APPETAMINE CAPSULE (CAPSULE)

Dosage: AGE DOSE 2-6 yrs old 5 mL (1 teaspoonful) 7-14 yrs od 10 mL (2 teaspoonfuls) Above 14 yrs old 15 mL (1 tablespoonful) (To be taken daily or as prescribed by the physician.) Contraindications: Contraindicated in patients with history of hypersensitivity to the components. Special Precautions: Buclizine hydrochloride may cause drowsiness and patients taking the drug should be cautioned against engaging in activities requiring mental alertness like driving automobile. Also, it has central nervous system depressant effect and may potentiate other CNS depressant compounds. Adverse Reactions: Hypersensitivity reaction ranges from very mild to very rarely, anaphylactic shock, adverse effects seldom occur after oral administration of thiamine and cyanocobalamin. Administration of large doses of pyridoxine for long-term is associated with the development of severe peripheral neuropathies. Interactions: Vitamins - high dose of calcium and phosphorus containing compounds, drugs with same content to avoid overdose, antibiotics, non-steroidal anti-inflammatory drugs, anticoagulants, insulin, HMG-CoA reductase inhibitors, milk and levodopa. Buclizine - alcohol, antihistamines and other CNS depressants. Mechanism of Action Pharmacology: Properties and Functions: L-LYSINE: Lysine as an essential amino acid is a necessary building block for all protein in the body. It plays a major role in calcium absorption, building muscle protein; recovering from surgery or sports-related injuries and is utilized in the production of antibodies, hormones and enzymes which aid in digestion. Also, it can act as an appetite enhancer and is needed for proper growth and bone development in children. It aids in the improvement of calcium absorption and lessens loss of calcium in the urine. BUCLIZINE HCl: Buclizine HCl is mainly used for anti-emetic action and as an appetite stimulant that increase both appetite and absorption of food in the body. It does not affect the growth hormone levels and it can maintain weight gain even after discontinuation of treatment. ASCORBIC ACID (VITAMIN C): Vitamin C is required for the proper development and function of many parts of the body. It also plays an important role in maintaining proper immune function. THIAMINE (VITAMIN B1)/RIBOFLAVIN (VITAMIN B2): Thiamine, Riboflavin, like several other B-Vitamins is essential for normal development, growth, reproduction, lactation, physical performance, and well-being. Thiamine is involved in releasing energy from the macronutrients which provide energy, especially from carbohydrates. Thiamine enhances production of energy from glucose and storage of energy as fat, making energy available to support normal cellular processes. Vitamin B1 helps improve muscle tone of the stomach, intestines, heart and blood vessels. Riboflavin is involved in a wide array of essential biochemical oxidation-reduction reactions, especially those that yield energy. It is converted to two other coenzymes that are necessary for normal tissue respiration and energy production. PYRIDOXINE (VITAMIN B6): Vitamin B6 in blood and tissues occurs phosphorylated in three primary forms. These pyridoxines are pyridoxol (the alcohol), pyridoxal (the aldehyde) and pyridoxamine (the amine). The activated forms of pyridoxal and pyridoxamine are the active coenzyme forms, and the inter-conversion between them is involved in many of the biological functions of the vitamin. This vitamin is required for many enzymatic reactions and extensively involved in the metabolism of amino acids and other nitrogen-containing compounds, and also in the metabolism of lipids and the production and activities of certain hormones. These include transam-ions, deamination, decarboxylation, and sulfation. It plays a part in protein metabolism, the synthesis of fat from protein, haemopoiesis and nutrition of the skin. CYANOCOBALAMIN (VITAMIN B12): Vitamin B12 is a large complex compound consisting of porphyrin ring containing cobalt. Cyanocobalamin functions as an integral part of the cobarnide enzymes which are involved in nucleic acid synthesis, carbohydrate metabolism, lipid metabolism, and amino acid metabolism. Cyanocobalamin is a cofactor in two enzymes that are fundamental in facilitating growth essential for the function and maintenance of central nervous system. Severe deficiency in cases of pernicious anemia produces a neurological disease called posterolateral spinal cord degeneration. The immediate cause of pernicious anemia is Vitamin B12 deficiency but the underlying defect is the absence of intrinsic factor produced by cells of the stomach needed for intestinal absorption of Vitamin B12. Therefore, daily high oral intake can be sufficient to treat pernicious anemia. NICOTINAMIDE: Nicotinamide or niacinamide performs all the essential biochemical functions of Niacin has fundamental role as reduction/oxidation coenzymes essential for tissue respiration, lipid metabolism and glycogenolysis, involved in energy metabolism and detoxification reactions for drugs and other substances. Pharmacokinetics: Thiamine is absorbed from the GI tract and is widely distributed to most body tissues. It is not stored to any appreciable extent in the body and amounts in excess of requirements are excreted in the urine as unchanged thiamine or metabolites. Riboflavin is absorbed from the GI tract and in the circulation is bound to plasma proteins. Although widely distributed, little is stored in the body, and amounts in excess of requirements are excreted in the urine. Nicotinamide is readily absorbed from the GI tract following oral administration and is widely distributed in the body tissues. Small amounts of nicotinamide are excreted unchanged in urine following therapeutic doses, however, the amount excreted unchanged is increased with larger doses. Pyridoxine is absorbed from the GI tract and is converted to the active form pyridoxal phosphate. It is stored mainly in liver with lesser amounts in muscle and brain. It also crosses the placenta and is distributed into milk. It is excreted in the urine as 4-pyridoxic acid. Cyanocobalamin is irregularly absorbed from the distal small intestine following oral administration. It requires gastric intrinsic factor for active absorption from the GI tract. It is distributed into liver, bone marrow, and other tissues. It also crosses the placenta and is distributed into milk. More than 50-98% may be excreted in urine. Ascorbic acid is readily absorbed by an active process that may be limited after very large doses and is widely distributed in body tissues. It can cross the placenta and can be distributed into milk. Upon metabolism, it is reversibly oxidized to dehydroascorbic acid and is excreted through urine. Lysine upon ingestion is absorbed from the lumen of the small intestine into the enterocytes via active transport and moves from the gut to the liver via the portal circulation. Once in the liver, lysine joins other amino acids to facilitate protein synthesis. Lysine is rapidly transported into muscle tissue, within 5-7 hours after ingestion, and is more concentrated in the intracellular space of muscle tissue compared to other essential amino acids. Buclizine is readily absorbed in the GI tract. Its onset of action is after one hour and the duration of the drug ranges from 4-6 hrs.