[In vitro and in vivo antibacterial activities of pazufloxacin mesilate, a new injectable quinolone]
| العنوان: | [In vitro and in vivo antibacterial activities of pazufloxacin mesilate, a new injectable quinolone] |
|---|---|
| المؤلفون: | Nobuhiko, Nomura, Junichi, Mitsuyama, Yousuke, Furuta, Hisashi, Yamada, Mitsunori, Nakata, Toshiko, Fukuda, Hiroshi, Yamada, Masahiro, Takahata, Shinzaburo, Minami |
| المصدر: | The Japanese journal of antibiotics. 55(4) |
| سنة النشر: | 2002 |
| مصطلحات موضوعية: | DNA Topoisomerase IV, Male, Cilastatin, Imipenem Drug Combination, Microbial Sensitivity Tests, Gram-Positive Bacteria, Ceftazidime, Mice, Anti-Infective Agents, Gram-Negative Bacteria, Oxazines, Animals, Humans, Topoisomerase II Inhibitors, Infusions, Intravenous, 4-Quinolones, Dose-Response Relationship, Drug, Ceftriaxone, Meropenem, Anti-Bacterial Agents, Rats, Drug Combinations, Imipenem, Cilastatin, beta-Alanine, Ampicillin, Female, Methicillin Resistance, Thienamycins, Topoisomerase I Inhibitors, Fluoroquinolones |
| الوصف: | We investigated the in vitro and in vivo antibacterial activities of pazufloxacin mesilate (PZFX mesilate), a new injectable quinolone, and obtained the following results. 1) The MIC50 and MIC90 values of PZFX against clinically isolated Gram-positive and -negative bacteria, ranged from 0.0125 to 12.5 micrograms/ml and 0.025 to 100 micrograms/ml, respectively. PZFX showed broad spectrum activity. The antibacterial activities of PZFX against quinolone-susceptible, methicillin-resistant Staphylococcus aureus, beta-lactamase-negative, ampicillin-resistant Haemophilus influenzae, extended spectrum beta-lactamase possessing Klebsiella pneumoniae and imipenem/cilastatine (IPM/CS)-resistant Pseudomonas aeruginosa were superior to those of ceftazidime (CAZ), ceftriaxone, IPM/CS, meropenem and panipenem/betamipron. 2) PZFX showed superior bactericidal activity against S. aureus, Escherichia coli, Proteus mirabilis, Serratia marcescens and P. aeruginosa to those of CAZ and IPM/CS after treatment for 15 minutes at the drug concentration equivalent to that in human serum at clinical dose to be continued for 15 minutes. 3) CAZ and IPM/CS had no bactericidal activity at the 16 times of MIC against P. aeruginosa in human polymorphonuclear leucocytes, while PZFX exhibited potent bactericidal activity in a dose-dependent manner against such bacteria. 4) PZFX inhibited both DNA gyrase and topoisomerase IV from S. aureus at nearly the same level. PZFX showed poor inhibitory activity against topoisomerase II from human placenta and showed high selectivity to bacterial topoisomerase. 5) PZFX mesilate showed superior therapeutic activity to that of CAZ with following infection model caused by S. aureus and P. aeruginosa or each; systemic infection with cyclophosphamide-treated mice, systemic infection in mice with high challenge doses, CMC pouch infection in rat, and calculus infection in rat bladder. 6) Intravenous administration of PZFX with high plasma concentration just after administration, showed more excellent therapeutic effect against the rat intraperitoneal infection, than p.o. and s.c. administration. |
| تدمد: | 0368-2781 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=pmid________::ee6b645d4774c0f5ba1ffb97896d1816 https://pubmed.ncbi.nlm.nih.gov/12378871 |
| رقم الانضمام: | edsair.pmid..........ee6b645d4774c0f5ba1ffb97896d1816 |
| قاعدة البيانات: | OpenAIRE |
| ResultId |
1 |
|---|---|
| Header |
edsair OpenAIRE edsair.pmid..........ee6b645d4774c0f5ba1ffb97896d1816 758 3 unknown 757.806030273438 |
| PLink |
https://search.ebscohost.com/login.aspx?direct=true&site=eds-live&scope=site&db=edsair&AN=edsair.pmid..........ee6b645d4774c0f5ba1ffb97896d1816&custid=s6537998&authtype=sso |
