Retinol acetate

Retinol acetate is an analogue of natural retinol (belongs to the subgroup of fat-soluble vitamins). The medicine helps restore the normal level of vitamin A in the body.

Retinol is extremely important for protein, mucopolysaccharide and lipid binding, and in addition, it stabilizes the mineral balance. The most specific function of retinol is to ensure visual activity (photoreception). In addition, the vitamin is a participant in the processes of binding rhodopsin - this is the visual purple located inside the retinal rods. [ 1 ]

Indications Retinol acetate

It is used to treat hypovitaminosis or avitaminosis of subtype A, as well as eye pathologies (including conjunctivitis, keratitis, which has a superficial form, xerophthalmia or lesions in the cornea, as well as pigment form of retinitis, pyoderma with hemeralopia, as well as eczema in the eyelid area).

It is also used in the combined treatment of such disorders:

• hypotrophy;
• rickets;
• collagenoses;
• developing in connection with diathesis of the exudative type of acute respiratory viral infection;
• bronchopulmonary pathologies in chronic or active form;
• epidermal lesions (including cutaneous tuberculosis, psoriasis, frostbite wounds, ichthyosis, burns, senile keratosis, follicular dyskeratosis and certain types of eczema);
• intestinal lesions of an ulcerative-erosive or inflammatory nature;
• liver cirrhosis.

Release form

The drug is released in the form of an oil solution for oral administration - in bottles (may have special stoppers in the form of a dropper), with a volume of 10 ml. Inside the box - 1 such bottle.

Pharmacodynamics

Retinol modulates the processes of differentiation of epithelial cells, is involved in keratinization, development of excretory glands, as well as healing of the epidermis and mucous membranes.

Retinol is required for the healthy functioning of the endocrine glands, as well as the growth of the body - this is due to the fact that this vitamin acts as a synergist of somatomedins. [ 2 ]

In addition, the vitamin promotes the division of immunocompetent cells and the binding of protective factors of a specific (immunoglobulin) and non-specific (lysozyme with interferon) type (in infectious and other forms of diseases); it also stimulates the processes of myelopoiesis. [ 3 ]

Retinol increases the intrahepatic glycogen index, stimulates the production of lipase with trypsin inside the digestive system. The substance slows down the oxidation of cysteine together with the photochemical response of free radicals. The drug activates the processes of sulfate penetration into cartilage, connective tissue elements and bones.

The vitamin also satisfies the body's need to obtain myelin with sulfocerebrosides, facilitating the transmission and conduction of neural impulses.

Pharmacokinetics

After oral administration, Retinol acetate is well absorbed in the upper part of the small intestine. Then, together with chylomicrons, it moves from the intestinal walls into the lymph and through the thoracic duct penetrates into the bloodstream. The movement of retinol esters in the blood is carried out with the help of β-lipoproteins. The values of serum Cmax are noted after 3 hours from the moment of use.

Retinol is deposited inside the liver parenchyma, where it accumulates in a stable ether form. At the same time, a high retinol index is observed inside the retinal pigment epithelium. Such a depot is required for the constant supply of retinol to the outer segments of the cones with rods.

Retinol is converted inside the liver and then excreted through the kidneys as metabolic components that have no therapeutic activity.

Part of the drug may be excreted with bile and also become a participant in intrahepatic circulation processes. Elimination of the vitamin is realized at a low rate - 34% of the administered portion of the drug is excreted from the body over a 3-week period.

Dosing and administration

The medication is taken orally, 10-15 minutes after eating. It is also used externally.

1 ml of LS contains 100,000 IU (in 25 drops) of retinol. 1 drop obtained through a dropper contains approximately 4,000 IU of retinol.

When selecting doses of medicine, the following proportions are taken into account:

• an adult can be administered a maximum of 50 thousand IU at a time (12 drops of the substance contain 48 thousand IU);
• for a child over 7 years old – no more than 5 thousand IU (1 drop of medicine contains 4 thousand IU);
• An adult can take a maximum of 100 thousand IU of Retinol Acetate (25 drops) per day;
• A child over 7 years of age is given no more than 20 thousand IU (5 drops) per day.

In case of mild or moderate avitaminosis, the size of the therapeutic dose of the drug is equal to a maximum of 33 thousand IU per day (8 drops (equivalent to 32 thousand IU)).

For epidermal diseases, xerophthalmia, pigment retinitis and hemeralopia, the daily dosage of retinol is 50-100 thousand IU (12-25 drops of the medication (equivalent to 48-100 thousand IU)).

For a child over 7 years old, 3-6 thousand IU (in 1 drop - 4 thousand IU) are used per day, taking into account the course and nature of the pathology.

In case of epidermal lesions (burns, ulcers or frostbite), such areas after hygienic cleaning are treated with a medicinal liquid and covered with a gauze bandage (5-6 times a day, with a reduction in the number of applications to 1 time, taking into account epithelialization).

• Application for children

Retinol acetate can be used by people over 7 years of age.

Use Retinol acetate during pregnancy

Due to the high content of retinol in the indicated form of the drug, it cannot be used during breastfeeding or pregnancy.

Contraindications

Among the contraindications:

• severe sensitivity associated with elements of the drug;
• nephritis, active or chronic;
• decompensated type of heart failure;
• hyperlipidemia;
• cholelithiasis;
• chronic pancreatitis;
• hypervitaminosis A;
• retinoid poisoning;
• obesity;
• alcoholism of a chronic nature;
• sarcoidosis (also present in the anamnesis).

Side effects Retinol acetate

With prolonged administration of retinol in large doses, hypervitaminosis type A develops. Among other side effects:

• disorders associated with the functioning of the nervous system and sensory organs: drowsiness, headaches, discomfort, fatigue, cramps and lethargy, as well as irritability, loss of sleep, visual disturbances and increased intraocular pressure;
• problems affecting the digestive system: weight loss, loss of appetite and nausea. Vomiting may occur sporadically. Exacerbation of liver pathologies may be observed, as well as an increase in the values of alkaline phosphatase and transaminase activity;
• urinary disorders: nocturia, pollakiuria and polyuria;
• damage to hematopoietic activity: hemolytic type of anemia;
• signs associated with the functioning of the musculoskeletal system: gait disturbance, bone changes on X-ray images, pain in the bones of the legs;
• allergy symptoms: swelling under the skin, cracks affecting the skin on the lips, as well as the appearance of yellow-orange spots on the palms, soles and in the nasolabial triangle. Sometimes during the 1st day of taking the drug, itchy rashes of the maculopapular type develop, in which case the drug should be discontinued. Erythema, xerostomia, itching with rashes, dry epidermis, increased temperature and facial hyperemia accompanied by peeling may be observed;
• Others: menstrual cycle disorder, photophobia, alopecia, aphthae, hypercalcemia and abdominal pain.

Reducing the dosage or temporarily discontinuing the drug can eliminate the above-mentioned disorders.

In case of epidermal lesions, the use of large doses of the drug after 7-10 days of therapy may lead to an exacerbation of local inflammation (it does not require additional treatment, it soon subsides on its own). Such a reaction is caused by the immuno- and myelostimulating effect of the drug.

Overdose

Signs of intoxication: confusion, dizziness, irritability, dehydration, diarrhea and generalized rashes with further development of peeling (in a large layer), starting on the face. In addition, xerostomia, ulceration of the oral mucosa, bleeding in the gums, peeling of the lips and severe pain when palpating the tubular bones (due to hemorrhages in the subperiosteal region) are observed.

In the case of chronic or active hypervitaminosis type A, drowsiness, pain in the muscle and joint area, vomiting, severe headaches and visual disturbances (diplopia) appear. The temperature also increases, pigment spots appear, epidermal dryness or jaundice develops, the size of the spleen and liver increases, there is a loss of appetite and strength, and a change in the blood picture. With severe intensity of the disorder, hydrocephalus and heart weakness occur, and seizures also appear.

Symptomatic actions are performed.

Interactions with other drugs

Estrogens increase the likelihood of developing hypervitaminosis A.

The drug weakens the anti-inflammatory activity of GCS.

The drug is prohibited to be combined with cholestyramine, as well as nitrites, since they interfere with its absorption processes.

Retinol acetate should not be used in combination with other retinol derivatives, as this may lead to intoxication or the development of hypervitaminosis subtype A.

Administration together with tocopherol helps to maintain the activity of the drug, and also promotes intestinal absorption and the development of anabolic symptoms.

Use with vaseline oil may interfere with intestinal absorption of the drug.

The use of retinol with anticoagulants increases the tendency to develop bleeding.

Storage conditions

Retinol acetate should be stored in a place closed to small children. Temperature values are within the range of 2-8ºС.

Shelf life

Retinol acetate is allowed to be used within a 2-year period from the date of manufacture of the medicinal product.

Analogues

Analogues of the drug are the substances Videstim and Retinol palmitate.