Capsule: Pharmacology: Pharmacodynamics: 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.
Cholecalciferol is a steroid hormone produced in the skin when exposed to ultraviolet light or obtained from dietary sources. The active form of cholecalciferol, 1,25-dihydroxycholecalciferol (calcitriol) plays an important role in maintaining blood calcium and phosphorus levels and mineralization of bone. The activated form of cholecalciferol binds to vitamin D receptors and modulates gene expression. This leads to an increase in serum calcium concentrations by increasing intestinal absorption of phosphorus and calcium, promoting distal renal tubular reabsorption of calcium and increasing osteoclastic resorption.
Thiamine is a vitamin required in cellular aerobic metabolism, cell growth, nerve impulse transmission and production of acetylcholine.
Riboflavin is an essential human nutrient that is a heat-stable and water-soluble flavin belonging to the vitamin B family. Riboflavin is a precursor of the coenzymes flavin mononucleotide (FMN) and flavin adenine dinucleotide (FAD). These coenzymes are of vital importance in normal tissue respiration, pyridoxine activation, tryptophan to niacin conversion, fat, carbohydrate, and protein metabolism, and glutathione reductase mediated detoxification. Riboflavin may also be involved in maintaining erythrocyte integrity. This vitamin is essential for healthy skin, nails, and hair.
Nicotinamide is the active form of vitamin B3 and a component of the coenzyme nicotinamide adenine dinucleotide (NAD). Nicotinamide acts as a chemo- and radio-sensitizing agent by enhancing tumor blood flow, thereby reducing tumor hypoxia. This agent also inhibits poly (ADP-ribose) polymerases, enzymes involved in the rejoining of DNA strand breaks induced by radiation or chemotherapy.
Pyridoxine hydrochloride is the hydrochloride salt form of pyridoxine, a water-soluble vitamin B. Pyridoxine hydrochloride is converted into the active form, pyridoxal 5'-phosphate (PLP), an essential cofactor in many enzymatic activities including synthesis of amino acids, neurotransmitters, and sphingolipids. This vitamin is essential to red blood cell, nervous system, and immune systems functions and helps maintain normal blood glucose levels.
Cyanocobalamin or vitamin B12 is a water-soluble organometallic compound containing a trivalent cobalt ion bound to a corrin ring. Vitamin B12 is an essential coenzyme in nucleic acid synthesis as well as nerve functions and blood cell production. Adult recommended requirements is about 1 to 2 micrograms per day.
Ferrous sulfate replenishes iron, an essential component in hemoglobin, myoglobin, and various enzymes. It replaces the iron that is usually found in hemoglobin and myoglobin. Iron participates in oxygen transport and storage, electron transport and energy metabolism, antioxidant and beneficial pro-oxidant functions, oxygen sensing, tissue proliferation and growth, as well as DNA replication and repair.
Buclizine is a piperazine-derivative antihistamine used as an antivertigo/antiemetic agent. Buclizine is used in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. Additionally, it has been used in the management of vertigo in diseases affecting the vestibular apparatus.
Lysine belongs to one of the nine essential amino acids in humans. Amino acids serve as the building blocks of protein and are important for growth and tissue repair. Unlike the non-essential amino acids, essential amino acids are not synthesized by the human body and are usually supplied from dietary sources.
Pharmacokinetics: Absorption: Retinol (Vitamin A): Retinol is readily absorbed from the normal gastrointestinal tract.
Cholecalciferol (Vitamin D3): Cholecalciferol is readily absorbed from the small intestine if fat absorption is normal. Moreover, bile is necessary for absorption as well.
Thiamine (Vitamin B1): Small amounts of thiamine are well absorbed from the gastrointestinal tract after oral doses.
Riboflavin (Vitamin B2): Riboflavin is readily absorbed from the gastrointestinal tract.
Nicotinamide (Vitamin B3): Nicotinamide is readily absorbed from the gastrointestinal tract after oral doses.
Pyridoxine (Vitamin B6): Pyridoxine is readily absorbed from the gastrointestinal tract after oral doses.
Cyanocobalamin (Vitamin B12): Vitamin B12 substances bind to intrinsic factor, a glycoprotein secreted by the gastric mucosa, and are then actively absorbed from the gastrointestinal tract.
Ferrous sulfate (Iron): Iron is irregular and incompletely absorbed from the gastrointestinal tract, the main sites of absorption being the duodenum and jejunum.
Buclizine: Buclizine is rapidly absorbed following oral administration.
Lysine: Free amino acids, including free lysine, are absorbed in the small intestines.
Free amino acids in the intestinal lumen are transported into the mucosal cells by an amino acid-specific carrier system. The amino acids are then secreted out to the portal circulation.
Distribution: Retinol (Vitamin A): Less than 5% of circulating vitamin A is bound to lipoproteins in blood in normal condition but may be up to 65% when hepatic stores are saturated because of excessive intake. When released from liver, vitamin A is bound to retinol-binding protein (RBP). Most vitamin A circulates in the form of retinol bound to RBP.
