β-Lactamase Inhibitor
   HOME





β-Lactamase Inhibitor
Beta-lactamases are a family of enzymes involved in bacterial antimicrobial resistance, resistance to β-lactam antibiotic, beta-lactam antibiotics. In bacterial resistance to beta-lactam antibiotics, the bacteria have beta-lactamase which degrade the beta-lactam rings, rendering the antibiotic ineffective. However, with beta-lactamase inhibitors, these enzymes on the bacteria are inhibited, thus allowing the antibiotic to take effect. Strategies for combating this form of resistance have included the development of new beta-lactam antibiotics that are more resistant to cleavage and the development of the class of enzyme inhibitors called beta-lactamase inhibitors. Although β-lactamase inhibitors have little antibiotic activity of their own, they prevent bacterial degradation of beta-lactam antibiotics and thus extend the range of bacteria the drugs are effective against. Medical uses The most important use of beta-lactamase inhibitors is in the treatment of infections known or ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

Clavulanic Acid
Clavulanic acid is a β-lactam antibiotic, β-lactam drug that functions as a Suicide inhibition, mechanism-based β-lactamase inhibitor. While not effective by itself as an antibiotic, when combined with penicillin-group antibiotics, it can overcome antibiotic resistance in bacteria that secrete Beta-lactamase, β-lactamase, which otherwise inactivates most penicillins. In its most common preparations, potassium clavulanate (clavulanic acid as a salt of potassium) is combined with: * amoxicillin (co-amoxiclav, trade names Augmentin, Clavulin, Tyclav, Clavaseptin (veterinary), Clavamox (veterinary), Synulox (veterinary), and others) * ticarcillin (co-ticarclav, trade name Timentin) Clavulanic acid was patented in 1974. In addition to its β-lactamase inhibition, clavulanic acid shows off-target activity in the nervous system by upregulating the glutamate transporter 1 (GLT-1) and has been studied in the potential treatment of a variety of central nervous system disorders. Medi ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

Methicillin-resistant Staphylococcus Aureus (MRSA)
Methicillin-resistant ''Staphylococcus aureus'' (MRSA) is a group of gram-positive bacteria that are genetically distinct from other strains of ''Staphylococcus aureus''. MRSA is responsible for several difficult-to-treat infections in humans. It caused more than 100,000 deaths worldwide attributable to antimicrobial resistance in 2019. MRSA is any strain of ''S. aureus'' that has developed (through mutation) or acquired (through horizontal gene transfer) a multiple drug resistance to beta-lactam antibiotics. Beta-lactam (β-lactam) antibiotics are a broad-spectrum group that include some penams (penicillin derivatives such as methicillin and oxacillin) and cephems such as the cephalosporins. Strains unable to resist these antibiotics are classified as methicillin-susceptible ''S. aureus'', or MSSA. MRSA infection is common in hospitals, prisons, and nursing homes, where people with open wounds, invasive devices such as catheters, and weakened immune systems are at greater ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


Unasyn
Unasyn is the trade name for two related antibiotic drugs: * Ampicillin/sulbactam, a fixed-dose combination medication of the penicillin antibiotic combination ampicillin/sulbactam * Sultamicillin Sultamicillin, sold under the brand name Unasyn among others, is an oral form of the penicillin antibiotic combination ampicillin/sulbactam. It is used for the treatment of bacterial infections of the upper and lower respiratory tract, the kidney ...
, an oral form of the penicillin antibiotic combination ampicillin/sulbactam {{chemistry index ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

Ampicillin
Ampicillin is an antibiotic belonging to the aminopenicillin class of the penicillin family. The drug is used to prevent and treat several bacterial infections, such as respiratory tract infections, urinary tract infections, meningitis, salmonellosis, and endocarditis. It may also be used to prevent group B streptococcal infection in newborns. It is used by mouth, by injection into a muscle, or intravenously. Common side effects include rash, nausea, and diarrhea. It should not be used in people who are allergic to penicillin. Serious side effects may include ''Clostridioides difficile'' colitis or anaphylaxis. While usable in those with kidney problems, the dose may need to be decreased. Its use during pregnancy and breastfeeding appears to be generally safe. Ampicillin was discovered in 1958 and came into commercial use in 1961. It is on the World Health Organization's List of Essential Medicines. The World Health Organization classifies ampicillin as critical ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


Cefepime/enmetazobactam
Cefepime/enmetazobactam, sold under the brand name Exblifep, is a medication used for the treatment of urinary tract infections. It is a fixed dose combination containing cefepime, a cephalosporin antibacterial; and enmetazobactam, a beta-lactamase inhibitor. The combination was approved for medical use in the United States in February 2024, and in the European Union in March 2024. Medical uses In the US, cefepime/enmetazobactam is indicated for the treatment of people with complicated urinary tract infections including pyelonephritis, caused by the following susceptible microorganisms: ''Escherichia coli'', ''Klebsiella pneumoniae'', ''Pseudomonas aeruginosa'', ''Proteus mirabilis'', and ''Enterobacter cloacae'' complex. In the EU, cefepime/enmetazobactam is indicated for the treatment of complicated urinary tract infections, including pyelonephritis; hospital-acquired pneumonia, including ventilator-associated pneumonia; and the treatment of people with bacteremia that ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


Cefepime
Cefepime is a fourth-generation cephalosporin antibiotic. Cefepime has an extended spectrum of activity against Gram-positive and Gram-negative bacteria, with greater activity against both types of organism than third-generation agents. A 2007 meta-analysis suggested when data of trials were combined, mortality was increased in people treated with cefepime compared with other β-lactam antibiotics. In response, the U.S. Food and Drug Administration (FDA) performed their own meta-analysis which found no mortality difference. Cefepime was patented in 1982 by Bristol-Myers Squibb and approved for medical use in 1994. It is available as a generic drug and sold under a variety of trade names worldwide. It was removed from the World Health Organization's List of Essential Medicines in 2019. Medical use Cefepime is usually reserved to treat moderate to severe nosocomial pneumonia, infections caused by multiple drug-resistant microorganisms (e.g. ''Pseudomonas aeruginosa'') and ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  




