Phase 1 and phase 2 reactions in drug metabolism pdf
– Metabolism is often divided into two phases of biochemical reaction – phase 1 and phase 2. Some drugs may undergo just phase 1 or just phase 2 metabolism, but more often, the drug will undergo phase 1 and then phase 2 sequentially.
Overview: Phase I metabolism . oxidation (via cytochrome P450), reduction, and hydrolysis reactions ; phase I reactions convert a parent drug to more polar (water soluble) active metabolites by unmasking or inserting a polar functional group (-OH, -SH, -NH2)
Oxidation (MOST CRITICAL PATHWAY IN PHASE 1 reactions) Catalyzed by oxidative enzymes (e.g. CYP-450) Non polar fat soluble molecules into more water soluble metabolites by adding oxygen to the group. Hydrolysis A chemical decomposition process that uses water to split the chemical bonds of a drug Reduction Addition of a proton to the
Phase 1 is utterly dependent on the cytochrome P4 50 enzymes whose speed of metabolism is in turn affected by things like genetics, exercise and the presence or absence of certain substances/supplements in the diet that can either speed them up …
Phase 1 & 2 Liver Detoxification Inside the liver cells there are sophisticated mechanisms that have evolved over millions of years to break down toxic substances. Every drug, artificial chemical, pesticide and hormone, is broken down (metabolised) by enzyme pathways inside the liver cells.
The primary site of drug metabolism is the liver, the organ that plays a major role in metabolism, digestion, detoxification, and elimination of substances from the body.
Phase I reaction definition of Phase I reaction by
https://www.youtube.com/embed/3xBmWDW0mqw
Fast Mimicking of Figure 10 Phase 1 and 2 Metabolism of
Phase I and Phase II Reactions — Overview Phase I characteristics : Parent drug is altered by introducing or exposing a functional group (-OH,-NH 2 , -SH)
Phase 1 and 2 metabolism refer to a range of chemical reactions. They can be distinguished by a They can be distinguished by a number of unique features, as shown in the table below.
– Developed concept of Phase 1 & Phase 2 Reactions. Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological activity (increased or decreased)
4/05/2011 · Biotransformation of drugs by phase 1 and phase 2 reactions Phase 1 reactions Oxidative reactions involving N- and O-dealkylation, aliphatic and aromatic hydroxylation, N- and S-oxidation, deamination.
What phase 1 reaction is mainly performed by the cytochrome P450 enzymes also called mixed-function enzymes?
Drug metabolism can be divided into the Phase I reactions (functionalisation) and the Phase II reactions (conjugation). Phase I biotransformations include oxidation , reduction , and hydrolysis reactions.
metabolism (phase 1 reactions), thereby mimicking the metabolic pathway of CYP450 reactions. MS voltammograms can be record-ed automatically to obtain a meta-bolic fi ngerprint of the compound of interest in less than 10 min. In addition, rapid and easy studies of adduct formations can be per-formed simply by adding GSH after the ReactorCell (phase II reactions). To confirm that the peak at m
Phase 1 metabolism can involve reduction or hydrolysis of the drug, but the most common biochemical process that occurs is oxidation. (Oxidation is the chemical reaction that occurs when apples turn brown when exposed to the oxygen in air).
phase 1 metabolism (modification reactions) and phase 2 metabolism (conjugation reactions). Phase 1 metabolism typically subjects the drug to oxida-tion or hydrolysis. It involves the cytochrome P450 (CYP) enzymes, which facilitate reactions that include N-,0-, and S-dealkylation; aromatic, aliphatic, or A^-hydroxylation; A^-oxidation; sulfoxidation; deamination; and dehalogenation. Phase 2
Metabolism of drugs is usually divided into phase 1 and phase 2. Some drugs just undergo one or the Some drugs just undergo one or the other but the majority will undergo phase 1 and then phase 2 …
Drug metabolism. Drug metabolism is an immense area of study where drugs undergo a range of enzyme-mediated chemical reactions, such as oxidation, reduction, hydrolysis, hydration, conjugation, and …
Phase I Drug Metabolism: Enzymes, Substrates, and Antibodies 12 Drug Conjugate Analysis: Enzymes, Substrates and Inhibitors, and Derivitization Reagents 22 Cover: Although phase I drug metabolism occurs in most tissues, the primary and first pass site of metabolism occurs during hepatic circulation. Biofilesonline Your gateway to Biochemicals and Reagents for Life Science Research Biofiles
Fig. 1 The reactions and putative products of Phase II drug metabolism. (a) Typical glucuronidation of nucleophilic groups (Nu) in drugs during (a) Typical glucuronidation of nucleophilic groups (Nu) in …
Phase I reactions are not necessary if a drug molecule already contains functional groups suitable for conjugation. An example is morphine, which has two hydroxyl groups. The conjugation of either, or both, with glucuronic acid is sufficient for excretion. Interestingly, one of the two single glucuronides—the one
Species differences with respect to phase II metabolism also need to be taken into consideration when selecting an in vitro system to evaluate various aspects of drug metabolism. View Show abstract
Phase 1 and Phase 2 Drug Metabolism and Bile Acid Production of HepaRG Cells in a Bioartificial Liver in Absence of Dimethyl Sulfoxide . Article (PDF Available) in Drug metabolism …
In this work we show phase 1 and 2 drug metabolism using a miniaturized electrochemical cell followed by on-line metabolite detection using electrospray ionization – mass spectrometry (ESI-MS). The most common form of in vivo drug
Drug metabolism is conventionally described as consisting of phase 1 oxidation reactions, primarily mediated by cytochrome P450 enzymes in the liver, and phase 2 conjugations such as glucuronidation, sulphation and acetylation. The first drug metabolising polymorphism was described over 40 years ago for acetylation. It is now known that N-acetyltransferase (NAT) is controlled by two genes
It is important to bear in mind that some phase II reactions can occur without phase I metabolism, but phase I and phase II reactions are complimentary and not mutually exclusive. This report describes the chemical reactions of drug metabolism and explains how they occur in vivo.
–Developed concept of Phase 1 & Phase 2 Reactions. • Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological
LAB 1 DRUG METABOLISM (part1) fmhs.auckland.ac.nz
Phase 2: Conjugation. Masking of an exist. funct. group by for instance acetylation, glycosylation, attachment amino acid etc More hydrophilic drug Renal excretion HO O OH N CH3 Morphine Demethylation Phase 1 O HO OH NH Conjugation glucuronic acid Phase 2 HO O O NH O OH CO2H HO OH. Phase 1 Metabolism by cytochrome P450 enzyme systhem (CYP450) •Located in …
1 Liver phases 1 and 2 detoxification pathways What are the symptoms of a dysfunctional liver? Abnormal metabolism of fats (lipids) leading to –
Phase 1 metabolism involveschemical reactions such as oxidation (most common), reduction and hydrolysis. There are three possible results of phase 1 metabolism. Thedrug becomes completely inactive. In other words, the metabolites are pharmacologically inactive.
General Pathway of Drug Metabolism. PHASE 1 & PHASE 2 REACTION. Oxidation & Conjugation Reaction. Phase 1 & Phase 2 . reactions complement one another in detoxifying & facilitating the elimination of drugs & Xenobiotics. Allylic. Hydroxylation of Marijuana (Δ . 1. tetra . Hydrocannabinol) CH. 3. CH. 2. OH. General Pathway of Drug Metabolism. H. H-C-H. Allylic Hydroxylation of Marijuana (Δ 1
Drug Metabolism What is mean by Phase I Reactions The purpose of this phase is to introduce a polar functional group into the xenobiotic or drug molecule to increase its water solubility so that it can be easily excreted and /or conjugated and excreted. This can be achieved by: 1- Direct introduction of the functional group (e.g., aromatic and aliphatic hydroxylation). 2- Modifying orFor many drugs, metabolism occurs in 2 phases. Phase I reactions involve formation of a new or modified functional group or cleavage (oxidation, reduction, hydrolysis); these reactions …
Phase 2 conjugation of a drug can occur in the absence of phase 1 metabolism. The hydroxylated product produced from phase 1 reactions can also be conjugated by conjugation enzymes to more hydrophilic products, easier to excrete. Often, phases 1 and 2 pathways work together to help in the removal of the xenobiotic. An example is shown in Fig. 6 for the conversion of benzene to phenyl …
The enzyme-catalyzed reactions of Phase I metabolism bind oxygen, hydrogen, water, or amino acids to the lipophilic drug molecule to expose or introduce a hydroxyl (-OH), amino (-NH 2), sulfhydryl (-SH), or carboxyl (-COOH) polar functional group, and thus, result in a modest increase in the parent drug’s …
Two general categories of drug metabolism occur in the liver: phase 1 reactions (oxidations-reductions and hydrolyses) and phase 2 reactions (synthetic conjugations). Phase 1 reactions produce functional groups that can participate in phase 2 reactions. Phase 1 reactions are almost nonexistent in the fetuses of laboratory animals; however, many appear in primates during the first trimester of
CONCLUSIONS: Phase II drug metabolizing enzymes play an important role in biotransformation of endogenous compounds and xenobiotics to more easily excretable forms as well as in the metabolic inactivation of pharmacologically active compounds. Reduced metabolising capacity of Phase II enzymes can lead to toxic effects of clinically used drugs. Gene polymorphism/ lack of these …
Phase I reactions prepare a drug for the subsequent phase II reactions. The latter are the true detoxification pathways which result in products that are generally water-soluble and easily excreted in urine or bile.5 The metabolic biotransformation of paracetamol predominantly proceeds through phase II pathways in the liver (Figure I). The main reaction is hepatic conjugation with glucuronic
1.1.1.7. Drug metabolism. 1.1.1.7.1. Phase I enzymes. Phase I enzymes [Ref: SH4:p15] Enzymes involved in phase I reactions include: Cytochrome P-450 enzymes Non-cytochrome P-450 Enzymes (Esters) Flavin-containing monooxygenase enzymes 1. Cytochrome P-450 enzymes. aka mixed function oxidase system, or monooxygenases Superfamily of membrane-bound heme proteins * …
The H 2 O 2 formed in reaction 2 is then reduced by glutathione peroxidase. The glutathione disulfide formed in reactions 1 and 3 is reduced at the expense of NADPH in reaction 4 by glutathione reductase. The NADPH, in turn, must be regenerated by other pathways.
