奈替米星
奈替米星用途
为氨基糖苷类抗生素西梭霉素的衍生物。抗菌谱和庆大霉素、妥布霉素、西梭霉素、丁胺卡那霉素相似，但对金黄色葡萄球菌、肠道细菌更为有效，抑制绿脓杆菌、普罗威斯登菌则稍差。其最大的优点是对听觉神经及肾脏的毒性比临床常用的氨基糖苷类抗生素为小，对耐庆大霉素的肠道细菌及绿脓杆菌有高效。用于呼吸系统感染、皮肤软组织感染、泌尿系统感染、创面感染、骨关节感染、产后感染、胃肠道及胆道感染、败血症等。
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奈替米星作用
本品属半合成氨基糖甙类抗生素，其抗菌谱广，对大肠肝菌、克霉伯菌属、肠肝菌属、沙雷菌属、枸橼酸杆菌属、变形杆菌属、沙门菌属、志贺菌属、嗜血质流感杆菌等具有高度抗菌活性；对缘脓杆菌等假单胞菌、普鲁威登菌和不动杆菌属等的某些菌株亦具有抗菌活性；对葡萄球菌属，包括甲氧西林敏感菌株和部分甲氧西林耐药菌株也具抗菌作用，对肺炎球菌、溶血性链球菌、粪肠球菌的抗菌作用较差。性状：本品为无色或几乎无色的澄明液体。
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奈替米星名称
[ CAS 号 ]:
56391-56-1
[ 中文名 ]:
奈替米星
[ 英文名 ]:
NETILMICIN
[中文别名 ]:
[英文别名 ]:
- certomycin
- ntromycin
- netillin
- 1-N-ethylsisomicin
- ntl
- NETILMICIN
- vectacin
- nettacin
- netroymcin
- ntromicine
奈替米星物理化学性质
[ 密度 ]:
1.32g/cm3
[ 沸点 ]:
684.3ºC at 760mmHg
[ 分子式 ]:
C21H41N5O7
[ 分子量 ]:
475.58000
[ 闪点 ]:
367.7ºC
[ 精确质量 ]:
475.30100
[ PSA ]:
199.73000
[ 折射率 ]:
1.597
奈替米星毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- WK2285000
- CHEMICAL NAME :
- D-Streptamine, O-3-deoxy-4-C-methyl-3-(methylamino)-beta-L-arabinopy ranosyl(1-6)-O-(2,6- diamino-2,3,4,6-tetradeoxy-alpha-D-glycero-hex-4-enop yranosyl(1-4))-2-deox y-N(sup 1)-ethyl-
- CAS REGISTRY NUMBER :
- 56391-56-1
- LAST UPDATED :
- 199612
- DATA ITEMS CITED :
- 17
- MOLECULAR FORMULA :
- C21-H41-N5-O7
- MOLECULAR WEIGHT :
- 475.67
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Human
- DOSE/DURATION :
- 52 mg/kg/7D-C
- TOXIC EFFECTS :
- Kidney, Ureter, Bladder - other changes
- REFERENCE :
- CMAJAX Canadian Medical Association Journal. (Canadian Medical Assoc., POB 8650, Ottawa, ON K1G 0G8, Canada) V.1- 1911- Volume(issue)/page/year: 120,161,1979
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 25200 ug/kg
- TOXIC EFFECTS :
- Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Blood - hemorrhage
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,816,1981
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 40 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 29,543,1986
- TYPE OF TEST :
- LDLo - Lowest published lethal dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 500 mg/kg
- TOXIC EFFECTS :
- Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Blood - hemorrhage
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,816,1981
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intramuscular
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 125 mg/kg
- TOXIC EFFECTS :
- Brain and Coverings - changes in circulation (hemorrhage, thrombosis, etc.) Lungs, Thorax, or Respiration - chronic pulmonary edema Blood - hemorrhage
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,816,1981
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - guinea pig
- DOSE/DURATION :
- 207 mg/kg
- TOXIC EFFECTS :
- Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Blood - hemorrhage
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,816,1981
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intramuscular
- SPECIES OBSERVED :
- Rodent - guinea pig
- DOSE/DURATION :
- 181 mg/kg
- TOXIC EFFECTS :
- Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Blood - hemorrhage
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,816,1981 ** OTHER MULTIPLE DOSE TOXICITY DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 1350 mg/kg/15D-I
- TOXIC EFFECTS :
- Kidney, Ureter, Bladder - other changes in urine composition Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Metabolism (Intermediary) - other proteins
- REFERENCE :
- AMACCQ Antimicrobial Agents and Chemotherapy. (American Soc. for Microbiology, 1913 I St., NW, Washington, DC 20006) V.1- 1972- Volume(issue)/page/year: 10,845,1976
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intravenous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 322 mg/kg/2W-I
- TOXIC EFFECTS :
- Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - changes in bladder weight Related to Chronic Data - death
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,816,1981
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Unreported
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 560 mg/kg/14D-I
- TOXIC EFFECTS :
- Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
- REFERENCE :
- CLREAS Clinical Research. (Slack Inc., 6900 Grove Rd., Thorofare, NJ 08086) V.6- 1958- Volume(issue)/page/year: 26,141A,1978
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intramuscular
- SPECIES OBSERVED :
- Mammal - dog
- DOSE/DURATION :
- 700 mg/kg/2W-I
- TOXIC EFFECTS :
- Kidney, Ureter, Bladder - changes in bladder weight
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,816,1981
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Primate - monkey
- DOSE/DURATION :
- 2100 mg/kg/21D-I
- TOXIC EFFECTS :
- Behavioral - ataxia Related to Chronic Data - death
- REFERENCE :
- JIDIAQ Journal of Infectious Diseases. (Univ. of Chicago Press, Journals Div., POB 37005, Chicago, IL 60637) V.1- 1904- Volume(issue)/page/year: 137,476,1978
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Mammal - cat
- DOSE/DURATION :
- 4200 mg/kg/30W-I
- TOXIC EFFECTS :
- Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)
- REFERENCE :
- TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 77,479,1985
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - guinea pig
- DOSE/DURATION :
- 31500 mg/kg/21D-I
- TOXIC EFFECTS :
- Related to Chronic Data - death
- REFERENCE :
- APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 53,230,1983 ** REPRODUCTIVE DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intramuscular
- DOSE :
- 2720 mg/kg
- SEX/DURATION :
- female 14 day(s) pre-mating female 1-20 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Embryo or Fetus - other effects to embryo
- REFERENCE :
- APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 45,145,1979
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intramuscular
- DOSE :
- 3040 mg/kg
- SEX/DURATION :
- female 6-22 day(s) after conception lactating female 21 day(s) post-birth
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)
- REFERENCE :
- APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 45,145,1979
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Intramuscular
- DOSE :
- 250 mg/kg
- SEX/DURATION :
- female 6-15 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Specific Developmental Abnormalities - musculoskeletal system
- REFERENCE :
- ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 31,816,1981
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奈替米星合成路线
奈替米星上下游产品
奈替米星上游产品
奈替米星下游产品
奈替米星制备
方法1：发酵法，产生菌为Micromonospora inyoensis 155OF-1G，由N-乙基-α-去氧-D-链霉胺发酵，提纯而得。
方法2：以西梭霉素为原料，调节Ph值为5，乙醛烷化再氰基氢硼化钠还原即得奈替米星。
方法3：部分氨上乙酰化的西梭霉素，用乙醛和氰基硼氢化钠引入乙基后，经碱性树脂脱去乙酰基，即得奈替米星。
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