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Retinoids are derivatives of vitamin A. Due to their properties and healing properties, retinoids are mainly used in the treatment of dermatological diseases, especially acne, as well as in skin care. They have also found application in the treatment of certain types of cancer. What else do retinoids do? What are the contraindications and side effects of their use?

Retinoidsis a group of chemicals that exhibit the properties of vitamin A. Retinoids have many different functions throughout the body: they are involved in the process of vision, regulation of proliferation and cell differentiation , growth of bone tissue, in the activities of the immune system and protecting the body against many types of diseases.1Thanks to their properties, these substances are mainly used in the treatment of dermatological diseases, as well as in skin care. They are also used in the treatment of certain types of cancer.

Due to their structure and properties, there are 3 generations of retinoids:3

  • 1st generation - natural, non-selective retinoids - retinol (vitamin A) and its metabolite retinal, tretinoin, isotretinoin
  • 2nd generation - monoaromatic retinoids, synthetic analogues of vitamin A (etretinate, acitretina)
  • 3rd generation - polyaromatic retinoids, characterized by selective receptor action (arotinoid, adapalene, tazarotene)

Retinoids in cancer therapy

Due to the influence of retinoids on the processes regulating cell division, they have been used in the treatment of some precancerous conditions and neoplastic diseases:1,2

  • precancerous conditions such as actinic keratosis, oral mucosa leukoplakia
  • proliferative diseases (keratoacanthoma, squamous cell carcinoma, cutaneous T-cell lymphomas
  • skin lesions associated with Kaposi's sarcoma in AIDS patients
  • acute promyelocytic leukemia

Due to their mechanism of action, retinoids are also the subject of in vitro experiments in inhibiting ovarian and breast cancer.

Retinoids - application in dermatology

Retinoids are used primarily in dermatology,both locally and generally. Due to their regenerative effect on the skin, they are used in the case of excessive skin dryness, inflammation, burns and frostbites. They are also used in the treatment of numerous dermatological diseases. Retinoids are used primarily in the treatment of acne. In this case, retinoids work in two ways - they accelerate the exchange of the outer layers of the epidermis and the exfoliation of dead cells. Thanks to this, they inhibit the keratinization of the sebaceous glands, lead to the removal of mature blackheads and reduce the secretion of sebum. Secondly, by exerting an influence on the immune system, they reduce the existing inflammatory changes. In the treatment of acne vulgaris, retinoids are used both locally and systemically in monotherapy, as well as in combination with other agents, such as: steroid hormones, antibacterial drugs, UV radiation.2

The best known and most commonly used natural retinoid is retinol (vitamin A1).

Retinoids are also used in the treatment of psoriasis. Psoriasis is a chronic, recurrent immune and inflammatory skin disease. The retinoids used in the treatment of this disease act by normalizing the proliferation of epidermal cells, in particular by inhibiting cell division in the case of excessive proliferation and accelerating the process when it occurs too slowly. In addition, they modulate the immune response by regulating the functions of skin Langerhans cells, T lymphocytes, and inhibiting the production of chemotactic factors. As in the treatment of acne, in psoriasis, retinoids are used as topical and oral agents in monotherapy, as well as in combination therapy with steroid hormones, UV radiation, vitamin D analogues, tar and cytotoxic drugs.2

Other skin diseases in which retinoids can be used are: rosacea, papulopapular diseases (except psoriasis, lichen planus, red follicle dandruff), genodermatosis with keratosis disorders (Darier's disease, ichthyosis), skin parchmental disease, autoimmune diseases (lupus erythematosus), viral diseases (flat warts, molluscum contagiosum).3

Treatments with retinol help solve many skin problems

Source: lifestyle.newseria.pl

Retinoids and pregnancy

The absolute contraindication to the use of retinoids is pregnancy and the period of breastfeeding. The use of retinoids in the first trimester of pregnancy may cause serious developmental disorders, including defects, in the fetusfacial skeleton (hydrocephalus, microcephaly), microphthalmia (small eyes), developmental defects of the external ear, cardiovascular system, central nervous system. Therefore, it is imperative for the patient to follow effective contraceptive measures. Before starting retinoid treatment, the patient must provide a negative result from a reliable pregnancy test.

According to an expertDr. Elżbieta Szymańska, MD, a dermatologist

Treatment of acne with oral Isotretinoin and pregnancy

Women of childbearing potential must use effective contraception for 1 month before starting treatment, during treatment and 1 month after treatment. Isotretinoin should be used in women of childbearing potential only after ensuring that the patient is not pregnant (negative pregnancy test prior to treatment initiation). Pregnancy tests are performed before, during and 5 weeks after treatment is started. The drug should be used under medical supervision and laboratory tests in order to maximize the safety of the therapy.

Retinoids - use in cosmetics

Retinoids contained in cosmetics are used not only for the care of oily skin prone to acne lesions, but also for mature skin. Retinoids contained in anti-wrinkle creams improve skin appearance, elasticity, reduce wrinkles and smooth the skin. Thanks to retinol, discoloration is also effectively removed. Retinol also contributes to the formation of new blood vessels in the skin, decisive for the nutrition and oxygenation of the connective tissue and epidermis, and thus for a nice, fresh skin tone.