Drug metabolism University of Waterloo
2 Phase II Drug Metabolism Petra Jančov 2. Phase II reactions 2.1 Glucuronidation UDP–glucuronosyltransferases (UGTs) belong among the key enzymes of metabolism of various exogenous as well as endogenous compounds. Conjugation reactions catalyzed by the superfamily of these enzymes serve as the most important detoxification pathway for broad spectrum of drugs, …
Phase I reactions involve hydrolysis, reduction and oxidation, exposing or introducing a functional group (-OH, -NH 2 , -SH or –COOH) to slightly increase hydrophilicity.
Start studying Drug Metabolism Phase 1 & 2 Reactions. Learn vocabulary, terms, and more with flashcards, games, and other study tools. Learn vocabulary, terms, and more with flashcards, games, and other study tools.
Phase 1 Detoxification Pathway A Delicate Balance
Phase I enzymes ld99.com
Drug metabolism 1. Drug Metabolism 2. METABOLISM OR BIOTRANSFORMATION The conversion from one chemical form of a substance to another. The term metabolism is commonly used probably because products of drug transformation are called metabolites. Metabolism is an essential pharmacokinetic process, which renders
· Phase II metabolism takes place if phase I is insufficient to clear a compound from circulation, or if phase I generates a reactive metabolite. These reactions usually involve adding a large polar group (conjugation reaction), such as glucuronide, to further increase the compound’s solubility.
PHASE 2 METABOLISM PDF The metabolites of phase I metabolic reactions can either be directly excreted in the urine or undergo further metabolic reactions. An important point to note is. Liver contains the necessary enzymes for metabolism of drugs and other xenobiotics.
Phases of Metabolism Drug biotransformation could be classified into two phases 1. Phase I (functionalization): Non polar drugs are either inactivated; or activated in
A. Kinetics of metabolism 1. First-order kinetics: The metabolic transformation of drugs is catalyzed by enzymes, and most of the reactions obey Michaelis-Menten kinetics: • In most clinical situations, the concentration of the drug, [C], is much less than the Michaelis constant, K m, and the Michaelis-Menten equation reduces to • That is, the rate of drug metabolism is directly
PHASE I The initial stage of the drug metabolic process is a catabolic reaction consisting of different oxidase systems responsible for the oxidation, reduction or hydrolysis of a drug molecule [1].
phase of drug metabolism; reactions carried out by phase 1 enzymes usually lead to the inactivation of an active drug. In certain instances, metabolism, usually the hydrol- ysis of an ester or amide linkage, results in bioactivation of a drug. Inactive drugs that undergo metabolism to an active drug are called prodrugs. An example is the anti-tumor drug cyclophosphamide, which is bioactivated
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Drug metabolism in the newborn.
(PDF) Phase 1 and Phase 2 Drug Metabolism and Bile Acid
Phase II drug metabolizing enzymes.
Drug Metabolism Phase 1 & 2 Reactions Flashcards Quizlet
x treme dungeon mastery pdf Phases 1 and 2 acetaminophen metabolism. Acetaminophen
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Phase 1 and phase 2 chemical reactions in drug metabolism
Oxidation MOST CRITICAL PATHWAY IN PHASE 1 reactions
Biotransformation of drugs by phase 1 and phase 2 reactions
Fast Mimicking of Figure 10 Phase 1 and 2 Metabolism of
Drug Metabolism What is mean by Phase I Reactions The purpose of this phase is to introduce a polar functional group into the xenobiotic or drug molecule to increase its water solubility so that it can be easily excreted and /or conjugated and excreted. This can be achieved by: 1- Direct introduction of the functional group (e.g., aromatic and aliphatic hydroxylation). 2- Modifying or
phase 1 metabolism (modification reactions) and phase 2 metabolism (conjugation reactions). Phase 1 metabolism typically subjects the drug to oxida-tion or hydrolysis. It involves the cytochrome P450 (CYP) enzymes, which facilitate reactions that include N-,0-, and S-dealkylation; aromatic, aliphatic, or A^-hydroxylation; A^-oxidation; sulfoxidation; deamination; and dehalogenation. Phase 2
phase of drug metabolism; reactions carried out by phase 1 enzymes usually lead to the inactivation of an active drug. In certain instances, metabolism, usually the hydrol- ysis of an ester or amide linkage, results in bioactivation of a drug. Inactive drugs that undergo metabolism to an active drug are called prodrugs. An example is the anti-tumor drug cyclophosphamide, which is bioactivated
Phase 1 metabolism can involve reduction or hydrolysis of the drug, but the most common biochemical process that occurs is oxidation. (Oxidation is the chemical reaction that occurs when apples turn brown when exposed to the oxygen in air).
Phase 1 and 2 metabolism refer to a range of chemical reactions. They can be distinguished by a They can be distinguished by a number of unique features, as shown in the table below.
Phase I reactions are not necessary if a drug molecule already contains functional groups suitable for conjugation. An example is morphine, which has two hydroxyl groups. The conjugation of either, or both, with glucuronic acid is sufficient for excretion. Interestingly, one of the two single glucuronides—the one
Protein of the Month European Bioinformatics Institute
Metabolism of drugs and xenobiotics University of Waterloo
The primary site of drug metabolism is the liver, the organ that plays a major role in metabolism, digestion, detoxification, and elimination of substances from the body.
1 Liver phases 1 and 2 detoxification pathways What are the symptoms of a dysfunctional liver? Abnormal metabolism of fats (lipids) leading to –
General Pathway of Drug Metabolism. PHASE 1 & PHASE 2 REACTION. Oxidation & Conjugation Reaction. Phase 1 & Phase 2 . reactions complement one another in detoxifying & facilitating the elimination of drugs & Xenobiotics. Allylic. Hydroxylation of Marijuana (Δ . 1. tetra . Hydrocannabinol) CH. 3. CH. 2. OH. General Pathway of Drug Metabolism. H. H-C-H. Allylic Hydroxylation of Marijuana (Δ 1
Phase 1 & 2 Liver Detoxification Inside the liver cells there are sophisticated mechanisms that have evolved over millions of years to break down toxic substances. Every drug, artificial chemical, pesticide and hormone, is broken down (metabolised) by enzyme pathways inside the liver cells.
Oxidation (MOST CRITICAL PATHWAY IN PHASE 1 reactions) Catalyzed by oxidative enzymes (e.g. CYP-450) Non polar fat soluble molecules into more water soluble metabolites by adding oxygen to the group. Hydrolysis A chemical decomposition process that uses water to split the chemical bonds of a drug Reduction Addition of a proton to the
– Developed concept of Phase 1 & Phase 2 Reactions. Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological activity (increased or decreased)
Metabolism of drugs is usually divided into phase 1 and phase 2. Some drugs just undergo one or the Some drugs just undergo one or the other but the majority will undergo phase 1 and then phase 2 …
It is important to bear in mind that some phase II reactions can occur without phase I metabolism, but phase I and phase II reactions are complimentary and not mutually exclusive. This report describes the chemical reactions of drug metabolism and explains how they occur in vivo.
1.1.1.7. Drug metabolism. 1.1.1.7.1. Phase I enzymes. Phase I enzymes [Ref: SH4:p15] Enzymes involved in phase I reactions include: Cytochrome P-450 enzymes Non-cytochrome P-450 Enzymes (Esters) Flavin-containing monooxygenase enzymes 1. Cytochrome P-450 enzymes. aka mixed function oxidase system, or monooxygenases Superfamily of membrane-bound heme proteins * …
–Developed concept of Phase 1 & Phase 2 Reactions. • Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological
Phase I reactions involve hydrolysis, reduction and oxidation, exposing or introducing a functional group (-OH, -NH 2 , -SH or –COOH) to slightly increase hydrophilicity.
Phase I Drug Metabolism: Enzymes, Substrates, and Antibodies 12 Drug Conjugate Analysis: Enzymes, Substrates and Inhibitors, and Derivitization Reagents 22 Cover: Although phase I drug metabolism occurs in most tissues, the primary and first pass site of metabolism occurs during hepatic circulation. Biofilesonline Your gateway to Biochemicals and Reagents for Life Science Research Biofiles
Overview: Phase I metabolism . oxidation (via cytochrome P450), reduction, and hydrolysis reactions ; phase I reactions convert a parent drug to more polar (water soluble) active metabolites by unmasking or inserting a polar functional group (-OH, -SH, -NH2)
Phase I reactions prepare a drug for the subsequent phase II reactions. The latter are the true detoxification pathways which result in products that are generally water-soluble and easily excreted in urine or bile.5 The metabolic biotransformation of paracetamol predominantly proceeds through phase II pathways in the liver (Figure I). The main reaction is hepatic conjugation with glucuronic
What phase 1 reaction is mainly performed by the cytochrome P450 enzymes also called mixed-function enzymes?
Phase 1 and phase 2 chemical reactions in drug metabolism
Phase II drug metabolizing enzymes.
–Developed concept of Phase 1 & Phase 2 Reactions. • Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological
Phase 1 & 2 Liver Detoxification Inside the liver cells there are sophisticated mechanisms that have evolved over millions of years to break down toxic substances. Every drug, artificial chemical, pesticide and hormone, is broken down (metabolised) by enzyme pathways inside the liver cells.
