Cholecalciferol에 대한 Mechanism_Of_Action 정보 The first step involved in the activation of vitamin D3 is a 25-hydroxylation which is catalysed by the 25-hydroxylase in the liver and then by other enzymes. The mitochondrial sterol 27-hydroxylase catalyses the first reaction in the oxidation of the side chain of sterol intermediates. The active form of vitamin D3 (calcitriol) binds to intracellular receptors that then function as transcription factors to modulate gene expression. Like the receptors for other steroid hormones and thyroid hormones, the vitamin D receptor has hormone-binding and DNA-binding domains. The vitamin D receptor forms a complex with another intracellular receptor, the retinoid-X receptor, and that heterodimer is what binds to DNA. In most cases studied, the effect is to activate transcription, but situations are also known in which vitamin D suppresses transcription. Calcitriol increases the serum calcium concentrations by: increasing GI absorption of phosphorus and calcium, increasing osteoclastic resorption, and increasing distal renal tubular reabsorption of calcium. Calcitriol appears to promote intestinal absorption of calcium through binding to the vitamin D receptor in the mucosal cytoplasm of the intestine. Subsequently, calcium is absorbed through formation of a calcium-binding protein. calcium에 대한 Mechanism_Of_Action 정보 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. Pyridoxine에 대한 Mechanism_Of_Action 정보 Vitamin B6 is the collective term for a group of three related compounds, pyridoxine (PN), pyridoxal (PL) and pyridoxamine (PM), and their phosphorylated derivatives, pyridoxine 5'-phosphate (PNP), pyridoxal 5'-phosphate (PLP) and pyridoxamine 5'-phosphate (PMP). Although all six of these compounds should technically be referred to as vitamin B6, the term vitamin B6 is commonly used interchangeably with just one of them, pyridoxine. Vitamin B6, 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). Thiamine에 대한 Mechanism_Of_Action 정보 It is thought that the mechanism of action of thiamine on endothelial cells is related to a reduction in intracellular protein glycation by redirecting the glycolytic flux.
Pharmacology
Cholecalciferol에 대한 Pharmacology 정보 Cholecalciferol (vitamin D3) is a steroid hormone that has long been known for its important role in regulating body levels of calcium and phosphorus, in mineralization of bone, and for the assimilation of Vitamin A. The classical manifestations of vitamin D deficiency is rickets, which is seen in children and results in bony deformaties including bowed long bones. Deficiency in adults leads to the disease osteomalacia. Both rickets and osteomalacia reflect impaired mineralization of newly synthesized bone matrix, and usually result from a combination of inadequate exposure to sunlight and decreased dietary intake of vitamin D. Common causes of vitamin D deficiency include genetic defects in the vitamin D receptor, severe liver or kidney disease, and insufficient exposure to sunlight. Vitamin D plays an important role in maintaining calcium balance and in the regulation of parathyroid hormone (PTH). It promotes renal reabsorption of calcium, increases intestinal absorption of calcium and phosphorus, and increases calcium and phosphorus mobilization from bone to plasma. Pyridoxine에 대한 Pharmacology 정보 Vitamin B6 (pyridoxine) is a water-soluble vitamin used in the prophylaxis and treatment of vitamin B6 deficiency and peripheral neuropathy in those receiving isoniazid (isonicotinic acid hydrazide, INH). Vitamin B6 has been found to lower systolic and diastolic blood pressure in a small group of subjects with essential hypertension. Hypertension is another risk factor for atherosclerosis and coronary heart disease. Another study showed pyridoxine hydrochloride to inhibit ADP- or epinephrine-induced platelet aggregation and to lower total cholesterol levels and increase HDL-cholesterol levels, again in a small group of subjects. Vitamin B6, in the form of pyridoxal 5'-phosphate, was found to protect vascular endothelial cells in culture from injury by activated platelets. Endothelial injury and dysfunction are critical initiating events in the pathogenesis of atherosclerosis. Human studies have demonstrated that vitamin B6 deficiency affects cellular and humoral responses of the immune system. Vitamin B6 deficiency results in altered lymphocyte differentiation and maturation, reduced delayed-type hypersensitivity (DTH) responses, impaired antibody production, decreased lymphocyte proliferation and decreased interleukin (IL)-2 production, among other immunologic activities. Thiamine에 대한 Pharmacology 정보 Thiamine is a vitamin with antioxidant, erythropoietic, cognition-and mood-modulatory, antiatherosclerotic, putative ergogenic, and detoxification activities. Thiamine has been found to protect against lead-induced lipid peroxidation in rat liver and kidney. Thiamine deficiency results in selective neuronal death in animal models. The neuronal death is associated with increased free radical production, suggesting that oxidative stress may play an important early role in brain damage associated with thiamine deficiency. Thiamine plays a key role in intracellular glucose metabolism and it is thought that thiamine inhibits the effect of glucose and insulin on arterial smooth muscle cell proliferation. Inhibition of endothelial cell proliferation may also promote atherosclerosis. Endothelial cells in culture have been found to have a decreased proliferative rate and delayed migration in response to hyperglycemic conditions. Thiamine has been shown to inhibit this effect of glucose on endothelial cells.
