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解説
C19H37N5O7(447.52)．リカマイシンともいう．Micromonospora inyoesisが産生するアミノ配糖体抗生物質．針状晶の一水和物は融点198～201 ℃．[α]26D＋189°(水)．硫酸塩は白色-淡黄色の粉末．[α]20D＋100～110°(水)．ゲンタマイシンCに似た構造であるが，副作用はゲンタマイシンより弱い．硫酸塩が注射または点眼で使用される．LD50 58 mg/kg(雄ラット，静注)．[CAS 32385-11-8][CAS 53179-09-2:硫酸塩]
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森北出版「化学辞典（第2版）
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効能
抗生物質, タンパク質合成阻害薬
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説明
Sisomicin was found in the culture broth of Micromonospora inyoensis by Schering-Plough Co. in 1970, following the discovery of gentamicin by the same research group. The structure and activity of sisomicin are very similar to those of gentamicin C1a, the major component of the gentamicin complex. Sisomicin shows stronger bacterial activity and lower renal and ototoxicity than gentamicin C1a .
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化学的特性
Off-White Solid
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使用
Sisomicin is an Antibacterial. Gentamicin-like aminoglycoside antibiotic; has broad spectrum antibiotic activity.
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抗菌性
A fermentation product of Micromonospora inyoensis. A dehydro
derivative of gentamicin C1a, supplied as the sulfate salt.
It is virtually identical to gentamicin in activity and pharmacokinetic
behavior. An intramuscular dose of 1–1.5 mg/kg
achieves a peak plasma concentration of 1.5–9.0 mg/L after
0.5–1 h. It is widely distributed in body water, but concentrations
in CSF are low, even in the presence of inflammation.
The plasma half-life is 2.5 h and protein binding is <10%.
It is eliminated almost completely over 24 h in the glomerular
filtrate. Excretion decreases proportionately with renal impairment and because of the virtual identity of the behavior
of the two compounds, a gentamicin nomogram can be used
to adjust dosage. About 40% of the dose is eliminated during
a 6-h dialysis period, during which the elimination half-life
falls to about 8 h.
Mild and reversible impairment of renal function occurs in
about 5% of patients. Nephrotoxicity is more likely to be seen
in those with pre-existing renal disease or treated concurrently
with other potentially nephrotoxic drugs. Ototoxicity mainly
affecting vestibular function has been found in about 1% of
patients. Neuromuscular blockade and other effects common
to aminoglycosides including rashes, paresthesiae, eosinophilia
and abnormal liver function tests have been described.
Its uses are identical to those of gentamicin, which it closely
resembles. It is of limited availability.
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一般的な説明
This aminoglycoside antibiotic is produced by Micromonospora inyoensis. Sisomicin is very similar to gentamicin in its antimicrobial spectrum and all other properties. It is as active as gentamicin against all Enterobacteriaceae . Against Pseudomonas aeruginosa, sisomicin is more active than gentamicin, but not as active as tobramycin. There is almost complete cross-resistance between gentamicin and sisomicin with most Gram-negative bacilli. The reason for this is that sisomicin, like gentamicin, is affected by at least eight of the plasmid-coded modifying enzymes, which can be produced by Gram-negative bacilli). On the other hand, sisomicin is active against some organisms which resist gentamicin by nonenzymatic mechanisms. Sisomicin does not offer significant advantages over gentamicin. It has had limited clinical trials, and has been available commercially in Europe as a sulfate, but not in the USA, UK, and Australia. The drug dosage of sisomicin (3–6 mg/kg/day), its methods of administration, and pharmacokinetics, are similar to those of gentamicin. The toxicity of these two drugs is also probably about the same. Results of treatment of conditions, such as urinary tract infections or Gramnegative bacillary septicemias, have, in general, been similar to what would be expected from an identical gentamicin regimen.
