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Topic: First pass metabolism


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In the News (Fri 1 Jan 10)

  
  Ethanol metabolism and aging: the role of "first pass metabolism" and gastric alcohol dehydrogenase activity.   (Site not responding. Last check: 2007-10-15)
Ethanol metabolism and aging: the role of "first pass metabolism" and gastric alcohol dehydrogenase activity.
To investigate the effect of age and gender on ethanol metabolism, first-pass metabolism (FPM) and gastric alcohol-dehydrogenase (ADH) activity were compared in 32 elderly and 30 young adult nonalcoholic subjects.
The FPM was obtained from the difference between the area under the curve of ethanol blood concentration after intravenous or oral administration of ethanol 0.3 g/Kg b.w.
www.arclab.org /medlineupdates/abstract_7743392.html   (162 words)

  
 First pass effect - Wikipedia, the free encyclopedia
The first pass effect (or first pass metabolism) is a phenomenon of drug metabolism.
The liver is responsible for metabolizing many drugs.
Some drugs are so extensively metabolized by the liver that only a small amount of unchanged drug may enters the systemic circulation, so the bioavailability of the drug is reduced.
en.wikipedia.org /wiki/First_pass_effect   (115 words)

  
 First pass metabolism of ethanol is strikingly influenced by the speed of gastric emptying -- Oneta et al. 43 (5): 612 ...   (Site not responding. Last check: 2007-10-15)
First pass metabolism of ethanol is strikingly influenced by the speed of gastric emptying -- Oneta et al.
First pass metabolism of ethanol is strikingly influenced by the speed of gastric emptying
First pass metabolism of ethanol: gastric or hepatic, mountain or molehill.
gut.bmjjournals.com /cgi/content/full/43/5/612   (4432 words)

  
 AWARE: Alliance for Worldwide Alcohol Research and Education   (Site not responding. Last check: 2007-10-15)
Metabolism involves a number of processes, one of which is referred to as oxidation.
Most of the alcohol consumed is metabolized in the liver, but the small quantity that remains unmetabolized permits alcohol concentration to be measured in breath and urine.
The rate of alcohol metabolism depends, in part, on the amount of metabolizing enzymes in the liver, which varies among individuals and appears to have genetic determinants (1,4).
www.awareonline.org /alcohol_metabolism.htm   (2317 words)

  
 Application of a First-Pass Effect Model to Characterize the Pharmacokinetic Disposition of Venlafaxine after Oral ...
The consequences of presystemic metabolism on the bioavailability of orally administered compounds are well-established.
A model of presystemic metabolism was used to describe the time-course disposition of VEN after oral administration to humans.
Gillette: A theoretical examination of the effects of gut wall metabolism, hepatic elimination, and enterohepatic recycling on estimates of bioavailability and hepatic blood flow.
dmd.aspetjournals.org /cgi/content/full/25/10/1215   (2102 words)

  
 Catabolism Dominates the First-Pass Intestinal Metabolism of Dietary Essential Amino Acids in Milk Protein-Fed Piglets ...   (Site not responding. Last check: 2007-10-15)
First, the method that we used to quantify the utilization of the enteral tracer amino acids in mucosal protein is not a measure of the mucosal protein synthetic rate.
It appears that approximately one third of the dietary EAA intake may be metabolized in the first pass by the intestinal mucosa.
Finally, the quantities of dietary amino acids that were utilized in the first pass by the intestine were closely related to the mucosal mass of the piglets, implying that environmental conditions that affect intestinal mass have an important effect on the overall nutritional efficiency of dietary protein utilization.
nutrition.org /cgi/content/full/128/3/606   (7216 words)

  
 first pass metabolism
First pass metabolism of Phenobarbital increases as the metabolic capability of the liver increases.
Passing into the blood system, the drug may undergo extensive first pass metabolism in the liver, before being introduced into the general blood circulation.
The problem with the first available protease inhibitor, saquinavir (Invirase), was that it was almost totally cleared from the body by first pass metabolism.
www.health-get.com /info/first_pass_metabolism.html   (2255 words)

