Color Atlas of Pharmacology (Thieme Flexibook) by H. Luellmann, D. Bieger

By H. Luellmann, D. Bieger

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02 %, and the amount of drug eliminated per unit of time remains constant at concentrations above this level. L llmann, Color Atlas of Pharmacology ' 2000 Thieme All rights reserved. Usage subject to terms and conditions of license. 45 Pharmacokinetics Concentration (c) of drug in plasma [amount/vol] Co Plasma half life t 1 1 c t 1 = — co 2 2 ln 2 t 1 = —– 2 k 2 ct = co · e-kt ct: Drug concentration at time t co: Initial drug concentration after administration of drug dose e: Base of natural logarithm k: Elimination constant Unit of time Time (t) Notional plasma volume per unit of time freed of drug = clearance [vol/t] Amount excreted per unit of time [amount/t] Total amount of drug excreted (Amount administered) = Dose Time A.

Certain drugs may bind strongly to tissue structures, so that plasma concentrations fall significantly even before elimination has begun (4). After being distributed in blood, macromolecular substances remain largely confined to the vascular space, because their permeation through the blood-tissue barrier, or endothelium, is impeded, even where capillaries are fenestrated. , by infusion of dextran solutions (p. 152). The vascular space is, moreover, predominantly occupied by substances bound with high affinity to plasma proteins (p.

Glucuronidases. Soluble cytoplasmic sulfotransferases conjugate activated sulfate (3’phosphoadenine-5’-phosphosulfate) with alcohols and phenols. The conjugates are acids, as in the case of glucuronides. In this respect, they differ from conjugates formed by acetyltransferases from activated acetate (acetylcoenzyme A) and an alcohol or a phenol. Acyltransferases are involved in the conjugation of the amino acids glycine or glutamine with carboxylic acids. , formation of salicyluric acid from salicylic acid and glycine).

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