Tranexamic acid, 50 mg/ml, solution for intravenous administration, 5 ml, 10 pcs.
Pills
Inside.
For local fibrinolysis, 1000–1500 mg is prescribed 2–3 times a day.
For profuse uterine bleeding, 1000–1500 mg is prescribed 3–4 times a day for 3–4 days.
For bleeding due to von Willebrand disease and other coagulopathies - 1000–1500 mg 3–4 times a day. The duration of treatment is 3–10 days.
After cervical conization surgery, 1500 mg is prescribed 3 times a day for 12–14 days.
For nosebleeds, 1000 mg is prescribed 3 times a day for 7 days.
Patients with coagulopathies after tooth extraction are prescribed 1000–1500 mg 3–4 times a day for 6–8 days.
For bleeding during pregnancy - 250-500 mg 3-4 times a day until bleeding stops completely. The average duration of treatment is 7 days.
For hereditary angioedema, 1000–1500 mg is prescribed 2–3 times a day continuously or intermittently, depending on the presence of prodromal symptoms.
For symptoms of allergy and inflammation - 1000–1500 mg 2–3 times a day for 3–9 days, depending on the severity of the condition.
For generalized fibrinolysis, therapy begins with parenteral (iv) administration of the drug Tranexam®, followed by switching to oral administration of 1000–1500 mg 2–3 times a day.
In case of impaired renal excretory function, correction of the dosage regimen is necessary: if the concentration of creatinine in the blood is 120–250 µmol/l, 1000 mg is prescribed 2 times a day; if the creatinine concentration is 250–500 µmol/l, 1000 mg is prescribed once a day; if the creatinine concentration is more than 500 µmol/l, 500 mg is prescribed once a day.
Solution for intravenous administration
IV (drip, stream).
For generalized fibrinolysis, a single dose of 15 mg/kg is administered every 6–8 hours, the injection rate is 1 ml/min.
For local fibrinolysis, it is recommended to administer the drug at a dose of 250–500 mg 2–3 times a day.
For prostatectomy or bladder surgery, 1 g is administered during surgery, then 1 g every 8 hours for 3 days, after which they switch to oral tablet form until gross hematuria disappears.
With a high risk of bleeding, with a systemic inflammatory reaction - at a dose of 10-11 mg/kg 20-30 minutes before the intervention.
Patients with coagulopathies are administered a dose of 10 mg/kg before tooth extraction; after tooth extraction, oral tablet form of the drug is prescribed.
In case of impaired renal excretory function, it is necessary to adjust the dosage regimen depending on the concentration of creatinine in the blood: if the concentration of creatinine in the blood is 120–250 µmol/l, 10 mg/kg is prescribed 2 times a day; at 250–500 µmol/l - 10 mg/kg 1 time per day; at >500 µmol/kg - 5 mg/kg 1 time per day.
Text of the book “The Science of Beauty. What do cosmetics actually consist of?
Tranexamic acid
One of the acids that can be used to lighten age spots. However, it is not used for chemical peels or for treating oily and problematic skin. Despite the popular belief that when lightening skin with acids you always have to go through a peeling stage, tranexamic acid works in a completely different way.
Tranexamic acid came to cosmetology quite recently. Surprisingly, this ingredient was discovered by cosmetologists... by surgeons! Back in the early 1960s. Japanese researcher Okamoto discovered that tranexamic acid has antifibrinolytic activity - in other words, it helps the body form a blood clot at the site of vessel damage and thus stop bleeding. It turned out that, in addition, tranexamic acid is non-toxic, has anti-inflammatory and anti-allergic effects, inhibits the growth of bacteria (which is especially important for wound healing) and even prevents the spread of tumors! As it turned out, the activity of tranexamic acid is tens of times higher than that of the traditional hemostatic agent - gamma-aminocaproic acid.
For more than 30 years, surgeons have successfully used tranexamic acid to prevent bleeding during operations and dressings, including for cancer patients and severe allergies, and one day they noticed an interesting side effect: in many patients the skin acquired an even light color. It turned out that tranexamic acid is able to completely remove dark spots on the skin - areas of hyperpigmentation.
