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83 Cards in this Set
- Front
- Back
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True/False
The water solubility of a drug usually decreases following biotransformation of the drug. |
False. increases
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True/False
Glucuronide conjugates excreted in the bile may be hydrolyzed in the intestine and the parent compound reabsorbed. |
True
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True/False
Elderly people tend to metabolize drugs more slowly than young adults. |
True
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True/False
In an average US population, the active form of CYP2C19 is missing in about 30% of people. |
False. 3-5%
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True/False
The liver is the major organ of drug metabolism. |
True
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True/False
About 50% of an average US population metabolizes isoniazid more slowly than the rest of the population. |
True
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True/False
People who cook and eat a lot of charcoal-broiled food have more CYP1A2 in their livers than people who are not exposed to smoke. |
True
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True/False
A person who has a viral disease will metabolize drugs more rapidly than when he or she is healthy. |
False. slowly
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True/False
Binge drinking can result in an acute lowering of NADPH in the liver. |
True
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True/False
Ritonavir will stimulate the biotransformation of drugs that are substrates for CYP3A4. |
False. inhibit
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True/False
The pharmacological activity of a drug may change following biotransformation. |
True
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True/False
Glucuronide conjugates can undergo entero-hepatic cycling. |
True
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True/False
Newborn babies can readily sulfate acetaminophen. |
True
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True/False
About 50% of people in the US population have an inactive form of CYP2D6. |
False. 1-15%
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True/False
The liver is the major organ of drug metabolism. |
True
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True/False
Gilbert’s syndrome is a deficiency in bilirubin glucuronidation. |
True
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True/False
Cigarette smokers who also drink ethanol chronically will have the same complement of cytochrome P450 in their livers as people who do not smoke or drink. |
False. different complement
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True/False
A person who has a viral disease may have a lower ability to metabolize drugs than when he or she is healthy. |
True
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True/False
A malnourished person is likely to have more glutathione in their cells than a well-nourished person. |
False. less
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True/False
Drug-drug interactions can occur when two drugs are biotransformed by the same enzyme. |
True
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True/False
The ability of a drug to bind to a receptor often changes following biotransformation of the drug. |
True
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True/False
Glucuronide conjugates of molecular weight less than 350 are usually excreted in bile. |
False. more
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True/False
Newborn babies cannot readily glucuronidate acetaminophen. |
True
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True/False
Between 5 and 10% of people in the US population do not have an active form of CYP2D6 |
True
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True/False
The liver is the major organ of drug metabolism. |
True
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True/False
People with Gilbert’s syndrome cannot readily form bilirubin glucuronide, due to polymorphism in UGT1A1. |
True
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True/False
Cigarette smokers have more CYP1A2 in their livers than people who do not smoke and are not exposed to smoke. |
True
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True/False
A person who has a viral disease may have a lower ability to metabolize drugs than when he or she is healthy. |
True
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True/False
A person on a protein-poor diet is likely to have less glutathione in their cells than someone who eats meat daily. |
True
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True/False
Drug-drug interactions can occur when two drugs are biotransformed by the same enzyme. |
True
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Which of the following drugs inhibit cytochrome P450
A. acetaminophen B. ketoconazole C. acetylsalicyclic acid D. cimetidine. E. isoniazid |
B. ketoconazole
D. cimetidine. |
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Which natural product in the following list is associated with the grapefruit juice effect on drug bioavailability?
A. epicatechin gallate B. rutin C. quercetin D. 6’,7’-dihydroxybergamottin E. Chrysin |
D. 6’,7’-dihydroxybergamottin
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Which of the following statements apply to a typical drug molecule?
1. A typical orally-administered drug has molecular weight less than 800 and is readily soluble in lipid. 2. A typical drug undergoes biotransformation to more lipid-soluble metabolites. 3. The pharmacological activity of a drug is often changed by biotransformation. 4. Biotransformation usually increases the toxicity of a drug. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
B = Only 1 and 3 are correct
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The therapeutic, clinically effective oral dose of Drug A is 100 mg, and the effective i.v. dose is 5 mg. Which of the following statement(s) are true for Drug A?
1. Drug A is not readily soluble in the fluid vehicle used in intravenous dose preparations. 2. Drug A undergoes extensive first-pass metabolism. 3. Drug A is has its site of action in the gastrointestinal tract. 4. Drug A is therapeutically active as the parent compound. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
C = Only 2 and 4 are correct
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Drug Z has a molecular weight of 310, contains a phenolic hydroxyl group, and is effective orally as an analgesic. Which of the following statements are correct?
