Active substance: retinol acetate (vitamin A-acetate);
1 ml of solution contains retinol acetate (vitamin A-acetate), in terms of 100% retinol acetate - 34.4 mg (100,000 ME);
auxiliary substance: sunflower oil refined deodorized brand P, frozen.
Pharmacotherapeutic group
Vitamins. Vitamin A.
Pharmacological properties
Pharmacodynamics
Vitamin A belongs to the fat-soluble vitamins. As a consequence a large number unsaturated bonds plays an important role in redox processes, is involved in the synthesis of mucopolysaccharides, proteins, lipids. Retinol plays an important role in maintaining the normal state of the skin and epithelium of the mucous membranes, ensuring normal differentiation of epithelial tissue, in the processes of photoreception (contributes to human adaptation to darkness). Retinol is involved in mineral metabolism, cholesterol formation processes, enhances the production of lipase and trypsin, enhances myelopoiesis, cell division processes; essential for bone growth, normal reproductive function, embryonic development. Local action is mediated by the presence of specific retinol-binding receptors on the surface of epithelial cells. It inhibits keratinization processes, enhances the proliferation of epithelial cells, rejuvenates cell populations and reduces the number of cells that follow the path of terminal differentiation.
Pharmacokinetics
Retinol acetate taken internally is well absorbed in the upper regions small intestine... Then, as part of chylomicrons, it is transported from the intestinal wall to lymphatic system and through the thoracic duct enters the bloodstream. The transport of retinolesters in the blood is carried out by β-lipoproteins. The maximum level of vitamin A esters in the blood serum is observed 3 hours after ingestion. The place of deposition of vitamin A is the liver parenchyma, where it accumulates in stable ester forms. In addition, a high content of vitamin A is found in the retina pigment epithelium. This depot is necessary for the regular supply of the outer segments of rods and cones with vitamin A.
Retinol is biotransformed in the liver, then in the form of inactive metabolites, it is excreted by the kidneys. Retinol can be partially excreted in the bile and is involved in enterohepatic circulation. Elimination of retinol occurs slowly - 34% of the taken dose of the drug is excreted from the body in 3 weeks.
Indications for use
Vitamin A deficiency, which cannot be compensated for with food.
Contraindications
Hypersensitivity to the components of the drug, acute and chronic nephritis, heart failure in the stage of decompensation, cholelithiasis, chronic pancreatitis, hypervitaminosis A, overdose of retinoids, hyperlipidemia, obesity, chronic alcoholism, sarcoidosis (including history), increased intracranial pressure.
Sharp inflammatory diseases skin, pregnancy, children under 7 years of age. With care: liver cirrhosis, viral hepatitis, nephritis, renal failure, old age.
Interaction with other medicinal products
If you are taking any other medicines, be sure to inform your doctor!
Estrogens increase the risk of developing hypervitaminosis A.
Retinol acetate reduces the anti-inflammatory effect of glucocorticoids.
Retinol acetate should not be taken simultaneously with nitrites, cholestyramine, colestipol, neomycin, as they interfere with the absorption of the drug.
Retinol acetate cannot be used in conjunction with other derivatives of vitamin A due to the risk of overdose, the development of hypervitaminosis A.
The combination with vitamin E contributes to the retention of retinol acetate in an active form, absorption from the intestines and the occurrence of anabolic effects.
The simultaneous use of petroleum jelly oil can interfere with the absorption of the vitamin in the intestine.
The simultaneous intake of vitamin A and anticoagulants increases the tendency to bleeding. Isotretinoin increases the risk of developing toxic effects when taken simultaneously.
Precautionary measures
Consult your doctor before starting treatment!
When using the drug, you must adhere to the doses recommended by your doctor!
The drug should be taken under medical supervision. With prolonged use of Retinol acetate, it is necessary to monitor the biochemical parameters and blood clotting time.
In the treatment of impaired twilight vision (night blindness), Retinol acetate should be used in complex treatment.
Use with caution in case of severe damage to the hepatobiliary system, diseases accompanied by blood clotting disorders.
The drug tends to accumulate and stay in the body for a long time. Women who have taken high doses of retinol can plan a pregnancy no earlier than 6-12 months later. This is due to the fact that during this time there is a risk of abnormal development of the fetus under the influence of the high content of vitamin A in the body.
For the normal absorption of vitamin A, a prerequisite is the presence of fat in food.
Alcohol and tobacco abuse interferes with the absorption of the drug from the digestive tract.
The use of the drug in patients on hemodialysis can lead to hypervitaminosis A in combination with hypercalcemia.
Patients with severe type V hypertriglyceridemia are also at risk of developing hypervitaminosis A.
Concomitant use of alcohol can lead to toxic effects on the liver. The drug contains butylhydroxytoluene.
Use during pregnancy or lactation
Due to the high dose of vitamin A in this dosage form, the drug is contraindicated for oral administration during pregnancy or lactation.
The ability to influence the reaction rate when driving or operating other mechanisms
There are no data on the effect of the drug on the ability to drive a car or work with complex mechanisms.
Children
The drug is prescribed for children over 7 years old.
Method of administration and dosage
The use of the medicinal product should be carried out under the supervision of a physician.
The duration of the course of treatment and the dose of the drug are determined by the doctor individually for each patient, depending on the severity clinical picture vitamin A deficiency, course of the disease, drug tolerance.
Is taken orally, 10-15 minutes after eating.
1 ml of the preparation contains 100,000 IU of vitamin A. 1 drop from an eye dropper, which is attached to the package, contains about 3,000 IU of vitamin A.
In the treatment of mild to moderate vitamin A deficiency in adults, therapeutic doses are up to 33,000 IU per day.
The highest single dose of vitamin A for adults is 50,000 ME, for children from 7 years old - 5,000 ME. The highest daily dose vitamin A for adults is 100,000 ME, for children from 7 years old - 20,000 ME.
Overdose
If the level of retinol in the blood serum is higher than 1 mg / l, signs of hypervitaminosis A may develop. In pregnant women, the teratogenic effect of the drug on the fetus is possible.
Acute hypervitaminosisA can develop from a single dose of the drug in a dose of 500 mg of retinol, which is equivalent to 1.5 million IU of vitamin A in adults, 100 mg or 300,000 IU in children and 30 mg or 100,000 IU in young children.
