Azlocillin sodium salt

Azlocillin is an acylampicillin with a broad spectrum against bacteria.Target: AntibacterialAzlocillin (12.5 μg/mL) inhibits over 75% of the isolates of Pseudomonas aeruginosa. Azlocillin (12.5 μg/mL) is also active against indole-negative and -positive Proteus spp., inhibiting 98 and 71%, respectively. Azlocillin is more active than mezlocillin, ticarcillin, and carbenicillin and as active as BLP-1654 against isolates of P. aeruginosa [1]. The acyl side chains of Azlocillin have an ureido-(urea) structurehence the name "ureidopenicillins" or, more specifically, "acylureidopenicillins." In vitro studies against P. aeruginosa demonstrates that piperacillin has activity that is twice that of azlocillin, 4 times that of mezlocillin and ticarcillin, and about 8 times that of carbenicillin. Azlocillin produces elongated bacterial forms with delayed or no lysis in morphologic studies [2].Azlocillin has MICs of 12.5 μg/mL on Pseudomonas aeruginosa. Azlocillin (3.125 μg/mL) results in a reduction in the rate of growth but no bactericidal phase on Pseudomonas aeruginosa. Azlocillin decreases an initial lag phase with increasing drug concentration. At the lower concentration of tobramycin (0.5 μg/ml), the combinations with both the high and the low concentrations of Azlocillin are more effective than the individual components on Pseudomonas aeruginosa [3]. Isolates with derepression of AmpC enzyme are one to two doubling dilutions more resistant to azlocillin than are those in which increased efflux or impermeability is inferred. Those with secondary β-lactamases are mostly (12/14 cases) susceptible to ceftazidime at 4 mg/L, but are amongst the most resistant to Azlocillin (MIC ≥128 mg/L in 10/14 cases) [4].

Signaling Pathways >> Anti-infection >> Bacterial

Research Areas >> Infection

[1]. Stewart, D. and G.P. Bodey, Azlocillin: in vitro studies of a new semisynthetic penicillin. Antimicrob Agents Chemother, 1977. 11(5): p. 865-70.

[2]. Wright, A.J., The penicillins. Mayo Clin Proc, 1999. 74(3): p. 290-307.

[3]. McFarland, M.M., E.M. Scott, and A. Li Wan Po, Time-survival studies for quantifying effects of azlocillin and tobramycin on Pseudomonas aeruginosa. Antimicrob Agents Chemother, 1994. 38(6): p. 1271-6.

[4]. Livermore, D.M. and H.Y. Chen, Quality of antimicrobial susceptibility testing in the UK: a Pseudomonas aeruginosa survey revisited. J Antimicrob Chemother, 1999. 43(4): p. 517-22.

Puromycin 2HCl | Geneticin | Tunicamycin | Hygromycin B | Salinomycin | Avibactam sodium | Neomycin sulfate | Vaborbactam | Methicillin SodiuM | Rifampicin | Metronidazole | Carbenicillin disodium | Ceftazidime | Eravacycline dihydrochloride | cefotaxime sodium

MOLECULAR FORMULA :

C20-H22-N5-O6-S.Na

MOLECULAR WEIGHT :

483.52

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

1793 mg/kg

TOXIC EFFECTS :

Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Lungs, Thorax, or Respiration - dyspnea

REFERENCE :

AMBIEH Antibiotiki i Meditsinskaya Biotekhnologiya. Antibiotics and Medical Biotechnology. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.30-V.32, 1985-1987 Volume(issue)/page/year: 32,453,1987

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

6690 mg/kg

TOXIC EFFECTS :

Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Lungs, Thorax, or Respiration - dyspnea

REFERENCE :

AMBIEH Antibiotiki i Meditsinskaya Biotekhnologiya. Antibiotics and Medical Biotechnology. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.30-V.32, 1985-1987 Volume(issue)/page/year: 32,453,1987

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

5065 mg/kg

TOXIC EFFECTS :

Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - excitement

REFERENCE :

AMBIEH Antibiotiki i Meditsinskaya Biotekhnologiya. Antibiotics and Medical Biotechnology. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.30-V.32, 1985-1987 Volume(issue)/page/year: 32,453,1987

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intramuscular

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

15420 mg/kg

TOXIC EFFECTS :

Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor Lungs, Thorax, or Respiration - dyspnea

REFERENCE :

AMBIEH Antibiotiki i Meditsinskaya Biotekhnologiya. Antibiotics and Medical Biotechnology. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.30-V.32, 1985-1987 Volume(issue)/page/year: 32,453,1987 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

27 gm/kg/4W-I

TOXIC EFFECTS :

Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :

AMBIEH Antibiotiki i Meditsinskaya Biotekhnologiya. Antibiotics and Medical Biotechnology. (V/O Mezhdunarodnaya Kniga, 113095 Moscow, USSR) V.30-V.32, 1985-1987 Volume(issue)/page/year: 32,453,1987 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5282 No. of Facilities: 7 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 307 (estimated) No. of Female Employees: 251 (estimated)