When applying topical retinoids, avoid overexposure to UV radiation. Failure to do so may result in sun damage to the skin. In order to minimize the negative effects of the use of retinoids in the cosmetics industry, retinoic acid precursors are used, the most commonly used of which is retinol. Cosmetic products are characterized by a relatively low content of this compound, or from 0.01% to 0.08%, which is due to the occurring side effects in the form of skin irritation.

According to an expertAgnieszka Denis, MSc - cosmetologist

How to use face creams with retinolI am asking for advice. I am 30 years old, I have combination skin with enlarged pores (mainly on the cheeks), sun discoloration and the first signs of aging. I bought a cream with retinol (Sesderma Retises 0.25%). After three months of use, the manufacturer recommends the Retises 0.5% therapy. I do an almond acid treatment once a month. Recently, I also acquired an acid tonicalmond 5%. The skin is slightly red after it, but in the morning it repays with a bright, rested complexion. How to use face creams with retinol? Can I use both products at the same time? Should I give up acid peeling once a month?

Agnieszka Denis, MA, cosmetologist: Please do not overdo the treatments. Treatments with acids to improve the condition of the skin after the summer should be done in series every 2 weeks for 2-3 months, but daily retinol should be excluded during this time. After the treatment is finished, you can go back to the cream. Everything in moderation so as not to shock the skin.

Retinoids in dietary supplements

In addition to medicinal and cosmetic products, retinoids are also a common ingredient in dietary supplements. These are mainly complex preparations containing vitamin complexes, minerals and plant extracts, taken to supplement the diet in states of nutrient deficiencies or increased demand for these ingredients. They are used in states of reduced immunity, exhaustion, problems with concentration, focus, in the absence of appetite, during convalescence after illness, as well as in excessive stress. Dietary supplements are not medicinal products, so the content of a number of biologically active ingredients, especially those that accumulate in the body, are much lower than therapeutic doses.2

Important

Retinoids - contraindications

As mentioned, an absolute contraindication to the use of retinoids is pregnancy and the period of breastfeeding. Relative contraindications include leukopenia, hypercholesterolaemia, hypertriglyceridemia, liver and kidney dysfunction, hypothyroidism, obesity, and diabetes.1Remember that retinoids interact with tetracyclines, anticonvulsants, methotrexate, and alcohol. Vitamin A should not be given simultaneously.3

Retinoids - side effect

1) SKIN, HAIR, NAILS

The side effects that appear on the skin during retinoid treatment include:

  • drying, redness of the skin and mucous membranes
  • itching
  • irritation
  • blush
  • increased skin sensitivity
  • skin rashes
  • sweating

In patients from higher risk groups (lipid metabolism disorders, diabetes, obesity, alcoholism) long-term use of retinoids increases the risk of accelerating atherosclerosis and coronary heart disease.

Disturbances in hair growth such as thinning and hair loss may appear.These disorders also affect the nails, they are manifested by increased brittleness, loss of gloss and deformation of the nail plates.

2) SIGHT

Dryness around the eyes and eyeballs, burning eyes and tearing are also very common.

3) Digestive System

Cases of nausea, inflammatory bowel diseases (ileitis), and pancreatitis have been reported. High doses and long-term use of drugs containing retinoids may also cause liver dysfunction. Retinoids should be discontinued immediately in patients who experience diarrhea or gastrointestinal bleeding.

4) RESPIRATORY SYSTEM

There may be very rare cases of bronchospasm.

5) BONE-JOINT SYSTEM

Bone pain is a common consequence of retinoid therapy. Calcification of tendons and ligaments is also observed, especially in the ankles. These substances can also contribute to the development of osteoporosis.

6) NERVOUS SYSTEM

Side effects from the central nervous system are rarely observed. There are also, although not very often, symptoms of increased intracranial pressure, such as headaches or nausea.

Additionally, during retinoid therapy, the following are observed: leukopenia, erythropenia, lowering hematocrit, and acceleration of the fall of blood cells. Lipid metabolism disorders are quite common (increased serum triglycerides and cholesterol, decreased HDL cholesterol, increased LDL cholesterol). In patients at high risk (lipid metabolism disorders, diabetes, obesity, alcoholism), long-term use of retinoids increases the risk of accelerating atherosclerosis and coronary heart disease.3

Adverse reactions in most cases depend on the dosage of the drug and generally disappear after dose reduction or discontinuation of the preparation. Occasionally, a temporary worsening of the symptoms of the disease is observed after the initiation of retinoid treatment.

Worth knowing

Retinoids - sources of natural retinoids

The main source of dietary retinoids is retinyl esters found in animal foods. These esters are hydrolyzed in the intestinal lumen to give free retinol. The source of retinol may also be beta-carotene (provitamin A) introduced into the body with plant food products. In the human body, β-carotene is converted into retinol in the small intestine.

Bibliography:

1. Boryczka M., Pasker B., Sosada M., Retinoids as active substances of medicinal products, cosmetics and supplementsdiets, "Pharmaceutical Scientific Review" 2010, No. 8

2. Marona H., Gunia A., Pękala E., Retinoids - role in pharmacotherapy in terms of cellular mechanism of action, "Terapia i Leki" 2010, no. 3

3. Bronikowska A., Wojnowska D., The use of retinoids in dermatology, Nowa Medycyna 2003, No. 1

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