Neomycin에 대한 Mechanism_Of_Action 정보 Aminoglycosides like neomycin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically neomycin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes. Nystatin에 대한 Mechanism_Of_Action 정보 Nystatin interacts with 14-α demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol. This results in inhibition of ergosterol synthesis and increased fungal cellular permeability.
Pharmacology
Neomycin에 대한 Pharmacology 정보 Neomycin is an aminoglycoside antibiotic. Aminoglycosides work by binding to the bacterial 30S ribosomal subunit, causing misreading of t-RNA, leaving the bacterium unable to synthesize proteins vital to its growth. Aminoglycosides are useful primarily in infections involving aerobic, Gram-negative bacteria, such as Pseudomonas, Acinetobacter, and Enterobacter. In addition, some mycobacteria, including the bacteria that cause tuberculosis, are susceptible to aminoglycosides. Infections caused by Gram-positive bacteria can also be treated with aminoglycosides, but other types of antibiotics are more potent and less damaging to the host. In the past the aminoglycosides have been used in conjunction with penicillin-related antibiotics in streptococcal infections for their synergistic effects, particularly in endocarditis. Aminoglycosides are mostly ineffective against anaerobic bacteria, fungi and viruses. Nystatin에 대한 Pharmacology 정보 Nystatin is an antibiotic which is both fungistatic and fungicidal in vitro against a wide variety of yeasts and yeast-like fungi, including Candida albicans, C. parapsilosis, C. tropicalis, C. guilliermondi, C. pseudotropicalis, C. krusei, Torulopsis glabrata, Tricophyton rubrum, T. mentagrophytes. Nystatin acts by binding to sterols in the cell membrane of susceptible species resulting in a change in membrane permeability and the subsequent leakage of intracellular components. On repeated subculturing with increasing levels of nystatin, Candida albicans does not develop resistance to nystatin. Generally, resistance to nystatin does not develop during therapy. However, other species of Candida (C. tropicalis, C. guilliermondi, C. krusei, and C. stellatoides) become quite resistant on treatment with nystatin and simultaneously become cross resistant to amphotericin as well. This resistance is lost when the antibiotic is removed. Nystatin exhibits no appreciable activity against bacteria, protozoa, or viruses.
Metabolism
Neomycin에 대한 Metabolism 정보 # Phase_1_Metabolizing_Enzyme:Not Available Nystatin에 대한 Metabolism 정보 # Phase_1_Metabolizing_Enzyme:Cytochrome P450 3A4 (CYP3A4)
Protein Binding
Neomycin에 대한 단백결합 정보 Protein binding studies have shown that the degree of aminoglycoside protein binding is low and, depending upon the methods used for testing, may be between 0% and 30%.
Half-life
Neomycin에 대한 반감기 정보 2 to 3 hours Nystatin에 대한 반감기 정보 Not Available
Absorption
Neomycin에 대한 Absorption 정보 Poorly absorbed from the normal gastrointestinal tract. Although only approximately 3% of neomycin is absorbed through intact intestinal mucosa, significant amounts may be absorbed through ulcerated or denuded mucosa or if inflammation is present. Nystatin에 대한 Absorption 정보 Nystatin is not absorbed from intact skin or mucous membrane
Pharmacokinetics
Nystatin의 약물동력학자료
작용발현시간 : 칸디다증의 증상 완화 : 24-72 시간
흡수 :
점막이나 정상 피부를 통해서는 흡수되지 않는다.
위장관에서 거의 흡수되지 않는다.
소실 : 미변화체로 변배설
Polymyxin B Sulfate의 약물동력학자료
흡수 :
복막에서 잘 흡수된다.
위장관(신생아 제외), 점막, 피부에서는 잘 흡수되지 않는다.
분포 :
뇌척수액으로의 분포는 미미하다.
태반통과
반감기 : 4.5-6 시간, 신기능 저하시 연장된다.
혈중최고농도 도달시간 : IM : 2시간 이내
소실 : 사구체 여과를 통해 60% 이상이 미변화체로 신배설된다.
Neomycin Sulfate의 약물동력학자료
흡수 : 경구, 경피 : 흡수되는 양이 미미하다. (3%)
분포 : 분포용적 : 0.36 L/kg
대사 : 소량이 간에서 대사된다.
반감기 : 3 시간 (나이와 신기능에 의존)
혈중최고농도 도달시간 :
경구 : 1-4 시간
근육주사 : 2 시간 이내
소실 :
주사제 : 신배설 (30-50%가 미변화체로 배설)
경구 : 97%가 미변화체로 변배설
Biotransformation
Neomycin에 대한 Biotransformation 정보 Neomycin undergoes negligible biotransformation after parenteral administration.
