Imipenem Cilastatin
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Imipenem Cilastatin
Imipenem (trade name Primaxin among others) is an intravenous β-lactam antibiotic discovered by Merck scientists Burton Christensen, William Leanza, and Kenneth Wildonger in the mid-1970s. Carbapenems are highly resistant to the β-lactamase enzymes produced by many multiple drug-resistant Gram-negative bacteria, thus play a key role in the treatment of infections not readily treated with other antibiotics. Imipenem was patented in 1975 and approved for medical use in 1985. It was discovered via a lengthy trial-and-error search for a more stable version of the natural product thienamycin, which is produced by the bacterium ''Streptomyces cattleya''. Thienamycin has antibacterial activity, but is unstable in aqueous solution, so impractical to administer to patients. Imipenem has a broad spectrum of activity against aerobic and anaerobic, Gram-positive and Gram-negative bacteria. It is particularly important for its activity against ''Pseudomonas aeruginosa'' and the '' Enteroc ...
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Intramuscular Injection
Intramuscular injection, often abbreviated IM, is the injection of a substance into a muscle. In medicine, it is one of several methods for parenteral administration of medications. Intramuscular injection may be preferred because muscles have larger and more numerous blood vessels than subcutaneous tissue, leading to faster absorption than subcutaneous or intradermal injections. Medication administered via intramuscular injection is not subject to the first-pass metabolism effect which affects oral medications. Common sites for intramuscular injections include the deltoid muscle of the upper arm and the gluteal muscle of the buttock. In infants, the vastus lateralis muscle of the thigh is commonly used. The injection site must be cleaned before administering the injection, and the injection is then administered in a fast, darting motion to decrease the discomfort to the individual. The volume to be injected in the muscle is usually limited to 2–5 milliliters, depending on in ...
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Acinetobacter Calcoaceticus
''Acinetobacter calcoaceticus'' is a bacterial species of the genus ''Acinetobacter''. It is a nonmotile, Gram-negative coccobacillus. It grows under aerobic conditions, is catalase positive and oxidase negative. ''A. calcoaceticus'' is a part of the A. calcoaceticus-A. baumannii complex together with ''Acinetobacter baumannii'', ''Acinetobacter nosocomialis'', ''Acinetobacter pitti'' and ''Acinetobacter seifertii''. Habitat ''A. calcoaceticus'' is a soil bacterium. It has been shown to be prevalent in the tiger mosquito ''Aedes albopictus'' microflora. Metabolism Phloroglucinol carboxylic acid is a degradation product excreted by ''A. calcoaceticus'' grown on (+)-catechin Catechin is a flavan-3-ol, a type of secondary metabolite providing antioxidant roles in plants. It belongs to the subgroup of polyphenols called flavonoids. The name of the catechin chemical family derives from ''catechu'', which is the tannic ... as the sole source of carbon. Uses ''A. calcoaceticus' ...
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Enantiopure Drugs
An enantiopure drug is a pharmaceutical that is available in one specific enantiomeric form. Most biological molecules (proteins, sugars, etc.) are present in only one of many chiral forms, so different enantiomers of a chiral drug molecule bind differently (or not at all) to target receptors. Chirality can be observed when the geometric properties of an object is not superimposable with its mirror image. Two forms of a molecule are formed (both mirror images) from a chiral carbon, these two forms are called enantiomers. One enantiomer of a drug may have a desired beneficial effect while the other may cause serious and undesired side effects, or sometimes even beneficial but entirely different effects. The desired enantiomer is known as an eutomer while the undesired enantiomer is known as the distomer. When equal amounts of both enantiomers are found in a mixture, the mixture is known as a racemic mixture. If a mixture for a drug does not have a 1:1 ratio of its enantiomers it is a ...
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Carbapenem Antibiotics
Carbapenems are a class of very effective antibiotic agents most commonly used for the treatment of severe bacterial infections. This class of antibiotics is usually reserved for known or suspected multiple drug resistance, multidrug-resistant (MDR) bacterial infections. Similar to penicillins and cephalosporins, carbapenems are members of the beta lactam class of antibiotics, which kill bacteria by binding to penicillin-binding proteins, thus inhibiting bacterial cell wall synthesis. However, these agents individually exhibit a broader spectrum of activity compared to most cephalosporins and penicillins. Furthermore, carbapenems are typically unaffected by emerging antimicrobial resistance, antibiotic resistance, even to other beta-lactams. Carbapenem antibiotics were originally developed at Merck & Co. from the carbapenem thienamycin, a naturally derived product of ''Streptomyces cattleya''. Concern has arisen in recent years over increasing rates of resistance to carbapenems, as ...
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Penicillin
Penicillins (P, PCN or PEN) are a group of β-lactam antibiotics originally obtained from ''Penicillium'' moulds, principally '' P. chrysogenum'' and '' P. rubens''. Most penicillins in clinical use are synthesised by P. chrysogenum using deep tank fermentation and then purified. A number of natural penicillins have been discovered, but only two purified compounds are in clinical use: penicillin G (intramuscular or intravenous use) and penicillin V (given by mouth). Penicillins were among the first medications to be effective against many bacterial infections caused by staphylococci and streptococci. They are still widely used today for different bacterial infections, though many types of bacteria have developed resistance following extensive use. 10% of the population claims penicillin allergies but because the frequency of positive skin test results decreases by 10% with each year of avoidance, 90% of these patients can tolerate penicillin. Additionally, those with ...
