ネチルマイシン

ネチリマイシン · ネトロマイシン · 1-N-エチルシソミシン · ネチルマイシン · 4-O-[[3α-アミノ-6-(アミノメチル)-3,4-ジヒドロ-2H-ピラン]-2α-イル]-6-O-[4-C-メチル-3-(メチルアミノ)-3-デオキシ-β-L-アラビノピラノシル]-N1-エチル-2-デオキシ-D-ストレプタミン · ネチルミシン · 1-N-エチルシソマイシン · (2R,3R,4R,5R)-2-{[(1S,2S,3R,4S,6R)-4-アミノ-3-{[(2S,3R)-3-アミノ-6-(アミノメチル)-3,4-ジヒドロ-2H-ピラン-2-イル]オキシ}-6-(エチルアミノ)-2-ヒドロキシシクロヘキシル]オキシ}-5-メチル-4-(メチルアミノ)オキサン-3,5-ジオール

https://huagongshe.com/ja/chemical/441306

識別子と物理属性

CAS No.	56391-56-1
分子式	C21H41N5O7
平均分子量	475.6 g/mol
単同位体質量	475.30059865 g/mol
SMILES	CCN[C@@H]1C[C@H](N)[C@@H](O[C@H]2OC(CN)=CC[C@H]2N)[C@H](O)[C@H]1O[C@H]1OC[C@](C)(O)[C@H](NC)[C@H]1O
InChIKey	CIDUJQMULVCIBT-MQDUPKMGSA-N
PubChem CID	441306
ChEMBL	CHEMBL1572
EC No.	260-146-8
DTXSID	DTXSID1048542
現地名	ネチルマイシン

化学・物理的性質

XLogP	-4.2
極性表面積	200
水素結合供与体数	8
水素結合受容体数	12
回転可能結合数	8
重原子数	33
形式電荷	0
複雑度	673
医薬品	Pharmaceuticals -> AntibioticsPharmaceuticals -> Listed in ZINC15
Human Drugs	Ophthalmological preparations > Anti-infective agents
Decomposition	When heated to decomposition it emits acrid smoke and irritating fumes.
Optical Rotation	Specific optical rotation: +164 deg at 26 °C/D (3 in water)
Collision Cross Section	216.82 Å² [M+Na]+ [CCS Type: TWMethod: calibrated with polyalanine and drug standards]
比旋光度	D26 +164° (c = 3 in water)
沸点	575.33°C (rough estimate)
密度	1.2404 (rough estimate)
屈折率	1.7500 (estimate)
pKa（酸解離定数）	13.29±0.70(Predicted)

安全性と法規制

FDA 要件	Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended21 U.S.C. 321-392).
保管条件	Commercially available netilmicin sulfate injection should be stored at 2 - 30 °C. /Netilmicin sulfate/
処分方法	SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.
相互作用	Concurrent and/or sequential use of 2 or more aminoglycosides by any route or concurrent use of capreomycin with aminoglycosides should be avoided since the potential for ototoxicity, nephrotoxicity, and neuromuscular blockade may be increasedhearing loss may occur and may progress to deafness even after discontinuation of the drugloss of hearing may be reversible, but usually is permanentneuromuscular blockade may result in skeletal muscle weakness and respiratory depression or paralysis (apnea). Also, concurrent use of 2 or more aminoglycosides may result in reduced bacterial uptake of each one since the medications compete for the same uptake mechanism. /Aminoglycosides/Concurrent use of medications with neuromuscular blocking activity, including halogenated hydrocarbon inhalation anesthetics, opioid analgesics, and massive transfusions with citrate anticoagulated blood, with aminoglycosides should be carefully monitored since neuromuscular blockade may be enhanced, resulting in skeletal muscle weakness and respiratory depression or paralysis (apnea)caution is recommended when these medications and aminoglycosides are used concurrently during surgery or in the postoperative period, especially if there is a possibility of incomplete reversal of neuromuscular blockade postoperativelytreatment with anticholinesterase agents or calcium salts may help reverse the blockade. /Aminoglycosides/Vancomycin and aminoglycosides must often be administered concurrently in the prophylaxis of bacterial endocarditis, in the treatment of endocarditis caused by streptococci and Corynebacteria species, in the treatment of resistant staphylococcal infections, or in penicillin-allergic patientsappropriate monitoring will help to reduce the risk of nephrotoxicity or ototoxicity

用途

説明

This is a semisynthetic derivative of sisomicin, which was developed by ethylation of the 1-N position of the deoxystreptamine ring of sisomicin . Clinically, netilmicin is used as a sulfate. Netilmicin has a similar in vitro antibacterial spectrum to that of gentamicin but, unlike sisomicin, it is active against a proportion of gentamicin-resistant Gram-negative bacilli. However, netilmicin is not active against as wide a range of gentamicin-resistant Gram-negative bacilli as amikacin. Nevertheless, it may be occasionally indicated as an alternative to amikacin for the treatment of infections caused by gentamicin-resistant but netilmicin-susceptible Gram-negative organisms. The following details apply only to netilmicin