The enzyme-catalyzed reactions of Phase I metabolism bind oxygen, hydrogen, water, or amino acids to the lipophilic drug molecule to expose or introduce a hydroxyl (-OH), amino (-NH 2), sulfhydryl (-SH), or carboxyl (-COOH) polar functional group, and thus, result in a modest increase in the parent drug’s …
1 Liver phases 1 and 2 detoxification pathways What are the symptoms of a dysfunctional liver? Abnormal metabolism of fats (lipids) leading to –
Drug metabolism is conventionally described as consisting of phase 1 oxidation reactions, primarily mediated by cytochrome P450 enzymes in the liver, and phase 2 conjugations such as glucuronidation, sulphation and acetylation. The first drug metabolising polymorphism was described over 40 years ago for acetylation. It is now known that N-acetyltransferase (NAT) is controlled by two genes
It is important to bear in mind that some phase II reactions can occur without phase I metabolism, but phase I and phase II reactions are complimentary and not mutually exclusive. This report describes the chemical reactions of drug metabolism and explains how they occur in vivo.
PHASE 2 METABOLISM PDF The metabolites of phase I metabolic reactions can either be directly excreted in the urine or undergo further metabolic reactions. An important point to note is. Liver contains the necessary enzymes for metabolism of drugs and other xenobiotics.
Drug metabolism. Drug metabolism is an immense area of study where drugs undergo a range of enzyme-mediated chemical reactions, such as oxidation, reduction, hydrolysis, hydration, conjugation, and …
Phase 1 metabolism involveschemical reactions such as oxidation (most common), reduction and hydrolysis. There are three possible results of phase 1 metabolism. Thedrug becomes completely inactive. In other words, the metabolites are pharmacologically inactive.
Phases of Metabolism Drug biotransformation could be classified into two phases 1. Phase I (functionalization): Non polar drugs are either inactivated; or activated in
Phase I enzymes ld99.com
Phase 1 & 2 Liver Detoxification www.carahealth.com
Fig. 1 The reactions and putative products of Phase II drug metabolism. (a) Typical glucuronidation of nucleophilic groups (Nu) in drugs during (a) Typical glucuronidation of nucleophilic groups (Nu) in …
phase 1 metabolism (modification reactions) and phase 2 metabolism (conjugation reactions). Phase 1 metabolism typically subjects the drug to oxida-tion or hydrolysis. It involves the cytochrome P450 (CYP) enzymes, which facilitate reactions that include N-,0-, and S-dealkylation; aromatic, aliphatic, or A^-hydroxylation; A^-oxidation; sulfoxidation; deamination; and dehalogenation. Phase 2
2 Phase II Drug Metabolism Petra Jančov 2. Phase II reactions 2.1 Glucuronidation UDP–glucuronosyltransferases (UGTs) belong among the key enzymes of metabolism of various exogenous as well as endogenous compounds. Conjugation reactions catalyzed by the superfamily of these enzymes serve as the most important detoxification pathway for broad spectrum of drugs, …
Phase 2 conjugation of a drug can occur in the absence of phase 1 metabolism. The hydroxylated product produced from phase 1 reactions can also be conjugated by conjugation enzymes to more hydrophilic products, easier to excrete. Often, phases 1 and 2 pathways work together to help in the removal of the xenobiotic. An example is shown in Fig. 6 for the conversion of benzene to phenyl …
Drug metabolism can be divided into the Phase I reactions (functionalisation) and the Phase II reactions (conjugation). Phase I biotransformations include oxidation , reduction , and hydrolysis reactions.
Metabolism of drugs and xenobiotics University of Waterloo
(PDF) Comparison of Major Phase I and Phase II Metabolism
The primary site of drug metabolism is the liver, the organ that plays a major role in metabolism, digestion, detoxification, and elimination of substances from the body.
Phase 1 & 2 Liver Detoxification Inside the liver cells there are sophisticated mechanisms that have evolved over millions of years to break down toxic substances. Every drug, artificial chemical, pesticide and hormone, is broken down (metabolised) by enzyme pathways inside the liver cells.
Two general categories of drug metabolism occur in the liver: phase 1 reactions (oxidations-reductions and hydrolyses) and phase 2 reactions (synthetic conjugations). Phase 1 reactions produce functional groups that can participate in phase 2 reactions. Phase 1 reactions are almost nonexistent in the fetuses of laboratory animals; however, many appear in primates during the first trimester of
General Pathway of Drug Metabolism. PHASE 1 & PHASE 2 REACTION. Oxidation & Conjugation Reaction. Phase 1 & Phase 2 . reactions complement one another in detoxifying & facilitating the elimination of drugs & Xenobiotics. Allylic. Hydroxylation of Marijuana (Δ . 1. tetra . Hydrocannabinol) CH. 3. CH. 2. OH. General Pathway of Drug Metabolism. H. H-C-H. Allylic Hydroxylation of Marijuana (Δ 1
4/05/2011 · Biotransformation of drugs by phase 1 and phase 2 reactions Phase 1 reactions Oxidative reactions involving N- and O-dealkylation, aliphatic and aromatic hydroxylation, N- and S-oxidation, deamination.
The enzyme-catalyzed reactions of Phase I metabolism bind oxygen, hydrogen, water, or amino acids to the lipophilic drug molecule to expose or introduce a hydroxyl (-OH), amino (-NH 2), sulfhydryl (-SH), or carboxyl (-COOH) polar functional group, and thus, result in a modest increase in the parent drug’s …
Phase 1 and Phase 2 Drug Metabolism and Bile Acid Production of HepaRG Cells in a Bioartificial Liver in Absence of Dimethyl Sulfoxide . Article (PDF Available) in Drug metabolism …
Phase 1 and 2 metabolism refer to a range of chemical reactions. They can be distinguished by a They can be distinguished by a number of unique features, as shown in the table below.
What phase 1 reaction is mainly performed by the cytochrome P450 enzymes also called mixed-function enzymes?
–Developed concept of Phase 1 & Phase 2 Reactions. • Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological
Drug metabolism can be divided into the Phase I reactions (functionalisation) and the Phase II reactions (conjugation). Phase I biotransformations include oxidation , reduction , and hydrolysis reactions.
Opioid Metabolism Ether
Phase 1 and phase 2 chemical reactions in drug metabolism
Overview: Phase I metabolism . oxidation (via cytochrome P450), reduction, and hydrolysis reactions ; phase I reactions convert a parent drug to more polar (water soluble) active metabolites by unmasking or inserting a polar functional group (-OH, -SH, -NH2)
Phase 1 and Phase 2 Drug Metabolism and Bile Acid Production of HepaRG Cells in a Bioartificial Liver in Absence of Dimethyl Sulfoxide . Article (PDF Available) in Drug metabolism …
phase 1 metabolism (modification reactions) and phase 2 metabolism (conjugation reactions). Phase 1 metabolism typically subjects the drug to oxida-tion or hydrolysis. It involves the cytochrome P450 (CYP) enzymes, which facilitate reactions that include N-,0-, and S-dealkylation; aromatic, aliphatic, or A^-hydroxylation; A^-oxidation; sulfoxidation; deamination; and dehalogenation. Phase 2
Phase 2: Conjugation. Masking of an exist. funct. group by for instance acetylation, glycosylation, attachment amino acid etc More hydrophilic drug Renal excretion HO O OH N CH3 Morphine Demethylation Phase 1 O HO OH NH Conjugation glucuronic acid Phase 2 HO O O NH O OH CO2H HO OH. Phase 1 Metabolism by cytochrome P450 enzyme systhem (CYP450) •Located in …
Drug Metabolism What is mean by Phase I Reactions The purpose of this phase is to introduce a polar functional group into the xenobiotic or drug molecule to increase its water solubility so that it can be easily excreted and /or conjugated and excreted. This can be achieved by: 1- Direct introduction of the functional group (e.g., aromatic and aliphatic hydroxylation). 2- Modifying or
Phase 2 conjugation of a drug can occur in the absence of phase 1 metabolism. The hydroxylated product produced from phase 1 reactions can also be conjugated by conjugation enzymes to more hydrophilic products, easier to excrete. Often, phases 1 and 2 pathways work together to help in the removal of the xenobiotic. An example is shown in Fig. 6 for the conversion of benzene to phenyl …
–Developed concept of Phase 1 & Phase 2 Reactions. • Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological
· Phase II metabolism takes place if phase I is insufficient to clear a compound from circulation, or if phase I generates a reactive metabolite. These reactions usually involve adding a large polar group (conjugation reaction), such as glucuronide, to further increase the compound’s solubility.
– Developed concept of Phase 1 & Phase 2 Reactions. Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological activity (increased or decreased)
What phase 1 reaction is mainly performed by the cytochrome P450 enzymes also called mixed-function enzymes?
A. Kinetics of metabolism 1. First-order kinetics: The metabolic transformation of drugs is catalyzed by enzymes, and most of the reactions obey Michaelis-Menten kinetics: • In most clinical situations, the concentration of the drug, [C], is much less than the Michaelis constant, K m, and the Michaelis-Menten equation reduces to • That is, the rate of drug metabolism is directly
The primary site of drug metabolism is the liver, the organ that plays a major role in metabolism, digestion, detoxification, and elimination of substances from the body.
4/05/2011 · Biotransformation of drugs by phase 1 and phase 2 reactions Phase 1 reactions Oxidative reactions involving N- and O-dealkylation, aliphatic and aromatic hydroxylation, N- and S-oxidation, deamination.
PHASE I The initial stage of the drug metabolic process is a catabolic reaction consisting of different oxidase systems responsible for the oxidation, reduction or hydrolysis of a drug molecule [1].
