Aekol (Beta Carotene,Vitamin E (Alpha Tocoferol),Menadione, Retinol)
Aekol (Beta Carotene,Vitamin E (Alpha Tocoferol),Menadione, Retinol) Uses, Dosage, Side Effects, Food Interaction and all others data.
Beta-carotene, with the molecular formula C40H56, belongs to the group of carotenoids consisting of isoprene units. The presence of long chains of conjugated double bonds donates beta-carotene with specific colors. It is the most abundant form of carotenoid and it is a precursor of the vitamin A. Beta-carotene is composed of two retinyl groups. It is an antioxidant that can be found in yellow, orange and green leafy vegetables and fruits. Under the FDA, beta-carotene is considered as a generally recognized as safe substance (GRAS).
Oral administration of beta-carotene increases the serum concentration of beta-carotene by 60% but it does not change the concentration found in the heart, liver or kidneys. In vitro studies in hepatocytes have shown that beta-carotene ameliorates oxidative stress, enhances antioxidant activity and decreases apoptosis.
Other than the antioxidant activities, some other actions have been correlated to beta-carotene. It is thought to have detoxifying properties, as well as to help increase resistance to inflammation and infection and increase immune response and enhance RNA production.
A synthetic naphthoquinone without the isoprenoid side chain and biological activity, but can be converted to active vitamin K2, menaquinone, after alkylation in vivo.
Menadione (Vitamin K3) is a fat-soluble vitamin precursor that is converted into menaquinone in the liver. Vitamin K1 and K2 are the naturally occurring types of vitamin K. The former, which is also known as phylloquinone, is synthesized by plants and can be found in such foods as spinach, broccoli, lettuce, and soybeans. The latter, sometimes alternatively referred to as menaquinone, is primarily produced by bacteria in the anterior part of the gut and the intestines. Vitamin K3, on the other hand, is one of the many manmade versions of vitamin K. Also called menadione, this yellowish, synthetic crystalline substance is converted into the active form of the K2 vitamin inside of the animal body. While a vitamin K deficiency can be dangerous, especially to infants that may easily suffer from extensive hemorrhaging, an overdose can be as equally detrimental. Newborns that are administered too great a dosage of vitamin K3 can suffer from kernicterus, a form of severe brain damage that may produce decreased movement, loss of appetite, seizures, deafness, mental retardation, and even death. This condition is associated with an abnormally high concentration of bilirubin, a bile pigment, in the tissues of the brain, which can be caused by the presence of K3. For this reason, K3 is less often utilized medically than it was in former times.
Vitamin A plays an essential role in the function of retina and is essential for growh and differentiation of epithelial tissue.
Vitamin A is effective for the treatment of Vitamin A deficiency. Vitamin A refers to a group of fat-soluble substances that are structurally related to and possess the biological activity of the parent substance of the group called all-trans retinol or retinol. Vitamin A plays vital roles in vision, epithelial differentiation, growth, reproduction, pattern formation during embryogenesis, bone development, hematopoiesis and brain development. It is also important for the maintenance of the proper functioning of the immune system.
Table Of contents
| Trade Name | Aekol (Beta Carotene,Vitamin E (Alpha Tocoferol),Menadione, Retinol) |
| Generic | Beta Carotene + Menadione + Vitamin A + Vitamin E (alpha Tocoferol) |
| Type | |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Russia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Beta carotene is a vitamin A precursor found in various nutritional supplements and health products.
Beta-carotene is FDA approved to be used as a nutrient supplement and to be even added in infant formula as a source of vitamin A. It is also approved to be used as a color additive for food products, drugs (with the label of "only as a color additive") and cosmetics.
It is used commonly for the reduction of photosensitivity in patients with erythropoietic protoporphyria and other photosensitivity diseases.
The primary known function of vitamin K is to assist in the normal clotting of blood, but it may also play a role in normal bone calcification.
Effective for:
- Vitamin A deficiency. Taking vitamin A by mouth is effective for preventing and treating symptoms of vitamin A deficiency. Vitamin A deficiency can occur in people with protein deficiency, diabetes, over-active thyroid, fever, liver disease, cystic fibrosis, or an inherited disorder called abetalipoproteinemia.
Possibly Effective for:
- Breast cancer. Premenopausal women with a family history of breast cancer who consume high levels of vitamin A in their diet seem to have reduced risk of developing breast cancer. It is not known if taking vitamin A supplements has the same benefit.
