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Why isotretinoin treats acne. Clinical experience with the use of isotretinoin in the treatment of severe forms of acne

Page numbers in the issue: 18-21

V.R.Khairutdinov*, Yu.G.Gorbunov, A.V.Statsenko

Federal State Educational Institution of Higher Professional Education Military Medical Academy named after. S.M.Kirova. 194044, St. Petersburg, st. Academician Lebedeva, 6

Key words: acne, isotretinoin, systemic retinoids, Sotret.

*[email protected]

For quotation: Khairutdinov V.R., Gorbunov Yu.G., Statsenko A.V. How to start using isotretinoin in acne treatment? Consilium Medicum.

Dermatology (Add.). 2016; 1: 18-21.

How to start using isotretinoin in acne therapy?

V.R.Khairutdinov*, Iu.G.Gorbunov, A.V.Statsenko

S.M.Kirov Military Medical Academy. 194044, Russian Federation, Saint Petersburg, st. Akademika Lebedeva, d. 6

The article presents practical recommendations for the prescription of systemic retinoids (isotretinoin) for acne patients. Considered evidence, examination, methods of calculation of daily and course doses of isotretinoin.

Key words: acne, isotretinoin, systemic retinoids, Sotret.

*[email protected]

For citation: Khairutdinov V.R., Gorbunov Iu.G., Statsenko A.V. How to start using isotretinoin in acne therapy? Consilium Medicum. Dermatology (Suppl.). 2016; 1:18–21.

Acne (acne vulgaris), a chronic inflammatory disease of the sebaceous glands, is one of the most common dermatoses, occurring in 80–90% of people. Damage to exposed skin due to acne causes aesthetic discomfort in patients and disrupts their quality of life. Most doctors consider acne solely as a disease of young people that does not require thorough treatment. A number of epidemiological studies clearly demonstrate that in a significant proportion of patients this disease becomes persistent. In the age groups 30–39 and 40–49 years, acne was reported in 44 and 24% of the population, respectively. The lack of timely and adequate treatment leads to the formation of scars and persistent hyperpigmented spots on the skin, and the development of psycho-emotional disorders in patients, including depression, anxiety and hypochondriacal syndrome.

The list of medications recommended for the treatment of acne includes systemic retinoids (isotretinoin), antibiotics and oral antiandrogens; For topical therapy, benzoyl peroxide, azelaic acid, antibiotics and retinoids (adapalene) are indicated. Severe forms of acne are treated with systemic isotretinoin. Monotherapy with isotretinoin has a high level of recommendations, while the prescription of antibiotics or antiandrogens has received, according to experts, a medium or low level of recommendations; combination with topical drugs is necessary. About 30% of acne patients require systemic therapy with isotretinoin.

According to the results of online voting conducted among dermatovenerologists as part of a satellite symposium organized by the pharmaceutical company Sun Pharmaceutical Industries Limited (India) at the IX Russian scientific and practical conference “St. Petersburg Dermatological Readings”, it was found that only 28, 3% of all respondents regularly use systemic isotretinoin in the treatment of acne, 40% recommended the drug only a few times, and 31.7% of specialists have never prescribed oral retinoids. Among the reasons why dermatovenerologists do not use isotretinoin, the following were selected: possible side effects - 38.6%, lack of personal experience in using the drug - 34.1%, high cost of a course of treatment - 27.3%. However, none of the doctors surveyed doubted the effectiveness of systemic retinoids in the treatment of acne.

In 2012, the drug Sotret (isotretinoin) appeared on the domestic pharmaceutical market. Sotret has been used for the treatment of acne patients in the USA since 2002, and is approved for use in the European Union and the UK.

When determining the most effective and adequate method of treating acne, a dermatovenerologist must take into account a number of criteria. First of all, it is necessary to correctly formulate a diagnosis, determine the form and severity of the disease. The method of choice for the treatment of severe papulopustular acne, nodular and conglobate acne is systemic isotretinoin. For papulopustular acne of moderate severity, it is advisable to prescribe oral retinoids if previous external therapy is ineffective, the rash is prone to scar formation, and the patient is clearly motivated for this type of treatment.

