms of azelaic acid.

Warnings and Precautions

Hypersensitivity

• Hypersensitivity reactions, such as angioedema (swelling), difficulty breathing, swelling of the eyes or face, skin reactions, and hives, have been reported with the use of azelaic acid.
• If you experience any signs or symptoms of hypersensitivity while using azelaic acid, it's important to discontinue use and seek medical attention promptly.

Hypopigmentation

• Some cases of hypopigmentation (lightening of the skin) have been reported after using azelaic acid.
• It's important to monitor your skin for any changes in color, especially if you have a darker complexion.

Skin irritation:

• Skin irritation, such as itching, burning, or stinging, may occur, especially during the initial weeks of using azelaic acid.
• If you experience severe skin irritation or heightened sensitivity, it's advisable to discontinue its use.

Asthma

• Exacerbation of asthma has been reported in some cases with the use of azelaic acid.

Monitoring Parameters:

None required.

How to administer Azelaic acid?

• Clean and Dry Skin: Apply a thin layer of azelaic acid to clean, dry skin. Gently massage it in. After applying, make sure to wash your hands.
• Avoid Occlusive Dressings: Don't use bandages or tight wrappings over the treated area.
• Cosmetics: For foam and gel forms, you can apply cosmetics after the foam or gel has dried.
• Use Gentle Cleansers: Use mild soaps or soapless cleansing lotions when washing your face. Avoid harsh cleansers.
• Not for Certain Uses: Azelaic acid is not meant to be used internally (like in the vagina or mouth) or in the eyes.

Specific Instructions for Foam:

• Shake Well: Before using the foam, shake it well to ensure proper mixing.

Mechanism of action of Azelaic acid:

• Azelaic acid is a natural component found in whole grain cereals and can also be made by your body.
• While its exact workings aren't fully understood, it's known to have antimicrobial effects against acne-causing bacteria like Cutibacterium acnes and Staphylococcus epidermidis.
• It's thought to work by potentially reducing the formation of tiny acne-causing plugs called microcomedones.

Onset of Action (Cream):

• Within 4 Weeks: Typically, the effects of using azelaic acid cream start to become noticeable within about four weeks of starting treatment.

Absorption:

• Cream Penetration: Around 3% to 5% of azelaic acid in cream form penetrates the outermost layer of the skin, called the stratum corneum.
• Tissue Absorption: Up to 10% of the applied dose can be found in the deeper layers of the skin, including the epidermis and dermis.
• Systemic Absorption: Approximately 4% of the applied dose gets absorbed into the bloodstream.

Metabolism:

• Negligible Metabolism: After topical application, there is minimal metabolism of azelaic acid. Some may undergo beta-oxidation, breaking down into shorter chain dicarboxylic acids.

Half-life Elimination:

• Topical Use: In healthy individuals, the half-life of azelaic acid after topical application is approximately 12 hours.

Excretion:

• Primarily in Urine: Azelaic acid is primarily excreted in the urine, with most of it being eliminated unchanged as the drug itself.

International Brands of Azelaic acid:

• Acne Foundation
• Acnean
• Acnederm
• Acnederm Medicated Lotion
• Acnestop
• Acnezac
• Ami
• Anzela
• Av F Aza Acne Foundation
• Aza 20
• Azaderm
• Azalea
• Azclear
• Azeclear
• Azel
• Azelan
• Azelderm
• Azelec
• Azelin
• Aziderm
• Azogel
• Cutacelan
• Ezalic
• Finacea
• Scene
• Skinorem
• ZA
• Zelface
• Zeliris

Azelaic acid Brands in Pakistan: