Pharmacokinetics of ketoconazole in patients with neoplastic diseases.

Abstract:

:Twenty-seven patients with advanced malignancies were given 200 mg of ketoconazole orally every 6 or 12 h. Blood samples were collected during these intervals and after the last dose to determine plasma concentrations and half-lives. The mean plasma concentrations measured after the initial dose were 1.7 +/- 1.1 microgram/ml at 2 h, 0.9 +/- 0.2 microgram/ml at 6 h, and 0.7 +/- 0.4 microgram/ml at 8 h. Plasma concentrations rose significantly in patients on the every-6-h schedule. Concentrations were more variable in patients on the every-12-h schedule, and changes in mean plasma concentrations after 7 and 14 days were not significant. Half-lives ranged from 1.3 to 11.6 h in individual patients. The mean half-life for all patients studied was 3.7 +/- 0.6 h on day 1. The calculated area under the curve was 12.0 +/- 4.7 micrograms-h/ml on day 1; it increased after 7 and 14 days of administration (every-6-h schedule), suggesting plasma binding or wide drug distribution or both. Saturation of storage compartments is also suggested. Less than 1% of the administered dose was recoverable as active drug from the urine over 6 h.

authors

Maksymiuk AW,Levine HB,Bodey GP

doi

10.1128/aac.22.1.43

subject

Has Abstract

pub_date

1982-07-01 00:00:00

pages

43-6

issue

1

eissn

0066-4804

issn

1098-6596

journal_volume

22

pub_type

杂志文章
  • RFI-641, a potent respiratory syncytial virus inhibitor.

    abstract::Human respiratory syncytial virus (RSV), a paramyxovirus, is a major cause of acute upper and lower respiratory tract infections in infants, young children, and adults. RFI-641 is a novel anti-RSV agent with potent in vitro and in vivo activity. RFI-641 is active against both RSV type A and B strains. The viral specif...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.46.3.841-847.2002

    authors: Huntley CC,Weiss WJ,Gazumyan A,Buklan A,Feld B,Hu W,Jones TR,Murphy T,Nikitenko AA,O'Hara B,Prince G,Quartuccio S,Raifeld YE,Wyde P,O'Connell JF

    更新日期:2002-03-01 00:00:00

  • Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.

    abstract::Linezolid was tested against 32 species of uncommonly isolated gram-positive organisms (3,251 strains) by reference MIC methods and found to be highly active (MIC50 range, 0.25 to 2 microg/ml; MIC90 range, 0.25 to 2 microg/ml). Only one isolate (viridans group streptococcus; 0.03% of tested strains) was resistant to l...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01496-06

    authors: Jones RN,Stilwell MG,Hogan PA,Sheehan DJ

    更新日期:2007-04-01 00:00:00

  • Extrusion of penem antibiotics by multicomponent efflux systems MexAB-OprM, MexCD-OprJ, and MexXY-OprM of Pseudomonas aeruginosa.

    abstract::The high intrinsic penem resistance of Pseudomonas aeruginosa is due to the interplay among the outer membrane barrier, the active efflux system MexAB-OprM, and AmpC beta-lactamase. We studied the roles of two other efflux systems, MexCD-OprJ and MexXY-OprM, in penem resistance by overexpressing each system in an AmpC...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.46.8.2696-2699.2002

    authors: Okamoto K,Gotoh N,Nishino T

    更新日期:2002-08-01 00:00:00

  • Inhibition of host cell invasion and intracellular replication of Trypanosoma cruzi by N,N'-bis(benzyl)-substituted polyamine analogs.

    abstract::We studied the effects of two N,N'-bis(benzyl)-substituted polyamine analogs on the capacities of Trypanosoma cruzi to invade and multiply within a mammalian host cell. At concentrations as low as 1 microM, these compounds reduced significantly the infectivity of the parasite for rat heart myoblasts in a time-dependen...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.37.10.2235

    authors: Majumder S,Kierszenbaum F

    更新日期:1993-10-01 00:00:00

  • Selective phosphorylation of antiviral drugs by vaccinia virus thymidine kinase.

    abstract::The antiviral activity of a new series of thymidine analogs was determined against vaccinia virus (VV), cowpox virus (CV), herpes simplex virus, and varicella-zoster virus. Several compounds were identified that had good activity against each of the viruses, including a set of novel 5-substituted deoxyuridine analogs....