1. Drug Z should not be given to newborn babies. 2. Drug Z is likely to be metabolized to a glucuronide that could undergo entero-hepatic cycling. 3. Drug Z is absorbed from the gastrointestinal tract. 4. Biotransformation of Drug Z is likely to be slower in elderly women than in young adults. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
E = All of the statements are correct
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A new drug for treatment of a chronic disease is under development. This drug contains an amine group, and the major pathway of metabolism of the drug is through phase II metabolism of this amine group to an inactive metabolite. Which of the following statements are likely to be included in the package insert?
1. This drug will not be metabolized by persons with a polymorphic variant of UGT2B15. 2. The dosage of this drug should be adjusted depending on the NAT- 2 acetylation activity status of the patient. 3. This drug will be poorly metabolized by patients with a viral infection. 4. Some patients will metabolize this drug more rapidly than others, depending on their genetic make-up. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
C = Only 2 and 4 are correct
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Which of the following factor(s) is or are likely to be important in relation to the safe use of drug F? Drug F is known to undergo phase 1 biotransformation by CYP2D6 to an inactive metabolite, followed by phase 2 metabolism by UDP-glucuronosyltransferase. The drug will be taken on a chronic basis and is not readily metabolized by CYP1A2, 2C8, 2C9, 2C18, 2C19 or 3A4.
1. Whether the patient regularly eats charcoal-broiled foods. 2. Whether or not the patient drinks orange juice in the morning, because natural products in oranges inhibit CYP2D6. 3. Whether or not the patient is taking phenobarbital, because phenobarbital will induce CYP2D6. 4. Whether or not the patient is a poor metabolizer of CYP2D6 substrates. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct |
D = Only 4 is correct
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In early August an asthmatic patient taking theophylline told you that his usual dose of theophylline had not been controlling his asthma attacks in the past few weeks as well as it used to in the cooler months. The patient was taking no other drugs, but did state that he drank more iced tea in the summer than the winter. What questions might help his pharmacist determine why the theophylline is less effective in August?
1. Do you use spend more time outdoors in summer, where you might be exposed to agents causing the asthma attacks? 2. Do you cook and eat more charcoal-barbecued food in the summer? 3. Have you taken up smoking, or have you spent a lot of time with smokers? 4. Do you eat more fish in the summer? A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct |
A = Only 1,2 and 3 are correct
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The effective oral dose of morphine for relieving severe pain is three to six times higher than the effective intravenous dose. Which of the following statement(s) best explain(s) this discrepancy in effective dose?
1. Morphine is very readily metabolized in the blood. 2. More of the intravenous dose of morphine arrives unchanged at the site of action in the brain compared to oral morphine. 3. Morphine is rapidly absorbed from the gastrointestinal tract. 4. Orally administered morphine is extensively metabolized in the intestine and liver to inactive metabolites before absorption to the systemic circulation. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
C = Only 2 and 4 are correct
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Which of the following statement(s) is (are) true with respect to entero-hepatic cycling?
1. Morphine (molecular weight 285) may form a glucuronide conjugate that undergoes entero-hepatic cycling 2. Acetaminophen (molecular weight 151) may form a glucuronide conjugate that undergoes entero-hepatic cycling. 3. Glucuronides excreted in bile may be hydrolyzed in the gastrointestinal tract and the parent drug reabsorbed. 4. Glucuronides excreted in bile may be hydrolyzed in the gall bladder and the parent drug reabsorbed A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
B = Only 1 and 3 are correct
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The major pathway of metabolism of a drug is found to be phase 1 biotransformation by CYP2D6 to an inactive metabolite, followed by phase 2 metabolism by UGT1A1. The drug will be taken on a chronic basis and is not metabolized by CYP3A4. Which of the following factors may be of clinical importance in deciding the appropriate dosage?
1. Whether or not the patient is taking other drugs that are metabolized by CYP3A4. 2. Whether or not the patient has an active form of CYP2D6. 3. The nutritional status of the patient, because poorly nourished patients have low concentrations of UDPGA in their liver. 4. Whether or not the patient expresses a polymorphic variant of UGT1A1 with low activity. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
C = Only 2 and 4 are correct
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Which of the following xenobiotics are likely to have a clinically observable effect on drug biotransformation pathways?
