Acetaminophen에 대한 Mechanism_Of_Action 정보 Acetaminophen is thought to act primarily in the CNS, increasing the pain threshold by inhibiting both isoforms of cyclooxygenase, COX-1 and COX-2, enzymes involved in prostaglandin (PG) synthesis. Unlike NSAIDs, acetaminophen does not inhibit cyclooxygenase in peripheral tissues and, thus, has no peripheral anti-inflammatory affects. While aspirin acts as an irreversible inhibitor of COX and directly blocks the enzyme's active site, studies have found that acetaminophen indirectly blocks COX, and that this blockade is ineffective in the presence of peroxides. This might explain why acetaminophen is effective in the central nervous system and in endothelial cells but not in platelets and immune cells which have high levels of peroxides. Studies also report data suggesting that acetaminophen selectively blocks a variant of the COX enzyme that is different from the known variants COX-1 and COX-2. This enzyme is now referred to as COX-3. Its exact mechanism of action is still poorly understood, but future research may provide further insight into how it works. Cyanocobalamin에 대한 Mechanism_Of_Action 정보 Vitamin B12 is used in the body in two forms: Methylcobalamin and 5-deoxyadenosyl cobalamin. The enzyme 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. 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
Acetaminophen에 대한 Pharmacology 정보 Acetaminophen (USAN) or Paracetamol (INN) is a popular analgesic and antipyretic drug that is used for the relief of fever, headaches, and other minor aches and pains. It is a major ingredient in numerous cold and flu medications and many prescription analgesics. It is extremely safe in standard doses, but because of its wide availability, deliberate or accidental overdoses are not uncommon. Acetaminophen, unlike other common analgesics such as aspirin and ibuprofen, has no anti-inflammatory properties or effects on platelet function, and so it is not a member of the class of drugs known as non-steroidal anti-inflammatory drugs or NSAIDs. In normal doses acetaminophen does not irritate the lining of the stomach nor affect blood coagulation, the kidneys, or the fetal ductus arteriosus (as NSAIDs can). Like NSAIDs and unlike opioid analgesics, acetaminophen does not cause euphoria or alter mood in any way. Acetaminophen and NSAIDs have the benefit of being completely free of problems with addiction, dependence, tolerance and withdrawal. Acetaminophen is used on its own or in combination with pseudoephedrine, dextromethorphan, chlorpheniramine, diphenhydramine, doxylamine, codeine, hydrocodone, or oxycodone. Cyanocobalamin에 대한 Pharmacology 정보 Cyanocobalamin (Vitamin B12) is a water-soluble organometallic compound with a trivalent cobalt ion bound inside a corrin ring. It is needed for nerve cells and red blood cells, and to make DNA. Vitamin B12 deficiency is the cause of several forms of anemia. 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.
Metabolism
Acetaminophen에 대한 Metabolism 정보 # Phase_1_Metabolizing_Enzyme:Cytochrome P450 1A2 (CYP1A2)Cytochrome P450 2E1 (CYP2E1) Cyanocobalamin에 대한 Metabolism 정보 # Phase_1_Metabolizing_Enzyme:Methylenetetrahydrofolate reductase Pyridoxine에 대한 Metabolism 정보 # Phase_1_Metabolizing_Enzyme:Methylenetetrahydrofolate reductase
Protein Binding
Cyanocobalamin에 대한 단백결합 정보 Very high (to specific plasma proteins called transcobalamins); binding of hydroxocobalamin is slightly higher than cyanocobalamin. Pyridoxine에 대한 단백결합 정보 22% Thiamine에 대한 단백결합 정보 90-94%
Half-life
Acetaminophen에 대한 반감기 정보 1 to 4 hours Cyanocobalamin에 대한 반감기 정보 Approximately 6 days (400 days in the liver). Pyridoxine에 대한 반감기 정보 15-20 days
Absorption
Acetaminophen에 대한 Absorption 정보 Rapid and almost complete Cyanocobalamin에 대한 Absorption 정보 Readily absorbed in the lower half of the ileum. 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
Pharmacokinetics
Acetaminophen의 약물동력학자료
단백결합 : 20-50%
대사 :
상용량에서 : 간에서 sulfate와 glucuronide 포합체로 대사되며, 소량은 microsomal mixed function oxidases에 의해 반응성이 매우 높은 중간대사체(acetylimidoquinone)로 대사된 후 glutathione 포합으로 비활성화된다.
중독량에서 (4g을 단 하루 복용한 정도까지도 포함된다) : glutathione 포합이 점점 불충분하게 되어 acetylimidoquinone 농도가 증가하게 되며 이것이 간세포 괴사를 유발하는 것으로 여겨지고 있다.
Vitamin B12를 투여받는 경우 : 0.1-1 mg 근육주사 또는 정맥주사 후 48시간 이내에 50-90%가 신배설된다.
Thiamine nitrate의 약물동력학자료
흡수 :
경구 : 최대흡수량 : 8-15 mg/day
근육주사 : 신속하고 완전하게 흡수된다.
분포 : 최소요구량 (약 1 mg/day)을 초과 섭취시 조직 저장에 포화가 나타난다.
소실 : 과잉 섭취된 양은 뇨를 통해 배설된다.
