Tretinoin - a universal solution for acne and wrinkles

The only product that is guaranteed to improve skin condition

Progress in the cosmetology medicine industry is developing rapidly and proof of this is tretinoin cream. Possessing healing and rejuvenating qualities, it is gaining increasing popularity. Buying tretinoin cream means taking the first step towards the health and youth of your skin.

Tretinoin is the only anti-wrinkle cream approved by the American Drug Administration (FDA)

Tretinoin cream - against pimples and acne:

A person who is faced with the problem of acne at least feels uncomfortable. Firstly, it causes quite a lot of discomfort, and secondly, it greatly spoils the appearance. Tretinoin cream is an anti-inflammatory, moisturizing, healing and vitamin-rich product. This cream is widely used to treat pimples, acne and even fights very well against some forms of dermatitis. Tretinoin cream is quickly and deeply absorbed into the skin, providing anti-inflammatory, nourishing, healing and smoothing properties, protecting the subcutaneous tissue from lesions and diseases.

Long testing and the use of high-precision technologies made it possible to obtain this high-quality product, leaving far behind previously presented products for the care and treatment of the skin. And many positive reviews from people who have already experienced the healing properties of the cream only prove the effectiveness of this product. And if a person is faced with a problem, acne, blackheads or other skin lesions, then, of course, you should buy tretinoin cream .

Compound

Tretinoin (transretinoic acid) is the active substance and is a crystalline powder with a distinct floral odor. The substance is highly soluble in dimethyl sulfoxide , difficult to dissolve in polyethylene glycol , octanol and 100% alcohol ( ethanol ), almost insoluble in water (solubility index at a temperature of 25 ° C is 0.126 mg/l), mineral oils and glycerin . The color of the powder can vary from yellow to light orange.

pharmachologic effect

The substance Tretinoin belongs to the groups “Other antitumor drugs”, “Dermatotropic drugs”, as well as to the group “Vitamins and vitamin-like drugs”.

By affecting the body, it provokes:

• antitumor;
• keratolytic;
• antiseborrheic;
• comedolytic;
• immunostimulating;
• stimulating tissue regeneration;
• local anti-inflammatory effect.

Tretinoin is also used as a treatment for acne vulgaris and as a provitamin A.

Pharmacodynamics and pharmacokinetics

Tretinoin is classified as a systemic retinoid , which is an inducer of cellular differentiation. Its structure is similar to vitamin A and is a product of the metabolization of retinol .

The substance promotes the induction of cell differentiation processes, while inhibiting the proliferation of promyelocytes (precursors of granulocytes ), which is caused by a change in the binding of trans-retinoic acid to the receptors of the cell nuclei of retinoic acid (including in myeloid leukemia ).

promyelocytes originating from the leukemic clone is activated , as well as the processes of their replacement in the bone marrow and peripheral blood by non-transformed normal hematopoietic polyclonal cells .

Against this background, the patient develops remission of the disease, which averages from two to four months.

When applied topically, Tretinoin is able to penetrate cell membranes , forming a cytoplasmic complex that enters the cell nucleus. The resulting hormone-receptor complex has the ability to bind to DNA and interfere with the transcription process, thereby disrupting protein biosynthesis (it is on these processes that the hypopigment effect of Tretinoin is based).

The substance has a stimulating effect on the mitosis of cells of the epidermal layer of the skin, helps to increase the amount of mucopolysaccharides and elastic fibers formed by the protein elastin, which are located in the papillary layer of the skin.

In addition, Tretinoin:

• suppresses the process of melanin ;
• stimulates the growth and differentiation of epithelial ;
• inhibits the adhesion of cells that form acne ;
• when applied to open acne it evens out the epidermis without leaving signs of inflammation;
• when applied to closed acne , it promotes their opening or transformation into papular nodules and further healing without scarring after removing the keratin plug from them;
• prevents the formation of new acne .

The keratolytic effect of Tretinoin is to eliminate the phenomena of keratosis . Its mechanism is due to the suppression of keratinocyte proliferation and improvement of their exfoliation processes.