The following overdose symptoms may occur: headache, dizziness, extreme fatigue, drowsiness, confusion, convulsions, nausea, indomitable vomiting, profuse diarrhea, disc edema optic nerve, visual disturbances, bleeding gums, massive peeling of the skin. In children - protrusion of the large fontanelle.
Overdose leads to activation of fibrinolysis, impaired blood clotting, increased activity of ACT and ALT in serum.
Chronic hypervitaminosisA, accompanied by an increase in the size of the liver and impaired renal function can develop with prolonged daily intake of vitamin A in adults at a dose of 100,000 ME, children - from 18,000 to 60,000 ME. Chronic overdose is possible with prolonged use of lower doses.
Early symptoms of chronic overdose: dry skin followed by coarse peeling, itching, cracking, impaired hair growth, fatigue, osteoalgia and hemorrhages.
Late symptoms of chronic overdose: hepatosplenomegaly, liver cirrhosis with manifestations of portal hypertension and ascites, increased intracranial pressure, increased alkaline phosphatase activity and serum calcium levels. In children, late symptoms are manifested: chronic intoxication, premature closure of the epiphyseal growth zones, growth retardation.
Treatment: if symptoms of an overdose appear, the drug should be canceled; in case of acute poisoning, measures should be taken to prevent absorption of the drug.
Treatment is symptomatic. There is no specific antidote.
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Side effect
Long-term intake of large doses of vitamin A can cause the development of hypervitaminosis A.
From the nervous system and sensory organs: fatigue, drowsiness, lethargy, irritability, headache, loss of sleep, convulsions, discomfort, intraocular hypertension, visual impairment.
From the digestive system: loss of appetite, weight loss, nausea, abdominal pain, aphthae, dry mouth, very rarely - vomiting.
Possible exacerbation of liver disease, increased activity of transaminases and alkaline phosphatase.
From the urinary system: pollakiuria, nocturia, polyuria.
From the hematopoietic system: hemolytic anemia.
On the part of the musculoskeletal system: changes in bone radiographs, gait disorder, soreness of the bones of the lower extremities.
From the immune system: hypersensitivity reactions.
On the part of the skin and subcutaneous tissue: cracks in the skin of the lips, yellow-orange spots on the soles, palms, part of the nasolabial triangle, subcutaneous edema; in some cases, on the first day of use, an itchy maculopapular rash may occur, which requires discontinuation of the drug; itching, erythema and rash, dry skin, hair loss, photosensitivity.
Other: violation of the menstrual cycle, hypercalcemia, fever, hyperemia of the face, followed by desquamation.
With dose reduction or with temporary cancellation medicinal product side effects go away on their own.
In case of skin diseases, the use of high doses of the drug after 7-10 days of treatment may be accompanied by an exacerbation of the local inflammatory reaction, which does not require additional treatment and further weakens. This effect is associated with the myelo- and immunostimulating effects of the drug.
In case of any undesirable reactions, consult your doctor regarding the further use of the drug!
Storage conditions
Store in original packaging in a refrigerator (at temperatures from + 2 ° C to + 8 C).
Best before date
Do not use the medicinal product after the expiry date indicated on the package. Keep out of the reach of children.
Vacation conditions
On prescription.
Package
10 ml of solution in glass vials. 1 bottle and an eye dropper in a cardboard box.
Manufacturer (applicant) information
PJSC "Technologist", Ukraine, 20300, Uman, Cherkasy region, st. Manuilsky, 8.
Retinol acetate is a synthetically obtained vitamin A. Everyone knows about its benefits for vision, but many do not even know about its other pharmacological effects... This compound is indispensable for the beauty of the skin, normal growth of hair, nails, health of the mucous membranes of the mouth and digestive tract.
In conditions of its shortage (which is observed in most of the inhabitants of the middle lane), chronic fatigue and immunodeficiency appear. To compensate for the deficiency of essential substances, they resort to the use of their pharmaceutical counterparts, which are available on the market (over-the-counter).
Details about retinol acetate: what kind of vitamin is it, what is it for and its sources, in the video:
What is the composition of the drug
The main active ingredient of all drugs is retinol acetate. The pharmaceutical industry produces it in both liquid and solid form. Manufacturers offer us three options for funds:
- Drops come with an active substance concentration of 3.44% and 8.6%. They can be ingested or used externally. Butylhydroxyanisole and oil are used as additional components. It is a yellowish liquid with a greasy consistency.
- Retinol acetate solution in sunflower oil. Liquid oil solution with a concentration of 100,000 and 250,000 ME in one milliliter.
- Gelatin capsules, film-coated tablets. For ease of administration, the active ingredient in an amount of 0.15 ml is enclosed in a gelatin, glycerin and starch shell.
Retinol acetate solution is sold in darkened vials of 10 and 50 ml, as it is destroyed by ultraviolet radiation.
Pharmacology
Pharmacodynamics: how does it affect the body
Retinol accelerates the reaction of formation of rhodopsin in the cells of the retina - the visual pigment. Its presence provides a person with normal twilight vision. Its deficiency leads to the development of hemeralopia, popularly called "night blindness".
Another important function of vitamin A is participation in the process of epithelialization (the formation and growth of cells in the outer layer of the skin and mucous membranes). Thus, the constant renewal of the epithelium, its regeneration in case of damage, is maintained. Hypovitaminosis on the part of the skin is manifested by dermatitis, dryness and peeling of the skin. Due to a violation of the renewal process of the epithelium of the gastrointestinal mucosa, stomatitis, gastritis, and digestive disorders develop.
Vitamin A has an immunostimulating effect. There is evidence of its participation in the synthesis of sex hormones, regulation of reproductive functions and regulation of pigment metabolism.
Pharmacokinetics: metabolism of drug components
It is a fat-soluble substance. It is absorbed only in the presence of fats. Therefore, all forms of drug release include sunflower oil. The agent is absorbed into the bloodstream in the duodenum, where it is transported in free form or bound to proteins to target cells.
Vitamin A is able to accumulate in liver cells, but here it is metabolized after use and excreted by the kidneys in the urine. May cross the placental barrier and into breast milk during feeding.
When Retinol Acetate is Used
Vitamin A can be both part of a general strengthening therapy and an independent remedy. Indications for use:
- deficiency (hypo- and vitamin A deficiency) - the diagnosis is made on the basis of symptoms and biochemical blood test;
- xerophthalmia - dry eye syndrome;
- keratoses and keratitis - corneal pathology;
- hemeralopia - decreased visual acuity in low light conditions;
- retinitis - inflammation of the retina of the eye;
- inflammatory lesions of the eyelids (blepharitis)
- conjunctivitis;
- skin diseases (ulcers, furunculosis, dermatitis, dry skin, trauma, burns, frostbite, etc.);
- in dentistry it is used to eliminate stomatitis (inflammation of the oral mucosa);
- atopic (allergic) dermatitis;
- gastritis, gastroduodenitis, peptic ulcer;
- cirrhosis of the liver;
- chronic laryngitis, bronchitis, bronchoadenitis, etc.
Vitamin A is a full-fledged medicine only in case of hypovitaminosis A. For other diseases, it is part of the complex treatment prescribed by the doctor.
Contraindications
It is worth knowing not only what retinol acetate is used for, but also in what cases it is contraindicated.
There are a number of situations in which retinol acetate is hazardous to health:
- hypervitaminosis A;
- individual intolerance to one of the components of the product;
- cholelithiasis;
- skin inflammatory diseases in the acute stage;
- pancreatitis;
- stage of exacerbation of hepatitis;
- insufficiency of the functions of the urinary system;
- pregnancy and lactation.
Retinol acetate should not be given to children under 7 years of age. To avoid toxic effects on the body, it is recommended to consult a doctor before taking vitamins.
Directions for the use of various forms of the drug
To know how to take retinol acetate, you need to determine the safe amount of retinol. When calculating the daily intake of a substance, it is taken into account that the maximum safe daily dosage of retinol acetate for an adult is 90,000-100,000 IU, for children - 16,000-20,000 IU.
Instructions for the use of retinol acetate have features for each form of drug release.
Retinol acetate oil solution 3.44%
Retinol acetate (vitamin A oil solution) is also recommended to be consumed 1-2 times a day after the main meal. The maximum therapeutic dose for people over 18 years old is 8-10 drops, for children - 2. Dosages are indicated for a solution with an active substance concentration of 3.44. If a drug with a concentration of 8.6% is used, the number of drops is halved:
- adults with hypovitaminosis 8 drops per day, children - 1;
- in ophthalmology for adults, 10-20 drops, it is recommended to combine with the use of vitamin B2;
- in dermatology and dentistry for adults, 10-20 drops, for children - 1-4 drops.
To wipe the skin and mucous membranes, a solution of retinol acetate in sunflower oil is used in the same way as drops for external use.
Drops
The drops have an oily consistency, which provides active substance sufficient absorption. Retinol acetate oral solution in drops. The optimal time for taking is after meals. It comes in 3.44% and 8.6% concentration. For convenience, it is produced in bottles with dropper stoppers. Recommended dosages:
- in order to eliminate the manifestations of a lack of vitamin A, it is recommended that adults take 8 drops of a 3.44% solution (4 drops of 8.6%);
- for skin diseases, dry eye syndrome, keratosis, hemeralopia, the daily dose of the drug is 13-25 drops of 3.44% (6-12 drops of 8.6%);
- children from 7 years old are prescribed 1-2 drops of a 3.44% solution inside.
In order to accelerate skin regeneration after burns, wounds, frostbite with a solution of retinol acetate, wipe the affected skin areas (pre-cleaned and fat-free). Next, an aseptic bandage is applied. It is necessary to lubricate the skin with vitamin A 4-6 times a day, gradually reducing the number of daily procedures to one as the healing progresses.
Retinol acetate capsules
The modern pharmaceutical industry offers more convenient dosage forms. Retinol acetate in capsules or film-coated tablets can only be used by adults, since one capsule contains more active substance than can be consumed by a child at one time. Recommended doses:
- with hypovitaminosis 1 capsule 1 time per day;
- for eye diseases, 1 capsule 3 times a day after meals, plus 20 g of vitamin B2;
- for treatment skin diseases 1 capsule 3 times a day after meals.
The instructions for use of the retinol preparation indicate the maximum permissible daily dose of vitamin A of 100,000 IU, which corresponds to 3 capsules.
Dangers of overdose
If the permissible dosages are exceeded and the excretion of the substance from the body is impaired (kidney disease), the following symptoms are observed:
- dizziness, weakness, confusion, acute headache;
- severe diarrhea that leads to dehydration;
- skin rashes all over the body with itching and scaling;
- minor hemorrhages under the skin;
- increased blood clotting time.
Prolonged vitamin A poisoning (hypervitaminosis) is manifested by weakness, sleep disturbances, severe headaches, blurring and double vision, a feeling of a veil before the eyes, dyspeptic disorders, muscle and bone soreness when pressure is applied to them.
If signs of an overdose appear, it is necessary to urgently stop taking vitamin preparations and seek medical help.
Alcohol abuse, smoking sharply reduces the absorption of retinol preparations.
There are precautions for use in pregnancy, kidney disease, children and the elderly.
For pregnant and lactating mothers
The substance is contraindicated at all stages of pregnancy. You can not take it while breastfeeding.
You can plan a new pregnancy at least six months after you stop taking retinol acetate. This is done to prevent the toxic effects of excess vitamin A.
For kids
Retinol acetate for children from 7 years old is approved for use under the supervision of a physician with strict adherence to dosages.
With kidney disease
For nephritis, the drug is used with caution according to the testimony of a doctor. It is recommended to take blood and urine tests every 2-4 weeks to monitor the functions of the urinary system and the general blood picture.
For liver diseases
Contraindicated in acute hepatitis, cholelithiasis. In chronic processes (liver cirrhosis), use with caution with regular monitoring of blood tests.
For the elderly
The need for this substance in older people decreases, and metabolism and kidney function deteriorate. Therefore, in order to avoid intoxication, the doses are halved, they are used only according to the testimony of a doctor.
Interaction with other drugs
Taking nutritional supplements with retinol acetate, you need to remember how dangerous this vitamin is. It cannot be taken simultaneously with vitamin A complexes, as this leads to an overdose.
In combination with antibiotics of the tetracycline group (Doxycycline, Metacyclin, Glycocycline, Oletetrin, etc.) it causes an increase in intracranial pressure. With prolonged use, hydrocephalus may develop.
It is not recommended to take orally with drugs that reduce the absorption of fats in the intestine (Cholestyramine, Colestipol, Colextran). The interval between taking retinol and bile acid sequestrants should be at least 4-6 hours.
Glucocorticosteroids (Dexamethasone, Corticosterone, etc.) increase the risk of side effects: headache, nausea, fever, drowsiness, muscle pain.
Retinol acetate reduces the effectiveness of calcium supplements.
Vitamin E reduces the ability of retinol to accumulate in the liver and thereby reduces its toxic effect on the body.
Storage conditions
The shelf life of drops is 3 years, retinol acetate oil solution and capsules - 2 years.
Retinol is rapidly degraded by high temperatures and sunlight. It should be stored out of the reach of children, at temperatures up to 10 degrees (capsules up to 25 degrees). Protect from direct sunlight.
International name: Retinol
Group: Vitamins and vitamin-like agents. Antihypoxants and antioxidants
Active ingredients: Retinol acetate or retinol palmitate
Chemical formula:
Chemical formula of Vitamin A
Release form:
- dragee (insert instructions attached)
- oral drops
- oral drops [in oil]
- capsules
- solution for intramuscular injection[oil]
- oral solution [oily]
- solution for oral administration and external use [oily]
- coated tablets
Instructions
pharmachologic effect
Retinol is an essential component for the normal functioning of the retina of the eye, as it binds to opsin (the red pigment of the retina), forming the visual purple rhodopsin, which is necessary for visual adaptation in the dark. Vitamin A is necessary for bone growth, normal reproductive function, embryonic development, for the regulation of division and differentiation of the epithelium (enhances the reproduction of skin epithelial cells, rejuvenates the cell population, inhibits keratinization processes). Vitamin A takes part as a cofactor in various biochemical processes.
Indications for use
According to the instructions, it is necessary to take retinol in the following cases:
- Hypo- and vitamin A deficiency, as well as states of increased body demand for vitamin A: gastrectomy, diarrhea, steatorrhea, celiac disease, sprue, Crohn's disease, malabsorption syndrome, cystic fibrosis of the pancreas, frequent infectious (including chronic) and “colds »Diseases
- Inadequate and unbalanced nutrition (including parenteral nutrition)
- Fast weight loss
- Nicotine addiction, drug addiction, alcoholism
- Long-term stress
- Taking cholestyramine, colestipol, mineral oils, and neomycin
- Hyperthyroidism
- Hemeralopia, xerophthalmia, keratomalacia
Currently, retinol is not recommended for the treatment of dry skin, wrinkles, eye diseases and infections not associated with vitamin A deficiency. The effectiveness of vitamin A in the treatment of kidney stones, hyperthyroidism, anemia, degenerative changes in the nervous system, sunburn, diseases lungs, hearing loss, osteoarthritis, inflammatory bowel disease, psoriasis.
Contraindications for use
- Hypersensitivity
- Vitamin A hypervitaminosis
- 1 trimester of pregnancy
Take retinol for alcoholism, liver cirrhosis, viral hepatitis, renal failure, pregnancy (especially the first trimester), during lactation, in the elderly and childhood worth only as prescribed by a doctor and in strict accordance with the instructions for use.
Side effects
- Parenteral administration - pain at the injection site, infiltration
- Overdose
Overdose
Retinol is a fat-soluble vitamin, and therefore, taking a large dose in a short time or long-term use at an increased dosage can lead to an overdose of the vitamin in the body.
Symptoms of an acute overdose (develop 6 hours after administration) of vitamin A:
- in adults - drowsiness, lethargy, double vision, dizziness, severe headache, nausea, severe vomiting, diarrhea, irritability, osteoporosis, bleeding from the gums, dryness and ulceration, agitation, oral mucosa, peeling lips, skin (especially palms ), confusion, increased intracranial pressure
- in children infancy- hydrocephalus, protrusion of the fontanelle
Chronic intoxication symptoms:
- loss of appetite, bone pain, cracks and dryness of the skin, lips, dryness of the oral mucosa, gastralgia, vomiting, hyperthermia, asthenia, excessive fatigue, discomfort, headache, photosensitivity, pollakiuria, nocturia, polyuria, irritability, hair loss, yellow - orange spots on the soles, palms, in the area of the nasolabial triangle, hepatotoxic phenomena, intraocular hypertension, oligomenorrhea, portal hypertension, hemolytic anemia, changes in bone X-rays, convulsions;
- fetotoxic phenomena: in humans - malformations of the urinary system, growth retardation, early closure of the epiphyseal growth zones; in animals - malformations of the central nervous system, spine, chest, heart, eyes, upper palate, genitourinary system.
Overdose treatment - drug withdrawal and symptomatic therapy.
Vitamin A is taken orally (capsules, oil) for prophylactic and therapeutic purposes (10-15 minutes after eating). With severe vitamin deficiency or impaired absorption in the gastrointestinal tract, intramuscular injections of a vitamin (ampoules with an oil solution) are indicated. Oil for injection has a high viscosity, therefore, before the intramuscular injection, they are heated to body temperature. In cases requiring long-term treatment (diseases of the skin, eyes), courses of intramuscular injections can be alternated with oral administration. Inside, i / m.
- With mild and moderate vitamin deficiencies, adults - 33 thousand IU / day, children - 1-5 thousand IU / day (depending on age).
- With hemeralopia, xerophthalmia, adults - 50-100 thousand IU / day, children as prescribed by a doctor.
