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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/06/23 16:03:22」(JST)

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Lincomycin

Clindamycin. (Note extra chlorine compared to lincomycin, but disregard inversion of image.)

Lincosamides (e.g. lincomycin, clindamycin) are a class of antibiotics.

Mechanism of action

Lincosamides prevent bacteria replicating by interfering with the synthesis of proteins. They bind to the 23s portion of the 50S subunit of bacterial ribosomes and cause premature dissociation of the peptidyl-tRNA from the ribosome.^[1] Lincosamides do not interfere with protein synthesis in human cells (or those of other eukaryotes) because human ribosomes are structurally different from those of bacteria.

History and uses

The first lincosamide to be discovered is lincomycin, isolated from Streptomyces lincolnensis in a soil sample from Lincoln, Nebraska (hence the bacterial name).

Lincomycin has been superseded by clindamycin, which exhibits improved antibacterial activity. Clindamycin also exhibits some activity against parasitic protozoa, and has been used in toxoplasmosis and malaria.

They are normally used to treat staphylococci and streptococci, and have proved useful in treating Bacteroides fragilis and some other anaerobes. They are used in the treatment of Toxic Shock Syndrome and thought to directly block the M protein production that leads to the severe inflammatory response.

Lincosamide antibiotics are one of the classes of antibiotics most associated with pseudomembranous colitis caused by C. difficile.^[2]

Resistance

Target bacteria may alter the drug's binding site (similar to resistance found in macrolides and streptogramins). The resistance mechanism is methylation of the 23s binding site. If this occurs then the bacteria are resistant to both the macrolides and the lincosamides. Also, enzymatic inactivation of clindamycin has been described (rare).

Formulation

The lincosamides, as the hydrochloride salt, are bitter to taste, so for oral formulation they are given as the palmitate esters, or formulated in capsules. Clindamycin is given intravenously as clindamycin phosphate, which is then converted into active clindamycin within the body.

Pharmacodynamics

These are bacteriostatic drugs and antagonists of macrolides and streptogramins.

References

^ The Mechanism of Action of Macrolides, Lincosamides and Streptogramin B Reveals the Nascent Peptide Exit Path in the Ribosome Martin Lovmar and Måns Ehrenberg
^ http://www.nlm.nih.gov/medlineplus/ency/article/000259.htm. Missing or empty |title= (help)

UpToDate Contents

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1. クリンダマイシン：概要 clindamycin an overview
2. メチシリン耐性黄色ブドウ球菌およびバンコマイシン耐性腸球菌の治療のための抗菌薬の
薬理 pharmacology of antimicrobial agents for treatment of methicillin resistant staphylococcus aureus and vancomycin resistant enterococcus
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4. 成人におけるA群レンサ球菌（Streptococcus pyogenes）
性菌血症 group a streptococcal streptococcus pyogenes bacteremia in adults
5. 抗菌薬感受性試験の概要 overview of antibacterial susceptibility testing

English Journal

Genetic lineages and antimicrobial resistance genotypes in Staphylococcus aureus from children with atopic dermatitis: detection of clonal complexes CC1, CC97 and CC398.

Benito D1, Aspiroz C2, Gilaberte Y3,4, Sanmartín R3,4, Hernández-Martin Á5, Alonso M6, Gómez P1, Lozano C1, Torres C1.
Journal of chemotherapy (Florence, Italy).J Chemother.2016 Oct;28(5):359-66. doi: 10.1179/1973947815Y.0000000044. Epub 2016 Jul 25.
The objective was to analyse the genetic lineages of Staphylococcus aureus recovered from nasal and skin samples of atopic dermatitis (AD) paediatric patients, and to characterize the antimicrobial resistance phenotype-genotype and the immune-evasion-cluster (IEC) type of isolates. Forty S. aureus i
PMID 26027683

Novel Structure of Enterococcus faecium-Originated ermB-Positive Tn1546-Like Element in Staphylococcus aureus.

Wan TW1, Hung WC2, Tsai JC3, Lin YT1, Lee H1, Hsueh PR4, Lee TF5, Teng LJ6.
Antimicrobial agents and chemotherapy.Antimicrob Agents Chemother.2016 Sep 23;60(10):6108-14. doi: 10.1128/AAC.01096-16. Print 2016 Oct.
We determined the resistance determinants in 274 erythromycin-resistant methicillin-susceptible Staphylococcus aureus (MSSA) isolates during a 13-year period, 2000 to 2012. The resistance phenotypes, inducible macrolide-lincosamide-streptogramin (iMLS), constitutive MLS (cMLS), and macrolide-strepto
PMID 27480862

Development and validation of a multiclass method for the determination of antibiotic residues in honey using liquid chromatography-tandem mass spectrometry.

El Hawari K1,2, Mokh S1, Doumyati S3, Al Iskandarani M1,3, Verdon E2.
Food additives & contaminants. Part A, Chemistry, analysis, control, exposure & risk assessment.Food Addit Contam Part A Chem Anal Control Expo Risk Assess.2016 Sep 7. [Epub ahead of print]
A new, simple, and fast method has been developed for the determination of multi-class antibiotic residues in honey (sulfonamides, tetracyclines, macrolides, lincosamides, and aminoglycosides). The separation and the determination are carried out by liquid chromatography coupled to mass spectrometry
PMID 27601204