Tobramycin Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S37/39:Bei der Arbeit geeignete Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
Beschreibung
Tobramycin is one component (factor 6) of a mixture produced by fermentation of Streptomyces tenebrari us.
Lacking the C-3′ hydroxyl group, it is not a substrate for APH(3′)-1 and APH(3′)-II and so has an intrinsically
broader spectrum than kanamycin. It is a substrate, however, for adenylation at C-2′ by ANT (2′) and
acetylation at C-3 by AAC(3)-I and AAC(3)-II and at C-2′ by AAC(2′).
Chemische Eigenschaften
White or almost white powder.
Verwenden
Tobramycin is an aminoglycoside antibiotic.
Definition
ChEBI: A amino cyclitol glycoside that is kanamycin B lacking the 3-hydroxy substituent from the 2,6-diaminoglucose ring.
Indications
Tobramycin is highly active with respect to Gram-negative microorganisms (blue-pus
bacillus and gastric bacilli, rabbit fever, serratia, providencia, enterobacteria, proteus, salmonella, shigella), as well as Gram-positive microorganisms (staphylococci, including
those resistant to penicillin and some cephalosporins), and a few strains of streptococci.
It is used for severe bacterial infections: peritonitis, sepsis, meningitis, osteomyelitis,
endocarditis, pneumonia, pleural empyema, pulmonary abscess, purulent skin infections
and soft tissue infections, and infections of the urinary tract caused by microorganisms that
are sensitive to the drug. Synonyms of this drug are nebicine, obracine, and others.
Antimicrobial activity
In-vitro activity against Ps. aeruginosa
is usually somewhat greater than that of gentamicin; against
other organisms activity is similar or a little lower. Other
Pseudomonas species are generally resistant, as are streptococci
and most anaerobic bacteria. Other organisms usually susceptible
in vitro include Acinetobacter, Legionella and Yersinia
spp. Alkaligenes, Flavobacterium spp. and Mycobacterium spp.
are resistant. It exhibits bactericidal activity at concentrations
close to the MIC and bactericidal synergy typical of aminoglycosides
in combination with penicillins or cephalosporins.
Acquired resistance
It is inactivated by many aminoglycoside-modifying enzymes
that inactivate gentamicin. However,
AAC(3′)-I does not confer tobramycin resistance and
AAC(3′)-II confers a lower degree of tobramycin resistance
than of gentamicin resistance. Conversely, ANT(4′) confers
tobramycin but not gentamicin resistance, as do some types
of AAC(6′). Overproduction of APH(3′), conferring a low
degree of resistance to tobramycin (MIC 8 mg/L), but not
gentamicin (MIC 2 mg/L), was ascribed to ‘trapping’ rather
than phosphorylation.
Resistance rates are generally similar to those of gentamicin,
although they may vary locally because of the prevalence
of particular enzyme types.
Biologische Aktivität
Pharmacologically, tobramycin is quite similar to gentamicin. The drug is somewhat more active against Ps. aeruginosa than gentamicin. Tobramycin also acts synergistically with penicillin, but to a lesser degree than gentamicin.
Clinical Use
Severe infections caused by susceptible micro-organisms
Ps. aeruginosa infections, including chronic pulmonary infections in cystic
fibrosis (administration by injection or nebulizer)
For practical purposes use is identical to that of gentamicin,
except possibly for Pseudomonas infection, where it has somewhat
greater activity against gentamicin-susceptible and some
gentamicin-resistant strains. Its value as a substitute for gentamicin
in the speculative treatment of severe undiagnosed
infection is offset by its lower activity against other organisms
that may be implicated.
It has been used extensively to treat Ps. aeruginosa infections
in patients with cystic fibrosis.
Tobramycin Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