  
 Route dependent pulmonary first-pass metabolism of a series of biphenylacetic acid esters in rats   (Site not responding. Last check: 2007-10-15)
The influence of route of administration of a series of biphenylacetic acid aliphatic esters on their pulmonary first-pass metabolism in rats was investigated, The results were compared with in vitro data and with the physicochemical properties of the esters.
Pre- and post-absorptive first-pass metabolism was assessed by comparing area under blood concentration-time curves after intra-arterial administration of the esters with those seen after intravenous (to assess post-absorptive) and intratracheal (to assess pre-absorptive) administration.
The extent of pulmonary metabolism was dependent on the route of administration.
www.cf.ac.uk /phrmy/PHRMY-STAFF/PAD/PADL5.html   (173 words)

  
 Alcohol Research & Health: Alcohol and Medication Interactions - a combination of alcohol and medication can impair ...
A portion of the ingested alcohol is metabolized during its initial passage through the liver; the remainder of the ingested alcohol leaves the liver, enters the general (i.e., systemic) circulation, and is distributed throughout the body's tissues.
Alcohol metabolism (or the metabolism of any other substance) that occurs in the gastrointestinal tract and during the substance's initial passage through the liver is called "first-pass metabolism" [ILLUSTRATION FOR FIGURE 1 OMITTED].
First-pass metabolism is readily detectable after consumption of low alcohol doses(2) that leave the stomach slowly (e.g., because they have been consumed with a meal).
www.findarticles.com /p/articles/mi_m0CXH/is_1_23/ai_57050108   (1360 words)

  
 NEJM -- High blood alcohol levels in women. The role of decreased gastric alcohol dehydrogenase activity and first-pass ...
The first-pass metabolism was determined on the basis of the difference in areas under the curves of blood alcohol concentrations after intravenous and oral administration of ethanol (0.3 g per kilogram of body weight).
In nonalcoholic subjects, the first-pass metabolism and gastric alcohol dehydrogenase activity of the women were 23 and 59 percent, respectively, of those in the men, and there was a significant correlation (rs = 0.659) between first-pass metabolism and gastric mucosal alcohol dehydrogenase activity.
In the alcoholic men, the first-pass metabolism and gastric alcohol dehydrogenase activity were about half those in the nonalcoholic men; in the alcoholic women, the gastric mucosal alcohol dehydrogenase activity was even lower than in the alcoholic men, and first-pass metabolism was virtually abolished.
content.nejm.org /cgi/content/abstract/322/2/95   (1153 words)

  
 BioMed Central | Full text | PKQuest: measurement of intestinal absorption and first pass metabolism – ...
For the non-linear case, the intuitive idea that FPM is equal to the fraction of the absorbed drug that is metabolized in its first pass through the liver is no longer valid [2].
Clearly, at this time, the rate of drug metabolism for an oral input must be identical to that for an IV input so that FPM must be zero, even though a large fraction of the absorbed drug may be metabolized in its first pass through the liver.
This change in ethanol metabolism is consistent with earlier observations that the rate of ethanol disappearance from the blood is increased by a coincident meal [25,26].
www.biomedcentral.com /1472-6904/2/4   (6298 words)

  
 First pass metabolism   (Site not responding. Last check: 2007-10-15)
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lose-weight-fast.yehindo.org /first_pass_metabolism   (131 words)

  
 Use of measurements of ethanol absorption from stomach and intestine to assess human ethanol metabolism -- Levitt et ...
Ranitidine increases the bioavailability of postprandial ethanol by the reduction of first pass metabolism.
First pass metabolism of ethanol: an important determinant of blood levels after alcohol consumption.
First pass gastric mucosal metabolism of ethanol is negligible in the rat.
ajpgi.physiology.org /cgi/content/full/273/4/G951   (4533 words)