Before starting therapy with Sotret, the patient performs a biochemical blood test (lipid profile, alanine aminotransferase, aspartate aminotransferase, g-glutamyl transpeptidase, total bilirubin, glucose, creatinine). A prerequisite for prescribing the drug is the normal value of these indicators. During treatment, the patient must be examined by a dermatovenerologist at least once a month; a control biochemical blood test is carried out 1 and 3 months after the start of therapy. The most common deviation (about 30% of patients) is an increase in the levels of triacylglycerides and total cholesterol (increased content of all fractions). These changes do not lead to a significant change in the atherogenicity coefficient, are reversible and do not require any correction. A transient increase in the level of transaminases in the blood (30–40% above normal) is observed in no more than 10% of patients, which is comparable to the dynamics of these indicators in healthy people.

Patients of childbearing age are explained the teratogenic properties of isotretinoin, a pregnancy test is performed, instructions are given on contraceptive methods, and informed consent to take the drug is signed. The half-life of Sotret is 19 hours, that of its main metabolite is 29 hours. Endogenous concentrations of retinoids in the body are restored 14 days after the last dose of the drug. Pregnancy planning can be carried out 1 month after the end of therapy. Isotretinoin has no effect on spermatogenesis, and there are no contraindications for reproductive function in men when taking it.

The course dose of the drug Sotret is 120–150 mg/kg and is calculated in accordance with the patient’s body weight. The daily dose can vary from 0.3 to 1.0 mg/kg, usually starting treatment with 0.5 mg/kg per day. The use of low doses of isotretinoin (0.2–0.3 mg/kg per day) is acceptable in patients with moderate papulopustular acne and is ineffective in severe forms.

As an example, let’s calculate the course and daily doses of isotretinoin for patient K. (see figure), body weight – 60.0 kg. The patient has severe papulopustular acne (more than 30 inflammatory elements on one half of the face). With this form, the effective course dose will be 120 mg/kg: 120 mg/kg × 60 kg = 7200 mg. To make this figure clear to the patient, it is necessary to divide it into the dose of the drug in 1 capsule (20 mg) and the number of capsules in one pack (30 pieces). We get: 7200 mg: 20 mg: 30 = 12 packs (20 mg each) for the entire course of treatment. The daily dose of isotretinoin is 0.5 mg/kg, we calculate: 60 kg × 0.5 mg/kg = 30 mg/day – 2 capsules (20 mg + 10 mg) per day. The daily dose can be adjusted once a month; if the drug is well tolerated, it can be increased to 1.0 mg/kg per day; if side effects are severe, it can be reduced. To ensure accurate recording of isotretinoin intake, patients are advised not to throw away empty packs of the drug until the end of therapy.

Isotretinoin is a fat-soluble substance. Its absorption and entry into the blood (bioavailability) largely depend on the presence of lipids in the intestinal lumen. For better intestinal absorption of Sotret, it must be taken once during meals, when the fat content in food is highest (lunch, dinner). Supplementation with ω-3 unsaturated fatty acids increases the bioavailability of isotretinoin and reduces the likelihood of elevated blood triglycerides. Dividing the daily dose of the drug into 2-3 doses reduces the patient's adherence to treatment.

When prescribing therapeutic doses of Sotret, like any other systemic retinoid, side effects always develop - cheilitis, dryness and flaking of the skin of the face, hands, erythema in the facial area, which are observed in almost all patients. It is necessary to warn the patient about this in advance and prescribe external moisturizing skin care products from the 1st day of taking the drug. Regular preventive use of emollients and protective topical medications is the key to minimizing side effects. Less commonly, undesirable effects such as dryness of the mucous membranes of the eyes and nasal cavity (feeling of a foreign body in the eye, bleeding from the nose), increased hair loss, muscle-joint pain (with high physical activity) may be observed. It is important to convey to the patient information that all side effects are dose-dependent and reversible. When the daily dosage of Sotret is reduced, a decrease in adverse events is observed, and upon completion of treatment, all side effects always disappear completely.

It is important to remember about increased skin sensitivity to ultraviolet radiation during the use of topical or systemic retinoids. In this regard, it is more advisable to carry out a course of treatment with Sotret in the autumn-winter period of the year. Patients are advised to refrain from beach holidays and, in sunny weather, use external products with a photoprotective effect (sun protection factor SPF>50). The combination of systemic retinoids and tetracyclines, which also cause photosensitization and can lead to increased intracranial pressure, is extremely undesirable.

In conclusion, it should be noted that the advent of systemic isotretinoin has revolutionized our understanding of the possibilities of acne treatment. In dermatovenerology, there are few events comparable in significance to the introduction of retinoids: the discovery of antibiotics, glucocorticosteroids, the emergence of genetically engineered biological drugs.

