1. Introduction
Acne, commonly known as acne. It is a common chronic inflammatory disease of hair follicle sebaceous glands, which occurs in adolescence. There are many factors. Generally speaking, the main reason is: the increase of androgen secretion in adolescence causes sebaceous glands to swell and secrete more sebaceous glands, and at the same time makes hair follicles and sebaceous glands keratinize and embolize. The accumulation of sebum in hair follicles is called fat embolism, that is, acne. In anaerobic environment, anaerobic bacteria such as Propionibacterium acnes proliferate in large quantities, producing lipolytic enzymes, separating sebum to produce free acids, stimulating hair follicles to cause inflammation, causing hair follicle wall damage and rupture, and deposited sebum entering the dermis, thus causing different degrees of inflammatory reactions around hair follicles. In addition, heredity, endocrine disorders, lipopolysaccharide and irritating diet, high temperature and some chemical factors also play a role in the occurrence and development of acne.
Although acne does not affect the normal physiological function of human body, it affects people's appearance and causes certain psychological burden and mental stress to patients, so pharmaceutical companies pay more and more attention to the research and development of acne drugs. According to the related literature, the acne treatment drugs and their progress were reviewed.
2. Anti-acne drugs currently used in clinic.
2. 1 azelaic acid is a naturally occurring saturated linear dicarboxylic acid, which has antibacterial and bactericidal activities against various aerobic and anaerobic bacteria in skin acne. External use of 20% azelaic acid cream can significantly reduce the density of Propionibacterium in skin microspheres and hair follicles, and reduce the content of free fatty acids in skin surface fat. 20% azelaic acid cream was marketed in France by Schering AC Company of Germany on 1989, and was approved by FDA to be marketed in the United States on 1996 for the treatment of acne.
2.2 cimetidine, this product is histamine h? Receptor blockers can inhibit gastric acid secretion caused by histamine or pentagastrin stimulation, and are clinically suitable for treating diseases such as gastric and duodenal ulcers and upper gastrointestinal bleeding. In recent years, it has been found that it has many functions such as immunomodulation, antiandrogen and antivirus. The mechanism of treating acne is to inhibit the secretion of sebaceous glands by blocking the combination of testosterone dioxygen and hair follicle receptors. It is effective for both internal and external use. 2% cimetidine cream is often used locally in clinic.
2.3 benzoyl peroxide, an organic peroxide, has strong bactericidal, exfoliating, acne dissolving and sebum secretion inhibiting effects, and is suitable for papular acne and pustular acne, with the common concentration of 1% ~ 10%. The drug can be used alone or in combination with other anti-acne drugs. For example, the "Bimaisen" gel of Rudong Ke Mei Pharmaceutical Company is "5% benzoyl peroxide +3% erythromycin", and the "Acne Ping" of Jilin Dongfang Pharmaceutical Company is 5% benzoyl peroxide ointment.
2.4 Adapalene, a new derivative of naphthoic acid, belongs to the third generation retinoic acid. It can selectively bind to retinoic acid receptor R, which can regulate the growth and differentiation of skin keratinocytes, thus regulating the differentiation of hair follicles and sebaceous epithelial cells and reducing the formation of acne. At the same time, adapalene can inhibit the chemotaxis of human polymorphonuclear granulocytes and inhibit arachidonic acid from being oxidized by lipids to produce inflammatory mediators, thus playing an anti-inflammatory role in the treatment of acne and improving inflammatory lesions. For example, the "Dafuwen" gel of French company Gaudemei is 0. 1% adapalene gel.
2.5 Oral isotretinoin drugs, drug tests show that this product has the functions of contracting sebaceous gland tissue, inhibiting sebaceous gland activity, reducing sebum secretion, reducing keratinization of epithelial cells and reducing propionibacterium acne, and is suitable for severe acne, especially for nodular cyst acne. For example, Terez from Shanghai Yan 'an Pharmaceutical Factory is isotretinoin capsules.
