Pipemidic acid: absorption, distribution, and excretion.

Abstract:

:Pipemidic acid was absorbed well by the oral route. Its peak levels in plasma ranged from 4 to 12 mug/ml at an oral dose of about 50 mg/kg in mice, rats, dogs, monkeys, and men. The protein binding of pipemidic acid was about 20% in dog plasma and about 30% in human serum. Pipemidic acid was distributed to most of the organs and tissues tested at the concentrations comparable to or higher than the plasma level. Its concentrations in bile and urine were much higher than the plasma level. About 25 to 88% of orally administered pipemidic acid was excreted into urine in a bacteriologically active form, the percentage depending on the animals and doses employed. The remainder was excreted into feces in men. The main active principle in vivo was unchanged pipemidic acid itself. The mean lethal dose of pipemidic acid after a single oral dose was more than 16,000 mg/kg in mice. No abnormalities were observed in mice orally receiving pipemidic acid once a day for 4 weeks at doses of 1,000, 2,000, and 4,000 mg/kg per day, and in rats orally receiving the drug once a day for 2 weeks at doses of 400 and 1,600 mg/kg per day.

authors

Shimizu M,Nakamura S,Takase Y,Kurobe N

doi

10.1128/aac.7.4.441

subject

Has Abstract

pub_date

1975-04-01 00:00:00

pages

441-6

issue

4

eissn

0066-4804

issn

1098-6596

journal_volume

7

pub_type

杂志文章
  • G484S amino acid substitution in lanosterol 14-alpha demethylase (ERG11) is related to fluconazole resistance in a recurrent Cryptococcus neoformans clinical isolate.

    abstract::Five sequential Cryptococcus neoformans isolates recovered from an AIDS patient with recurrent meningitis were analyzed. Four isolates were fluconazole susceptible, while the fifth isolate developed fluconazole resistance. Analysis of the 14-alpha lanosterol demethylase gene (ERG11) showed a point mutation in the resi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.11.3653-3656.2003

    authors: Rodero L,Mellado E,Rodriguez AC,Salve A,Guelfand L,Cahn P,Cuenca-Estrella M,Davel G,Rodriguez-Tudela JL

    更新日期:2003-11-01 00:00:00

  • Methicillin-resistant Staphylococcus aureus susceptibility testing by an automated system, Autobac I.

    abstract::The Autobac I system was used to evaluate the antibiotic susceptibility pattern of methicillin-resistant Staphylococcus aureus isolates. The results of the Autobac I were compared with the results of the disk diffusion method. The disk diffusion susceptibility pattern showed resistance to methicillin/oxacillin, penici...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.13.5.837

    authors: Cleary TJ,Maurer D

    更新日期:1978-05-01 00:00:00

  • Self-resistance and cell wall composition in the glycopeptide producer Amycolatopsis balhimycina.

    abstract::The prevailing resistance mechanism against glycopeptides in Gram-positive pathogens involves reprogramming the biosynthesis of peptidoglycan precursors, resulting in d-alanyl-d-lactate depsipeptide termini. Amycolatopsis balhimycina produces the vancomycin-like glycopeptide balhimycin and therefore has to protect its...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01372-10

    authors: Schäberle TF,Vollmer W,Frasch HJ,Hüttel S,Kulik A,Röttgen M,von Thaler AK,Wohlleben W,Stegmann E

    更新日期:2011-09-01 00:00:00

  • Rifabutin Is Active against Mycobacterium abscessus Complex.

    abstract::Lung infections caused by Mycobacterium abscessus are emerging as a global threat to individuals with cystic fibrosis and to other patient groups. Recent evidence for human-to-human transmission worsens the situation. M. abscessus is an intrinsically multidrug-resistant pathogen showing resistance to even standard ant...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00155-17

    authors: Aziz DB,Low JL,Wu ML,Gengenbacher M,Teo JWP,Dartois V,Dick T

    更新日期:2017-05-24 00:00:00

  • Triazole-based compound as a candidate to develop novel medicines to treat toxoplasmosis.

