Pharmacokinetics Ppt: Slides 64-95, Megan's Portion
Questions and Answers
- 1.
In a _______________, all drug administration occurs directly into the central compartment and distribution of drug is instantaneous throughout the volume.
- A.
One compartment model
- B.
Multiple compartment model
Correct Answer
A. One compartment modelExplanation
In a one compartment model, all drug administration occurs directly into the central compartment and distribution of the drug is instantaneous throughout the volume. This means that there is only one compartment or space in the body where the drug is distributed, and it is assumed that the drug is evenly distributed throughout this compartment. This simplifies the pharmacokinetic analysis and calculations, as there is no need to account for multiple compartments or complex distribution processes.Rate this question:
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- 2.
Clearance from this compartment in a one compartment model is a _____-order process: the amount of drug eliminated per unit of time depends on the amount (concentration) of drug in the body compartment.
- A.
Second
- B.
First
- C.
Zero
Correct Answer
B. FirstExplanation
In a one compartment model, the clearance from the compartment is a first-order process. This means that the rate at which the drug is eliminated from the body depends on the concentration of the drug in the compartment. As the concentration decreases, the elimination rate also decreases. This is characteristic of a first-order process, where the elimination rate is proportional to the drug concentration.Rate this question:
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- 3.
After drugs are distributed, they are: 1.Redistributed (away from or towards)the tissues 2.Eliminated through Metabolism(aka biotransformation) and elimination
- A.
Towards;metabolism, elimination
- B.
Away from;elimination, metabolism
- C.
Away from ;metabolism, elimination
- D.
Away from;metabolism, absorption
Correct Answer
C. Away from ;metabolism, eliminationExplanation
After drugs are distributed, they are eliminated through metabolism and elimination. This means that the drugs undergo biotransformation in the body and are then eliminated from the body. They are not redistributed back to the tissues or absorbed further into the body. Instead, they are broken down and eliminated through processes such as urine or feces.Rate this question:
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- 4.
A drug that makes an inactive drug active is called a _______
- A.
Activator
- B.
Prodrome
- C.
Prodrug
- D.
Proformer
Correct Answer
C. ProdrugExplanation
A drug that makes an inactive drug active is called a prodrug. Prodrugs are biologically inactive compounds that are converted into an active form within the body. This conversion can occur through various mechanisms such as enzymatic reactions or chemical transformations. The purpose of using prodrugs is to enhance the drug's therapeutic effects, improve its stability, or reduce its side effects. By converting an inactive drug into an active form, prodrugs can increase the drug's bioavailability and improve its pharmacokinetic properties.Rate this question:
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- 5.
Through metabolism, an active drug may become inactive, which is an abnormal process of elimination.
- A.
True
- B.
False
Correct Answer
B. FalseExplanation
=NORMAL processRate this question:
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- 6.
Which is NOT an effect of metabolism?
- A.
Make an active drug inactive:
- B.
Make a toxic drug non-toxic
- C.
Make an inactive drug active
- D.
Make a drug toxic
Correct Answer
B. Make a toxic drug non-toxicExplanation
Metabolism is the process by which the body breaks down substances, such as drugs, and transforms them into different forms. One of the effects of metabolism is the conversion of inactive drugs into active forms, which can then exert their intended effects in the body. Another effect is the detoxification of toxic drugs, which involves converting them into non-toxic forms that can be easily eliminated from the body. However, the given answer states that metabolism does not make a toxic drug non-toxic, which contradicts the known effects of metabolism. Therefore, the given answer is incorrect.Rate this question:
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- 7.
The _is the main metabolic organ.
- A.
Thyroid
- B.
Kidneys
- C.
Spleen
- D.
Liver
Correct Answer
D. LiverExplanation
The liver is the main metabolic organ in the body. It plays a crucial role in breaking down nutrients, producing energy, and detoxifying harmful substances. It metabolizes carbohydrates, proteins, and fats, and stores vitamins and minerals. Additionally, the liver produces bile, which aids in digestion and absorption of fats. Overall, the liver is essential for maintaining overall metabolic balance and proper functioning of the body.Rate this question:
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- 8.
What type of drug metabolism is important for activation or break down of a drug, and will help determine the dosage you'll give the patient?
- A.
Second-pass metabolism
- B.
First-pass metabolism
- C.
Zero-order metabolism
- D.
First-order metabolism
Correct Answer
B. First-pass metabolismExplanation
First-pass metabolism is the type of drug metabolism that is important for the activation or breakdown of a drug. It occurs when a drug is metabolized in the liver before it enters the systemic circulation. This process can greatly affect the bioavailability and effectiveness of a drug, as well as determine the dosage that should be given to a patient. Therefore, understanding first-pass metabolism is crucial in determining the appropriate dosage for a patient.Rate this question:
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- 9.
Following Phase I metabolism, a drug is MOST often:
- A.
Activated
- B.
Inactivated
- C.
Unchanged
- D.
Changed
Correct Answer
B. InactivatedExplanation
After Phase I metabolism, a drug is most often inactivated. Phase I metabolism involves oxidation, reduction, or hydrolysis reactions, which introduce or expose functional groups on the drug molecule. These reactions typically increase the polarity of the drug, making it more water-soluble and easier to eliminate from the body. Inactivation of the drug occurs when these reactions render the drug less pharmacologically active or completely inactive. Therefore, it is common for drugs to undergo inactivation during Phase I metabolism.Rate this question:
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- 10.
A conjugated drug is usually:
- A.
Inactive
- B.
Active
Correct Answer
A. InactiveExplanation
A conjugated drug is usually inactive. Conjugation refers to the process of attaching a molecule or group to a drug molecule, which can alter its properties. In the case of conjugated drugs, the attached molecule or group typically reduces the drug's activity or renders it inactive altogether. This modification is often done to improve the drug's stability, increase its solubility, or enhance its targeting to specific cells or tissues. Therefore, a conjugated drug is generally not active on its own.Rate this question:
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- 11.
What event (according to her notes) will NOT happen to a drug after Phase I metabolism?
- A.
Oxidation
- B.
Hydrolysis
- C.
Reduction
- D.
Protonation
Correct Answer
D. ProtonationExplanation
After Phase I metabolism, a drug undergoes various chemical reactions that modify its structure. Oxidation, hydrolysis, and reduction are common events that can occur during Phase I metabolism. However, protonation is not a typical event in Phase I metabolism. Protonation refers to the addition of a proton to a molecule, which typically occurs during Phase II metabolism. Therefore, according to the notes, protonation is the event that will NOT happen to a drug after Phase I metabolism.Rate this question:
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- 12.
Phase I reactions do NOT utilize P450 system at all.
- A.
True
- B.
False
Correct Answer
B. FalseExplanation
both. There are Phase I reactions which use the P450 system and ones that do not.Rate this question:
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- 13.
True or false: Phase I and Phase II drug metabolism both make hydrophobic drugs more polar to promote their elimination.
- A.
True
- B.
False
Correct Answer
A. TrueExplanation
Phase I and Phase II drug metabolism both involve processes that aim to make hydrophobic drugs more polar. Phase I reactions, such as oxidation, reduction, and hydrolysis, introduce or expose functional groups that increase the polarity of the drug. Phase II reactions, such as glucuronidation, sulfation, and methylation, further increase the polarity by conjugating the drug with highly polar molecules. These modifications enhance the solubility of the drug, facilitating its elimination from the body through urine or bile. Therefore, both Phase I and Phase II drug metabolism contribute to the conversion of hydrophobic drugs into more polar forms for efficient elimination.Rate this question:
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- 14.
Phase I reactions generally add a___________ on the drug to slightly increase water solubility.
- A.
Hydroxyl group
- B.
Amine group
- C.
Large polar group
Correct Answer
A. Hydroxyl groupExplanation
Phase I reactions generally add a hydroxyl group on the drug to slightly increase water solubility. This is because the addition of a hydroxyl group (-OH) increases the polarity of the molecule, making it more soluble in water. This increased solubility allows the drug to be more easily transported and eliminated from the body. Additionally, the hydroxyl group can also serve as a site for further metabolism or conjugation reactions in Phase II metabolism.Rate this question:
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- 15.
Phase II reactions generally add ___________ to the hydroxyl group on the drug to greatly increase water solubility.
