Azelaic Acid and its Use for Acne

Overview

Azelaic acid is a dietary product extracted from whole-grain cereals and animal products. It is ideally formed endogenously by long chains of dicarboxylic acids, oleic acid metabolism, and the oxidation of monocarboxylic acids. It is used to treat acne vulgaris and inflammatory pustules and papules. Azelaic acid is applied topically over the skin only. It can cause eye and mucous membranes irritation if accidentally or mistakenly applied over the eyes or mucous membranes. It is available in different forms of gels, foams, and creams.

What Is the Indication of Azelaic Acid?

Azelaic acid is indicated for topical use on:

• Inflammatory papules and pustules of rosacea.

• Mild to moderate inflammatory acne vulgaris.

Dosage:

Dosage Form: Foam, gel, and creams.

Dosage Strength: 20 percent and 15 percent.

Dosage Supplied: It is supplied as a white to off-white foam color containing 0.15 grams of Azelaic acid, which is 15 percent by weight in cases of gel and foam but in creams of Azelaic acid has 20 percent, which is 0.2 grams of Azelaic acid in it.

Administration:

• Apply Azelaic acid twice a day, once in the morning followed by evening over the entire face.

• Shake the medication before using it.

• For once a use, use a small amount of Azelaic acid to cover the face with a thin layer.

• Cosmetics are applied over it.

• It is recommended to use Azelaic acid for four weeks continuously.

• It is not recommended to use it for oral, ophthalmic, or any other intravaginal use.

Contraindications:

• Azelaic acid is contraindicated in cases with hypersensitivity to any of the Azelaic acid components present in the cream or gels.

Warning and Precautions:

• Skin Reactions: Sometimes, after using Azelaic acid, hypopigmentation has been reported in a few cases. Few studies on dark complexion people have yet to be researched.

• Eyes and Mucous Membranes Irritation: Azelaic acid has also been noticed in irritation in the eyes. Hence, Azelaic acid is avoided to have contact with eyes, mouth, and mucous membranes.

Adverse Reactions:

The adverse effects of Azelaic acid are:

• Pruritus (itchy skin).

• Burning.

• Stinging.

• Tingling.

• Erythema (redness over the skin).

• Dryness.

• Rash.

• Peeling.

• Irritation.

• Dermatitis.

• Contact dermatitis.

• Allergic reactions.

• Small depigmented spots.

• Hypertrichosis (excessive hair on the body).

• Reddening and exacerbation of recurrent herpes labialis.

• Hypopigmentation.

• Eye and mucous membranes irritation if applied over eyes or mucus membranes.

Special Considerations:

• Pregnancy: There are no specific and adequate studies present to evaluate the safety and effectiveness of Azelaic acid on pregnant women. But, studies performed on animals (rats, rabbits, and monkeys) have shown no teratogenic effects on the administration of Azelaic acid.

• Nursing Mothers: Azelaic acid is passed through the maternal milk as four percent is systemically absorbed, but there is no significant change in the milk secretions. But still, the effects of Azelaic acid on nursing mothers are studied. So, it is used cautiously in nursing mothers or, if required, discontinued breastfeeding for a while until the patients use Azelaic acid.

• Pediatric Use: The safety and effectiveness of Azelaic acid are not determined in children who are below the age of 18.

• Geriatric Use: The safety and effectiveness of Azelaic acid are not determined in elderly patients as there is no adequate data present, but these patients require greater sensitivity while being treated.

For Patients:

Why Is Azelaic Acid Medication Used?

Azelaic acid is available in gels, foams, and creams. The gels and foam available are used over lesions, bumps, and swelling, usually caused by rosacea. The cream available in Azelaic acid is used to treat the pimples and swelling which are caused by acne. It belongs to the class of dicarboxylic acids, which treat acne by harming the bacteria that has been infected by pores and also decreasing the production of keratin which also leads to acne formation.

How Is Azelaic Acid Used?

