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Extensive metabolizer

In terms of activity there seems little to prevent some of these compounds finding a place in therapy, especially those such as SCH 29482, SUN 5555, and FCE 25199 which have oral absorption properties. However, as is the case for the carbapenems, some penems ate extensively metabolized by human renal dehydropeptidase-1 enzyme (144). Although no penem has received approval for clinical use as of this writing, expectations ate high that future research and development will change that. [Pg.15]

The samples of l,6-T2-DBpD and l,6-T2-2,3,7,8-Cl4-DBpD are useful in metabolism and mode of action studies. For example, when incubated with rabbit liver microsomes, l,6-T.>-DBpD is extensively metabolized to polar product(s) but only when these preparations are fortified with reduced nicotinamide-adenine dinucleotide phosphate. Under the same conditions l,6-T2-2,3,7,8-Cl4-DBpD is completely resistant to metabolic attack. In some types of studies, a higher specific activity possibly is desirable i.e., >1 Ci/mmole), and this can be achieved, with the methodology already developed, by using larger amounts of tritium gas or working on a larger synthetic scale so that it is not necessary to add unlabeled materials to assist in crystallization steps where a certain minimum amount of compound is necessary. [Pg.13]

Finally, the fact that anthocyanins can reach the brain represents a beginning of an explanation of the purported neuroprotection effects of anthocyanins. Anthocyanins may be eliminated via urinary and biliary excretion routes. " The extent of elimination of anthocyanins via urine is usually very low (< 0.2% intake) in rats and in humans, indicating either a more pronounced elimination via the bile route or extensive metabolism. As mentioned earlier, in the colon, non-absorbed or biliary excreted anthocyanins can be metabolized by the intestinal microflora into simpler break-down compounds such as phenolic acids that may be (re)absorbed and conjugated with glycine, glucuronic acid, or sulfate and also exhibit some biological... [Pg.168]

Polychaete worms belonging to the genera Nereis and Scolecolepides have extensive metabolic potential. Nereis virens is able to metabolize PCBs (McElroy and Means 1988) and a nnmber of PAHs (McElroy 1990), while N. diversicolor and Scolecolepides viridis are able to metabolize benzo[a]pyrene (Driscoll and McElroy 1996). It is worth noting that apart from excretion of the toxicant, polar, and mnch more water-soluble metabolites such as the glycosides formed from pyrene by Porcellio sp. (Larsen et al. 1998) may be mobile in the interstitial water of the sediment phase. [Pg.97]

Like other xenobiotics, cannabinoids also undergo extensive metabolism in the human body to increase their hydrophihc properties for a facihtated ehmination. The metaboHsm of A9-THC has been very well investigated. More than 100 metabolites of A9-THC are known [99] and a good overview of the most important human metaboHtes is given in [100]. MetaboHsm takes place mainly in hepatic microsomes, but also in intestines, brain. [Pg.28]

As with urine, saliva (spumm) is easy to collect. The levels of protein and lipids in saliva or spumm are low (compared to blood samples). These matrices are viscous, which is why extraction efficiency of xenobioties amoimts to only 5 to 9%. By acidifying the samples, extraction efficiencies are improved as the samples are clarified, and proteinaceous material and cellular debris are precipitated and removed. Some xenobioties and their metabohtes are expressed in hair. Hair is an ideal matrix for extraction of analytes to nonpolar phases, especially when the parent xenobioties are extensively metabolized and often nondetectable in other tissues (parent molecules of xenobioties are usually less polar than metabolites). Hair is a popular target for forensic purposes and to monitor drug compliance and abuse. Human milk may be an indicator of exposure of a newborn to compounds to which the mother has been previously exposed. The main components of human milk are water (88%), proteins (3%), lipids (3%), and carbohydrates in the form of lactose (6%). At present, increasing attention is devoted to the determination of xenobioties in breath. This matrix, however, contains only volatile substances, whose analysis is not related to PLC applications. [Pg.195]

Cyclosporine and tacrolimus are calcineurin inhibitors that are administered as part of immunosuppressive regimens in kidney, liver, heart, lung, and bone marrow transplant recipients. In addition, they are used in autoimmune disorders such as psoriasis and multiple sclerosis. The pathophysiologic mechanism for ARF is renal vascular vasoconstriction.41 It often occurs within the first 6 to 12 months of treatment, and can be reversible with dose reduction or drug discontinuation. Risk factors include high dose, elevated trough blood concentrations, increased age, and concomitant therapy with other nephrotoxic drugs.41 Cyclosporine and tacrolimus are extensively metabolized by... [Pg.370]

Mineral Oil and Polyalphaolefin Hydraulic Fluids. No studies were located regarding metabolism in humans or animals after exposure to mineral oil hydraulic fluids or polyalphaolefin hydraulic fluids. It should be noted, however, that hydrocarbons found in mineral oils generally are not expected to undergo extensive metabolism in animals or humans (Cannon 1940 IARC 1984). It may be speculated that polyalphaolefins may undergo limited metabolism of a similar nature. [Pg.171]


See other pages where Extensive metabolizer is mentioned: [Pg.410]    [Pg.139]    [Pg.787]    [Pg.923]    [Pg.948]    [Pg.949]    [Pg.989]    [Pg.126]    [Pg.222]    [Pg.87]    [Pg.128]    [Pg.138]    [Pg.249]    [Pg.223]    [Pg.811]    [Pg.41]    [Pg.42]    [Pg.75]    [Pg.103]    [Pg.113]    [Pg.173]    [Pg.135]    [Pg.506]    [Pg.202]    [Pg.311]    [Pg.124]    [Pg.128]    [Pg.207]    [Pg.166]    [Pg.39]    [Pg.61]    [Pg.272]    [Pg.296]    [Pg.447]    [Pg.479]    [Pg.480]    [Pg.494]    [Pg.496]    [Pg.497]    [Pg.531]    [Pg.392]   
See also in sourсe #XX -- [ Pg.155 ]

See also in sourсe #XX -- [ Pg.107 ]




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