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Durlobactam
Durlobactam is a beta-lactamase inhibitor used in combination with sulbactam to treat susceptible strains of bacteria in the genus ''Acinetobacter'' It is an analog of avibactam. The combination therapy sulbactam/durlobactam Sulbactam/durlobactam, sold under the brand name Xacduro (by Innoviva Specialty Therapeutics), is a co-packaged medication used for the treatment of bacterial pneumonia caused by '' Acinetobacter baumannii-calcoaceticus'' complex. It contains ... was approved for medical use in the United States in May 2023. See also * ETX0462 References Further reading * * Beta-lactamase inhibitors Ureas Amides Sulfate esters Heterocyclic compounds with 2 rings Nitrogen heterocycles {{Pharma-stub ...
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Sulbactam/durlobactam
Sulbactam/durlobactam, sold under the brand name Xacduro (by Innoviva Specialty Therapeutics), is a co-packaged medication used for the treatment of bacterial pneumonia caused by '' Acinetobacter baumannii-calcoaceticus'' complex. It contains sulbactam, a beta-lactam antibacterial and beta-lactamase inhibitor; and durlobactam, a beta-lactamase inhibitor. Sulbactam/durlobactam was approved for medical use in the United States in May 2023. Medical uses Sulbactam/durlobactam is indicated for the treatment of hospital-acquired bacterial pneumonia and ventilator-associated bacterial pneumonia, caused by susceptible isolates of ''Acinetobacter baumannii-calcoaceticus'' complex. History The efficacy of sulbactam/durlobactam was established in a multicenter, active-controlled, open-label (investigator-unblinded, assessor-blinded), non-inferiority clinical trial in 177 hospitalized adults with pneumonia caused by carbapenem-resistant ''A. baumannii''. Participants received eit ...
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Acinetobacter
''Acinetobacter'' is a genus of Gram-negative bacteria belonging to the wider class of Gammaproteobacteria. ''Acinetobacter'' species are oxidase-negative, exhibit twitching motility, and occur in pairs under magnification. They are important soil organisms, where they contribute to the mineralization of, for example, aromatic compounds. ''Acinetobacter'' species are a key source of infection in debilitated patients in the hospital, in particular the species '' Acinetobacter baumannii''. Description Species of the genus ''Acinetobacter'' are strictly aerobic, nonfermentative, Gram-negative bacilli. They show mostly a coccobacillary morphology on nonselective agar. Rods predominate in fluid media, especially during early growth. The morphology of ''Acinetobacter'' species can be quite variable in Gram-stained human clinical specimens, and cannot be used to differentiate ''Acinetobacter'' from other common causes of infection. Most strains of ''Acinetobacter'', except som ...
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Sulbactam
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 antibiotic An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting pathogenic bacteria, bacterial infections, and antibiotic medications are widely used in the therapy ...s. It was patented in 1977 and approved for medical use in 1986. Medical uses The combination ampicillin/sulbactam (Unasyn) is available in the United States. The combination cefoperazone/sulbactam (Sulperazon) is available in many countries but not in the United States. The co-packaged combination sulbactam/durlobactam was approved for medical use in the United States in May 2023. Mechanism Sulbactam is primarily used as a suicide inhibitor of β-lactamase, shielding more potent beta-lactams such as ampicillin. Sulbactam itself contains a ...
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Intravenous
Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutrients for those who cannot, or will not—due to reduced mental states or otherwise—consume food or water per os, by mouth. It may also be used to administer pharmaceutical drug, medications or other medical therapy such as blood transfusion, blood products or electrolytes to correct electrolyte imbalances. Attempts at providing intravenous therapy have been recorded as early as the 1400s, but the practice did not become widespread until the 1900s after the development of techniques for safe, effective use. The intravenous route is the fastest way to deliver medications and fluid replacement throughout the body as they are introduced directly into the circulatory system and thus quickly distributed. For this reason, the intravenous route ...
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Antibacterial
An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting bacterial infections, and antibiotic medications are widely used in the treatment and prevention of such infections. They may either kill or inhibit the growth of bacteria. A limited number of antibiotics also possess antiprotozoal activity. Antibiotics are not effective against viruses such as the ones which cause the common cold or influenza. Drugs which inhibit growth of viruses are termed antiviral drugs or antivirals. Antibiotics are also not effective against fungi. Drugs which inhibit growth of fungi are called antifungal drugs. Sometimes, the term ''antibiotic''—literally "opposing life", from the Greek roots ἀντι ''anti'', "against" and βίος ''bios'', "life"—is broadly used to refer to any substance used against microbes, but in the usual medical usage, antibiotics (such as penicillin) are those produced ...
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Beta-lactamase Inhibitor
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 are relatively resistant to beta-lactamase. Beta-lactamase provides antibiotic resistance by breaking the antibiotics' structure. These antibiotics all have a common element in their molecular structure: a four-atom ring known as a beta-lactam (β-lactam) ring. Through hydrolysis, the enzyme lactamase breaks the β-lactam ring open, deactivating the molecule's antibacterial properties. Beta-lactamases produced by gram-negative bacteria are usually secreted, especially when antibiotics are present in the environment. Structure The structure of a ''Streptomyces'' serine β-lactamase (SBLs) is given by . The alpha-beta fold () resembles that of a DD-transpeptidase, from which the enzyme is thought to have evolved. β-lactam antibiotics ...