- For skin diseases for adults - 50-100 thousand IU / day, for children as prescribed by a doctor.
special instructions
Since vitamin A is fat-soluble and is excreted from the body slowly, in order to avoid the development of hypervitaminosis A, the recommended doses indicated in the instructions for use should not be exceeded. For treatment acne high doses of Retinol are required, which increases the risk of toxic complications, therefore, in this nosology, local forms of Retinol (including tretinoin or isotretinoin) are most preferred. The daily requirement for vitamin A for an adult is 5 thousand IU (1.5 mg); for pregnant women - 6.6 thousand IU (2 mg); for lactating women - 8.25 thousand IU (2.5 mg); children under 1 year old - 1.65 thousand IU (0.5 mg); 1-6 years - 3.3 thousand IU (1 mg); 7-14 years old - 5 thousand IU (1.5 mg). In the Far North, doses for pregnant and lactating women and children are increased by 50%.
Interaction with other medicinal products
- Weakens the effect of Ca2 + preparations, increases the risk of developing hypercalcemia.
- Cholestyramine, colestipol, mineral oils, neomycin reduce the absorption of vitamin A (an increase in its dose may be required).
- Oral contraceptives increase the plasma concentration of Retinol.
- Isotretinoin increases the risk of toxic effects.
- The simultaneous use of tetracycline and vitamin A in high doses (50 thousand / U and above) increases the risk of developing intracranial hypertension.
- Vitamin E reduces toxicity, absorption, liver deposition and vitamin A utilization; high doses of vitamin E can reduce the body's stores of Retinol.
Retinol acetate: instructions for use and reviews
Latin name: Retinol acetate
ATX code: A11CA01
Active substance: retinol
Producer: Polisintez (Russia), Pharmaceutical Factory of St. Petersburg, OJSC (Russia), Marbiopharm, OJSC (Russia)
Description and photo update: 13.08.2019
Retinol acetate - vitamin A.
Release form and composition
Dosage forms of Retinol acetate:
- drops for oral administration and external use 3.44% and 8.6%: oily liquid from dark yellow to light yellow in color with a transparent structure, without rancid odor (10, 15, 30, 50 ml each in dark glass vials or 10, 30 or 50 ml in vials with a dropper cap, in a cardboard box 1 bottle);
- solution for oral administration and external use oily 3.44% and 8.6%: transparent from dark yellow to light yellow oily liquid without rancid odor (10, 15, 30, 50 or 100 ml each in dark glass vials or 10 ml in a dropper bottle, in a cardboard box 1 bottle; 10 ml (3.4% solution) in a polymer bottle, in a cardboard box 1 bottle);
- capsules: yellow, spherical, without mechanical contamination and sagging; the contents of the capsules are oily liquid from light yellow to dark yellow, there is no rancidity in the smell (10 pcs. in a blister, in a cardboard box 1-3 or 5 packs; 25 or 50 pcs. in dark glass jars , in a cardboard box 1 can).
In 1 ml of drops for oral administration and external use 3.44% and 8.6% contains:
- active substance: retinol acetate (including butylhydroxytoluene and peanut oil) 100,000 International Units (IU) and 250,000 IU, respectively;
- auxiliary components: butylhydroxyanisole, sunflower oil (refined deodorized sunflower oil).
1 ml of solution for oral administration and external use of oil 3.44% and 8.6% contains:
- active substance: retinol acetate 100,000 IU (34.4 mg) and 250,000 IU, respectively;
- auxiliary components: frozen-out refined deodorized sunflower oil, grade P.
1 capsule contains:
- active substance: retinol acetate solution for oral administration and external use oily 8.6% - 0.132 ml (33,000 IU);
- auxiliary components: refined deodorized sunflower oil;
- shell composition: glycerin (glycerol), methyl parahydroxybenzoate (nipagin), gelatin, quinoline yellow dye (E-104).
Pharmacological properties
Pharmacodynamics
Retinol acetate, vitamin A is an essential component for the normal functioning of the retina of the eye, which binds to the pigment opsin with the formation of visual purpura rhodopsin, which provides visual adaptation in the dark. Vitamin A also participates in the processes of bone growth, embryonic development, regulation of division, differentiation of the epithelium (stimulates the reproduction of epithelial cells, rejuvenates the cell population, suppresses keratinization processes), and ensures normal reproductive function. Vitamin A is a cofactor in various biochemical processes.
Pharmacokinetics
Vitamin A is rapidly absorbed from the duodenum, jejunum and other organs of the gastrointestinal tract in the presence of bile acids, proteins, fats and pancreatic lipase. Normally, less than 5% binds to plasma proteins. With excessive consumption of food with vitamin A and an overflow of the liver depot, the connection with lipoproteins can be up to 65%. Also, hyperlipoproteinemia may influence the increase in the amount of vitamin A associated with lipoproteins. Vitamin A, being released from the liver depot, forms a complex with retinol-binding protein, in the form of which it is found in the blood. Small amounts cross the placenta and into breast milk. In the equivalent of a two-year need for an adult, it is deposited in the liver, in a small amount - in the kidneys and lungs. Mobilization from a depot requires zinc-containing substances.
Vitamin A is metabolized in the liver. It is excreted by the kidneys, and the non-absorbed part through the rectum.
Indications for use
The use of Retinol acetate is indicated for vitamin A deficiency, hypovitaminosis and in the composition complex therapy:
- eye pathologies: hemeralopia, retinitis pigmentosa, xerophthalmia, eczematous lesions of the eyelids, keratomalacia with concomitant vitamin A deficiency;
- diseases and skin lesions: ulcers, ichthyosis, psoriasis, hyperkeratosis, tylotic (corn-like, horny) eczema, subacute and acute stages of eczema, neurodermatitis, burns, frostbite, erosion, cracks, wounds.
In addition, oily solution for oral and external use and Retinol acetate capsules are used as part of complex therapy:
- seborrheic dermatitis, skin tuberculosis;
- gastrointestinal diseases: stomach ulcer and duodenum, erosive gastroduodenitis;
- colds and infectious and inflammatory (including chronic forms) diseases (including measles, dysentery, tracheitis, flu, bronchitis).
Also, Retinol acetate capsules are taken in the treatment of liver cirrhosis, and drops are prescribed as part of the complex therapy of atopic dermatitis.
Contraindications
- acute inflammatory skin diseases;
- cholelithiasis;
- hypervitaminosis A;
- chronic pancreatitis;
- period of pregnancy;
- age up to 7 years;
- individual intolerance to the components of the drug.