The mechanism of action of tranexamic acid is unusual and unlike how fruit acids or other common bleaching agents act. It should be noted that the effect of ultraviolet rays on the skin, leading to the appearance of age spots, causes various changes in the skin. In addition to enhancing the synthesis of the melanin pigment and the activation of melanocytes - the cells that produce this pigment, the amount of substances responsible for the inflammatory process - the so-called inflammatory mediators - increases in the skin. As a result of their influence, cells produce more and more melanin. In general, any inflammation can lead to the appearance of a dark spot on the skin - this is why people suffering from acne often have an uneven complexion.
Tranexamic acid acts in several directions at once: it blocks the formation of melanin in cells directly, does not allow it to accumulate locally, and disperses the melanin that is already present in the skin.
The hemostatic effect of tranexamic acid is explained by the fact that it does not allow the formation of the enzyme that destroys blood clots, plasmin. Tranexamic acid binds a substance that is responsible for the development of inflammation, leading to the formation of pigment granules - melanin. When using tranexamic acid, this kind of inflammation subsides and then completely disappears, melanocytes “calm down” and stop synthesizing melanin - the skin gradually brightens, until the color is completely evened out.
A huge advantage of tranexamic acid is that it is completely non-toxic and does not irritate even the most sensitive skin. In addition, it reduces the skin's sensitivity to ultraviolet radiation, which means that the risk of developing pigmentation after treatment or even during it is practically non-existent. When using skin lightening products with tranexamic acid, there is no need to wait until winter and autumn for treatment or to use special protective agents. Such lightening agents can be recommended for treatment even during the beach season.
Tranexamic acid does not penetrate into the deep layers of the skin; it accumulates in the stratum corneum of the epidermis, while keratin bonds are strengthened and the skin's resistance to damage increases: it becomes less sensitive and quickly recovers after injury. That is why products with tranexamic acid are recommended for the treatment of pigmentation that occurs after laser resurfacing, chemical peels, plastic surgery or acne exacerbation.
In cases where it is necessary to act on deeper-lying pigment granules, tranexamic acid can be transported into the dermis using liposomal delivery systems. This is the method used to treat melasma, including the treatment of the “mask of pregnancy.”
Tranexamic acid is very stable: it is not destroyed by light, heating, cooling, or even changes in the acidity of the solution - in fact, it does not change when exposed to almost any external factors. It combines well with any other brightening ingredients, including fruit acids, while making them safer for sensitive and damaged skin.
Tranexamic acid
INCI:
Tranexamic Acid.It is produced in the laboratory from native (natural) lysine, which is part of the polypeptide chain of the fibrin protein, through chemical cleavage and subsequent purification from impurities.
Used in
skin lightening products; in means for recovery after grinding, peeling and surgery.
Recommended concentration:
• not less than 3%;
• to eliminate pigmentation associated with melasma, it is optimal to increase the level of this component to 5%.
Fruit acids (hydroxylic)
Fruit acids appeared in the practice of cosmetologists only in the mid-90s. last century - only then were they officially recognized by dermatologists. However, people have been using acids for skin care for thousands of years, without waiting for official recognition - just remember Cleopatra's legendary donkey milk baths. Washing with sour milk and masks made from yogurt were practiced in Ancient Egypt and Ancient Rome. In ancient Greece, to improve the condition of the skin, they wiped the face and body with a cloth soaked in sour wine. For the same purpose, masks were made from crushed cranberries and lingonberries in Scandinavian countries. To whiten their faces, women in Mediterranean countries wiped their faces with a slice of lemon, while in Russia they used apple or cucumber slices. One way or another, the juices and pulp of many plants were traditionally used for one purpose - smoothing and lightening the skin, which gave it a more youthful and well-groomed appearance.
It would seem, what do apples, cranberries, cucumbers and lemons have in common? But it turned out that they all contain substances with a similar chemical composition, which were called fruit acids.