1. Ethanol 2. Polycyclic aromatic hydrocarbons produced by pyrolysis of organic matter 3. Carbamazepine 4. Ketoconazole. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
E = All of the statements are correct
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A new drug developed in Japan was very effective for a particular condition. Less than 30% of the Japanese patients reported toxicity, and toxicity was averted by lowering the dose. When the drug was introduced to Sweden, a much higher incidence of toxicity was found at the dose that was effective in most Japanese patients. What is the most likely explanation of this finding?
1. The new drug was better absorbed when taken with a typical Japanese diet. 2. The patients in Sweden did not comply with the dosing instructions as well as the Japanese. 3. The Japanese patients excreted the drug more slowly than the Swedish patients. 4. The drug was metabolized chiefly by N-acetyltransferase 2. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
D = Only 4 is correct
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Infants under 6 months of age were found to retain a size-adjusted dose of drug X in the body for much longer than adults. What is/are the most reasonable explanation(s).
1. Drug X has to be given by intramuscular injection to babies, so it is not metabolized in their livers. 2. Entero-hepatic cycling occurs for more drugs in babies than in adults so that more of drug X is re-absorbed by babies. 3. The major pathway of metabolism of drug X is sulfation, and babies can efficiently sulfate drugs. 4. The major pathway of metabolism of drug X is glucuronidation, and infants have low UDP-glucuronosyltransferase activity. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
D = Only 4 is correct
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A new drug for treatment of a chronic disease is under development. The major pathway of metabolism of this drug is monooxygenation by a single form of CYP to an inactive metabolite. It was shown that about 8% of an average US population metabolized the drug very slowly. Which of the following statements are likely to be included in the package insert?
1. This dosage of this drug may need to be adjusted in persons with a slow-metabolizer phenotype for CYP2D6. 2. Patients should not take this drug with grapefruit juice. 3. Some patients may exhibit a prolonged duration of action of this drug. 4. This drug should not be prescribed to patients over the age of 65. A = 1,2 3 are correct B = 1 and 3 are correct C = 2 and 4 are correct D = 4 is correct E = All are correct |
B = 1 and 3 are correct
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The effective oral dose of morphine is 3-4 times higher than the effective intravenous dose. Which of the following statement(s) best explain this differential.
1. Orally-administered morphine undergoes first pass metabolism in the intestine and liver, so less is available systemically. 2. Following oral administration, morphine undergoes glucuronidation, but this does not occur after intravenous administration. 3. It is likely that some orally administered morphine will not be absorbed across the gastrointestinal tract, whereas intravenous administration ensures the drug will be in the blood stream. 4. People become tolerant to oral morphine, but not to intravenously administered morphine. A = 1,2 3 are correct B = 1 and 3 are correct C = 2 and 4 are correct D = 4 is correct E = All are correct |
B = 1 and 3 are correct
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A drug is orally effective for treating an infectious disease caused by a microorganism, even though the drug itself, in laboratory testing with this micro-organism, does not kill or arrest growth of the microorganism. What is/are likely explanations for the effectiveness of this drug?
1. The drug acts as a placebo. 2. The drug is metabolized in the liver to an active metabolite but the micro-organism cannot perform this biotransformation. 3. The drug stimulates the immune system, and the body fights the disease. 4. The drug is a prodrug for an active anti-infective agent. A = 1,2 3 are correct B = 1 and 3 are correct C = 2 and 4 are correct D = 4 is correct E = All are correct |
C = 2 and 4 are correct
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Which of the following xenobiotics can interact with drug metabolizing systems to produce an effect on the metabolism of a second drug or xenobiotic.
1. Alcohol 2. 6’,7’-dihydroxybergamottin 3. Erythromycin 4. Acetylsalicyclic acid. A = 1,2 3 are correct B = 1 and 3 are correct C = 2 and 4 are correct D = 4 is correct E = All are correct |
A = 1,2 3 are correct
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A patient who is taking Phenobarbital to control seizures must take an antibiotic to treat an infection. If there was a choice of antibiotic what criteria would you apply to select the best one for this patient .
1. The antibiotic should be orally effective. 2. The antibiotic should not be metabolized to an inactive metabolite by CYP in the 2 and 3 family, because these are induced by Phenobarbital, and it may be difficult to select the correct dose. 3. The antibiotic should be effective with one-a-day dosing. 4. The antibiotic should not be inactivated by glucuronidation, because Phenobarbital induces glucuronosyltransferases. A = 1,2 3 are correct B = 1 and 3 are correct C = 2 and 4 are correct D = 4 is correct E = All are correct |
E = All are correct
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Gender contributes to variability in drug response via pharmacokinetic variables.
