Newer Antibacterial and Antimycotic Drugs: Critical Appraisal

McHenry, Martin C.; Fieker, Dan H.

doi:10.1016/s0025-7125(16)31745-x

Cited by 8 publications

(2 citation statements)

References 200 publications

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“…Furthermore, longer dosing intervals appear to slow the appearance of the so-called 'adaptive postexposure resistance' phenomenon, while persistent low-level exposure of a given pathogen to amikacin may markedly reduce the antimicrobial activity of this drug (Karlowsky et al, 1994). Table 1 Pharmacokinetic variables calculated for amikacin through compartmental analysis, after either the IV or IM administration of 25 mg/kg of amikacin sulphate once a day for three days It has been postulated that amikacin is less nephrotoxic than gentamicin (McHenry and Fieker, 1978;Conzelman, 1980), probably due to a lower uptake by the renal cells (Brown and Riviere, 1991), hence the lack of toxicity observed as far as the serum variables assessed are concerned. However, histological damage cannot be ruled out.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics and renal toxicity of three once-a-day doses of amikacin in cows

López

Gutiérrez

Velázquez

et al. 2005

Acta Veterinaria Hungarica

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Pharmacokinetic variables of amikacin in cows were determined after administration of amikacin sulphate either intravenously (IV) or intramuscularly (IM) at a dose of 25 mg/kg per day for three days. Amikacin concentrations at time zero and maximum serum concentrations were 240.8 µg/mL and 122.53 µg/mL, respectively. The elimination half-life remained unchanged during the three days of administration (T ½β = 1.33 ± 0.029 h for the IV route and T ½β = 2.75 ± 0.38 h for the IM route). Apparent volumes of distribution suggest limited distribution out of the central compartment (Vd AUC = 0.154 ± 0.005 L/kg; Vd c = 36.50 ± 2.35 L; Vd ss = 0.092 ± 0.004 L/kg). Bioavailability after IM administration was 95%. Serum profiles of urea, creatinine, albumin, electrolytes and pH after 5-day treatment with amikacin at a dose of 25 mg/kg per day IM revealed no changes. Assessment of diffusion of amikacin to milk by a commercially available screening method to detect antibiotic residues revealed that amikacin could not be detected by the fifth milking period after the last treatment. These results suggest that it would be rational to use a large single-daily dose of amikacin for future clinical trials in cows.

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetics and renal toxicity of three once-a-day doses of amikacin in cows

López

Gutiérrez

Velázquez

et al. 2005

Acta Veterinaria Hungarica

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“…SPC is an aminocyclitol antibiotic resembling kanamycin and gentamicin but is not an aminoglycoside (28)(29)(30). It binds to the 30S ribosomal subunit of the microorganism and inhibits protein synthesis by interfering with peptidyl tRNA translocation and preventing elongation of the polypeptide chain at the translocation step (31).…”

Section: Mechanism Of Action and Indicationsmentioning

confidence: 99%

Pharmacokinetic and Pharmacodynamic Studies of a Novel Spectinamide Series of Antituberculosis Agents

Vaddady¹

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iii To my parents, sister and fiancée for their endless love and support and To all my teachers who taught from their hearts and not merely from the books iv ACKNOWLEDGEMENTSThe daunting task of obtaining my Doctorate in Philosophy could not have come true without the tremendous support and encouragement from so many people. First and foremost, I would like to express my deepest gratitude and sincere appreciation to my mentor Dr. Bernd Meibohm for providing me with an opportunity to work in his lab and being my biggest advocate throughout this endeavor. I am thankful to him for instilling in me the qualities of being a good scientist. His co-operation and continued support have been major driving forces throughout my graduate career at the University of Tennessee. I would also like to thank my committee members, Dr. Richard Lee, Dr. Charles Ryan Yates, Dr. Phillip D. Rogers, Dr. James E. Bina and Dr. Terreia Jones for their invaluable suggestions, guidance and assistance over the years. I would like to thank the National Institutes of Health and the American Lebanese Syrian Associated Charities (ALSAC) for providing the financial support to my research work. My special thanks to Dr. Jack Cook, Dr. Sriram Krishnaswami and Dr. Pankaj Gupta for providing me an opportunity to work as an intern at Clinical Pharmacology, Pfizer Inc., New London, CT.A special thanks to my friends and colleagues, Nitin, Shailly, Nate, Maggie, Yi, Wararat, Satyendra, Karin, Chaela, Fei, Les, Faith, Lisa, Paras, Vinay, Puvi and Praveen for their support and wonderful company over all these years. I also extend my gratitude to the rest of my friends for all their friendship and for making my stay in Memphis a memorable experience.I would like to thank my parents, sister and my fiancée; no words would be enough to thank their support and patience during the completion of this dissertation. I would also like to thank all my teachers from the kindergarten to the graduate school for igniting in me the light of knowledge. Finally, I would like to thank Almighty for everything that I have today.v ABSTRACT Spectinamides are novel amide derivatives of the antibiotic spectinomycin that have emerged as a new class of agents to treat tuberculosis. These agents showed potent in vitro activity against Mycobacterium tuberculosis (MTB) compared to spectinomycin and in a preliminary in vivo study in interferon gamma (IFN-γ) knockout mice, spectinamide Lee1329 reduced the lung bacillary load of TB comparable to streptomycin. We hypothesized that the application of an iterative pharmacokinetics and pharmacodynamics (PK/PD) guided approach would facilitate the optimization of these lead compounds suitable for further development.A series of in vitro experiments including parallel artificial membrane permeability assay (PAMPA), microsomal metabolic stability using rat liver microsomes and protein binding assay were designed to characterize the in vivo biopharmaceutic and pharmacokinetic behavior. Drug uptake studies into Mycobacterium bovis BCG and into J774 ...

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Improving the prediction of the brain disposition for orally administered drugs using BDDCS

Broccatelli

Larregieu

Cruciani

et al. 2012

Advanced Drug Delivery Reviews

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In modeling blood–brain barrier (BBB) passage, in silico models have yielded ~80% prediction accuracy, and are currently used in early drug discovery. Being derived from molecular structural information only, these models do not take into account the biological factors responsible for the in vivo outcome. Passive permeability and P-glycoprotein (Pgp, ABCB1) efflux have been successfully recognized to impact xenobiotic extrusion from the brain, as Pgp is known to play a role in limiting the BBB penetration of oral drugs in humans. However, these two properties alone fail to explain the BBB penetration for a significant number of marketed central nervous system (CNS) agents. The Biopharmaceutics Drug Disposition Classification System (BDDCS) has proved useful in predicting drug disposition in the human body, particularly in the liver and intestine. Here we discuss the value of using BDDCS to improve BBB predictions of oral drugs. BDDCS class membership was integrated with in vitro Pgp efflux and in silico permeability data to create a simple 3-step classification tree that accurately predicted CNS disposition for more than 90% of 153 drugs in our data set. About 98% of BDDCS class 1 drugs were found to markedly distribute throughout the brain; this includes a number of BDDCS class 1 drugs shown to be Pgp substrates. This new perspective provides a further interpretation of how Pgp influences the sedative effects of H1-histamine receptor antagonists.

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Newer Antibacterial and Antimycotic Drugs: Critical Appraisal

Cited by 8 publications

References 200 publications

Pharmacokinetics and renal toxicity of three once-a-day doses of amikacin in cows

Pharmacokinetics and renal toxicity of three once-a-day doses of amikacin in cows

Pharmacokinetic and Pharmacodynamic Studies of a Novel Spectinamide Series of Antituberculosis Agents

Improving the prediction of the brain disposition for orally administered drugs using BDDCS

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