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.01447-06

    authors: Prichard MN,Keith KA,Johnson MP,Harden EA,McBrayer A,Luo M,Qiu S,Chattopadhyay D,Fan X,Torrence PF,Kern ER

    更新日期:2007-05-01 00:00:00

  • Inducible high resistance to colistin in Proteus strains.

    abstract::Wild-type Proteus strains are usually resistant to colistin. We have observed an increase in the level of colistin resistance in four clinical isolates of P. vulgaris, P. morganii, and P. rettgeri by prior treatment with subinhibitory concentrations of the drug. The enhanced resistance in these strains was lost after ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.12.1.1

    authors: Shimizu S,Iyobe S,Mitsuhashi S

    更新日期:1977-07-01 00:00:00

  • Activity of ribavirin against Hantaan virus correlates with production of ribavirin-5'-triphosphate, not with inhibition of IMP dehydrogenase.

    abstract::Ribavirin (RBV) is a broad-spectrum antiviral agent that inhibits the production of infectious Hantaan virus (HTNV). Although the mechanism of action of RBV against HTNV is not understood, RBV is metabolized in human cells to both RBV-5'-monophosphate, which inhibits IMP dehydrogenase, resulting in a decrease in intra...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00790-06

    authors: Sun Y,Chung DH,Chu YK,Jonsson CB,Parker WB

    更新日期:2007-01-01 00:00:00

  • 1,5-benzodiazepines, a novel class of hepatitis C virus polymerase nonnucleoside inhibitors.

    abstract::The exogenous control of hepatitis C virus (HCV) replication can be mediated through the inhibition of the RNA-dependent RNA polymerase (RdRp) activity of NS5B. Small-molecule inhibitors of NS5B include nucleoside and nonnucleoside analogs. Here, we report the discovery of a novel class of HCV polymerase nonnucleoside...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00669-08

    authors: Nyanguile O,Pauwels F,Van den Broeck W,Boutton CW,Quirynen L,Ivens T,van der Helm L,Vandercruyssen G,Mostmans W,Delouvroy F,Dehertogh P,Cummings MD,Bonfanti JF,Simmen KA,Raboisson P

    更新日期:2008-12-01 00:00:00

  • Triethyl-n-hexylammonium triethyl-n-hexylboride: a new antimicrobial showing activity against Candida albicans and gram-positive bacteria.

    abstract::The organic salt triethyl-n-hexylammonium triethyl-n-hexylboride (N(2226)B(2226)) has biostatic effects against two gram-positive bacteria, Bacillus subtilis and Micrococcus luteus, and the yeast Candida albicans. Escherichia coli and chicken embryo fibroblasts grown in tissue culture are more refractory to this compo...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.8.4.510

    authors: Rosenthal KS,Storm DR,Ford WT

    更新日期:1975-10-01 00:00:00

  • Evaluation of antimicrobial activities of clarithromycin and 14-hydroxyclarithromycin against three strains of Haemophilus influenzae by using an in vitro pharmacodynamic model.

    abstract::An in vitro pharmacodynamic model was used to simulate the in vivo pharmacokinetics of clarithromycin and 14-hydroxyclarithromycin in order to generate time-kill curves for three clinical isolates of Haemophilus influenzae (isolates 2019, 91-183, and 1746). Representative concentrations in serum or lung tissue and the...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.38.9.2003

    authors: Walker KJ,Larsson AJ,Zabinski RA,Rotschafer JC

    更新日期:1994-09-01 00:00:00

  • Identification of a Novel Gene Associated with High-Level β-Lactam Resistance in Heterogeneous Vancomycin-Intermediate Staphylococcus aureus Strain Mu3 and Methicillin-Resistant S. aureus Strain N315.