The therapeutic effectiveness of any topical or systemic antibacterial drug recommended for the treatment of acne is significantly inferior to the effectiveness of Sotret (isotretinoin), and the clinical results obtained are usually temporary; continued treatment is necessary to maintain the achieved effect. Only after a course of isotretinoin therapy do most patients achieve stable remission (recovery) and have healthy skin.

Khairutdinov Vladislav Rinatovich– Dr. med. Sciences, Associate Professor Department of Skin and Venereal Diseases of the Military Medical Academy named after. S.M.Kirova. Email: [email protected]

Gorbunov Yuri Gennadievich– Ph.D. honey. Sciences, Associate Professor Department of Skin and Venereal Diseases of the Military Medical Academy named after. S.M.Kirova. Email: [email protected]

Statsenko Anatoly Vasilievich– Dr. med. Sciences, Associate Professor Department of Skin and Venereal Diseases of the Military Medical Academy named after. S.M.Kirova. Email: [email protected]

List of used literature

1. Rocha MA, Costa CS, Bagatin E. Acne vulgaris: an inflammatory disease even before the onset of clinical lesions. Inflamm Allergy Drug Targets 2014; 13 (3): 162–7.
2. Samtsov A.V. Acne and acneiform dermatoses. M.: Farmtek, 2014. / Samtsov A.V. Akne i akneformnye dermatozy. M.: Farmtek, 2014.
3. Schafer T, Nienhaus A, Vieluf D et al. Epidemiology of acne in the general population: the risk of smoking. Br J Dermatol 2001; 145(1):100–4.
4. Rzancy B, Kahl C. Epidemiology of acne vulgaris. J Dtsch Dermatol Ges 2006; 4(1):8–9.
5. Dawson AL, Dellavalle RP. Acne vulgaris. BMJ 2013; 346:f2634.
6. Federal clinical guidelines for the management of acne patients. M.: RODVK, 2013. / Federal "nye klinicheskie rekomendatsii po vedeniiu bol"nykh akne. M.: RODVK, 2013.
7. Nast A, Dreno B, Bettoli V et al. European evidence-based (S3) guidelines for the treatment of acne. J Eur Acad Dermatol Venereol 2012; 26 (1): 1–29.
8. Silverberg JI, Silverberg NB. Epidemiology and extracutaneous comorbidities of severe acne in adolescence: a U.S. population based study. Br J Dermatol 2014; 170:1136–42
9. Center for drug evaluation and research. Appl. No. 76-041. URL: http://www.accessdata.fda.gov/drugsatfda_docs/nda/2002/076041.pdf
10. Kungurov N.V., Kokhan M.M., Shabardina O.V. Experience in treating patients with moderate and severe acne with isotretinoin. Vestn. dermatology and venereology. 2013; 1:56–62. / Kungurov N.V., Kokhan M.M., Shabardina O.V. Opyt terapii bol"nykh srednetiazhelymi i tiazhelymi akne preparatom izotretinoin. Vestn. dermatologii i venerologii. 2013; 1: 56–62.
11. Perlamutrov Yu.N., Olkhovskaya K.B. Modern aspects of effective therapy for acne vulgaris. Ross. magazine skin and venereal diseases. 2014; 17 (5): 51–4. / Perlamutrov Iu.N., Ol"khovskaia K.B. Sovremennye aspekty effektivnoi terapii acne vulgaris. Ros. zhurn. kozhnykh i venericheskikh boleznei. 2014; 17 (5): 51–4.
12. Statsenko A.V., Belousova I.E., Khairutdinov V.R. and others. Clinical experience with the use of isotretinoin in the treatment of severe forms of acne. Effective pharmacotherapy. 2014; 4:4–7. / Statsenko A.V., Belousova I.E., Khairutdinov V.R. i dr. Klinicheskii opyt primeneniia izotretinoina v terapii tiazhelykh form akne. Effektivnaia farmakoterapiia. 2014; 4:4–7.
13. Isotretinoin: instructions, use and formula. Register of Medicines of Russia (RLS). URL: http://www.rlsnet.ru/mnn_index_id_1162.htm/ Izotretinoin (Isotretinoin): instructions, primenenie i formula. Registr lekarstvennykh sredstv Rossii (RLS). URL: http://www.rlsnet.ru/mnn_index_id_1162.htm
14. Lee JW, Yoo KH, Park KY et al. Effectiveness of conventional, low-dose and intermittent oral isotretinoin in the treatment of acne: a randomized, controlled comparative study. Br J Dermatol 2011; 164(6):1369–75.
15. Colburn WA, Gibson DM, Wiens RE et al. Food increases the bioavailability of isotretinoin. J Clin Pharmacol 1983; 23 (11–12): 534–9.
16. Krishna S, Okhovat JP, Kim J, Kim CN. Influence of ω-3 fatty acids on triglyceride levels in patients using isotretinoin. JAMA Dermatol 2015; 151(1):101–2.
17. Perlamutrov Yu.N., Olkhovskaya K.B. Treatment of patients with severe and moderate acne. Vestn. dermatology and venereology. 2015; 3: 141–6. / Perlamutrov Iu.N., Ol"khovskaia K.B. Terapiia bol"nykh s tiazheloi i srednei stepen"iu tiazhesti akne. Vestn. dermatologii i venerologii. 2015; 3: 141–6.
18. Chivot M. Retinoid therapy for acne. A comparative review. Am J Clin Dermatol 2005; 6 (1): 13–9.

