Calcium¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Calcium plays a vital role in the anatomy, physiology and biochemistry of organisms and of the cell, particularly in signal transduction pathways. More than 500 human proteins are known to bind or transport calcium. The skeleton acts as a major mineral storage site for the element and releases Ca2+ ions into the bloodstream under controlled conditions. Circulating calcium is either in the free, ionized form or bound to blood proteins such as serum albumin. Parathyroid hormone (secreted from the parathyroid gland) regulates the resorption of Ca2+ from bone. Calcitonin stimulates incorporation of calcium in bone, although this process is largely independent of calcitonin. Although calcium flow to and from the bone is neutral, about 5 mmol is turned over a day. Bone serves as an important storage point for calcium, as it contains 99% of the total body calcium. Low calcium intake may also be a risk factor in the development of osteoporosis. The best-absorbed form of calcium from a pill is a calcium salt like carbonate or phosphate. Calcium gluconate and calcium lactate are absorbed well by pregnant women. Seniors absorb calcium lactate, gluconate and citrate better unless they take their calcium supplement with a full breakfast. The currently recommended calcium intake is 1,500 milligrams per day for women not taking estrogen and 800 milligrams per day for women on estrogen. There is close to 300 milligrams of calcium in one cup of fluid milk. Calcium carbonate is currently the best and least expensive form of calcium supplement available. Hydroxocobalamin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Vitamin B12 exists in four major forms referred to collectively as cobalamins; deoxyadenosylcobalamin, methylcobalamin, hydroxocobalamin, and cyanocobalamin. Two of these, methylcobalamin and 5-deoxyadenosyl cobalamin, are primarily used by the body. Methionine synthase needs methylcobalamin as a cofactor. This enzyme is involved in the conversion of the amino acid homocysteine into methionine. Methionine in turn is required for DNA methylation. 5-Deoxyadenosyl cobalamin is a cofactor needed by the enzyme that converts L-methylmalonyl-CoA to succinyl-CoA. This conversion is an important step in the extraction of energy from proteins and fats. Furthermore, succinyl CoA is necessary for the production of hemoglobin, the substances that carries oxygen in red blood cells. Pyridoxal¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Pyridoxal is the precursor to pyridoxal phosphate. Pyridoxal 5'-phosphate is involved in a wide range of biochemical reactions, including the metabolism of amino acids and glycogen, the synthesis of nucleic acids, hemogloblin, sphingomyelin and other sphingolipids, and the synthesis of the neurotransmitters serotonin, dopamine, norepinephrine and gamma-aminobutyric acid (GABA). Riboflavin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Binds to riboflavin hydrogenase, riboflavin kinase, and riboflavin synthase. Riboflavin is the precursor of flavin mononucleotide (FMN, riboflavin monophosphate) and flavin adenine dinucleotide (FAD). The antioxidant activity of riboflavin is principally derived from its role as a precursor of FAD and the role of this cofactor in the production of the antioxidant reduced glutathione. Reduced glutathione is the cofactor of the selenium-containing glutathione peroxidases among other things. The glutathione peroxidases are major antioxidant enzymes. Reduced glutathione is generated by the FAD-containing enzyme glutathione reductase.
Pharmacology
Hydroxocobalamin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Hydroxocobalamin is a synthetic, injectable form of Vitamin B12. Hydroxocobalamin is actually a precursor of two cofactors or vitamins (Vitamin B12 and Methylcobalamin) which are involved in various biological systems in man. Vitamin B12 is required for the conversion of methylmalonate to succinate. Deficiency of this enzyme could therefore interfere with the production of lipoprotein in myelin sheath tissue and so give rise to neurological lesions. The second cofactor, Methylcobalamin, is necessary for the conversion of homocysteine to methionine which is essential for the metabolism of folic acid. Deficiency of tetrahydrafolate leads to reduced synthesis of thymidylate resulting in reduced synthesis of DNA which is essential for cell maturation. Vitamin B12 is also concerned in the maintenance of sulphydryl groups in reduced form, deficiency leading to decreased amounts of reduced SH content of erythrocytes and liver cells. Overall, vitamin B12 acts as a coenzyme for various metabolic functions, including fat and carbohydrate metabolism and protein synthesis. It is necessary for growth, cell replication, hematopoiesis, and nucleoprotein as well as myelin synthesis. This is largely due to its effects on metabolism of methionine folic acid, and malonic acid. Pyridoxal¿¡ ´ëÇÑ Pharmacology Á¤º¸ Pyridoxal principally in the form of the coenzyme pyridoxal 5'-phosphate, is involved in a wide range of biochemical reactions, including the metabolism of amino acids and glycogen, the synthesis of nucleic acids, hemogloblin, sphingomyelin and other sphingolipids, and the synthesis of the neurotransmitters serotonin, dopamine, norepinephrine and gamma-aminobutyric acid (GABA). Riboflavin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Riboflavin or vitamin B2 is an easily absorbed, water-soluble micronutrient with a key role in maintaining human health. Like the other B vitamins, it supports energy production by aiding in the metabolising of fats, carbohydrates, and proteins. Vitamin B2 is also required for red blood cell formation and respiration, antibody production, and for regulating human growth and reproduction. It is essential for healthy skin, nails, hair growth and general good health, including regulating thyroid activity. Riboflavin also helps in the prevention or treatment of many types of eye disorders, including some cases of cataracts.
