Lincosamides
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Lincosamides
Lincosamides are a class of antibiotics, which include lincomycin, clindamycin, and pirlimycin. Structure Lincosamides consist of a pyrrolidine ring linked to a pyranose moiety (methylthio-lincosamide) via an amide bond. Hydrolysis of lincosamides, specifically lincomycin, splits the molecule into its building blocks of the sugar and proline moieties. Both of these derivatives can conversely be recombined into the drug itself or a derivative. Synthesis Biosynthesis of lincosamides occurs through a biphasic pathway, in which propylproline and methylthiolincosamide are independently synthesized immediately before condensation of the two precursor molecules. Condensation of the propylproline carboxyl group with the methylthiolincosamide amine group via an amide bond forms ''N''-demethyllincomycin. ''N''-Demethyllincomycin is subsequently Methylation, methylated via S-Adenosyl methionine, ''S''-adenosyl methionine to produce lincomycin A. Lincomycin is naturally produced by bac ...
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Clindamycin Mechanism
Clindamycin is a Lincosamides, lincosamide antibiotic medication used for the treatment of a number of bacterial infections, including osteomyelitis (bone) or joint infections, pelvic inflammatory disease, strep throat, pneumonia, acute otitis media (middle ear infections), and endocarditis. It can also be used to treat acne vulgaris, acne, and some cases of methicillin-resistant Staphylococcus aureus, methicillin-resistant ''Staphylococcus aureus'' (MRSA). In combination with quinine, it can be used to treat malaria. It is available by mouth, by intravenously, injection into a vein, and as a cream or a gel to be applied to the skin or in the vagina. Common side effects include nausea and vomiting, diarrhea, skin rashes, and pain at the site of injection. It increases the risk of hospital-acquired Clostridioides difficile infection, ''Clostridioides difficile'' colitis about fourfold and thus is only recommended for use when other antibiotics are not appropriate. It appears t ...
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Clindamycin
Clindamycin is a lincosamide antibiotic medication used for the treatment of a number of bacterial infections, including osteomyelitis (bone) or joint infections, pelvic inflammatory disease, strep throat, pneumonia, acute otitis media (middle ear infections), and endocarditis. It can also be used to treat acne, and some cases of methicillin-resistant ''Staphylococcus aureus'' (MRSA). In combination with quinine, it can be used to treat malaria. It is available by mouth, by injection into a vein, and as a cream or a gel to be applied to the skin or in the vagina. Common side effects include nausea and vomiting, diarrhea, skin rashes, and pain at the site of injection. It increases the risk of hospital-acquired ''Clostridioides difficile'' colitis about fourfold and thus is only recommended for use when other antibiotics are not appropriate. It appears to be generally safe in pregnancy. It is of the lincosamide class and works by blocking bacteria from making protein. ...
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Pirlimycin
Pirlimycin, sold under the brand name Pirsue, is used in the treatment of mastitis in cattle. It is used as the salt pirlimycin hydrochloride and it belongs to the lincosamide class of antimicrobials. __TOC__ Activity Pirlimycin is active against Gram-positive bacteria, specifically ''Staphylococcus aureus'' and coagulase negative species of ''Staphylococcus'' and ''Streptococcus''. It has no activity against Gram-negative bacteria. Mechanism of action It is bacteriostatic and acts by inhibiting bacterial protein synthesis via binding with the 50S 50 S is the larger subunit of the 70S ribosome of prokaryotes, i.e. bacteria and archaea. It is the site of inhibition for antibiotics such as macrolides, chloramphenicol, clindamycin, and the pleuromutilins. It includes the 5S ribosom ... subunit of the ribosome. References Lincosamides Veterinary drugs Organochlorides {{antibiotic-stub ...
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Lincomycin A Synthesis
Lincomycin is a lincosamide antibiotic that comes from the actinomycete '' Streptomyces lincolnensis''. A related compound, clindamycin, is derived from lincomycin by using thionyl chloride to replace the 7-hydroxy group with a chlorine atom with inversion of chirality. It was released for medical use in September 1964. Uses Although similar in antibacterial spectrum and mechanism of action to macrolides, lincomycin is also effective against other organisms including actinomycetes and some species of ''Mycoplasma'' and ''Plasmodium''. However, because of its adverse effects and toxicity, it is rarely used today and reserved for patients allergic to penicillin or where bacteria have developed resistance. Clinical pharmacology Intramuscular administration of a single dose of 600 mg of Lincomycin produces average peak serum levels of 11.6 μg/mL at 60 min, and maintains therapeutic levels for 17 h to 20 h, for most susceptible gram-positive organ ...
