Color Atlas of Pharmacology by Lullmann H.

By Lullmann H.

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John’s wort Transplant rejection Accelerated ciclosporin elimination Itraconazole Ciclosporin Induction of CYP3A4 Inhibition of CYP3A4 Ciclosporin nephrotoxicity Delayed ciclosporin elimination 40 ‡ Drug Elimination The Kidney as an Excretory Organ Most drugs are eliminated in urine either chemically unchanged or as metabolites. The kidney permits elimination because the vascular wall structure in the region of the glomerular capillaries (B) allows unimpeded passage into urine of blood solutes having molecular weights (MW) < 5000.

The endothelial cells are “riveted” to each other by tight junctions or occluding zonulae (labeled Z in the electron micrograph, upper left) such that no clefts, gaps, or pores remain that would permit drugs to pass unimpeded from the blood into the interstitial fluid. The blood–tissue barrier is developed differently in the various capillary beds. Permeability of the capillary wall to drugs is determined by the structural and functional characteristics of the endothelial cells. In many capillary beds, e.

Permeability of the capillary wall to drugs is determined by the structural and functional characteristics of the endothelial cells. In many capillary beds, e. , those of cardiac muscle, endothelial cells are characterized by pronounced endocytotic and transcytotic activity, as evidenced by numerous invaginations and vesicles (arrows in the electron micrograph, upper right). Transcytotic activity entails transport of fluid or macromolecules from the blood into the interstitium and vice versa. Any solutes trapped in the fluid, including drugs, may traverse the blood–tissue barrier.

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