Biotransformation
Acetaminophen에 대한 Biotransformation 정보 Approximately 90 to 95% of a dose is metabolized in the liver via the cytochrome P450 enzyme pathways (primarily by conjugation with glucuronic acid, sulfuric acid, and cysteine). An intermediate metabolite is hepatotoxic and most likely nephrotoxic and can accumulate after the primary metabolic pathways have been saturated. Cyanocobalamin에 대한 Biotransformation 정보 Hepatic Thiamine에 대한 Biotransformation 정보 Hepatic
Toxicity
Acetaminophen에 대한 Toxicity 정보 Oral, mouse: LD50 = 338 mg/kg; Oral, rat: LD50 = 1944 mg/kg. Acetaminophen is metabolized primarily in the liver, where most of it is converted to inactive compounds by conjugation with sulfate and glucuronide, and then excreted by the kidneys. Only a small portion is metabolized via the hepatic cytochrome P450 enzyme system. The toxic effects of acetaminophen are due to a minor alkylating metabolite (N-acetyl-p-benzo-quinone imine), not acetaminophen itself nor any of the major metabolites. This toxic metabolite reacts with sulfhydryl groups. At usual doses, it is quickly detoxified by combining irreversibly with the sulfhydryl group of glutathione to produce a non-toxic conjugate that is eventually excreted by the kidneys. The toxic dose of paracetamol is highly variable. In adults, single doses above 10 grams or 140 mg/kg have a reasonable likelihood of causing toxicity. In adults, single doses of more than 25 grams have a high risk of lethality. Cyanocobalamin에 대한 Toxicity 정보 Anaphylactic reaction (skin rash, itching, wheezing)-after parenteral administration. ORL-MUS LD50 > 8000 mg/kg 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
Acetaminophen에 대한 Drug_Interactions 정보 Anisindione Acetaminophen increases the anticoagulant effectWarfarin Acetaminophen increases the anticoagulant effectImatinib Increased hepatic toxicity of both agentsIsoniazid Risk of hepatotoxicityDicumarol Acetaminophen increases the anticoagulant effectDicumarol Increases the anticoagulant effectAcenocoumarol Increases the anticoagulant effect Cyanocobalamin에 대한 Drug_Interactions 정보 Not Available Pyridoxine에 대한 Drug_Interactions 정보 Not Available Thiamine에 대한 Drug_Interactions 정보 Not Available
Acetaminophen에 대한 Description 정보 Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage. [PubChem] Cyanocobalamin에 대한 Description 정보 Cyanocobalamin (commonly known as Vitamin B12) is the most chemically complex of all the vitamins. Cyanocobalamin's structure is based on a corrin ring, which, although similar to the porphyrin ring found in heme, chlorophyll, and cytochrome, has two of the pyrrole rings directly bonded. The central metal ion is Co (cobalt). Cyanocobalamin cannot be made by plants or by animals, as the only type of organisms that have the enzymes required for the synthesis of cyanocobalamin are bacteria and archaea. Higher plants do not concentrate cyanocobalamin from the soil and so are a poor source of the substance as compared with animal tissues. Cyanocobalamin is naturally found in foods including meat (especially liver and shellfish), eggs, and milk products. [HMDB] 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
Acetaminophen에 대한 Dosage_Form 정보 Capsule OralElixir OralLiquid OralSolution OralSolution / drops OralSuppository RectalSuspension OralSyrup OralTablet OralTablet, effervescent OralTablet, extended release Oral Cyanocobalamin에 대한 Dosage_Form 정보 Capsule OralLiquid IntramuscularLiquid OralPowder OralSolution IntramuscularTablet OralTablet, extended release Oral Pyridoxine에 대한 Dosage_Form 정보 Liquid IntramuscularSolution IntramuscularSolution / drops OralTablet Oral Thiamine에 대한 Dosage_Form 정보 Liquid IntramuscularLiquid IntravenousSolution IntravenousTablet Oral
Drug Category
Acetaminophen에 대한 Drug_Category 정보 Analgesics, Non-NarcoticAntipyretics Cyanocobalamin에 대한 Drug_Category 정보 Antianemic AgentsEssential VitaminVitamins (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
Acetaminophen에 대한 Smiles_String_canonical 정보 CC(=O)NC1=CC=C(O)C=C1 Cyanocobalamin에 대한 Smiles_String_canonical 정보 [Co+3].[C-] 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
Acetaminophen에 대한 Smiles_String_isomeric 정보 CC(=O)NC1=CC=C(O)C=C1 Cyanocobalamin에 대한 Smiles_String_isomeric 정보 [Co+3].[C-] 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
Acetaminophen에 대한 InChI_Identifier 정보 InChI=1/C8H9NO2/c1-6(10)9-7-2-4-8(11)5-3-7/h2-5,11H,1H3,(H,9,10)/f/h9H Cyanocobalamin에 대한 InChI_Identifier 정보 InChI=1/C62H90N13O14P.CN.Co/c1-29-20-39-40(21-30(29)2)75(28-70-39)57-52(84)53(41(27-76)87-57)89-90(85,86)88-31(3)26-69-49(83)18-19-59(8)37(22-46(66)80)56-62(11)61(10,25-48(68)82)36(14-17-45(65)79)51(74-62)33(5)55-60(9,24-47(67)81)34(12-15-43(63)77)38(71-55)23-42-58(6,7)35(13-16-44(64)78)50(72-42)32(4)54(59)73-56;1-2;/h20-21,23,28,31,34-37,41,52-53,56-57,76,84H,12-19,22,24-27H2,1-11H3,(H15,63,64,65,66,67,68,69,71,72,73,74,77,78,79,80,81,82,83,85,86);;/q;-1;+3/p-1/t31?,34-,35-,36-,37+,41+,52?,53?,56?,57+,59-,60+,61+,62+;;/m1../s1/fC62H89N13O14P.CN.Co/h69,85H,63-68H2;;/q-1;2m/b42-23-,54-32-,55-33-;; 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
Acetaminophen에 대한 Chemical_IUPAC_Name 정보 N-(4-hydroxyphenyl)acetamide Cyanocobalamin에 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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