Sulbactam is a β-lactamase inhibitor. This drug is given in combination with β-lactam antibiotics to inhibit β-lactamase, an enzyme produced by bacteria that destroys the antibiotics.
Mechanism
Sulbactam is an irreversible inhibitor of β-lactamase; it binds to the enzyme and does not allow it to degrade the antibiotic.
Uses
Sulbactam is able to inhibit the most common forms of β-lactamase but is not able to interact with the AmpC cephalosporinase. Thus, it confers little protection against bacteria such as Pseudomonas aeruginosa, Citrobacter, Enterobacter, and Serratia, which often express this gene.
In the United States, sulbactam is combined to form cefoperazone/sulbactam and ampicillin/sulbactam. It does possess some antibacterial activity when administered alone, but it is too weak to have any clinical importance. Its use in the UK is restricted to hospitals.
Recently, its use in treating Acinetobacter septicemia is receiving renewed interest.
Basic information
| Product Name: | Sulbactam |
| Synonyms: | (2S,5R)-3,3-DIMETHYL-4,4,7-TRIOXO-4LAMBDA6-THIA-1-AZA-BICYCLO[3.2.0]HEPTANE-2-CARBOXYLIC ACID;(2S-CIS)-3,3-DIMETHYL-7-OXO-4-THIA-1-AZABICYCLO[3,2,0]HEPTANE-2-CARBOXYLIC ACID 4,4-DIOXIDE;3,3-DIMETHYL-4,4,7-TRIOXO-4LAMBDA6-THIA-1-AZA-BICYCLO[3.2.0]HEPTANE-2-CARBOXYLIC ACID;SULBACTAM;SULBACTAM ACID;sulbactam acid (base);PENICILLANIC ACID SULFONE;(2S,5R)-3,3-Dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid 4,4-dioxide |
| CAS: | 68373-14-8 |
| MF: | C8H11NO5S |
| MW: | 233.24 |
| Product Categories: | Peptide Synthesis/Antibiotics;MERITAL |
| Mol File: | 68373-14-8.mol |
Chemical Properties
| boiling point | 567.7 °C at 760 mmHg |
| density | 1.62 g/cm3 |
| vapor pressure | 2.26E-14 mmHg at 25°C |
| flashing point | 297.1 °C |
| storage temp. | −20°C |
| solubility | dissolved in water, methanol and ethyl acetate |
Specification:
ITEMS
|
STANDARD
|
RESULTS
|
Characters
|
White or almost white crystalline granule and powder
|
A white crystalline granule and powder
|
Identification
|
(1) The spectrum obtained with the substance to be examined corresponds with that obtained with reference standard
(2) Should meet the requirement under water
|
Comforms
|
Appearance of solution
|
≤reference suspension II
(1 mol/L hydrochloric acid)
≤reference suspension II
(2 mol/L ammonia)
|
≤Reference suspension I
≤Reference suspension I
|
PH
|
3.5~5.5
|
4.4
|
Specific optical rotation
|
+280~ +305
|
+296
|
Related substances
|
Any impurity≤1.0%
|
0.26%
|
Dimethylaniline
|
≤20ppm
|
Complies
(not used in process)
|
Water
|
12.0%~15.0%
|
13.3%
|
Sulphated ash
|
≤0.5%
|
0.07%
|
Bulk density
|
0.45g/ml - 0.65g/ml
|
0.57g/ml
|
Tapped density
|
≥0.65g/ml
|
0.76g/ml
|
Assay
|
96.0%~102.0% C16H19N3O4S
(calculated on the anhydrous basis)
|
99.7%
|
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