    abstract::β-Lactam resistance levels vary among methicillin-resistant Staphylococcus aureus (MRSA) clinical isolates, mediated by chromosomal mutations and exogenous resistance gene mecA However, MRSA resistance mechanisms are incompletely understood. A P440L mutation in the RNA polymerase β' subunit (RpoC) in slow-vancomycin-i...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00712-18

    authors: Matsuo M,Yamamoto N,Hishinuma T,Hiramatsu K

    更新日期:2019-01-29 00:00:00

  • Enhanced Efflux Pump Expression in Candida Mutants Results in Decreased Manogepix Susceptibility.

    abstract::Manogepix is a broad-spectrum antifungal agent that inhibits glycosylphosphatidylinositol (GPI) anchor biosynthesis. Using whole-genome sequencing, we characterized two efflux-mediated mechanisms in the fungal pathogens Candida albicans and Candida parapsilosis that resulted in decreased manogepix susceptibility. In C...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00261-20

    authors: Liston SD,Whitesell L,Kapoor M,Shaw KJ,Cowen LE

    更新日期:2020-04-21 00:00:00

  • Rifampin resistance of Legionella pneumophila is not increased during therapy for experimental Legionnaires disease: study of rifampin resistance using a guinea pig model of Legionnaires disease.

    abstract::Isolates of Legionella pneumophila serogroup 1, obtained from guinea pigs with experimentally induced Legionnaires disease, were tested for rifampin resistance. Thirteen isolates were from animals treated with rifampin alone, four isolates were from animals treated with saline, and three isolates each were from animal...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.35.1.5

    authors: Edelstein PH

    更新日期:1991-01-01 00:00:00

  • In vivo effects of rufloxacin and ciprofloxacin on T-cell subsets and tumor necrosis factor production in mice infected with Bacteroides fragilis.

    abstract::We investigated the in vivo effects of rufloxacin and ciprofloxacin on T-cell subsets and tumor necrosis factor production in mice infected with Bacteroides fragilis. These quinolones did not alter the helper/suppressor ratio but did modulate the kinetics of tumor necrosis factor production in infected animals. This r...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.37.8.1711

    authors: Gollapudi SV,Chuah SK,Harvey T,Thadepalli HD,Thadepalli H

    更新日期:1993-08-01 00:00:00

  • Activities of the modified polyene N-D-ornithyl amphotericin methyl ester and the azoles ICI 153066, Bay n 7133, and Bay l 9139 compared with those of amphotericin B and ketoconazole in the therapy of experimental blastomycosis.

    abstract::We studied the efficacy of new experimental antifungal drugs, which represent molecular modifications of present active agents, in a murine model of blastomycosis. Ketoconazole, previously the best azole drug studied and which is protective when administered orally, was superior to a new oral imidazole, Bay l 9139, an...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.27.3.363

    authors: Lefler E,Brummer E,Perlman AM,Stevens DA

    更新日期:1985-03-01 00:00:00

  • In vitro activities of free and liposomal drugs against Mycobacterium avium-M. intracellulare complex and M. tuberculosis.

    abstract::We compared MICs and MBCs of various free- and liposome-incorporated antimicrobial agents against several patient isolates of Mycobacterium avium-M. intracellulare complex and certain American Type Culture Collection strains of M. avium, M. intracellulare, and Mycobacterium tuberculosis. Seven of 19 agents were select...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.37.12.2584

    authors: Mehta RT,Keyhani A,McQueen TJ,Rosenbaum B,Rolston KV,Tarrand JJ

    更新日期:1993-12-01 00:00:00

  • Evaluation of topical polyinosinic acid-polycytidylic acid in treatment of localized herpes zoster in children with cancer: a randomized, double-blind controlled study.

    abstract::Twenty-four children with cancer and localized herpes zoster were randomized to receive either topical polyinosinic acid-polycytidylic acid [poly(I:C)] or a saline placebo. Solutions containing 1.0 or 2.5 mg of drug per ml were applied to the lesions every 3 h, seven times a day for 7 consecutive days. Serial, standar...