The antiseborrheic effect is caused by inhibition of the proliferation of epidermal cells , inhibition of the proliferation of epithelial tissue of the excretory ducts of the sebaceous glands , a decrease in the production of sebum and the normalization of the processes of its evacuation, a decrease in the severity of the inflammatory reaction around the sebaceous glands , as well as stimulation of skin regeneration .

Comedolytic and local anti-inflammatory effects are expressed in the form of absorption of excess amounts of sebaceous secretion, inhibition of its production by the sebaceous glands , narrowing of pores and elimination of signs of the inflammatory process .

A noticeable therapeutic effect from the use of Tretinoin is observed approximately one and a half months after starting to use the drug (usually at 6 or 7 weeks). The maximum effect is observed after 8-12 weeks of its use.

Transretinoic acid is an endogenous metabolite of vitamin A , which is normally always present in human plasma After oral administration, the substance is well absorbed in the stomach and intestines, its maximum concentration in the blood plasma is observed after three hours.

Tretinoin absorption rates may vary, both in different groups of patients and in each individual patient. The substance is capable of significantly binding to proteins in the blood plasma (mainly albumin ). The binding rate is within 95%.

The half-life averages 0.7 hours. After a single dose of Tretinoin at a dose of 40 mg, its maximum concentration in the blood plasma returns to its original level after approximately 7-12 hours.

The drug does not accumulate in the body and does not linger in its various tissues even after repeated administration.

Transretinoic acid is characterized by the ability to induce its own metabolism , which is reflected in a decrease in AUC and a decrease in plasma concentrations by an average of one third a week after continuous use of the drug. However, increasing the dose does not adequately increase plasma concentrations.

About 60% of Tretinoin in the form of metabolites , which are formed during the process of oxidation and glucuronidation, is eliminated by the kidneys within 3 days (72 hours). Metabolites partially excreted with the intestinal contents within 3 to 6 days.

Repeated administration provokes a decrease in concentration, which is caused by the induction of the enzyme system cytochrome c-oxidases (cytochrome P450). As a result, clearance increases and the bioavailability of the substance decreases after oral administration.

If the drug is used for cutaneous application, the absorption rate of Tretinoin varies from 1.41-31%. First of all, it is influenced by such parameters as:

• general condition of the patient’s skin;
• surface area to be treated;
• duration of drug use.

After cutaneous application, 4.45% of the absorbed dose of Tretinoin is eliminated by the kidneys along with urine and about 1.6% along with bile.

Indications for use

Oral Tretinoin is prescribed to patients who have been diagnosed with a variant of acute myeloid leukemia , characterized by an abnormal accumulation of one of the types of myeloid cells - promyelocytes .

Moreover, the use of the drug provokes the induction of remission of the disease both in patients who have not previously undergone a course of treatment, and in patients who have suffered relapse/relapses of APML (an acute form of promyelocytic leukemia ), or are refractory to standard chemotherapy carried out using rubomycin , cytorabine or their analogues.

After the onset of complete remission of the disease, patients are shown consolidation chemotherapy in full doses.

The drug instructions warn that patients undergoing maintenance therapy with Tretinoin may experience a loss of response to treatment.

As an external agent, Tretinoin is used to treat:

• confluent eels (that is, eels that are the result of the merger of several indurative eels connected to each other through deep passages);
• acne vulgaris , which is accompanied by the formation of papules (nodules), comedones (plugs formed by sebum at the mouth of the hair follicles) or pustules (filled with purulent contents of the rash elements);
• Favre-Rakucho disease (colloid degeneration of the skin, which is a dermatosis of unknown origin);
• skin hyperpigmentation.

Contraindications

Contraindications to the use of Tretinoin in capsule form are:

• increased individual sensitivity to tretinoin;
• pregnancy (the drug has a teratogenic effect on the fetus, causing serious disorders of embryonic development);
• breastfeeding (if the drug cannot be avoided, breastfeeding should be stopped).

External use is prohibited:

• during pregnancy;
• people who have acute inflammatory lesions of the skin;
• for eczema ;
• in the presence of wounds and burns;
• with cutaneous epithelioma (including those cases where the disease was noted in the family history).

Pharmacological properties

Tretinoin is a cream (reviews about the therapeutic effect of the product help a person evaluate its effectiveness) with pronounced regenerating properties. The product helps speed up the process of restoration of skin cells in case of various injuries.