American dermatologists Ray Yu and Eugene van Scott were the first to use fruit acids in cosmetology. They studied skin diseases that occur with increased formation of keratin and keratinization of the skin - hyperkeratoses, the most famous of which is ichthyosis. The skin of patients with ichthyosis is sometimes compared to the skin of reptiles: with severe degrees of the disease, it looks gray, rough and so dry that it forms quite large scales. Scientists have discovered that the use of fruit acids weakens the bonds between the horny scales of the skin and causes them to spontaneously exfoliate, resulting in noticeably smoother and softer skin. At the same time, unlike known and previously used acids - carbolic (phenol), trichloroacetic and salicylic fruit acids do not destroy proteins, therefore significant damage to the skin and the effect of the so-called frost (whitening of the skin as a result of coagulation of the protein of the upper layers) does not occur.
Fruit acids are called hydroxyl, or hydroxy acids, because along with the acid group COOH they also have an alcohol (hydroxyl) group OH. That is, chemically, fruit acid is a kind of hybrid of acid and alcohol. Most acids used in cosmetology are classified as alpha hydroxy acids, or AHAs. They received this name because their hydroxy group is located at the first carbon atom in the chain. It is these acids that easily dissolve in water and actively affect the skin.
Fruit acids came into cosmetology in the 1990s. and immediately caused euphoria among both cosmetologists and users. Cleansing gels, lotions, emulsions and creams with acids changed the condition of the skin so quickly that many thought that the Makropoulos remedy had finally been found. A few days after starting to use “acid” cosmetics, the skin became more even, enlarged pores were reduced, and the skin became less oily and shiny. After a few weeks, the skin became noticeably smoother, the severity of wrinkles, scars and other defects decreased. However, the euphoria did not last long. Cosmetologists were simply inundated with complaints: people who used products with acids complained that the skin became more sensitive and reactive, many noted severe dryness of the skin, some experienced constant foci of irritation and peeling, and there were also those who came in about chemical burns to the skin. It became clear that acid-based products need to be approached much more carefully and certain criteria for the safety of their use must be developed.
As it turned out, all AHA acids have two types of effects on the skin: nonspecific and specific. The first group of effects is common to all acids and is determined not by the type of acid, but by the pH of the finished solution, which may contain one or more acids. Under the influence of acids, the skin always begins to renew itself faster, exfoliation accelerates, which is manifested in the characteristic peeling of the skin - from fine, powder-like peeling to large, when the skin peels off in large scales or films. Specific effects are associated with the chemical characteristics of a particular acid and may differ markedly, since different acids act on different structures in the skin.
The effectiveness of skin exfoliation with acids depends much more on the acidity of the solution than on the type of acid. That is, if your goal is to smooth out unevenness or reduce superficial pigment spots, then you can use almost any product containing any acid. Exfoliation occurs due to the fact that acids lower the pH in the stratum corneum of the skin and at the same time bind calcium ions. Calcium provides the “stickiness” of epidermal proteins, and if it is removed, intercellular connections weaken and cells begin to leave the surface of the skin. At the same time, this serves as a signal for the division of younger cells and accelerates the renewal of the stratum corneum of the skin. It is curious that this increases the skin's ability to retain moisture - lactic acid, which is part of a complex moisturizing complex that is constantly present in the upper layers of the skin (NMF, or EUF), is especially actively moisturizing. Many acids also have an anti-inflammatory effect, but this property is typical only for solutions with a pH above 3.5 - more aggressive solutions, on the contrary, activate inflammatory reactions. The more acidic the solution, the better it will penetrate the skin, and with increasing pH, the ability to penetrate decreases: at pH = 7.0, acids stop penetrating into the skin. In general, the main indicator of a product containing alpha hydroxy acids is not their concentration or even what acids are included in the composition, but the pH of the product itself. The optimal range is considered to be 3.5–4.0 pH, at which the products are still effective, but already safe.