    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.8.3.289

    authors: Feldman S,Hughes WT,Darlington RW,Kim HK

    更新日期:1975-09-01 00:00:00

  • Rifampin: inhibition of ribonucleic acid synthesis after potentiation by amphotericin B in Saccharomyces cerevisiae.

    abstract::The inhibition of Saccharomyces cerevisiae growth by amphotericin B and rifampin was studied. Rifampin alone had no effect on growth or macromolecular syntheses. Lethal amounts of amphotericin B produced a late inhibition of ribonucleic acid (RNA) synthesis simultaneous with the arrest of growth and protein synthesis....

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.5.4.371

    authors: Battaner E,Kumar BV

    更新日期:1974-04-01 00:00:00

  • Method of evaluating effects of antibiotics on bacterial biofilm.

    abstract::Antibiotics are generally not effective against organisms in exopolysaccharide biofilms. A simple method of studying the effect of antibiotics on bacteria in established biofilms is reported. Escherichia coli ATCC 25922 cells grown overnight at 37 degrees C on Mueller-Hinton agar were suspended in buffer and dispensed...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.31.10.1502

    authors: Prosser BL,Taylor D,Dix BA,Cleeland R

    更新日期:1987-10-01 00:00:00

  • HIV-positive nigerian adults harbor significantly higher serum lumefantrine levels than HIV-negative individuals seven days after treatment for Plasmodium falciparum infection.

    abstract::Management of coinfection with malaria and HIV is a major challenge to public health in developing countries, and yet potential drug-drug interactions between antimalarial and antiviral regimens have not been adequately investigated in people with both infections. Each of the constituent components of artemether-lumef...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.02508-12

    authors: Chijioke-Nwauche I,van Wyk A,Nwauche C,Beshir KB,Kaur H,Sutherland CJ

    更新日期:2013-09-01 00:00:00

  • Biochemical study of the comparative inhibition of hepatitis C virus RNA polymerase by VX-222 and filibuvir.

    abstract::Filibuvir and VX-222 are nonnucleoside inhibitors (NNIs) that bind to the thumb II allosteric pocket of the hepatitis C virus (HCV) RNA-dependent RNA polymerase. Both compounds have shown significant promise in clinical trials and, therefore, it is relevant to better understand their mechanisms of inhibition. In our s...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.05438-11

    authors: Yi G,Deval J,Fan B,Cai H,Soulard C,Ranjith-Kumar CT,Smith DB,Blatt L,Beigelman L,Kao CC

    更新日期:2012-02-01 00:00:00

  • Activities of Tedizolid and Linezolid Determined by the Reference Broth Microdilution Method against 3,032 Gram-Positive Bacterial Isolates Collected in Asia-Pacific, Eastern Europe, and Latin American Countries in 2014.

    abstract::Tedizolid and linezolid in vitro activities against 3,032 Gram-positive pathogens collected in Asia-Pacific, Eastern European, and Latin American medical centers during 2014 were assessed. The isolates were tested for susceptibility by the current reference broth microdilution methods. Due to concern over the effect o...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00881-16

    authors: Pfaller MA,Flamm RK,Jones RN,Farrell DJ,Mendes RE

    更新日期:2016-08-22 00:00:00

  • Inhibition of antibacterial activity of himastatin, a new antitumor antibiotic from Streptomyces hygroscopicus, by fatty acid sodium salts.

    abstract::Himastatin, a cyclohexadepsipeptide antibiotic, had in vivo antitumor activity against localized P388 leukemia and B16 melanoma but had no distal site antitumor activity. An in vitro Bacillus subtilis well-agar diffusion assay was employed to test the hypothesis that himastatin was enzymatically inactivated. The activ...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.38.11.2633

    authors: Mamber SW,Brookshire KW,Dean BJ,Firestone RA,Leet JE,Matson JA,Forenza S

    更新日期:1994-11-01 00:00:00

  • Trioxaquines are new antimalarial agents active on all erythrocytic forms, including gametocytes.

    abstract::Malaria is the third most significant cause of infectious disease in the world. The search for new antimalarial chemotherapy has become increasingly urgent due to parasite resistance to classical drugs. Trioxaquines are synthetic hybrid molecules containing a trioxane motif (which is responsible for the antimalarial a...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00967-06

    authors: Benoit-Vical F,Lelièvre J,Berry A,Deymier C,Dechy-Cabaret O,Cazelles J,Loup C,Robert A,Magnaval JF,Meunier B