| FullText |
Array
(
[Availability] => 0
)
Array ( [0] => Array ( [Url] => https://explore.openaire.eu/search/publication?articleId=pmid________::ee6b645d4774c0f5ba1ffb97896d1816# [Name] => EDS - OpenAIRE [Category] => fullText [Text] => View record in OpenAIRE [MouseOverText] => View record in OpenAIRE ) ) |
| Items |
Array
(
[Name] => Title
[Label] => Title
[Group] => Ti
[Data] => [In vitro and in vivo antibacterial activities of pazufloxacin mesilate, a new injectable quinolone]
)
Array ( [Name] => Author [Label] => Authors [Group] => Au [Data] => <searchLink fieldCode="AR" term="%22Nobuhiko%2C+Nomura%22">Nobuhiko, Nomura</searchLink><br /><searchLink fieldCode="AR" term="%22Junichi%2C+Mitsuyama%22">Junichi, Mitsuyama</searchLink><br /><searchLink fieldCode="AR" term="%22Yousuke%2C+Furuta%22">Yousuke, Furuta</searchLink><br /><searchLink fieldCode="AR" term="%22Hisashi%2C+Yamada%22">Hisashi, Yamada</searchLink><br /><searchLink fieldCode="AR" term="%22Mitsunori%2C+Nakata%22">Mitsunori, Nakata</searchLink><br /><searchLink fieldCode="AR" term="%22Toshiko%2C+Fukuda%22">Toshiko, Fukuda</searchLink><br /><searchLink fieldCode="AR" term="%22Hiroshi%2C+Yamada%22">Hiroshi, Yamada</searchLink><br /><searchLink fieldCode="AR" term="%22Masahiro%2C+Takahata%22">Masahiro, Takahata</searchLink><br /><searchLink fieldCode="AR" term="%22Shinzaburo%2C+Minami%22">Shinzaburo, Minami</searchLink> ) Array ( [Name] => TitleSource [Label] => Source [Group] => Src [Data] => <i>The Japanese journal of antibiotics</i>. 55(4) ) Array ( [Name] => DatePubCY [Label] => Publication Year [Group] => Date [Data] => 2002 ) Array ( [Name] => Subject [Label] => Subject Terms [Group] => Su [Data] => <searchLink fieldCode="DE" term="%22DNA+Topoisomerase+IV%22">DNA Topoisomerase IV</searchLink><br /><searchLink fieldCode="DE" term="%22Male%22">Male</searchLink><br /><searchLink fieldCode="DE" term="%22Cilastatin%2C+Imipenem+Drug+Combination%22">Cilastatin, Imipenem Drug Combination</searchLink><br /><searchLink fieldCode="DE" term="%22Microbial+Sensitivity+Tests%22">Microbial Sensitivity Tests</searchLink><br /><searchLink fieldCode="DE" term="%22Gram-Positive+Bacteria%22">Gram-Positive Bacteria</searchLink><br /><searchLink fieldCode="DE" term="%22Ceftazidime%22">Ceftazidime</searchLink><br /><searchLink fieldCode="DE" term="%22Mice%22">Mice</searchLink><br /><searchLink fieldCode="DE" term="%22Anti-Infective+Agents%22">Anti-Infective Agents</searchLink><br /><searchLink fieldCode="DE" term="%22Gram-Negative+Bacteria%22">Gram-Negative Bacteria</searchLink><br /><searchLink fieldCode="DE" term="%22Oxazines%22">Oxazines</searchLink><br /><searchLink fieldCode="DE" term="%22Animals%22">Animals</searchLink><br /><searchLink fieldCode="DE" term="%22Humans%22">Humans</searchLink><br /><searchLink fieldCode="DE" term="%22Topoisomerase+II+Inhibitors%22">Topoisomerase II Inhibitors</searchLink><br /><searchLink fieldCode="DE" term="%22Infusions%2C+Intravenous%22">Infusions, Intravenous</searchLink><br /><searchLink fieldCode="DE" term="%224-Quinolones%22">4-Quinolones</searchLink><br /><searchLink fieldCode="DE" term="%22Dose-Response+Relationship%2C+Drug%22">Dose-Response Relationship, Drug</searchLink><br /><searchLink fieldCode="DE" term="%22Ceftriaxone%22">Ceftriaxone</searchLink><br /><searchLink fieldCode="DE" term="%22Meropenem%22">Meropenem</searchLink><br /><searchLink fieldCode="DE" term="%22Anti-Bacterial+Agents%22">Anti-Bacterial Agents</searchLink><br /><searchLink fieldCode="DE" term="%22Rats%22">Rats</searchLink><br /><searchLink fieldCode="DE" term="%22Drug+Combinations%22">Drug Combinations</searchLink><br /><searchLink fieldCode="DE" term="%22Imipenem%22">Imipenem</searchLink><br /><searchLink fieldCode="DE" term="%22Cilastatin%22">Cilastatin</searchLink><br /><searchLink fieldCode="DE" term="%22beta-Alanine%22">beta-Alanine</searchLink><br /><searchLink fieldCode="DE" term="%22Ampicillin%22">Ampicillin</searchLink><br /><searchLink fieldCode="DE" term="%22Female%22">Female</searchLink><br /><searchLink fieldCode="DE" term="%22Methicillin+Resistance%22">Methicillin Resistance</searchLink><br /><searchLink fieldCode="DE" term="%22Thienamycins%22">Thienamycins</searchLink><br /><searchLink fieldCode="DE" term="%22Topoisomerase+I+Inhibitors%22">Topoisomerase I Inhibitors</searchLink><br /><searchLink fieldCode="DE" term="%22Fluoroquinolones%22">Fluoroquinolones</searchLink> ) Array ( [Name] => Abstract [Label] => Description [Group] => Ab [Data] => We investigated the in vitro and in vivo antibacterial activities of pazufloxacin mesilate (PZFX mesilate), a new injectable quinolone, and obtained the following results. 1) The MIC50 and MIC90 values of PZFX against clinically isolated Gram-positive and -negative bacteria, ranged from 0.0125 to 12.5 micrograms/ml and 0.025 to 100 micrograms/ml, respectively. PZFX showed broad spectrum activity. The antibacterial activities of PZFX against quinolone-susceptible, methicillin-resistant Staphylococcus aureus, beta-lactamase-negative, ampicillin-resistant Haemophilus influenzae, extended spectrum beta-lactamase possessing Klebsiella pneumoniae and imipenem/cilastatine (IPM/CS)-resistant Pseudomonas aeruginosa were superior to those of ceftazidime (CAZ), ceftriaxone, IPM/CS, meropenem and panipenem/betamipron. 2) PZFX showed superior bactericidal activity against S. aureus, Escherichia coli, Proteus mirabilis, Serratia marcescens and P. aeruginosa to those of CAZ and IPM/CS after treatment for 15 minutes at the drug concentration equivalent to that in human serum at clinical dose to be continued for 15 minutes. 3) CAZ and IPM/CS had no bactericidal activity at the 16 times of MIC against P. aeruginosa in human polymorphonuclear leucocytes, while PZFX exhibited potent bactericidal activity in a dose-dependent manner against such bacteria. 4) PZFX inhibited both DNA gyrase and topoisomerase IV from S. aureus at nearly the same level. PZFX showed poor inhibitory activity against topoisomerase II from human placenta and showed high selectivity to bacterial topoisomerase. 5) PZFX mesilate showed superior therapeutic activity to that of CAZ with following infection model caused by S. aureus and P. aeruginosa or each; systemic infection with cyclophosphamide-treated mice, systemic infection in mice with high challenge doses, CMC pouch infection in rat, and calculus infection in rat bladder. 6) Intravenous administration of PZFX with high plasma concentration just after administration, showed more excellent therapeutic effect against the rat intraperitoneal infection, than p.o. and s.c. administration. ) Array ( [Name] => ISSN [Label] => ISSN [Group] => ISSN [Data] => 0368-2781 ) Array ( [Name] => URL [Label] => Access URL [Group] => URL [Data] => <link linkTarget="URL" linkTerm="https://explore.openaire.eu/search/publication?articleId=pmid________::ee6b645d4774c0f5ba1ffb97896d1816" linkWindow="_blank">https://explore.openaire.eu/search/publication?articleId=pmid________::ee6b645d4774c0f5ba1ffb97896d1816</link><br /><link linkTarget="URL" linkTerm="https://pubmed.ncbi.nlm.nih.gov/12378871" linkWindow="_blank">https://pubmed.ncbi.nlm.nih.gov/12378871</link> ) Array ( [Name] => AN [Label] => Accession Number [Group] => ID [Data] => edsair.pmid..........ee6b645d4774c0f5ba1ffb97896d1816 ) |
| RecordInfo |
Array
(
[BibEntity] => Array
(
[Languages] => Array
(
[0] => Array
(
[Text] => Undetermined
)
)
[Subjects] => Array
(
