Retinol acetate

Retinol acetate is an analogue of natural retinol (included in the subgroup of fat-soluble vitamins). The medicine helps to restore the normal level of A-vitamin inside 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 provide visual activity (photoreception). In addition, the vitamin is a participant in the binding processes of rhodopsin - it is visual purple located inside the retinal rods. [1]

Indications Retinol acetate

It is used for the treatment of hypovitaminosis or avitaminosis of subtype A, as well as eye pathologies (among those, conjunctivitis is , keratitis , which has a superficial form, xerophthalmia or lesions in the corneal region, and in addition, the pigmented form of retinitis, pyoderma with hemeralopia, as well as eczema in the eyelids).

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

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

Release form

The release of drugs is realized in the form of an oily solution for oral administration - in vials (they may have special stoppers in the form of a dropper) with a volume of 10 ml. There is 1 such bottle inside the box.

Pharmacodynamics

Retinol modulates the processes of differentiation of epithelial cells, is a participant 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), as well as nonspecific (lysozyme with interferon) type (for infectious and other diseases); it also stimulates the processes of myelopoiesis. [3]

Retinol increases the intrahepatic glycogen index, stimulates the production of lipase with trypsin within the digestive system. The substance slows down the oxidation of cysteine along with the photochemical response of free radicals. The medicine activates the processes of the passage of sulfates into the cartilage, elements of connective tissues and bones.

Also, the vitamin satisfies the body's need for obtaining myelin with sulfocerebrosides, promoting the transmission and conduction of neuronal impulses.

Pharmacokinetics

After oral administration, Retinol acetate is well absorbed within 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 blood circulation. The movement of retinolesters within the blood is carried out with the help of β-lipoproteins. Serum Cmax values are noted after 3 hours from the moment of use.

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

Retinol is converted inside the liver, and then, under the guise of metabolic components that have no therapeutic activity, it is excreted through the kidneys.

Part of the drug can be excreted in the bile, and also become a participant in the processes of intrahepatic circulation. Elimination of the vitamin is carried out 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, after 10-15 minutes from the moment of eating. It is also used externally.

Inside 1 ml of the drug contains 100,000 IU (in 25 drops) retinol. The first drop given through a dropper contains approximately 4000 IU of retinol.

During the selection of portions, medicines are based on the following proportions:

• an adult can enter a maximum of 50 thousand IU at a time (in 12 drops of a substance - 48 thousand IU);
• a child over 7 years old - no more than 5 thousand IU (in the first drop of the medicine - 4 thousand IU);
• per day, an adult can use a maximum of 100 thousand IU of Retinol acetate (25 drops);
• a child over 7 years old is injected no more than 20 thousand IU (5 drops) per day.

In the case of mild or moderate vitamin deficiencies, the size of the therapeutic portion of the drug is equal to a maximum of 33 thousand IU per day (8 drops (corresponds to 32 thousand IU)).

In case of epidermal diseases, xerophthalmia, pigmented retinitis and hemeralopia, the daily dosage of retinol is 50-100 thousand IU (12-25 drops of the medication (corresponding to 48-100 thousand IU)).

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

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

• Application for children

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

Use Retinol acetate during pregnancy

Due to the high content of retinol in the indicated form of drug release, it cannot be used for HB or pregnancy.

Contraindications

Among the contraindications:

• severe sensitivity associated with the elements of the medication;
• nephritis, which is active or chronic;
• decompensated type of HF;
• hyperlipidemia;
• cholelithiasis;
• chronic pancreatitis;
• type A hypervitaminosis;
• retinoid poisoning;
• obesity;
• chronic alcoholism;
• sarcoidosis (also present in history).

Side effects Retinol acetate

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

• disorders associated with the work of the NS and sensory organs: drowsiness, headaches, discomfort, accelerated fatigue, convulsions and lethargy, and in addition, irritability, loss of sleep, visual disturbances and increased IOP values;
• problems affecting the digestive system: weight loss, loss of appetite and nausea. Vomiting appears occasionally. There may be an exacerbation of hepatic pathologies, as well as an increase in alkaline phosphatase and transaminase activity;
• disorders of urinary function: nocturia, pollakiuria and polyuria;
• lesions of hematopoietic activity: hemolytic type of anemia;
• signs associated with the work of ODA: gait disturbance, bone changes on radiographs, pain in the bones in the legs;
• allergy symptoms: puffiness under the skin, cracks affecting the skin on the lips, as well as the appearance of yellow-orange spots in the palms, soles and in the nasolabial triangle. Sometimes during the 1st day of taking drugs, itchy rashes of a maculopapular type develop, in which the drug must be canceled. There may be erythema, xerostomia, itching with rashes, dry epidermis, fever and facial hyperemia, accompanied by desquamation;
• others: disorder of the menstrual cycle, photophobia, alopecia, aphthae, hypercalcemia and abdominal pain.

Reducing the dosage or temporarily canceling the drug allows you to eliminate the above violations.

In case of epidermal lesions, the use of large portions of the drug after 7-10 days of therapy can lead to an exacerbation of local inflammation (it does not need to be further treated, it soon weakens on its own). A similar reaction is caused by the immuno- and myelo-stimulating effect of drugs.

Overdose

Signs of intoxication: confusion, dizziness, irritability, dehydration, diarrhea and generalized rash with further development of scaling (a large layer) beginning on the face. In addition, there is xerostomia, ulceration of the oral mucosa, bleeding in the gums, peeling on the lips and severe pain on palpation of the tubular bones (due to hemorrhages in the subperiosteal region).

In the case of a chronic or active form of type A hypervitaminosis, drowsiness, pain in the area of muscles and joints, vomiting, severe headaches and visual disturbances (diplopia) appear. Also, the temperature increases, age spots appear, epidermal dryness or jaundice develops, the size of the spleen and liver increases, there is a loss of appetite and strength, as well as a change in the blood picture. With severe intensity disorders, hydrocephalus and weakness of the heart occur, as well as seizures.

Symptomatic actions are performed.

Interactions with other drugs

Estrogens increase the likelihood of subtype A hypervitaminosis.

The drug weakens the anti-inflammatory activity of GCS.

It is forbidden to combine the drug with cholestyramine, as well as nitrites, since they interfere with the processes of its absorption.

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

The introduction together with tocopherol helps to maintain the activity of the drug, and in addition, promotes intestinal absorption and the development of anabolic symptoms.

Application with vaseline oil can interfere with the intra-intestinal absorption of drugs.

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

Storage conditions

Retinol acetate must be kept out of the reach of small children. Temperature values are within the range of 2-8 ° C.

Shelf life

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

Analogs

Analogs of drugs are the substances Videstim, as well as Retinol palmitate.