Procaine에 대한 Mechanism_Of_Action 정보 Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex. 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). Riboflavin에 대한 Mechanism_Of_Action 정보 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. 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
Procaine에 대한 Pharmacology 정보 Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It is metabolized in the plasma by the enzyme pseudocholinesterase through hydrolysis into para-aminobenzoic acid (PABA), which is then excreted by the kidneys into the urine. 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. Riboflavin에 대한 Pharmacology 정보 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. 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
Pyridoxine에 대한 Metabolism 정보 # Phase_1_Metabolizing_Enzyme:Methylenetetrahydrofolate reductase Riboflavin에 대한 Metabolism 정보 # Phase_1_Metabolizing_Enzyme:Monoamine oxidase type A (MAO-A)Methylenetetrahydrofolate reductase
Protein Binding
Procaine에 대한 단백결합 정보 Not Available Pyridoxine에 대한 단백결합 정보 22% Riboflavin에 대한 단백결합 정보 60% Thiamine에 대한 단백결합 정보 90-94%
Half-life
Procaine에 대한 반감기 정보 7.7 minutes Pyridoxine에 대한 반감기 정보 15-20 days Riboflavin에 대한 반감기 정보 66-84 minutes
Absorption
Procaine에 대한 Absorption 정보 Not Available 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. Riboflavin에 대한 Absorption 정보 Vitamin B2 is readily absorbed from the upper gastrointestinal tract. Thiamine에 대한 Absorption 정보 Absorbed mainly from duodenum, by both active and passive processes
대사 : 혈장 효소에 의해 p-aminobenzoic acid, diethylaminoethanol로 빠르게 가수분해됨. 배설되기 전에 80%는 포합됨
반감기 : 7.7분
소실 : 대사체 및 일부 미변화체로 신배설
Garlic oil의 약물동력학자료
작용 발현 시간 :
초기 반응 : 항혈소판 응집 효과 : 경구 : 2-4 시간
고혈압 : 경구 : 5시간
고콜레스테롤혈증 : 1개월
작용 지속 시간 : 고혈압 : 14시간
Retinol Palmitate의 약물동력학자료
흡수 :
Retinol은 소장에서 흡수되며 retinoic acid는 문맥을 통해 전신적으로 흡수된다.
생리적 보충량의 용량 이하에서는 잘 흡수된다.
유화 제제보다 수용성 제제가 보다 신속하게 흡수된다.
고용량, 지질 흡수장애, 저단백식이, 간질환, 췌장 질환에서는 흡수가 저하된다.
림프의 chylomicrons에 의해 간으로 수송된다.
분포 :
간에 고농도로 저장된다. (약 2년 동안의 요구량이 간에 저장됨)
유즙 분비
RBP (retinol-binding protein)에 결합된 retinol의 형태로 간으로부터 운반된다.
대사 : glucuronide 포합, 장간순환
소실 : 담즙을 통해 대변으로 배설된다.
Tocopherol의 약물동력학자료
흡수 : 경구 :
소장으로부터 흡수되는 데에는 담즙이 필요하다.
흡수 저하 : 흡수장애 환자, 저체중 미숙아, 고용량 투여
유화제제보다 수용성 제제가 더 잘 흡수된다.
분포 : 모든 조직에 분포하며, 특히 지방조직에 고농도로 분포하고 저장된다.
대사 : 간에서 glucuronides 포합
소실 : 주로 담즙을 통해 (70-80%) 배설된다.
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.
Riboflavin의 약물동력학자료
흡수 :
위장관으로부터 잘 흡수된다.
음식물에 의해 흡수양이 증가한다.
간염, 간경화, 담관폐색이 있는 환자에서 흡수가 감소한다.
분포 : 체내 모든 조직에 널리 분포한다.
반감기 :
초기 상 : 1.4 시간
말기 상 : 14시간
소실 : 미변화체로 신배설되는 양은 약 9%이다.