Phase I Drug Metabolism: Enzymes, Substrates, and Antibodies 12 Drug Conjugate Analysis: Enzymes, Substrates and Inhibitors, and Derivitization Reagents 22 Cover: Although phase I drug metabolism occurs in most tissues, the primary and first pass site of metabolism occurs during hepatic circulation. Biofilesonline Your gateway to Biochemicals and Reagents for Life Science Research Biofiles
Fast Mimicking of Figure 10 Phase 1 and 2 Metabolism of
Phase 1 & 2 Liver Detoxification www.carahealth.com
Phase I reactions are not necessary if a drug molecule already contains functional groups suitable for conjugation. An example is morphine, which has two hydroxyl groups. The conjugation of either, or both, with glucuronic acid is sufficient for excretion. Interestingly, one of the two single glucuronides—the one
Drug metabolism 1. Drug Metabolism 2. METABOLISM OR BIOTRANSFORMATION The conversion from one chemical form of a substance to another. The term metabolism is commonly used probably because products of drug transformation are called metabolites. Metabolism is an essential pharmacokinetic process, which renders
· Phase II metabolism takes place if phase I is insufficient to clear a compound from circulation, or if phase I generates a reactive metabolite. These reactions usually involve adding a large polar group (conjugation reaction), such as glucuronide, to further increase the compound’s solubility.
Drug metabolism is conventionally described as consisting of phase 1 oxidation reactions, primarily mediated by cytochrome P450 enzymes in the liver, and phase 2 conjugations such as glucuronidation, sulphation and acetylation. The first drug metabolising polymorphism was described over 40 years ago for acetylation. It is now known that N-acetyltransferase (NAT) is controlled by two genes
Drug metabolism can be divided into the Phase I reactions (functionalisation) and the Phase II reactions (conjugation). Phase I biotransformations include oxidation , reduction , and hydrolysis reactions.
CONCLUSIONS: Phase II drug metabolizing enzymes play an important role in biotransformation of endogenous compounds and xenobiotics to more easily excretable forms as well as in the metabolic inactivation of pharmacologically active compounds. Reduced metabolising capacity of Phase II enzymes can lead to toxic effects of clinically used drugs. Gene polymorphism/ lack of these …
Phase 1 & 2 Liver Detoxification Inside the liver cells there are sophisticated mechanisms that have evolved over millions of years to break down toxic substances. Every drug, artificial chemical, pesticide and hormone, is broken down (metabolised) by enzyme pathways inside the liver cells.
Drug metabolism. Drug metabolism is an immense area of study where drugs undergo a range of enzyme-mediated chemical reactions, such as oxidation, reduction, hydrolysis, hydration, conjugation, and …
– Metabolism is often divided into two phases of biochemical reaction – phase 1 and phase 2. Some drugs may undergo just phase 1 or just phase 2 metabolism, but more often, the drug will undergo phase 1 and then phase 2 sequentially.
Two general categories of drug metabolism occur in the liver: phase 1 reactions (oxidations-reductions and hydrolyses) and phase 2 reactions (synthetic conjugations). Phase 1 reactions produce functional groups that can participate in phase 2 reactions. Phase 1 reactions are almost nonexistent in the fetuses of laboratory animals; however, many appear in primates during the first trimester of
Metabolism of drugs is usually divided into phase 1 and phase 2. Some drugs just undergo one or the Some drugs just undergo one or the other but the majority will undergo phase 1 and then phase 2 …
Phase I enzymes ld99.com
Biotransformation of drugs by phase 1 and phase 2 reactions
– Developed concept of Phase 1 & Phase 2 Reactions. Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological activity (increased or decreased)
Drug metabolism 1. Drug Metabolism 2. METABOLISM OR BIOTRANSFORMATION The conversion from one chemical form of a substance to another. The term metabolism is commonly used probably because products of drug transformation are called metabolites. Metabolism is an essential pharmacokinetic process, which renders
Phase I Drug Metabolism: Enzymes, Substrates, and Antibodies 12 Drug Conjugate Analysis: Enzymes, Substrates and Inhibitors, and Derivitization Reagents 22 Cover: Although phase I drug metabolism occurs in most tissues, the primary and first pass site of metabolism occurs during hepatic circulation. Biofilesonline Your gateway to Biochemicals and Reagents for Life Science Research Biofiles
Drug metabolism is conventionally described as consisting of phase 1 oxidation reactions, primarily mediated by cytochrome P450 enzymes in the liver, and phase 2 conjugations such as glucuronidation, sulphation and acetylation. The first drug metabolising polymorphism was described over 40 years ago for acetylation. It is now known that N-acetyltransferase (NAT) is controlled by two genes
1.1.1.7. Drug metabolism. 1.1.1.7.1. Phase I enzymes. Phase I enzymes [Ref: SH4:p15] Enzymes involved in phase I reactions include: Cytochrome P-450 enzymes Non-cytochrome P-450 Enzymes (Esters) Flavin-containing monooxygenase enzymes 1. Cytochrome P-450 enzymes. aka mixed function oxidase system, or monooxygenases Superfamily of membrane-bound heme proteins * …
Phase 1 metabolism can involve reduction or hydrolysis of the drug, but the most common biochemical process that occurs is oxidation. (Oxidation is the chemical reaction that occurs when apples turn brown when exposed to the oxygen in air).
Drug metabolism in the newborn.
Phases 1 and 2 acetaminophen metabolism. Acetaminophen
Start studying Drug Metabolism Phase 1 & 2 Reactions. Learn vocabulary, terms, and more with flashcards, games, and other study tools. Learn vocabulary, terms, and more with flashcards, games, and other study tools.
Fig. 1 The reactions and putative products of Phase II drug metabolism. (a) Typical glucuronidation of nucleophilic groups (Nu) in drugs during (a) Typical glucuronidation of nucleophilic groups (Nu) in …
PHASE I The initial stage of the drug metabolic process is a catabolic reaction consisting of different oxidase systems responsible for the oxidation, reduction or hydrolysis of a drug molecule [1].
Drug Metabolism What is mean by Phase I Reactions The purpose of this phase is to introduce a polar functional group into the xenobiotic or drug molecule to increase its water solubility so that it can be easily excreted and /or conjugated and excreted. This can be achieved by: 1- Direct introduction of the functional group (e.g., aromatic and aliphatic hydroxylation). 2- Modifying or
A. Kinetics of metabolism 1. First-order kinetics: The metabolic transformation of drugs is catalyzed by enzymes, and most of the reactions obey Michaelis-Menten kinetics: • In most clinical situations, the concentration of the drug, [C], is much less than the Michaelis constant, K m, and the Michaelis-Menten equation reduces to • That is, the rate of drug metabolism is directly
Drug metabolism. Drug metabolism is an immense area of study where drugs undergo a range of enzyme-mediated chemical reactions, such as oxidation, reduction, hydrolysis, hydration, conjugation, and …
2 Phase II Drug Metabolism Petra Jančov 2. Phase II reactions 2.1 Glucuronidation UDP–glucuronosyltransferases (UGTs) belong among the key enzymes of metabolism of various exogenous as well as endogenous compounds. Conjugation reactions catalyzed by the superfamily of these enzymes serve as the most important detoxification pathway for broad spectrum of drugs, …
PHASE 2 METABOLISM PDF The metabolites of phase I metabolic reactions can either be directly excreted in the urine or undergo further metabolic reactions. An important point to note is. Liver contains the necessary enzymes for metabolism of drugs and other xenobiotics.
Oxidation (MOST CRITICAL PATHWAY IN PHASE 1 reactions) Catalyzed by oxidative enzymes (e.g. CYP-450) Non polar fat soluble molecules into more water soluble metabolites by adding oxygen to the group. Hydrolysis A chemical decomposition process that uses water to split the chemical bonds of a drug Reduction Addition of a proton to the
Phase 2: Conjugation. Masking of an exist. funct. group by for instance acetylation, glycosylation, attachment amino acid etc More hydrophilic drug Renal excretion HO O OH N CH3 Morphine Demethylation Phase 1 O HO OH NH Conjugation glucuronic acid Phase 2 HO O O NH O OH CO2H HO OH. Phase 1 Metabolism by cytochrome P450 enzyme systhem (CYP450) •Located in …
1 Liver phases 1 and 2 detoxification pathways What are the symptoms of a dysfunctional liver? Abnormal metabolism of fats (lipids) leading to –
– Developed concept of Phase 1 & Phase 2 Reactions. Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological activity (increased or decreased)
Overview: Phase I metabolism . oxidation (via cytochrome P450), reduction, and hydrolysis reactions ; phase I reactions convert a parent drug to more polar (water soluble) active metabolites by unmasking or inserting a polar functional group (-OH, -SH, -NH2)
(PDF) Phase 1 and Phase 2 Drug Metabolism and Bile Acid
Opioid Metabolism Ether
Phase I reactions involve hydrolysis, reduction and oxidation, exposing or introducing a functional group (-OH, -NH 2 , -SH or –COOH) to slightly increase hydrophilicity.
The primary site of drug metabolism is the liver, the organ that plays a major role in metabolism, digestion, detoxification, and elimination of substances from the body.
Drug metabolism. Drug metabolism is an immense area of study where drugs undergo a range of enzyme-mediated chemical reactions, such as oxidation, reduction, hydrolysis, hydration, conjugation, and …
Phase 2: Conjugation. Masking of an exist. funct. group by for instance acetylation, glycosylation, attachment amino acid etc More hydrophilic drug Renal excretion HO O OH N CH3 Morphine Demethylation Phase 1 O HO OH NH Conjugation glucuronic acid Phase 2 HO O O NH O OH CO2H HO OH. Phase 1 Metabolism by cytochrome P450 enzyme systhem (CYP450) •Located in …
–Developed concept of Phase 1 & Phase 2 Reactions. • Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological
Drug Metabolism What is mean by Phase I Reactions The purpose of this phase is to introduce a polar functional group into the xenobiotic or drug molecule to increase its water solubility so that it can be easily excreted and /or conjugated and excreted. This can be achieved by: 1- Direct introduction of the functional group (e.g., aromatic and aliphatic hydroxylation). 2- Modifying or
Phase 1 & 2 Liver Detoxification Inside the liver cells there are sophisticated mechanisms that have evolved over millions of years to break down toxic substances. Every drug, artificial chemical, pesticide and hormone, is broken down (metabolised) by enzyme pathways inside the liver cells.