- A.
A large polar group
- B.
Another hydroxyl group
- C.
An amine group
- D.
A fat soluble group
Correct Answer
A. A large polar groupExplanation
Phase II reactions generally add a large polar group to the hydroxyl group on the drug to greatly increase water solubility. This is because adding a large polar group, such as a sulfate or glucuronide, increases the polarity of the drug molecule, making it more soluble in water. Increased water solubility is important for the elimination of drugs from the body, as they can be easily excreted through urine or bile. Adding another hydroxyl group, an amine group, or a fat soluble group would not have the same effect on water solubility.Rate this question:
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- 16.
The consequence of Phase I reaction is a _______ in the drug's activity.
- A.
Increase
- B.
Inactivation
- C.
Decrease
- D.
Change
Correct Answer
D. ChangeExplanation
The consequence of Phase I reaction is a change in the drug's activity. Phase I reactions involve the modification of the drug's structure, such as oxidation, reduction, or hydrolysis. These modifications can alter the drug's pharmacological properties, including its potency, efficacy, and toxicity. Therefore, the drug's activity is likely to be different after undergoing Phase I metabolism.Rate this question:
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- 17.
The consequence of Phase II reaction is _______ in the drug's elimination.
- A.
A decrease
- B.
An increase
- C.
A change
- D.
No effect
Correct Answer
B. An increaseExplanation
During Phase II reactions, drugs are metabolized by enzymes in the liver, which often leads to the addition of certain molecules, such as glucuronic acid or sulfate. This process increases the drug's polarity and makes it more water-soluble, facilitating its elimination from the body. Therefore, the consequence of Phase II reaction is an increase in the drug's elimination.Rate this question:
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- 18.
What does DMMS stand for?
- A.
Drug minimizing metabolic stereoisomer
- B.
Drug microsomal metabolizing system
- C.
Drug minimizing metabolizing stereoisomer
Correct Answer
B. Drug microsomal metabolizing systemExplanation
The correct answer is "drug microsomal metabolizing system." DMMS stands for drug microsomal metabolizing system. This term refers to the enzymatic system present in the liver that is responsible for metabolizing drugs and other foreign substances. The microsomal metabolizing system plays a crucial role in drug metabolism, as it helps to break down drugs into smaller, more easily eliminated molecules. This system is important in determining the effectiveness and toxicity of drugs in the body.Rate this question:
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- 19.
When a parent drug is metabolized by a DMMS enzyme, the oxidized metabolite gives off _____ and ______
- A.
H20, NADP+
- B.
NADP+, OH-
- C.
H+, NADP+
- D.
ADP+, H20
Correct Answer
A. H20, NADP+Explanation
Didn't know I was in Chem 101 againRate this question:
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- 20.
Fill in blanks regarding the nomenclature of CYP enzymes: CYP+ number (_______)+ capital letter (_________)+ number (_____________) example: CYP3A4
- A.
Subfamily,family, specific isozyme
- B.
Family, subfamily,specific isozyme
- C.
Phase reaction, family, subfamily
- D.
Family, subfamily, phase reaction
Correct Answer
B. Family, subfamily,specific isozymeExplanation
The correct answer is family, subfamily, specific isozyme. This is the correct nomenclature for CYP enzymes, where the family is identified first, followed by the subfamily, and then the specific isozyme.Rate this question:
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- 21.
Fill in blanks: -The Cytochrome P450 system is made of Microsomal mixed-function _________. -It metabolizes many ________compounds (steroids, lipids, etc) and biotransforms _________substances (xenobiotics). -It is a superfamily of _____-containing isozymes located in most cells but primarily in liver and GI tract
- A.
Oxidases, endogenous, exogenous, heme
- B.
Proteases,endogenous, exogenous, hydroxyl
- C.
Hydroxylases, exogenous, endogenous,protein
Correct Answer
A. Oxidases, endogenous, exogenous, hemeExplanation
see slide 78Rate this question:
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- 22.
What CYP enzyme is found in high concentrations in the intestinal mucosa, and participates in first-pass metabolism of chlorpromazine and clonazepam?
- A.
CYP637
- B.
CYP3B4
- C.
