Unit 1
A new drug called "Bahia" has been discovered! The Bahia drug binds to hepatocyte receptors irreversibly and covalently. Bahia's activity is limited to one receptor molecule. When another drug, "Olivihaar" is added, new receptors may be synthesized to compensate for those lost to Bahia. Which of the following defines the Bahia drug? A. Statin B. Suicide substrate C. Agonist D. Both A and B
Answer: B
Drug reactions that occur rarely and unpredictably amongst the population called: A. Adverse drug reaction B. Drug allergies C. Idiosyncratic drug reaction D. All of them
Answer: C
GLUT2 Transporters are A. Uptake B. Efflux C. Bidirectional D. None of the above
Answer: C
Disulfide bonds are part of __________ structure of a protein, and the kind of intermolecular interaction between the two sulfur atoms is called _________. A. Secondary, hydrogen bond B. Secondary, covalent bond C. Tertiary, hydrogen bond D. Tertiary, covalent bond E. None of the above
Answer: D
Drug A has a clearance of 4 L/h and a half life of 10 hours. Which of the following is the Vd of Drug A? A. 0.6 L B. 17L C. 46 L D. 58 L E. 150 L
Answer: D
Drug W has a half life of 8 hours. A patient receiving Drug W begins to seize when the drug W reaches steady state levels. The drug is immediately discontinued. How long will it take until his plasma levels of Drug W are approximately 6% of the steady state levels? A. 8 hours B. 16 hours C. 24 hours D. 32 hours E. 48 hours
Answer: D
Group 2 was articulating questions for their midterm. Student B said that competitive antagonists and non-competitive antagonists are different while Student C argued that they are the same thing. Student A said that competitive antagonists affect potency and efficacy while Student H said that competitive antagonists only affect potency whereas noncompetitive antagonists effect efficacy. Student Z said that non-competitive active site antagonists bind only irreversibly. Which student is correct? A. Student A and Z B. Student C and H C. Student A, B and Z D. Student B, H, and Z
Answer: D
In terms of hepatic physiology, where might you locate the BSEP (Bile Salt Export Pump) transporter (ABCB11)? A. Apical membrane of enterocytes B. Basolateral membrane of endothelial cells C. Sinusoidal membrane of hepatocytes D. Canalicular membrane of hepatocytes
Answer: D
Inhibition of drug uptake into the liver and kidney can result in what? A. Decreased plasma levels and decreased efficacy of the drug B. Limitations in transport and clearance via the kidney proximal tube C. An increase in the bioavailability of OAT substrates D. Increased plasma levels and improved efficacy of the drug
Answer: D
Organic Anion-Transporting Polypeptide (OATP) family transporters move ____ substrates ____ of a cell via ____ A. Small, Out, Tertiary Active Transport B. Large, In, Secondary Active Transport C. Small, In, Tertiary Active Transport D. Large, In, Tertiary Active Transport
Answer: D
Which compartment model takes the longest time for drugs to reach the highest fraction of dose distribution? A. Blood B. Vessel-rich group C. Muscle-rich tissues D. Adipose-rich tissues
Answer: D
Which diseases will affect drug metabolism? A. Hypotension B. Hyperthyroidism C. Diabetes D. All of the above E. None of the above
Answer: D
Which form of metabolism utilizes Cytochrome P450 to activate prodrugs with polar molecules? A. Conjugation B. Oxidation C. Reduction D. B & C
Answer: D
Which of the following does not describe a difference between chemical and physiological non-receptor antagonists? A. A chemical antagonist inactivates the agonist of interest by modifying or sequestering it. B. A physiological antagonist blocks a receptor that mediates the physiological response of the receptor for an agonist. C. A physiological antagonist activates a receptor that mediates a response physiologically opposite to that of the receptor for an agonist. D. A chemical antagonist inactivates the agonist of interest by modifying the receptor to no longer be compatible with the agonist.