Azelaic acid is applied over the skin as it is available in the form of gel, foam, and cream. It is usually applied two times a day, Once in the morning and once in the evening. It is recommended to use Azelaic acid every day at the same time. The patient should follow the instructions as recommended by the doctor. Avoid using Azelaic acid more or less; use it as prescribed by the doctor. The patients need to be very careful while applying the Azelaic acid over the skin because if it is mistakenly placed in the eyes or mouth, it can lead to irritation. And if by mistake it comes in contact with the eyes, wash the eyes thoroughly with a lot of water as it can irritate the eyes. Azelaic acid foam is flammable, so keeping it away from fire or flames is recommended.

How to Apply the Azelaic Acid Over the Skin?

The steps to apply the Azelaic acid are as follows:

• Wash the skin with water and mild soap or a soapless cleansing lotion, followed by patting with dry and soft towels, before applying Azelaic acid over the skin.

• Avoid using astringents, alcohol-based cleansers, and peeling agents while using Azelaic acid.

• Apply a very thin layer of Azelaic acid over the affected skin. Gently massage it thoroughly over the skin.

• Do not cover the areas applied with Azelaic acid with bandages or dressings.

• Apply cosmetics only after the Azelaic acid application gets dry.

• Wash the hands thoroughly with soap and water after the application is finished.

What Are the Precautions Required While Using Azelaic Acid?

Precautions required while using Azelaic acid are:

• The patient should watch if they are allergic to Azelaic acid and let the doctor know about it.

• The patient should inform the doctor about the medications being prescribed to the patient or the supplements the patient is taking.

• The patient should inform the doctor about the asthma conditions the patient is suffering.

• Inform the doctor about the pregnancy or if the patient is planning to become pregnant while using Azelaic acid.

• Inform the patient about breastfeeding if the patient is doing while using Azelaic acid.

• The patient is informed by the doctor about the pigmentation that can develop after the use of Azelaic acid. If pigmentation or unusual or abnormal changes appear on the skin, then do inform the doctor about it.

What Dietary Instructions Should the Patient Follow While Using Azelaic Acid?

If the patient is suffering from acne, then continue the normal regular diet unless the doctor recommends any other supplementary diet.

What If the Patient Misses a Regularly Scheduled Dose?

If the patient misses the regular dose, then the patient should apply the Azelaic acid soon on remembering, but if the timing for the next dose is near, then the patient should go for the next dose and skip the missed dose. Avoid the double dose application to cover the missed dose.

What Are the Side Effects of Azelaic Acid?

Azelaic acid can cause side effects, but if these side effects become severe, the patient should consult the doctor soon. Side effects of Azelaic acid are:

• Itchiness.

• Burning.

• Stinging.

• Tingling.

• Tenderness.

• Dryness.

A few side effects can be serious and require immediate doctor attention. Some serious side effects are

• Swelling of the face.

• Swelling over the throat, tongue, and eyes.

• Difficulty while swallowing.

• Hoarseness in voice.

• Rash.

• Hives.

How to Store and Dispose of Azelaic Acid?

Keep the medicine in closely tight containers. The medicine is stored at room temperature and away from heat and moisture. Avoid freezing the medicine. Keep the medicine away from the reach of children. The medicine needs to be disposed of by the gel pump after the eight wells of opening the containers.

The unrequited medicines are disposed of in a special way to prevent pets, children, or unknown people from having the medicine application. Avoid flushing the medicine in the toilet or garbage; instead, use the take-back programs, which is the best way of disposing of the unusual medicine. It is very important to keep the medicine in closely tight containers and away from children so that the children do not have the medicine unknowingly, which can cause poisoning on use.

For Doctors:

Azelaic Acid:

It is naturally formed as a saturated dicarboxylic acid. It is used for topical application over the affected skin. It has a chemical name of a 1,7-heptane dicarboxylic acid with an empirical formula of C9H16O4 and a molecular weight of 188.22. It is available in cream form.

Each gram of Azelaic acid cream contains 0.2 grams (20 percent by weight) as the active ingredient, and other inactive ingredients are also present, like benzoic acid as a preservative, cetearyl octanoate; glycerin; glyceryl stearate; Cetostearyl alcohol, cetyl palmitate; coco glycerides; PEG-5 glyceryl stearate; propylene glycol; and purified water.