Fat to muscle ratio contributes to variability in drug response mostly via pharmacokinetic variables. A= Both statements are true: B= Both statements are false: C= The first statement is true and the second statement is false: D= The first statement is false and the second statement is true: |
A= Both statements are true:
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Which of the following statements apply to a typical drug molecule.
1. A typical orally-administered drug is more soluble in fat than water. 2. During biotransformation a typical drug is converted to readily excreted water-soluble metabolites. 3. The pharmacological activity of a drug can be altered by biotransformation. 4. Biotransformation usually increases the toxicity of a drug. A = 1,2 3 are correct B = 1 and 3 are correct C = 2 and 4 are correct D = 4 is correct E = All are correct |
A = 1,2 3 are correct
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Drug A is orally effective for treating an infectious disease caused by a microorganism, even though drug A itself, in laboratory testing with this micro-organism, does not kill or arrest growth of the microorganism. What is/are likely explanations for the effectiveness of drug B?
1. Drug B acts as a placebo. 2. Drug B is rapidly metabolized to an inactive metabolite by the infectious agent in the laboratory, but not in the body . 3. Drug B is inactivated by metabolism in the gastrointestinal tract. 4. Drug B is a prodrug for an active anti-infective agent, and is metabolized in the gastrointestinal tract to the active agent. A = 1,2 3 are correct B = 1 and 3 are correct C = 2 and 4 are correct D = 4 is correct E = All are correct |
D = 4 is correct
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A new drug for treatment of a chronic disease is under development. This drug contains an amine group, and phase 2 metabolism of this amine group to an inactive metabolite is the major pathway of metabolism of the drug. Which of the following statements are likely to be included in the package insert?
1. This drug should not be used by persons with a slow-metabolizer polymorphism for CYP2C19. 2. The dosage of this drug should be adjusted depending on the NAT-2 acetylator status of the patient. 3. This drug will be poorly metabolized by patients who eat a high carbohydrate diet. 4.Some patients will metabolize this drug more rapidly than others, depending on their genetic make-up. A = 1,2 3 are correct B = 1 and 3 are correct C = 2 and 4 are correct D = 4 is correct E = All are correct |
C = 2 and 4 are correct
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Drug M has a molecular weight of 350, contains a phenolic hydroxyl group, and is effective orally, though the effective oral dose is 20-times higher than the effective iv dose. Which of the following statements describe what happens when drug M is taken orally.
1. Drug Z does not become effective as quickly as when it is given i.v. 2. Drug Z is likely to be metabolized to a glucuronide that could undergo entero-hepatic cycling. 3. Drug Z is readily absorbed from the gastrointestinal tract. 4. Drug Z is extensively metabolized in the liver to inactive metabolites. A = 1,2 3 are correct B = 1 and 3 are correct C = 2 and 4 are correct D = 4 is correct E = All are correct |
E = All are correct
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Infants under 6 months of age were found to retain a size-adjusted dose of drug X in the body for much longer than adults. What is/are the most reasonable explanation(s).
1. Babies have poorly developed kidneys and cannot excrete drug X efficiently. 2. Babies have more fat than adults and the drug distributes into the fat. 3. The major pathway of metabolism of drug X is sulfation, and babies are unable to synthesize PAPS in their livers. 4. The major pathway of metabolism of drug X is glucuronidation, and infants have low UDP-glucuronosyltransferase activity A = 1,2 3 are correct B = 1 and 3 are correct C = 2 and 4 are correct D = 4 is correct E = All are correct |
D = 4 is correct
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Which of the following statements apply to a typical drug molecule that is orally effective.
1. The drug is lipid soluble. 2. During biotransformation the drug will be converted to water-soluble metabolites that are readily excreted. 3. The pharmacological activity of a drug can be altered by biotransformation. . 4. Biotransformation usually increases the toxicity of a drug. a = 1,2,3 are true b=1,3 are true c=2,4 are true d=4 is true e=all are true |
a = 1,2,3 are true
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Drug Z has a molecular weight of 300, contains a phenolic hydroxyl group, and is effective orally, though a much higher dose is needed orally than if the drug is given iv. Which of the following statements describe what happens when drug Z is taken orally.
