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33 Cards in this Set
- Front
- Back
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What are the most common sources of Adverse Drug Reactions?
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1. Because you cannot metabolize it
2. Because it is metabolized too quickly 3. Another drug increases or decreases metabolism |
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What should we know about the structure of Cytochrome P-450?
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Know it contains a heme group and involves O2
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What are the regulation differences between Phase I and Phase II metabolism?
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Phase I is Regulated
Phase II is NOT usually regulated |
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What is the general purpose of Phase II metabolism?
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Conjugate drug to a water soluble adduct using the polar handle (OH, COOH, NH2) from phase I. Makes it even more Hydrophilic
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What has to happen to lipophilic drugs in order to be eliminated?
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Must be made water soluble
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What are three types of metabolites?
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Active
Inactive Toxic |
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T/F
Drugs can be substrates AND inhibitors of P450 isozymes |
True
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What factors increase gastric emptying?
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Cold
Liquids (Fat) |
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What factors delay gastric emptying?
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Heat
Food Calcium |
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What is the primary determinant of drug distribution?
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Solubility and physicochemical properties
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A drug that is a Weak Organic Base with a large oil:water partition coefficient is likely to be characterized by?
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High affinity binding to alpha1-acid-glycoprotein
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Molecular oxygen is an iron-bound ligand for each of the following hemoproteins EXCEPT.
a) cytochrome c b) myoglobin c) hemoglobin d) cytochrome p450 |
cytochrome c
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Competitive inhibition of the metabolism of drug A by drug B could occur under which conditions?
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Drug A is present at a concentration in excess of its metabolic Km value
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Each of the following drug metabolic reactions require the action of cytochrome P450 Except.
a) epoxidation of benzo[a]pyrene b) hydrolysis of aspirin c) dealkylation of phenacetin d) hydroxylation of benzene e) S-oxidation of chlorpromazine |
Hydrolysis of aspirin
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Cytochrome P450 isozymes display each of the following properties Except.
a) one iron atom per enzyme molecule b) inhibition by carbon monoxide c) calcium dependent activation d) affinity for molecular oxygen e) broad substrate specificity |
calcium dependent activation
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Which of the following serves as a substrate for the drug metabolic activity of the cutochrome P450 system?
a) carbon monoxide b) adenosine triphosphate c) molecular oxygen d) glutathione e) water |
Molecular oxygen
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Formation of acetaminophen glucuronide is described by each of the following Except
a) Phase II conjugation reactions b) Glucose and UTP are precursors c) A transferase enzyme catalyzes the reaction d) A glutathione adduct with an activated metabolite e) A water soluble metabolite of acetaminophen |
A glutathione adduct with an activated metabolite
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What is characteristic of sulfate ester formation?
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Involves activation by ATP
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Glutathione transferase is a drug metabolic enzyme that?
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Leads to the detoxification of drug metabolites
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Each of the following can affect the distribution of a small, lipid soluble weak organic acidic drug Except?
a) tissue protein binding b) plasma protein binding c) pH of body compartments d) obesity e) capillary permeability |
Obesity
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The general mode of inhibition of the metabolism of other drugs by isoniazid and cimetidine is?
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Non-competitive with respect to molecular O2
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The induction of the metabolism of a drug may?
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Be caused by acute administration of another drug
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Administration of sodium bicarbonate enhances the renal clearance of salicylate but not penicillin. Both drugs are weak organic acids. You suspect this difference is primarily due to their different?
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PKa
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Drug A is a Weak organic acid with a narrow therapeutic window. The drug is given by mouth once a day and excreted unchanged in the urine. Its systemic clearance from the plasma of a 70 year old, 70 kg patient is 1.5 ml per min. which of the following is least likely?
a) Drug A has an F oral of 0.9 b) Drug A is 90% bound to plasma albumin c) Drug has a volume of distribution of 10 Liters d) Drug A is secreted by the proximal renal tubules and partially reabsorbed e) Onset of cardiac failure could result in long-lasting toxicity from Drug A |
Drug C is a highly lipophilic weak organic base that takes 4 hours to reach its peak plasma level when taken by the oral route. Drug C is least likely to?
a) be poorly absorbed from the GI tract b) concentrate in gastric contents c) undergo enterohepatic circulation d) be secreted by proximal renal tubules as acidic metabolites e) be secreted into the bile in the form of metabolites |
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The effect of an agonist can NOT be prevented by addition of a sufficient concentration of a
a) noncompetitive antagonist b) competitive antagonist c) partial agonist d) inverse agonist |
partial agonist
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What can be concluded if one knows a drug has a large volume of distribution?
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At steady state a small percentage of the total drug in the body will be in the plasma
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Drug A is a weak organic acid with a pKa of 4.0 . At duodenal pH of 6.0, Drug A is?
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99% ionized
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All of the following properties of tissues (organs) determine the rate and extent of drug distribution to the Except.
a) pH of the tissue environment b) percent cardiac output to a tissue c) membrane potential d) mass of the tissue e) nature/composition of the cell membranes |
Membrane potential
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T/F
An antagonist can block the action of both a partial agonist and a full agonist |
True
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Regarding intramuscular administration of drug...
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The speed with which drug is absorbed can be erratic
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The effect of an agonist can NOT be prevented by addition of a sufficient concentration of a?
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inverse agonist
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Following withdrawal of a beta adrenergic antagonist, an enhanced or supersensitive response to endogenous circulating catecholamines may occur. Which of the following is a correct statement about this process?
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The enhanced physiological responses result in part from an increase in beta receptor density
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Development of resistance to drugs may result from any of the following mechanisms Except?
a) increased metabolism b) altered receptor coupling to its intracellular signaling system c) decreased receptor affinity for agonist d) increased receptor density e) increased endosomal cycling of a receptor |
Increased receptor density
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