    更新日期:2007-04-01 00:00:00

  • Enzymatic detachment of Staphylococcus epidermidis biofilms.

    abstract::The gram-positive bacterium Staphylococcus epidermidis is the most common cause of infections associated with catheters and other indwelling medical devices. S. epidermidis produces an extracellular slime that enables it to form adherent biofilms on plastic surfaces. We found that a biofilm-releasing enzyme produced b...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.48.7.2633-2636.2004

    authors: Kaplan JB,Ragunath C,Velliyagounder K,Fine DH,Ramasubbu N

    更新日期:2004-07-01 00:00:00

  • Evaluation of susceptibility of gram-positive and -negative bacteria to human defensins by using radial diffusion assay.

    abstract::Defensins are small cationic bactericidal peptides present abundantly in the granules of polymorphonuclear neutrophils (PMNs). Human PMNs contain four defensins termed HNP-1 to HNP-4. We used a new assay system in agar plates, the radial diffusion assay, to evaluate the effects of human defensins against gram-positive...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.40.10.2280

    authors: Takemura H,Kaku M,Kohno S,Hirakata Y,Tanaka H,Yoshida R,Tomono K,Koga H,Wada A,Hirayama T,Kamihira S

    更新日期:1996-10-01 00:00:00

  • Pharmacokinetics and therapeutic efficacy of gentamicin in an experimental pleural empyema rabbit model.

    abstract::The pharmacokinetics and therapeutic efficacy of gentamicin were investigated in an experimental pleural empyema rabbit model. Pleural effusion was induced by the intrapleural administration of turpentine, and empyema was induced by direct inoculation of the effusion with Klebsiella pneumoniae. Pleural empyema compare...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.31.7.982

    authors: Shohet I,Yellin A,Meyerovitch J,Rubinstein E

    更新日期:1987-07-01 00:00:00

  • Inhibition of gene expression and growth by antisense peptide nucleic acids in a multiresistant beta-lactamase-producing Klebsiella pneumoniae strain.

    abstract::Klebsiella pneumoniae causes common and severe hospital- and community-acquired infections with a high incidence of multidrug resistance. The emergence and spread of beta-lactamase-producing K. pneumoniae strains highlight the need to develop new therapeutic strategies. In this study, we developed antisense peptide nu...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/AAC.00709-06

    authors: Kurupati P,Tan KS,Kumarasinghe G,Poh CL

    更新日期:2007-03-01 00:00:00

  • Randomized comparison of safety and pharmacokinetics of caspofungin, liposomal amphotericin B, and the combination of both in allogeneic hematopoietic stem cell recipients.

    abstract::The combination of liposomal amphotericin B (LAMB) and caspofungin (CAS) holds promise to improve the outcome of opportunistic invasive mycoses with poor prognosis. Little is known, however, about the safety and pharmacokinetics of the combination in patients at high risk for these infections. The safety and pharmacok...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章,多中心研究,随机对照试验

    doi:10.1128/AAC.00425-10

    authors: Groll AH,Silling G,Young C,Schwerdtfeger R,Ostermann H,Heinz WJ,Gerss J,Kolve H,Lanvers-Kaminsky C,Vieira Pinheiro JP,Gammelin S,Cornely OA,Wuerthwein G

    更新日期:2010-10-01 00:00:00

  • In vitro antibacterial activity of AM-1155, a novel 6-fluoro-8-methoxy quinolone.

    abstract::The in vitro antibacterial activity of AM-1155 against a wide variety of clinical isolates was compared with those of other fluoroquinolones. The MICs of AM-1155 for 90% of Staphylococcus aureus, Streptococcus pneumoniae, and Enterococcus faecalis isolates tested were 0.10, 0.39, and 0.78 microgram/ml, respectively. T...

    journal_title:Antimicrobial agents and chemotherapy

    pub_type: 杂志文章

    doi:10.1128/aac.38.3.594

    authors: Wakabayashi E,Mitsuhashi S

    更新日期:1994-03-01 00:00:00