- Cataracts. Research suggests that high intake of vitamin A in the diet is linked to a lower risk of developing cataracts.
- Diarrhea related to HIV. Taking vitamin A along with conventional medicines seems to decrease the risk of death from diarrhea in HIV-positive children with vitamin A deficiency.
- Malaria. Taking vitamin A by mouth seems to decrease malaria symptoms in children less than 3 years-old living in areas where malaria is common.
- Measles. Taking vitamin A by mouth seems to reduce the risk of measles complications or death in children with measles and vitamin A deficiency.
- Precancerous lesions in the mouth (oral leukoplakia). Research suggests that taking vitamin A can help treat precancerous lesions in the mouth.
- Recovery from laser eye surgery (photoreactive keratectomy). Taking vitamin A by mouth along with vitamin E seems to improve healing after laser eye surgery.
- Complications after pregnancy. Taking vitamin A seems to reduce the risk of diarrhea and fever after pregnancy in malnourished women.
- Complications during pregnancy. Taking vitamin A by mouth seems to reduce the risk of death and night blindness during pregnancy in malnourished women.
- Eye disease affecting the retina (retinitis pigmentosa). Research suggests that taking vitamin A can slow the progression of an eye disease that causes damage to the retina.
Aekol (Beta Carotene,Vitamin E (Alpha Tocoferol),Menadione, Retinol) is also used to associated treatment for these conditions: Deficiency, Vitamin A, Nutritional supplementationFactor II deficiency, Vitamin B12 DeficiencyDeficiency, Vitamin A, Deficiency, Vitamin D, Degenerative Retinal Disorders, Disorder of the Epithelium, Disorder of the Mesoderm, Inner ear disorder, Vitamin Deficiency, Vitamin E Deficiency, Nutritional supplementation
How Aekol (Beta Carotene,Vitamin E (Alpha Tocoferol),Menadione, Retinol) works
Beta-carotene is an antioxidant that presents significant efficacy against the reactive oxygen species singlet oxygen. Beta-carotene acts as a scavenger of lipophilic radicals within the membranes of every cell compartments. It also presents an oxidative modification of LDL. The presence of long chains of conjugated double bonds is responsible for its antioxidative properties by allowing beta-carotene to chelate oxygen-free radicals and dissipate their energy. The chelation of free radicals inhibits the peroxidation of lipids.
The effect of beta-carotene in the immune response is thought to be related to the direct effect on the thymus which increases the production of immune cells.
Menadione (vitamin K3) is involved as a cofactor in the posttranslational gamma-carboxylation of glutamic acid residues of certain proteins in the body. These proteins include the vitamin K-dependent coagulation factors II (prothrombin), VII (proconvertin), IX (Christmas factor), X (Stuart factor), protein C, protein S, protein Zv and a growth-arrest-specific factor (Gas6). In contrast to the other vitamin K-dependent proteins in the blood coagulation cascade, protein C and protein S serve anticoagulant roles. The two vitamin K-dependent proteins found in bone are osteocalcin, also known as bone G1a (gamma-carboxyglutamate) protein or BGP, and the matrix G1a protein or MGP. Gamma-carboxylation is catalyzed by the vitamin K-dependent gamma-carboxylases. The reduced form of vitamin K, vitamin K hydroquinone, is the actual cofactor for the gamma-carboxylases. Proteins containing gamma-carboxyglutamate are called G1a proteins.
Vision:Vitamin A (all-trans retinol) is converted in the retina to the 11-cis-isomer of retinaldehyde or 11-cis-retinal. 11-cis-retinal functions in the retina in the transduction of light into the neural signals necessary for vision. 11-cis-retinal, while attached to opsin in rhodopsin is isomerized to all-trans-retinal by light. This is the event that triggers the nerve impulse to the brain which allows for the perception of light. All-trans-retinal is then released from opsin and reduced to all-trans-retinol. All-trans-retinol is isomerized to 11-cis-retinol in the dark, and then oxidized to 11-cis-retinal. 11-cis-retinal recombines with opsin to re-form rhodopsin. Night blindness or defective vision at low illumination results from a failure to re-synthesize 11-cis retinal rapidly.
