| Azelaic Acid Pharmacology |
| Azelaic Acid |
| About Azelaic Acid |
| Anti bacterial, Acne Product (Topical), AntiAcne,in rosacea treatment, a hair growth stimulant. |
| Mechanism of Action of Azelaic Acid |
| Azelaic acid is used in acne vulgaris due to its antimicrobial and an anti-keratinizing effect on the follicular epidermis. The antimicrobial effect is due to inhibition of synthesis of microbial cellular proteins. Azelaic acid possesses bacteriostatic and bactericidal (at high concentrations) properties against Staphylococcus epidermidis and Propionibacterium acnes which produce acne By reducing the concentration of bacteria present on the skin, Azelaic acid decreases the inflammation associated0 with acne lesions. Azelaic acid also possesses a direct anti-inflammatory effect by scavenging oxygen radicals. The anti-keratinizing effects of Azelaic acid may be due to decreased synthesis of filaggrin (keratin filament aggregating protein). By inhibiting filaggrin, Azelaic acid normalizes the keratinization of the follicle and produces a reduction in non-inflamed acne lesions. Azelaic acid does not affect sebum excretion The antiproliferative and cytotoxic actions of Azelaic acid may be due to reversible inhibition of a variety of oxido-reductive enzymes including DNA polymerase, tyrosinase, and mitochondrial enzymes of the respiratory chain. At the cellular level, Azelaic acid causes mitochondrial swelling and accumulation of cytoplasmic lipid droplets. Azelaic acid has shown efficacy in treating lentigo, cutaneous malignant melanoma, and melasma (chloasma). When Azelaic acid is applied topically in these conditions, there is a reduction in epidermal melanogenesis and replacement of abnormal melanocytes by normal cells; flattening of nodular areas may also occur. Hyperactive and malignant melanocytes are much more susceptible to the effects of Azelaic acid than are normal melanocytes. |
| Pharmacokinets of Azelaic Acid |
| Absorption: About 4 % of the applied medicament is absorbed in to the systemic circulation. |
| Onset of Action for Azelaic Acid |
| N/A |
| Duration of Action for Azelaic Acid |
| N/A |
| Half Life of Azelaic Acid |
| N/A |
| Side Effects of Azelaic Acid |
| 1.Local irritation 2.Burning 3.Pruritis 4.Stinging 5.Tingling 6.Itching 7.Redness 8.Dryness 9.Peeling 10.Warmth |
| Contra-indications of Azelaic Acid |
| 1. Hypersensitivity to Azelaic acid |
| Special Precautions while taking Azelaic Acid |
| 1.Avoid contact with eyes mucous membrane 2.Stop the use of medicament if irritation occurs 3.Avoid use of Azelaic acid topical on dry chapped or irritated skin wounds or in Eczema 4.Avoid occlusive dressing |
| Pregnancy Related Information |
| Use with caution. |
| Old Age Related Information |
| Use with caution. |
| Breast Feeding Related Information |
| Use with caution. |
| Children Related Information |
| Use with caution NEONATES: contraindicated |
| Indications for Azelaic Acid |
| 1. Acne 2.Lentigo 3.Cutaneous malignant melanoma 4.Melasma (chloasma) |
| Interactions for Azelaic Acid |
| N/A |
| Typical Dosage for Azelaic Acid |
| Topical: Azelaic acid 10 – 20 % is used. Clean and dry the face apply the medicament 1-2 times daily. |
| Schedule of Azelaic Acid |
| N/A |
| Storage Requirements for Azelaic Acid |
| Store at 15 – 30 degree C. Keep out the reach of children. |
| Effects of Missed Dosage of Azelaic Acid |
| Apply the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose. |
| Effects of Overdose of Azelaic Acid |
| Give supportive measures and symptomatic treatment |