Gentamicin에 대한 Mechanism_Of_Action 정보 Aminoglycosides like gentamicin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically gentamicin 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. Streptomycin에 대한 Mechanism_Of_Action 정보 Aminoglycosides like Streptomycin "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically Streptomycin 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.
Pharmacology
Gentamicin에 대한 Pharmacology 정보 Gentamicin is a broad spectrum 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. Streptomycin에 대한 Pharmacology 정보 Streptomycin 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.
Protein Binding
Gentamicin에 대한 단백결합 정보 Low (between 0 and 30%) Streptomycin에 대한 단백결합 정보 Not Available
Half-life
Gentamicin에 대한 반감기 정보 3-3½ hours in infants one week to six months of age; this increases to 5½ hours in full-term and large premature infants less than one week old. Streptomycin에 대한 반감기 정보 Not Available
Absorption
Gentamicin에 대한 Absorption 정보 Injections lead to peak serum concentrations in 30-60 minutes. Topical gentamicin is readily absorbed from large burned, denuded, or granulating areas but not through intact skin. Absorption of gentamicin is faster and greater with the cream compared to the ointment. Gentamicin is absorbed in small quantities following topical application to the eye. Gentamicin is also absorbed in small amounts following topical application to the ear (especially if the eardrum is perforated or if tissue damage is present). Streptomycin에 대한 Absorption 정보 Not Available
분포용적 : 부종이나 복수가 있거나 수액을 과다 투여했을 때 증가되고, 탈수시에 감소된다.
신생아 : 0.4-0.6 L/kg
소아 : 0.3-0.35 L/kg
성인 : 0.2-0.3 L/kg
표 1. 다양한 조직으로 분포된 정도 (혈액과의 비율 (%))
위치
분포 정도
눈
미미하다.
중추신경계
미미하다.(25% 이하)
흉막
우수하다
기관지 분비물
미미하다.
타액
어느정도 분포된다.(10-50%)
폐조직
우수하다.
복수
다양하다.(43-132%)
복막액
미미하다.
담즙
다양하다.(25-90%)
담도 패색시 답즙
미미하다.
활액
우수하다.
뼈
미미하다.
전립선
미미하다.
요
우수하다.
신장조직
우수하다.
뇌척수액으로의 분포는 뇌막에 염증이 있을 때도 미미하다.
뇌척수액 대 혈액의 농도비 (%)
정상 뇌막 : 0
염증성 뇌막 : 10-30
단백결합 : 30% 이하
반감기 :
신생아
1주 이하 : 3-11.5 시간
1주-6개월 : 3-3.5 시간
성인 :
1.5-3 시간
말기 신질환 : 36-70 시간
혈중최고농도 도달시간 :
근육주사 : 30-90 분 이내
정맥주사 : 30분 주입 후 30분 이내
소실 : 클리러런스는 환자의 신기능에 의존한다. 대부분이 사구체 여과를 통해 미변화체로 신배설
Biotransformation
Streptomycin에 대한 Biotransformation 정보 Not Available
Toxicity
Gentamicin에 대한 Toxicity 정보 Mouse, intravenous LD50: 52 mg/kg; rat, intravenous LD50: 96 mg/kg. Streptomycin에 대한 Toxicity 정보 LD50=430 mg/kg (Orally in rats with Streptomycin Sulfate); Side effect include nausea, vomiting, and vertigo, paresthesia of face, rash, fever, urticaria, angioneurotic edema, and eosinophilia.
Drug Interactions
Gentamicin에 대한 Drug_Interactions 정보 Atracurium The agent increases the effect of muscle relaxantDoxacurium The agent increases the effect of muscle relaxantGallamine Triethiodide The agent increases the effect of muscle relaxantMetocurine The agent increases the effect of muscle relaxantMivacurium The agent increases the effect of muscle relaxantPancuronium The agent increases the effect of muscle relaxantPipecuronium The agent increases the effect of muscle relaxantRocuronium The agent increases the effect of muscle relaxantSuccinylcholine The agent increases the effect of muscle relaxantTubocurarine The agent increases the effect of muscle relaxantVecuronium The agent increases the effect of muscle relaxantBumetanide Increased ototoxicityEthacrynic acid Increased ototoxicityFurosemide Increased ototoxicityTorasemide Increased ototoxicityThalidomide Thalidomide increases the renal toxicity of the aminoglycosideCisplatin Increased risk of nephrotoxicityCefradine Increased risk of nephrotoxicityCephapirin Increased risk of nephrotoxicityCefamandole Increased risk of nephrotoxicityCefazolin Increased risk of nephrotoxicityCefonicid Increased risk of nephrotoxicityCefoperazone Increased risk of nephrotoxicityCeforanide Increased risk of nephrotoxicityCefotaxime Increased risk of nephrotoxicityCefotetan Increased risk of nephrotoxicityCefoxitin Increased risk of nephrotoxicityCeftazidime Increased risk of nephrotoxicityCeftizoxime Increased risk of nephrotoxicityCeftriaxone Increased risk of nephrotoxicityCefuroxime Increased risk of nephrotoxicityCephalothin Group Increased risk of nephrotoxicity Streptomycin에 대한 Drug_Interactions 정보 Not Available