Start studying Drug Metabolism Phase 1 & 2 Reactions. Learn vocabulary, terms, and more with flashcards, games, and other study tools. Learn vocabulary, terms, and more with flashcards, games, and other study tools.
phase of drug metabolism; reactions carried out by phase 1 enzymes usually lead to the inactivation of an active drug. In certain instances, metabolism, usually the hydrol- ysis of an ester or amide linkage, results in bioactivation of a drug. Inactive drugs that undergo metabolism to an active drug are called prodrugs. An example is the anti-tumor drug cyclophosphamide, which is bioactivated
Drug Metabolism Phase 1 & 2 Reactions Flashcards Quizlet
LAB 1 DRUG METABOLISM (part1) fmhs.auckland.ac.nz
Oxidation (MOST CRITICAL PATHWAY IN PHASE 1 reactions) Catalyzed by oxidative enzymes (e.g. CYP-450) Non polar fat soluble molecules into more water soluble metabolites by adding oxygen to the group. Hydrolysis A chemical decomposition process that uses water to split the chemical bonds of a drug Reduction Addition of a proton to the
4/05/2011 · Biotransformation of drugs by phase 1 and phase 2 reactions Phase 1 reactions Oxidative reactions involving N- and O-dealkylation, aliphatic and aromatic hydroxylation, N- and S-oxidation, deamination.
Phase I Drug Metabolism: Enzymes, Substrates, and Antibodies 12 Drug Conjugate Analysis: Enzymes, Substrates and Inhibitors, and Derivitization Reagents 22 Cover: Although phase I drug metabolism occurs in most tissues, the primary and first pass site of metabolism occurs during hepatic circulation. Biofilesonline Your gateway to Biochemicals and Reagents for Life Science Research Biofiles
The primary site of drug metabolism is the liver, the organ that plays a major role in metabolism, digestion, detoxification, and elimination of substances from the body.
The enzyme-catalyzed reactions of Phase I metabolism bind oxygen, hydrogen, water, or amino acids to the lipophilic drug molecule to expose or introduce a hydroxyl (-OH), amino (-NH 2), sulfhydryl (-SH), or carboxyl (-COOH) polar functional group, and thus, result in a modest increase in the parent drug’s …
Drug metabolism can be divided into the Phase I reactions (functionalisation) and the Phase II reactions (conjugation). Phase I biotransformations include oxidation , reduction , and hydrolysis reactions.
–Developed concept of Phase 1 & Phase 2 Reactions. • Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological
Two general categories of drug metabolism occur in the liver: phase 1 reactions (oxidations-reductions and hydrolyses) and phase 2 reactions (synthetic conjugations). Phase 1 reactions produce functional groups that can participate in phase 2 reactions. Phase 1 reactions are almost nonexistent in the fetuses of laboratory animals; however, many appear in primates during the first trimester of
PHASE 2 METABOLISM PDF The metabolites of phase I metabolic reactions can either be directly excreted in the urine or undergo further metabolic reactions. An important point to note is. Liver contains the necessary enzymes for metabolism of drugs and other xenobiotics.
Drug metabolism 1. Drug Metabolism 2. METABOLISM OR BIOTRANSFORMATION The conversion from one chemical form of a substance to another. The term metabolism is commonly used probably because products of drug transformation are called metabolites. Metabolism is an essential pharmacokinetic process, which renders
Phase I reactions involve hydrolysis, reduction and oxidation, exposing or introducing a functional group (-OH, -NH 2 , -SH or –COOH) to slightly increase hydrophilicity.
Phase 1 metabolism involveschemical reactions such as oxidation (most common), reduction and hydrolysis. There are three possible results of phase 1 metabolism. Thedrug becomes completely inactive. In other words, the metabolites are pharmacologically inactive.
Opioid Metabolism Ether
Phase I vs. Phase II Metabolism Pharmacology
phase of drug metabolism; reactions carried out by phase 1 enzymes usually lead to the inactivation of an active drug. In certain instances, metabolism, usually the hydrol- ysis of an ester or amide linkage, results in bioactivation of a drug. Inactive drugs that undergo metabolism to an active drug are called prodrugs. An example is the anti-tumor drug cyclophosphamide, which is bioactivated
For many drugs, metabolism occurs in 2 phases. Phase I reactions involve formation of a new or modified functional group or cleavage (oxidation, reduction, hydrolysis); these reactions …
metabolism (phase 1 reactions), thereby mimicking the metabolic pathway of CYP450 reactions. MS voltammograms can be record-ed automatically to obtain a meta-bolic fi ngerprint of the compound of interest in less than 10 min. In addition, rapid and easy studies of adduct formations can be per-formed simply by adding GSH after the ReactorCell (phase II reactions). To confirm that the peak at m
In this work we show phase 1 and 2 drug metabolism using a miniaturized electrochemical cell followed by on-line metabolite detection using electrospray ionization – mass spectrometry (ESI-MS). The most common form of in vivo drug
Phase 1 and Phase 2 Drug Metabolism and Bile Acid Production of HepaRG Cells in a Bioartificial Liver in Absence of Dimethyl Sulfoxide . Article (PDF Available) in Drug metabolism …
Phase I and Phase II Reactions — Overview Phase I characteristics : Parent drug is altered by introducing or exposing a functional group (-OH,-NH 2 , -SH)
Fig. 1 The reactions and putative products of Phase II drug metabolism. (a) Typical glucuronidation of nucleophilic groups (Nu) in drugs during (a) Typical glucuronidation of nucleophilic groups (Nu) in …
Drug metabolism is conventionally described as consisting of phase 1 oxidation reactions, primarily mediated by cytochrome P450 enzymes in the liver, and phase 2 conjugations such as glucuronidation, sulphation and acetylation. The first drug metabolising polymorphism was described over 40 years ago for acetylation. It is now known that N-acetyltransferase (NAT) is controlled by two genes
Phase I reactions involve hydrolysis, reduction and oxidation, exposing or introducing a functional group (-OH, -NH 2 , -SH or –COOH) to slightly increase hydrophilicity.
PHASE 2 METABOLISM PDF The metabolites of phase I metabolic reactions can either be directly excreted in the urine or undergo further metabolic reactions. An important point to note is. Liver contains the necessary enzymes for metabolism of drugs and other xenobiotics.
Metabolism of drugs is usually divided into phase 1 and phase 2. Some drugs just undergo one or the Some drugs just undergo one or the other but the majority will undergo phase 1 and then phase 2 …
Drug metabolism 1. Drug Metabolism 2. METABOLISM OR BIOTRANSFORMATION The conversion from one chemical form of a substance to another. The term metabolism is commonly used probably because products of drug transformation are called metabolites. Metabolism is an essential pharmacokinetic process, which renders
Phase I Drug Metabolism: Enzymes, Substrates, and Antibodies 12 Drug Conjugate Analysis: Enzymes, Substrates and Inhibitors, and Derivitization Reagents 22 Cover: Although phase I drug metabolism occurs in most tissues, the primary and first pass site of metabolism occurs during hepatic circulation. Biofilesonline Your gateway to Biochemicals and Reagents for Life Science Research Biofiles
Drug metabolism. Drug metabolism is an immense area of study where drugs undergo a range of enzyme-mediated chemical reactions, such as oxidation, reduction, hydrolysis, hydration, conjugation, and …
Phases 1 and 2 acetaminophen metabolism. Acetaminophen
Phase I Reactions Hydrolysis Reduction and Oxidation
Phase 1 and Phase 2 Drug Metabolism and Bile Acid Production of HepaRG Cells in a Bioartificial Liver in Absence of Dimethyl Sulfoxide . Article (PDF Available) in Drug metabolism …
Phase 1 and 2 metabolism refer to a range of chemical reactions. They can be distinguished by a They can be distinguished by a number of unique features, as shown in the table below.
– Metabolism is often divided into two phases of biochemical reaction – phase 1 and phase 2. Some drugs may undergo just phase 1 or just phase 2 metabolism, but more often, the drug will undergo phase 1 and then phase 2 sequentially.
4/05/2011 · Biotransformation of drugs by phase 1 and phase 2 reactions Phase 1 reactions Oxidative reactions involving N- and O-dealkylation, aliphatic and aromatic hydroxylation, N- and S-oxidation, deamination.
Phase 1 metabolism involveschemical reactions such as oxidation (most common), reduction and hydrolysis. There are three possible results of phase 1 metabolism. Thedrug becomes completely inactive. In other words, the metabolites are pharmacologically inactive.
Phase 2 conjugation of a drug can occur in the absence of phase 1 metabolism. The hydroxylated product produced from phase 1 reactions can also be conjugated by conjugation enzymes to more hydrophilic products, easier to excrete. Often, phases 1 and 2 pathways work together to help in the removal of the xenobiotic. An example is shown in Fig. 6 for the conversion of benzene to phenyl …
Fig. 1 The reactions and putative products of Phase II drug metabolism. (a) Typical glucuronidation of nucleophilic groups (Nu) in drugs during (a) Typical glucuronidation of nucleophilic groups (Nu) in …
Oxidation (MOST CRITICAL PATHWAY IN PHASE 1 reactions) Catalyzed by oxidative enzymes (e.g. CYP-450) Non polar fat soluble molecules into more water soluble metabolites by adding oxygen to the group. Hydrolysis A chemical decomposition process that uses water to split the chemical bonds of a drug Reduction Addition of a proton to the
Drug metabolism SlideShare
Fast Mimicking of Figure 10 Phase 1 and 2 Metabolism of
Two general categories of drug metabolism occur in the liver: phase 1 reactions (oxidations-reductions and hydrolyses) and phase 2 reactions (synthetic conjugations). Phase 1 reactions produce functional groups that can participate in phase 2 reactions. Phase 1 reactions are almost nonexistent in the fetuses of laboratory animals; however, many appear in primates during the first trimester of
Phase 1 and 2 metabolism refer to a range of chemical reactions. They can be distinguished by a They can be distinguished by a number of unique features, as shown in the table below.