Toxicity
Neomycin에 대한 Toxicity 정보 LD50 = 200 mg/kg (rat). Because of low absorption, it is unlikely that acute overdosage would occur with oral neomycin. However, prolonged administration could result in sufficient systemic drug levels to produce neurotoxicity, ototoxicity and/or nephrotoxicity. Nystatin에 대한 Toxicity 정보 Not Available
Drug Interactions
Neomycin에 대한 Drug_Interactions 정보 Not Available Nystatin에 대한 Drug_Interactions 정보 Not Available
Neomycin에 대한 Description 정보 A component of neomycin that is produced by Streptomyces fradiae. On hydrolysis it yields neamine and neobiosamine B. (From Merck Index, 11th ed) Nystatin에 대한 Description 정보 Nystatin is a polyene antifungal drug to which many molds and yeasts are sensitive, including Candida spp. Nystatin has some toxicity associated with it when given intravenously, but it is not absorbed across intact skin or mucous membranes. It is considered a relatively safe drug for treating oral or gastrointestinal fungal infections.
Drug Category
Neomycin에 대한 Drug_Category 정보 Anti-Bacterial AgentsAntibiotics Nystatin에 대한 Drug_Category 정보 Anti-Bacterial AgentsAntifungal AgentsIonophores
Smiles String Canonical
Neomycin에 대한 Smiles_String_canonical 정보 NCC1OC(OC2C(N)CC(N)C(O)C2OC2OC(CO)C(OC3OC(CN)C(O)C(O)C3N)C2O)C(N)C(O)C1O Nystatin에 대한 Smiles_String_canonical 정보 CC1OC(=O)CC(O)CC(O)CC(O)CCC(O)C(O)CC(=O)CC(O)C(C(O)CC(OC2OC(C)C(O)C(N)C2O)C=CC=CC=CC=CCCC=CC=CC(C)C(O)C1C)C(O)=O
Smiles String Isomeric
Neomycin에 대한 Smiles_String_isomeric 정보 NC[C@H]1O[C@H](O[C@@H]2[C@@H](N)C[C@@H](N)[C@H](O)[C@H]2O[C@@H]2O[C@H](CO)[C@@H](O[C@H]3O[C@@H](CN)[C@@H](O)[C@H](O)[C@H]3N)[C@H]2O)[C@H](N)[C@@H](O)[C@@H]1O Nystatin에 대한 Smiles_String_isomeric 정보 C[C@H]1OC(=O)C[C@H](O)C[C@H](O)C[C@H](O)CC[C@H](O)[C@@H](O)CC(=O)C[C@@H](O)[C@@H]([C@@H](O)C[C@H](O[C@@H]2O[C@H](C)[C@@H](O)[C@H](N)[C@@H]2O)\C=C\C=C\C=C\C=C\CC\C=C\C=C\[C@H](C)[C@H](O)[C@H]1C)C(O)=O
InChI Identifier
Neomycin에 대한 InChI_Identifier 정보 InChI=1/C23H46N6O13/c24-2-7-13(32)15(34)10(28)21(37-7)40-18-6(27)1-5(26)12(31)20(18)42-23-17(36)19(9(4-30)39-23)41-22-11(29)16(35)14(33)8(3-25)38-22/h5-23,30-36H,1-4,24-29H2/t5-,6+,7-,8+,9-,10-,11-,12+,13-,14-,15-,16-,17-,18-,19-,20-,21-,22-,23+/m1/s1 Nystatin에 대한 InChI_Identifier 정보 InChI=1/C47H75NO17/c1-27-17-15-13-11-9-7-5-6-8-10-12-14-16-18-35(65-47-45(60)42(48)44(59)30(4)64-47)26-39(56)41(46(61)62)38(55)24-34(52)23-37(54)36(53)20-19-31(49)21-32(50)22-33(51)25-40(57)63-29(3)28(2)43(27)58/h5-6,8,10-18,27-33,35-39,41-45,47,49-51,53-56,58-60H,7,9,19-26,48H2,1-4H3,(H,61,62)/b6-5+,10-8+,13-11+,14-12+,17-15+,18-16+/t27?,28?,29?,30-,31?,32?,33?,35?,36?,37?,38?,39?,41?,42+,43?,44-,45+,47?/m1/s1/f/h61H
Chemical IUPAC Name
Neomycin에 대한 Chemical_IUPAC_Name 정보 (2R,3S,4R,5R,6R)-5-amino-2-(aminomethyl)-6-[(1R,2R,3S,4R,6S)-4,6-diamino-2-[(2S,3R,4S,5R)-4-[(2R,3R,4R,5S,6S)-3-amino-6-(aminomethyl)-4,5-dihydroxyoxan-2-yl]oxy-3-hydroxy-5-(hydroxymethyl)oxolan-2-yl]oxy-3-hydroxycyclohexyl]oxyoxane-3,4-diol Nystatin에 대한 Chemical_IUPAC_Name 정보 (21E,23E,25E,27E,31E,33E)-20-[(3S,4S,5S,6R)-4-amino-3,5-dihydroxy-6-methyloxan-2-yl]oxy-4,6,8,11,12,16,18,36-octahydroxy-35,37,38-trimethyl-2,14-dioxo-1-oxacyclooctatriaconta-21,23,25,27,31,33-hexaene-17-carboxylic acid
Drug-Induced Toxicity Related Proteins
NEOMYCIN 의 Drug-Induced Toxicity Related Protein정보 Replated Protein:NMDA receptor-regulated protein Drug:neomycin Toxicity:excitotoxic activation. [바로가기]
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