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Adapalene Gel

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Indication: The product can be used to 
treat common acne such
 as acne vulgaris,
Usage volume: A thin film of Adapalene Gel 
should be applied to the 
affected areas 
Product specifications: PE-Al-PE composite tube, 
5g/tube/box,15g/tube/box, 
30g/tube/box

Product introduction


Generic Name:
Adapalene Gel
Composition
Active ingredient: Adapalene
Chemical name: 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid
Chemical structure:
 

                
Molecular formular:C28H28O3
Molecular weight: 412.53
Description: A white translucent gel
Indications: The product can be used to treat common acne such as acne vulgaris, papule, pustule. It also can be used to treat acne vulgaris on the face, breast and back.
Specification: 0.1%
Dosage and Administration:
A thin film of Adapalene Gel should be applied to the affected areas of the skin once daily in the evening, after washing gently and till the affected areas dryness. The patients who should reduce the frequency of application of Adapalene gel or suspend the product may recover the the frequency of application of Adapalene gel when the patients tolerance to Adapalene was recovered. Please don’t use the cosmetic which can induce the acne.
Adverse Reactions:
During the first 2~4 weeks of treatment the common adverse reaction is erythema, dryness, scale, itching, burns or pricking pain. The mostly mild to moderate in intensity are very common. Less occurrence of adverse reaction includes: sunburn, skin irritation, unpleasant cutaneous sensations burns or pricking pain. Rarely occurrence of adverse reaction includes: acne red swelling, dermatitis, contact dermatitis, eye edema, conjunctivitis, erythema, itching, dyschromia, roseola and eczema. If the adverse reaction is severe the patients should be reduced the frequency of application of Adapalene gel or suspended the product.
Contraindications: Patients who is hypersensitivity to Adapalene or excipients should be forbiden. 
Precautions:
1. If a reaction suggesting sensitivity or chemical irritation occurs, the medication should be stopped using. After being confirmed the degree of local irritation reaction the patients should be reduced the frequency of application of Adapalene gel or should be suspended the product.
2. Exposure to sunlight, including sunlamps, dosage should be minimized during therapy. Patients who normally experience high levels exposure to sunlight, and those with inherent sensitivity to sun, should be warned to  caution especially. Use of sunscreen products and protective clothing over treated areas is recommended when sunlight cannot be avoided. Weather extremes, such as wind or cold, also may be irritating to patients under treatment with adapalene gel.
3. Avoid contacting with the eyes, lips, oral, angles of the nose, inner canthus and mucous membranes. The product should not be applied to cuts, abrasions, eczematous or sunburned skin. And it should not be used to the very severe acne or eczematous skin lesion. As with other retinoids, use of “waxing” as a depilatory method should be avoided on skin treated with adapalene gel.
For pregnant and lactation women:
The efficacy of Adapalene Gel in pregnancy has not been established. So the product should not be used during the pregnancy.
It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Adapalene Gel is administered to a nursing woman. Please don’t use the product on the breast.
Pediatric Use: Safety and effectiveness in pediatric patients below the age of 12 have not been established.
Geriatric Use: Clinical studies of Adapalene Gel include subjects 12~30 age, so it is not known whether the subjects not less than 65 years of age respond differently than the younger subjects.
Drug Interactions:
It is not known whether the drug interaction exists when combining with other drug. However the drug having the same mechanism as Adapalene such as retinoids should not be combinined with the product.
The chemical structure of Adapalene is stability and it is difficult to decompose in the air and sunlight. The animal and human studies indicate that the product has no phototoxicity and Photosensitivity. However safety in the patients who exposure to sunlight, including sunlamp have not been established. Patients using the product should avoid the sunlight and ultraviolet irradiation. The percutaneous absorption of Adapalene is very low, so the drug interactions can not occur. There is no evidence that effectiveness in some oral drug such as contraceptive drug and antibiotics has been effected by the product.
As Adapalene Gel has the potential to induce local irritation in some patients, concomitant use of other potentially irritating topical products (peeling agent, astringents and irritant substances) should cause excess irritation reaction. So the patients who using other dermatological anti-acne drug such as Erythromycin (concentration<4%), phosphate Clindamycin solution (1%) or Benzoyl peroxide Water base gel (concentration<10%) in the morning; using the product in the evening can avoid mutual degradation and accumulation irritation reaction in the two kinds of drug.
Overdodage:
Adapalene Gel is intended for topical use only. If the medication is applied excessively, no more rapid or better results will be obtained and marked redness, scaling, or skin discomfort may occur.
Pharmacology and Toxicology:
Adapalene acts on retinoid. Inflammatory in vivo and vitro model have been established. The chemical structure of Adapalene is stability and it is difficult to decompose in the air and sunlight. Mechanistically, adapalene binds to specific retinoic acid nuclear receptors but does not bind to the cytosolic receptor protein.
The dermatologic drug experimental studies with mice model domonstrate that Adapalene can treat acne and have an effect on adjusting cellular differentiation and proliferative reaction. The mechanism of Adapalene has been considered that the product can reduce the slight acne formation by normal cellular differentiation of hair follicle epithelial cells.
Adapalene is superior to retinoid in standard anti-inflammation analysis of vivo and vitro experiment. It can inhibit chemotactic responses of human polynuclear leucocyte. In addition, the product can inhibit metabolism of polymorphonuclear leukocytes by means of restraining arachidonic acid from transfering into inflammatory mediators by lipid oxidation reaction. This shows that Adapalene can relieve inflammatory reaction by cell reaction. The clinic trials indicate that Adapalene can treat the inflammatory reaction of acne (such as pustule, papule, and so on)
The oral LD50 of the product is more than 10ml/kg in mice and rats. Long term using the product can induce the same side effects as overdosage oral Vitamin A.
Animal experiments indicate that the product has carcinogenesis. When exposure sunlight the skin carcinoma incidence can increase. Adapalene did not exhibit mutagenic or genotoxic effects in vitro and in vivo. There is no reproductive toxicity in the rats administered oral doses of adapalene in amounts up to 20 mg/kg/day. Adapalene has been shown to be teratogenic in rats and rabbits when administered orally at doses representing 24 and 48 times of the maximum recommended human dose (MRHD), respectively.
Pharmacokinetics:
Absorption of adapalene through human skin is low. Serum adapalene concentration was not measured in the patients who had been administrated the product for long term in the large acne area, the analysis sensitivity was 0.15ng/ml.
After Adapalene marked with 14C was respectively administrated by (Intravenous Injection, intraperitoneal injection, oral and skin application ) in rats and by (Intravenous Injection, oral and skin application) in rabbits, the level of 14C Adapalene was high in the liver, spleen, adrenal and ovary. Adapalene can be metabolized by oxygen-demethylation, hydroxylation and binding reaction in animals. Excretion of adapalene appears to be primarily by the biliary route.
Storage: Protect in tightly closed containers, stored in a cool and dark (not more than 20℃) place.
Package: PE-Al-PE composite tube, 5g/tube/box, 15g/tube/box, 30g/tube/box
Shelf life: 24 months
Registration number: Guo-Yao-Zhun-Zi H20083655