Acido Azelaico/Azelaic Acid is a naturally occurring dicarboxylic acid produced by Malassezia furfur and found in whole grain cereals, rye, barley, and animal products. Azelaic acid possesses antibacterial, keratolytic, comedolytic, and anti-oxidant activity. Azelaic acid is bactericidal against Propionibacterium acnes and Staphylococcus epidermidis due to its inhibitory effect on the synthesis of microbial cellular proteins. Azelaic acid exerts its keratolytic and comedolytic effects by reducing the thickness of the stratum corneum and decreasing the number of keratohyalin granules by reducing the amount and distribution of filaggrin in epidermal layers. Azelaic acid also possesses a direct anti-inflammatory effect due to its scavenger activity of free oxygen radicals. This drug is used topically to reduce inflammation associated with acne and rosacea.
Azelaic acid is a saturated dicarboxylic acid found naturally in wheat, rye, and barley. It is also produced by Malassezia furfur, also known as Pityrosporum ovale, which is a species of fungus that is normally found on human skin. Azelaic acid is effective against a number of skin conditions, such as mild to moderate acne when applied topically in a cream formulation of 20%. It works in part by stopping the growth of skin bacteria that cause acne, and by keeping skin pores clear. Azelaic acid’s antimicrobial action may be attributable to inhibition of microbial cellular protein synthesis.
Another Name of Azelaic Acid
- 1,9-nonanedioic acid
- Acide azélaïque
- Ácido azelaico
- Acidum acelaicum
- Acidum azelaicum
- Anchoic acid
- Azelaic acid
- Azelainsäure
- Lepargylic acid
- n-nonanedioic acid
- Nonandisäure
- Nonanedioic acid
Mechanism of Action of Azelaic Acid
The exact mechanism of action of azelaic acid is not known. It is thought that azelaic acid manifests its antibacterial effects by inhibiting the synthesis of cellular protein in anaerobic and aerobic bacteria, especially Staphylococcus epidermidis and Propionibacterium acnes. In aerobic bacteria, azelaic acid reversibly inhibits several oxidoreductive enzymes including tyrosinase, mitochondrial enzymes of the respiratory chain, thioredoxin reductase, 5-alpha-reductase, and DNA polymerases. In anaerobic bacteria, azelaic acid impedes glycolysis. Along with these actions, azelaic acid also improves acne vulgaris by normalizing the keratin process and decreasing microcomedo formations. Azelaic acid may be effective against both inflamed and noninflamed lesions. Specifically, azelaic acid reduces the thickness of the stratum corneum, shrinks keratohyalin granules by reducing the amount and distribution of filaggrin (a component of keratohyalin) in epidermal layers, and lowers the number of keratohyalin granules.
Indications of Azelaic Acid
- For the topical treatment of mild-to-moderate inflammatory acne vulgaris.
- Acne Vulgaris
- Inflammatory lesions caused by rosacea
- Azelaic acid 20% cream is used topically in the treatment of mild to moderate inflammatory acne vulgaris. The drug is not indicated in the treatment of noninflammatory acne vulgaris.
- Azelaic acid 15% gel is used topically for the treatment of inflammatory lesions (papules and pustules) associated with mild to moderate rosacea in adults. In 2 clinical studies in adults with mild to moderate papulopustular rosacea, therapy with azelaic acid 15% gel (applied twice daily for 12 weeks) resulted in a 50-58% reduction in the number of papules and pustules compared with a 38-40% reduction in patients receiving vehicle alone.
- The physiopathologic mechanism of acne seems to be dependent on four main factors: a) sebum production and excretion; b) type of keratinization of the follicular channel; c) microbial colonization of the pilosebaceous unit and d) inflammatory reaction of the perifollicular area. Azelaic acid is effective in the treatment of acne because it possesses activity against all of this factor.
- Azelaic acid is also used as a topical gel treatment for rosacea, due to its ability to reduce inflammation.[rx] It clears the bumps and swelling caused by rosacea. Azelaic acid has been used for the treatment of skin pigmentation including melasma and postinflammatory hyperpigmentation, particularly in those with darker skin types. It has been recommended as an alternative to hydroquinone. As a tyrosinase inhibitor, azelaic acid reduces the synthesis of melanin.
Contraindications of Azelaic Acid
- Data or information not available
Dosage of Acidum Acelaicum
Strengths: 20%; 15%; 15% with emollients
Acne
- 20% Cream Formulations: Apply a thin layer to the affected area(s) 2 times a day
Acne Rosacea
- 15% Gel/Foam Formulations: Apply a thin layer to the affected area(s) 2 times a day
Pediatric Dose for Acne
12 years and older
- 20% Cream Formulations: Apply a thin layer to the affected area(s) 2 times a day
Side Effects Of Acido Azelaico
The Most Common
- Burning, stinging, or tingling of the skin
- dryness, itching, peeling, or redness of the skin
- ashen-grey discoloration of the skin
- blistering, peeling, or loosening of the skin
- bloody or cloudy urine
- chills or fever
- cough
- decreased amount of urine or less frequent urination
- increased sensitivity of the skin to sunlight, especially for patients with burns on large areas
- red skin lesions, often with a purple center
- sore throat
- sores, ulcers, or white spots on lips or in mouth
- swollen glands
- unusual bleeding or bruising
- unusual tiredness or weakness
Common
- signs of kidney problems (e.g., increased urination at night, decreased urine production, blood in the urine)
- signs of liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
- any mouth sores
- cold or flu-like symptoms (such as fever or sore throat)
- confusion
- changes in mood or emotions
- difficulty sleeping or nightmares
- headache
- loss of appetite
- stomach pain
- tiredness or fatigue
- vomiting
- weakness
Rare
- signs of posterior encephalopathy syndrome (e.g., headache, seizures, visual disturbances, altered mental state)
- signs of reduced red blood cells (e.g., fatigue, a general feeling of being unwell, weakness, dizziness, fainting, pale skin, pale stool)
- swelling or tingling in your hands or feet
- blistering, peeling, or loosening of the skin
- blue-green to black skin discoloration
- dark urine
- fever with or without chills
- general body swelling
- increased sensitivity of the skin to sunlight, especially in patients with burns on large areas
- joint pain, stiffness, or swelling
- large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
- swelling of the eyes
- nausea or vomiting
- pinpoint red spots on the skin
- red skin lesions, often with a purple center
- red, swollen skin
- Blurred vision
- muscle cramps
- numbness or pain in the legs
Drug Interactions of Acido Azelaico
Since caffeine, alcohol, isotretinoin the nicotine from cigarettes or street drugs can affect the action of many medications, you should let your prescriber know if you use them. Depending on your specific circumstances, your doctor may want you to
- stop taking one of the medications,
- change one of the medications to another,
- change how you are taking one or both of the medications, or
- leave everything as is.
Pregnancy Category of Acido Azelaico
Pregnancy
This medication should not be used during pregnancy unless the benefits outweigh the risks. If you become pregnant while taking this medication, contact your doctor immediately.
Breast-feeding
This medication may pass into breast milk. If you are a breast-feeding mother and are using azelaic acid, it may affect your baby. Talk to your doctor about whether you should continue breast-feeding. The safety and effectiveness of using this medication have not been established for children.
References
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