Metabolism
Hydroxocobalamin¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available Pyridoxal¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Not Available Riboflavin¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Monoamine oxidase type A (MAO-A)Methylenetetrahydrofolate reductase
Protein Binding
Hydroxocobalamin¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ Very high (90%). Cobalamins are extensively bound to two specific plasma proteins called transcobalamin 1 and 2; 70% to transcobalamin 1, 5% to transcobalamin 2. Riboflavin¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ 60%
Half-life
Hydroxocobalamin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ Approximately 6 days (peak plasma concentration after 8-12 hours from oral administration) Pyridoxal¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ Not Available Riboflavin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 66-84 minutes
Absorption
Hydroxocobalamin¿¡ ´ëÇÑ Absorption Á¤º¸ Readily absorbed from the gastrointestinal tract, except in malabsorption syndromes. Vitamin B12 is absorbed in the lower half of the ileum. Pyridoxal¿¡ ´ëÇÑ Absorption Á¤º¸ Not Available Riboflavin¿¡ ´ëÇÑ Absorption Á¤º¸ Vitamin B2 is readily absorbed from the upper gastrointestinal tract.
Hydroxocobalamin¿¡ ´ëÇÑ Biotransformation Á¤º¸ Primarily hepatic. Cobalamins are absorbed in the ileum and stored in the liver. They continuously undergo enterohepatic recycling via secretion in the bile. Part of a dose is excreted in the urine, most of it in the first 8 hours. Pyridoxal¿¡ ´ëÇÑ Biotransformation Á¤º¸ Not Available Riboflavin¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic.
Toxicity
Hydroxocobalamin¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available Pyridoxal¿¡ ´ëÇÑ Toxicity Á¤º¸ Oral LD50 Rat: 2150 mg/kg, Oral LD50 Mouse: 1800 mg/kg Riboflavin¿¡ ´ëÇÑ Toxicity Á¤º¸ Not Available
Drug Interactions
Calcium¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alendronate Formation of non-absorbable complexesAmprenavir The antiacid decreases the absorption of amprenavirAtazanavir This gastric pH modifier decreases the levels/effects of atazanavirChloroquine The antiacid decreases the absorption of chloroquineCiprofloxacin Formation of non-absorbable complexesDapsone Formation of non-absorbable complexesDelavirdine The antiacid decreases the effect of delavirdineDemeclocycline Formation of non-absorbable complexesDoxycycline Formation of non-absorbable complexesEnoxacin Formation of non-absorbable complexesFosamprenavir The antiacid decreases the absorption of amprenavirGrepafloxacin Formation of non-absorbable complexesIbandronate Formation of non-absorbable complexesIndinavir The antiacid decreases the absorption of indinavirItraconazole The antacid decreases the effect of the imidazoleKetoconazole The antacid decreases the effect of the imidazoleLevofloxacin Formation of non-absorbable complexesLevothyroxine Calcium decreases absorption of levothyroxineLomefloxacin Formation of non-absorbable complexesMethacycline Formation of non-absorbable complexesMinocycline Formation of non-absorbable complexesMoxifloxacin Formation of non-absorbable complexesNorfloxacin Formation of non-absorbable complexesOfloxacin Formation of non-absorbable complexesOxytetracycline Formation of non-absorbable complexesPefloxacin Formation of non-absorbable complexesPolystyrene sulfonate Formation of non-absorbable complexesRisedronate Formation of non-absorbable complexesTetracycline Formation of non-absorbable complexesTrovafloxacin Formation of non-absorbable complexesClodronate Formation of non-absorbable complexesEtidronic acid Formation of non-absorbable complexesMycophenolate mofetil Formation of non-absorbable complexesTemafloxacin Formation of non-absorbable complexes Hydroxocobalamin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Alfentanil The macrolide increases the effect and toxicity of alfentanilAlprazolam The macrolide increases the effect of the benzodiazepineAminophylline The macrolide increases the effect and toxicity of theophyllineAmiodarone Increased risk of cardiotoxicity