CYP3A4
Correct Answer
C. CYP3A4Explanation
CYP3A4 is the correct answer because it is an enzyme that is found in high concentrations in the intestinal mucosa and is involved in the first-pass metabolism of drugs such as chlorpromazine and clonazepam. This means that CYP3A4 plays a significant role in breaking down these drugs in the intestines before they are absorbed into the bloodstream.Rate this question:
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- 23.
Activation of ________, a prodrug, requires both metabolism by CYP2C19 and CYP3A4
- A.
Clonazepam
- B.
Clopidogrel
- C.
Ativan
Correct Answer
B. ClopidogrelExplanation
slide 81 kineticsRate this question:
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- 24.
Inducers of CYPs cause ___________in drug metabolism.
- A.
An increase
- B.
A decrease
- C.
No effect
Correct Answer
A. An increaseExplanation
Inducers of CYPs (cytochrome P450 enzymes) increase the activity of these enzymes, leading to an increase in drug metabolism. This means that drugs are broken down more quickly in the body, resulting in a decrease in their effectiveness and potentially requiring higher doses for the desired therapeutic effect. Inducers can include certain medications, herbal supplements, and environmental factors, and their impact on drug metabolism should be considered when prescribing or adjusting medication regimens.Rate this question:
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- 25.
Inducers of CYPs, which cause an increase in drug metabolism, have consequences. What choice below is NOT one such consequence?
- A.
Decreased plasma drug concentrations ●
- B.
Increased drug activity if metabolite is active
- C.
Decreased drug activity if the metabolite is inactive
- D.
Increased drug activity if the metabolite is inactive
- E.
Decreased therapeutic drug effect
Correct Answer
D. Increased drug activity if the metabolite is inactiveExplanation
Inducers of CYPs increase drug metabolism, leading to the production of metabolites. If the metabolite is active, it can result in increased drug activity. If the metabolite is inactive, it may not contribute to the drug's activity. However, the given answer states that there is an increased drug activity if the metabolite is inactive, which contradicts the expected outcome. Therefore, this choice is NOT one of the consequences of inducers of CYPs.Rate this question:
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- 26.
What are two common inducers for Warfarin, Ibuprofen,Tolbutamide, and Phenytoin?
- A.
Phenobarbital, Rifampin
- B.
Rifampin, Warfarin
- C.
Warfarin, Phenobarbital
Correct Answer
A. Phenobarbital, RifampinExplanation
Phenobarbital and Rifampin are two common inducers for Warfarin, Ibuprofen, Tolbutamide, and Phenytoin. These drugs are known to increase the metabolism of other medications by inducing certain liver enzymes, such as cytochrome P450 enzymes. Phenobarbital is a barbiturate that is commonly used as an anticonvulsant, while Rifampin is an antibiotic used to treat tuberculosis and other bacterial infections. Both drugs can enhance the breakdown of Warfarin, Ibuprofen, Tolbutamide, and Phenytoin in the liver, leading to reduced levels and potentially decreased efficacy of these medications.Rate this question:
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- 27.
Desipramine, Imipramine,Haloperidol,propanolol are VERY susceptible to enzyme induction.
- A.
True
- B.
False
Correct Answer
B. FalseExplanation
They don't really have inducers and are not commonly susceptible to induction.Rate this question:
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- 28.
Inhibitors of CYPs cause __________ in drug metabolism.
- A.
A decrease
- B.
An increase
- C.
No effect
Correct Answer
A. A decreaseExplanation
Inhibitors of CYPs (cytochrome P450 enzymes) cause a decrease in drug metabolism. CYPs are responsible for the metabolism of many drugs in the liver, and inhibitors of these enzymes can interfere with their activity. When CYP activity is inhibited, the metabolism of drugs is slowed down, leading to higher drug levels in the body and potentially increased drug toxicity. Therefore, the correct answer is a decrease in drug metabolism.Rate this question:
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- 29.
Inhibitors of CYPs cause a decrease in drug metabolism, of which there are consequences. Of the choices below, which is NOT a consequence of CYP inhibitors? : 1.Increased plasma drug concentrations ● 2.Increased drug activity if the metabolite is inactive ● 3.Decreased drug activity if metabolite is active ● 4.Increased therapeutic drug effect
- A.