Drug metabolism 1. Drug Metabolism 2. METABOLISM OR BIOTRANSFORMATION The conversion from one chemical form of a substance to another. The term metabolism is commonly used probably because products of drug transformation are called metabolites. Metabolism is an essential pharmacokinetic process, which renders
1 Liver phases 1 and 2 detoxification pathways What are the symptoms of a dysfunctional liver? Abnormal metabolism of fats (lipids) leading to –
phase 1 metabolism (modification reactions) and phase 2 metabolism (conjugation reactions). Phase 1 metabolism typically subjects the drug to oxida-tion or hydrolysis. It involves the cytochrome P450 (CYP) enzymes, which facilitate reactions that include N-,0-, and S-dealkylation; aromatic, aliphatic, or A^-hydroxylation; A^-oxidation; sulfoxidation; deamination; and dehalogenation. Phase 2
Drug metabolism can be divided into the Phase I reactions (functionalisation) and the Phase II reactions (conjugation). Phase I biotransformations include oxidation , reduction , and hydrolysis reactions.
4/05/2011 · Biotransformation of drugs by phase 1 and phase 2 reactions Phase 1 reactions Oxidative reactions involving N- and O-dealkylation, aliphatic and aromatic hydroxylation, N- and S-oxidation, deamination.
Phases of Metabolism Drug biotransformation could be classified into two phases 1. Phase I (functionalization): Non polar drugs are either inactivated; or activated in
Phase 2 conjugation of a drug can occur in the absence of phase 1 metabolism. The hydroxylated product produced from phase 1 reactions can also be conjugated by conjugation enzymes to more hydrophilic products, easier to excrete. Often, phases 1 and 2 pathways work together to help in the removal of the xenobiotic. An example is shown in Fig. 6 for the conversion of benzene to phenyl …
It is important to bear in mind that some phase II reactions can occur without phase I metabolism, but phase I and phase II reactions are complimentary and not mutually exclusive. This report describes the chemical reactions of drug metabolism and explains how they occur in vivo.
Phase 1 is utterly dependent on the cytochrome P4 50 enzymes whose speed of metabolism is in turn affected by things like genetics, exercise and the presence or absence of certain substances/supplements in the diet that can either speed them up …
CONCLUSIONS: Phase II drug metabolizing enzymes play an important role in biotransformation of endogenous compounds and xenobiotics to more easily excretable forms as well as in the metabolic inactivation of pharmacologically active compounds. Reduced metabolising capacity of Phase II enzymes can lead to toxic effects of clinically used drugs. Gene polymorphism/ lack of these …
Phase I reactions prepare a drug for the subsequent phase II reactions. The latter are the true detoxification pathways which result in products that are generally water-soluble and easily excreted in urine or bile.5 The metabolic biotransformation of paracetamol predominantly proceeds through phase II pathways in the liver (Figure I). The main reaction is hepatic conjugation with glucuronic
Drug Metabolism What is mean by Phase I Reactions The purpose of this phase is to introduce a polar functional group into the xenobiotic or drug molecule to increase its water solubility so that it can be easily excreted and /or conjugated and excreted. This can be achieved by: 1- Direct introduction of the functional group (e.g., aromatic and aliphatic hydroxylation). 2- Modifying or
Phase I reactions involve hydrolysis, reduction and oxidation, exposing or introducing a functional group (-OH, -NH 2 , -SH or –COOH) to slightly increase hydrophilicity.
The chemistry of drug metabolism UK Essays UKEssays
LAB 1 DRUG METABOLISM (part1) fmhs.auckland.ac.nz
Drug metabolism. Drug metabolism is an immense area of study where drugs undergo a range of enzyme-mediated chemical reactions, such as oxidation, reduction, hydrolysis, hydration, conjugation, and …
–Developed concept of Phase 1 & Phase 2 Reactions. • Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological
The primary site of drug metabolism is the liver, the organ that plays a major role in metabolism, digestion, detoxification, and elimination of substances from the body.
Oxidation (MOST CRITICAL PATHWAY IN PHASE 1 reactions) Catalyzed by oxidative enzymes (e.g. CYP-450) Non polar fat soluble molecules into more water soluble metabolites by adding oxygen to the group. Hydrolysis A chemical decomposition process that uses water to split the chemical bonds of a drug Reduction Addition of a proton to the
4/05/2011 · Biotransformation of drugs by phase 1 and phase 2 reactions Phase 1 reactions Oxidative reactions involving N- and O-dealkylation, aliphatic and aromatic hydroxylation, N- and S-oxidation, deamination.
The H 2 O 2 formed in reaction 2 is then reduced by glutathione peroxidase. The glutathione disulfide formed in reactions 1 and 3 is reduced at the expense of NADPH in reaction 4 by glutathione reductase. The NADPH, in turn, must be regenerated by other pathways.
Drug metabolism can be divided into the Phase I reactions (functionalisation) and the Phase II reactions (conjugation). Phase I biotransformations include oxidation , reduction , and hydrolysis reactions.
Phase 2 conjugation of a drug can occur in the absence of phase 1 metabolism. The hydroxylated product produced from phase 1 reactions can also be conjugated by conjugation enzymes to more hydrophilic products, easier to excrete. Often, phases 1 and 2 pathways work together to help in the removal of the xenobiotic. An example is shown in Fig. 6 for the conversion of benzene to phenyl …
For many drugs, metabolism occurs in 2 phases. Phase I reactions involve formation of a new or modified functional group or cleavage (oxidation, reduction, hydrolysis); these reactions …
phase 1 metabolism (modification reactions) and phase 2 metabolism (conjugation reactions). Phase 1 metabolism typically subjects the drug to oxida-tion or hydrolysis. It involves the cytochrome P450 (CYP) enzymes, which facilitate reactions that include N-,0-, and S-dealkylation; aromatic, aliphatic, or A^-hydroxylation; A^-oxidation; sulfoxidation; deamination; and dehalogenation. Phase 2
Drug metabolism is conventionally described as consisting of phase 1 oxidation reactions, primarily mediated by cytochrome P450 enzymes in the liver, and phase 2 conjugations such as glucuronidation, sulphation and acetylation. The first drug metabolising polymorphism was described over 40 years ago for acetylation. It is now known that N-acetyltransferase (NAT) is controlled by two genes
General Pathway of Drug Metabolism. PHASE 1 & PHASE 2 REACTION. Oxidation & Conjugation Reaction. Phase 1 & Phase 2 . reactions complement one another in detoxifying & facilitating the elimination of drugs & Xenobiotics. Allylic. Hydroxylation of Marijuana (Δ . 1. tetra . Hydrocannabinol) CH. 3. CH. 2. OH. General Pathway of Drug Metabolism. H. H-C-H. Allylic Hydroxylation of Marijuana (Δ 1
The enzyme-catalyzed reactions of Phase I metabolism bind oxygen, hydrogen, water, or amino acids to the lipophilic drug molecule to expose or introduce a hydroxyl (-OH), amino (-NH 2), sulfhydryl (-SH), or carboxyl (-COOH) polar functional group, and thus, result in a modest increase in the parent drug’s …
Phase 2: Conjugation. Masking of an exist. funct. group by for instance acetylation, glycosylation, attachment amino acid etc More hydrophilic drug Renal excretion HO O OH N CH3 Morphine Demethylation Phase 1 O HO OH NH Conjugation glucuronic acid Phase 2 HO O O NH O OH CO2H HO OH. Phase 1 Metabolism by cytochrome P450 enzyme systhem (CYP450) •Located in …
Phase 1 is utterly dependent on the cytochrome P4 50 enzymes whose speed of metabolism is in turn affected by things like genetics, exercise and the presence or absence of certain substances/supplements in the diet that can either speed them up …
(PDF) Comparison of Major Phase I and Phase II Metabolism
LAB 1 DRUG METABOLISM (part1) fmhs.auckland.ac.nz
Phase 2 conjugation of a drug can occur in the absence of phase 1 metabolism. The hydroxylated product produced from phase 1 reactions can also be conjugated by conjugation enzymes to more hydrophilic products, easier to excrete. Often, phases 1 and 2 pathways work together to help in the removal of the xenobiotic. An example is shown in Fig. 6 for the conversion of benzene to phenyl …
Phase I reactions are not necessary if a drug molecule already contains functional groups suitable for conjugation. An example is morphine, which has two hydroxyl groups. The conjugation of either, or both, with glucuronic acid is sufficient for excretion. Interestingly, one of the two single glucuronides—the one
Drug metabolism can be divided into the Phase I reactions (functionalisation) and the Phase II reactions (conjugation). Phase I biotransformations include oxidation , reduction , and hydrolysis reactions.
The primary site of drug metabolism is the liver, the organ that plays a major role in metabolism, digestion, detoxification, and elimination of substances from the body.
The H 2 O 2 formed in reaction 2 is then reduced by glutathione peroxidase. The glutathione disulfide formed in reactions 1 and 3 is reduced at the expense of NADPH in reaction 4 by glutathione reductase. The NADPH, in turn, must be regenerated by other pathways.
Drug metabolism is conventionally described as consisting of phase 1 oxidation reactions, primarily mediated by cytochrome P450 enzymes in the liver, and phase 2 conjugations such as glucuronidation, sulphation and acetylation. The first drug metabolising polymorphism was described over 40 years ago for acetylation. It is now known that N-acetyltransferase (NAT) is controlled by two genes
Phase 1 and 2 metabolism refer to a range of chemical reactions. They can be distinguished by a They can be distinguished by a number of unique features, as shown in the table below.
– Metabolism is often divided into two phases of biochemical reaction – phase 1 and phase 2. Some drugs may undergo just phase 1 or just phase 2 metabolism, but more often, the drug will undergo phase 1 and then phase 2 sequentially.
Phase I reactions involve hydrolysis, reduction and oxidation, exposing or introducing a functional group (-OH, -NH 2 , -SH or –COOH) to slightly increase hydrophilicity.
