Lincosamides

The lincosamide class of antimicrobial drugs includes lincomycin, clindamycin, and pirlimycin two of these drugs—lincomycin and pirlimycin—are approved for use in food-producing species. Lincosamides are derivatives of an amino acid and a sulfur-containing galactoside. Lincomycin was isolated in 1962 from the fermentation product of Streptomyces lincolnensis subsp. lincolnensis. Clindamycin is a semi-synthetic derivative of lincomycin, and pirlimycin is an analog of clindamycin. 

Several combination products containing lincomycin are approved for use in food-producing species. A lincomycin-spectinomycin product administered in drinking water is used for the treatment and control of respiratory 

The use of lincosamides (see list in Table 1.5) is contraindicated in horses because of the potential risk of serious or fatal enterocolitis and diarrhea. This commonly involves overgrowth of the normal microflora by nonsusceptible bacteria such as Clostridium species. Oral administration of lincomycin to ruminants has also been associated with adverse side effects such as anorexia, ketosis, and diarrhea. Such use is therefore contraindicated in ruminants. 

The limited information available suggests that lincomycin does not pose a risk to organisms in those environments where the drug is known to be used. A 2006 UK study that used targeted monitoring detected a maximum concentration of 21.1 xg lincomycin per liter of streamwater, which compares with the predicted no-effect concentration for lincomycin of 379.4 xg per liter.  

From a food safety perspective, the JECFA has allocated ADI values for lincomycin and pirlimycin. On the basis of JECFA recommendations, CAC MRLs for lincomycin in muscle, liver, kidney, and fat of pigs and chickens, and in cow s milk and for pirlimycin in muscle, liver, kidney, and fat of cattle and in cow s milk have also been established. Details of residue studies reviewed by JECFA to develop MRL recommendations for CCRVDF may be found in monographs published for lincomycin and pirlimycin. 

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Leclercq R, Courvalin P (1991) Bacterial resistance to macrolide, lincosamide, and streptogramin antibiotics by target modification. Antimicrob Agents Chemother 35 1267-1272... 

Clindamycin, a lincosamide derivative, inhibits protein biosynthesis within a unique organelle of the parasite, termed apicoplast. Its mode of action is similar to that of spiramycin. 

Nucleotidylation - the addition of adenylate-residues by Lnu enzymes - can also be the cause of resistance to lincosamide antibiotics in staphylococci and enterococci. A plasmid encoded ADP-ribosylating transferase (Arr-2) that leads to rifampicin resistance has been detected in various Enterobacteriaceae as well as in Pseudomonas aeruginosa. 

Macrolide, lincosamide and streptogramin B resistance (MLSb phenotype) can be linked to specific nucleotide changes within the 23 S rRNA of the large ribosomal subunit, mainly at position A2058 or neighbouring bases (E. coli numbering). This is the... 

Roberts MC, Sutcliffe J, Courvalin P et al (1999) Nomenclature for macrolide and macrolide-lincosamide-streptogramin B resistance determinats. Antimicrob Agents Chemother 43 2823-2830... 

Discuss important preadministration and ongoing assessment activities the nurse should perform on the patient taking a tetracycline, macrolide, or lincosamide. 

The tetracyclines exert their effect by inhibiting bacterial protein syndiesis, which is a process necessary for reproduction of die microorganism. The ultimate effect of diis action is tiiat the bacteria are either destroyed or dieir multiplication rate is slowed. The tetracyclines are bacteriostatic (capable of slowing or retarding die multiplication of bacteria), whereas die macrolides and lincosamides may be bacteriostatic or bactericidal (capable of destroying bacteria). 

SUMMARY DRUG TABLE TETRACYCLINES, MACROLIDES AND LINCOSAMIDES... 

The lincosamides, another group of anti-infectives, are effective against many gram-positive organisms, such as streptococci and staphylococci. However, because of their high potential for toxicity, the lincosamides are usually used only for the treatment of serious infections in which penicillin or erythromycin (a macrolide) is not effective... 

