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PharmD clinical pharmacy program            Level 3, Semester 2          Biopharmaceutics & Pharmacokinetics (PT608(

                 ‒  Binding to tissue proteins:



                    Many  drugs  accumulate  in  tissues  at  higher  concentrations  than  those  in  the

                   extracellular fluids and blood which is called localization



                 ‒  Significance:


                   ▪     Firstly, it increases the apparent volume of distribution (in contrast to plasma

                         protein binding which decreases it).

                   ▪     Secondly  it  results  in  localization  of  a  drug  at  a  specific  site  in  the  body

                         producing local toxicity.




                                       Drug                                       local toxicity


                    Aminoglycoside antibiotic gentamicin           Nephro and vestibular toxicity





                    Chlorpromazine, chloroquine                    Retinopathy



                    Tetracyclines, fluoride                        permanent brown-yellow discoloration
                                                                   of teeth.
                    (infants      or      children)       during
                    odontogenesis


                    Paracetamol and chloroform                     Hepatotoxicity
                    metabolites













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