and arrhythmiasAnisindione The macrolide increases anticoagulant effectAprepitant This CYP3A4 inhibitor increases effect and toxicity of aprepitantAstemizole Increased risk of cardiotoxicity and arrhythmiasAtorvastatin The macrolide possibly increases the statin toxicityBretylium Increased risk of cardiotoxicity and arryhthmiasBromocriptine Erythromycin increases serum levels of bromocriptineBuspirone The macrolide increases the effect and toxicity of buspironeCabergoline Erythromycin increases serum levels and toxicity of cabergolineCarbamazepine The macrolide increases the effect of carbamazepineCerivastatin The macrolide possibly increases the statin toxicityCilostazol Erythromycin increases the effect of cilostazolCinacalcet This macrolide increases the serum levels and toxicity of cinacalcetCisapride Increased risk of cardiotoxicity and arrhythmiasCitalopram Possible serotoninergic syndrome with this combinationClozapine Erythromycin increases the effect of clozapineColchicine Severe colchicine toxicity can occurCyclosporine The macrolide increases the effect of cyclosporineDiazepam The macrolide increases the effect of the benzodiazepineDicumarol The macrolide increases anticoagulant effectDigoxin The macrolide increases the effect of digoxin in 10% of patientsDihydroergotamine Possible ergotism and severe ischemia with this combinationDihydroergotoxine Possible ergotism and severe ischemia with this combinationDyphylline The macrolide increases the effect and toxicity of theophyllineDisopyramide Increased risk of cardiotoxicity and arrhythmiasDivalproex sodium Erythromycin increases the effect of valproic acidDocetaxel The agent increases the serum levels and toxicity of docetaxelDofetilide Increased risk of cardiotoxicity and arrhythmiasEletriptan The macrolide increases the effect and toxicity of eletriptanEplerenone This CYP3A4 inhibitor increases the effect and toxicity of eplerenoneErgotamine Possible ergotism and severe ischemia with this combinationErlotinib This CYP3A4 inhibitor increases levels/toxicity of erlotinibImatinib The macrolide increases levels of imatinibFelodipine Erythromycin increases the effect of felodipineFluoxetine Possible serotoninergic syndrome with this combinationGefitinib This CYP3A4 inhibitor increases levels/toxicity of gefitinibGrepafloxacin Increased risk of cardiotoxicity and arrhythmiasItraconazole The macrolide increases the effect and toxicity of itraconazoleLevofloxacin Increased risk of cardiotoxicity and arrhythmiasMesoridazine Increased risk of cardiotoxicity and arrhythmiasMethylergonovine Possible ergotism and severe ischemia with this combinationLovastatin The macrolide possibly increases the statin toxicityMethylprednisolone The macrolide increases the effect of corticosteroidMethysergide Possible ergotism and severe ischemia with this combinationMidazolam The macrolide increases the efect of the benzodiazepineMoxifloxacin Increased risk of cardiotoxicity and arrhythmiasOxtriphylline The macrolide increases the effect and toxicity of theophyllinePimozide Increased risk of cardiotoxicity and arrhythmiasQuetiapine This macrolide increases the effect/toxicity of quetiapineQuinidine Increased risk of cardiotoxicity and arrhythmiasQuinidine barbiturate Increased risk of cardiotoxicity and arrhythmiasQuinupristin This combination presents an increased risk of toxicityRanolazine Increased levels of ranolazine - risk of toxicityRepaglinide This macrolide increases effect of repaglinideRifabutin The rifamycin decreases the effect of the macrolideRifampin The rifamycin decreases the effect of the macrolideRitonavir Increased toxicity of both agentsSertraline Possible serotoninergic syndrome with this combinationSibutramine Erythromycin increases the effect and toxicity of sibutramineSildenafil The macrolide increases the effect and toxicity of sildenafilSimvastatin The macrolide possibly increases the statin toxicitySirolimus The macrolide increases sirolimus levelsSotalol Increased risk of cardiotoxicity and arrhythmiasSparfloxacin Increased risk of cardiotoxicity and arrhythmiasTacrolimus Erythromycin increases the effect and