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NETILMICIN

NETILMICIN
NETILMICIN
CAS No.
56391-56-1
Chemical Name:
NETILMICIN
Synonyms
ntl;netilyn;netillin;vectacin;sch20569;nettacin;ntromycin;ntromicine;certomycin;NETILMICIN
CBNumber:
CB1461174
Molecular Formula:
C21H41N5O7
Formula Weight:
475.58
MOL File:
56391-56-1.mol

NETILMICIN Properties

alpha 
D26 +164° (c = 3 in water)
Boiling point:
575.33°C (rough estimate)
Density 
1.2404 (rough estimate)
refractive index 
1.7500 (estimate)

SAFETY

Toxicity LD50 in mice (mg/kg): 40 i.v.; 125 i.p.; 175 s.c. (Miller)

NETILMICIN price

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NETILMICIN Chemical Properties,Uses,Production

Antimicrobial activity

It is active against a wide range of enterobacteria as well as many Acinetobacter, Pseudomonas, Citrobacter, Proteus and Serratia spp. Staphylococci, including methicillin-resistant and coagulase-negative strains, are usually susceptible. Nocardiae are inhibited by 0.04–1 mg/L. Providencia spp. and anaerobic bacteria are generally resistant.
It is active against some gentamicin-resistant strains, particularly those that synthesize ANT(2″) or AAC(3)-I. It exhibits typical aminoglycoside properties: bactericidal activity at or close to the MIC; greater activity at alkaline pH; depression of activity against Pseudomonas by divalent cations; and synergy with β-lactam antibiotics. Bactericidal synergy can be demonstrated regularly with benzylpenicillin against viridans streptococci and E. faecalis, but seldom against E. faecium, which characteristically synthesizes AAC(6′), to which netilmicin is susceptible.

Acquired resistance

It is resistant to ANT(2), AAC(3)-I and AAC(3)-III, but sensitive to AAC(6). AAC(3)-II confers resistance, but generally to a lesser degree than to gentamicin.
Resistance rates are generally about the same as, or a little lower than, those for gentamicin.

Pharmacokinetics

Cmax 1 mg/kg intramuscular: 4–6 mg/L after 0.5–1 h
2 mg/kg intravenous 30-min infusion: c. 12 mg/L end infusion
5 mg/kg: >10 mg/L after 1 h
Plasma half-life: 2–2.5 h
Volume of distribution: 0.25 L/kg
Plasma protein binding: <10%
The pharmacokinetics are similar to those of gentamicin. In patients receiving 200 mg (2.2–3.6 mg/kg) intramuscularly every 8 h for 10 days, a mean peak plasma concentration of around 14 mg/L was found. Peak concentrations of about 10 mg/L were found in children with pyelonephritis treated with 5 mg/kg per day, compared with peaks of about 5 mg/L in children given 2 mg/kg every 8 h. The serum half-life is linearly inversely related to creatinine clearance in patients with renal impairment. Plasma concentrations decreased by 63% during hemodialysis. In older patients with a mean creatinine clearance of 63 mL/min, the half-life was 6.2 h after a dose of 2 mg/kg.
In the newborn, intramuscular injection of 2.5 mg/kg produced peak plasma concentrations of 1–5 mg/L 1 h after the dose, with a plasma half-life of 4 h. In newborns given 6 mg/kg per day, plasma concentrations were 7.4–13.2 mg/L after 2 h. Half-lives were greater (mean 6.7 h) than in those of >36 weeks postmenstrual age (mean 4.6 h), and pre-dose concentrations were 2.1 and 1.6 mg/L, respectively, suggesting that a lower daily dose (4.5 mg/kg) may be appropriate. Children with cystic fibrosis had a higher total body clearance.
Distribution
Netilmicin is distributed in the extracellular water and in patients with cystic fibrosis the apparent volume of distribution seems not to be increased.
Very little reaches the CSF even in the presence of inflammation. Concentrations of 0.13–0.45 mg/L were found in patients without meningeal inflammation following an intravenous dose of 400 mg. In patients with meningitis, the drug was undetectable, although concentrations of 0.2–5 mg/L could be found later in the course of treatment in some cases.
Excretion
It is excreted unchanged in the urine in the glomerular filtrate, with some tubular reabsorption. Over the first 6 h, about 50% and by 24 h about 80% of the dose appears. No metabolites are known and it is likely that this represents binding to tissues.Clearance on hemodialysis is similar to that reported for gentamicin.

Clinical Use

Severe infections (including septicemia, lower respiratory tract infections, urinary tract infections, peritonitis, endometritis) caused by susceptible strains of Gram-negative bacilli and staphylococci

Side effects

It is considered to be less nephrotoxic than gentamicin, a difference not easily explained since the renal clearance and renal and medullary concentrations of the drugs appear to be similar. Both vestibular and cochlear toxicity appear to be low and vestibular toxicity without audiometric abnormality is rare. In some patients, plasma concentrations up to 30 mg/L over periods exceeding 1 week have not resulted in ototoxicity. Evidence of some renal toxicity in the excretion of granular casts has occurred fairly frequently in patients receiving 7.5 mg/kg per day, and is more likely to occur in the elderly and in those receiving higher doses or longer courses. In patients treated for an average of 35 days with 2.4–6.9 mg/kg per day, there was no effect on initially normal renal function, even in the elderly. Long-term treatment led to an increase in elimination half-life from 1.5 to 1.9 h. Nephrotoxicity has been observed in some diabetic patients. Overall estimates of the frequency of nephrotoxicity have ranged from 1% to 18%. Increases in serum transaminase and alkaline phosphatase concentrations have been seen in some patients without other evidence of hepatic impairment.
Once-daily dosing is thought to be safer than twice or three times daily dosing.

NETILMICIN Preparation Products And Raw materials

Raw materials

Preparation Products


NETILMICIN Suppliers

Global( 16)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Beijing HuaMeiHuLiBiological Chemical 010-56205725;010-86181995
010-65763397 waley188@sohu.com China 12388 58
Wuhan Dahua Weiye Pharmaceutical Chemical Co., Ltd. 027-59262863 13277907145 QQ 3091977954
027-83322098 dh.luna@whdhwy.com China 2008 50
Hubei Jusheng Technology Co.,Ltd North:027-59599241,18871490274,QQ:1400878000 South:027-59599240,18871490354,QQ:1400868000
FAX:027-59599240 sales@hubeijusheng.com China 9917 58
Alta Scientific Co., Ltd. (0086) 22-6537-8550; 185-2256-9193; 185-2256-9194
(0086) 22-2532-9655 contact@altascientific.com China 8345 55

56391-56-1(NETILMICIN)Related Search:


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