2.6 topical tretinoin, this product can regulate the mitosis of epidermal cells and promote the renewal of epidermal cells. Restore the growth and differentiation of diseased skin to normal. In particular, it can promote the renewal of hair follicle epithelium, prevent keratin embolism, inhibit protein production and make acne lesions subside. Its common concentration is 0.0 1% ~ 0. 1%. For example, the vitamin cream/gel of Rudong Ke Mei Pharmaceutical Co., Ltd. is 0.025% tretinoin cream/gel, and the Bangli brand Di Wei cream of Chongqing Huabang Pharmaceutical Co., Ltd. is 0. 1% and 0.025% tretinoin cream.
2.7 viaminate, vitamin a ester drugs, local use can promote the differentiation and production of epithelial cells, regulate the keratinization process, inhibit sebum secretion, inhibit propionibacterium acne, and resist inflammation. For example, Chongqing Huabang Pharmaceutical's Bangli brand "Acne King" is 0.3% viaminate cream.
2.8 Oral zinc preparation At present, the mechanism of zinc preparation in treating acne is still controversial. Some people think that the mechanism of oral zinc preparation in treating acne is that there may be absolute or relative zinc deficiency in adolescence, which leads to the disorder of androgen synthase system. It is also considered that zinc deficiency makes the vitamin A transporter synthase system disorder, reduces the level of vitamin A in serum, and makes the available vitamin A in tissues insufficient, thus affecting the normal differentiation of epidermis. Some people think that oral zinc preparation is related to the fact that zinc can reduce sebum and zinc itself has anti-inflammatory effect. At present, the commonly used oral zinc preparations are zinc sulfate, zinc gluconate and zinc glycyrrhizinate.
2.9 Oral contraceptives have a strong anti-androgen effect. It competes with dihydrotestosterone in sebaceous glands, prevents the influence of dihydrotestosterone on sebaceous glands and reduces the secretion of sebaceous glands. For example, Diane -35 from Schilling Pharmaceutical Factory in Germany is "cyproterone plus androstenol", and the FDA of the United States has also approved Norgestrel/androstenol from ortho Company for the treatment of acne.
2. 10 antibiotic, whose main mechanism is to kill the inflammatory mediators produced by Propionibacterium acne. Commonly used antibiotics for local treatment include erythromycin, clindamycin, metronidazole, chloramphenicol and clindamycin. For example, 1% chlorhexidine phosphate produced by Puqiang Pharmaceutical Factory in the United States, 2% chloramphenicol liniment produced by Fuyanning liniment in Miracle, Guilin, and the "acne king" of Dianhong Pharmaceutical Company in Kunming is clindamycin+metronidazole compound liniment. The Bimaisen gel system of Shandong Demeike is "3% erythromycin +5% benzoyl peroxide". The gel system of compound isotretinoin of Steffel Company in Britain is "2% erythromycin +0.0 15% isotretinoin". The commonly used oral antibiotics for acne are tetracycline, erythromycin, roxithromycin, minocycline, doxycycline, clindamycin and trimethoprim-sulfamethoxazole. The usual dosage of tetracycline and erythromycin is 500 ~ 1000mg/ time, twice a day.
2. 1 1 Other therapeutic drugs Some medical units in China use androgen antagonists (such as spironolactone, diethylstilbestrol and estradiol benzoate)+trace hormones (such as dexamethasone)+antibiotics for topical treatment of acne, and have also achieved good clinical results.
3. New drugs for acne are being developed.
3. 1 tazarotene is an inhibitor of protein synthesis.
3.2 nadifloxacin, a topoisomerase inhibitor of DNA.
3.3 G- 10 1, protein 50 ribosome subunit inhibitor.
3.45- aminolevulinic acid as oxidant
3.5 Androgen Antagonist Clodron
3.6 Rauvulin, a cell wall synthesis inhibitor.
3.7 MK-386 is a 5A- reductase inhibitor.
3.8 l-751788, a 5A- reductase inhibitor.
4. Conclusion
According to relevant data, nearly 80% of people aged 12 ~ 25 suffer from acne. This huge potential market has attracted many pharmaceutical companies to develop drugs to treat acne. It is predicted that the field of acne drugs may produce blockbuster drugs, so the market competition of acne drugs will become more and more fierce.
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