Drug Metabolism What is mean by Phase I Reactions The purpose of this phase is to introduce a polar functional group into the xenobiotic or drug molecule to increase its water solubility so that it can be easily excreted and /or conjugated and excreted. This can be achieved by: 1- Direct introduction of the functional group (e.g., aromatic and aliphatic hydroxylation). 2- Modifying or
Phase I reactions prepare a drug for the subsequent phase II reactions. The latter are the true detoxification pathways which result in products that are generally water-soluble and easily excreted in urine or bile.5 The metabolic biotransformation of paracetamol predominantly proceeds through phase II pathways in the liver (Figure I). The main reaction is hepatic conjugation with glucuronic
Drug Metabolism Phase 1 & 2 Reactions Flashcards Quizlet
Oxidation MOST CRITICAL PATHWAY IN PHASE 1 reactions
Metabolism of drugs is usually divided into phase 1 and phase 2. Some drugs just undergo one or the Some drugs just undergo one or the other but the majority will undergo phase 1 and then phase 2 …
The primary site of drug metabolism is the liver, the organ that plays a major role in metabolism, digestion, detoxification, and elimination of substances from the body.
Phase I reactions are not necessary if a drug molecule already contains functional groups suitable for conjugation. An example is morphine, which has two hydroxyl groups. The conjugation of either, or both, with glucuronic acid is sufficient for excretion. Interestingly, one of the two single glucuronides—the one
Phases of Metabolism Drug biotransformation could be classified into two phases 1. Phase I (functionalization): Non polar drugs are either inactivated; or activated in
Phase I reactions involve hydrolysis, reduction and oxidation, exposing or introducing a functional group (-OH, -NH 2 , -SH or –COOH) to slightly increase hydrophilicity.
Drug Metabolism What is mean by Phase I Reactions The purpose of this phase is to introduce a polar functional group into the xenobiotic or drug molecule to increase its water solubility so that it can be easily excreted and /or conjugated and excreted. This can be achieved by: 1- Direct introduction of the functional group (e.g., aromatic and aliphatic hydroxylation). 2- Modifying or
1.1.1.7. Drug metabolism. 1.1.1.7.1. Phase I enzymes. Phase I enzymes [Ref: SH4:p15] Enzymes involved in phase I reactions include: Cytochrome P-450 enzymes Non-cytochrome P-450 Enzymes (Esters) Flavin-containing monooxygenase enzymes 1. Cytochrome P-450 enzymes. aka mixed function oxidase system, or monooxygenases Superfamily of membrane-bound heme proteins * …
Phases 1 and 2 acetaminophen metabolism. Acetaminophen
Drug metabolism SlideShare
PHASE 2 METABOLISM PDF The metabolites of phase I metabolic reactions can either be directly excreted in the urine or undergo further metabolic reactions. An important point to note is. Liver contains the necessary enzymes for metabolism of drugs and other xenobiotics.
CONCLUSIONS: Phase II drug metabolizing enzymes play an important role in biotransformation of endogenous compounds and xenobiotics to more easily excretable forms as well as in the metabolic inactivation of pharmacologically active compounds. Reduced metabolising capacity of Phase II enzymes can lead to toxic effects of clinically used drugs. Gene polymorphism/ lack of these …
Drug Metabolism What is mean by Phase I Reactions The purpose of this phase is to introduce a polar functional group into the xenobiotic or drug molecule to increase its water solubility so that it can be easily excreted and /or conjugated and excreted. This can be achieved by: 1- Direct introduction of the functional group (e.g., aromatic and aliphatic hydroxylation). 2- Modifying or
Phase 2 conjugation of a drug can occur in the absence of phase 1 metabolism. The hydroxylated product produced from phase 1 reactions can also be conjugated by conjugation enzymes to more hydrophilic products, easier to excrete. Often, phases 1 and 2 pathways work together to help in the removal of the xenobiotic. An example is shown in Fig. 6 for the conversion of benzene to phenyl …
2 Phase II Drug Metabolism Petra Jančov 2. Phase II reactions 2.1 Glucuronidation UDP–glucuronosyltransferases (UGTs) belong among the key enzymes of metabolism of various exogenous as well as endogenous compounds. Conjugation reactions catalyzed by the superfamily of these enzymes serve as the most important detoxification pathway for broad spectrum of drugs, …
phase 1 metabolism (modification reactions) and phase 2 metabolism (conjugation reactions). Phase 1 metabolism typically subjects the drug to oxida-tion or hydrolysis. It involves the cytochrome P450 (CYP) enzymes, which facilitate reactions that include N-,0-, and S-dealkylation; aromatic, aliphatic, or A^-hydroxylation; A^-oxidation; sulfoxidation; deamination; and dehalogenation. Phase 2
Phase I and Phase II Reactions — Overview Phase I characteristics : Parent drug is altered by introducing or exposing a functional group (-OH,-NH 2 , -SH)
–Developed concept of Phase 1 & Phase 2 Reactions. • Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological
4/05/2011 · Biotransformation of drugs by phase 1 and phase 2 reactions Phase 1 reactions Oxidative reactions involving N- and O-dealkylation, aliphatic and aromatic hydroxylation, N- and S-oxidation, deamination.
(PDF) Phase 1 and Phase 2 Drug Metabolism and Bile Acid
Phase I Reactions Hydrolysis Reduction and Oxidation
Phase 1 metabolism involveschemical reactions such as oxidation (most common), reduction and hydrolysis. There are three possible results of phase 1 metabolism. Thedrug becomes completely inactive. In other words, the metabolites are pharmacologically inactive.
Metabolism of drugs is usually divided into phase 1 and phase 2. Some drugs just undergo one or the Some drugs just undergo one or the other but the majority will undergo phase 1 and then phase 2 …
Phase I reactions prepare a drug for the subsequent phase II reactions. The latter are the true detoxification pathways which result in products that are generally water-soluble and easily excreted in urine or bile.5 The metabolic biotransformation of paracetamol predominantly proceeds through phase II pathways in the liver (Figure I). The main reaction is hepatic conjugation with glucuronic
It is important to bear in mind that some phase II reactions can occur without phase I metabolism, but phase I and phase II reactions are complimentary and not mutually exclusive. This report describes the chemical reactions of drug metabolism and explains how they occur in vivo.
The enzyme-catalyzed reactions of Phase I metabolism bind oxygen, hydrogen, water, or amino acids to the lipophilic drug molecule to expose or introduce a hydroxyl (-OH), amino (-NH 2), sulfhydryl (-SH), or carboxyl (-COOH) polar functional group, and thus, result in a modest increase in the parent drug’s …
Phase 2 conjugation of a drug can occur in the absence of phase 1 metabolism. The hydroxylated product produced from phase 1 reactions can also be conjugated by conjugation enzymes to more hydrophilic products, easier to excrete. Often, phases 1 and 2 pathways work together to help in the removal of the xenobiotic. An example is shown in Fig. 6 for the conversion of benzene to phenyl …
Phase 1 and Phase 2 Drug Metabolism and Bile Acid Production of HepaRG Cells in a Bioartificial Liver in Absence of Dimethyl Sulfoxide . Article (PDF Available) in Drug metabolism …
– Developed concept of Phase 1 & Phase 2 Reactions. Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological activity (increased or decreased)
Phase I and Phase II Reactions — Overview Phase I characteristics : Parent drug is altered by introducing or exposing a functional group (-OH,-NH 2 , -SH)
1 Liver phases 1 and 2 detoxification pathways What are the symptoms of a dysfunctional liver? Abnormal metabolism of fats (lipids) leading to –
The primary site of drug metabolism is the liver, the organ that plays a major role in metabolism, digestion, detoxification, and elimination of substances from the body.
– Metabolism is often divided into two phases of biochemical reaction – phase 1 and phase 2. Some drugs may undergo just phase 1 or just phase 2 metabolism, but more often, the drug will undergo phase 1 and then phase 2 sequentially.
Drug metabolism University of Waterloo
Phase I vs. Phase II Metabolism Pharmacology
Drug metabolism is conventionally described as consisting of phase 1 oxidation reactions, primarily mediated by cytochrome P450 enzymes in the liver, and phase 2 conjugations such as glucuronidation, sulphation and acetylation. The first drug metabolising polymorphism was described over 40 years ago for acetylation. It is now known that N-acetyltransferase (NAT) is controlled by two genes
Two general categories of drug metabolism occur in the liver: phase 1 reactions (oxidations-reductions and hydrolyses) and phase 2 reactions (synthetic conjugations). Phase 1 reactions produce functional groups that can participate in phase 2 reactions. Phase 1 reactions are almost nonexistent in the fetuses of laboratory animals; however, many appear in primates during the first trimester of
Phase 1 & 2 Liver Detoxification Inside the liver cells there are sophisticated mechanisms that have evolved over millions of years to break down toxic substances. Every drug, artificial chemical, pesticide and hormone, is broken down (metabolised) by enzyme pathways inside the liver cells.
1.1.1.7. Drug metabolism. 1.1.1.7.1. Phase I enzymes. Phase I enzymes [Ref: SH4:p15] Enzymes involved in phase I reactions include: Cytochrome P-450 enzymes Non-cytochrome P-450 Enzymes (Esters) Flavin-containing monooxygenase enzymes 1. Cytochrome P-450 enzymes. aka mixed function oxidase system, or monooxygenases Superfamily of membrane-bound heme proteins * …
For many drugs, metabolism occurs in 2 phases. Phase I reactions involve formation of a new or modified functional group or cleavage (oxidation, reduction, hydrolysis); these reactions …
Species differences with respect to phase II metabolism also need to be taken into consideration when selecting an in vitro system to evaluate various aspects of drug metabolism. View Show abstract
The enzyme-catalyzed reactions of Phase I metabolism bind oxygen, hydrogen, water, or amino acids to the lipophilic drug molecule to expose or introduce a hydroxyl (-OH), amino (-NH 2), sulfhydryl (-SH), or carboxyl (-COOH) polar functional group, and thus, result in a modest increase in the parent drug’s …
Phase 1 is utterly dependent on the cytochrome P4 50 enzymes whose speed of metabolism is in turn affected by things like genetics, exercise and the presence or absence of certain substances/supplements in the diet that can either speed them up …
Metabolism of drugs is usually divided into phase 1 and phase 2. Some drugs just undergo one or the Some drugs just undergo one or the other but the majority will undergo phase 1 and then phase 2 …
Phase I and Phase II Reactions — Overview Phase I characteristics : Parent drug is altered by introducing or exposing a functional group (-OH,-NH 2 , -SH)
4/05/2011 · Biotransformation of drugs by phase 1 and phase 2 reactions Phase 1 reactions Oxidative reactions involving N- and O-dealkylation, aliphatic and aromatic hydroxylation, N- and S-oxidation, deamination.