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Macrolide
Macrolides are a class of mostly natural products with a large macrocyclic lactone ring to which one or more deoxy sugars, usually cladinose and desosamine, may be attached. Macrolides belong to the polyketide class of natural products. Some macrolides have antibiotic or antifungal activity and are used as pharmaceutical drugs. Rapamycin is also a macrolide and was originally developed as an antifungal, but has since been used as an immunosuppressant drug and is being investigated as a potential longevity therapeutic. Macrolides are a diverse group with many members of very different properties: * Macrolides with 14-, 15-, or 16-membered rings and two attached sugar molecules are antibiotics that bind to bacterial ribosomes, the key representative being erythromycin. The term "macrolide antibiotics" tend to refer to just this class. * Some macrolides with very large (20+ membered) rings are immunosuppresants, the prototypical one being rapamycin. * Some 23-membered ...
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Bacteriostatic Agent
A bacteriostatic agent or bacteriostat, abbreviated Bstatic, is a biological or chemical agent that stops bacteria from reproducing, while not necessarily killing them otherwise. Depending on their application, bacteriostatic antibiotics, disinfectants, antiseptics and preservatives can be distinguished. When bacteriostatic antimicrobials are used, the duration of therapy must be sufficient to allow host defense mechanisms to eradicate the bacteria. Upon removal of the bacteriostat, the bacteria usually start to grow rapidly. This is in contrast to bactericides, which kill bacteria. Bacteriostats are often used in plastics to prevent growth of bacteria on surfaces. Bacteriostats commonly used in laboratory work include sodium azide (which is acutely toxic) and thiomersal. __TOC__ Bacteriostatic antibiotics Bacteriostatic antibiotics limit the growth of bacteria by interfering with bacterial protein production, DNA replication, or other aspects of bacterial cellular metabolism. Th ...
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Lincomycin
Lincomycin is a lincosamide antibiotic that comes from the actinomycete ''Streptomyces lincolnensis''. A related compound, clindamycin, is derived from lincomycin by using thionyl chloride to replace the 7-hydroxy group with a chlorine atom with inversion of chirality. It was released for medical use in September 1964. Uses Although similar in antibacterial spectrum and mechanism of action to macrolides, lincomycin is also effective against other organisms including actinomycetes and some species of ''Mycoplasma'' and ''Plasmodium''. However, because of its adverse effects and toxicity, it is rarely used today and reserved for patients allergic to penicillin or where bacteria have developed Antibiotic resistance, resistance. Clinical pharmacology Intramuscular administration of a single dose of 600 mg of Lincomycin produces average peak serum levels of 11.6 μg/mL at 60 min, and maintains therapeutic levels for 17 h to 20 h, for most susceptible g ...
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Staphylococcus
''Staphylococcus'', from Ancient Greek σταφυλή (''staphulḗ''), meaning "bunch of grapes", and (''kókkos''), meaning "kernel" or " Kermes", is a genus of Gram-positive bacteria in the family Staphylococcaceae from the order Bacillales. Under the microscope, they appear spherical ( cocci), and form in grape-like clusters. ''Staphylococcus'' species are facultative anaerobic organisms (capable of growth both aerobically and anaerobically). The name was coined in 1880 by Scottish surgeon and bacteriologist Alexander Ogston (1844–1929), following the pattern established five years earlier with the naming of '' Streptococcus''. It combines the prefix "staphylo-" (from ), and suffixed by the (from ). Staphylococcus was one of the leading infections in hospitals and many strains of this bacterium have become antibiotic resistant. Despite strong attempts to get rid of them, staphylococcus bacteria stay present in hospitals, where they can infect people who are most at ...
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Ribosome
Ribosomes () are molecular machine, macromolecular machines, found within all cell (biology), cells, that perform Translation (biology), biological protein synthesis (messenger RNA translation). Ribosomes link amino acids together in the order specified by the codons of messenger RNA molecules to form polypeptide chains. Ribosomes consist of two major components: the small and large ribosomal subunits. Each subunit consists of one or more ribosomal RNA molecules and many ribosomal proteins (). The ribosomes and associated molecules are also known as the ''translational apparatus''. Overview The sequence of DNA that encodes the sequence of the amino acids in a protein is transcribed into a messenger RNA (mRNA) chain. Ribosomes bind to the messenger RNA molecules and use the RNA's sequence of nucleotides to determine the sequence of amino acids needed to generate a protein. Amino acids are selected and carried to the ribosome by transfer RNA (tRNA) molecules, which enter the riboso ...
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Gram-negative Bacteria
Gram-negative bacteria are bacteria that, unlike gram-positive bacteria, do not retain the Crystal violet, crystal violet stain used in the Gram staining method of bacterial differentiation. Their defining characteristic is that their cell envelope consists of a thin peptidoglycan gram-negative cell wall, cell wall sandwiched between an inner (Cytoplasm, cytoplasmic) Cell membrane, membrane and an Bacterial outer membrane, outer membrane. These bacteria are found in all environments that support life on Earth. Within this category, notable species include the model organism ''Escherichia coli'', along with various pathogenic bacteria, such as ''Pseudomonas aeruginosa'', ''Chlamydia trachomatis'', and ''Yersinia pestis''. They pose significant challenges in the medical field due to their outer membrane, which acts as a protective barrier against numerous Antibiotic, antibiotics (including penicillin), Detergent, detergents that would normally damage the inner cell membrane, and the ...
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