Acne is a multifactorial disease, the main development factors of which are:

  • advanced education,
  • violation of hair follicles,
  • with the development of inflammation.

Among the drugs used, they only act on ALL factors of acne development. Other drugs for the treatment of acne have one-sided activity, so these drugs have to be combined.

Treatment of mild to moderate acne

For effective acne treatment easy 1 drug is sufficient. For acne average severity, it is necessary to combine drugs to influence all factors of pathogenesis. The most successful combination is with:

  • retinoids slow down the formation of comedones, reduce the formation of sebum and improve exfoliation of the epithelium.
  • antibiotics and antimicrobials count bacteria on the skin and have an anti-inflammatory effect.

Solutions are usually prescribed in the morning, and creams or gels - for the night:

  • Zenerit solution + Retinoic ointment,
  • Zenerit + adapalene (Differin gel/cream or Klenzit gel),
  • (Baziron AS gel) + Retinoic ointment,
  • gel Baziron AC + adapalene,
  • Retasol solution + gel/cream with clindamycin (Dalacin, Clindavit).

Retinoids(and to a lesser extent salicylic acid) reduce the formation of comedones, so they are very important for long-term acne treatment. Retinoids also thin the superficial (stratum corneum) layer of the epidermis, which makes it easier for other medications to penetrate and enhances the overall effect of the treatment.

For more severe acne, it is prescribed, and locally - topical retinoids 2 times a day.

Treatment of severe forms of acne

  • benzoyl peroxide + topical antibiotics (erythromycin or clindamycin),
  • or topical retinoids + topical antibiotics.

As supportive Treatment after the end of systemic therapy is used:

  • in the morning - topical antibiotic or benzoyl peroxide,
  • at night - a topical retinoid.

Selection drug basics (solutions, gels, creams, ointments) should provide the best tolerability of acne treatment. With seborrhea ( increased function of the sebaceous glands) in the morning, solutions are prescribed for a neat and dry appearance of the skin, and in the evening, gels or creams are recommended to prevent peeling and excessive dryness. A combination of 2 forms with isotretinoin is considered successful: Retasol solution + Retinoic ointment.

External treatment with a combination of:

  • clindamycin phosphate
  • + benzoyl peroxide
  • + salicylic acid.

Used ready-made combination drugs:

  • gel Klenzit S (adapalene + clindamycin),
  • gel Isotrexin (isotretinoin + erythromycin),
  • solution Zenerite (zinc acetate + erythromycin),
  • new gel Effezel (0.1% adapalene + 2.5% benzoyl peroxide).

I talked about the main causes of acne. Brief summary: acne is caused by true or false hormonal imbalance. In the comments there was something like: “Well, I don’t know, my friend’s dysbacteriosis was found, treated, everything returned to normal.”

Here I want to talk a little about something painful: the diagnosis of “dysbacteriosis” or “dysbiosis” is a myth of Russian medicine, or more precisely, of its individual representatives. There is no such disease in the International Classification of Diseases, Tenth Revision (ICD-10 ICD-10). Moreover, it is not included in the regulatory document of the Ministry of Health of the Russian Federation “Standards (protocols) for the diagnosis and treatment of diseases of the digestive system.” Therefore, there is no need to treat it and it cannot affect acne. You can drink kefir to calm yourself.

And a little from myself: I have never had any stomach problems in my life, I don’t even have gastritis. And there were acne. C'est la vie.