Biotransformation
Procaine에 대한 Biotransformation 정보 Hydrolysis by plasma esterases to PABA Riboflavin에 대한 Biotransformation 정보 Hepatic. Thiamine에 대한 Biotransformation 정보 Hepatic
Toxicity
Procaine에 대한 Toxicity 정보 Not Available Pyridoxine에 대한 Toxicity 정보 Oral Rat LD50 = 4 gm/kg. Toxic effects include convulsions, dyspnea, hypermotility, diarrhea, ataxia and muscle weakness. Riboflavin에 대한 Toxicity 정보 Not Available 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
Procaine에 대한 Drug_Interactions 정보 Aluminium Formation of non-absorbable complexesBismuth Formation of non-absorbable complexesCalcium Formation of non-absorbable complexesDihydroxyaluminium Formation of non-absorbable complexesEstramustine Increases the levels of estramustineMagnesium oxide Formation of non-absorbable complexesMagnesium Formation of non-absorbable complexesSucralfate Formation of non-absorbable complexesIron Formation of non-absorbable complexes Pyridoxine에 대한 Drug_Interactions 정보 Not Available Riboflavin에 대한 Drug_Interactions 정보 Not Available Thiamine에 대한 Drug_Interactions 정보 Not Available
Procaine에 대한 Description 정보 A local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016). [PubChem] 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] Riboflavin에 대한 Description 정보 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] Thiamine에 대한 Description 정보 3-((4-Amino-2-methyl-5-pyrimidinyl)methyl)-5-(2- hydroxyethyl)-4-methylthiazolium chloride. [PubChem]
Dosage Form
Procaine에 대한 Dosage_Form 정보 Capsule OralSolution InfiltrationSolution IntramuscularTablet, extended release Oral Pyridoxine에 대한 Dosage_Form 정보 Liquid IntramuscularSolution IntramuscularSolution / drops OralTablet Oral Riboflavin에 대한 Dosage_Form 정보 Not Available Thiamine에 대한 Dosage_Form 정보 Liquid IntramuscularLiquid IntravenousSolution IntravenousTablet Oral
Drug Category
Procaine에 대한 Drug_Category 정보 AnestheticsAnesthetics, LocalLocal Anesthetics Pyridoxine에 대한 Drug_Category 정보 Anti-inflammatory AgentsEssential VitaminVitamin B ComplexVitamins (Vitamin B Complex) Riboflavin에 대한 Drug_Category 정보 Photosensitizing AgentsRadiation-Sensitizing AgentsVitamin B ComplexVitamins (Vitamin B Complex) Thiamine에 대한 Drug_Category 정보 Anti-inflammatory AgentsEssential VitaminVitamin B ComplexVitamins (Vitamin B Complex)
Smiles String Canonical
Procaine에 대한 Smiles_String_canonical 정보 CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 Pyridoxine에 대한 Smiles_String_canonical 정보 CC1=NC=C(CO)C(CO)=C1O Riboflavin에 대한 Smiles_String_canonical 정보 CC1=CC2=C(C=C1C)N(CC(O)C(O)C(O)CO)C1=NC(=O)NC(=O)C1=N2 Thiamine에 대한 Smiles_String_canonical 정보 CC1=NC=C(C[N+]2=CSC(CCO)=C2C)C(N)=N1
Smiles String Isomeric
Procaine에 대한 Smiles_String_isomeric 정보 CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 Pyridoxine에 대한 Smiles_String_isomeric 정보 CC1=NC=C(CO)C(CO)=C1O Riboflavin에 대한 Smiles_String_isomeric 정보 CC1=CC2=C(C=C1C)N(C[C@@H](O)[C@@H](O)[C@@H](O)CO)C1=NC(=O)NC(=O)C1=N2 Thiamine에 대한 Smiles_String_isomeric 정보 CC1=NC=C(C[N+]2=CSC(CCO)=C2C)C(N)=N1
InChI Identifier
Procaine에 대한 InChI_Identifier 정보 InChI=1/C13H20N2O2/c1-3-15(4-2)9-10-17-13(16)11-5-7-12(14)8-6-11/h5-8H,3-4,9-10,14H2,1-2H3 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 Riboflavin에 대한 InChI_Identifier 정보 InChI=1/C17H20N4O6/c1-7-3-9-10(4-8(7)2)21(5-11(23)14(25)12(24)6-22)15-13(18-9)16(26)20-17(27)19-15/h3-4,11-12,14,22-25H,5-6H2,1-2H3,(H,20,26,27)/t11-,12+,14-/m1/s1/f/h20H 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
Procaine에 대한 Chemical_IUPAC_Name 정보 2-diethylaminoethyl 4-aminobenzoate Pyridoxine에 대한 Chemical_IUPAC_Name 정보 4,5-bis(hydroxymethyl)-2-methylpyridin-3-ol Riboflavin에 대한 Chemical_IUPAC_Name 정보 7,8-dimethyl-10-[(2R,3R,4S)-2,3,4,5-tetrahydroxypentyl]benzo[g]pteridine-2,4-dione 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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최근정보수정일 2025-10-13
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