Increased plasma drug concentrations
- B.
Increased drug activity if the metabolite is inactive
- C.
Decreased drug activity if metabolite is active
- D.
Increased therapeutic drug effect
- E.
Decreased therapeutic drug effect
Correct Answer
E. Decreased therapeutic drug effectExplanation
Inhibitors of CYPs cause a decrease in drug metabolism, which leads to increased plasma drug concentrations. This can result in increased drug activity if the metabolite is inactive and decreased drug activity if the metabolite is active. However, it does not lead to an increased therapeutic drug effect. In fact, a decreased therapeutic drug effect is a consequence of decreased drug metabolism, not CYP inhibitors.Rate this question:
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- 30.
The oxidation reactions NOT catalyzed by Cytochrome P450 include: 1) Flavin containing monoxygenase system 2) Alcohol dehydrogenase 3) Aldehyde oxidation 4) Xanthine oxidase 5) Amine oxidases 6) Flavin oxidases
- A.
1-4
- B.
1,3,5
- C.
1-5
- D.
1-4, 6
Correct Answer
C. 1-5Explanation
The correct answer is 1-5 because the oxidation reactions not catalyzed by Cytochrome P450 include the Flavin containing monoxygenase system, Alcohol dehydrogenase, Aldehyde oxidation, Xanthine oxidase, and Amine oxidases. Flavin oxidases are not mentioned in the list of oxidation reactions not catalyzed by Cytochrome P450.Rate this question:
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- 31.
The Flavin containing monoxygenase system, an oxidation rxn that is not catalyzed by CYP450. Fill in the blanks regarding this system below: –Present mainly in ______but some is expressed in gut and lung –Located in ____________ –_________compounds containing sulfur and nitrogen –Uses ____________ as cofactors
- A.
Liver, smooth ER, oxidizes, NAD/NADPH
- B.
Brain, golgi, reduces, NAD/NADPH
- C.
Kidneys, smooth ER, oxidizes, NAD/NADPH
Correct Answer
A. Liver, smooth ER, oxidizes, NAD/NADPHExplanation
The correct answer is liver, smooth ER, oxidizes, NAD/NADPH. The Flavin containing monoxygenase system is mainly present in the liver, but some is also expressed in the gut and lung. It is located in the smooth endoplasmic reticulum. This system oxidizes compounds containing sulfur and nitrogen. It uses NAD/NADPH as cofactors.Rate this question:
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- 32.
What two oxidation rxns that are not catalyzed by CYP450 take place in cellular cytosol? Alcohol dehydrogenase Aldehyde oxidation •Xanthine oxidase •Amine oxidases
- A.
Alcohol dehydrogenase, Amine oxidases
- B.
Aldehyde oxidation, Xanthine oxidase
- C.
Aldehyde oxidation, Amine oxidases
- D.
Alcohol dehydrogenase, Aldehyde oxidation
Correct Answer
D. Alcohol dehydrogenase, Aldehyde oxidationExplanation
Think Al.d, Al.oRate this question:
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- 33.
Of the amine oxidases, (oxidation rxns not catalyzed by CYP450): Monoamine oxidase is found in ________________, while Diamine oxidase found in _____________ and have __________metabolism.
- A.
Kidneys, brain, endogenous
- B.
Liver microsomes, nerve terminals/mitochondria, exogenous
- C.
Nerve terminals/mitochondria, liver microsomes, endogenous
Correct Answer
C. Nerve terminals/mitochondria, liver microsomes, endogenousExplanation
Monoamine oxidase is found in nerve terminals/mitochondria, while Diamine oxidase is found in liver microsomes. Both enzymes are involved in the metabolism of endogenous substances.Rate this question:
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- 34.
The most important Phase II conjugation reaction according to her ppt, is :
- A.
Sulfation by Sulfotransferase
- B.
Glucuronidation by UDP-Glucuronosyltransferase
- C.
Amino acid conjugation
- D.