[0] => Array
(
[SubjectFull] => DNA Topoisomerase IV
[Type] => general
)
[1] => Array
(
[SubjectFull] => Male
[Type] => general
)
[2] => Array
(
[SubjectFull] => Cilastatin, Imipenem Drug Combination
[Type] => general
)
[3] => Array
(
[SubjectFull] => Microbial Sensitivity Tests
[Type] => general
)
[4] => Array
(
[SubjectFull] => Gram-Positive Bacteria
[Type] => general
)
[5] => Array
(
[SubjectFull] => Ceftazidime
[Type] => general
)
[6] => Array
(
[SubjectFull] => Mice
[Type] => general
)
[7] => Array
(
[SubjectFull] => Anti-Infective Agents
[Type] => general
)
[8] => Array
(
[SubjectFull] => Gram-Negative Bacteria
[Type] => general
)
[9] => Array
(
[SubjectFull] => Oxazines
[Type] => general
)
[10] => Array
(
[SubjectFull] => Animals
[Type] => general
)
[11] => Array
(
[SubjectFull] => Humans
[Type] => general
)
[12] => Array
(
[SubjectFull] => Topoisomerase II Inhibitors
[Type] => general
)
[13] => Array
(
[SubjectFull] => Infusions, Intravenous
[Type] => general
)
[14] => Array
(
[SubjectFull] => 4-Quinolones
[Type] => general
)
[15] => Array
(
[SubjectFull] => Dose-Response Relationship, Drug
[Type] => general
)
[16] => Array
(
[SubjectFull] => Ceftriaxone
[Type] => general
)
[17] => Array
(
[SubjectFull] => Meropenem
[Type] => general
)
[18] => Array
(
[SubjectFull] => Anti-Bacterial Agents
[Type] => general
)
[19] => Array
(
[SubjectFull] => Rats
[Type] => general
)
[20] => Array
(
[SubjectFull] => Drug Combinations
[Type] => general
)
[21] => Array
(
[SubjectFull] => Imipenem
[Type] => general
)
[22] => Array
(
[SubjectFull] => Cilastatin
[Type] => general
)
[23] => Array
(
[SubjectFull] => beta-Alanine
[Type] => general
)
[24] => Array
(
[SubjectFull] => Ampicillin
[Type] => general
)
[25] => Array
(
[SubjectFull] => Female
[Type] => general
)
[26] => Array
(
[SubjectFull] => Methicillin Resistance
[Type] => general
)
[27] => Array
(
[SubjectFull] => Thienamycins
[Type] => general
)
[28] => Array
(
[SubjectFull] => Topoisomerase I Inhibitors
[Type] => general
)
[29] => Array
(
[SubjectFull] => Fluoroquinolones
[Type] => general
)
)
[Titles] => Array
(
[0] => Array
(
[TitleFull] => [In vitro and in vivo antibacterial activities of pazufloxacin mesilate, a new injectable quinolone]
[Type] => main
)
)
)
[BibRelationships] => Array
(
[HasContributorRelationships] => Array
(
[0] => Array
(
[PersonEntity] => Array
(
[Name] => Array
(
[NameFull] => Nobuhiko, Nomura
)
)
)
[1] => Array
(
[PersonEntity] => Array
(
[Name] => Array
(
[NameFull] => Junichi, Mitsuyama
)
)
)
[2] => Array
(
[PersonEntity] => Array
(
[Name] => Array
(
[NameFull] => Yousuke, Furuta
)
)
)
[3] => Array
(
[PersonEntity] => Array
(
[Name] => Array
(
[NameFull] => Hisashi, Yamada
)
)
)
[4] => Array
(
[PersonEntity] => Array
(
[Name] => Array
(
[NameFull] => Mitsunori, Nakata
)
)
)
[5] => Array
(
[PersonEntity] => Array
(
[Name] => Array
(
[NameFull] => Toshiko, Fukuda
)
)
)
[6] => Array
(
[PersonEntity] => Array
(
[Name] => Array
(
[NameFull] => Hiroshi, Yamada
)
)
)
[7] => Array
(
[PersonEntity] => Array
(
[Name] => Array
(
[NameFull] => Masahiro, Takahata
)
)
)
[8] => Array
(
[PersonEntity] => Array
(
[Name] => Array
(
[NameFull] => Shinzaburo, Minami
)
)
)
)
[IsPartOfRelationships] => Array
(
[0] => Array
(
[BibEntity] => Array
(
[Dates] => Array
(
[0] => Array
(
[D] => 16
[M] => 10
[Type] => published
[Y] => 2002
)
)
[Identifiers] => Array
(
[0] => Array
(
[Type] => issn-print
[Value] => 03682781
)
[1] => Array
(
[Type] => issn-locals
[Value] => edsair
)
)
[Numbering] => Array
(
[0] => Array
(
[Type] => volume
[Value] => 55
)
[1] => Array
(
[Type] => issue
[Value] => 4
)
)
[Titles] => Array
(
[0] => Array
(
[TitleFull] => The Japanese journal of antibiotics
[Type] => main
)
)
)
)
)
)
)
|
| IllustrationInfo |