The lincosamides act by inhibiting protein synthesis in susceptible bacteria, causing death. 

These antibiotics are effective in the treatment of infections caused by a wide range of gram-negative and gram-positive microorganisms. The lincosamides are used for the more serious infections. In serious infections they may be used in conjunction with other antibiotics. 

Abdominal pain, esophagitis, nausea, vomiting, diarrhea, skin rash, and blood dyscrasias may be seen with the use of the lincosamides. These drag s also can cause pseudomembranous colitis, which may range from mild to very severe Discontinuing the drag may relieve mild symptoms of pseudomembranous colitis. 

The lincosamides are contraindicated in patients with hypersensitivity to the lincosamides, those with minor bacterial or viral infections, and during lactation and infancy. 

It is important to use these drag with caution in patients with a history of gastrointestinal disorders, renal disease, or liver impairment. The neuromuscular blocking action of die lincosamides poses a danger to patients widi myasthenia gravis (an autoimmune disease manifested by extreme weakness and exhaustion of die muscles). 

When kaolin or aluminum is administered widi die lincosamides, die absorption of the lincosamide is decreased. When the lincosamides are administered with the neuromuscular blocking drag (drag diat are used as adjuncts to anesthetic drag diat cause paralysis of the respiratory system) die action of die neuromuscular blocking drug is enhanced, possibly leading to severe and profound respiratory depression. 

An ongoing assessment is important during therapy widi die tetracyclines, macrolides, and lincosamides. The nurse should take vital signs every 4 hours or as ordered by die primary health care provider. The nurse must notify the primary health care provider if tiiere are changes in the vital signs, such as a significant drop in blood pressure, an increase in die pulse or respiratory rate, or a sudden increase in temperature. 

ORAL ADMINISTRATION. To control the infectious process or prevent a bacterial infection, the nurse must keep several important things in mind when administering the tetracyclines, macrolides, and lincosamides. 

Lincosamides Pbod impairs the absorption of lincomycin. The patient should take nothing by mouth (except water) for 1 to 2 hours before and after taking lincomycin. Oindamycin may be given without regard to food. 

A gene designated msrA has been identified in Staph, aureus which confers resistance to macrolides and streptogramins but not to lincosamides. Its function is unknown but the DNA sequence is homologous to genes coding for known efflux proteins. 

Horinouchi, S. and Weisblum, B. (1982) Nucleotide sequence and functional map of pE194, a plasmid that specifies inducible resistance to macrolide, lincosamide, and streptogramin type B antibodies. Journal of... 

Systemic therapy with a variety of (3-lactams, macro-lides and lincosamides (clindamycin) has been the cornerstone of skin infection therapy for many years [17]. However, topical antibiotics can play an important role in both treatment and prevention of many primary cutaneous bacterial infections commonly seen in the dermatological practice [18], Indeed, while systemic antimicrobials are needed in the complicated infections of skin and skin structure, the milder forms can be successfully treated with topical therapy alone [18], The topical agents used most often in the treatment of superficial cutaneous bacterial infections are tetracyclines, mupirocin, bacitracin, polymyxin B, and neomycin. 

Protein synthesis inhibitors Chloramphenicol Tetracyclines Macrolides Lincosamides Aminoglycosides... 

Linalool, 3 231, 232, 233 24 477, 495, 496, 500-503, 546 acid treatment of, 24 502 epoxidation of, 24 502 main producers of, 24 501 Linalool oxide, 24 502 Linalyl, 24 479 Linalyl acetate, 24 501 Linalyl alcohol, 24 500 Linalyl esters, 3 231 Linalyl oxide, 24 503 Lincomycin, registered for use in aquaculture in Japan, 3 221t Lincosamide, bacterial resistance mechanisms, 3 32t Lindane, 13 145-147... 

Tetracyclines, quinolones, macrolides, sulfonamides, lincosamides, diamino-pyrimidine derivatives... 

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