Instructions for Retinol acetate oily solution cutaneous/oral 34.4 mg/ml bottle 10 ml
Composition
active ingredient: retinol (vitamin A);
1 ml of solution contains retinol (in the form of retinol acetate) – 34.4 mg (100,000 IU of vitamin A) – 18-20 drops;
1 drop contains about 5000 IU of vitamin A;
excipient: soybean oil.
Dosage form
Transdermal and oral solution, oily.
Main physicochemical properties: transparent oily liquid from light yellow to dark yellow, without rancid taste; the presence of a specific odor is allowed.
Pharmacotherapeutic group
Simple preparations of vitamin A. Retinol (vitamin A). ATX code A11C A01.
Pharmacological properties
Pharmacodynamics.
Vitamin A (retinol) belongs to the group of fat-soluble vitamins.
The drug Retinol acetate is an analogue of natural vitamin A and is necessary to restore the normal concentration of retinol in the body. Vitamin A plays an important role in the synthesis of proteins, lipids, mucopolysaccharides, and regulates the balance of minerals.
The most specific function of vitamin A is to ensure the processes of vision (photoreception). Retinol is involved in the synthesis of visual purple – rhodopsin, located in the rods of the retina.
Vitamin A modulates the processes of differentiation of epithelial cells, participates in the development of secretory glands, keratinization processes, and regeneration of mucous membranes and skin.
Vitamin A is necessary for the normal functioning of the endocrine glands and body growth, because it is a synergist of somatomedins.
Vitamin A affects the division of immunocompetent cells, the synthesis of factors of specific (immunoglobulin) and nonspecific (interferon, lysozyme) protection of the body against infectious and other diseases, and stimulates myelopoiesis.
Retinol increases the level of glycogen in the liver, stimulates the production of trypsin and lipase in the digestive system; inhibits photochemical free radical reactions and cysteine oxidation; activates the incorporation of sulfates into the components of connective tissue, cartilage, and bones; satisfies the need for sulfocerebrosides and myelin, ensuring the conduction and transmission of nerve impulses.
With a lack of vitamin A, twilight vision disorders (night blindness) and atrophy of the epithelium of the conjunctiva, cornea, and lacrimal glands develop. Degenerative-dystrophic processes are observed in the respiratory tract (mucous membranes of the nasopharynx, paranasal sinuses, trachea, and bronchi), in the genitourinary system (epithelium of the renal pelvis, ureters, bladder, urethra, vagina, ovaries, fallopian tubes, and endometrium, seminal vesicles and cords, and prostate gland), in the digestive system (mucous membrane of the digestive tract, salivary glands, and pancreas). Vitamin A deficiency leads to impaired skin trophism (hyperkeratosis), impaired growth and quality of hair and nails, and impaired function of the sebaceous and sweat glands. In addition, there is a decrease in body weight and a slowdown in bone growth, a decrease in the synthesis of glucocorticoids and steroid hormones, a violation of the body's resistance to infectious and other diseases. There is a tendency to cholelithiasis and nephrolithiasis.
A lack or excess of vitamin A in a woman's body can cause abnormalities in the intrauterine development of the fetus.
Retinol has an antitumor effect that does not extend to non-epithelial tumors.
Pharmacokinetics.
Retinol is biotransformed in the liver, and then excreted by the kidneys as inactive metabolites. Retinol can be partially excreted in the bile and participate in enterohepatic circulation. Retinol is eliminated slowly - 34% of the dose is excreted from the body in 3 weeks.
Retinol acetate taken orally is well absorbed in the upper parts of the small intestine. Then, as part of chylomicrons, it is transported from the intestinal wall into the lymphatic system and enters the bloodstream through the thoracic duct. Retinol esters are transported in the blood by β-lipoproteins. The maximum level of vitamin A esters in the blood serum is observed 3 hours after administration. 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 determined in the retinal pigment epithelium. This depot is necessary for the regular supply of the outer segments of rods and cones with vitamin A.
Indication
A-vitaminosis and A-hypovitaminosis, eye diseases (retinitis pigmentosa, xerophthalmia, hemeralopia, superficial keratitis, corneal lesions, conjunctivitis, pyoderma and eczematous lesions of the eyelids), in complex therapy:
- rickets;
- acute respiratory diseases that occur against the background of exudative diathesis;
- acute and chronic bronchopulmonary diseases;
- hypotrophy;
- collagenoses;
- with pathological skin processes (frostbite, burns, wounds, ichthyosis, follicular dyskeratosis, senile keratosis, skin tuberculosis, some forms of eczema, psoriasis);
- for inflammatory and ulcerative-erosive lesions of the intestine;
- liver cirrhosis.
Contraindication
Hypersensitivity to the components of the drug, acute and chronic nephritis, heart failure in the decompensation stage, cholelithiasis, chronic pancreatitis, hypervitaminosis A, retinoid overdose, hyperlipidemia, obesity, chronic alcoholism.
Interaction with other medicinal products and other types of interactions
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 and cholestyramine, because they impair the absorption of the drug.
Retinol acetate should not be used together with other vitamin A derivatives due to the risk of overdose and development of hypervitaminosis A.