Cholecalciferol (Vitamin D3): Studies have determined that the mean central volume of distribution of administered cholecalciferol supplementation in a group of 49 kidney transplant patients was approximately 237 L.
Thiamine (Vitamin B1): Thiamine is widely distributed to most body tissues and appears in breastmilk.
Riboflavin (Vitamin B2): About 60% of FMN and FAD are bound to plasma proteins.
Nicotinamide (Vitamin B3): Nicotinamide is widely distributed in the body tissues.
Pyridoxine (Vitamin B6): Pyridoxine is mainly stored in the liver with lesser amounts in muscle & brain.
Cyanocobalamin (Vitamin B12): Vitamin B12 is released from food and salivary binding protein and bound to gastric intrinsic factor. When the vitamin B12 intrinsic factor complex reaches the ileum, it interacts with the receptor on the mucosal cell surface and is actively transported into circulation.
Ferrous sulfate (Iron): Most of absorbed iron is bound to transferrin and transported to the bone marrow where it is incorporated into hemoglobin. The remainder is contained within the storage forms, ferritin, or hemosiderin, or as myoglobin, with smaller amounts occurring in heme containing enzymes or in plasma bound to transferrin.
Buclizine: Buclizine is rapidly absorbed following oral administration.
Lysine: The free amino acids in the portal circulation will pass through the liver, a portion of which will be utilized. The remaining amino acids are then transported to the systemic circulation for utilization by the peripheral tissues.
Metabolism: Retinol (Vitamin A): Retinol undergoes hepatic metabolism. Retinol is conjugated with glucuronic acid; the B-glucuronide undergoes enterohepatic circulation and oxidation to retinol and retinoic acid. Retinoic acid undergoes decarboxylation and conjugation with glucuronic acid.
Cholecalciferol (Vitamin D3): Within the liver, cholecalciferol is hydroxylated to calcifediol (25-hydroxycholecalciferol) by the enzyme vitamin D-25-hydroxylase. At the kidney, calcifediol subsequently serves as a substrate for 1-alpha-hydroxylase, yielding calcitriol (1,25-dihydroxycholecalciferol), the biologically active form of vitamin D3.
Thiamine (Vitamin B1): Thiamin from dietary supplements is absorbed by the small intestine through active transport at nutritional doses and by passive diffusion at pharmacologic doses.
Riboflavin (Vitamin B2): Riboflavin is converted in the body to the coenzyme flavin mononucleotide and then to another coenzyme flavin adenine dinucleotide (FAD).
Nicotinamide (Vitamin B3): Niacin is converted in the body to the amide, which is incorporated into niacinamide adenine dinucleotide (NAD).
Pyridoxine (Vitamin B6): After oral administration of pyridoxine, it is converted into active forms pyridoxal phosphate and pyridoxamine phosphate. Pyridoxine is oxidized in the liver to form 4-pyridoxic acid and other inactive metabolites.
Cyanocobalamin (Vitamin B12): Vitamin B12 is extensively bound to plasma proteins transcobalamin. Transcobalamin II appears to be involved in the rapid transport of the cobalamins to tissues.
Ferrous sulfate (Iron): Absorption of iron is aided by the acid secretion of the stomach and by some dietary acids (such as ascorbic acid) and occurs more readily when iron is in the ferrous state or is part of the heme complex (heme-iron).
Lysine: Lysine is metabolized via protein synthesis or oxidative catabolism. During protein synthesis, lysine is utilized for the formation of substances such as carnitine, collagen and elastin. With oxidative catabolism, lysine is broken down to products that can be further used for the biosynthetic pathways for glucose and fat.
Excretion: Retinol (Vitamin A): Vitamin A is excreted via the feces and urine and has a half-life of 1.9 hours.
Cholecalciferol (Vitamin D3): It has been observed that administered cholecalciferol and its metabolites are excreted primarily in the bile and feces.
Thiamine (Vitamin B1): In excess amount of thiamine in the body's requirement are excreted in the urine unchanged or as metabolites.
Riboflavin (Vitamin B2): Riboflavin is excreted in urine, partly as metabolites.
Nicotinamide (Vitamin B3): Small amount of nicotinamide is excreted unchanged in urine after therapeutic doses; The amount excreted unchanged is increased with larger doses.
Pyridoxine (Vitamin B6): Pyridoxine is excreted in urine.
Cyanocobalamin (Vitamin B12): Vitamin B12 is excreted in the bile and undergoes extensive enterohepatic recycling and part of a dose is excreted in the urine.
Ferrous sulfate (Iron): A very small amount of iron is excreted as the majority is released after the destruction of the hemoglobin molecule is re-used.
Lysine: Nitrogen is excreted through the urine mostly in the form of urea. Urea is the end product of amino acid catabolism.
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