Let's return to our pimples, that is, sheep. The main areas of systemic therapy are retinoids, antiandrogens and antibiotics. Systemic therapy is an effect on the entire body, in this case in most cases it is taken orally. I will dwell in detail only on systemic retinoids. Your gynecologist can tell you better about antiandrogens (oral contraceptives) than I can, I’ll just say that they work, yes (I hope it’s clear why?). I think taking antibiotics orally is pointless. As an external remedy as monotherapy, too. This is my personal opinion. In the next post I will explain why.

However, despite the impressive results of systemic basic therapy, achieving an aesthetic treatment result is impossible without external influence.*

*Protsenko T.V., Kaplan A.V. Innovative approaches to external therapy of common acne //Ukrainian Journal of Dermatology, Venereology, Cosmetology. – 2007. – No. 2. – pp. 12-14.

So, the gold standard for acne treatment is retinoids and benzoyl peroxide.

In this post I will talk about retinoids.

Retinoids have found very wide use in dermatological practice since 1963, when the effectiveness of retinoic acid was proven for acne.*

* Protsenko T.V. Local therapy of acne vulgaris using fixed combinations of drugs (literature review) //Ukr. magazine dermatol., venereol., cosmetol. – 2010. – T. 2010. – P. 55t61.

Retinoids are a chemically related class of compounds to retinol, its biological forms, as well as structural synthetic derivatives, which differ significantly from the isoprene structure of natural vitamin A, but act in a similar way: through the activation of nuclear retinoic receptors, they regulate the processes of proliferation, differentiation and intercellular communication.*

*Batkaev E. A., Molodova Yu. S. Acnecutane in the treatment of acne: a new low-dose regimen // Klin. dermatol. and venerol. – 2014. – T. 2014. – P. 84t89.

Simply put, retinoids are structural analogues of vitamin A.

The term "retinoid" is used as a general designation for any substance, both synthetic and natural. The mechanism of action of retinoids is based on reducing the secretion of sebum, normalizing follicular hyperkeratosis and suppressing the activity of bacteria. In addition, it has an anti-inflammatory effect*

*Korneva L.V. Treatment of severe forms of acne vulgaris // Almanac of Clinical Medicine. 2007. No. 15. P.194-198

All retinoids can be divided into 3 (some authors divide into 4) generations:

1) derivatives of retinoic acid - retinol (aka vitamin A), retinal (aka retinaldehyde), tretinoin (aka all-trans-retinoic acid, or ATRA), isotretinoin (aka 13-cis-retinoic acid), alitretinoin;

2) etretinate and its metabolite acitretin;

3) adapalene, bexarotene, tazarotene.

Retinoids are also divided into natural, which are synthesized in the human body, and synthetic, which are obtained in the laboratory. Natural ones include first-generation retinoids, and synthetic ones include second- and subsequent-generation retinoids.

Some first-generation retinoids are widely used for the treatment of acne, second-generation retinoids are used as systemic drugs for the treatment of psoriasis and dermatoses, tretinoin, isotretinoin, bexarotene and alitretinoin are also used in oncological practice, and adapalene, although not essentially a retinoid, has proven itself An excellent remedy for treating acne.

Since the topic of our meeting is the treatment of acne, I will dwell in detail on those retinoids that are effective in the treatment of acne.

Retinol is a true vitamin A. Fat-soluble vitamin, antioxidant. In its pure form it is unstable and is found in both plant products and animal sources. Participates in redox processes, regulation of protein synthesis, promotes normal metabolism, the function of cellular and subcellular membranes, plays an important role in the formation of bones and teeth, as well as fat deposits; necessary for the growth of new cells, slows down the aging process.

Retinaldehyde/retinal is an aldehyde of retinoic acid, which is very actively used in cosmetology. Upon penetration into the dermis, it is easily converted into retinoic acid with subsequent beneficial and side effects.

Isotretinoin is 13-cis-retinoic acid. Biologically active form of retinoic acid synthesized naturally in small quantities in the human body; has a positive effect on the differentiation of keratinocytes and suppresses the production of sebaceous glands. In many cases, it allows you to completely inhibit excess sebum production and normalize the regenerative functions of the skin. The form is unstable and, when interacting with the internal microflora of the body, it turns into tretinoin (trans-retinoic acid), therefore it is less active compared to tretinoin.

