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Questions and Answers
What is the primary substrate for glucuronidation?
What is the primary substrate for glucuronidation?
Which enzyme is responsible for the process of glucuronidation?
Which enzyme is responsible for the process of glucuronidation?
What substance is formed when tryptophan undergoes sulfation?
What substance is formed when tryptophan undergoes sulfation?
What is a consequence of low glutathione levels in tissues?
What is a consequence of low glutathione levels in tissues?
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Which compound acts as the active sulfate donor in sulfation?
Which compound acts as the active sulfate donor in sulfation?
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What is a xenobiotic?
What is a xenobiotic?
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Which organ is primarily responsible for biotransformation of xenobiotics?
Which organ is primarily responsible for biotransformation of xenobiotics?
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Which phase of xenobiotic metabolism primarily involves hydroxylation?
Which phase of xenobiotic metabolism primarily involves hydroxylation?
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What role do prodrugs play in xenobiotic metabolism?
What role do prodrugs play in xenobiotic metabolism?
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Which of the following effects is NOT associated with xenobiotics?
Which of the following effects is NOT associated with xenobiotics?
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Which reaction is catalyzed by Mono-oxygenases in phase 1 metabolism?
Which reaction is catalyzed by Mono-oxygenases in phase 1 metabolism?
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What is a common result of xenobiotic exposure in terms of DNA?
What is a common result of xenobiotic exposure in terms of DNA?
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What cofactor is involved in the reactions of cytochrome P450 during phase 1 metabolism?
What cofactor is involved in the reactions of cytochrome P450 during phase 1 metabolism?
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What effect does erythromycin have when taken with mevastatin?
What effect does erythromycin have when taken with mevastatin?
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Which CYP enzyme is primarily involved in the activation of carcinogenic substances from polycyclic aromatic hydrocarbons?
Which CYP enzyme is primarily involved in the activation of carcinogenic substances from polycyclic aromatic hydrocarbons?
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How many functional cytochrome P450 genes do humans have?
How many functional cytochrome P450 genes do humans have?
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Which of the following correctly describes CYP nomenclature?
Which of the following correctly describes CYP nomenclature?
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What defines obesity according to the provided content?
What defines obesity according to the provided content?
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What is the primary method used for diagnosing obesity?
What is the primary method used for diagnosing obesity?
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Which statement regarding most cytochrome P450 enzymes is correct?
Which statement regarding most cytochrome P450 enzymes is correct?
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Which of the following correctly describes energy intake?
Which of the following correctly describes energy intake?
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What is the primary function of methyl transferase in xenobiotic metabolism?
What is the primary function of methyl transferase in xenobiotic metabolism?
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What is the main aim of the phase 1 and phase 2 reactions in xenobiotic metabolism?
What is the main aim of the phase 1 and phase 2 reactions in xenobiotic metabolism?
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Which of the following statements is true about Cytochrome P450?
Which of the following statements is true about Cytochrome P450?
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What percentage of total drug metabolism is attributed to Cytochrome P450 enzymes?
What percentage of total drug metabolism is attributed to Cytochrome P450 enzymes?
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What factors can influence the activity of Cytochrome P450 enzymes?
What factors can influence the activity of Cytochrome P450 enzymes?
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How do many drugs interact adversely with CYP enzymes?
How do many drugs interact adversely with CYP enzymes?
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What is a potential consequence of CYP's role in drug metabolism?
What is a potential consequence of CYP's role in drug metabolism?
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Which drug interaction example was mentioned regarding mevastatin?
Which drug interaction example was mentioned regarding mevastatin?
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What is the initial treatment goal for weight loss?
What is the initial treatment goal for weight loss?
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Which of the following choices is NOT recommended as a part of dietary changes?
Which of the following choices is NOT recommended as a part of dietary changes?
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What is the typical recommended calorie intake for women aiming to lose weight?
What is the typical recommended calorie intake for women aiming to lose weight?
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How much physical activity is recommended weekly for obesity treatment?