Ticarcillin/clavulanic Acid
Ticarcillin/clavulanic acid, or co-ticarclav, is a combination antibiotic consisting of ticarcillin, a β-lactam antibiotic, and clavulanic acid, a β-lactamase inhibitor. This combination results in an antibiotic with an increased spectrum of action and restored efficacy against ticarcillin-resistant bacteria that produce certain β-lactamase Beta-lactamases (β-lactamases) are enzymes () produced by bacteria that provide Multiple drug resistance, multi-resistance to beta-lactam antibiotics such as penicillins, cephalosporins, cephamycins, monobactams and carbapenems (ertapenem ...s. References Combination antibiotics {{antibiotic-stub ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

Ticarcillin
Ticarcillin is a carboxypenicillin. It can be sold and used in combination with clavulanate as ticarcillin/clavulanic acid. Because it is a penicillin, it also falls within the larger class of beta-lactam, β-lactam antibiotics. Its main clinical use is as an injectable antibiotic for the treatment of Gram-negative bacteria, particularly ''Pseudomonas aeruginosa'' and ''Proteus vulgaris''. It is also one of the few antibiotics capable of treating ''Stenotrophomonas maltophilia'' infections. It is provided as a white or pale-yellow powder. It is highly soluble in water, but should be dissolved only immediately before use to prevent degradation. It was patented in 1963. Mechanism of action Ticarcillin's antibiotic properties arise from its ability to prevent cross-linking of peptidoglycan during cell wall synthesis, when the bacteria try to Binary fission, divide, causing cell death. Ticarcillin, like penicillin, contains a β-lactam ring that can be cleaved by beta-lactamase, ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


Amoxicillin/clavulanic Acid
Amoxicillin/clavulanic acid, also known as co-amoxiclav or amox-clav, sold under the brand name Augmentin, among others, is an antibiotic medication used for the treatment of a number of bacterial infections. It is a combination consisting of amoxicillin, a β-lactam antibiotic, and potassium clavulanate, a β-lactamase inhibitor. It is specifically used for otitis media, streptococcal pharyngitis, pneumonia, cellulitis, urinary tract infections, and animal bites. It can be administered orally or intravenously. Common side effects include diarrhea, vomiting, and allergic reactions. It also increases the risk of yeast infections, headaches, and blood clotting problems. It is not recommended in people with a history of a penicillin allergy. It is relatively safe for use during pregnancy. Amoxicillin/clavulanic acid was approved for medical use in the United States in 1984. It is on the World Health Organization's List of Essential Medicines. The World Health Organizatio ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


Amoxicillin
Amoxicillin is an antibiotic medication belonging to the aminopenicillin class of the penicillin family. The drug is used to treat bacterial infections such as middle ear infection, strep throat, pneumonia, skin infections, odontogenic infections, and urinary tract infections. It is taken orally (swallowed by mouth), or less commonly by either intramuscular injection or by an IV bolus injection, which is a relatively quick intravenous injection lasting from a couple of seconds to a few minutes. Common adverse effects include nausea and rash. It may also increase the risk of yeast infections and, when used in combination with clavulanic acid, diarrhea. It should not be used in those who are allergic to penicillin. While usable in those with kidney problems, the dose may need to be decreased. Its use in pregnancy and breastfeeding does not appear to be harmful. Amoxicillin is in the β-lactam family of antibiotics. Amoxicillin was discovered in 1958 and came into med ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

New Delhi Metallo-beta-lactamase 1
NDM-1 is an enzyme that makes bacteria Antibiotic resistance, resistant to a broad range of beta-lactam antibiotics. These include the antibiotics of the carbapenem family, which are a mainstay for the treatment of antibiotic-resistant bacterial infections. The gene for NDM-1 is one member of a large gene family that encodes beta-lactamase enzymes called Beta-lactamase#Carbapenemases, carbapenemases. Bacteria that produce carbapenemases are often referred to in the news media as "Antibiotic resistance, superbugs" because infections caused by them are difficult to treat. Such bacteria are usually sensitive only to polymyxins and tigecycline. NDM-1 was first detected in 2008 in a culture plate of ''Klebsiella pneumoniae'' isolated from a Sweden, Swedish patient of Indian origin. It was later detected in bacteria in India, Pakistan, the United Kingdom, the United States, Canada, Japan, Egypt, and Iraq. The most common bacteria that make this enzyme are Gram-negative bacteria, gram-n ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


Metalloproteases
A metalloproteinase, or metalloprotease, is any protease enzyme whose catalytic mechanism involves a metal. An example is ADAM12 which plays a significant role in the fusion of muscle cells during embryo development, in a process known as myogenesis. Most metalloproteases require zinc, but some use cobalt. The metal ion is coordinated to the protein via three ligands. The ligands coordinating the metal ion can vary with histidine, glutamate, aspartate, lysine, and arginine. The fourth coordination position is taken up by a labile water molecule. Treatment with chelating agents such as EDTA leads to complete inactivation. EDTA is a metal chelator that removes zinc, which is essential for activity. They are also inhibited by the chelator orthophenanthroline. Classification There are two subgroups of metalloproteinases: * Exopeptidases, metalloexopeptidases ( EC number: 3.4.17). * Endopeptidases, metalloendopeptidases (3.4.24). Well known metalloendopeptidases include ADAM prote ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]