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Unbound Medicine.
(carbacephem)
63 results
  • Different antibiotic treatments for group A streptococcal pharyngitis. [Review]
    Cochrane Database Syst Rev. 2016 Sep 11; 9:CD004406.van Driel ML, De Sutter AI, … Christiaens T
  • CONCLUSIONS: There were no clinically relevant differences in symptom resolution when comparing cephalosporins and macrolides with penicillin in the treatment of GABHS tonsillopharyngitis. Limited evidence in adults suggests cephalosporins are more effective than penicillin for relapse, but the NNTB is high. Limited evidence in children suggests carbacephem is more effective than penicillin for symptom resolution. Data on complications are too scarce to draw conclusions. Based on these results and considering the low cost and absence of resistance, penicillin can still be regarded as a first choice treatment for both adults and children. All studies were in high-income countries with low risk of streptococcal complications, so there is need for trials in low-income countries and Aboriginal communities where risk of complications remains high.
  • Kinetic study of the effect of histidines 240 and 164 on TEM-149 enzyme probed by β-lactam inhibitors. [Journal Article]
    Antimicrob Agents Chemother. 2014 Oct; 58(10):6294-6.Perilli M, Mancini A, … Amicosante G
  • In the present study, we performed a detailed kinetic analysis of the enzymes TEM-149, TEM-149(H240), and TEM-149(H164-H240) versus a large panel of inhibitors/inactivators, including penicillins, penems, carbapenems, monobactams, cephamycin, and carbacephem. These compounds behaved as poor substrates versus TEM-149, TEM-149(H240), and TEM-149(H164-H240) β-lactamases, and the Ki (inhibition const…
  • Different antibiotic treatments for group A streptococcal pharyngitis. [Review]
    Cochrane Database Syst Rev. 2013 Apr 30van Driel ML, De Sutter AI, … Christiaens T
  • CONCLUSIONS: Evidence is insufficient to show clinically meaningful differences between antibiotics for GABHS tonsillopharyngitis. Limited evidence in adults suggests cephalosporins are more effective than penicillin for relapse, but the NNTB is high. Limited evidence in children suggests carbacephem is more effective for symptom resolution. Data on complications are too scarce to draw conclusions. Based on these results and considering the low cost and absence of resistance, penicillin can still be recommended as first choice.
  • Different antibiotic treatments for group A streptococcal pharyngitis. [Review]
    Cochrane Database Syst Rev. 2010 Oct 06van Driel ML, De Sutter AI, … Christiaens T
  • CONCLUSIONS: Evidence is insufficient for clinically meaningful differences between antibiotics for GABHS tonsillopharyngitis. Limited evidence in adults suggests cephalosporins are more effective than penicillin for relapse, but the NNTB is high. Limited evidence in children suggests carbacephem is more effective for symptom resolution. Data on complications are too scarce to draw conclusions. Based on these results and considering the low cost and absence of resistance, penicillin can still be recommended as first choice.