With caution, only after consulting the attending physician, Retinol acetate can be used for liver cirrhosis, alcoholism, viral hepatitis, renal failure, in old age.
In addition, care should be taken when prescribing the solution and capsules to patients with heart failure of II and III degrees, with nephritis.
Instructions for the use of Retinol acetate: method and dosage
The use of Retinol acetate is carried out only under the supervision of the attending physician.
Drops for oral and external use 3.44% and 8.6%
Drops are taken orally after meals, after 10-15 minutes.
- mild to moderate vitamin deficiency: adults - 11.35 mg (33,000 IU) each, which corresponds to 0.33 ml drops with a concentration of 3.44% (13 drops from an eye pipette or 10 drops from a dropper cap) or 0.13 ml 8.6% of the drug (5 drops from an eye dropper or 4 drops from a dropper cap) per day;
- eye diseases: adults - 17.2-34.4 mg (50,000-100,000 ME), which corresponds to 0.5-1 ml drops with a concentration of 3.44% (20-40 drops from an eye pipette or 14-28 - from a dropper cap) or 0.2-0.4 ml with a concentration of 8.6% (8-16 drops from an eye pipette or 6-8 - from a dropper cap) per day; children (taking into account age) - 0.34-1.72 mg each (1000-5000 ME), which corresponds to 0.01-0.05 ml of 3.44% drug (1-2 drops from an eye pipette or 1 drop from dropper caps) or 0.004-0.02 ml of the drug with a concentration of 8.6% (1 drop from an eye pipette or from a dropper cap) per day;
- skin pathologies: adults - 17.2-34.4 mg (50,000-100,000 ME), which corresponds to 0.5-1 ml of 3.44% of the drug (20-40 drops from an eye pipette or 14-28 - from dropper caps) or 0.2-0.4 ml drops of 8.6% (8-16 drops from an eye pipette or 6-8 - from a dropper cap) per day; children - 1.72-6.88 mg each (5000-20,000 ME), which corresponds to 0.05-0.2 ml drops of 3.44% (2-8 drops from an eye pipette or 2-6 drops - from the lid -drops) or 0.02-0.08 ml of the drug with a concentration of 8.6% (1-4 drops from an eye pipette or 1-2 drops from a dropper cap) per day.
The doctor determines the duration of treatment individually.
When treating ulcers, burns and frostbite, it is simultaneously recommended to treat skin lesions with an oil solution of Retinol acetate. For this, the preparation is applied to the previously cleaned surface of the lesion 5-6 times a day and covered with gauze. Frequency rate of lubrication frequency as epithelialization and scarring is reduced to 1 time per day.
Solution for oral and external use, oil 3.44% and 8.6%
Retinol acetate solution is taken orally, 10-15 minutes after meals (early in the morning or late in the evening).
- mild and moderate severity of vitamin deficiency: adults - up to 33,000 ME, children over 7 years old - 5,000 ME per day;
- eye diseases: adults - 50,000-100,000 IU per day with simultaneous intake of 20 mg of riboflavin;
- skin pathologies: adults - 50,000-100,000 ME, children - 5,000 to 20,000 ME per day. In the treatment of burns, frostbite and ulcers, in addition to oral administration, local applications with the drug are prescribed, which are applied to the cleansed affected areas 5-6 times a day during the acute period of the condition, then, as the healing progresses, the frequency of procedures is reduced.
A single dose should not exceed 50,000 ME for adults, 5,000 ME for children, and a daily dose of 100,000 ME and 20,000 ME, respectively.
Capsules
Retinol acetate capsules are taken orally after meals late in the evening or early in the morning.
- avitaminosis of mild and moderate severity: 1 pc. (33,000 IU) per day;
- eye pathologies: adults - 3 pcs. (100,000 IU) per day in combination with 20 mg of riboflavin;
- skin diseases: adults - 3 pcs. (100,000 ME) per day.
The maximum daily intake for adults is 100,000 IU.
Side effects
With Retinol acetate therapy, it is possible to develop hypervitaminosis A, allergic reactions, with prolonged use, the risk of intoxication increases.
Symptoms of hypervitaminosis A:
- adults: drowsiness, headache, lethargy, nausea, vomiting, facial flushing, gait disturbance, pain in the bones of the lower extremities;
- children: skin rashes, fever, vomiting, drowsiness, sweating.
Overdose
In case of acute overdose in adults, the following symptoms of hypervitaminosis A develop after 6 hours: lethargy, drowsiness, dizziness, double vision, nausea, vomiting, severe headache, irritability, diarrhea, bleeding gums, dryness and ulceration of the oral mucosa, peeling lips, skin (especially palms), increased intracranial pressure, confusion.
Symptoms of chronic intoxication: bone pain, loss of appetite, dryness of the oral mucosa, cracks and dry skin, vomiting, gastralgia, fatigue, hyperthermia, asthenia, strong pain in the abdomen, headaches, pollakiuria, nocturia, polyuria, photosensitivity, irritability, the appearance of yellow-orange spots on the palms, soles, in the areas of the nasolabial triangle, hair loss, convulsions, hepatotoxic phenomena, oligomenorrhea, portal hypertension, intraocular hypertension, hemolytic anemia, hemolytic anemia the appearance of changes on radiographs of bones.
Acute hypervitaminosis in children is characterized by excitement, anxiety, insomnia during the first day, drowsiness, signs of suffocation, vomiting, fever up to 39 ºC, protrusion of the large fontanel.
Treatment: drug withdrawal and symptomatic therapy.
special instructions
Retinol acetate should not be used in combination with other multivitamin preparations containing vitamin A in order to prevent hypervitaminosis.
For adults, the daily requirement of retinol is 0.9 mg, for children - 0.4-1 mg.
For lactating women and children living in the Far North, it is recommended to increase the dose by 50%.
Application during pregnancy and lactation
According to the instructions, Retinol acetate is contraindicated for treatment during pregnancy.
Childhood use
Retinol acetate is contraindicated for the treatment of patients under the age of 7 years. When treating children over 7 years old, the drug should be used with caution.
With impaired renal function
In renal failure, the drug should be used with caution.
For violations of liver function
With cirrhosis of the liver, Retinol acetate should be used with caution.