Clinical Pharmacology:

Mechanism of Action:

The mechanism of Azelaic acid is unknown. But the data available have shown that Azelaic acid has an antimicrobial activity that works against Propionibacterium acnes and Staphylococcus epidermidis. This antimicrobial activity leads to the prevention of microbial protein synthesis as the keratinization process normally leads to the anti-comedonal effect of Azelaic acid. But the evaluation of the subjects noticed a decrease in a layer of stratum corneum and the size of keratohyalin granules. It has suggested the ability of micro-comedo formation has decreased.

Pharmacodynamics:

The use of Azelaic acid causes effectiveness as it is taken up by local mechanisms which are present within the skin.

Pharmacokinetics:

When a single layer of Azelaic acid is applied to human skin, then, it starts penetrating the stratum corneum, which is three to five percent of the dose applied, and the other ten percent to the epidermis and the dermis layers. No or negligible cutaneous activity occurs on Azelaic acid application. And nearly four percent is absorbed systemically. Azelaic acid is excreted in the urine unchanged and undergoes beta oxidation to shorter-chain dicarboxylic acids. And the half-life was 45 minutes after its oral use and 12 hours after its topical dose, which indicates percutaneous absorption. The plasma concentration is 20 to 80 nanograms per milliliter, and urination excretion is 4 to 28 milligrams of Azelaic acid, which is mainly on dietary intake.

Nonclinical Toxicology:

• Carcinogenesis: There was no evidence present to locate carcinogenesis in animals, as studies have shown no carcinogenicity effects. But there are no reports or studies present to evaluate the effects of Azelaic acid on humans based on carcinogenesis, as Azelaic acid is a human dietary constituent with a simple molecular structure.

• Mutagenesis: The use of Azelaic acid has been reported with no mutagenic or clastogenic effects on the animals as studies are being performed on them. But no determination of the effects on humans is present.

• Impairment of Fertility: There are no reports related to the impairment of fertility or effects on reproductive organs present in animals as being determined in studies. But there is no evidence related to the effects of Azelaic acid on the fertility of humans.

How Is It Supplied?

Azelaic acid is supplied in a closed tube with an orifice of a white, spiked screw cap, which can be of two sizes, 30 grams, and 50 grams.

How Is It Stored?

Azelaic acid is stored at 15 to 30 degrees Celsius, which is 59 to 86 degrees Fahrenheit. It is also protected from freezing.

Patient Counseling Information:

The doctor should inform the patient about the Azelaic acid.

Instructions For Administration:

• It is used topically only.

• Before applying the Azelaic acid over the face, clean the affected area with the help of mild forms of soap or lotions, which are soapless effects, followed by patting with a dry towel.

• It is recommended to use cosmetics after the Azelaic acid application gets dried over the face.

• Avoid the use of occlusive dressing and wrapping after the Azelaic acid.

• Avoiding the application of astringents, alcohol cleansers, tinctures, and peeling agents while using the Azelaic acid.

Adverse Reactions:

• If the patient notices any hypersensitivity over the face or an allergic reaction occurring on using Azelaic acid, then discontinue the use of Azelaic acid.

• Suppose the patient suffers a skin irritation like pruritis or a burning sensation over the areas of Azelaic acid application, especially in the first week of usage of Azelaic acid. If irritation is more persistent, then discontinue the Azelaic acid immediately and consult the doctor.

• The patients can also suffer from hypopigmentation or unusual or abnormal changes seen over the skin. If such a condition appears, consult the doctor and notify them of the changes.

• If mistaken, the Azelaic acid comes in contact with the eye, mouth, or mucous membranes; then it can cause irritation in the areas. The patient dealing with such a problem should contact the doctor and wash the area with excessive usage of water.

• The patients can also deal with some problems of asthma; if asthma appears or causes the worsening in the health of the patient on using Azelaic acid, then the condition requires immediate doctor attention.