The product also has antiseborrheic properties, helps eliminate the external manifestations of acne, acne and other cosmetic defects.

As a result of course use:

• damaged skin is restored;
• signs of inflammation are eliminated;
• local immunity improves.

The drug also has keratolytic properties, which improves the condition of the outer layer of the skin and prevents the progression of the pathological condition. The complex effect of the drug helps to quickly eliminate acute manifestations of the disease and prevent the recurrence of manifestations.

Side effects

When taking the drug orally, approximately a quarter of patients develop the so-called “ retinoic acid syndrome ,” which can be fatal if not properly treated.

The main signs of “ retinoic acid syndrome ” are shortness of breath , fever , acute respiratory distress syndrome , the formation of infiltrates in the lungs, hyperleukocytosis (increased levels of leukocytes, in which their concentration in the blood exceeds 40-50 thousand per 1 cubic mm), hypotension , pathological accumulation of fluid in the pleural cavity ( pleural effusion ), liver, as well as renal and multiple organ failure .

Other possible adverse reactions include:

• Skin reactions, which are expressed in the form of symptoms of xeroderma (increased dryness and flaking of the skin), increased dry mouth, cheilosis (inflammatory lesions of the red border of the skin and lips), rashes, itching, intradermal hemorrhages, increased sweating, hair loss ( alopecia ), the appearance of cellulite, increased sensitivity of the body to the action of ultraviolet rays ( photosensitization ), the appearance of blisters or crusts on the skin, the appearance of temporary foci of hyper- or hypopigmentation .
• Disorders of the digestive system, including nausea , vomiting , pain in the epigastric region, stool disorders (both constipation and diarrhea are possible), the development of bullous stomatitis , increased activity of intracellular liver enzymes ALT and AST ( alanine and aspartate aminotransferases ).
• Disturbances in the function of the central nervous system , which are expressed in the form of depression , impairment of consciousness, hearing and vision, the appearance of dizziness , increased levels of anxiety, increased levels of intracranial pressure .
• Metabolic disorders, expressed in the form of increased plasma concentrations of cholesterol and triglycerides , as well as changes in body weight.
• Disturbances in the function of the respiratory system, which are expressed in the form of cough , infection of the upper and lower respiratory tract , shortness of breath , dyspnea , swelling of the mucous membrane of the nose and larynx , the appearance of pleural effusion and wheezing in the lungs, the development of pharyngitis and the appearance of stridor .
• Disorders of the musculoskeletal system, expressed in the form of muscle pain and bone pain .
• Disturbances in the function of the heart and vascular system, which are expressed in the form of arrhythmias .
• Increased bleeding .
• Increased weakness and drowsiness.
• Development of secondary infections .
• The appearance of pain in the chest and back.

Depending on the severity of side effects, the patient may be advised to completely stop treatment with the drug or to temporarily discontinue it.

Restrictions on appointment are:

• children under one year of age when administered orally;
• children under twelve years of age when prescribing Tretinoin as an external agent;
• lack of reliable contraception among women of childbearing age;
• renal dysfunction;
• liver dysfunction;
• increased intracranial pressure ;
• age over fifty years;
• leukocytosis;
• chronic intoxication (in particular, alcoholic beverages);
• hypertriglyceridermia;
• hypercholesterolemia;
• pancreatitis;
• diabetes.