Use in the elderly
When treating elderly patients, the drug should be used with caution.
Drug interactions
With the simultaneous use of Retinol acetate:
- oral contraceptives - increase the concentration of vitamin A in blood plasma;
- glucocorticosteroids, salicylates - reduce the risk of unwanted effects;
- colestipol, cholestyramine, neomycin, mineral oils - reduce the absorption of the drug (it may be necessary to increase the dose of retinol acetate);
- isotretinoin - increases the risk of developing a toxic effect;
- calcium preparations - reduce their therapeutic effect, causing the risk of developing hypercalcemia;
- vitamin E - causes a decrease in the deposition in the liver and the use of vitamin A, the toxicity of the drug and its absorption, taking high doses of vitamin E can reduce the reserves of vitamin A in the body.
Analogs
Retinol Acetate analogues are: Retinol Palmitate, Retinol Acetate solution in oil, Retinol, Vitamin A.
Terms and conditions of storage
Keep out of the reach of children.
Store at a temperature: drops and solution - up to 10 ° C, capsules - up to 25 ° C, in a dark place, protect capsules from moisture.
Shelf life: drops - 3 years; solution and capsules - 2 years.
- In what cases vitamin A is usually taken and what important nuances can not be found in the instructions for its use;
- What forms of release of vitamin A preparations are on sale today and which one should you prefer in your case;
- How to take drugs correctly (including capsules when used for cosmetic purposes);
- Vitamin A drug names;
- And also what can lead to ignoring contraindications for taking appropriate funds and how you can get poisoned with vitamin A unknowingly.
If you are going to use vitamin A for certain purposes, then first of all you need to understand that this substance, despite its huge benefit for the body (at normal dosages), if the instructions for use are not followed, it can cause significant harm to health. Therefore, before taking the appropriate drug inside, injecting it intramuscularly or even simply adding it to the face mask, it is first useful to take into account a number of important nuances - and not only contraindications, but also some other points, which we will consider further.
But first, let's remember, so to speak, the basic properties of vitamin A (retinol) and its effect on the human body. The most important functions of retinol are:
- maintenance of the visual system (visual pigment rhodopsin is synthesized in the body only in the presence of vitamin A);
- anti-cancer effect (a healthy person does not feel this effect - free radicals, including those constantly formed in the skin under the influence of ultraviolet radiation and oxygen, simply bind and no longer show themselves in any way. However, there would be no such protection - and problems would not force wait for yourself);
- stimulating the immune system;
- stimulation of tissue regeneration processes;
- as well as ensuring the synthesis of a number of hormones.
Accordingly, vitamin A is used in the composition medicines and therapeutic complexes for:
- eye diseases - keratitis, conjunctivitis, twilight blindness, near and far vision disorders, xerophthalmia;
- skin diseases - eczema, allergic dermatoses, dry skin, ichthyosis, keratoderma, urticaria, furunculosis, seizures;
- baldness, hair growth disorders and early graying;
- diseases of the nails;
- inflammatory processes different localization;
- thrush, edema and some diseases of the mucous membranes;
- pneumonia;
- immunodeficiencies and seasonal weakening of the immune system;
- peptic ulcer diseases of the digestive tract (gastritis, duodenitis, pancreatitis, hepatitis);
- liver inflammation of various etiologies;
- various infectious diseases;
- treatment of skin lesions - ulcers, frostbite, burns, open wounds;
- anemia.
In addition, vitamin A is widely used in cosmetology to improve the condition of the skin and hair, to slow down the processes of general aging of the body and normalize metabolism.
Meanwhile, retinol preparations also have serious contraindications, therefore, vitamin A should be taken in each specific case in strict accordance with the instructions for use and the doctor's instructions.
On a note
Vitamin A is a fat-soluble substance, and therefore is usually sold in the form of oil solutions. The only exceptions are multivitamin complexes in the form of pills and powders. The instructions for them are quite simple, but this does not negate the seriousness of the approach when choosing any of them.
Forms of production of preparations with vitamin A
Vitamin A for therapeutic and prophylactic use is available in the form of:
- oil solutions for intramuscular injection;
- oil solutions for ingestion or external use;
- capsules, which are sometimes also called film-coated tablets (inside of them, again, there is an oil solution of retinol acetate or palmitate);
- and, as noted above, as a component of multivitamin complexes in the most different forms- pills, powders, syrups, capsules.
It should be borne in mind that in most cases the therapeutic effect will be much more pronounced if an oily solution of retinol is taken internally (or injected intramuscularly), rather than when applied externally. The fact is that the external use of vitamin A allows the beneficial substance to affect only the outer layers of the skin, and at the same time retinol is absorbed in extremely low quantities. Often, when applied topically, a visible improvement in the condition skin it is observed not even due to vitamin A, but due to softening of the skin with oil in which retinol is dissolved.
Capsules with an oil solution are used internally, and usually the useful substance is absorbed well from them. In the case of injections, the bioavailability of retinol is even higher.
In accordance with the instructions, vitamin A capsules should be taken during or after meals - the gelatinous shell of the capsule dissolves rather quickly in gastric juice.
As part of multivitamin preparations, the use of vitamin A is justified only for correcting the vitamin balance in general and as a general support for the body - for example, for the prevention of seasonal weakening of immunity and hypovitaminosis. For the treatment of diseases, retinol in this form is practically not used.
On a note
In multivitamin complexes, not vitamin A itself is often used, but the so-called provitamin A - beta-carotene (sometimes they write "beta-carotene"). Beta-carotene, even in the case of significant overdoses, does not have such a strong toxic effect on the body as in the case of retinol acetate or retinol palmitate.
Rules for the use of vitamin A capsules
Vitamin A capsules are usually taken to treat diseases of the digestive tract, visual system, as well as to correct the development of the skeleton in children. Such treatment is always extended in time and therefore the shock doses characteristic of retinol injections are not needed here.
The number of vitamin A capsules that should be taken per day depends significantly on the clinical case and the concentration of retinol in the oil solution enclosed in the capsules. So, for example, in different preparations of vitamin A, capsules contain from 3300 IU to 100,000 IU at daily rate about 5000 IU for an adult, 8000 IU for pregnant and lactating women and 650 IU for children under the age of 1 year.
