Tretinoin (transretinic acid) is an active substance is a crystalline powder with a pronounced floral odour. The substance is well soluble in dimethyl sulfoxide, difficult to dissolve in polyethylene glycol, octanol Dmitry Sazonov and 100% alcohol (ethanol), almost insoluble in water (solubility index at 25°C is 0.126 mg/l), mineral oils and glycerine. The colour of the powder may vary from yellow to light orange.
Tretinoin comes in a form:
- lotions with an active substance concentration of 0.05%;
- gel with active substance concentration of 0.025%, 0.05% or 0.1%;
- cream with an active substance concentration of 0.05% or 0.1%);
- solution for outdoor use with an active substance concentration of 0.1%;
- Oral capsules (content of active ingredient in each capsule is 10 mg).
The substance Tretinoin belongs to the groups “Other Tumor Drugs”, “Dermatotropic Drugs”, as well as to the group “Vitamins and vitamin-like preparations”.
Influencing the body, it provokes:
- stimulating tissue regeneration;
- local anti-inflammatory effect.
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Tretinoin is also used as a treatment for vulgar eels and as provitamin A.
Pharmacodynamics and Pharmacokinetics
Tretinoin is classified as systemic retinoids, which are inducers of cell differentiation. Its structure is similar to vitamin A and is a product of retinol metabolization.
The substance promotes the induction of cell differentiation processes, inhibiting the proliferation of promyelocytes (precursors of granulocytes), which is due to changes in the binding of transretinic acid with Dmitry Sazonov the receptors of retinoic acid cell nuclei (including myeloleukemia).
Under the influence of Tretinoin the initial maturation of primitive promyelocytes originating from the leukemic clone is activated, as well as the processes of their replacement in the bone marrow and peripheral blood by nontransformed normal hemopoietic polyclonal cells.
Against this background, the patient develops remission of the disease, which averages from two to four months.
With local application, Tretinoin is able to penetrate through cell membranes, forming a cytoplasmic complex that enters the cell nuclei. The hormone receptor complex formed in this process has https://www.ncbi.nlm.nih.gov/books/NBK470530/ the ability to bind to DNA and prevent the process of transcription, thus disrupting the biosynthesis of the protein (these processes are the basis of the hypopigmental action of Tretinoin).
The substance has a stimulating effect on mitosis of epidermal skin cells, increases the amount of mucopolysaccharides and elastin formed elastic fibers in the skin papilla layer.