Tretinoin is trans-retinoic acid. The carboxylic acid form of vitamin A is a natural metabolite of retinol. When applied externally, it increases cell proliferation in the papillary layer of the skin, reduces the adhesion of cells involved in the formation of acne vulgaris. When treating open acne, it helps smooth the skin surface without signs of inflammation. When treating closed blackheads, it promotes their transition to open blackheads or papules, which then heal without scarring after removal of the keratin plug. Prevents the formation of new acne. In addition to its therapeutic effect on acne, retinoic acid has a stimulating effect on fibroblasts, which synthesize the extracellular matrix, including collagen, hyaluronic acid and elastin.

Adapalene is a derivative of naphthoic acid with a retinoid-like effect. Adapalene molecules are resistant to sunlight and oxygen, and due to their lipophilicity, they quickly penetrate the upper layers of the skin. It is believed that it does not penetrate well into the deep layers of the skin, which ensures its high concentration in the upper layers, therefore it is more suitable for acne therapy.

Retinoids are either topical (for external use) or systemic (for oral use). When used externally and systemically, retinoids have anticomedogenic, sebostatic, anti-inflammatory, kerato- and immunomodulatory effects, activate regeneration processes in the skin, stimulate collagen synthesis, increase the production of mucopolysaccharides and glycosaminoglycans.

All drugs in this group have these effects to one degree or another, but they are most pronounced in retinoic acid. Retinoic acid exists as two isomers: all-trans retinoic acid (tretinoin) and 13-cis retinoic acid (isotretinoin). Both isomers are used in dermatology to treat acne. 13-cis-retinoic acid has better bioavailability.*

*Albanova V.I., Sazykina L.N. TREATMENT OF ACNE //NEW DOMESTIC MEDICINE FOR SCABIES. – T. 13.

Topical retinoids use retinol, retinal, tretinoin, isotretinoin, and adapalene as the active ingredient. Existing in different forms of release (ointments, creams, gels) and under different brands. Let's look at some of them.

Retinol is widely used in cosmetics. It has a similar effect on the skin as tretinoin, although it requires higher concentrations. It has proven effective in thickening the epidermis, improving skin texture and lightening pigmentation. There are plenty of funds on the market, there is plenty to choose from. I can’t recommend anything, since retinol has never been interesting to me.

Adapalene was developed by the French company Galderma Laboratories. Available in the form of cream and gel in various concentrations, in Russia and some other countries it is registered under the name “Differin”. There is a generic from the Israeli company Teva, but it is not available in Russia.

Tretinoin is available in cream, gel, liquid and solid form. The most famous brand names: Retin-A (Silag, Switzerland, a division of Johnson and Johnson), Retin-A micro (patent of Valent Pharmaceuticals, Canada), Airol (Roche, Switzerland), Lokacid (Pierre Fabre, France), Renova (Valent Pharmaceuticals, Canada). Not registered in Russia and a number of other countries. In the USA it is available by prescription.

Isotretinoin is a topical and systemic retinoid. Registered in Russia. As a means for external use, it is available in the form of ointments. The most famous brand in Russia is Retinoic ointment (FNPP "Retinoids"), also produced under the name Isotrex (Glaxosmithkline, UK), in combination with erythromycin - under the name Izotrexin (Glaxosmithkline, UK).

As a systemic retinoid it is known under the brands Roaccutane (Roche, Switzerland), Acnecutane (Jadran, Croatia), Curacne (Pierre Fabre, France). Prescribed by a doctor and issued strictly according to prescription.

Important Note: all retinoids (including seemingly harmless vitamin A in large dosages) cause side effects and are teratogens, that is, they can cause irreversible defects in the fetus. A reservation, perhaps, can only be made for Adapalene, whose teratogenic effect has not been proven. This is most likely due to the fact that not enough research has been conducted. Therefore, we will conditionally classify it as a teratogen. In this regard, women of childbearing age are prescribed systemic retinoids with reliable contraception and a negative pregnancy test. In the medical history, a note is usually made about the woman's awareness of possible side effects. Retinoids do not have a negative effect on the reproductive function of men. *

* Albanova V.I., Sazykina L.N. TREATMENT OF ACNE //NEW DOMESTIC MEDICINE FOR SCABIES. – T. 13.

Retinoids also cause the following side effects: dry skin, mucous membranes, including lips (cheilitis), nasal cavity (bleeding), laryngopharynx (hoarseness), eyes (conjunctivitis, contact lens intolerance). An exacerbation reaction may occur, expressed in redness, moderate itching of the skin, and the appearance of additional rashes. Side effects usually disappear or are minimized after some time. *

* Safonova T. G. et al. Systemic retinoids in the treatment of severe and resistant forms of acne // Clinical dermatology and venereology. – 2013. – T. 11. – No. 3. – pp. 60-62.