1. Drug Z does not become effective as quickly as when it is given i.v. 2. Drug Z is likely to be metabolized to a glucuronide that could undergo entero-hepatic cycling. 3. Drug Z is readily absorbed from the gastrointestinal tract. 4. Drug Z is extensively metabolized in the liver to inactive metabolites. a = 1,2,3 are true b=1,3 are true c=2,4 are true d=4 is true e=all are true |
e=all are true
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A drug company has just developed a new drug that was very effective for treating type II diabetes in clinical trials with a small group of patients. In further studies it was shown that the drug was metabolized to inactive metabolites by CYP2C19 and CYP2D6. The drug was not metabolized by CYP3A4 or CYP2E1. What should be taken into consideration in setting the dose to be used?
1. Whether or not the patient drinks grapefruit juice on a regular basis. 2. Whether or not the patient expresses an active form of CYP2D6. 3. The patient should be cautioned not to take rifampicin with the new drug. 4. Whether or not the patient expresses a polymorphic variant of CYP2C19 with low activity. a = 1,2,3 are true b=1,3 are true c=2,4 are true d=4 is true e=all are true |
c=2,4 are true
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Drug B contains an amino group, and its main pathway of biotransformation is conversion to an inactive phase 2 metabolite. Drug B is used to treat a chronic disease, so that patient should take the drug daily for several years. Which of the following statements are true.
1. The rate of biotransformation of Drug B will vary considerably from person to person in a group of 500 US residents. 2. Drug B should not be given to newborn infants, because they lack the ability to metabolize drugs. 3. It would be a good idea to screen patients before giving them drug B, to determine if they are rapid or slow acetylators. 4. The nutritional status of the patient will affect how well they metabolize drug B. a = 1,2,3 are true b=1,3 are true c=2,4 are true d=4 is true e=all are true |
b=1,3 are true
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A patient with AIDS has developed a fungal disease. The patient is being treated with saquinavir (a protease inhibitor antiviral drug) to treat the HIV infection. Ketoconazole is an effective antifungal drug. Would ketoconazole be a good drug to use to treat the fungal disease in this patient?
1.Yes, as long as it is given at the same time as the saquinavir, so that both infections will be adequately treated. 2.No, because in patients with AIDS, drug absorption is lowered and the ketoconazole won’t be effective. 3.No, because patients with AIDS are often malnourished, and ketoconazole inhibits the formation of NADPH, which is needed to metabolize saquinavir. 4.If Ketoconazole and Saquinavir are given at the same time, the ketoconazole could inhibit the metabolism of saquinavir, which may lead to toxicity. Therefore, it would be better to use a different antifungal drug in this patient. a = 1,2,3 are true b=1,3 are true c=2,4 are true d=4 is true e=all are true |
d=4 is true
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True/False
The pharmacological activity of a drug may change following biotransformation. |
True
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True/False
The pharmacological activity of a drug is not altered by biotransformation. |
False. may change following
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True/False
Glutathione conjugates can undergo entero-hepatic cycling. |
False. cannot undergo
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True/False
Newborn babies cannot readily glucuronidate acetaminophen. |
True
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True/False
Newborn babies can readily sulfate acetaminophen. |
True
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True/False
Approximately 8% of people in the US population cannot readily metabolize substrates for CYP2D6. |
True
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True/False
About 50% of people in the US population have an inactive form of CYP2D6. |
False. 1-15%
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True/False
Gilbert’s syndrome is a syndrome in which bilirubin is glucuronidated slowly. |
True
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True/False
Women who take oral contraceptives containing ethynylestradiol should be careful about taking omeprazole for heartburn, because the omeprazole induces a form of cytochrome P450 that metabolizes the ethynylestradiol, and not enough ethynylestradiol will be absorbed to effectively suppress ovulation. |
False. ?