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Adverse Drug Reaction
An adverse drug reaction (ADR) is a harmful, unintended result caused by taking medication. ADRs may occur following a single dose or prolonged administration of a drug or result from the combination of two or more drugs. The meaning of this term differs from the term "side effect" because side effects can be beneficial as well as detrimental. The study of ADRs is the concern of the field known as ''pharmacovigilance''. An adverse drug event (ADE) refers to any unexpected and inappropriate occurrence at the time a drug is used, whether or not associated with the administration of the drug. An ADR is a special type of ADE in which a causative relationship can be shown. ADRs are only one type of medication-related harm, as harm can also be caused by omitting to take indicated medications. Classification ADRs may be classified by e.g. cause and severity. Cause *Type A: Augmented pharmacologic effects - dose dependent and predictable :Type A reactions, which constitute approximate ...
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Cilastatin
Cilastatin inhibits the human enzyme dehydropeptidase. Uses Dehydropeptidase is an enzyme found in the kidney and is responsible for degrading the antibiotic imipenem. Cilastatin can therefore be combined intravenously with imipenem in order to protect it from degradation, prolonging its antibacterial effect. Imipenem alone is an effective antibiotic and can be given without cilastatin. Cilastatin itself does not have antibiotic activity, although it has been proved to be active against a zinc-dependent beta-lactamase that usually confers antibiotic resistance to certain bacteria, more precisely, the carbapenem family of antibiotics. This property is due to the physicochemical similarities between membrane dipeptidase (MDP), the compound it is usually set to target, and the bacterial metallo-beta-lactamase carried by the CphA gene. The combination allows the antibiotic to be more effective by changing the pharmacokinetics involved. Thus imipenem/cilastatin, like amoxicillin/cla ...
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Dehydropeptidase
Dipeptidases are enzymes secreted by enterocytes into the small intestine. Dipeptidases hydrolyze bound pairs of amino acids, called dipeptides. Dipeptidases are secreted onto the brush border of the villi in the small intestine, where they cleave dipeptides into their two component amino acids prior to absorption. They are also found within the enterocytes themselves, performing cytosolic digestion of absorbed dipeptides. Dipeptidases are exopeptidases, classified under EC number 3.4.13. See also * Membrane dipeptidase Membrane dipeptidase (, ''renal dipeptidase'', ''dehydropeptidase I (DPH I)'', ''dipeptidase'', ''aminodipeptidase'', ''dipeptide hydrolase'', ''dipeptidyl hydrolase'', ''nonspecific dipeptidase'', ''glycosyl-phosphatidylinositol-anchored renal di ... References External links * Enzymes EC 3.4.13 {{enzyme-stub ...
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Stenotrophomonas Maltophilia
''Stenotrophomonas maltophilia'' is an aerobic, nonfermentative, Gram-negative bacterium. It is an uncommon bacterium and human infection is difficult to treat. Initially classified as ''Bacterium bookeri'', then renamed ''Pseudomonas maltophilia'', ''S. maltophilia'' was also grouped in the genus ''Xanthomonas'' before eventually becoming the type species of the genus ''Stenotrophomonas'' in 1993. ''S. maltophilia'' is slightly smaller (0.7–1.8 × 0.4–0.7 μm) than other members of the genus. They are motile due to polar flagella, and grow well on MacConkey agar producing pigmented colonies. ''S. maltophilia'' is catalase-positive, oxidase-negative (which distinguishes it from most other members of the genus) and has a positive reaction for extracellular DNase. ''S. maltophilia'' is ubiquitous in aqueous environments, soil, and plants; it has also been used in biotechnology applications. In immunocompromised patients, ''S. maltophilia'' can lead to nosocomial inf ...
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Enterococcus Faecalis
''Enterococcus faecalis'' – formerly classified as part of the group D ''Streptococcus'' system – is a Gram-positive, commensal bacterium inhabiting the gastrointestinal tracts of humans. Like other species in the genus ''Enterococcus'', ''E. faecalis'' is found in healthy humans and can be used as a probiotic. The probiotic strains such as Symbioflor1 and EF-2001 are characterized by the lack of specific genes related to drug resistance and pathogenesis. As an opportunistic pathogen, ''E. faecalis'' can cause life-threatening infections, especially in the nosocomial (hospital) environment, where the naturally high levels of antibiotic resistance found in ''E. faecalis'' contribute to its pathogenicity. ''E. faecalis'' has been frequently found in reinfected, root canal-treated teeth in prevalence values ranging from 30% to 90% of the cases. Re-infected root canal-treated teeth are about nine times more likely to harbor ''E. faecalis'' than cases of primary infections. Physi ...
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Bacteroides Fragilis
''Bacteroides fragilis'' is an anaerobic, Gram-negative, pleomorphic to rod-shaped bacterium. It is part of the normal microbiota of the human colon and is generally commensal, but can cause infection if displaced into the bloodstream or surrounding tissue following surgery, disease, or trauma. Habitat ''Bacteroides fragilis'' resides in the human gastrointestinal tract and is essential to healthy gastrointestinal function such as mucosal immunity and host nutrition. As a mesophile, optimal growth occurs at 37 °C and a pH around 7. Morphology Cells of ''B. fragilis'' are rod-shaped to pleomorphic with a cell size range of 0.5-1.5 x 1.0-6.0 μm.''B. fragilis'' is a Gram-negative bacterium and does not possess flagella or cilia making it immotile. However, it does utilize peritrichous fimbriae for adhesion to other molecular structures. ''B. fragilis'' also utilizes a complex series of surface proteins, lipopolysaccharide chains, and outer membrane vesicles to help su ...
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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 some o ...
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