Β-Lactamase Inhibitor

	Β-Lactamase Inhibitor Beta-lactamases are a family of enzymes involved in bacterial resistance to beta-lactam antibiotics. They act by breaking the beta-lactam ring that allows penicillin-like antibiotics to work. 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 believed to be caused by gram-negative bacteria, as beta-lactamase production is an important contributor to beta-lactam resistance in these pathogens. In contrast, most beta-lactam resistance in gram-positive bacteria is due to variations in peni ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
picture info	Clavulanic Acid Clavulanic acid is a β-lactam drug that functions as a 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 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, Tyclav, Clavamox (veterinary), Synulox (veterinary), and others) * ticarcillin (co-ticarclav, trade name Timentin) Clavulanic acid was patented in 1974. Medical uses Amoxicillin-clavulanic acid is a first-line treatment for many types of infections, including sinus infections, and urinary tract infections, including pyelonephritis. This is, in part, because of its efficacy against gram-negative bacteria which tend to be more difficult to control than gram-positive bacteria with chemotherapeutic antibiot ... [...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 attributable to antimicrobial resistance in 2019. MRSA is any strain of ''S. aureus'' that has developed (through natural selection) 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 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 risk of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	Cefoperazone Cefoperazone is a third-generation cephalosporin antibiotic, marketed by Pfizer under the name Cefobid. It is one of few cephalosporin antibiotics effective in treating ''Pseudomonas'' bacterial infections which are otherwise resistant to these antibiotics. It was patented in 1974 and approved for medical use in 1981. Cefoperazone/sulbactam (Sulperazon) is a co-formulation with sulbactam. Spectrum of bacterial susceptibility Cefoperazone has a broad spectrum of activity and has been used to target bacteria responsible for causing infections of the respiratory and urinary tract, skin, and the female genital tract. The following represents MIC susceptibility data for a few medically significant microorganisms. * ''Haemophilus influenzae'': 0.12 - 0.25 µg/ml * ''Staphylococcus aureus'': 0.125 - 32 µg/ml * ''Streptococcus pneumoniae'': ≤0.007 - 1 µg/ml Adverse effects Cefoperazone contains an ''N''-methylthiotetrazole (NMTT or 1-MTT) side chain. As the antib ... [...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 kidneys ... , 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 used to prevent and treat a number of 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 ''Clostridium 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 critically important for human medicine. It is available as a generic medication. Medical uses ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	Timentin 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 multi-resistance to beta-lactam antibiotics such as penicillins, cephalosporins, cephamycins, monobactams and carbapenems ( ertapenem), although carbapenems ...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 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 divide, causing cell death. Ticarcillin, like penicillin, contains a β-lactam ring that can be cleaved by beta-lactamases, resulting in inactivation of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	Augmentin 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 is taken by mouth or by injection into a vein. 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 Organization cl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	Amoxicillin Amoxicillin is an antibiotic medication used to treat a number of bacterial infections. These include middle ear infection, strep throat, pneumonia, skin infections, and urinary tract infections among others. It is taken by mouth, or less commonly by injection. 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 beta-lactam family of antibiotics. Amoxicillin was discovered in 1958 and came into medical use in 1972. Amoxil was approved for medical use in the United States in 1974, and in the United Kingdom in 1977. It is on the (WHO) World Health Organization's List of Essential Medicines. It is one of the most commonly prescribed anti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
	Tebipenem Tebipenem (brand name Orapenem) is a broad-spectrum orally-administered antibiotic, from the carbapenem subgroup of β-lactam antibiotics. It was developed as a replacement drug to combat bacteria that had acquired antibiotic resistance to commonly used antibiotics. Tebipenem is formulated as the ester tebipenem pivoxil due to the better absorption and improved bioavailability of this form. It has performed well in clinical trial Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, diet ...s for ear infection and looks likely to be further developed in future. It is only marketed in Japan. Tebipenem is the first carbapenem whose prodrug form, the pivalyl ester, is orally available. References Carbapenem antibiotics Prodrugs Thiazolines Formals {{antiinfective-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]
picture info	New Delhi Metallo-beta-lactamase 1 NDM-1 is an enzyme that makes bacteria 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 carbapenemases. Bacteria that produce carbapenemases are often referred to in the news media as " 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 a ''Klebsiella pneumoniae'' isolate from a Swedish patient of Indian origin in 2008. It was later detected in bacteria in India, Pakistan, the United Kingdom, the United States, Canada, Japan, and Egypt. The most common bacteria that make this enzyme are gram-negative such as ''Escherichia coli'' and ''Klebsiella pneumoniae'', but the gene for NDM-1 can spread from one strain of bacteria ... [...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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu]