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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[edit]

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[edit]

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Lincomycin has been superseded by clindamycin, which exhibits improved antibacterial activity.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[edit]

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[edit]

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[edit]

These are bacteriostatic drugs and antagonists of macrolides and streptogramins.

References[edit]

^ 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. マクロライド系抗菌薬、アザライド系抗菌薬、リンコサミン系抗菌薬、ケトライド系抗菌薬に対する肺炎レンサ球菌の耐性 resistance of streptococcus pneumoniae to the macrolides azalides lincosamides and ketolides
2. 小児における急性中耳炎：治療 acute otitis media in children treatment
3. β-ラクタム系抗菌薬に対する肺炎レンサ球菌の耐性 resistance of streptococcus pneumoniae to beta lactam antibiotics
4. 骨盤内炎症性疾患：治療 pelvic inflammatory disease treatment
5. 侵襲性肺炎球菌（Streptococcus pneumoniae）感染症および菌血症 invasive pneumococcal streptococcus pneumoniae infections and bacteremia

English Journal

Biofilm formation and antimicrobial resistance genes of coagulase-negative staphylococci isolated from cows with mastitis in Argentina.

Srednik ME1, Tremblay YD2, Labrie J2, Archambault M2,3, Jacques M2,3,4, Alicia FC5, Gentilini ER6.
FEMS microbiology letters.FEMS Microbiol Lett.2017 Jan 12. pii: fnx001. doi: 10.1093/femsle/fnx001. [Epub ahead of print]
Mastitis affects the health and welfare of dairy cows worldwide. Coagulase-negative staphylococci (CNS) are known to form biofilms and are increasingly recognized as a cause of persistent bovine intramammary infections. A total of 90 CNS isolated from cows with clinical and subclinical mastitis in A
PMID 28087612

A Novel erm(44) Gene Variant from a Human Staphylococcus saprophyticus Isolate Confers Resistance to Macrolides and Lincosamides but Not Streptogramins.

Strauss C1, Hu Y2, Coates A2, Perreten V3.
Antimicrobial agents and chemotherapy.Antimicrob Agents Chemother.2016 Dec 27;61(1). pii: e01655-16. doi: 10.1128/AAC.01655-16. Print 2017 Jan.
A novel erm(44) gene variant, erm(44)v, has been identified by whole-genome sequencing in a Staphylococcus saprophyticus isolate from the skin of a healthy person. It has the particularity to confer resistance to macrolides and lincosamides but not to streptogramin B when expressed in S. aureus The
PMID 27799208

Antibiotics in Endodontics: a review.

Segura-Egea JJ1, Gould K2, Şen BH3, Jonasson P4, Cotti E5, Mazzoni A6, Sunay H7, Tjäderhane L8,9, Dummer PM10.
International endodontic journal.Int Endod J.2016 Dec 22. doi: 10.1111/iej.12741. [Epub ahead of print]
The overuse of antibiotics and the emergence of antibiotic-resistant bacterial strains is a global concern. This concern is also of importance in terms of the oral microbiota and the use of antibiotics to deal with oral and dental infections. The aim of this paper was to review the current literatur
PMID 28005295

Japanese Journal

長野県諏訪地域における抗菌薬使用量と耐性菌の検出頻度について

具芳明
保健医療科学 60(5), 431-432, 2011-10-00
… MLS (macrolides, lincosamides, and streptogramins) was the most prescribed drug group, followed by beta-lactams other than penicillin and quinolone. …
NAID 110009585556

Phenotypic Differentiation of Macrolide Resistance among Streptococcus pneumoniae Carrying mefA and/or ermB Genes

Kaieda Satoru,Yano Hisakazu,Okitsu Naohiro,Hosaka Yoshio,Okamoto Ryoichi,Inoue Matsuhisa,Takahashi Haruo
Acta medica Nagasakiensia 49(1/2), 19-24, 2004-06-00
… Of the other 40 isolates, 25 carried the ermB gene and 15 carried the both mefA and ermB genes, all of them showed high resistance to clindamycin (MIC?128 μg/mL) and were resistant to macrolides, lincosamides and streptogramin B (MLSB resistance phenotype). …
NAID 110000939710

Distribution of genes encoding resistance to macrolides, lincosamides, and streptogramins among staphylococci

LINA G.
Antimicrob. Agents Chemother. 43, 1062-1066, 1999
NAID 80011052885

Related Pictures

★リンクテーブル★

リンク元	「リンコサミド系薬」

「リンコサミド系薬」

　　[★]

英: lincosamides, lincosamide drugs
関: リンコマイシン。リンコサミド

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リンコサミド系薬剤 : 2 件
リンコサミド系薬物 : 0 件
リンコサミド系薬 : 4 件

[lovmar-1] The Mechanism of Action of Macrolides, Lincosamides and Streptogramin B Reveals the Nascent Peptide Exit Path in the Ribosome Martin Lovmar and Måns Ehrenberg

[2] ttp://www.nlm.nih.gov/medlineplus/ency/article/000259.htm. Missing or empty |title= (help)

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lincosamides