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Chemical Compound Review

clindamycin     N-[2-chloro-1-(3,4,5- trihydroxy-6...

Synonyms: AG-C-17669, SureCN12356681, AC1L1EGQ, BBL005238, CTK6D4956, ...
 
 
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Disease relevance of Clindamycin hydrochloride

  • Epidemics of diarrhea caused by a clindamycin-resistant strain of Clostridium difficile in four hospitals [1].
  • Both treatment regimens--cefoxitin given alone and clindamycin and gentamicin given together--resulted in similar infection rates, drug toxicity, duration of hospitalization, and costs [2].
  • A quantifiable neurologic assessment was used prospectively to evaluate the clinical outcome of patients with AIDS and toxoplasmic encephalitis who were treated with oral clindamycin (600 mg four times a day) and pyrimethamine (75 mg every day) for six weeks [3].
  • BACKGROUND: Babesiosis is a tick-borne, malaria-like illness known to be enzootic in southern New England. A course of clindamycin and quinine is the standard treatment, but this regimen frequently causes adverse reactions and occasionally fails [4].
  • Although treatment with clindamycin and quinine reduces the duration of parasitemia, infection may still persist and recrudesce and side effects are common [5].
 

Psychiatry related information on Clindamycin hydrochloride

 

High impact information on Clindamycin hydrochloride

  • CONCLUSIONS: For the treatment of babesiosis, a regimen of atovaquone and azithromycin is as effective as a regimen of clindamycin and quinine and is associated with fewer adverse reactions [4].
  • The most common adverse effects with atovaquone and azithromycin were diarrhea and rash (each in 8 percent of the subjects); with clindamycin and quinine the most common adverse effects were tinnitus (39 percent), diarrhea (33 percent), and decreased hearing (28 percent) [4].
  • Moreover, parasite death occurs with peculiar kinetics that are identical to those observed after exposure to clindamycin and macrolide antibiotics, which have been proposed to target protein synthesis in the apicoplast [8].
  • Conversely, clindamycin (and functionally related compounds) immediately inhibits plastid replication upon drug application-the earliest effect so far described for these antibiotics [8].
  • MAIN OUTCOME MEASURES: Trends in macrolide use (1993-1999) and resistance and factors associated with resistance, including examination of 2 subtypes, the M phenotype, associated with moderate minimum inhibitory concentrations (MICs), and the MLS(B) phenotype, associated with high MICs and clindamycin resistance [9].
 

Chemical compound and disease context of Clindamycin hydrochloride

 

Biological context of Clindamycin hydrochloride

 

Anatomical context of Clindamycin hydrochloride

  • Ribosomes encoded by these genes are predicted to be sensitive to the lincosamide/macrolide class of antibiotics, and may serve as the functional target for azithromycin, clindamycin, and other protein synthesis inhibitors in Toxoplasma and related parasites [20].
  • These studies indicate that clindamycin colitis in rabbits is caused by overgrowth of a clostridial species, which releases a heat-labile toxic protein of mol wt of 45,000 capable of necrosing colonic epithelial cells [21].
  • The findings that clindamycin markedly inhibits intestinal water transport and induces net secretion in the ileum may explain the reversible watery diarrhea that many patients experience when treated with clindamycin [22].
  • We demonstrated the presence of a toxic substance(s) in the feces of hamsters developing clindamycin-induced enterocolitis [23].
  • Cell-free, sterile filtrates of cecal contents of rabbits with clindamycin colitis contained a toxin that was lethal for mice and cytotoxic for HeLa-cell monolayers [21].
 

Associations of Clindamycin hydrochloride with other chemical compounds

 

Gene context of Clindamycin hydrochloride

  • We examined the suppressive effect of clindamycin (CLDM) on CAZ-induced release of endotoxin by cultured E. coli and the subsequent production of inflammatory cytokines (tumor necrosis factor alpha [TNF-alpha] and interleukin-1 beta [IL-1 beta]) [28].
  • Proton pump inhibitor treatment of clindamycin-treated mice elevated the gastric pH and facilitated the establishment of colonization of the large intestine by vancomycin-resistant Enterococcus spp [29].
  • Here it is shown that the Escherichia coli msbB mutant, which elaborates defective, penta-acylated lipid A, is practically as resistant to a representative set of hydrophobic solutes (rifampin, fusidic acid, erythromycin, clindamycin, and azithromycin) as the parent-type control strain [30].
  • Thus, it is concluded that CYP3A4 appears to account for the largest proportion of the observed P450 catalytic clindamycin S-oxidase activity in vitro, and this activity may be extrapolated to the in vivo condition [31].
  • Of the P450 enzymes examined, only the activity of CYP3A4 was inhibited (approximately 26%) by coincubation with clindamycin (100 microM) [31].
 