– Metabolism is often divided into two phases of biochemical reaction – phase 1 and phase 2. Some drugs may undergo just phase 1 or just phase 2 metabolism, but more often, the drug will undergo phase 1 and then phase 2 sequentially.
PHASE I The initial stage of the drug metabolic process is a catabolic reaction consisting of different oxidase systems responsible for the oxidation, reduction or hydrolysis of a drug molecule [1].
Drug metabolism. Drug metabolism is an immense area of study where drugs undergo a range of enzyme-mediated chemical reactions, such as oxidation, reduction, hydrolysis, hydration, conjugation, and …
General Pathway of Drug Metabolism. PHASE 1 & PHASE 2 REACTION. Oxidation & Conjugation Reaction. Phase 1 & Phase 2 . reactions complement one another in detoxifying & facilitating the elimination of drugs & Xenobiotics. Allylic. Hydroxylation of Marijuana (Δ . 1. tetra . Hydrocannabinol) CH. 3. CH. 2. OH. General Pathway of Drug Metabolism. H. H-C-H. Allylic Hydroxylation of Marijuana (Δ 1
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(PDF) Comparison of Major Phase I and Phase II Metabolism
–Developed concept of Phase 1 & Phase 2 Reactions. • Biotransformation involves metabolic oxygenation, reduction, or hydrolysis; result in changes in biological
1 Liver phases 1 and 2 detoxification pathways What are the symptoms of a dysfunctional liver? Abnormal metabolism of fats (lipids) leading to –
Overview: Phase I metabolism . oxidation (via cytochrome P450), reduction, and hydrolysis reactions ; phase I reactions convert a parent drug to more polar (water soluble) active metabolites by unmasking or inserting a polar functional group (-OH, -SH, -NH2)
General Pathway of Drug Metabolism. PHASE 1 & PHASE 2 REACTION. Oxidation & Conjugation Reaction. Phase 1 & Phase 2 . reactions complement one another in detoxifying & facilitating the elimination of drugs & Xenobiotics. Allylic. Hydroxylation of Marijuana (Δ . 1. tetra . Hydrocannabinol) CH. 3. CH. 2. OH. General Pathway of Drug Metabolism. H. H-C-H. Allylic Hydroxylation of Marijuana (Δ 1
Phase 1 & 2 Liver Detoxification Inside the liver cells there are sophisticated mechanisms that have evolved over millions of years to break down toxic substances. Every drug, artificial chemical, pesticide and hormone, is broken down (metabolised) by enzyme pathways inside the liver cells.
Phase I reactions prepare a drug for the subsequent phase II reactions. The latter are the true detoxification pathways which result in products that are generally water-soluble and easily excreted in urine or bile.5 The metabolic biotransformation of paracetamol predominantly proceeds through phase II pathways in the liver (Figure I). The main reaction is hepatic conjugation with glucuronic
Phase I reactions are not necessary if a drug molecule already contains functional groups suitable for conjugation. An example is morphine, which has two hydroxyl groups. The conjugation of either, or both, with glucuronic acid is sufficient for excretion. Interestingly, one of the two single glucuronides—the one
What phase 1 reaction is mainly performed by the cytochrome P450 enzymes also called mixed-function enzymes?
It is important to bear in mind that some phase II reactions can occur without phase I metabolism, but phase I and phase II reactions are complimentary and not mutually exclusive. This report describes the chemical reactions of drug metabolism and explains how they occur in vivo.
Metabolism of drugs is usually divided into phase 1 and phase 2. Some drugs just undergo one or the Some drugs just undergo one or the other but the majority will undergo phase 1 and then phase 2 …
phase 1 metabolism (modification reactions) and phase 2 metabolism (conjugation reactions). Phase 1 metabolism typically subjects the drug to oxida-tion or hydrolysis. It involves the cytochrome P450 (CYP) enzymes, which facilitate reactions that include N-,0-, and S-dealkylation; aromatic, aliphatic, or A^-hydroxylation; A^-oxidation; sulfoxidation; deamination; and dehalogenation. Phase 2
1.1.1.7. Drug metabolism. 1.1.1.7.1. Phase I enzymes. Phase I enzymes [Ref: SH4:p15] Enzymes involved in phase I reactions include: Cytochrome P-450 enzymes Non-cytochrome P-450 Enzymes (Esters) Flavin-containing monooxygenase enzymes 1. Cytochrome P-450 enzymes. aka mixed function oxidase system, or monooxygenases Superfamily of membrane-bound heme proteins * …
CONCLUSIONS: Phase II drug metabolizing enzymes play an important role in biotransformation of endogenous compounds and xenobiotics to more easily excretable forms as well as in the metabolic inactivation of pharmacologically active compounds. Reduced metabolising capacity of Phase II enzymes can lead to toxic effects of clinically used drugs. Gene polymorphism/ lack of these …
Phase 2: Conjugation. Masking of an exist. funct. group by for instance acetylation, glycosylation, attachment amino acid etc More hydrophilic drug Renal excretion HO O OH N CH3 Morphine Demethylation Phase 1 O HO OH NH Conjugation glucuronic acid Phase 2 HO O O NH O OH CO2H HO OH. Phase 1 Metabolism by cytochrome P450 enzyme systhem (CYP450) •Located in …
Phase 1 Detoxification Pathway A Delicate Balance
Drug metabolism University of Waterloo
1 Liver phases 1 and 2 detoxification pathways What are the symptoms of a dysfunctional liver? Abnormal metabolism of fats (lipids) leading to –
Phase 1 and 2 metabolism refer to a range of chemical reactions. They can be distinguished by a They can be distinguished by a number of unique features, as shown in the table below.
What phase 1 reaction is mainly performed by the cytochrome P450 enzymes also called mixed-function enzymes?
phase 1 metabolism (modification reactions) and phase 2 metabolism (conjugation reactions). Phase 1 metabolism typically subjects the drug to oxida-tion or hydrolysis. It involves the cytochrome P450 (CYP) enzymes, which facilitate reactions that include N-,0-, and S-dealkylation; aromatic, aliphatic, or A^-hydroxylation; A^-oxidation; sulfoxidation; deamination; and dehalogenation. Phase 2
Phase I and Phase II Reactions — Overview Phase I characteristics : Parent drug is altered by introducing or exposing a functional group (-OH,-NH 2 , -SH)
Phase 1 metabolism involveschemical reactions such as oxidation (most common), reduction and hydrolysis. There are three possible results of phase 1 metabolism. Thedrug becomes completely inactive. In other words, the metabolites are pharmacologically inactive.
CONCLUSIONS: Phase II drug metabolizing enzymes play an important role in biotransformation of endogenous compounds and xenobiotics to more easily excretable forms as well as in the metabolic inactivation of pharmacologically active compounds. Reduced metabolising capacity of Phase II enzymes can lead to toxic effects of clinically used drugs. Gene polymorphism/ lack of these …
The primary site of drug metabolism is the liver, the organ that plays a major role in metabolism, digestion, detoxification, and elimination of substances from the body.
Phases of Metabolism Drug biotransformation could be classified into two phases 1. Phase I (functionalization): Non polar drugs are either inactivated; or activated in
phase of drug metabolism; reactions carried out by phase 1 enzymes usually lead to the inactivation of an active drug. In certain instances, metabolism, usually the hydrol- ysis of an ester or amide linkage, results in bioactivation of a drug. Inactive drugs that undergo metabolism to an active drug are called prodrugs. An example is the anti-tumor drug cyclophosphamide, which is bioactivated
(PDF) Comparison of Major Phase I and Phase II Metabolism
Phase I vs. Phase II Metabolism Pharmacology
General Pathway of Drug Metabolism. PHASE 1 & PHASE 2 REACTION. Oxidation & Conjugation Reaction. Phase 1 & Phase 2 . reactions complement one another in detoxifying & facilitating the elimination of drugs & Xenobiotics. Allylic. Hydroxylation of Marijuana (Δ . 1. tetra . Hydrocannabinol) CH. 3. CH. 2. OH. General Pathway of Drug Metabolism. H. H-C-H. Allylic Hydroxylation of Marijuana (Δ 1
The chemistry of drug metabolism UK Essays UKEssays
Drug Metabolism Phase 1 & 2 Reactions Flashcards Quizlet
CONCLUSIONS: Phase II drug metabolizing enzymes play an important role in biotransformation of endogenous compounds and xenobiotics to more easily excretable forms as well as in the metabolic inactivation of pharmacologically active compounds. Reduced metabolising capacity of Phase II enzymes can lead to toxic effects of clinically used drugs. Gene polymorphism/ lack of these …
(PDF) Comparison of Major Phase I and Phase II Metabolism
Phase I Drug Metabolism: Enzymes, Substrates, and Antibodies 12 Drug Conjugate Analysis: Enzymes, Substrates and Inhibitors, and Derivitization Reagents 22 Cover: Although phase I drug metabolism occurs in most tissues, the primary and first pass site of metabolism occurs during hepatic circulation. Biofilesonline Your gateway to Biochemicals and Reagents for Life Science Research Biofiles
Phase I reaction definition of Phase I reaction by