The combination with vitamin E helps preserve retinol acetate in its active form, absorb it from the intestines, and produce anabolic effects.
Simultaneous use of vaseline oil may disrupt the absorption of the vitamin in the intestines.
Concomitant use of vitamin A and anticoagulants increases the tendency to bleed.
Application features
The drug should be taken under the supervision of a doctor. With prolonged use of Retinol acetate, it is necessary to monitor biochemical parameters and blood clotting time.
When treating night vision impairment (night blindness), Retinol acetate should be used with riboflavin and nicotinic acid.
Use with caution in severe damage to the hepatobiliary system, diseases accompanied by blood clotting disorders.
It is not recommended to use the drug during long-term therapy with tetracyclines.
Retinol should be taken 1 hour before or 4-6 hours after taking cholestyramine.
The drug has the property of accumulating and remaining in the body for a long time. Women who have taken high doses of retinol can plan 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 high levels of vitamin A in the body.
For normal absorption of vitamin A, the presence of fats in food is a necessary condition.
Alcohol and tobacco abuse disrupts the absorption of the drug from the digestive tract.
This medicine contains soybean oil. If you are allergic to peanuts or soybeans, you should not use this medicine.
Use during pregnancy or breastfeeding
Given the high dose of vitamin A in this dosage form, the drug is contraindicated for oral administration during pregnancy or breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
There is no data on the effect of the drug on the ability to drive a car or operate complex mechanisms.
Method of administration and doses
Retinol acetate should be administered orally 10-15 minutes after meals and externally. 1 drop contains approximately 5000 IU of vitamin A.
1 ml of the drug contains 100,000 IU (18-20 drops) of vitamin A.
When determining the doses of the drug, proceed from the fact that the highest single dose of vitamin A for adults is 50,000 IU. The highest daily dose of vitamin A for adults is 100,000 IU. Therapeutic doses of vitamin A for mild and moderate avitaminosis are up to 33,000 IU per day for adults. For this purpose, it is better to use the drug in dosage forms of dragees or capsules (1 dragee of 10 mg or 1 capsule per day). For skin diseases, as well as for retinitis pigmentosa, xerophthalmia, hemeralopia, the daily dose of vitamin A is 50,000-100,000 IU (simultaneously prescribe riboflavin (vitamin B2) in a daily dose of 0.02 g). In case of skin surface lesions (ulcers, burns, frostbite), after hygienic cleaning, lubricate the affected areas with the solution and cover with a gauze bandage (5-6 times a day, reducing the number of applications to one as epithelialization occurs). At the same time, prescribe the drugs internally. To prevent the formation of stones, prophylactic doses should be established based on the daily requirement of the human body for vitamin A. The duration of treatment is from 10 days to 1 month.
Children
Do not administer the drug internally to children in this dose.
Overdose
Symptoms: dizziness; confusion, diarrhea, severe dehydration, irritability; generalized rash with subsequent large-scale peeling, which begins with the face; bleeding gums, dryness and ulceration of the oral mucosa, peeling lips, sharply painful palpation of long tubular bones due to subperiosteal hemorrhages.
Acute and chronic hypervitaminosis A is accompanied by severe headache, fever, drowsiness, vomiting, visual impairment (double vision), dry skin, pain in joints and muscles, the appearance of age spots, an increase in the size of the liver and spleen, jaundice, changes in the blood picture, loss of strength and appetite. In severe cases, convulsions, heart failure and hydrocephalus develop.
Treatment: symptomatic, prescribe thyroxine as an antagonist, rational use of ascorbic acid, vitamin E.
Adverse reactions
Prolonged intake of large doses of vitamin A can cause the development of hypervitaminosis A.
From the nervous system and sensory organs: increased fatigue, drowsiness, lethargy, irritability, headache, sleep loss, convulsions, discomfort, intraocular hypertension, visual impairment.
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 disturbance, tenderness of the bones of the lower extremities.
Allergic reactions: cracks in the skin of the lips, yellow-orange spots on the soles of the feet, palms, and in the nasolabial triangle; subcutaneous edema; in some cases, itchy maculopapular rashes may occur on the first day of use, requiring discontinuation of the drug; itching; erythema and rash; dry skin; dry mouth; fever; facial flushing with subsequent peeling.
Others: hair loss, menstrual irregularities, abdominal pain, aphthae, photosensitivity, hypercalcemia.
With a decrease in the dose or with temporary discontinuation of the drug, side effects disappear on their own.
In 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 decreases. This effect is associated with the myelo- and immunostimulating effect of the drug.
Expiration date
2 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 ºС.
Keep out of reach of children.
Packaging
10 ml in vials enclosed in a pack.
Vacation category
Without a prescription.
Producer
PJSC "VITAMINS".
Location of the manufacturer and its business address
20300, Ukraine, Cherkasy region, Uman city, Leninskoi Iskra St., 31.
Applicant
PJSC "VITAMINS".
Location of the applicant and/or applicant's representative
20300, Ukraine, Cherkasy region, Uman city, Leninskoi Iskra St., 31.