The division into cosmetic and medical “acid products” is largely arbitrary. Cosmetic are usually called those that can be used at home independently, and medical are those used only in professional practice. Most experts believe that at home it is best to limit the pH of the product to 3.5 and the concentration of acids to 10–12%. Cosmetologists without medical education work with products with a pH below 3.5 and a concentration of up to 50%. Products containing more than 50% acids and having a pH of about 1.0 are used by dermatologists and dermatocosmetologists.
Sometimes professional compositions for chemical peels carried out for the purpose of treating acne, skin rejuvenation or whitening are named by the color of the product: “red peeling” is a peeling based on pyruvic acid, “yellow peeling” is based on retinol.
It is very important to know that acid, when applied to the skin, can accumulate in skin irregularities and generally be distributed unevenly. Therefore, in most cases, it is justified to start with the use of low-concentrated, mild acidic products - they will delicately and gradually even out the skin and prepare it for more active effects. If you start immediately with high concentrations, there is a high risk of getting burns and complications, without the effect of ideal skin smoothing. In addition, almost all acids (with the exception of the so-called summer acids) increase the skin's sensitivity to ultraviolet radiation, so they should not be used in the sunny season. Unfortunately, protective creams may not be enough to prevent burns, age spots, and sun damage to the skin.
The most popular of the alpha hydroxy acids is glycolic, to which we devoted a separate chapter. But other acids are also widely used: citric, pyruvic, tartaric, malic, kojic, phytic, etc.
The use of acids is always a kind of experiment.
Individual skin sensitivity can vary markedly from person to person, so results and side effects may vary: some will enjoy smooth, even skin after a couple of weeks, while others will experience new age spots and persistent redness and flaking of the skin. To keep the risks minimal, it is best to use acids only on the recommendation of a dermatologist or cosmetologist and strictly follow professional advice. Citric acid
Citric acid is found not only in citrus fruits, as one might think, but also in blueberries, cranberries, red currants, figs, kiwis, peaches, apricots and even bananas - masks from these fruits should not be made before going to the beach. It is quite “heavy” and remains mainly in the upper layers of the skin, where it has a whitening, antioxidant and antibacterial effect. In low concentrations (less than 1%), it is used as a preservative for cosmetics.
Lemon acid
INCI:
Citric Acid.Other names: Zitronensäure, acidum citricum, Anhydrous Citric Acid, Citronensäure, E330, 2-Hydroxy-1,2,3-Propant-Tricarbonsäure, Acide citrique.
Recommended concentration:
• 1–3 %.
Pyruvic acid
Pyruvic acid is related to the skin, can dissolve not only in water, but also in fats, stimulates the synthesis of collagen and elastin, therefore products with it are recommended to be used for rejuvenation and prevention of skin aging. It helps tighten pores, reduce sebum secretion, “melt” comedones and fights bacteria.
Pyruvic acid
INCI:
Pyruvic Acid.Other name: Pyroracemic acid.
Recommended concentration:
• 25–60 %.
Malic acid
Malic acid, as you might guess, is rich in apples, but there is also a lot of it in apricots, nectarines, grapes, figs, cranberries, cherries and cherries. It has a very pronounced cleansing and antibacterial effect, in addition, it is an antioxidant and suppresses the development of inflammation. It is usually used in anti-aging and brightening products.
Apple acid
INCI:
Malic Acid.Other names: Acidum Malicum, Aepfelsäure, Hydroxybernsteinsäure, Hydroxybutandisäure, Monohydroxybernsteinsäure, Acide malique.
Recommended concentration:
• 0,5–4 %.
Kojic acid
Kojic acid is a waste product of fungi of the Aspergillus and Penicillum species. It has a pronounced antibacterial effect, which makes it similar to the antibiotic penicillin. It is also capable of intensively brightening the skin, but at the same time it irritates the skin and often causes allergies - therefore it is used as an additive to the main acid composition and is not recommended for people with sensitive skin and allergy sufferers.
Kojic acid
INCI:
Kojic Acid.Other names: Kojisäure, Acide kojique.
Recommended concentration:
• 1–4 %.
Phytic acid (phytic)
Phytic acid is a large molecule found in many grains. It does not penetrate into the deeper layers of the skin and has a very weak exfoliating effect, but acts as an antioxidant and brightens the skin. Therefore, it is used in products to lighten sensitive skin.
