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Albumin bound drugs

Albumin Maintains plasma oncotic pressure. Transports fat-soluble substances, e.g. bilirubin, drugs Reduced levels Low levels cause ascites and increase free plasma concentration of albumin-bound drugs, e.g. oestradiol, phenytoin Albumin is a useful clinical indicator of the liver s synthetic function. The liver produces and exports up to 12 g of albumin per day. Low levels are also seen in malnutrition, hypercatabolism and nephrotic syndrome. Half-life of 20 days, therefore indicator of chronic liver disease... [Pg.26]

Cancer and burn injury are associated with increased concentrations of AAG and decreased concentrations of albumin in plasma. For AAG-bound drugs, a 20-30 /o decrease in the unbound fractions of lidocaine, methadone,propranolol,and imipramine is observed, whereas the unbound fractions of albumin-bound drugs increase for tolbutamide (30 /o),f diazepam (180%),[12 1 and phenytoin (150%).[ 1... [Pg.3037]

J. Serum albumin concentration T Vd protein-bounde drugs... [Pg.675]

A variety of hydrolases catalyze the hydrolysis of acetylsalicylic acid. In humans, high activities have been seen with membrane-bound and cytosolic carboxylesterases (EC 3.1.1.1), plasma cholinesterase (EC 3.1.1.8), and red blood cell arylesterases (EC 3.1.1.2), whereas nonenzymatic hydrolysis appears to contribute to a small percentage of the total salicylic acid formed [76a] [82], A solution of serum albumin also displayed weak hydrolytic activity toward the drug, but, under the conditions of the study, binding to serum albumin decreased chemical hydrolysis at 37° and pH 7.4 from tm 12 1 h when unbound to 27 3 h for the fully bound drug [83], In contrast, binding to serum albumin increased by >50% the rate of carboxylesterase-catalyzed hydrolysis, as seen in buffers containing the hydrolase with or without albumin. It has been postulated that either bound acetylsalicylic acid is more susceptible to enzyme hydrolysis, or the protein directly activates the enzyme. [Pg.405]

YS Fung, DX Sun, CY Yeung. Capillary electrophoresis for determination of free and albumin-bound bilirubin and the investigation of drug interaction with bilirubin-bound albumin. Electrophoresis 21 403-410, 2000. [Pg.248]

There are small changes in serum albumin concentration with age, with concomitant small effects on protein binding of some highly bound drugs such as naproxen, salicylate, and warfarin. For such drugs the free concentration rather than the total plasma concentration is a better predictor of drug dose requirements, particularly for drugs with low therapeutic index (difference between the therapeutic... [Pg.206]

Most estimates of diuretic binding to albumin assume that the protein itself is not altered as part of the disease process. In renal failure, however, the number of binding sites on the protein may change, which in turn affects the pharmacokinetics and dynamics of the response to an administered diuretic. Another setting associated with diminished effective diuretic concentrations occurs in nephrotic syndrome. In this disease, protein escaping from the glomerulus into the tubules binds the diuretic within the lumen. The bound drug is unavailable to exert its inhibitory effect on sodium transport. [Pg.240]

Albumin concentration Drugs such as phenytoin, salicylates, and disopyramide are extensively bound to plasma albumin. Albumin levels are low in many disease states, resulting in lower total drug concentrations. [Pg.73]

Fibrates are highly bound to albumin and displace other similarly bound drugs. This can affect treatment with sulfonylureas. Hypoglycemia occurred in a diabetic patient taking glibenclamide plus gemfibrozil (170). [Pg.452]

Drugs may compete for binding sites on the plasma or tissue protein, or may displace previously bound drugs. For example, phenylbutazone may compete with phenytoin for binding to albumin. [Pg.34]

Artificial liver support systems aim at the extracorporeal removal of water soluble and protein-bound toxins (albumin being the preferential binding protein) associated with hepatic failure. Albumin contains reversible binding sites for substances such as fatty acids, hormones, enzymes, dyes, trace metals and drugs [26] and therefore helps elimination by kidneys of substances that are toxic in the unbound state. It should be noticed that the range of substances to be removed is broad and not completely identified. Clinical studies showed that the critical issue of the clinical syndrome in liver failure is the accumulation of toxins not cleared by the failing liver. Based on this hypothesis, the removal of lipophilic, albumin-bound substances, such as bilirubin, bile adds, metabolites of aromatic amino acids, medium-chain fatty acids, and cytokines, should be benefidal to the dinical course of a patient in liver failure. [Pg.427]


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Albumin bound drugs protein binding

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