Description

AZELEX ® (azelaic acid cream) contains 20% azelaic acid, naturally occurring saturated dicarboxylic acid.
Structure: HOOC - (CH2) 7 - COOH
Chemical name: 1,7 - heptanedicarboxylic acid
Empirical formula: C9H16O4
MW: 188.22
Active Ingredients: Each gram contains azelaic acid ......... AZELEX ® 0.2 g (20% w / w).
Inactive Ingredients: cetearyl bitterness, glycerin, glyceryl stearate and cetearyl alcohol and cetyl palmitate and cocoglycerides; the PEG - 5 glycerol stearate, propylene glycol and purified water. Benzoate is a preservative present.
Journal of Clinical Pharmacology
The exact mechanism of action of azelaic acid is unclear. The following data is available in vitro, but their clinical significance is unclear. Azelaic acid has been shown to have anti-Propionibacterium acnes and Staphylococcus epidermidis antibacterial activity. The antibacterial effect may be due to inhibition of microbial protein synthesis.
Led to a normalization of azelaic acid anticomedonal impact keratinocytes may also contribute to their clinical activities. Electron microscopy and immunohistochemistry from AZELEX ® cream in the treatment evaluation of skin biopsy showed in the stratum corneum, decrease in number and size of keratohyalin granules, and reduce the number and distribution of filaggrin (a protein to reduce the thickness of the epidermis component keratohyalin layer). This is the formation of a reduced ability microcomedo implied.
Pharmacokinetics: Following AZELEX ® cream single application to human skin in vitro, azelaic acid penetrated into the stratum corneum (approximately 3 to 5% of the applied dose) and other viable skin layer (up to 10% of the dose was found in the epidermis and dermis). Negligible after the topical skin metabolism. About 4%, topical application of azelaic acid is a systemic absorption. Azelaic acid is mainly excreted unchanged in the urine, but experienced some β-oxidation of short chain dicarboxylic acid. The observed semi-normal life for about 45 minutes after oral administration and 12 hours after topical, indicating percutaneous absorption rate-limiting kinetics.
Azelaic acid is a dietary ingredient (whole grains and animal products), the formation of long chain dicarboxylic acid metabolism of oleic acid, ψ-endogenous monocarboxylic acid oxidation. Endogenous serum concentrations (20 to 80 ng / ml) and daily urinary excretion of azelaic acid (4-28 mg) is highly dependent on food intake. After treatment with AZELEX ® topical cream humans, plasma concentration and urinary excretion of azelaic acid is not significantly different from baseline levels.

Indications
AZELEX ® cream is used to relieve mild to moderate inflammatory acne vulgaris topical treatment.

Taboo
AZELEX ® Cream is contraindicated show who are allergic to any of its individual components.

Warning
AZELEX ® cream is the skin only and not for ophthalmic use.

Already after use of azelaic acid in the individual reports of hypopigmentation. Since azelaic acid has not been well in the study in patients with dark complexion, these patients should be monitored for early signs of hypopigmentation.

Notes

General:
If sensitivity or severe irritation develop with the AZELEX ® cream, treatment should be discontinued, the implementation of appropriate treatment.

Patients should be noted:

To use the full prescribed treatment period AZELEX ® cream.
In order to avoid use of occlusive dressings or packaging.
In order to maintain AZELEX ® cream from the mouth, eyes and other mucous membranes. If it is exposed to the eyes, immediately with plenty of water as soon as their eyes and ask a doctor if eye irritation exists.
If they have a dark complexion, report abnormal changes in skin color of their physicians.
Part because of azelaic acid, temporary skin irritation (itching, burning or tingling), low pH values may occur AZELEX ® Cream for damaged or irritated skin usually starts treatment. However, this stimulation to continue if the treatment is usually dissipated. If it continues, AZELEX ® cream should be applied only once a day, or should stop treatment until these effects have subsided. If the trouble still exists stimulus should stop using, the patient should consult a doctor.
(See adverse reactions.)

Cancer:
Azelaic acid is a simple human molecular structure, it does not show that part of the potential carcinogenic diet, which does not belong to a class of drugs which have a concern about carcinogenicity. Therefore, animal studies, to assess and AZELEX ® cream is not necessary for carcinogenesis. In a variety of test batteries (Ames test, HGPRT test in Chinese hamster ovary cells, human lymphocyte test, dominant lethal test in mice), azelaic acid is considered to be nonmutagenic. Animal studies have shown no adverse effects on fertility.

Pregnancy:

Teratogenic effects: Pregnancy Category B
The impact of embryos was observed in Division I and Part II Research and mice treated with oral 2500 mg / kg / day of azelaic acid. Similar effect in some two observational studies, given 150-500 mg / kg / day, given the 500 mg / kg / day monkey rabbit. In these effects, that the dam within the dose range of all toxic dose. No teratogenic effects observed. There are, however, in pregnant women without adequate and well controlled study. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only really need.