    abstract::This article reports anti-Toxoplasma gondii activity of 3-(thiophen-2-yl)-1,2,4-triazole-5-thione. The compound displayed significant and reproducible antiparasitic effects at nontoxic concentrations for the host cells, with an experimentally determined 50% inhibitory concentration (IC50) at least 30 times better than...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.03832-14

    authors: Dzitko K,Paneth A,Plech T,Pawełczyk J,Węglińska L,Paneth P

    更新日期:2014-12-01 00:00:00

  • Characterization of the inhibition mechanism of HIV-1 nucleocapsid protein chaperone activities by methylated oligoribonucleotides.

    abstract::Since currently available therapies against HIV/AIDS still show important drawbacks, the development of novel anti-HIV treatments is a key issue. We recently characterized methylated oligoribonucleotides (mONs) that extensively inhibit HIV-1 replication in primary T cells at nanomolar concentrations. The mONs were sho...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.05614-11

    authors: Avilov SV,Boudier C,Gottikh M,Darlix JL,Mély Y

    更新日期:2012-02-01 00:00:00

  • Variety of beta-lactamases produced by amoxicillin-clavulanate-resistant Escherichia coli isolated in the northeastern United States.

    abstract::This study analyzed the enzymatic basis and molecular epidemiology of amoxicillin-clavulanate-resistant Escherichia coli isolated by the microbiology laboratory of a United States tertiary care hospital. From October 1998 to December 1999, all E. coli isolates were screened for ampicillin-sulbactam resistance. Of 283 ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.48.5.1520-1525.2004

    authors: Kaye KS,Gold HS,Schwaber MJ,Venkataraman L,Qi Y,De Girolami PC,Samore MH,Anderson G,Rasheed JK,Tenover FC

    更新日期:2004-05-01 00:00:00

  • Efficacy of alcohol-based hand rinses under frequent-use conditions.

    abstract::Fifty volunteers randomly assigned to one of five hand washing agents (10 subjects per agent)--a nonantiseptic liquid soap (control), an antiseptic hand rinse containing 60% isopropyl alcohol (IPA) with emollients (Alc A), an antiseptic hand rinse containing 70% IPA and 0.5% chlorhexidine gluconate with emollients (Al...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1128/aac.30.4.542

    authors: Larson EL,Eke PI,Laughon BE

    更新日期:1986-10-01 00:00:00

  • Antimicrobial activity of curcumin against Helicobacter pylori isolates from India and during infections in mice.

    abstract::Treatment failure is a major cause of concern for the Helicobacter pylori-related gastroduodenal diseases like gastritis, peptic ulcer, and gastric cancer. Curcumin, diferuloylmethane from turmeric, has recently been shown to arrest H. pylori growth. The antibacterial activity of curcumin against 65 clinical isolates ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01242-08

    authors: De R,Kundu P,Swarnakar S,Ramamurthy T,Chowdhury A,Nair GB,Mukhopadhyay AK

    更新日期:2009-04-01 00:00:00

  • Novel functions of an iron-sulfur flavoprotein from Trichomonas vaginalis hydrogenosomes.

    abstract::Iron-sulfur flavoproteins (Isf) are flavin mononucleotide (FMN)- and FeS cluster-containing proteins commonly encountered in anaerobic prokaryotes. However, with the exception of Isf from Methanosarcina thermophila, which participates in oxidative stress management by removing oxygen and hydrogen peroxide, none of the...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02320-13

    authors: Smutná T,Pilarová K,Tarábek J,Tachezy J,Hrdý I

    更新日期:2014-06-01 00:00:00

  • The Race To Find Antivirals for Zika Virus.