Side effects of the drug Tretinoin

When treated with trans-retinoic acid at recommended doses, the most common side effects may be symptoms of hypervitaminosis A, which occur with all other retinoids. Skin and mucous membrane: dry skin, erythema, rash, itching, increased sweating, alopecia, cheilitis, dry mucous membrane of the mouth, nose, conjunctiva and other mucous membranes with or without signs of inflammation, occasionally - the formation of ulcers on the mucous membrane of the genital organs , Sweet's syndrome, erythema nodosum. CNS: headache, intracranial hypertension (mainly in children), fever, chills, dizziness, confusion, anxiety, agitation, depression, paresthesia, insomnia, weakness. Sense organs: visual and hearing impairment. Musculoskeletal system: bone pain, chest pain, in isolated cases - myositis. Gastrointestinal tract: nausea, vomiting, abdominal pain, diarrhea, constipation, loss of appetite, pancreatitis. Metabolic, liver and kidney disorders: increased concentrations of TG, cholesterol, creatinine in the blood serum, increased activity of transaminases (AlAT, AST), isolated cases of hypercalcemia. Respiratory organs: pleural effusion, shortness of breath, respiratory failure, bronchospasm. Cardiovascular system: cardiac arrhythmia, flushing, edema, isolated cases of thrombosis. Hematopoietic system: isolated cases of thrombocytosis, severe basophilia with or without clinically significant hyperhistaminemia, mainly in patients with a rare variant of APML with basophilic differentiation. The decision to interrupt or continue therapy should be based on an assessment of the balance between the benefits of treatment and the risk of side effects. “Retinoic acid syndrome” in APML: in clinical studies, hyperleukocytosis was often noted (75% of patients). Many patients with APML (up to 25%) develop retinoic acid syndrome (RAS) during treatment with tretinoin. IBS is characterized by fever, shortness of breath, acute respiratory distress syndrome, the occurrence of pulmonary infiltrates, arterial hypotension, pleural and pericardial effusion, edema, weight gain, hepatic, renal and multiple organ failure. IBS is often accompanied by hyperleukocytosis and can be fatal.

Tretinoin cream, instructions for use (Method and dosage)

The drug is prescribed exclusively by a doctor who has experience working with hematological and oncological diseases.

The recommended daily dose for oral administration is 45 mg of Tretinoin per square meter of body surface skin for ninety days (or for thirty days after the onset of complete remission of the disease; treatment is supplemented chemotherapy using cytostatic drugs ). The dose does not depend on the patient's age and is the same for adult patients, the elderly, and children.

The maximum permissible dose is considered to be a daily dose equal to 195 mg of Tretinoin for each square meter of body surface skin. The maximum permissible daily dose for children is 60 mg of Tretinoin for each square meter of skin on the body surface.

If the patient is diagnosed with renal and/or liver failure , then the daily dose is recommended to be reduced to 25 mg of Tretinoin for each square meter of body surface skin.

For patients with extensive tumors, the daily dose is one third of the maximum permissible; for children, it is lower than the maximum recommended, as prescribed by the attending physician.

Two to four months after completing the course of treatment with Tretinoin, a relapse of the disease .

When taking the drug orally, to reduce the likelihood of developing “ retinoic acid syndrome ” when the concentration of leukocytes or any of the signs of this condition appear, the patient is prescribed full chemotherapy , which involves the administration of cytostatic agents in adequate doses.

As a topical treatment, Tretinoin lotion, gel or cream is applied to the affected skin in a very thin layer once a day and left on for six hours. After this time, the drug must be washed off under running water.

A small amount of cream is squeezed onto the fingertip and distributed evenly on the face, starting from the forehead, chin and neck. Then move on to other affected areas.

The cream is rubbed in with light movements. At the same time, it should immediately become invisible or, at a minimum, unnoticeable. If the cream peels off after it dries or is too noticeable on the skin, this is evidence that the dose has been exceeded.

It is important to remember that excess amount of cream does not guarantee better or faster results.

For fair-skinned people, as well as people with extremely dry skin, it is recommended to apply Tretinoin for no more than half an hour at the initial stages of treatment. Then a gradual increase in the duration of skin contact with the drug is allowed.

During the treatment process, it is also possible to gradually remove mature and completely softened comedones and pustules.

According to the instructions, the duration of treatment can vary from one to two weeks to three months. To prevent the appearance of acne, Tretinoin is applied after a warm bath one to three times a day for a long period of time.

Use of the drug Tretinoin

The daily dose is 45 mg/m2 of body surface orally in 2 divided doses. For children, the same dose (45 mg/m2) is recommended unless severe toxic effects occur; in particular, the dose should be reduced if the child has an unbearable headache. Treatment should be continued for 30–90 days until complete remission is achieved. After this, it is necessary to immediately switch to a standard consolidation chemotherapy regimen, for example, three courses of daunomycin and cytosine arabinoside with an interval of 5-6 weeks. If remission occurs with tretinoin monotherapy, there is no need to change its dose when adding chemotherapy. Due to the lack of sufficient information regarding patients with renal or hepatic insufficiency, patients in this category should reduce the dose to 25 mg/m2.