Fatty acid conjugation
Correct Answer
B. Glucuronidation by UDP-GlucuronosyltransferaseExplanation
According to her ppt, the most important Phase II conjugation reaction is glucuronidation by UDP-Glucuronosyltransferase. This reaction involves the transfer of a glucuronic acid molecule from UDP-glucuronic acid to a substrate molecule, resulting in the formation of a glucuronide conjugate. Glucuronidation is a major pathway for the metabolism and elimination of many endogenous compounds and xenobiotics. It plays a crucial role in detoxification and clearance of drugs, toxins, and other foreign substances from the body.Rate this question:
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- 35.
A drug like Diazepam would reive a _____ from ______ in a Phase ____ reaction. In a Phase ____ reaction, Diazepam would receive a ________ from ___________.
- A.
Hydroxyl group, DMMP, II
- B.
Hydroxyl group, CYP450, II, I, sugar group, glucoronidation
- C.
Hydroxyl group, CYP450, I, II, sugar group, glucoronidation
Correct Answer
C. Hydroxyl group, CYP450, I, II, sugar group, glucoronidationExplanation
In a Phase I reaction, Diazepam would receive a hydroxyl group from CYP450. In a Phase II reaction, Diazepam would receive a sugar group from glucuronidation.Rate this question:
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- 36.
A drug is eliminated by metabolism and excretion, or by _______only .
- A.
Excretion
- B.
Absorption
- C.
Metabolism
Correct Answer
A. ExcretionExplanation
A drug is eliminated from the body through two main processes: metabolism and excretion. Metabolism involves the breakdown of the drug into various metabolites, which are then eliminated from the body. Excretion, on the other hand, refers to the removal of the drug or its metabolites from the body through urine, feces, sweat, or breath. Therefore, the correct answer is excretion, as it is the only process mentioned that is solely responsible for the elimination of drugs from the body.Rate this question:
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- 37.
In most clinical situations, the drug concentration [C] <<< Km. This represents the _________.
- A.
I JUST DONT CARE SERIOUSLY
- B.
Michaelis constant
- C.
I NEED DRUGS
Correct Answer
B. Michaelis constantExplanation
In most clinical situations, the drug concentration [C] is much smaller than the Michaelis constant (Km). This indicates that the drug concentration is significantly lower than the substrate concentration at which the enzyme is working at half of its maximum velocity. In other words, the drug concentration is not saturating the enzyme, and therefore, the enzyme is not working at its maximum efficiency.Rate this question:
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- 38.
The rate of drug metabolism and elimination is directly proportional to the concentration of free drug, known as __________.
- A.
First order kinetics
- B.
Zero order kinetics
- C.
Second order kinetics
- D.
I still have to write my PD write up! >:0
Correct Answer
A. First order kineticsExplanation
The rate of drug metabolism and elimination is directly proportional to the concentration of free drug, known as first order kinetics. This means that as the concentration of free drug increases, the rate of metabolism and elimination also increases. In first order kinetics, the rate of elimination is dependent on the concentration of the drug, leading to an exponential decrease in drug concentration over time. This type of kinetics is commonly observed for drugs that are metabolized by enzymes in the body.Rate this question:
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- 39.
The statement below represents what type of kinetics? The enzyme is saturated by a high free-drug concentration and the rate of metabolism remains constant over time.
- A.
Zero order
- B.
First order
- C.
Second order
Correct Answer
A. Zero orderExplanation
In zero order kinetics, the rate of metabolism remains constant over time regardless of the concentration of the substrate (in this case, the free-drug concentration). This means that the enzyme is saturated and working at its maximum capacity. Therefore, the given statement indicates zero order kinetics.Rate this question:
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- 40.
What are some common drugs that are zero order kinetics?aspirin, ethanol, phenytoin)
- A.
Aspirin
- B.
Phenytoin
- C.
Ethanol
- D.
Timbits!
- E.
All of the above, minus Timbits!
Correct Answer
E. All of the above, minus Timbits!Explanation
The correct answer is "All of the above, minus Timbits!" because aspirin, phenytoin, and ethanol are all examples of drugs that exhibit zero order kinetics. Zero order kinetics means that the rate of drug elimination remains constant regardless of the drug concentration in the body. This is in contrast to first order kinetics, where the rate of elimination is proportional to the drug concentration. Timbits is not a drug and therefore not relevant to the question.Rate this question:
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