Term
| Which of the following factors increases absorption of a drug from the GI tract into the bloodstream? |
|
Definition
| being fat-soluble (lipophilic) |
|
|
Term
| According to the models, which of the following statements about receptor activation is true? |
|
Definition
-antagonist don't prefer actice or inactice forms of receptors
-agonists stabilize the active conformation of receptors to varying degress
-agonists are not essential for receptors to activate signaling pathways
-inverse agonists stabilize the inactive form of the receptor |
|
|
Term
| Which of the following routes of administration produces the most predictable and consistent concentration of drug in plasma? |
|
Definition
|
|
Term
| Which of the following can cause the accumulation of a drug in a particular part of the body that is higher than the concentration of drug in plasma? |
|
Definition
|
|
Term
| Which of the following is the amount of drug it takes to produce half of its maximum effect? |
|
Definition
|
|
Term
| Which would help to increase the elimination of a basic drug in urine? |
|
Definition
| increasing the acididty of the urine |
|
|
Term
| Which of the following is the most common route of drug elimination? |
|
Definition
|
|
Term
| Which of the following mechanisms can move a drug up its concentration gradient (from a compartment of lower to higher concentration)? |
|
Definition
|
|
Term
| Which of the following routes of administration is subject to the "first pass effect" or "first pass metabolism"? |
|
Definition
|
|
Term
| Which of the following is an effect of drug binding to plasma proteins? |
|
Definition
| it increases the distribution of very lipophilic drugs |
|
|
Term
| Which of the following drug metabolism reactions is MOST likely to have active metabolites? |
|
Definition
| Hydroxylation (oxidation) |
|
|
Term
| Based on the nomenclature system for CYP450, which two of the following CYP450 enzymes are most similar? (select the two that are the most similar to each other) |
|
Definition
|
|
Term
| Which of the following is (are) consequece of drug metabolism? |
|
Definition
-conversion to inactive metabolites
-conversion to active metabolites
-conversion to toxic metabolites
-metabolites with little or no change in activity |
|
|
Term
| Which of the following is NOT a property of drug metabolizing enzymes? |
|
Definition
|
|
Term
| When are drug-drug interactions most critical (select the two that are true) |
|
Definition
-when one drug has a narrow therapeutic index (increased risk of toxicity)
-when starting or stopping treatment with an inhibitor ir inducer |
|
|
Term
| The absorption of xenobiotics from the GI tract fliws in the blood directly to the liver for metabolism is generally described as: |
|
Definition
|
|
Term
| Inducers of drug metabolizing enzymes can be described as: |
|
Definition
| drugs that result in more drug metabolizing enzymes |
|
|
Term
| An investigational drug contains a metabolically sensitive ester that is hydrolyzed after oral adminstration. With this information, what can be said about the activity of the metabolites of this investigational compound? |
|
Definition
| without testing the metabolites, there is no way to accurately predict their activity. |
|
|
Term
| The metabolism of acetaminophen to N-acetyl-p-quinoneimine (NAPQI) is an example of drug metabolizing enzymes: |
|
Definition
| converting a drug to a toxic metabolite |
|
|
Term
| In the New England Journal of Medicine article you were asked to read, which CYP450 is responsible for the metabolism of felodipine? |
|
Definition
|
|
Term
| Which of the following concerning phase I reactions are TRUE? |
|
Definition
| most Phase I enzymes are located in the endoplastic reticulum |
|
|
Term
| Which of the following PHASE II drug metabolizing enzymes usually results in active metabolites? |
|
Definition
-acetylation
-methylation |
|
|
Term
| Which of the following is an example of a Phase II drug metabolizing enzyme? |
|
Definition
|
|
Term
| Which of the following is a pharmacokinetic parameter that can influence drug metabolism? |
|
Definition
|
|
Term
| A chemical foreign to the body can best be classified as a(an): |
|
Definition
|
|
Term
| During oral administration by a multiple-dosing regimen, the difference between the peaks and troughs in the plateau region of a plot of body burden (S) against time ie equivalent to which of the following? |
|
Definition
|
|
Term
| What kinetic parameter due to the physiochemical properties of a drug is a proportionality constant (an ratio) of the amount of drug in the body (S) or dose (DoseIV) to the concentration of drug in a biological fluid such as blood or plasma? |
|
Definition
| volume of distribution (Vd) |
|
|
Term