  
 First-pass metabolism of ethanol in human beings: effect of intravenous infusion of fructose.   (Site not responding. Last check: 2007-10-15)
In the current study, the effect of fructose infusion on first-pass metabolism of ethanol was studied in human volunteers.
A significantly higher first-pass metabolism of ethanol was obtained after administration of fructose in comparison with findings for control experiments with an equimolar dose of glucose.
Because fructose is metabolized predominantly in the liver and can be presumed to have virtually no effects in the stomach, results of the current study support the assumption that only a negligible part of first-pass metabolism of ethanol occurs in the stomach.
www.uni-hohenheim.de /i3v/00068900/307713041.htm   (179 words)

  
 Effect of dexamethasone on the intestinal first-pass metabolism of indinavir in rats: evidence of cytochrome P-450 3A ...
The purpose of this study is to investigate and compare the inducing effect of dexamethasone (DEX) on CYP3A and p-glycoprotein in the hepatic and intestinal first-pass metabolism of indinavir in rats.
Analysis of in vitro kinetic data revealed that the increased intestinal and hepatic metabolism by DEX was attributed to an increase in the V(max), as a result of CYP3A induction, without a significant change in the K(m) values.
Although it has been suggested that the role of intestinal metabolism for some drugs is quantitatively greater than that of hepatic metabolism in the overall first-pass metabolism, the contribution of intestinal metabolism to the overall first-pass metabolism of indinavir in rats is not quantitatively as important as the hepatic metabolism, regardless of DEX induction.
www.aegis.com /aidsline/2000/jan/A0010816.html   (575 words)

  
 Naloxone, Flumazenil and Dantrolene as Antidotes
In the latter study, the effect of naloxone on ethanol- induced impairment of psychomotor performance was first studied in two placebo-controlled, double-blind, cross-over trials in 17 healthy male volunteers.
Flumazenil was first used clinically in patients with iatrogenic benzodiazepine overdose due to mechanical ventilation or status epilepticus (Scollo-Lavizzari, 1983).
It was first synthesized in 1967 and the initial use was to treat muscle spasm (Dykes, 1975).
www.intox.org /databank/documents/antidote/antidote/ant01.htm   (14737 words)

  
 The Early History of Smalltalk
Let me first present the genera development of the Smalltalk-72 system up to the transistion to Smalltalk-76, and then follow that with the several years of work with children that were the primary mnotivation for the prroject.
First, Butler's insight in the GENTE OS that it was worthwhile to expend a small percentage of tie purging dirty objects to make core as clean as possible [Lampson 1966].
About an hour into the first session one of the VPs (who had written a few programs in FORTRAN 15 years before) finally realized he was programming and mused "so it's finally come to this." Nine out of the ten executives were able to finish a simulation problem that related to their specific interests.
gagne.homedns.org /%7etgagne/contrib/EarlyHistoryST.html   (20054 words)

  
 Is the Role of the Small Intestine in First-Pass Metabolism Overemphasized? -- Lin et al. 51 (2): 135 -- ...
Numerous metabolic reactions occur in the gut wall, including those typically referred to as phase 1 and phase 2 processes.
from the enterocyte by p-glycoprotein, and the secondary metabolism
the intestinal lumen and the extent of intestinal first-pass metabolism
pharmrev.aspetjournals.org /cgi/content/full/51/2/135   (8971 words)

  
 Effect of Flow on First-Pass Metabolism of Drugs: Single Pass Studies on 4-Methylumbelliferone Conjugation in the ...
Hirayama, H. and Pang, K. First-pass metabolism of gentisamide: Influence of intestinal metabolism on hepatic formation of conjugates.
Shephard, A. and Granger, D. Metabolic regulation of the intestinal circulation.
Xu, X., Tang, B. and Pang, K. Sequential metabolism of salicylamide exclusively to gentisamide-5-glucuronide and not gentisamide sulfate conjugates in the single pass in situ perfused rat liver.
jpet.aspetjournals.org /cgi/content/full/280/1/24   (4948 words)