Doctors sometimes recommend drinking capsules with a high content of vitamin A in the treatment of serious delays in the development of the skeleton and in case of skin diseases.
Today, it has become very popular to apply vitamin A in capsules externally - to care for the skin of the face, scalp, to improve the condition of hair and nails. Manufacturers of drugs do not give instructions for such use of vitamin A, but craftsmen usually act like this: pierce capsules, add contents to shampoos and masks, and then apply to the appropriate area of the body.
On a note
Some vitamin A capsules contain cod oil, a rich natural source of retinol. And although the advantage of such drugs is their naturalness, nevertheless, in the event of an overdose, vitamin A poisoning will be no less pronounced than in the case of taking synthetic analogs.
The most well-known vitamin A capsules are as follows:
The instructions for using each vitamin A supplement may vary slightly.
On a note
Vitamins Aevit are also very popular today for skin and hair care - this drug is also produced in capsules, but in addition to retinol it also contains vitamin E, which is a powerful antioxidant.
Vitamin A solution in ampoules
Vitamin A in ampoules, as in the case of capsules, can be used in different ways:
- first of all, the instruction for such drugs implies their use in the form of injections (for the rapid administration of large doses as a therapeutic measure);
- you can also take the contents of the ampoules inside - for the prevention of hypovitaminosis and the treatment of diseases requiring the use of retinol (however, in such cases, the use of capsules is more convenient);
- and, finally, the contents of the ampoules can be applied externally - for the treatment of skin, wounds, hair.
Ampoules, as well as capsules, also contain an oily solution of vitamin A, and therefore the areas of its application do not differ significantly from those for encapsulated preparations. Retinol in ampoules is prescribed for:
- serious hypovitaminosis and vitamin A deficiency. In these cases, 33,000 IU are prescribed for adults and up to 5,000 IU for children;
- skin diseases - here adults are prescribed up to 100,000 IU per day, children - up to 5,000 IU;
- Crohn's disease;
- malabsorption (loss of nutrients entering the digestive tract);
- diarrhea;
- weakening of immunity;
- stress;
- multiple pregnancy.
In the case of external use, the contents of the ampoule are usually treated with the skin of the face or the solution is applied to the hair (as part of shampoos and masks). Some recipes involve the inclusion of the drug in face masks, homemade creams and lotions.
How to inject vitamin A intramuscularly?
Intramuscular injections of vitamin A are prescribed for serious eye diseases, dermatoses, disorders of the cardiovascular system.
In the case when injections are made on their own, it is important to adhere to the instructions as accurately as possible: before the procedure, the solution in the ampoule must be heated to body temperature, then break off the tip of the ampoule (sometimes this requires a special ampoule knife), draw the solution into the syringe and squeeze the bubbles out of the syringe air. After that, the tip of the needle is inserted into the femoral or gluteus muscle previously wiped with an alcohol napkin, and the solution is slowly squeezed out of the syringe.
Intravenous administration of vitamin A is unacceptable, since the penetration of the oil base into the bloodstream can lead to very unfavorable consequences!
The most popular vitamin A ampoules are:
- domestic "Retinol acetate" (produced by several pharmaceutical companies);
- serum "BeautyMed";
- Retinol Klapp.
It should be understood that if you, for example, just have dry skin or brittle hair, then you should absolutely not prescribe vitamin A injections yourself. Not only may the problem not be caused by a lack of retinol at all, but there is also a great risk of being mistaken with the dosage.
On a note
An example of vitamin A overdose is the severe poisoning by polar bear liver, sometimes observed in people in the Arctic. One gram of such a liver contains as much retinol as a person consumes in almost a month. Even 50 grams of polar bear liver causes very severe poisoning, and in some cases can lead to human death.
Vitamin A oil solution
Vitamin A oil solutions are available with different retinol content: there are preparations containing 100,000 IU (3.44%) and 200,000 IU (6.88%) retinol in 1 ml. Typically, these drugs are used by mouth.
Vitamin A oil solutions should be taken as directed by your doctor for each specific case. Such solutions are used not only for medicinal purposes, but also for prophylactic purposes.
Retinol multivitamins
Most multivitamin preparations contain vitamin A in one form or another (either retinol itself, or its precursor, beta-carotene, which was already mentioned above).
Examples of multivitamin preparations:
- various complexes Alphabet, Duovit, Complivit, Vitrum, Multi-Tabs, Merz, Centrum - designed for comprehensive support of the patient's body at any age;
- Separately, we can highlight the preparations Alphabet Cosmetics, Complivit Radiance, Vitrum Beauty and a whole line of Lady's Formula products - designed to support the skin, hair and overall beauty of women;
- You can also note the two-vitamin complexes - the drugs Aevit and Vitae, focused primarily on supporting the immune system.
When taking any multivitamin complex, you should remember that if you want to make up for the lack of vitamin A, you can easily get an excess of another component of the drug. Despite the seeming harmlessness of these "vitamins" they have their own contraindications, so do not forget to look at the instructions.
Contraindications and dangers of vitamin A intake
The main danger of consuming large doses of vitamin A is intoxication of the body, that is, in fact, poisoning. When consumed daily over 4000 IU for six months, chronic poisoning can develop, and with a single use of more than 250 000 - 500 000 IU, severe acute intoxication with paralysis, vomiting and convulsions can occur.
Chronic intoxication is characterized by headaches, nausea, vomiting, indigestion, joint pain.
Contraindications to the use of vitamin A are active allergic reactions and hypothyroidism. Also, you can not take retinol preparations together with retinoids, since the combination of these substances increases the toxic effect.
It is interesting
In addition to the liver of polar bears, the liver of sharks, walruses and some other animals also contains huge amounts of vitamin A. It is with the accidental consumption of these foods that rare cases of fatal retinol poisoning in humans are associated.
Consuming large doses of vitamin A during pregnancy can lead to fetal developmental disorders and birth defects in the baby's skeleton. Therefore, before starting the use of retinol preparations, pregnant women always need to consult a doctor.
Be healthy!
An interesting video about the importance of vitamin A for vision and skin, as well as how it can be dangerous ...
And some more interesting information about vitamin A