Renal elimination

AR-42, a new orally bioavailable, potent, hydroxamate-tethered phenylbutyrate class I/IIB histone deacetylase inhibitor currently is under evaluation in phase 1 and 2 clinical trials and has demonstrated activity in both hematologic and solid tumor malignancies. This report focuses on the preclinical characterization of the pharmacokinetics of AR-42 in mice and rats.

9p caothientrangnguyen 09-05-2020 18 3   Download

Pharmacokinetics (t1/2) and the apparent volume of distribution Vapp (p. 28) by the equation: Vapp t1/2 = In 2 x –––– Cltot The smaller the volume of distribution or the larger the total clearance, the shorter is the half-life. In the case of drugs renally eliminated in unchanged form, the half-life of elimination can be calculated from the cumulative excretion in urine; the final total amount eliminated corresponds to the amount absorbed.

8p bigbaby87 04-09-2010 106 15   Download

The kidneys comprise only 0.5% of body weight, yet they receive 25% of the cardiac output. Drugs that affect renal function have important roles in cardiac failure and hypertension. Disease of the kidney must be taken into account when prescribing drugs that are eliminated by it. Diuretic drugs: their sites and modes of action, classification, adverse effects and uses in cardiac, hepatic, renal and other conditions. Carbonic anhydrase inhibitors. Cation-exchange resins and their uses. Alteration of urine pH Drugs and the kidney. Adverse effects.

19p bigbaby87 03-09-2010 97 13   Download

The following mechanisms are involved. Glomerular filtration. The rate at which a drug enters the glomerular filtrate depends on the concentration of free drug in plasma water and on its molecular weight. Substances that have a molecular weight in excess of 50 000 are excluded from the glomerular filtrate while those of molecular weight less than 10 000 (which includes almost all drugs)21 pass easily through the pores of the glomerular membrane. Renal tubular excretion. Cells of the proximal renal tubule actively transfer strongly charged molecules from the plasma to the tubular fluid.

19p bigbaby87 03-09-2010 111 15   Download