Pharmacokinetics overview

Gonzalez MA, Estes KS. Pharmacokinetic overview of oral second-generation HI antihistamines. Int J Clin Pharmacol Ther 1998 36 292-300. 

Schacter LP, Igwemezie LN, Seyedsadr M, Morgenthien E, Randolph J, Albert E, Santabarbara P. Clinical and pharmacokinetic overview of parenteral etoposide phosphate. Cancer Chemother Pharmacol 1994 34(Suppl) S58-63. 

Overview of the non-clinical testing strategy Pharmacology Pharmacokinetics Toxicology... 

Benzodiazepines do not induce their own metabolism, and thete is no evidence for the development of pharmacokinetic toletance (Gteenblatt and Shader 1986). The behavioral tolerance seen with chronic dosing is explicable entirely on the basis of pharmacodynamic tolerance (as described earlier in the overview of neuropharmacology). 

This chapter will review some of the important methods for carrying out in vivo absorption and bioavailability studies, as well as attempt to provide an overview of how the information may be used in the drug discovery process. The chapter is aimed at medicinal chemists and thus will focus on the use of animals in discovery phase absorption, distribution, metabolism, and excretion/pharmacokinetic (ADME/PK) studies, rather than the design of studies that are for regulatory submission, or part of a development safety package. 

Joshi, A., Bauer, R., Kuebler, P, White, M., Leddy, C., Compton, P., Garovoy, M., Kwon, P., Walicke, P., and Dedrick, R. 2006. An overview of the pharmacokinetics and pharmacodynamics of efalizumab a monoclonal antibody approved for use in psoriasis. Journal of Clinical Pharmacology 46(1), 10-20. 

Kluwe WM. 1982. Overview of phthalate ester pharmacokinetics in mammalian species. Environ Health Perspect 45 3-9. 

Many drugs have been recognized to cross the intestinal epithelial cells via passive diffusion, thus their lipophilicity has been considered important. However, as described above, recent studies have demonstrated that a number of drug transporters including uptake and efflux systems determine the membrane transport process. In this chapter, we provide an overview of the basic characteristics of major drug transporters responsible not only for absorption but also for disposition and excretion in order to delineate the impact of drug transport proteins on pharmacokinetics. 

In an overview on CE for pharmaceutical applications, Altria describes the analysis of ionic salts, organic acids, and also water purity, which may have deleterious effects on synthetic processes. In her review, Natishan " also included indirect UV detection when performing pharmacokinetic studies. 

Pharmacokinetics and toxicity have been identified as important causes of costly late-stage failures in drug development. Hence, physicochemical as well as ADMET properties need to be fine-tuned even in the lead optimization phase. Recently developed in silica approaches will further increase model predictivity in this area to improve compound design and to focus on the most promising compounds only. A recent overview on ADME in silica models is given in Ref [128]. 

This short introduction to the terms used in pharmacokinetics is intended to provide a general overview of the subject. Those wishing to obtain a proper grounding in this important subject are recommended to consult a standard textbook of pharmacology. 

Nix DE, Majumdar AK, DiNubile MJ. (2004) Pharmacokinetics and pharmacodynamics of ertapenem An overview for clinicians. J Antimicrob Chemother 53 23-28. 

The pharmacokinetics of X-ray contrast agents used in angiography and urography are practically identical. These are characterized by extracellular distribution followed by renal excretion by glomerular filtration. The terminal half-life is approx. 1.5 h. An overview of the existing data on pharmacokinetics of X-ray contrast media in humans has been given by Bourin et al. [5]. 

Module 2 Common technical document summaries Overall common technical document table of contents Introduction Quahty overall summary Non-chnical overview Clinical overview Non-chnical summary Pharmacology Written summary Tabulated summary Pharmacokinetics Written summary Tabulated summary Toxicology... 

Having access to metabolism data in the early discovery stage is invaluable. For example, hepatic metabolism data could be used to characterize the pharmacokinetic behavior of a perspective lead. Several studies have reported how metabolism databases and software systems have been used at various settings (272). In this section, we will provide an overview of recent databases, software systems, websites, tools, and services that could be potential starting points for metabolism modeling at various stages in drug discovery process (271,273). 

VaishampayanU, Parchment RE, JastiBR, Hussain M. Taxanes an overview of the pharmacokinetics and pharmacodynamics. Urology 1999 54(6A Suppl) 22-29. 

Membrane permeability is one of the most important determinants of pharmacokinetics, not only for oral absorption, but also for renal re-absorption, biliary excretion, skin permeation, distribution to a specific organ and so on. In addition, modification of membrane permeability by formulation is rarely successful. Therefore, membrane permeability should be optimized during the structure optimization process in drug discovery. In this chapter, we give an overview of the physiology and chemistry of the membranes, in vitro permeability models and in silica predictions. This chapter focuses on progress in recent years in intestinal and blood-brain barrier (BBB) membrane permeation. There are a number of useful reviews summarizing earlier work [1-5]. 

The therapeutic outcome of topically applied agents used to control oral infections will depend on the characteristics of drugs that take advantage of the unique physiological and anatomical circumstances in the oral cavity. This section is a broad overview of important oral pharmacokinetic principles. 

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