toxicity of tacrolimusTerfenadine Increased risk of cardiotoxicity and arrhythmiasTheophylline The macrolide increases the effect and toxicity of theophyllineThioridazine Increased risk of cardiotoxicity and arrhythmiasVerapamil Increased risk of cardiotoxicity and arrhythmiasTriazolam The macrolide increases the effect of the benzodiazepineVardenafil The macrolide increases the effect and toxicity of vardenafilVinblastine Erythromycin increases vinblastine toxicityWarfarin The macrolide increases anticoagulant effectZafirlukast Erythromycin decreases the effect of zafirlukastErgonovine Possible ergotism and severe ischemia with this combinationEverolimus The macrolide increases everolimus levels/toxicityLincomycin Possible antagonism of action with this combinationAcenocoumarol The macrolide increases anticoagulant effect Pyridoxal¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available Riboflavin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Not Available
Calcium¿¡ ´ëÇÑ Description Á¤º¸ Calcium plays a vital role in the anatomy, physiology and biochemistry of organisms and of the cell, particularly in signal transduction pathways. The skeleton acts as a major mineral storage site for the element and releases Ca2+ ions into the bloodstream under controlled conditions. Circulating calcium is either in the free, ionized form or bound to blood proteins such as serum albumin. Although calcium flow to and from the bone is neutral, about 5 mmol is turned over a day. Bone serves as an important storage point for calcium, as it contains 99% of the total body calcium. Low calcium intake may also be a risk factor in the development of osteoporosis. The best-absorbed form of calcium from a pill is a calcium salt like carbonate or phosphate. Calcium gluconate and calcium lactate are absorbed well by pregnant women. Seniors absorb calcium lactate, gluconate and citrate better unless they take their calcium supplement with a full breakfast. Hydroxocobalamin¿¡ ´ëÇÑ Description Á¤º¸ Injectable form of vitamin B 12 that has been used therapeutically to treat vitamin B 12 deficiency. [PubChem] Nicotinamide¿¡ ´ëÇÑ Description Á¤º¸ An important compound functioning as a component of the coenzyme NAD. Its primary significance is in the prevention and/or cure of blacktongue and pellagra. Most animals cannot manufacture this compound in amounts sufficient to prevent nutritional deficiency and it therefore must be supplemented through dietary intake. [PubChem] Pyridoxal¿¡ ´ëÇÑ Description Á¤º¸ The 4-carboxyaldehyde form of vitamin B 6 which is converted to pyridoxal phosphate which is a coenzyme for synthesis of amino acids, neurotransmitters (serotonin, norepinephrine), sphingolipids, aminolevulinic acid. [PubChem] Riboflavin¿¡ ´ëÇÑ Description Á¤º¸ Nutritional factor found in milk, eggs, malted barley, liver, kidney, heart, and leafy vegetables. The richest natural source is yeast. It occurs in the free form only in the retina of the eye, in whey, and in urine; its principal forms in tissues and cells are as flavin mononucleotide and flavin-adenine dinucleotide. [PubChem]
Dosage Form
Calcium¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Capsule OralLiquid DentalLiquid IntravenousLiquid OralLiquid SublingualPaste DentalPowder OralPowder, for solution OralSolution IntramuscularSolution IntravenousSolution OralSolution / drops OralSyrup OralTablet OralTablet, chewable Oral Hydroxocobalamin¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Liquid IntramuscularSolution Oral Pyridoxal¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Not Available Riboflavin¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Not Available
Drug Category
Hydroxocobalamin¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anti-anemic AgentsHematinicsNutritional SupplementVitamin B Complex Nicotinamide¿¡ ´ëÇÑ Drug_Category Á¤º¸ Vitamin B Complex Pyridoxal¿¡ ´ëÇÑ Drug_Category Á¤º¸ Dietary supplementMicronutrientVitamin B ComplexVitamins (Vitamin B Complex) Riboflavin¿¡ ´ëÇÑ Drug_Category Á¤º¸ Photosensitizing AgentsRadiation-Sensitizing AgentsVitamin B ComplexVitamins (Vitamin B Complex)