    abstract::Zika virus (ZIKV), a flavivirus transmitted by mosquitoes, was an almost neglected pathogen until its introduction in the Americas in 2015 and its subsequent explosive spread throughout the continent, where it has infected millions of people. The virus has caused social and sanitary alarm, mainly due to its associatio...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,评审

    doi:10.1128/AAC.00411-17

    authors: Saiz JC,Martín-Acebes MA

    更新日期:2017-05-24 00:00:00

  • Effects of amphotericin B and fluconazole on the extracellular and intracellular growth of Candida albicans.

    abstract::The effects of amphotericin B and fluconazole on the extracellular and intracellular growth of Candida albicans were studied. With respect to the extracellular growth of C. albicans, antifungal activity was measured in terms of MICs and minimal fungicidal concentrations as well as by determination of the concentration...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.35.11.2275

    authors: van Etten EW,van de Rhee NE,van Kampen KM,Bakker-Woudenberg IA

    更新日期:1991-11-01 00:00:00

  • In vitro selection and in vivo efficacy of piperazine- and alkanediamide-linked bisbenzamidines against Pneumocystis pneumonia in mice.

    abstract::Bisbenzamidines, such as pentamidine isethionate, are aromatic dicationic compounds that are active against Pneumocystis and other microbes but are oftentimes toxic to the host. To identify potential anti-Pneumocystis agents, we synthesized bisbenzamidine derivatives in which the parent compound pentamidine was modifi...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00126-06

    authors: Cushion MT,Walzer PD,Ashbaugh A,Rebholz S,Brubaker R,Vanden Eynde JJ,Mayence A,Huang TL

    更新日期:2006-07-01 00:00:00

  • Specific inhibitors of herpes simplex virus thymidine kinase diminish reactivation of latent virus from explanted murine ganglia.

    abstract::Two specific inhibitors of herpes simplex virus thymidine kinase, N2-phenyl-2'-deoxyguanosine and N2-(m-trifluoromethylphenyl)guanine, were tested for their ability to inhibit the reactivation of virus from explant cultures of latently infected murine trigeminal ganglia. Both compounds significantly diminished the fre...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.34.6.1285

    authors: Leib DA,Ruffner KL,Hildebrand C,Schaffer PA,Wright GE,Coen DM

    更新日期:1990-06-01 00:00:00

  • Linezolid and vancomycin, alone and in combination with rifampin, compared with moxifloxacin against a multidrug-resistant and a vancomycin-tolerant Streptococcus pneumoniae strain in an in vitro pharmacodynamic model.

    abstract::Potential alternatives, including linezolid, adjunctive rifampin, and moxifloxacin, were evaluated against vancomycin-tolerant (P9802-020) and vancomycin-susceptible clinical isolates of Streptococcus pneumoniae in an in vitro pharmacodynamic model. Vancomycin exhibited maximal killing of 2-log(10) CFU/ml against P980...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.47.6.1984-1987.2003

    authors: Cha R,Rybak MJ

    更新日期:2003-06-01 00:00:00

  • Theaflavin-3,3'-digallate and lactic acid combinations reduce herpes simplex virus infectivity.

    abstract::The present study examined the efficacy of using multiple mechanisms as part of a topical microbicide to inactivate herpes simplex virus (HSV) by combining theaflavin-3,3'-digallate (TF-3) and lactic acid (LA) over the pH range of 4.0 to 5.7 to mimic conditions in the female reproductive tract. Six clinical isolates o...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00659-13

    authors: Isaacs CE,Xu W

    更新日期:2013-08-01 00:00:00

  • Ceftazidime resistance in Hafnia alvei.

    abstract::Two morphotypes of Hafnia alvei differed in their susceptibilities to beta-lactam antibiotics. Both produced an inducible Bush group 1 beta-lactamase. Hyperinducibility of this enzyme was associated with reduced susceptibility in one morphotype. ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.37.6.1375

    authors: Thomson KS,Sanders CC,Washington JA 2nd

    更新日期:1993-06-01 00:00:00

  • Effects of flavophospholipol on resistance in fecal Escherichia coli and enterococci of fattening pigs.

