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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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Clindamycin. (Note extra chlorine compared to lincomycin, but disregard inversion of image.)
Lincosamides (e.g. lincomycin, clindamycin) are a class of antibiotics.
Contents
- 1 Mechanism of action
- 2 History and uses
- 3 Resistance
- 4 Formulation
- 5 Pharmacodynamics
- 6 Further reading
- 7 References
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Lincomycin has been superseded by clindamycin, which exhibits improved antibacterial activity.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.
Further reading
- Van Bambeke F. Mechanisms of action. In Armstrong D, Cohen J. Infectious diseases. Mosby, London, 1999, pp7/1.1-7/1.14
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.
Antibacterials: protein synthesis inhibitors (J01A, J01B, J01F, J01G, QJ01XQ)
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30S |
Aminoglycosides
(initiation inhibitors) |
-mycin (Streptomyces) |
- Streptomycin#
- Dihydrostreptomycin
- Neomycin#
- Framycetin
- Paromomycin
- Ribostamycin
- Kanamycin#
- Amikacin
- Arbekacin
- Bekanamycin
- Dibekacin
- Tobramycin
- Spectinomycin#
- Hygromycin B
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-micin (Micromonospora) |
- Gentamicin#
- Netilmicin
- Sisomicin
- Isepamicin
|
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Tetracycline antibiotics
(tRNA binding) |
Tetracyclines |
- Doxycycline#
- Chlortetracycline
- Clomocycline
- Demeclocycline
- Lymecycline
- Meclocycline
- Metacycline
- Minocycline
- Oxytetracycline
- Penimepicycline
- Rolitetracycline
- Tetracycline
|
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Glycylcyclines |
|
|
|
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50S |
Oxazolidinone
(initiation inhibitors) |
- Eperezolid
- Linezolid
- Posizolid
- Radezolid
- Ranbezolid
- Sutezolid
- Tedizolid
|
|
Peptidyl transferase |
Amphenicols |
- Chloramphenicol#
- Azidamfenicol
- Thiamphenicol
- Florfenicol
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Pleuromutilins |
- Retapamulin
- Tiamulin
- Valnemulin
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|
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MLS (transpeptidation/translocation) |
Macrolides |
- Azithromycin#
- Clarithromycin
- Dirithromycin
- Erythromycin#
- Flurithromycin
- Josamycin
- Midecamycin
- Miocamycin
- Oleandomycin
- Rokitamycin
- Roxithromycin
- Spiramycin
- Troleandomycin
- Tylosin
- Ketolides
- Telithromycin
- Cethromycin
- Solithromycin†
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Lincosamides |
- Clindamycin#
- Lincomycin
- Pirlimycin
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Streptogramins |
- Pristinamycin
- Quinupristin/dalfopristin
- Virginiamycin
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EF-G |
|
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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gr+f/gr+a (t)/gr-p (c)/gr-o
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drug (J1p, w, n, m, vacc)
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UpToDate Contents
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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
Japanese Journal
- 誘導型MLSB耐性黄色ブドウ球菌におけるマクロライド系薬の耐性誘導能の定量化
- 遠藤 菊太郎,武田 龍馬,伊藤 三佳
- 北海道科学大学研究紀要 = Bulletin of Hokkaido University of Science (39), 21-26, 2015-03-30
- NAID 120005574669
- MLSB構成型耐性黄色ブドウ球菌に対するYM133の特異的作用機序
- 遠藤 菊太郎,伊藤 三佳
- 北海道科学大学研究紀要 = Bulletin of Hokkaido University of Science (39), 15-20, 2015-03-30
- NAID 120005574668
- 誘導型MLS[B]耐性黄色ブドウ球菌におけるマクロライド系薬の耐性誘導能の定量化
- 遠藤 菊太郎,武田 龍馬,伊藤 三佳
- 研究紀要 = Bulletin of Hokkaido University of Science (39), 21-26, 2014
- NAID 40020456704
Related Links
- lincosamide (lin-kōs'a-mīd), One of a class of antibiotics that work by inhibition of protein synthesis. ... Because all erythromycin-resistant strains were also resistant to clindamycin (data not shown), we deduced the resistance ...
- References for "Lincosamide" online, at universities and in literature... cyclopaedia.net ... Antibiotics Simplified Jason C. Gallagher, 2013 Antibiotics Simplified, Third Edition is a best-selling, succinct guide designed to bridge ...
Related Pictures
![lincosamide, class), 化学物質, struct](https://1mg.info/0/8/0/2856.jpg)
![Clindamycin is a lincosamide](https://1mg.info/0/8/0/2857.jpg)
![lincosamide, class), 化学物質, 構造](https://1mg.info/0/8/0/2858.jpg)
![drug (lincosamide class), chemical struct](https://1mg.info/0/8/0/2859.jpg)
![lincosamide, class), 化学物質, struct](https://1mg.info/0/8/0/2860.jpg)
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