Analytical, diagnostic and therapeutic context of Clindamycin hydrochloride

References

  1. Epidemics of diarrhea caused by a clindamycin-resistant strain of Clostridium difficile in four hospitals. Johnson, S., Samore, M.H., Farrow, K.A., Killgore, G.E., Tenover, F.C., Lyras, D., Rood, J.I., DeGirolami, P., Baltch, A.L., Rafferty, M.E., Pear, S.M., Gerding, D.N. N. Engl. J. Med. (1999) [Pubmed]
  2. Risk of infection after penetrating abdominal trauma. Nichols, R.L., Smith, J.W., Klein, D.B., Trunkey, D.D., Cooper, R.H., Adinolfi, M.F., Mills, J. N. Engl. J. Med. (1984) [Pubmed]
  3. Toxoplasmic encephalitis in patients with the acquired immunodeficiency syndrome. Members of the ACTG 077p/ANRS 009 Study Team. Luft, B.J., Hafner, R., Korzun, A.H., Leport, C., Antoniskis, D., Bosler, E.M., Bourland, D.D., Uttamchandani, R., Fuhrer, J., Jacobson, J. N. Engl. J. Med. (1993) [Pubmed]
  4. Atovaquone and azithromycin for the treatment of babesiosis. Krause, P.J., Lepore, T., Sikand, V.K., Gadbaw, J., Burke, G., Telford, S.R., Brassard, P., Pearl, D., Azlanzadeh, J., Christianson, D., McGrath, D., Spielman, A. N. Engl. J. Med. (2000) [Pubmed]
  5. Persistent parasitemia after acute babesiosis. Krause, P.J., Spielman, A., Telford, S.R., Sikand, V.K., McKay, K., Christianson, D., Pollack, R.J., Brassard, P., Magera, J., Ryan, R., Persing, D.H. N. Engl. J. Med. (1998) [Pubmed]
  6. Antimicrobial prophylaxis for contaminated head and neck surgery. Johnson, J.T., Myers, E.N., Thearle, P.B., Sigler, B.A., Schramm, V.L. Laryngoscope (1984) [Pubmed]
  7. Action of clindamycin-phosphate in foreign body infections due to Staphylococcus epidermidis in mice. Fichera, G.A., Pappalardo, C., Nicolosi, V.M., Gismondo, M.R., Stefani, S., Nicoletti, G. Chemioterapia : international journal of the Mediterranean Society of Chemotherapy. (1987) [Pubmed]
  8. A plastid organelle as a drug target in apicomplexan parasites. Fichera, M.E., Roos, D.S. Nature (1997) [Pubmed]
  9. Macrolide resistance among invasive Streptococcus pneumoniae isolates. Hyde, T.B., Gay, K., Stephens, D.S., Vugia, D.J., Pass, M., Johnson, S., Barrett, N.L., Schaffner, W., Cieslak, P.R., Maupin, P.S., Zell, E.R., Jorgensen, J.H., Facklam, R.R., Whitney, C.G. JAMA (2001) [Pubmed]
  10. Subtotal colectomy for refractory pseudomembranous enterocolitis. Boyd, W.C., DenBesten, L. JAMA (1976) [Pubmed]
  11. Clinical presentation of inhalational anthrax following bioterrorism exposure: report of 2 surviving patients. Mayer, T.A., Bersoff-Matcha, S., Murphy, C., Earls, J., Harper, S., Pauze, D., Nguyen, M., Rosenthal, J., Cerva, D., Druckenbrod, G., Hanfling, D., Fatteh, N., Napoli, A., Nayyar, A., Berman, E.L. JAMA (2001) [Pubmed]
  12. Prevention of recurrent staphylococcal skin infections with low-dose oral clindamycin therapy. Klempner, M.S., Styrt, B. JAMA (1988) [Pubmed]
  13. Acute osteomyelitis in a district general hospital. Glover, S.C., McKendrick, M.W., Padfield, C., Geddes, A.M., Dwyer, N.S. Lancet (1982) [Pubmed]
  14. Microbial causes of proven pelvic inflammatory disease and efficacy of clindamycin and tobramycin. Wasserheit, J.N., Bell, T.A., Kiviat, N.B., Wølner-Hanssen, P., Zabriskie, V., Kirby, B.D., Prince, E.C., Holmes, K.K., Stamm, W.E., Eschenbach, D.A. Ann. Intern. Med. (1986) [Pubmed]
  15. Potentiation of opsonization and phagocytosis of Streptococcus pyogenes following growth in the presence of clindamycin. Gemmell, C.G., Peterson, P.K., Schmeling, D., Kim, Y., Mathews, J., Wannamaker, L., Quie, P.G. J. Clin. Invest. (1981) [Pubmed]
  16. Effect of early oral clindamycin on late miscarriage and preterm delivery in asymptomatic women with abnormal vaginal flora and bacterial vaginosis: a randomised controlled trial. Ugwumadu, A., Manyonda, I., Reid, F., Hay, P. Lancet (2003) [Pubmed]