  
 Entrez-PubMed
Hepatotoxicity of citalopram in rats and first-pass metabolism.
Pretreatment of male rats with phenobarbital for 2 weeks caused increased metabolism and simultaneous administration of phenobarbital and citalopram gave more pronounced fatty infiltrations than citalopram alone.
A connection is suggested between the first-pass metabolism in male rats and the hepatotoxicity, which is possibly mediated through a metabolite or intermediate formed in toxic amount during the first passage of the liver.
www.antidepressantsfacts.com /celexa-hepatotoxicity-rats.htm   (117 words)

  
 Involvement of CYP2J2 on the Intestinal First-Pass Metabolism of Antihistamine Drug, Astemizole -- Matsumoto et al. 30 ...
Oxidative metabolism of orally applied drugs during the first-pass is often critical for the pharmacological efficacy of these
metabolism, the reaction was terminated after 10 min.
Matsumoto S and Yamazoe Y (2001) Involvement of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with terfenadine.
dmd.aspetjournals.org /cgi/content/full/30/11/1240   (4126 words)

  
 First pass metabolism   (Site not responding. Last check: 2007-10-15)
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 first pass metabolism - General Practice Notebook   (Site not responding. Last check: 2007-10-15)
First pass metabolism of drugs can occur in the gut and the liver.
The first pass effect of the liver is much reduced if there is shunting; this is much more important than damage to the liver in that it only requires a relatively small amount of functional liver to achieve adequate first pass metabolism.
Oxbridge Solutions Ltd® is an independent company owned by the authors which does not receive income from any other organisation or individual.
www.gpnotebook.com /cache/-1945763815.htm   (145 words)

  
 IngentaConnect Intestinal First-Pass Metabolism of Eperisone in the Rat   (Site not responding. Last check: 2007-10-15)
The purpose of this study was to clarify quantitatively the contribution of the intestine to the first-pass metabolism of eperisone in rats.
The first-pass metabolism of eperisone was confirmed in the perfused rat small intestine in situ.
Those data strongly suggest that eperisone may be metabolized to HMO by CYP1A in rat intestinal microsomes during the first-pass through the epithelium of the small intestine.
www.ingentaconnect.com /content/klu/pham/2001/00000018/00000008/00342158   (326 words)

  
 PharmPK Discussion List Archive - PK2000089.html - 2000
Is the hepatic first pass metabolism constant across the animal
Another factor is of course the degree of solubility of the compound.
First pass metabolism involves metabolism via the liver and to a large
www.boomer.org /pkin/PK00/PK2000089.html   (610 words)

  
 Reference #97: Intestinal first pass metabolism of midazolam in liver cirrhosis --effect of grapefruit juice.   (Site not responding. Last check: 2007-10-15)
Reference #97: Intestinal first pass metabolism of midazolam in liver cirrhosis --effect of grapefruit juice.
Intestinal first pass metabolism of midazolam in liver cirrhosis --effect of grapefruit juice.
These results indicate that patients with liver cirrhosis are more dependent on the intestine for metabolism of CYP3A4 substrates than subjects with normal liver function.
www.powernetdesign.com /grapefruit/references/ref97abstract.html   (343 words)

  
 APStracts 4:0185G, 1997.   (Site not responding. Last check: 2007-10-15)
Use of measurements of ethanol absorption from the stomach and intestine to assess human ethanol metabolism.
Application of observed ethanol absorption rates to a model of human hepatic ethanol metabolism indicated that only 30% and 4% of the dose underwent first-pass metabolism when administered with food and water, respectively.
We conclude that virtually all first-pass ethanol metabolism occurs in the liver and first-pass metabolism accounts for only a small fraction of total clearance.
www.uth.tmc.edu /apstracts/1997/gastro/July/185g.html   (234 words)

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