Protein Binding
Cholecalciferol에 대한 단백결합 정보 50% to 80% Pyridoxine에 대한 단백결합 정보 22% Thiamine에 대한 단백결합 정보 90-94%
Half-life
Cholecalciferol에 대한 반감기 정보 Several weeks Pyridoxine에 대한 반감기 정보 15-20 days
Absorption
Cholecalciferol에 대한 Absorption 정보 Readily absorbed Pyridoxine에 대한 Absorption 정보 The B vitamins are readily absorbed from the gastrointestinal tract, except in malabsorption syndromes. Pyridoxine is absorbed mainly in the jejunum. Thiamine에 대한 Absorption 정보 Absorbed mainly from duodenum, by both active and passive processes
분포 : 흡수 후 chylomicrons을 통해 혈중으로 수송되며, 주로 간에 저장되고 기타 지방, 근육, 피부 및 골 조직 등에도 존재한다.
단백결합 : 주로 vitamin D-binding α-globulin에 결합하며 albumin과도 결합한다.
대사 : 간에서 vitamin D 25-hydroxylase에 의해 25-[OH] D로 대사된 후, 신장에서 vitamin D 1-hydroxylase에 의해 활성형인 1,25-[OH]2 D로 대사된다.
반감기 : vitamin D : 혈장 내에서 19-25 시간
소실 : 주로 담즙 및 대변을 통해 배설되며 소량은 뇨를 통해 배설된다.
Nicotinamide의 약물동력학자료
작용발현시간 : pellagra : 24시간
흡수 : 위장관으로부터 신속하게 흡수된다.
분포 :
모든 조직으로 신속하게 분포한다.
태아 및 신생아에서의 농도가 모체의 농도보다 높다.
대사 : 간대사
Nicotinamide는 생체 내에서 niacin의 대사로부터 형성될 수 있다.
Dietrich pathway를 통해 효소적으로 NAD 및 NADP로 전환된다.
반감기 : 45분
혈중최고농도 도달시간 : 20-70분
소실 : 용량의존적으로 미변화체 및 대사체로서 신배설된다. (생리적 용량에서는 소량만이 미변화체로 신배설되나 고용량 투여시 주로 미변화체로 신배설된다.)
Biotransformation
Cholecalciferol에 대한 Biotransformation 정보 Within the liver, cholecalciferal is hydroxylated to calcidiol (25-hydroxycholecalciferol) by the enzyme 25-hydroxylase. Within the kidney, calcidiol serves as a substrate for 1-alpha-hydroxylase, yielding calcitriol (1,25-dihydroxycholecalciferol), the biologically active form of vitamin D3. Thiamine에 대한 Biotransformation 정보 Hepatic
Toxicity
Cholecalciferol에 대한 Toxicity 정보 Hypercalcemia - Early symptoms of hypercalcemia, include nausea and vomiting, weakness, headache, somnolence, dry mouth, constipation, metallic taste, muscle pain and bone pain. Late symptoms and signs of hypercalcemia, include polyuria, polydipsia, anorexia, weight loss, nocturia, conjunctivitis, pancreatitis, photophobia, rhinorrhea, pruritis, hyperthermia, decreased libido, elevated BUN, albuminuria, hypercholesterolemia, elevated ALT (SGPT) and AST (SGOT), ectopic calcification, nephrocalcinosis, hypertension and cardiac arrhythmias. Pyridoxine에 대한 Toxicity 정보 Oral Rat LD50 = 4 gm/kg. Toxic effects include convulsions, dyspnea, hypermotility, diarrhea, ataxia and muscle weakness. Thiamine에 대한 Toxicity 정보 Thiamine toxicity is uncommon; as excesses are readily excreted, although long-term supplementation of amounts larger than 3 gram have been known to cause toxicity. Oral mouse LD50 = 8224 mg/kg, oral rat LD50 = 3710 mg/kg.