  • Novel beta-lactam antibiotics synthesized by amination of catechols using fungal laccase. [Journal Article]
    Chem Pharm Bull (Tokyo). 2008 Jul; 56(7):902-7.Mikolasch A, Wurster M, … Lindequist U
  • Novel cephalosporins, penicillins, and carbacephems were synthesized by amination of catechols with amino-beta-lactams like cefadroxil, amoxicillin, ampicillin and the structurally related carbacephem loracarbef using laccase from Trametes sp. All isolated monoaminated products inhibited the growth of several Gram positive bacterial strains in the agar diffusion assay, among them methicillin-resi…
  • Antimicrobial agents in orthopaedic surgery: Prophylaxis and treatment. [Review]
    Drugs. 2006; 66(8):1089-105.Trampuz A, Zimmerli W
  • The pathogenesis of implant-associated infection involves interaction between the microorganisms (biofilm formation), the implant and the host. Despite improvement of perioperative prophylaxis, orthopaedic implants still remain highly susceptible to bacterial or fungal contamination, generally resulting in persistent implant-associated infection. Therefore, perioperative and life-long prevention …
  • Using steric hindrance to design new inhibitors of class C beta-lactamases. [Journal Article]
    Chem Biol. 2002 Sep; 9(9):971-80.Trehan I, Morandi F, … Shoichet BK
  • beta-lactamases confer resistance to beta-lactam antibiotics such as penicillins and cephalosporins. However, beta-lactams that form an acyl-intermediate with the enzyme but subsequently are hindered from forming a catalytically competent conformation seem to be inhibitors of beta-lactamases. This inhibition may be imparted by specific groups on the ubiquitous R(1) side chain of beta-lactams, suc…
  • Evolving enzyme technology for pharmaceutical applications: case studies. [Review]
    J Ind Microbiol Biotechnol. 1997 Nov-Dec; 19(5-6):334-43.Yeh WK
  • The case studies focus on two types of enzyme applications for pharmaceutical development. Demethylmacrocin O-methyltransferase, macrocin O-methyltransferase (both putatively rate-limiting) and tylosin reductase were purified from Streptomyces fradiae, characterized and the genes manipulated for increasing tylosin biosynthesis in S. fradiae. The rate-limiting enzyme, deacetoxycephalosporin C (DAO…
  • Penetration of loracarbef into the maxillary sinus: a pharmacokinetic assessment. [Journal Article]
    Clin Ther. 1996 Mar-Apr; 18(2):273-84.Stenquist M, Olen L, … Zeckel ML
  • Loracarbef, a beta-lactam antibiotic of the carbacephem class, is active in vitro against pathogens associated with acute maxillary sinusitis. To study the extent and duration of maxillary sinus fluid penetration after administration of loracarbef, 20 patients (10 men, 10 women; average age, 41 +/- 13 years) with acute sinusitis were treated with loracarbef 400 mg every 12 hours for 10 days. A la…
  • Cephalosporin and carbacephem nephrotoxicity. Roles of tubular cell uptake and acylating potential. [Journal Article]
    Biochem Pharmacol. 1996 Feb 23; 51(4):557-61.Tune BM, Hsu CY, Fravert D
  • Three beta-lactams, desacetylcephaloglycin, ampicillin, and loracarbef, were studied to test a hypothesis derived from retrospective analysis of previously studied cephalosporins: that beta-lactam nephrotoxicity develops in approximate proportion to tubular cell antibiotic concentrations and lactam ring reactivities. Concentrations of each beta-lactam (and insulin) in rabbit renal cortex and seru…
  • Pharmacokinetic disposition of loracarbef in healthy young men and women at steady state. [Randomized Controlled Trial]
    J Clin Pharmacol. 1994 Sep; 34(9):924-9.Sitar DS, Hoban DJ, Aoki FY
  • The pharmacokinetic disposition of 200- and 400-mg doses of a novel carbacephem, loracarbef, was determined over a dose interval on day 8, after ingestion of drug doses twice daily for 7 days, in 20 young, healthy volunteers of both genders. Drug was analyzed in plasma, urine, saliva, vaginal secretions, and fecal filtrate. Peak plasma concentration was proportional to dose for both men (4.0 +/- …
  • [Peroral preparations of cephalosporin antibiotics]. [Journal Article]
    Cas Lek Cesk. 1994 Jan 03; 133(1):22-4.Babálová M, Blahová J, … Krcméry V
