Drug distribution, consequences of protein binding, regulation of serum protein levels, distribution rate to tissues, drug permeation into tissues, teratogenesis, drug accumulation

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Colorado State University
Biomedical Science
BMS 450
Douglas Ishii

30 JanuaryDrug DistributionBack diffusion would oppose drug distributionLipophilic drug can passively diffuse through membrane but could do the same in the opposite directionSerum albumin binding sites for drugs119 positive charges96 negative chargesMany lipophilic sitesMany other serum proteinsBound drug is not available to actinactiveEquilibrium between bound and unboundBuffering systemDrug binding prevents back diffusionLipophilic drugs have low solubility in water but can piggyback on serum proteinsfasterConsequences of Protein BindingProteinbound drug is generally inactiveOnly free drug is activeProtein binding provides a drug reservoir and buffers against drug eliminationDrugdrug competitionDicoumarol anticoagulant 97 boundAspirin compete for bindingFree drug increased from 3 to 6Greater tendency to bleed less coagulation
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