Epithelial differentiation: The role of Vitamin A in epithelial differentiation, as well as in other physiological processes, involves the binding of Vitamin A to two families of nuclear retinoid receptors (retinoic acid receptors, RARs; and retinoid-X receptors, RXRs). These receptors function as ligand-activated transcription factors that modulate gene transcription. When there is not enough Vitamin A to bind these receptors, natural cell differentiation and growth are interrupted.
Dosage
Aekol (Beta Carotene,Vitamin E (Alpha Tocoferol),Menadione, Retinol) dosage
Vitamin A deficiency For severe deficiency with corneal changes: 500,000 unit/day for 3 days, followed by 50,000 unit/day for 2 wk and then 10,000-20,000 unit/day for 2 mth as follow-up therapy.
For cases without corneal changes: 10,000-25,000 unit/day until clinical improvement occurs (usually 1 -2 wk).
Side Effects
Hypervitaminosis A characterised by fatigue, irritability, anorexia, weight loss, vomiting and other Gl disturbances, low-grade fever, hepatosplenomegaly, skin changes, alopoecia, dry hair, cracking and bleeding lips, SC swelling, nocturia, pains in bones and joints.
Toxicity
Beta-carotene is not toxic but the high and constant administration of this substance can translate into skin yellow coloration. Some reports have indicated that administration of high and periodic doses of beta-carotene are correlated to the increase in cancer incidence. This risk seems to be very elevated in the case of smokers. The registered LD50 of beta-carotene is >5000 mg/kg.
Menadione (vitamin K3), which is not used as a nutritional supplemental form of vitamin K for humans, has been reported to cause adverse reactions, including hemolytic anemia. Large doses have also been reported to cause brain damage.
Acute toxicity to vitamin A can occur when adults or children ingest >100x or >20x the RDA, respectively, over a period of hours or a few days. The RDA for vitamin A differs depending on age and sex and can range from 300 - 900 μg retinol activity equivalents (RAE) per day. Symptoms of acute systemic toxicity generally include mucocutaneous involvement (e.g. xerosis, cheilitis, skin peeling) and may involve mental status changes. Children are typically more susceptible to acute vitamin A toxicity - daily intakes of as little as 1500 IU/kg have been observed to result in toxicity.
Chronic vitamin A toxicity can develop following the long-term ingestion of high vitamin A doses. While there is a wide variation in the lowest toxic vitamin A dose, the ingestion of >25 000 IU daily for 6 years or 100,000 IU daily for 6 months is considered to be toxic. Chronic vitamin A toxicity can affect many organ systems and can lead to the development of osteoporosis and CNS effects (e.g. headaches).
Precaution
Cholestatic jaundice; fat-malabsorption conditions. Monitor patients closely for toxicity. Liver impairment and children.
Interaction
Decreased absorption with neomycin. Increased risk of hypervitaminosis A with synthetic retinoids eg, acitretin, isotretinoin and tretinoin. Increased risk of toxicity when used with alcohol.
Volume of Distribution
No pharmacokinetic studies have been performed regarding the volume of distribution of beta-carotene.
Elimination Route
After administration of beta-carotene, some of the administered dose is absorbed into the circulatory system unchanged and stored in the fat tissue. The coadministration of beta-carotene and a high-fat content diet is correlated to a better absorption of beta-carotene. The absorption is also dependent on the isomeric form of the molecule where the cis conformation seems to present a higher bioavailability. The absorption of beta-carotene is thought to be performed in 6-7 hours.
The reported AUC of beta-carotene when administered orally from 0 to 440 hours after initial administration was reported to be 26.3 mcg.h/L. The maximal concentration of beta-carotene is attained in a dual pharmacokinetic profile after 6 hours and again after 32 hours with a concentration of 0.58 micromol/L.
Variable and ranges from 10% to 80%
Readily absorbed from the normal gastrointestinal tract
Half Life
The apparent half-life of beta-carotene is of 6-11 days after initial administration.
1.9 hours
Clearance
The clearance rate of beta-carotene administered orally is 0.68 nmol/L each hour.
Elimination Route
The unabsorbed carotene is excreted in feces. It is also excreted in feces and urine as metabolites. The consumption of dietary fiber can increase the fecal excretion of fats and other fat-soluble compounds such as beta-carotene.
Pregnancy & Breastfeeding use
Pregnancy Category A. Adequate and well-controlled human studies have failed to demonstrate a risk to the fetus in the first trimester of pregnancy (and there is no evidence of risk in later trimesters).
Contraindication
Hypervitaminosis A; pregnancy (dose exceeding RDA).
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