The substance Tretinoin facilitates the induction of cellular differentiation, while inhibiting the proliferation of promyelocytic (granulocyte progenitor), which is caused by a change in the binding transretinovoy acid receptor cell nuclei retinoic acid (including the myeloid leukemia).
Under the influence of tretinoin activates the initial maturation derived from primitive promyelocytic leukemic clone, as well as processes for their replacement in the bone marrow and peripheral blood is not transformed polyclonal normal hematopoietic cells.
Against this background, the patient develops a remission of the disease, which is an average of two to four months.
When applied topically Tretinoin is able to penetrate through the cell membrane, forming a cytoplasmic complex enters the cell nucleus. Formed with the hormone-receptor complex has the ability to bind to DNA and inhibit the process of transcription, thereby disrupting protein synthesis (this is based on these processes gipopigmentnoe action tretinoin).
The substance has a stimulatory effect on mitosis of the cells of the epidermal layer of the skin, helps to increase the amount of mucopolysaccharide and protein elastin formed elastic fibers that are in the papillary layer of the skin.
- inhibits the formation of melanin;
- It stimulates growth and differentiation of epithelial cells;
- inhibits cell adhesion, which form acne;
- when applied to open acne aligns epidermis without leaving evidence of inflammation;
- when applied to the closed acne contributes to their transformation into open or papular nodules and further healing without scarring after removing them from the keratin plug;
- It prevents the formation of new acne.
Keratolytic action of renova cream eliminates the effects of keratosis. Its mechanism is due to the suppression of keratinocyte proliferation and improvement of the processes of their exfoliation.
Antiseborrhoeic effect is due to inhibition of proliferation of epidermal cells, inhibition of proliferation of epithelial tissue of the excretory ducts of the sebaceous glands, decrease sebum production and normalization of its evacuation, decrease the severity of the inflammatory reaction around the sebaceous glands, and the stimulation of the regeneration of the skin.
What is Tretinoin cream?
Local anti-inflammatory effects are expressed in the form of absorption of excessive amounts of sebaceous secretion, suppression process its production by the sebaceous glands, narrowing the pores and eliminate the signs of inflammation.
Notable therapeutic effect of the tretinoin is noted after approximately six weeks after the start of use of the drug (usually 6 or 7 weeks). The maximum effect is observed after 8-12 weeks of its application.
Transretinovaya acid is an endogenous metabolite of vitamin A, which is normally always present in human plasma. Following oral administration of the substance is well absorbed in the stomach and intestine, the maximum concentration in the blood plasma observed after three hours.
Suction- tretinoin can vary, both in different groups of patients and each individual patient. The substance is capable of binding to a large extent to proteins in the plasma (primarily albumin). Indicator binding is within 95%.
The duration of the average half-life of 0.7 hours. After a single use of tretinoin in a dose of 40 mg, the maximum concentration in the plasma is returned to the original level after approximately 7-12 hours.
The drug does not accumulate in the body and fixed in its various tissues even after repeated administration.
Acid has the ability to induce its own metabolism, resulting in reduction of AUC and plasma concentrations decline in average a third week after continuous administration of the drug. The increase is not conducive to an adequate dose increased plasma concentrations.
About 60% tretinoin as metabolites, which are formed during oxidation and glyukuronirovaniya are eliminated by the kidneys within 3 days (72 hours). Partially metabolites are excreted into the intestinal contents for 3 to 6 days.
Repeated reception provokes reduction in the concentration, which is due to induction of the enzyme cytochrome c oxidase (cytochrome P450). As a result of this increased clearance, and reduced bioavailability indicator substance after oral administration.
If the drug is used for skin application, the rate of absorption of tretinoin range from 1,41-31%. Primarily it is influenced by parameters such as:
- General condition of the skin of the patient;
- surface area to be treated;
- the duration of the drug.
- After cutaneous application of 4.45% tretinoin absorbed dose is eliminated by the kidneys in the urine, and about 1.6% – together with bile.
- Oral administration of tretinoin administered to patients diagnosed with acute myeloid leukemia variant, characterized by abnormal accumulation of a form of myeloid cells – promyelocytes.
- Moreover, use of the drug triggers the induction of remission in patients who have not previously held a course of treatment, and patients who have suffered a relapse / recurrence of APL (acute promyelocytic leukemia form) or unresponsive to standard chemotherapy conducted using rubomycin, cytarabine or analogs.
- After the onset of complete remission of the disease patients showed a consolidating chemotherapy at full doses.
- Instructions drug warns that patients who undergo maintenance therapy with tretinoin, there may be a loss of response to treatment.
As an external agent Tretinoin is used to treat:
- acne drain (ie blackheads, which are the result of the merger of several induratum acne are interconnected by deep strokes);
- acne vulgaris, which are accompanied by the formation of papules (knots), comedones (traffic jams formed at the mouth of sebum hair follicles) or pustules (pus-filled content elements rash);
- Favre disease-coquina (colloidal degeneration of the skin, which is a dermatosis of unknown natural origin);
- hyperpigmentation of the skin.