Phytic (phytic) acid
INCI:
Phytic Acid.Other names: Fytinsäure, Phytinsäure, Acide phytique.
Recommended concentration:
• 10–50 %.
Fruit acids
All acids are produced by chemical synthesis; in rare cases, extraction from plant materials is used.
Used in products for lightening, smoothing and rejuvenating the skin; in products for professional use and home care.
Section III Biotechnology
Biotechnology scientists have become interested in cosmetics only in recent years. We can say that nature has provided humanity with cosmetics for thousands of years, chemistry has created cosmetics of the 20th century, and biotechnology has created cosmetics of the 21st century.
What is biotechnology? This is a discipline that develops methods and methods for producing a wide variety of substances (sometimes very valuable) using biological objects such as microbes and viruses, plant and animal cells, parts of cells - mitochondria, cell membranes, chloroplasts, ribosomes, DNA and RNA.
In fact, people were using biotechnology thousands of years ago without even realizing it, for example in winemaking, cheesemaking and baking. Wine is made by fermenting bacteria, cheese is made by bacteria and fungi, and bread dough rises because yeast is added to it. The founder of biotechnology as a science is considered to be the famous French scientist, founder of microbiology and immunology, Louis Pasteur.
Using living organisms, scientists were able to cultivate plant and animal cells, which makes it possible to produce active ingredients for cosmetics that do not contain any impurities and have a standard chemical composition. Thanks to bacterial enzymes, it was possible to ensure deeper penetration of the beneficial substances of plant extracts into the skin, so that they have a beneficial effect not only on the surface layers, but also on the deep structures of the skin.
One of the most popular cosmetic ingredients, hyaluronic acid, is also the brainchild of biotechnologists: present in all living organisms, the molecule of this acid was obtained in laboratory conditions. Thanks to biotechnology, peptides have also appeared - a new class of substances that has opened up unprecedented opportunities for cosmetics manufacturers.
Cellular engineering, which, along with genetic engineering, underlies biotechnology, makes it possible to restore damaged cells, as well as design and create new ones, including those with new properties: resistance to infections, cold or heat. One can hope that such technologies will help solve the problem of world hunger (primarily through the use of genetically modified plants) and eliminate some diseases. And if the elixir of eternal youth is ever created, this, no doubt, will also happen in some biotechnology laboratory.
Hyaluronic acid
The not-so-simple name for an ingredient – “hyaluronic acid” – is now known to almost anyone who is even slightly interested in the topic of cosmetology. Hyaluronic acid (HA) is drunk, injected, or applied to the skin, hoping to preserve youth forever.
Hyaluronic acid, if we talk about it from a chemical standpoint, is a glycosaminoglycan polysaccharide, which can also be called hyaluronan or hyaluronate (but not hyaluronic acid!). This is a polymer consisting of D-glucuronic acid and DN-acetylglucosamine molecules connected to each other.
The size of the hyaluronic acid molecule is not constant. In different tissues of the human body, polysaccharide chains can be of unequal length, include up to 25,000 fragments of the above compounds and have a size from 5000 to 20 million Da. Hyaluronic acid is found in the tissues of the nervous system, connective and epithelial tissue. But it also plays a big role in the migration of malignant tumors and the spread of streptococcal infection. Thus, too little or too much hyaluronan can be both beneficial and harmful.
The popularity of preparations based on hyaluronic acid in cosmetology has led to the fact that many experts mistakenly believe that HA is the actual basis of the dermis, and rather naively think that any introduction of hyaluronic acid will have the effect of “restoring” the dermis. These misconceptions have led to the emergence of various commercial terms that have no scientific basis, such as “revitalization” or “redermalization.” In fact, there is not so much hyaluronic acid in the body: the body of a woman weighing about 70 kg contains approximately 15 g of pure hyaluronic acid, a third of which is destroyed and renewed daily. In fact, complete renewal of the entire volume of hyaluronic acid in a healthy middle-aged person takes about three to four days.