Interaction

Tretinoin is metabolized in the liver under the influence of enzymes of the cytochrome c oxidases system. For this reason, combined use with the drug of drugs that affect this enzyme system may provoke changes in the pharmacokinetic parameters of Tretinoin.

With the simultaneous use of Tretinoin and contraceptives , which are based on progesterone , the effectiveness of the latter is significantly reduced.

The simultaneous use of Tretinoin with tetracyclines in patients may experience an increase in intracranial pressure .

Simultaneous use with vitamin A provokes the development of symptoms of hypervitaminosis .

Tretinoin drug interactions

Since trans-retinoic acid is metabolized in the liver by the cytochrome P450 system, there is a possibility of altering the pharmacokinetics of concomitantly administered drugs that are inducers or inhibitors of this enzyme system. Medicines that stimulate the activity of enzymes of the cytochrome P450 system include rifampicin, corticosteroids, phenobarbital and pentobarbital. Drugs that inhibit the activity of cytochrome P450 enzymes include ketoconazole, cimetidine, erythromycin, verapamil, diltiazem and cyclosporine. There are no data indicating changes in the effectiveness or toxicity of these drugs when used concomitantly with trans-retinoic acid. There is no information on possible pharmacokinetic interactions between trans-retinoic acid and daunomycin and cytosine arabinoside. Antifibrinolytic agents, such as tranexamic acid, aminocaproic acid and aprotinin: isolated cases of thrombotic complications with a fatal outcome have been described in patients who simultaneously used trans-retinoic acid and antifibrinolytic drugs. Caution must be exercised when prescribing trans-retinoic acid with these drugs. Low-dose progestogens (mini-pills): trans-retinoic acid reduces the contraceptive effectiveness of these drugs. Tetracyclines: Systemic retinoid therapy may lead to intracranial hypertension. Since tetracycline drugs can also increase intracranial pressure, they should not be used concomitantly with trans-retinoic acid. Vitamin A: Like other retinoids, trans-retinoic acid should not be used in combination with vitamin A due to the potential for hypervitaminosis A.

special instructions

When using creams, gels and lotions for external use, avoid getting the drug into the eyes, mouth, corners of the nose, open wounds and mucous membranes. If this happens, you must immediately rinse Tretinoin thoroughly with water.

During the course of treatment with the drug, it is recommended to avoid exposure to the sun. For those patients who have already tanned, treatment should begin after the tan has subsided somewhat.

Sunscreen should be applied over damaged skin areas or covered with clothing. When using Tretinoin preparations for external use, it is not recommended to be in the wind or cold.

acne may increase acne localized in the deep layers of the skin , which remained invisible before the start of treatment.

When taking the drug orally by women of childbearing age (even if they have been diagnosed with infertility), it is recommended to use reliable contraceptives . Their use begins at least a month before the start of therapy, continues throughout the course of treatment and then for another month after discontinuation of the drug.

Treatment usually begins on the second or third day of the normal menstrual cycle . Two weeks before starting therapy, laboratory confirmation should be made that the woman is not pregnant. Subsequently, pregnancy tests are recommended to be taken monthly.

If pregnancy occurs during the course of treatment with Tretinoin, due to the high teratogenicity of the drug, the risk of having a child with deformities and other developmental defects is very high.

There is insufficient information regarding the effectiveness and safety of treating children with Tretinoin. There is, however, evidence of an increase in toxic symptoms in children who were treated with the drug (in particular, there were cases of increased intracranial pressure ). For this reason, it is recommended to avoid the use of Tretinoin in pediatrics .

Treatment with the drug may impair the ability to drive vehicles and operate potentially dangerous mechanisms and devices. This is due to the fact that quite often taking Tretinoin is accompanied by severe headaches and dizziness .

The drug in the form of a cream is flammable, so open flames and smoking should be avoided while using it.

If symptoms of severe irritation appear, use of the drug as an external agent should be discontinued.