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Avibactam
Avibactam is a non-β-lactam Β-Lactamase inhibitor, β-lactamase inhibitor developed by Actavis (now Teva Pharmaceuticals, Teva) jointly with AstraZeneca. A new drug application for avibactam in Ceftazidime/avibactam, combination with ceftazidime was approved by the FDA in 2015 for treating complicated Urinary tract infection, urinary tract (cUTI) and complicated intra-abdominal infections (cIAI) caused by Antibiotic resistance, antibiotic-resistant pathogens, including those caused by multidrug resistant Gram-negative bacteria, Gram-negative bacterial pathogens. Increasing resistance to cephalosporins among Gram-negative bacterial pathogens, especially among hospital-acquired infections, results in part from the production of Beta-lactamase, β-lactamase enzymes that deactivate these antibiotics. While the co-administration of a β-lactamase inhibitor can restore antibacterial activity to the cephalosporin, previously approved β-lactamase inhibitors such as tazobactam and clavu ...
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ETX0462
ETX0462 is an experimental antibiotic drug which acts both as a β-Lactamase inhibitor and also has separate antibiotic activity in its own right. It is active against a range of drug-resistant bacteria of concern including ''Pseudomonas aeruginosa'', ''Stenotrophomonas maltophilia'' and ''Burkholderia cepacia''. While ETX0462 is still in pre-clinical research and has not yet reached clinical trials, it was hailed as a significant advance as it represents an example of a completely new structural class of antibiotics, so even if this particular molecule does not get developed for medical use it is likely that related compounds will continue to be developed. See also * Avibactam * Durlobactam Durlobactam is a beta-lactamase inhibitor used in combination with sulbactam to treat susceptible strains of bacteria in the genus ''Acinetobacter'' It is an analog of avibactam. The combination therapy sulbactam/durlobactam Sulbactam/dur ... References {{reflist Antibiotics
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Beta-lactamase Inhibitors
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 are relatively resistant to beta-lactamase. Beta-lactamase provides antibiotic resistance by breaking the antibiotics' structure. These antibiotics all have a common element in their molecular structure: a four-atom ring known as a beta-lactam (β-lactam) ring. Through hydrolysis, the enzyme lactamase breaks the β-lactam ring open, deactivating the molecule's antibacterial properties. Beta-lactamases produced by gram-negative bacteria are usually secreted, especially when antibiotics are present in the environment. Structure The structure of a ''Streptomyces'' serine β-lactamase (SBLs) is given by . The alpha-beta fold () resembles that of a DD-transpeptidase, from which the enzyme is thought to have evolved. β-lactam antibioti ...
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Ureas
image:Biotin_structure.svg, 220 px, Biotin, a water-soluble B vitamins, B vitamin, is a bicyclic urea. In chemistry, ureas are a class of organic compounds with the formula (R2N)2CO where R = H, alkyl, aryl, etc. Thus, in addition to describing the specific chemical compound urea ((H2N)2CO), urea is the name of a functional group that is found in many compounds and materials of both practical and theoretical interest. Generally ureas are colorless crystalline solids, which, owing to the presence of fewer hydrogen bonds, exhibit melting points lower than that of urea itself. Synthesis Ureas can be prepared many methods, but rarely by direct carbonation, which is the route to urea itself. Instead, methods can be classified according those that assemble the urea functionality and those that start with preformed urea. Assembly of N-substituted urea functionality Phosgenation entails the reaction of amines with phosgene, proceeding via the isocyanate (or carbamoyl chloride) as an i ...
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Amides
In organic chemistry, an amide, also known as an organic amide or a carboxamide, is a compound with the general formula , where R, R', and R″ represent any group, typically organyl groups or hydrogen atoms. The amide group is called a peptide bond when it is part of the main chain of a protein, and an isopeptide bond when it occurs in a side chain, as in asparagine and glutamine. It can be viewed as a derivative of a carboxylic acid () with the hydroxyl group () replaced by an amino group (); or, equivalently, an acyl (alkanoyl) group () joined to an amino group. Common amides are formamide (), acetamide (), benzamide (), and dimethylformamide (). Some uncommon examples of amides are ''N''-chloroacetamide () and chloroformamide (). Amides are qualified as primary, secondary, and tertiary according to the number of acyl groups bounded to the nitrogen atom. Nomenclature The core of amides is called the amide group (specifically, carboxamide group). In the usual no ...
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Sulfate Esters
The sulfate or sulphate ion is a polyatomic anion with the empirical formula . Salts, acid derivatives, and peroxides of sulfate are widely used in industry. Sulfates occur widely in everyday life. Sulfates are salts of sulfuric acid and many are prepared from that acid. Spelling "Sulfate" is the spelling recommended by IUPAC, but "sulphate" was traditionally used in British English. Structure The sulfate anion consists of a central sulfur atom surrounded by four equivalent oxygen atoms in a tetrahedral arrangement. The symmetry of the isolated anion is the same as that of methane. The sulfur atom is in the +6 oxidation state while the four oxygen atoms are each in the −2 state. The sulfate ion carries an overall charge of −2 and it is the conjugate base of the bisulfate (or hydrogensulfate) ion, , which is in turn the conjugate base of , sulfuric acid. Organic sulfate esters, such as dimethyl sulfate, are covalent compounds and esters of sulfuric acid. The tetrahedral mo ...
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