Project Description

Solutio Retinoli acetatis oleosa

in capsulis (Vitaminum A)

(capsules 5000 МЕ, 33000 МЕ) Solutio Retinoli palmitatis oleosa in capsulis (Vitaminum A) 100000 МЕ

international nonproprietary name

Retinol.

Ref

BP-0122

Pharmacotherapeutic group

Vitaminous medicalproduct.

Composition of the preparation

1 capsule contains Retinoli acetates – 5000 МЕ or 33000 МЕ and Retinoli palmitatis – 100000 МЕ.

Pharmacological action

Pharmacodynamics

Makes up for a deficiency in vitamin A. As a result of a great amount of unsaturated bonds, it activates redox processes, stimulates the synthesis of purine and pyrimidine bases, takes part in metabolism energy supply, creating favorable conditions for adenosine triphosphate (ATP) synthesis. It increases the synthesis of proteins in cartilaginous and bone tissue; it determines bones and cartilages growth. It stimulates epithelization and prevents from hyperkeratosis of epithelium (hyperkeratosis). It increases the amount of mitoses in epithelial cells, prevents them from keratohyalin accumulation, reinforces ribonucleic acid (RNA) and sulphated mucopolysaccharides synthesis, which are playing an important role in permeability of cellular, subcellular and , in particular, lysosomal membranes. It controls the speed of chain reactions in the lipidic phase of biomembranes and supports antioxidant potential of different tissues at the fixed level. It regulates the biosynthesis of glycoprotein of the cells surface membranes, which determine the level of cytodifferentiation processes. It regulates a normal function of monolayer pavement epithelium, which plays a role of a barrier, increases organism’s resistance to infections. It reinforces antibody formation and activates phagocytosis. It influences photoreception, taking part in visual purple formation. It stimulates the synthesis of adrenal cortex hormones. It impedes thyroxin liberation. It provides a normal activity of sebaceous and sweat-glands.

Pharmakokinetics

The ingested medical product is soaked almost in full, even if it is ingested excessively, it is oozed out with feces in the amount not more than 10% from the ingested amount. Retinoli palmitatis, retinol, retinal and retinoic acid appear during the process of metabolism. It is distributed in the organism non-uniformly: greater amount is allocated in liver and retina; lesser – in kidneys, heart, fat depots, lungs, lactating mammary gland, adrenal glands and other endocrine glands. Retinoli palmitatis is the preferred form of depositing. Retinol, retinal and retinoic acid are oozed out by hepatocytes in the composition of bile, retinolglucuronid is oozed out together with urine. Retinol elimination is carried out slowly, therefore repeated ingestion leads to cumulation and undesired effects persist for a long time.

Indications 

Hypovitaminosis and avitaminosis A; infectious diseases (measles, dysentery, tracheitis, bronchitis, pneumonia), skin diseases (burns, frostbites, wounds, cutaneous tuberculosis, hyperkeratosis, ichthyosis, psoriasis, pyodermatosis, some forms of eczema and other pathologic inflammatory and degenerative processes), eye diseases (pigmented retinitis, hemeralopia, xerophthalmia, keratomalacia, eczematous eyelids affection, conjunctivitis), rachitis, hypotropia, acute respiratory disease (ARD), chronic bronchopulmonary diseases, erosive and ulcerous and inflammatory affections of gastrointestinal tract, cirrhosis, epithelial neoplasm and leucosis (for increasing resistance of blood-forming tissue to cytostatic agents activity), mastopathy.

special indication

Teratogenic effect of retinol heightened doses is preserved even after discontinuation of the drug, therefore it is recommended to plan pregnancy while using the product only in 6-12 months.

special warning

Not established

Dosage and method of administration

The usage of the medical product shall be carried out under doctoral control. The product is ingested after meal early in the morning or late in the evening.

Medical doses when having avitaminosis of easy and medium severity level: for adults – up to 33000 МЕ/a day; when having hemeralopia, xerophthalmia and pigmented retinitis – 50000—100000 МЕ/a day; for children – 1000—5000 МЕ/a day depending on age. When having skin diseases: for adults – 50000—100000 МЕ/a day; for children is prescribed on the basis of – 5000—10000—20000 МЕ/a day.

Single doses of retinol shall not exceed 50000 МЕ for adults and 5000 МЕ for children; daily doses shall not exceed 100000 МЕ for adults and 20000 МЕ for children.

overdosage

Strong headache, dizziness, drowsiness, mental confusion, vision disorders, convulsions, intractable vomiting, profuse diarrhea, severe fluid loss take place during acute hypervitaminosis; extensive rash with further large-scaled desquamation appears on the second day starting with face; palpation of long cortical bones is sharply painful as a result of subperiosteal hemorrhage, bones and soft tissues changes. Child’s acute hypervitaminosis is characterized by anxiety, excitement, insomnia during the first day, sometimes drowsiness, rise in temperature up to 39 °С, vomiting, outpouching of prefontanel, signs of asthma can appear.

Curing: Symptomatic, thyroxin and also ascorbic acid are prescribed as an antagonist.

safety measures

Not established

Side effects

Headache, flabbiness, nausea, vomiting, fever, drowsiness, skin desquamation, gait disorders, painfulness in lower extremities bones, hypervitaminosis A are possible during the product ingestion. Children can experience a rise in temperature, drowsiness, hyperhidrosis, vomiting, appearance of skin rash, cerebrospinal fluid boost pressure (hydrocephalus and fontanel outpouching can be developing when speaking about infants). In individual cases itching maculosus and papulous appearance of skin rash can take place on the first day of ingestion; it requires discontinuation of the drug.

By-effects disappear on their own by eliminating doses or temporary discontinuing of the drug. When high doses are prescribed for skin diseases curing, exacerbation of local inflammatory reaction takes place in 7-10 day; it doesn’t require additional curing and decreases later on. This effect is connected with myelo- and immunostimulating action of the drug.

Contraindications

Estrogens and oral contraceptives, which contain them, potentize retinol soaking; that can lead to hypervitaminosis A development. It is not recommended to prescribe vitamin A during a long-term therapy with tetracyclines (increases the risk of intracranial hypertension development). Retinol shall be ingested 1 hour before or 4-6 hours after colestiramin ingestion. Nitrites disturb retinol soaking. It lessens (mutually) the danger of hypervitaminosis D. Corticosteroids and alcohol intake decrease the drug therapeutic effect.

Interactions with other medicinal preparations

The cases of negative drug interaction by using the ointment Reparaef-2 are not noted against a background of therapy by antiseptics, antiviral agents, antibiotics, analgesics, nonsteroidal and steroidal antiphlogistic agents and other medical products, included in the agreed scheme of curing of wound and ulcero-necrotic affection of skin and mucous membranes, burns and frostbites. The ointment Reparaef-2 is used on the last stage of local treatment in 5-10 minutes after application of the previous medical product. Food and beverages intake is recommended not earlier than in 1-1,5 hours.

The form of release

Soft gelatinous capsules. 50 capsulesincans.