    abstract::A "plasmid-curing effect" of multiresistant Escherichia coli by flavophospholipol, an antibiotic used as an antimicrobial growth promoter (AMGP) in animal feeds, has been reported to occur in vitro and in vivo under experimental conditions. In this study, the effect of flavophospholipol under field conditions was stud...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.46.1.110-118.2002

    authors: van den Bogaard AE,Hazen M,Hoyer M,Oostenbach P,Stobberingh EE

    更新日期:2002-01-01 00:00:00

  • Identification of VIM-2-producing Pseudomonas aeruginosa from Tanzania is associated with sequence types 244 and 640 and the location of blaVIM-2 in a TniC integron.

    abstract::Epidemiological data on carbapenemase-producing Gram-negative bacteria on the African continent are limited. Here, we report the identification of VIM-2-producing Pseudomonas aeruginosa isolates in Tanzania. Eight out of 90 clinical isolates of P. aeruginosa from a tertiary care hospital in Dar es Salaam were shown to...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01436-13

    authors: Moyo S,Haldorsen B,Aboud S,Blomberg B,Maselle SY,Sundsfjord A,Langeland N,Samuelsen Ø

    更新日期:2015-01-01 00:00:00

  • Mycobacterium abscessus Smooth and Rough Morphotypes Form Antimicrobial-Tolerant Biofilm Phenotypes but Are Killed by Acetic Acid.

    abstract::Mycobacterium abscessus has emerged as an important pathogen in people with chronic inflammatory lung diseases such as cystic fibrosis, and recent reports suggest that it may be transmissible by fomites. M. abscessus exhibits two major colony morphology variants: a smooth morphotype (MaSm ) and a rough morphotype (MaR...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01782-17

    authors: Clary G,Sasindran SJ,Nesbitt N,Mason L,Cole S,Azad A,McCoy K,Schlesinger LS,Hall-Stoodley L

    更新日期:2018-02-23 00:00:00

  • Dicyclic and tricyclic diaminopyrimidine derivatives as potent inhibitors of Cryptosporidium parvum dihydrofolate reductase: structure-activity and structure-selectivity correlations.

    abstract::A structurally diverse library of 93 lipophilic di- and tricyclic diaminopyrimidine derivatives was tested for the ability to inhibit recombinant dihydrofolate reductase (DHFR) cloned from human and bovine isolates of Cryptosporidium parvum (J. R. Vásquez et al., Mol. Biochem. Parasitol. 79:153-165, 1996). In parallel...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.45.12.3293-3303.2001

    authors: Nelson RG,Rosowsky A

    更新日期:2001-12-01 00:00:00

  • In vitro susceptibility testing methods for caspofungin against Aspergillus and Fusarium isolates.

    abstract::We investigated the relevance of prominent reduction in turbidity macroscopically (MIC) and formation of aberrant hyphal tips microscopically (minimum effective concentration; MEC) in measuring the in vitro activity of caspofungin against Aspergillus and Fusarium. Caspofungin generated low MICs and MECs against Asperg...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.45.1.327-330.2001

    authors: Arikan S,Lozano-Chiu M,Paetznick V,Rex JH

    更新日期:2001-01-01 00:00:00

  • Penicillin-resistant mechanisms in Pseudomonas aeruginosa: effects of penicillin G and carbenicillin on transpeptidase and C -alanine carboxypeptidase activities.

    abstract::A membrane fraction from Pseudomonas aeruginosa KM 338 was shown to catalyze in vitro peptidoglycan synthesis from uridine 5'-diphosphate-N-acetylmuramyl-l-alanyl-d- glutamyl-meso-diaminopimelyl-d-alanyl-d-alanine and uridine 5'-diphosphate-N-acetylglucosamine. Synthesized peptidoglycan was partially cross-linked by t...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.6.6.672

    authors: Suginaka H,Ichikawa A,Kotani S

    更新日期:1974-12-01 00:00:00

  • Effect of prolonged treatment with azithromycin, clarithromycin, or levofloxacin on Chlamydia pneumoniae in a continuous-infection Model.