All retinoids increase photosensitivity, so during the treatment period it is necessary to protect yourself from the sun and avoid direct sunlight (and it is better to do this for the rest of your life).

Many people are afraid of systemic retinoids, especially when they open the instructions from the box. Where complications and side effects are written in bold red font. And not all doctors have complete information.

But in some cases, systemic retinoids are practically the only remedy that can lead to stable remission. Now microdoses are used to achieve the effect and side effects occur much less frequently. There is a misconception that isotretinoin has a long half-life and that you cannot become pregnant for another 2 years, but this is not true. “The half-life of isotretinoin is only 19 hours, but protection from pregnancy is necessary for the entire period of therapy and 1 month. after its completion. Side effects can indeed accompany the course of treatment, but in most cases we are talking about cheilitis and dry skin. Other side effects, such as transient changes in transaminases, headache, myalgia, deterioration of night vision, described in the instructions for use of the drug, are much less common and, as a rule, do not require cessation of treatment. In order to minimize the risk of developing side effects from the liver and pancreas during treatment with isotretinoin, manufacturers recommend constant monitoring of biochemical blood parameters.”*

*Olisova O.Yu. Efficacy of systemic retinoids for acne // Breast Cancer. Dermatology. 2016. No. 10. pp. 602–606.

Therefore, if you have severe acne with cysts and a lot of inflammatory elements, and the doctor mentioned systemic retinoids, do not rush to run away with your heels sparkling, but think it over carefully. Prescribing retinoids for related indications is a clear sign that the doctor is up to date with the latest trends. But if in the same case the doctor continues to talk about cleansing, feel free to send him somewhere far away. The twenty-first century is just around the corner. If the treatment does not work, change your doctor!

At the moment, moderate and even mild acne is treated with systemic retinoids, prescribing microdoses, but I did without this. The doctor prescribed me adapalene, and subsequently I switched to tretinoin. There was a slight discomfort during the first time of use: the skin was dry, the eyes were dry (well, there is an aggravating circumstance here - I had laser correction), my whole face seemed to hurt a little, it was unpleasant to touch. But soon the unpleasant sensations passed. I didn't have any peeling as such.

After a month, I switched to 0.25% tretinoin under the brand name Retin-A. I still use it at a concentration of 0.5%. About 3 years have passed. The skin has objectively become better: cleaner, healthier, denser. Tretinoin has also been proven to slow down the aging process* and lighten pigmentation, so I plan to use it for the rest of my life, with a break for pregnancy and breastfeeding if I decide to. I always use reliable mineral sunscreen - even in winter in Moscow.

*Berardesca E. et al. In vivo tretinoin-induced changes in skin mechanical properties //British Journal of Dermatology. – 1990. – T. 122. – No. 4. – pp. 525-529.

In addition, I use other acne products, which I will talk about next time.

P.S. I ask everyone to use their heads. All information presented in this post is not a treatment recommendation, it is just an overview and a bit of personal experience. Treatment is prescribed only by a doctor.

P.P.S. I accidentally discovered the name of my doctor among the authors of the articles)

Beauty to all!


Retinoids are widely used in the treatment of acne in traditional medicine. But the greatest therapeutic effect is achieved in combination with other drugs. Retinoids come from the word “retinol,” which means vitamin A. They always contain this vitamin, its synthetic analogues or biological forms. By its action, vitamin A gives the skin a healthy appearance, but it is not recommended to use it in its pure form, as this can cause side effects.

Description and properties

Retinoids were discovered in 1909. Scientists have identified the properties of vitamin A for the skin. Its insufficient amount provokes follicular hyperkeratosis. It is considered one of the main causes of pimples and acne. An excessive amount of desquamated epithelial cells accumulates in the lumen of the hair follicles. They clog pores and predispose to acne.

Retinoids change the growth processes of epithelial cells, as well as their differentiation and functional activity

But in addition to the therapeutic effect, dermatologists have discovered other cosmetic properties - the skin becomes elastic and smooth, and acquires radiance. Wrinkles are less pronounced, pigment spots lighten, and signs of skin aging are reduced. Retinoids are used in cosmetology to combat age-related changes in the skin.