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True/False
Women who take oral contraceptives containing ethynylestradiol should be careful about taking St. John’s wort for depression, because the St. John’s wort induces a form of cytochrome P450 that metabolizes the ethynylestradiol, and not enough ethynylestradiol will be absorbed to effectively suppress ovulation. |
True
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True/False
A person who has a viral disease may have a lower ability to metabolize drugs than when he or she is healthy. |
True
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True/False
A person who does not eat enough protein for good nutrition is likely to have less glutathione in their cells than a well-nourished person |
True
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True/False
Drug-drug interactions can occur when two drugs are biotransformed by the same enzyme. |
True
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True/False
Someone who binge-drinks alcohol will transiently have lower NADPH in their liver and this could result in slower biotransformation of drugs that are normally metabolized by cytochrome P450. |
True
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Binge drinking affects which of the following cofactors or cosubstrates of drug biotransformation?
a. UDP-glucuronic acid b. PAP-sulfate c. NADPH d. Acetyl-Coenzyme A e. Glutathione |
c. NADPH
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Which natural product from the following list is a very potent inhibitor of CYP3A4 and p-glycoprotein transporter?
a. epicatechin gallate b. rutin c. quercetin d. 6', 7'-dihydroxybergamottin e. chrysin |
d. 6', 7'-dihydroxybergamottin
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The following drugs increase the expression of at least one form of cytochrome P450.
1. carbamazepine 2. omeprazole 3. phenobarbital 4. acetylsalicyclic acid A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
A = Only 1,2 and 3 are correct
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Which of the following statements apply to a typical drug molecule that is orally effective.
1. The drug is lipid soluble 2. The process of biotransformation will convert the drug to water-soluble metabolites that are readily excreted 3. The pharmacological activity of the drug may be altered by biotransformation 4. Biotransformation will increase the toxicity of the drug A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
A = Only 1,2 and 3 are correct
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Morphine has a molecular weight of 285 and contains a phenolic hydroxyl group. It is effective orally, through a 6-fold higher dose when needed orally than if the drug is given by intravenous or intramuscular injection. Which of the following statements describe what happens when morphine is taken orally?
1. Morphine does not become effective as quickly as when it is given intravenously. 2. Morphine is likely to be metabolized in the liver to a glucuronide conjugate, which could be excreted in bile. 3. Morphine is readily absorbed from the gastrointestinal tract 4. Morphine is metabolized in the intestine and liver to inactive metabolites. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
E = All of the statements are correct
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A drug company has just developed a new drug that was very effective for treating type II diabetes in clinical trials with a small group of patients (about 100). In further studies it was shown that the major pathway of metabolism in 95% of the patients was conversion by CYP2D6 to an inactive metabolite. The drug was also biotransformed to an inactive metabolite by CYP3A4, and this was a major pathway in 5% of the patients. What should be taken into consideration in setting the dose to be used?
1. Whether or not the patient drinks grapefruit juice on a regular basis. 2. Whether or not the patient has Gilbert's syndrome 3. The patient should be cautioned not to take rifampin with the new drug. 4. Whether or not the patient expresses an active form of CYP2D6. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
D = Only 4 is correct
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HIV positive patients are often given antiviral drugs to prevent the progression to AIDS. Which of the following statements are true about drug-drug interactions of ritonavir and other antiviral protease inhibitors?
1. Patients taking ritonavir should be cautious about eating apples, as there could be an interaction with bioflavonoids present in apples. 2. Ritonavir is given together with other protease inhibitors to increase the bioavailability of these antiviral agents. 3. HIV-positive patients are often malnourished, and may have insufficient NADPH in their liver to metabolize ritonavir. 4. Ritonavir has a very high affinity for CYP3A4 and can slow down the metabolism of other protease inhibitors. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
C = Only 2 and 4 are correct
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Drug B contains an amino group, and its main pathway of biotransformation is conversion to an inactive phase 2 metabolite. Drug B is used to treat a chronic disease, so that patients will need to take the drug daily for several years. Which of the following statements are true?
1. The rate of biotransformation of Drug B will vary considerably from person to person in a group of 500 US residents. 2. The most likely pathway of metabolism of Drug B is acetylation. 3. It would be a good idea to screen patients before giving them drug B, to determine if they are rapid or slow acetylators. 4. The nutritional status of the of the patient will affect how well they metabolize drug B. A = Only 1,2 and 3 are correct B = Only 1 and 3 are correct C = Only 2 and 4 are correct D = Only 4 is correct E = All of the statements are correct F = None of the statements are correct |
A = Only 1,2 and 3 are correct
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Which of the following statements apply to a typical drug molecule.
1. A typical orally-administered drug is more soluble in fat than water. 2. During biotransformation a typical drug is converted to readily excreted water-soluble metabolites. 3. The pharmacological activity of a drug can be altered by biotransformation. 4. Biotransformation usually increases the toxicity of a drug. A = 1,2 3 are correct B = 1 and 3 are correct C = 2 and 4 are correct D = 4 is correct E = All are correct |
A = 1,2 3 are correct
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