File Name: phase 1 and phase 2 reactions in drug metabolism .zip
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Chemical reactions are continually taking place in the body. They are a normal aspect of life, participating in the:. Within the body is a magnificent assembly of chemical reactions, which is well orchestrated and called upon as needed. Most of these chemical reactions occur at significant rates only because specific proteins, known as enzymes, are present to catalyze them, that is, accelerate the reaction. A catalyst is a substance that can accelerate a chemical reaction of another substance without itself undergoing a permanent chemical change.
Commonly there are four types of reactions involved in drug metabolism. These are: oxidation reduction hydrolysis conjugation The first three are often lumped together as phase I reactions, while the fourth process, conjugation, is called phase II metabolism. A common scheme in the overall metabolism of drugs is that metabolites are metabolized. In particular a drug may be oxidized, reduced or hydrolyzed and then another group may be added in a conjugation step. A common cause of capacity limited metabolism is a limit in the amount of the conjugate added in the conjugation step. Phase 0 Phase 0 has been described as the transport of drug from the blood into the heptacytes in the liver, the basolateral sinusoidal uptake processes see Chapter 11 Ishikawa,
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The liver is the principal site of drug metabolism for review, see [ 1 ]. Although metabolism typically inactivates drugs, some drug metabolites are pharmacologically active—sometimes even more so than the parent compound. An inactive or weakly active substance that has an active metabolite is called a prodrug, especially if designed to deliver the active moiety more effectively. Drugs can be metabolized by oxidation, reduction, hydrolysis, hydration, conjugation, condensation, or isomerization; whatever the process, the goal is to make the drug easier to excrete. The enzymes involved in metabolism are present in many tissues but generally are more concentrated in the liver.
Phase I biotransformation reactions introduce or expose functional groups on the drug with the goal of increasing the polarity of the compound. Although Phase I drug metabolism occurs in most tissues, the primary and first pass site of metabolism occurs during hepatic circulation. Additional metabolism occurs in gastrointestinal epithelial, renal, skin, and lung tissues.
If your institution subscribes to this resource, and you don't have a MyAccess Profile, please contact your library's reference desk for information on how to gain access to this resource from off-campus. Please consult the latest official manual style if you have any questions regarding the format accuracy. All organisms are exposed to foreign chemical compounds xenobiotics in the air, water, and food. To ensure elimination of pharmacologically active xenobiotics as well as to terminate the action of many endogenous substances, evolution has provided metabolic pathways that alter their activity and their susceptibility to excretion.
If your institution subscribes to this resource, and you don't have a MyAccess Profile, please contact your library's reference desk for information on how to gain access to this resource from off-campus. Please consult the latest official manual style if you have any questions regarding the format accuracy. All organisms are exposed to foreign chemical compounds xenobiotics in the air, water, and food.
Topics on Drug Metabolism. All organisms are constantly and unavoidably exposed to xenobiotics including both man—made and natural chemicals such as drugs, plant alkaloids, microorganism toxins, pollutants, pesticides, and other industrial chemicals. Formally, biotransformation of xenobiotics as well as endogenous compounds is subdivided into phase I and phase II reactions. On the other hand, these conjugations also play an essential role in the toxicity of many chemicals due to the metabolic formation of toxic metabolites such as reactive electrophiles. Gene polymorphism of biotransformation enzymes may often play a role in various pathophysiological processes. Conjugation reactions usually involve metabolite activation by a high—energy intermediate and have been classified into two general types: type I e. In this chapter, we will concentrate on the most important conjugation reactions, namely glucuronide conjugation, sulfoconjugation, acetylation, amino acid conjugation, glutathione conjugation and methylation.
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The liver is the principal site of drug metabolism for review, see [ 1 ].Lastenia O. 17.05.2021 at 16:49
Sony xperia mini pro pdf complex ptsd from surviving to thriving pdf downloadJosephe B. 23.05.2021 at 01:42
Phase 2 metabolism involves reactions that chemically change the drug or phase 1 metabolites into compounds that are soluble enough to be excreted in urine.Inmarlese 23.05.2021 at 03:48
Drug metabolism is the metabolic breakdown of drugs by living organisms , usually through specialized enzymatic systems.Larry D. 24.05.2021 at 11:12
Phase 1 drug metabolism = Functional conversion to polar metabolites in Phase 2 drug metabolism = Enzymatic conjugation reaction in the intestine and liver.