Nursing mothers:
Equilibrium dialysis was used to assess milk partitioning in vitro. Azelaic acid concentration of 25 micrograms / ml, milk / plasma distribution coefficient was 0.7 and the milk / buffer distribution was 1.0, that may occur through the drugs into breast milk. As a topical application of less than 4% of the dose of systemic absorption of azelaic acid to breast milk intake, milk is not expected to result in baseline azelaic acid levels were significantly changed. However, caution should be exercised to be executed when the AZELEX ® Cream nursing mothers.

Pediatric Use:
Children's safety and effectiveness in patients under 12 years of age has not been determined.

Old Purpose:
AZELEX ® cream clinical study did not include subjects aged 65 and above in sufficient quantity to determine whether they respond to the young from different disciplines.

Adverse reactions
Cream in the United States and AZELEX ® clinical trials, adverse reactions are mild, transient in nature. About 1-5% of most common adverse reactions in patients with itching, burning, tingling, and tingling. Such as erythema, dryness, rash, peeling, redness, dermatitis, contact dermatitis and other adverse reactions were reported in less than 1% of the study. There is on the face AZELEX ® cream allergy potential.

In patients using azelaic acid formulations, the following additional adverse reactions reported rarely: aggravated asthma, vitiligo depigmentation, small depigmented spots, accompanied by more congestion (keratosis pilaris logo), recurrent cold sores and deterioration.

DOSAGE AND ADMINISTRATION
Dry skin after thorough cleansing, pat, there AZELEX ® cream should be gently massage, but deep into the affected areas twice daily, morning and evening, film. Hands should be washed following application. AZELEX ® cream in the use of time can be determined by people who, on the severity of acne. Improvement in the conditions in the four weeks the majority of patients with inflammatory lesions.

How to provide
AZELEX ® Cream is available with a white screw cap closed the following orifice tube size spikes:

30 g
50 grams

AZELEX ®（壬二酸霜）20％
AZELEX ®是一种温和的润肤和保湿配方为轻度至中度的炎症性寻常痤疮的局部治疗表示。据估计有80至11和30岁的所有民众都在一些point.1 AZELEX ®被认为与痤疮的行动爆发双模式 - 抗菌活性和角化（正常化的过程，上皮细胞，因为它们成熟走向皮肤表面，然后抛弃） - 这攻击痤疮的两个主要原因.

化学名称
壬二酸。

适应症
Azelex（壬二酸）是用于治疗轻度至中度痤疮。
Azelex霜是用于皮肤的指示，通常一天两次。要应用，清洁，擦干患处。应用在皮肤上轻轻按摩，在薄薄的一层。以及使用后洗手。不要使用大量或申请往往比这更直接。不明确你的病情会更快，但副作用的机会可能会增加。用于治疗的全部课程。避免接触或靠近眼睛或鼻子和嘴巴里。如果它在您的眼睛立即用洗出大量的水，打电话给医生，如果刺激持续。不要施加任何敷料或奶油，除非涵盖了告诉您的医生做这样的类型。

副作用
轻微刺痛或灼痛，发痒，刺痛，红肿或皮肤干燥可能会发生。如果这些症状持续或变得严重，或者如果您开发了皮疹，皮肤颜色改变或哮喘症状的恶化，通知你的医生。奶油可能会刺激可能通过每日一次，每日两次，而不是控制。咨询你的医生。如果您发现上面没有列出的其他影响，请联系你的医生或药剂师。

注意事项
在使用Azelex（壬酸），告诉你的医生，如果您有：其他疾病，任何过敏。这种药物可能会谨慎使用，而在怀孕期间或哺乳。讨论的风险和医生的利益。

药物相互作用
告诉您的医生或任何非处方或处方药，你可以使用药剂师，特别是：其他护肤产品。不要启动或停止未经医生或药剂师批准任何药物。

Azelex壬二酸霜它是一种用于治疗黄褐斑；其二作为一种抗菌剂，能进入细胞内，抑制病菌的蛋白合成，产生抑杀效果，特别对痤疮丙酸杆菌有较强的作用。壬二酸在治疗痤疮上有3个作用，即抗菌作用、抗粉刺作用和抗炎作用。国外有Azelex(20壬二酸霜剂)，每日外用2次。其不良反应为皮肤发红，但不伴有脱屑和干燥等，无光敏感性。壬二酸不但对炎症性痤疮损害有治疗作用，还可以改善痤疮后的色素沉着。壬二酸是治疗炎症性痤疮和非炎症性痤疮的一种新药。目前国内尚无正式产品供应。