    abstract::Persistent infections with Chlamydia pneumoniae have been implicated in the development of chronic diseases, such as atherosclerosis and asthma. Although azithromycin, clarithromycin, and levofloxacin are frequently used for the treatment of respiratory C. pneumoniae infections, little is known about the dose and dura...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.46.2.409-412.2002

    authors: Kutlin A,Roblin PM,Hammerschlag MR

    更新日期:2002-02-01 00:00:00

  • Antimicrobial properties of 8-hydroxyserrulat-14-en-19-oic acid for treatment of implant-associated infections.

    abstract::Treatment options are limited for implant-associated infections (IAI) that are mainly caused by biofilm-forming staphylococci. We report here on the activity of the serrulatane compound 8-hydroxyserrulat-14-en-19-oic acid (EN4), a diterpene isolated from the Australian plant Eremophila neglecta. EN4 elicited antimicro...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01735-12

    authors: Nowakowska J,Griesser HJ,Textor M,Landmann R,Khanna N

    更新日期:2013-01-01 00:00:00

  • Two 2-hydroxy-3-alkyl-1,4-naphthoquinones with in vitro and in vivo activities against Toxoplasma gondii.

    abstract::Two 3-alkyl-substituted 2-hydroxy-1,4-naphthoquinones, NSC 113452 (NSC52) and NSC 113455 (NSC55), were evaluated for activity against Toxoplasma gondii in vitro and in murine models of acute toxoplasmosis. In vitro, both NSC52 and NSC55 significantly inhibited intracellular replication of T. gondii. In vivo, each comp...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.42.9.2284

    authors: Khan AA,Nasr M,Araujo FG

    更新日期:1998-09-01 00:00:00

  • Antibodies to nystatin demonstrate polyene sterol specificity and allow immunolabeling of sterols in Saccharomyces cerevisiae.

    abstract::Polyclonal antibodies elicited by injection into rabbits of a nystatin-bovine serum albumin conjugate were reactive with both nystatin and amphotericin B. Upon labeling of polyene-treated Saccharomyces cerevisiae sterol auxotrophs grown on various sterols, nystatin reacted specifically with ergosterol, while amphoteri...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.33.12.2092

    authors: Walker-Caprioglio HM,MacKenzie JM,Parks LW

    更新日期:1989-12-01 00:00:00

  • Mapping of trimethoprim resistance genes from epidemiologically related plasmids.

    abstract::Trimethoprim resistance dihydrofolate reductase genes from plasmids known to be exchanging between human and animal populations were mapped. The dihydrofolate reductase gene has been highly conserved in all plasmids, but differences in the flanking regions provide evidence that the most recent exchange of plasmids bet...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.31.9.1440

    authors: Campbell IG,Mee BJ

    更新日期:1987-09-01 00:00:00

  • Effects of ionenes on interferon induction by poly(inosinic acid) . poly(cytidylic acid).

    abstract::Depending on the spacing of their positive charges, ionenes, a class of quaternary ammonium polymers, increased the interferon-inducing activity of poly(inosinic acid).poly(cytidylic acid) in mouse L-929 cells, whereas they did not enhance poly(inosinic acid).poly(cytidylic acid) induced interferon production in prima...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.11.4.756

    authors: Clercq ED,Janik B,Sommer RG

    更新日期:1977-04-01 00:00:00

  • Novel Mutations Associated with Clofazimine Resistance in Mycobacterium abscessus.

    abstract::Mycobacterium abscessus is a major nontuberculous mycobacterial (NTM) pathogen and is responsible for about 80% of all pulmonary infections caused by rapidly growing mycobacteria. Clofazimine is an effective drug active against M. abscessus, but the mechanism of resistance to clofazimine in M. abscessus is unknown. To...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00544-18

    authors: Chen Y,Chen J,Zhang S,Shi W,Zhang W,Zhu M,Zhang Y

    更新日期:2018-06-26 00:00:00