Drug Interactions
Cholecalciferol에 대한 Drug_Interactions 정보 Not Available calcium에 대한 Drug_Interactions 정보 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 Pyridoxine에 대한 Drug_Interactions 정보 Not Available Thiamine에 대한 Drug_Interactions 정보 Not Available
Cholecalciferol에 대한 Description 정보 Derivative of 7-dehydroxycholesterol formed by ultraviolet rays breaking of the C9-C10 bond. It differs from ergocalciferol in having a single bond between C22 and C23 and lacking a methyl group at C24. [PubChem] Nicotinamide에 대한 Description 정보 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] calcium에 대한 Description 정보 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. Pyridoxine에 대한 Description 정보 The 4-methanol 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. Although pyridoxine and Vitamin B 6 are still frequently used as synonyms, especially by medical researchers, this practice is erroneous and sometimes misleading (EE Snell; Ann NY Acad Sci, vol 585 pg 1, 1990). [PubChem] Thiamine에 대한 Description 정보 3-((4-Amino-2-methyl-5-pyrimidinyl)methyl)-5-(2- hydroxyethyl)-4-methylthiazolium chloride. [PubChem]
Dosage Form
Cholecalciferol에 대한 Dosage_Form 정보 Capsule OralTablet Oral calcium에 대한 Dosage_Form 정보 Capsule OralLiquid DentalLiquid IntravenousLiquid OralLiquid SublingualPaste DentalPowder OralPowder, for solution OralSolution IntramuscularSolution IntravenousSolution OralSolution / drops OralSyrup OralTablet OralTablet, chewable Oral Pyridoxine에 대한 Dosage_Form 정보 Liquid IntramuscularSolution IntramuscularSolution / drops OralTablet Oral Thiamine에 대한 Dosage_Form 정보 Liquid IntramuscularLiquid IntravenousSolution IntravenousTablet Oral
Drug Category
Cholecalciferol에 대한 Drug_Category 정보 Antihypocalcemic AgentsAntihypoparathyroid AgentsBone Density Conservation AgentsEssential VitaminVitaminsVitamins (Vitamin D) Nicotinamide에 대한 Drug_Category 정보 Vitamin B Complex Pyridoxine에 대한 Drug_Category 정보 Anti-inflammatory AgentsEssential VitaminVitamin B ComplexVitamins (Vitamin B Complex) Thiamine에 대한 Drug_Category 정보 Anti-inflammatory AgentsEssential VitaminVitamin B ComplexVitamins (Vitamin B Complex)
Smiles String Canonical
Cholecalciferol에 대한 Smiles_String_canonical 정보 CC(C)CCCC(C)C1CCC2C(CCCC12C)=CC=C1CC(O)CCC1=C Nicotinamide에 대한 Smiles_String_canonical 정보 NC(=O)C1=CC=CN=C1 calcium에 대한 Smiles_String_canonical 정보 Not Available Pyridoxine에 대한 Smiles_String_canonical 정보 CC1=NC=C(CO)C(CO)=C1O Thiamine에 대한 Smiles_String_canonical 정보 CC1=NC=C(C[N+]2=CSC(CCO)=C2C)C(N)=N1
Smiles String Isomeric
Cholecalciferol에 대한 Smiles_String_isomeric 정보 CC(C)CCC[C@@H](C)[C@H]1CC[C@@H]2[C@]1(C)CCC\C2=C/C=C1\C[C@@H](O)CCC1=C Nicotinamide에 대한 Smiles_String_isomeric 정보 NC(=O)C1=CC=CN=C1 calcium에 대한 Smiles_String_isomeric 정보 Not Available Pyridoxine에 대한 Smiles_String_isomeric 정보 CC1=NC=C(CO)C(CO)=C1O Thiamine에 대한 Smiles_String_isomeric 정보 CC1=NC=C(C[N+]2=CSC(CCO)=C2C)C(N)=N1
InChI Identifier
Cholecalciferol에 대한 InChI_Identifier 정보 InChI=1/C27H44O/c1-19(2)8-6-9-21(4)25-15-16-26-22(10-7-17-27(25,26)5)12-13-23-18-24(28)14-11-20(23)3/h12-13,19,21,24-26,28H,3,6-11,14-18H2,1-2,4-5H3/t21-,24+,25-,26+,27-/m1/s1 Nicotinamide에 대한 InChI_Identifier 정보 InChI=1/C6H6N2O/c7-6(9)5-2-1-3-8-4-5/h1-4H,(H2,7,9)/f/h7H2 calcium에 대한 InChI_Identifier 정보 Not Available Pyridoxine에 대한 InChI_Identifier 정보 InChI=1/C8H11NO3/c1-5-8(12)7(4-11)6(3-10)2-9-5/h2,10-12H,3-4H2,1H3 Thiamine에 대한 InChI_Identifier 정보 InChI=1/C12H17N4OS/c1-8-11(3-4-17)18-7-16(8)6-10-5-14-9(2)15-12(10)13/h5,7,17H,3-4,6H2,1-2H3,(H2,13,14,15)/q+1/f/h13H2
Chemical IUPAC Name
Cholecalciferol에 대한 Chemical_IUPAC_Name 정보 (1S)-3-[2-[(1R,3aS,7aR)-7a-methyl-1-[(2R)-6-methylheptan-2-yl]-2,3,3a,5,6,7-hexahydro-1H-inden-4-ylidene]ethylidene]-4-methylidenecyclohexan-1-ol Nicotinamide에 대한 Chemical_IUPAC_Name 정보 pyridine-3-carboxamide calcium에 대한 Chemical_IUPAC_Name 정보 Not Available Pyridoxine에 대한 Chemical_IUPAC_Name 정보 4,5-bis(hydroxymethyl)-2-methylpyridin-3-ol Thiamine에 대한 Chemical_IUPAC_Name 정보 2-[3-[(4-amino-2-methylpyrimidin-5-yl)methyl]-4-methyl-1,3-thiazol-3-ium-5-yl]ethanol
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