scholarly journals Pharmacokinetic and Pharmacodynamic Integration and Resistance Analysis of Tilmicosin Against Mycoplasma gallisepticum in an In Vitro Dynamic Model

2019 ◽  
Vol 10 ◽  
Author(s):  
Zilong Huang ◽  
Yuzhi Wu ◽  
Zichong Zhou ◽  
Xirui Xia ◽  
Xiaoyan Gu ◽  
...  
Keyword(s):  
Dynamic Model ◽  
Mycoplasma Gallisepticum ◽  
Resistance Analysis

scholarly journals AZD-3043

2012 ◽  
Vol 116 (6) ◽  
pp. 1267-1277 ◽  
Author(s):  
Talmage D. Egan ◽  
Shinju Obara ◽  
Thomas E. Jenkins ◽  
Sarah S. Jaw-Tsai ◽  
Shanti Amagasu ◽  
...  
Keyword(s):  
Dynamic Model ◽  
Metabolic Pathway ◽  
Liver Microsomes ◽  
Allosteric Modulator ◽  
Positive Allosteric Modulator ◽  
Duration Of Action ◽  
Chloride Currents ◽  
Gaba A ◽  
Hypnotic Agent

Background Propofol can be associated with delayed awakening after prolonged infusion. The aim of this study was to characterize the preclinical pharmacology of AZD-3043, a positive allosteric modulator of the γ-aminobutyric acid type A (GABA(A)) receptor containing a metabolically labile ester moiety. The authors postulated that its metabolic pathway would result in a short-acting clinical profile. Methods The effects of AZD-3043, propofol, and propanidid were studied on GABA(A) receptor-mediated chloride currents in embryonic rat cortical neurons. Radioligand binding studies were also performed. The in vitro stability of AZD-3043 in whole blood and liver microsomes was evaluated. The duration of the loss of righting reflex and effects on the electroencephalograph evoked by bolus or infusion intravenous administration were assessed in rats. A mixed-effects kinetic-dynamic model using minipigs permitted exploration of the clinical pharmacology of AZD-3043. Results AZD-3043 potentiated GABA(A) receptor-mediated chloride currents and inhibited [(35)S]tert-butylbicyclophosphorothionate binding to GABA(A) receptors. AZD-3043 was rapidly hydrolyzed in liver microsomes from humans and animals. AZD-3043 produced hypnosis and electroencephalograph depression in rats. Compared with propofol, AZD-3043 was shorter acting in rats and pigs. Computer simulation using the porcine kinetic-dynamic model demonstrated that AZD-3043 has very short 50 and 80% decrement times independent of infusion duration. Conclusions AZD-3043 is a positive allosteric modulator of the GABA(A) receptor in vitro and a sedative-hypnotic agent in vivo. The esterase dependent metabolic pathway results in rapid clearance and short duration of action even for long infusions. AZD-3043 may have clinical potential as a sedative-hypnotic agent with rapid and predictable recovery.

Bactericidal activity of two different dosage regimens of imipenem in an in-vitro dynamic model

1993 ◽  
Vol 32 (2) ◽  
pp. 295-300 ◽  
Author(s):  
Franco Maggiolo ◽  
Alberto Taras ◽  
Stefano Frontespezi ◽  
Francesco Bottari ◽  
Maria Cristina Legnani ◽  
...  
Keyword(s):  
Dynamic Model ◽  
Bactericidal Activity ◽  
Dosage Regimens

scholarly journals Relationship between danofloxacin PK/PD parameters and emergence and mechanism of resistance of Mycoplasma gallisepticum in In Vitro model

PLoS ONE ◽  
2018 ◽  
Vol 13 (8) ◽  
pp. e0202070 ◽  
Author(s):  
Nan Zhang ◽  
Yuzhi Wu ◽  
Zilong Huang ◽  
Chuanzhen Zhang ◽  
Longfei Zhang ◽  
...  
Keyword(s):  
In Vitro Model ◽  
Mycoplasma Gallisepticum ◽  
Mechanism Of Resistance ◽  
Vitro Model

scholarly journals Role of the GapA and CrmA Cytadhesins of Mycoplasma gallisepticum in Promoting Virulence and Host Colonization

2013 ◽  
Vol 81 (5) ◽  
pp. 1618-1624 ◽  
Author(s):  
Ivana Indiková ◽  
Peter Much ◽  
László Stipkovits ◽  
Karin Siebert-Gulle ◽  
Michael P. Szostak ◽  
...  
Keyword(s):  
Point Mutation ◽  
Mycoplasma Gallisepticum ◽  
Chronic Respiratory Disease ◽  
Host Colonization ◽  
Content Type ◽  
Inner Organs ◽  
Avian Pathogen ◽  
Low Passage

ABSTRACTMycoplasma gallisepticumis an important avian pathogen that commonly induces chronic respiratory disease in chicken. To better understand the mycoplasma factors involved in host colonization, chickens were infected via aerosol with two hemadsorption-negative (HA−) mutants, mHAD3 and RCL2, that were derived from a low passage of the pathogenic strain R (Rlow) and are both deficient in the two major cytadhesins GapA and CrmA. After 9 days of infection, chickens were monitored for air sac lesions and for the presence of mycoplasmas in various organs. The data showed that mHAD3, in which thecrmAgene has been disrupted, did not promote efficient colonization or significant air sac lesions. In contrast, the spontaneous HA−RCL2 mutant, which contains a point mutation in thegapAstructural gene, successfully colonized the respiratory tract and displayed an attenuated virulence compared to that of Rlow. It has previously been shownin vitrothat the point mutation of RCL2 spontaneously reverts with a high frequency, resulting in on-and-off switching of the HA phenotype. Detailed analyses further revealed that such an event is not responsible for the observedin vivooutcome, since 98.4% of the mycoplasma populations recovered from RCL2-infected chickens still display the mutation and the associated phenotype. Unlike Rlow, however, RCL2 was unable to colonize inner organs. These findings demonstrate the major role played by the GapA and CrmA proteins inM. gallisepticumhost colonization and virulence.

scholarly journals Gastric digestion of milk protein ingredients: Study using an in vitro dynamic model

2018 ◽  
Vol 101 (8) ◽  
pp. 6842-6852 ◽  
Author(s):  
Xin Wang ◽  
Aiqian Ye ◽  
Quanquan Lin ◽  
Jianzhong Han ◽  
Harjinder Singh
Keyword(s):  
Dynamic Model ◽  
Milk Protein ◽  
Gastric Digestion

scholarly journals Biofilm formation on dental implant surfaces ‐ in vitro dynamic model

2019 ◽  
Vol 30 (S19) ◽  
pp. 8-8
Author(s):  
Honorato Ribeiro‐Vidal ◽  
Maria Del Carmen Sanchez ◽  
Elena Figuero ◽  
David Herrera ◽  
Mariano Sanz
Keyword(s):  
Dynamic Model ◽  
Dental Implant ◽  
Biofilm Formation

A dynamic model for in-vitro evaluation of antimicrobial action by simulation of the pharmacokinetic profiles of antibiotics

1989 ◽  
Vol 23 (3) ◽  
pp. 389-399 ◽  
Author(s):  
S. M. Navashin ◽  
I. P. Fomina ◽  
A. A. Firsov ◽  
V. M. Chernykh ◽  
S. Kuznetsova
Keyword(s):  
Dynamic Model ◽  
Antimicrobial Action ◽  
In Vitro Evaluation ◽  
Pharmacokinetic Profiles
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