Gentamicin에 대한 Description 정보 A complex of three different closely related aminoglycoside sulfates, Gentamicins C1, C2, and C1(subA), obtained from Micromonospora purpurea and related species. They are broad-spectrum antibiotics, but may cause ear and kidney damage. They act to inhibit protein synthesis (genetic translation). [PubChem] Streptomycin에 대한 Description 정보 An antibiotic produced by the soil actinomycete Streptomyces griseus. It acts by inhibiting the initiation and elongation processes during protein synthesis. [PubChem]
Dosage Form
Gentamicin에 대한 Dosage_Form 정보 Cream TopicalLiquid OphthalmicOintment OphthalmicOintment TopicalSolution Auricular (otic)Solution IntravenousSolution OphthalmicSolution / drops Auricular (otic)Solution / drops Ophthalmic Streptomycin에 대한 Dosage_Form 정보 Powder, for solution Intramuscular
Drug Category
Gentamicin에 대한 Drug_Category 정보 Anti-Bacterial AgentsProtein Synthesis Inhibitors Streptomycin에 대한 Drug_Category 정보 AminoglycosidesAnti-Bacterial AgentsProtein Synthesis Inhibitors
Smiles String Canonical
Gentamicin에 대한 Smiles_String_canonical 정보 CNC(C)C1CCC(N)C(O1)OC1C(N)CC(N)C(OC2OCC(C)(O)C(NC)C2O)C1O Streptomycin에 대한 Smiles_String_canonical 정보 CNC1C(O)C(O)C(CO)OC1OC1C(OC(C)C1(O)C=O)OC1C(O)C(O)C(N=C(N)N)C(O)C1N=C(N)N
Smiles String Isomeric
Gentamicin에 대한 Smiles_String_isomeric 정보 CN[C@H](C)[C@@H]1CC[C@@H](N)[C@@H](O1)O[C@H]1[C@H](N)C[C@H](N)[C@@H](O[C@@H]2OC[C@@](C)(O)[C@H](NC)[C@H]2O)[C@@H]1O Streptomycin에 대한 Smiles_String_isomeric 정보 CN[C@H]1[C@H](O)[C@@H](O)[C@H](CO)O[C@H]1O[C@H]1[C@@H](O[C@@H](C)[C@]1(O)C=O)O[C@H]1[C@H](O)[C@@H](O)[C@H](\N=C(/N)N)[C@@H](O)[C@@H]1\N=C(\N)N
InChI Identifier
Gentamicin에 대한 InChI_Identifier 정보 InChI=1/C21H43N5O7/c1-9(25-3)13-6-5-10(22)19(31-13)32-16-11(23)7-12(24)17(14(16)27)33-20-15(28)18(26-4)21(2,29)8-30-20/h9-20,25-29H,5-8,22-24H2,1-4H3 Streptomycin에 대한 InChI_Identifier 정보 InChI=1/C21H39N7O12/c1-5-21(36,4-30)16(40-17-9(26-2)13(34)10(31)6(3-29)38-17)18(37-5)39-15-8(28-20(24)25)11(32)7(27-19(22)23)12(33)14(15)35/h4-18,26,29,31-36H,3H2,1-2H3,(H4,22,23,27)(H4,24,25,28)/t5-,6-,7+,8-,9-,10-,11+,12-,13-,14+,15+,16-,17-,18-,21+/m0/s1/f/h22-25H2
Chemical IUPAC Name
Gentamicin에 대한 Chemical_IUPAC_Name 정보 2-[4,6-diamino-3-[3-amino-6-(1-methylaminoethyl)oxan-2-yl]oxy-2-hydroxycyclohexyl]oxy-5-methyl-4-methylaminooxane-3,5-diol Streptomycin에 대한 Chemical_IUPAC_Name 정보 2-[(1S,2R,3R,4S,5R,6R)-5-(diaminomethylideneamino)-2-[(2R,3R,4R,5S)-3-[(2S,3S,4S,5R,6S)-4,5-dihydroxy-6-(hydroxymethyl)-3-methylaminooxan-2-yl]oxy-4-formyl-4-hydroxy-5-methyloxolan-2-yl]oxy-3,4,6-trihydroxycyclohexyl]guanidine
Drug-Induced Toxicity Related Proteins
GENTAMICIN 의 Drug-Induced Toxicity Related Protein정보 Replated Protein:Phospholipase A Drug:gentamicin Toxicity:aminoglycoside toxicity. [바로가기]Replated Protein:phospholipases C Drug:gentamicin Toxicity:aminoglycoside toxicity. [바로가기]Replated Protein:Angiotensinase A Drug:gentamicin Toxicity:important consequences upon renal function and metabolism. [바로가기]Replated Protein:Dipeptidylpeptidase IV Drug:gentamicin Toxicity:important consequences upon renal function and metabolism. [바로가기]Replated Protein:Sodium/potassium-transporting ATPase Drug:Gentamicin Toxicity:necrosis. [바로가기]
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