Therapeutic Use:

  1. For the treatment of acne, retinoids in this case reduce the production of sebaceous glands, normalize the process of keratinization of the skin of the hair follicles, and exfoliate dead cells.
  2. For rejuvenation - reactions provoked by retinoids increase the elasticity of the skin and make wrinkles less noticeable. Accelerate the production of collagen, hyaluronate acid and elastin. The skin tone is evened out, dead skin cells are removed, regenerative processes in the skin are accelerated, and the negative impact of ultraviolet radiation on the epidermis is reduced.

Retinoids can be used throughout life at any age.


Retinoids reduce sebum production, have an anti-inflammatory effect and increase immunity at the site of the purulent process

Classification

For external use against acne, 2 groups of drugs are used:

  1. Natural. These include two isomers of retinoic acid - isotretinoin (Isotrexin, Retinoic ointment) and tretinoin (Airol, Retin-A).
  2. Synthetic. These include Adapalene (Klenzit S, Differin) and Tazarotene (not imported into the Russian Federation).

"Retasol" and "Retinoic ointment" can be used in the treatment of children. "Klenzit" is prescribed only from the age of seven. For oily skin types, the presence of ulcers and comedones, Retasol is more effective. For moderate skin types and with an excessive number of nodules, it is better to treat with Retinoic ointment. Mild acne is treated with topical retinoids. And for moderate acne damage, treatment can be supplemented with drugs such as “Zinerit”, “Isotrexin” gel, “Dalacin”.

Operating principle

Retinoids for the treatment of acne act on the skin in several stages:


Side effects of topical retinoids: dry skin, irritation of mucous membranes upon contact with the drug
  1. The first few days of using the product may cause concern due to symptoms such as flaking of the skin, redness or signs of irritation. Such symptoms are accompanied by an acceleration of the process of death of keratinized cells. As a result, the skin looks healthier and younger. Pores are cleansed by breaking down fatty plugs and removing impurities. After a month, acne treatment will give the first visible results. The pronounced effect will be noticeable after 8–10 weeks.
  2. Collagen production is stimulated. Retinoids penetrate deeply into the dermis, stimulating collagen production. The skin becomes elastic, the severity of wrinkles decreases. Closer to 40 years, collagen content decreases by half. This is clearly visible in the condition of the skin. It becomes less elastic and thickens. The first results after the procedure will be noticeable after 2–3 months, and pronounced results will be visible after 9 months.
  3. The skin is moisturized. The humidification process occurs for two reasons. The first is to stimulate the secretion of non-sulfonated glycosaminoglycan. It is this that moisturizes the dermis and maintains the necessary level of hydration of collagen fibers with water. This is especially important for the elasticity of the epidermis. The second reason is the ability of most retinoids to speed up the process of stem cell division. The deep layers of the epidermis thicken. Moisture evaporates less from the surface of the skin. And a thoroughly moisturized dermis looks young.

For acne, various preparations based on Vitamin A are used.


Antibacterial drugs can be used as part of official pharmacological agents for external use

Features of application

The drugs should be used in accordance with certain recommendations:

  1. Apply the product to clean skin 1 to 2 times a day. The course of therapy varies from 12 to 16 weeks.
  2. Negative skin reactions may occur, but there are no overall negative effects.
  3. To cleanse the skin, it is better to use gels or foam for washing, or an alcohol-free tonic.
  4. Since there is a high probability of drying out the skin, it is not recommended to use alcohol solutions and soap in solid form.
  5. Make sure that the product does not get on the mucous membranes.
  6. In the first two weeks of therapy, an exacerbation reaction may occur. It manifests itself as peeling, itching and redness. It goes away on its own within seven days. Therefore, there is no need to abandon the drug.
  7. When the desired effect is achieved, the use of the drug can be reduced or its concentration reduced.
  8. Systemic retinoids are used as prescribed by a doctor.

Following these tips will help cure acne faster.

Effective drugs

Retinoids for signs of skin aging and acne:


All drugs have the same therapeutic effect. It is better to consult a doctor before use.

Systemic retinoids are used for whole-body therapy. These include Isotretinoin, which has several names - Acnecutane or Roaccutane. Due to serious negative consequences, self-medication is not recommended. "Roaccutane" is available in capsules. It suppresses sebum production, reduces the number of comedones, and relieves inflammation. A course of therapy from 16 weeks twice a day in equal parts after meals. "Acnecutane" is similar to "Roaccutane". The drug is better absorbed and less dependent on food intake. Take the entire daily dose at one time during a meal. If desired, the dose can be divided into two equal parts.