In some cases, there may be incompatibility of the drug with certain products for topical use: soap (both regular and medical), washing gels, cosmetics, etc.

It is also necessary to take special care when using drugs that contain sulfur, resorcinol or salicylic acid .

Overdose

When applied externally, the likelihood of an overdose is quite low. Only sometimes such disorders are observed if the patient takes the medicine in higher doses and more often than required over a long period of time.

An overdose is accompanied by headache, weakness and bouts of vomiting. The condition worsens with the development of motor disorders. Among the external manifestations, one can note a deterioration in the condition of the skin, nails and hair.

If signs of overdose appear, it is important to immediately stop using the product and visit a doctor. The patient is provided with care in a hospital setting and under supervision. The drug does not have a specific antidote, but to eliminate the symptoms, Dexamethasone is administered for 3 days. Usually this time is enough to eliminate the manifestations.

Reviews of Tretinoin

The drug deservedly enjoys a reputation as an effective remedy for problem skin. Numerous positive reviews about Tretinoin cream indicate that if you follow all the recommendations listed in the instructions, acne and pimples disappear almost without a trace after two weeks of treatment.

However, according to reviews from pharmacists, Tretinoin has a number of serious side effects. After treatment with Tretinoin, the patient develops retinoid dermatitis. This is normal and even good. This means the drug starts working! But with Tretinoin, this dermatitis is very acute and can leave scars, and this active substance is not removed from the liver. The consequences of use have not yet been studied. Therefore, Tretinoin is not permitted in the Russian Federation.

Price

The cost of Tretinoin is unknown, since the drug is not sold in pharmacies in Ukraine and Russia. But its substitutes can be purchased for 200-1500 rubles. This difference in cost is explained by different manufacturers. Domestic drugs are cheaper than foreign analogues.

Tretinoin is an effective and popular cream that has pronounced regenerating and anti-inflammatory properties. It is used for various dermatological pathologies; if you study patient reviews, it helps eliminate acute manifestations. Use without prior examination is strictly contraindicated.

Tretinoin price, where to buy

On the Russian and Ukrainian markets, Tretinoin can be found in the form of generic drugs, which are:

• Vesanoid capsules , Hoffmann la Roche, Switzerland;
• cream and solution for external use Locacid , Pierre Fabre Medicament, France;
• cream and gel Retin-A (Retin-A) Janssen-Silag (Johnson & Johnson Corporation), India;
• cream Airol , Pierre Fabre Italia SpA, Italy.

The average price of Tretinoin cream, as well as the drug in capsule form, depends on the manufacturer.

So, Airol in the form of a cream or lotion will cost 2-2.5 thousand Russian rubles. The average price of Vesanoid capsules varies from 10 to 14 thousand Russian rubles per package of 100 pieces. Lokacid cream is approximately 1.5 thousand Russian rubles per tube with a capacity of 30 g.

However, you should know that the drug Tretinoin ( Retin-A ) is not registered in the Russian Federation and is not sold in retail pharmacies. The product is sold mainly on dubious sites that are not online pharmacies.

Considering the number of positive reviews about the drug, many people facing the problem of acne ask the question “where to buy Tretinoin in Moscow?” Since this drug is prohibited in the Russian Federation, it is recommended to use drugs based on Isotretinoin: Retinoic ointment and Retasol.

• Online pharmacies in RussiaRussia

Analogs

The drug has several analogues that have pronounced properties. They are used most often, since the original product is not available in Russia and Ukraine.

The most common substitutes:

• Retin-A is a popular tretinoin-based cream that has a pronounced anti-inflammatory and regenerating effect. Prescribed for various skin lesions, helps eliminate symptoms and prevent progression of the condition.
• Retasol is a solution for external use that contains isotretinoin as the main active substance. It has antiseborrheic, anti-inflammatory and regenerating properties. The product is considered effective and is often used when dermatological problems occur.
• Retinoic ointment is a product based on isotretinoin, which is considered the most popular analogue. It has pronounced properties and is used for skin lesions of varying shapes and severity. The drug is one of the most accessible medications, therefore it is used most often.

Substitutes can be used in the absence of contraindications and after consulting a doctor. Independent uncontrolled use often leads to the development of negative reactions.