How much physical activity is recommended weekly for obesity treatment?
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Which type of exercise is considered the most efficient way to burn calories?
Which type of exercise is considered the most efficient way to burn calories?
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What type of oils are recommended for replacing fats in the diet?
What type of oils are recommended for replacing fats in the diet?
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Which component is NOT a part of the treatment strategy for obesity?
Which component is NOT a part of the treatment strategy for obesity?
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What is suggested for maintaining weight loss after initial treatment?
What is suggested for maintaining weight loss after initial treatment?
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Study Notes
Metabolism of Xenobiotics
- Xenobiotic: A substance foreign to the body, including drugs, insecticides, and carcinogenic chemicals.
- Body's defense against xenobiotics includes redistribution, excretion, and metabolism, with metabolism being the primary mechanism.
- Biotransformation primarily occurs in the liver, which acts as a metabolic clearing house.
- The intestine serves as the initial site for drug metabolism and other organs like the lung, brain, and kidney are also involved.
- Xenobiotics can cause cell injury by binding to DNA, RNA, and proteins, leading to compromised cellular integrity.
- They may stimulate antibody production only when combined with cellular proteins, causing further cellular damage.
- Potential effects include carcinogenesis via DNA damage and impaired repair processes.
Phases of Xenobiotic Metabolism
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Phase 1: Involves drug modification primarily through hydroxylation, catalyzed by cytochrome P450 (CYP).
- Other reactions include oxidation, reduction, and hydrolysis.
- Some xenobiotics are converted from inactive to active forms (prodrugs).
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Phase 2: Focuses on conjugation processes like glucuronidation, sulfation, acetylation, and methylation.
- Glucuronidation: Conjugation with glucuronic acid via UDP glucuronic acid; bilirubin and certain acids are excreted as glucuronides.
- Sulfation: Involves sulfate conjugation mediated by PAPS; affects alcohol, phenols, and steroids.
- Glutathione Conjugation: Protects against toxic compounds; glutathione S-transferase facilitates this process.
- Both phases aim to make xenobiotics more soluble for easier excretion in urine or stool.
Cytochrome P450 (CYP)
- CYPs are hemoproteins primarily found in the liver, gut, and other organs, playing a vital role in drug metabolism.
- They participate in both Phase 1 and Phase 2 metabolism, as well as fat metabolism and steroid hormone production.
- Responsible for about 75% of drug metabolism, often making compounds inactive or sometimes activating them.
- Factors that influence CYP activity: genetic variations, age, gender, and health status.
- Drug interactions can occur when drugs alter CYP activity, leading to potential adverse effects (example: erythromycin and mevastatin interaction).
Types and Families of CYP
- Two main types: mitochondrial (inactivating O2) and microsomal (metabolizing xenobiotics).
- Humans possess 57 CYP genes categorized into 18 families and 43 sub-families, indicating diverse metabolic capabilities.
- CYP nomenclature involves the abbreviation CYP followed by gene family and subfamily indicators (e.g., CYP1A1).
- Most CYPs are inducible, meaning their production increases in response to the presence of xenobiotics.
Obesity
- Obesity is characterized by excessive body fat accumulation due to energy intake exceeding energy expenditure.
- Diagnosis primarily involves calculating Body Mass Index (BMI) and assessing for related health issues, such as hypertension and diabetes.
- Treatment plans typically aim for a 5% to 10% weight loss, focusing on dietary changes and increased physical activity.
- Diet should emphasize reducing caloric intake (1,200-1,800 calories/day), opting for nutrient-rich plant foods, lean proteins, and limiting sugars and fats.
- Exercise recommendations include at least 150 minutes of moderate physical activity weekly to support weight maintenance and loss.
- Medications may be prescribed to complement dietary and exercise efforts.
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Description
Test your knowledge on the metabolism of xenobiotics with this quiz. Learn about the different types of xenobiotics, including drugs and insecticides, and how the body processes these foreign compounds. Explore mechanisms like redistribution and excretion crucial for understanding biotransformation.