  17. Combination effects of ciprofloxacin, clindamycin, and metronidazole intravenously in volunteers. Deppermann, K.M., Boeckh, M., Grineisen, S., Shokry, F., Borner, K., Koeppe, P., Krasemann, C., Wagner, J., Lode, H. Am. J. Med. (1989) [Pubmed]
  18. Inhibition of peptide bond formation by pleuromutilins: the structure of the 50S ribosomal subunit from Deinococcus radiodurans in complex with tiamulin. Schlünzen, F., Pyetan, E., Fucini, P., Yonath, A., Harms, J.M. Mol. Microbiol. (2004) [Pubmed]
  19. Clinical risk factors for prolonged PT/PTT in abdominal sepsis patients treated with moxalactam or tobramycin plus clindamycin. Baxter, J.G., Marble, D.A., Whitfield, L.R., Wels, P.B., Walczak, P., Schentag, J.J. Ann. Surg. (1985) [Pubmed]
  20. Inhibition of cytoplasmic and organellar protein synthesis in Toxoplasma gondii. Implications for the target of macrolide antibiotics. Beckers, C.J., Roos, D.S., Donald, R.G., Luft, B.J., Schwab, J.C., Cao, Y., Joiner, K.A. J. Clin. Invest. (1995) [Pubmed]
  21. Role of clostridial toxin in the pathogenesis of clindamycin colitis in rabbits. LaMont, J.T., Sonnenblick, E.B., Rothman, S. Gastroenterology (1979) [Pubmed]
  22. Effect of clindamycin on intestinal water and glucose transport in the rat. Giannella, R.A., Serumaga, J., Walls, D., Drake, K.W. Gastroenterology (1981) [Pubmed]
  23. Gastrointestinal and systemic toxicity of fecal extracts from hamsters with clindamycin-induced colitis. Rifkin, G.D., Silva, J., Fekety, R. Gastroenterology (1978) [Pubmed]
  24. Resistance to methicillin and other antibiotics in isolates of Staphylococcus aureus from blood and cerebrospinal fluid, England and Wales, 1989-95. Speller, D.C., Johnson, A.P., James, D., Marples, R.R., Charlett, A., George, R.C. Lancet (1997) [Pubmed]
  25. Tissue concentration of clindamycin and gentamicin near ischaemic ulcers with transvenous injection in Bier's arterial arrest. Burgmann, H., Georgopoulos, A., Graninger, W., Koppensteiner, R., Maca, T., Minar, E., Schneider, B., Stümpflen, A., Ehringer, H. Lancet (1996) [Pubmed]
  26. Inhibition of neutrophil oxidative metabolism by lysosomotropic weak bases. Styrt, B., Klempner, M.S. Blood (1986) [Pubmed]
  27. Inactivation of lincosaminide antibiotics in Staphylococcus. Identification of lincosaminide O-nucleotidyltransferases and comparison of the corresponding resistance genes. Brisson-Noël, A., Delrieu, P., Samain, D., Courvalin, P. J. Biol. Chem. (1988) [Pubmed]
  28. Clindamycin suppresses endotoxin released by ceftazidime-treated Escherichia coli O55:B5 and subsequent production of tumor necrosis factor alpha and interleukin-1 beta. Kishi, K., Hirai, K., Hiramatsu, K., Yamasaki, T., Nasu, M. Antimicrob. Agents Chemother. (1999) [Pubmed]
  29. Suppression of Gastric Acid Production by Proton Pump Inhibitor Treatment Facilitates Colonization of the Large Intestine by Vancomycin-Resistant Enterococcus spp. and Klebsiella pneumoniae in Clindamycin-Treated Mice. Stiefel, U., Rao, A., Pultz, M.J., Jump, R.L., Aron, D.C., Donskey, C.J. Antimicrob. Agents Chemother. (2006) [Pubmed]
  30. Outer membrane permeability barrier in Escherichia coli mutants that are defective in the late acyltransferases of lipid A biosynthesis. Vaara, M., Nurminen, M. Antimicrob. Agents Chemother. (1999) [Pubmed]
  31. In vitro metabolism of clindamycin in human liver and intestinal microsomes. Wynalda, M.A., Hutzler, J.M., Koets, M.D., Podoll, T., Wienkers, L.C. Drug Metab. Dispos. (2003) [Pubmed]
  32. Prevention of clindamycin-induced colitis in hamsters by Clostridium sordellii antitoxin. Allo, M., Silva, J., Fekety, R., Rifkin, G.D., Waskin, H. Gastroenterology (1979) [Pubmed]
 
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