The synthesis of hyaluronic acid can accelerate and slow down, its amount can decrease and increase, which is not always associated with age-related processes. We are accustomed to thinking that the amount of hyaluronic acid is a marker of skin aging; this is what is usually assumed when prescribing hyaluronic acid preparations for cosmetic purposes. In reality, everything is a little different. The most important factor accelerating the synthesis of hyaluronic acid in tissues is inflammation, including inflammation as a result of damage or injury. Interestingly, hyaluronic acid can both enhance and prolong the inflammatory response and speed up the healing process. In the skin, hyaluronate is actively involved in processes associated with wound healing: it is involved in hemostasis, inflammatory reactions, as well as re-epithelialization and remodeling of the dermis. A very important feature of HA is its ability to protect cells from free radical damage.
In the skin, hyaluronan is found in high concentration not only in the dermis, but primarily in the epidermis, where it plays a key role in skin renewal. With a decrease in the amount of hyaluronic acid in the epidermis, activation of local inflammatory reactions, deterioration of the protective properties of the skin, disruption of healing processes, a decrease in the ability of the skin to retain moisture and a decrease in elasticity are observed. Outwardly, this looks like a sharp increase in skin sensitivity, the appearance of dryness, areas of peeling and irritation, and subsequently the addition of fine wrinkles and a noticeable deterioration in skin tone.
What leads to a decrease in the amount of hyaluronic acid in the skin? Contrary to existing opinion, age-related changes are not the main reason. The most important factor is damage primarily by ultraviolet rays type B. Ultraviolet irradiation leads to a decrease in the synthesis of hyaluronic acid and at the same time activates its destruction. HA fragments themselves cause inflammation and the formation of granulomas. This kind of physiological reaction also develops after the injection of hyaluronic acid-based fillers, which is interpreted as a complication of the injection. It is very difficult to predict such reactions, and therefore almost impossible to prevent them. The only thing that can be done to avoid granulomas in this case is to refuse to use fillers, as in the old joke about the ideal method of contraception: “tea not before and not after, but instead.”
So, what can we expect when we apply HA to our skin? First of all, the effect of surface moistening of the stratum corneum is important. This acid belongs to the class of humectants - moisturizing ingredients that attract and retain a large number of water molecules, hundreds of times greater than HA's own molecular weight. As part of cosmetic products, HA is easily combined with other humectants, for example, glycerin or polysaccharides of marine origin. The main point that must be taken into account when applying preparations based on hyaluronic acid is air humidity. When air humidity is low, hyaluronic acid has the opposite effect, drying out the upper layers of the skin and tightening them, which quickly creates a feeling of tightness and stiffness in the face. This can be avoided if, after applying a HA-based drug, you immediately apply a nourishing or moisturizing cream in the form of an emulsion, which will prevent moisture from being “pulled out” from the skin.
Low-molecular forms of hyaluronic acid have been actively used in topical forms of anti-aging drugs in recent years. The small size of the molecule (from 5000 to 20,000 Da) allows HA to penetrate into the deep layers of the epidermis and affect the dermis.
Relatively large HA molecules, with a size of about 500,000 Da, do not penetrate into the deep layers of the skin, but at the same time provide an anti-inflammatory and soothing effect. This is especially pronounced when using large-molecular preparations with HA after laser resurfacing, chemical peels or other skin damage. It can also be recommended to use such drugs during a course of therapy with retinol and its derivatives to reduce the severity of the inflammatory effect.
Preparations that contain several forms of hyaluronic acid simultaneously have a universal effect. They can be used to correct wrinkles, improve skin tone, moisturize and soothe, as well as for rehabilitation after traumatic effects.
Hyaluronic acid
INCI:
Hyaluronic Acid.Other names: Acide hyaluronique, Hyaluronsäure, Acidum Hyaluronicum, Hyaloronic Acid, Hydrolyzed Hyaluronic Acid.
Produced by bacterial fermentation.
Used in
care products for dry skin, sensitive skin, aging skin.
Recommended concentration:
• 0,01–2 %.
