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

                  In contrast, acidification of the urine will cause:

                  • the amphetamine to become more ionized (form a salt).


                  • The salt form is more water soluble and less likely to be reabsorbed and has a
                   tendency to be excreted into the urine more quickly.


                  In the case of weak acids (such as salicylic acid),

                  • acidification of the urine causes greater reabsorption of the drug and

                                                                                                .
                  • alkalinization of the urine causes more rapid excretion of the drug
                  • Consequently, it is important, when studying the pharmacokinetics of weak acids and

                   bases to consider the pH of urine.

                  Effect of urine flow rate on tubular reabsorption


                  •  In addition to the pH of the urine, the rate of urine flow influences the extent of

                     reabsorption of a drug from the distal tubule (i.e. the amount of filtered drug that

                     is reabsorbed).

                  •  The normal flow of urine is approximately 1–2 mL/min.


                  •  Nonpolar and nonionized drugs, which are normally well reabsorbed in the renal
                     tubules, are sensitive to changes in the rate of urine flow.


                  •  Drugs that increase urine flow, such as:

                  ›  Ethanol

                  ›  Large fluid intake

                  ›  Methylxanthines (e.g. caffeine or theophylline),

                  •  decrease the time for drug reabsorption and promote their excretion.

                  •  Thus,  forced  diuresis  through  the  use  of  diuretics  may  be  a  useful  adjunct  for

                     removing  excessive  drug  in  an  intoxicated  patient,  by  increasing  renal  drug

                     excretion.






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