| Which of the following is an advantage of taking a drug orally versus an injected route? |
|
Definition
| the oral route is more concenient/simple |
|
|
Term
| Which of the following factors nearly always increases absorption of a drug from the gastrointestinal tract into the bloodstream? |
|
Definition
| being small and lipophilic |
|
|
Term
| Which would help to increase the elimination of an acidic drug via the kidneys? |
|
Definition
| alkalinization of the urine (making urine more basic) |
|
|
Term
| Which type of drugs will cross membranes by passive diffusion most readily? |
|
Definition
| small unionized lipophilic drugs |
|
|
Term
| How does binding to plasma proteins affect drug distribution? |
|
Definition
| it slows the rate at which drugs are eliminated |
|
|
Term
| Which of the following would most likely be the safest for patients? |
|
Definition
| a drug with a Certain Safety Factor (CSF) of 1500 |
|
|
Term
| What does a TD50 value tell you about a drug? |
|
Definition
| the dose that produces a toxic effect in half of the subjects that take it |
|
|
Term
| What is the difference between a non-competitive antagonist (NCA) and an irreversible competitive antagonist (ICA)? |
|
Definition
| an ICA binds to the same site as an agonist, but a NCA does not interfere with agonist binding |
|
|
Term
| According ro more recent models, which of the following statements about receptor activation is true? |
|
Definition
| agonists stabilize the active conformation of receptors to varying degrees |
|
|
Term
| What physiologically based pharmacokinetic parameter is the ratio of rate of elmination (dS/dt) by all routes of elimination to the concentration of the drug in the plasma? |
|
Definition
| total sytemic clearance (CLT) |
|
|
Term
| When are drug-drug interactions most critical? (select the two that are true) |
|
Definition
-when starting or stopping treatment with an inhibitor or inducer
-when one drug has a narrow therapeutic index (increased risk of toxicity) |
|
|
Term
| Which of the following drug metabolism reaction is MOST likely to have active metabolites? |
|
Definition
| Hydroxylation (oxidation) |
|
|
Term
| In the New England Journal of Medicine article you were asked to read, the metabolism of felodipine was ________ by _______? |
|
Definition
1. inhibited
2.grapefruit juice |
|
|
Term
| Based on the nomenclature system for CYP450, which two of the following CYP450 enzymes are most similar? (selecct the two that are the most similar to each other) |
|
Definition
|
|
Term
| What kinetic parameter due to the physiochemical properties of a drug is a proportionality constant (and ratio) of the amount of drug in the body (S) or dose (DoseIV) to the concentration of drug in a biological fluid such as blood or plasma? |
|
Definition
| volume of distribution (Vd) |
|
|
Term
| Inducers of drug metabolizing enzymes can be described as: |
|
Definition
| drugs that result in more drug metabolizing enzymes |
|
|
Term
| Which of the following are inducers of drug metabolizing enzymes? |
|
Definition
-Phenobarbital
-Cigarette smoke
-Polyaromatic hydrocarbons (PAH)
-St. Johns Wart |
|
|
Term
| A chemical foreign to the body can best be classified as a: |
|
Definition
|
|
Term
| Which of the following pharmacokinetic parameter that can influence drug metabolism? |
|
Definition
|
|
Term
| Which of the following is an example of a phase II drug metabolizing enzyme? |
|
Definition
|
|
Term
| Which of the following drug metabolizing enzymes can be induced by St. Johns Wort, inhibited by grapefruit juice, and is localized in the intestine as well as the liver? |
|
Definition
|
|
Term
| Which of the following correctly matches the physical property of a drug and how it may move through the body? |
|
Definition
| hydrophilic character facilitates elimination |
|
|
Term
| The absorption of xenobiotics from the GI tract flows in the blood directly to the liver for metabolism that is generally described as: |
|
Definition
|
|
Term
| Phase II drug metabolizing enzymes: |
|
Definition
| generally modify chemicals to greatly increase the hydrophilicity |
|
|
Term
| The metabolism of acetaminophen to N-acetyl-p-quinoneimine (NAPQI) is an example of drug metabolizing enzymes: |
|
Definition
| converting a drug to a toxic metabolite |
|
|
Term
| Which of the following Phase II drug metabolizing enzymes usually results in active metabolites? |
|
Definition
|
|
Term
| Which of the following means of a drug crossing a barrier requires energy and can transport a drug up its concentration gradient? |
|
Definition
|
|
Term
| Polymorphisms in drug metabolizing enzymes can best be described as individual variations in drug metabolism explained by differences in: |
|
Definition
|
|
