硫酸フラジオマイシン

外観

白色〜うすい黄色, 結晶性粉末〜粉末

溶解性

水に溶けやすく、エタノール(95)にほとんど溶けない。

用途

アミノグリコシド系抗生物質 です。細菌リボソーム 30S に結合し、タン パク質合成阻害作用を示します。グラム陽性・ 陰性菌に対して強い抗菌力を示します。

用途

アミノグリコシド系抗生物質 です。細菌リボソーム 30s に結合し、タンパ ク質合成阻害作用を示します。グラム陽性・ 陰性菌に対して強い抗菌力を示します。

説明

Neomycin sulfate is an aminoglycoside antibiotic and calcium channel protein inhibitor. Neomycin sulfate also binds to prokaryotic ribosomes inhibiting translation and is effective against gram-positive and gram-negative bacteria. Neomycin sulfate inhibits PLC (Phospholipase C) via binding to inositol phospholipids. It also inhibits phosphatidylcholine-PLD activity and induces Ca2+ mobilization and PLA2 activation in human platelets. Neomycin sulfate inhibits DNase I induced DNA degradation. It is used to prevent or treat skin infections caused by bacteria. It is not effective against fungal or viral infections.

化学的特性

White or yellowish-white powder; odorless; highly hygroscopic; aqueous solution exhibits dextrorotation. High solubility in water, while almost insoluble in ethanol, ether, acetone or chloroform.

使用

Neomycin sulfate is an aminoglycoside antibiotic produced by S. fradiae that inhibits protein translation by binding to the small subunit of prokaryotic ribosomes. It blocks voltage-sensitive Ca2+ channels and is a potent inhibitor of skeletal muscle sarcoplasmic reticulum Ca2+ release. NEOMYCIN SULFATE has been shown to inhibit inositol phospholipid turnover, phospholipase C, and phosphatidylcholine-phospholipase D activity (IC50 = 65 μM). It is highly effective against Gram-positive and Gram-negative bacteria and is commonly used for the prevention of bacterial contamination of cell cultures.

適応症

This drug is obtained from species of the actinomycete Streptomyces and is an aminoglycoside antibiotic (as are streptomycin, gentamicin, and kanamycin) effective against most aerobic gram-negative organisms. Group A streptococci are relatively resistant. Neomycin acts to inhibit bacterial protein synthesis by irreversibly binding to the 30S subunit. It is responsible for a greater incidence of allergic contact sensitivity than any other topical antibiotic. This diagnosis often remains hidden, because morphologically the eruption is of a mild eczematous nature. Rarely, anaphylaxis may occur.

世界保健機関（WHO）

Neomycin sulfate, a broad-spectrum antibiotic, was first isolated in 1949 and has subsequently been included in topical, oral and parenteral preparations. Its value in the treatment of diarrhoea is widely questioned although it is still contained in a number of widely available antidiarrhoeal preparations. In some countries the officially approved indications for oral preparations are restricted to the preparation of the bowel prior to surgery and the management of hepatic coma.

一般的な説明

Chemical structure: aminoglycoside

接触アレルゲン

Neomycin is an antibiotic complex of the aminoglycosides group, extracted from Streptomyces fradiae. It is composed of neomycin A (neamin) and an isomer neobiosamin, either neomycin B (framycetin or Soframycin?) or neomycin C. Its use has been progressively forbidden in cosmetics and as an additive for animal feed. Occupational contact dermatitis occurs in workers at animal feed mills, in veterinaries, or in health workers. Nonoccupational dermatitis mainly concerns patients with chronic dermatitis, leg ulcers, or chronic otitis. Cross-sensitivity is usual with other aminoglycosides (amikacin, arbekacin, butirosin, dibekacin, gentamicin, isepamicin, kanamycin, paromomycin, ribostamycin, sisomycin, tobramycin), is rare with netilmicin and streptomycin, but nonexistent with spectinomycin.

臨床応用

In a search for antibiotics less toxic than streptomycin,Waksman and Lechevalier isolated neomycin (Mycifradin,Neobiotic) in 1949 from Streptomyces fradiae. Since then, theimportance of neomycin has increased steadily, and today, itis considered one of the most useful antibiotics for the treatmentof GI infections, dermatological infections, and acutebacterial peritonitis. Also, it is used in abdominal surgery toreduce or avoid complications caused by infections from bacterialflora of the bowel. It has broad-spectrum activityagainst various organisms and shows a low incidence of toxicand hypersensitivity reactions. It is absorbed very slightlyfrom the digestive tract, so its oral use ordinarily does not produce any systemic effect. The development of neomycinresistantstrains of pathogens is rarely reported in those organismsagainst which neomycin is effective.
Neomycin as the sulfate salt is a white to slightly yellow,crystalline powder that is very soluble in water. It is hygroscopicand photosensitive (but stable over a wide pH rangeand to autoclaving). Neomycin sulfate contains the equivalentof 60% of the free base.
Neomycin, as produced by S. fradiae, is a mixture ofclosely related substances. Included in the “neomycin complex”is neamine (originally designated neomycin A) andneomycins B and C. S. fradiae also elaborates another antibiotic,the fradicin, which has some antifungal propertiesbut no antibacterial activity. This substance is not present in“pure” neomycin.

副作用

The most common adverse reactions to oral neomycin sulfate are nausea, vomiting and diarrhea. The “Malabsorption Syndrome” characterized by increased fecal fat, decreased serum carotene and fall in xylose absorption has been reported with prolonged therapy.

安全性プロファイル

Poison by intramuscular, intravenous, and subcutaneous routes. Human systemic effects by ingestion: somnolence, hallucinations and distorted perceptions, and anorexia. A human skin irritant. When heated to decomposition it emits very toxic fumes of SOx.