  • Three successful generations of cephalosporin antibiotics can be divided into parenteral and peroral substances. Both have similar antibacterial and hence therapeutical properties. It is usual to include into the first generation of peroral cephalosporins the so-called phenylglycine, or hydroxyphenylglycine derivatives. The carbacephem variant of Cefaclor (Panoral Lilly), Loracarbef, however, has…
  • Comparative pharmacokinetics of the new oral cephalosporins. [Review]
    Drugs. 1994; 47 Suppl 3:10-9; discussion 19-20.Lode H, Fassbender M, … Koeppe P
  • The comparative pharmacokinetics of the new oral cephalosporins (ester and nonester types), together with that of the first generation carbacephem, loracarbef, are considered in healthy volunteers. Also in this review, pharmacokinetic and microbiological data are combined in order to predict the possible clinical efficacy of this group of agents. Despite apparent similarities in the structure of …
  • Effects of renal dysfunction on the pharmacokinetics of loracarbef. [Journal Article]
    Clin Pharmacol Ther. 1993 Sep; 54(3):311-6.Therasse DG, Farlow DS, … DeSante KA
  • Loracarbef, the first carbacephem antibiotic to undergo clinical development, is excreted primarily unchanged in the urine (> 90%). Data analyzed from subjects with various degrees of renal dysfunction who were given single oral doses of loracarbef indicated a linear relationship between creatinine clearance (CLCR) and plasma clearance [CLP (L/hr) = 0.106.CLCR (ml/min/1.73 m2)]. The mean area und…
  • Pharmacokinetics of new oral cephalosporins, including a new carbacephem. [Review]
    Clin Infect Dis. 1993 May; 16(5):646-53.Fassbender M, Lode H, … Koeppe P
  • This review analyzes the pharmacokinetics of new oral cephalosporins, including esters, non-esters, and the carbacephem loracarbef, in healthy volunteers, as described in the literature and evaluated in several studies of our own. Single-dose studies have demonstrated considerable pharmacokinetic differences among these compounds. Cefixime, cefpodoxime proxetil, and cefetamet pivoxil are characte…
  • Loracarbef: a new orally administered carbacephem antibiotic. [Review]
    Ann Pharmacother. 1993 Mar; 27(3):321-9.Force RW, Nahata MC
  • CONCLUSIONS: Preliminary data indicate that loracarbef may be an alternative agent for the treatment of a variety of community-acquired infections. Additional clinical experience and rigorously controlled comparative clinical trials are necessary to enable practitioners to fully define the therapeutic role of loracarbef.
  • General pharmacology of loracarbef in animals. [Journal Article]
    Arzneimittelforschung. 1993 Jan; 43(1):60-70.Shetler T, Bendele A, … Turk J
  • Loracarbef ((6R, 7S)-7-[(R)-2-amino-2-phenyl-acetamido]-3-chloro-8-oxo-1- azabicyclo [4.2.0]oct-2-ene-2-carboxylic acid, monohydrate, LY 163892, CAS 121961-22-6) is a carbacephem antibiotic targeted for use in the treatment of infectious disease. The potential pharmacological effects of this agent were examined on cardiovascular, respiratory, gastrointestinal, central nervous and autonomic nervou…
  • Pharmacokinetics of loracarbef and interaction with acetylcysteine. [Randomized Controlled Trial]
    Eur J Clin Microbiol Infect Dis. 1992 Sep; 11(9):851-5.Roller S, Lode H, … Koeppe P
  • A study was conducted to evaluate the pharmacokinetics of loracarbef, a new synthetic oral carbacephem antibiotic, following administration of 400 mg in normal male volunteers. The influence of food and possible interaction with acetylcysteine, a commonly used mucolytic agent, was also studied. Twelve healthy volunteers participated in the study and randomly received an oral dose of 400 mg loraca…
  • Loracarbef vs. cefaclor in pediatric skin and skin structure infections. [Randomized Controlled Trial]
    Pediatr Infect Dis J. 1992 Aug; 11(8 Suppl):S27-30.Hanfling MJ, Hausinger SA, Squires J
  • A double blind, randomized clinical trial involving 214 children, ages 6 months to 12 years, compared the safety and effectiveness of the new carbacephem loracarbef and the cephalosporin cefaclor for the treatment of skin and skin structure infections. The two agents were given primarily as oral suspensions. Dosages were 15 mg/kg/day in two divided doses for loracarbef and 20 mg/kg/day in three d…
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