Answer: D
Which of the following is most correct for treatment of drug-induced toxicity? A. dosing patients with drugs that strengthen the target organ B. discontinuing the medication C. reduction of exposure D. Administration of intravenous fluids E. B and C
Answer: D
Which of the following is not true regarding therapeutic index? A. It varies from 1.0 to more than 1000 B. It is found by dividing the toxic dose by the effective dose C. A low therapeutic index requires close monitoring D. Cancer drugs have a very high therapeutic index
Answer: D
Which of the following statements regarding the cellular mechanisms of toxicity is correct: A. Apoptosis is characterized by enzymatic digestion of cellular contents, denaturation of cellular proteins, and disruption of cellular membranes. B.Necrotic cells undergo cell death with minimal inflammation and disruption of adjacent tissue. C. Necrosis is defined as programmed cell death. D. Apoptosis allows the cell to undergo ordered self-destruction by the coordinated activation of a number of dedicated proteins.
Answer: D
Which one of the following drugs is highly selective to BCR-Abl tyrosine kinase fusion protein, making it a good therapy drug for patients with chronic myeloid leukemia? A. Everolimus B. Warfarin C. Interferon alpha D. Imatinib E. Atorvastatin
Answer: D
Which route of drug administration can bypass the Blood-brain Barrier? A. Subcutaneous B. Intramuscular C. Intravenous D. Intrathecal
Answer: D
Cholestasis, or the reduction or blockage of bile flow, may be induced by the drug, Bosentan (endothelin receptor antagonist) by: A. Inhibition of BSEP (ABCB11) B. Activation of BSEP (ABCB11) C. Inhibition of ABCE D. Activation of ABCE
Answer: A
Dapagliflozin's therapeutic benefit in treating diabetes stems from its selective inhibition of which transporter? A. SGLT2 B. SGLT1 C. SLC5 D. SGLT3
Answer: A
If NADPH Oxidase is inhibited, what will happen to digitoxin (which undergoes P450 dependent oxidation)? Drug + O 2 + NADPH + H + → Drug-OH + H 2 O + NADP + A. Digitoxin excretion levels will be lowered B. Digitoxin excretion levels will be increased C. Digitoxin excretion levels will be the same D. Digitoxin excretion levels will be doubled E. None of the above
Answer: A
OAT1 and OAT3 are implicated in the transport and clearance of a broad range of drugs such as antivirals via what? A. Kidney proximal B. Secondary messengers C. Signaling pathways D. Ion channels
Answer: A
OAT4 and URAT1 inhibition can be used to treat what disease? A. Gout B. Cirrhosis C. Cancer D. Melatonin
Answer: A
The Sodium-Potassium Pump creates a concentration gradient by using ATP to transport Na+ outside of the cell and transport K+ inside of the cell? A. Primary Active Transport B. Secondary Active Transport C. Tertiary Active Transport D. Osmosis
Answer: A
The dose at which 50% of subjects experience a therapeutic response is: A. ED50 B. TD50 C, LD50 D. None of the above
Answer: A
The majority of efflux pumps belong to _________ family of transporters: A. ATP-Binding Cassette (ABC) B. Solute Carrier (SLC) C. Peptide Transporter (PEPT) D. Sodium Glucose Transport Protein (SGLT)
Answer: A
What are drugs also capable of inducing? A. The expression of transporters B. Hyperglycemia C. Levels in the therapeutic index of a drug D. Renal uptake
Answer: A
When the drug binds to the receptor which of the following causes DR inactive form A. Inverse agonist B. Competitive antagonist C. Full agonist D. None of the above
Answer: A
Which form of drug transportation does not require energy to occur and is unable to transport large molecules across the cell membrane? A. Simple diffusion B. Passive transport C. Active transport D. 2 of the above
Answer: A
Why is it extremely important to carefully prescribe medications to patients taking multiple medications such as seen with older patients? Taking multiple drugs without careful consideration may result in A. Adverse effects due to drug-drug interactions B. One drug changes the absorption, distribution, metabolism, or excretion of another drug C. One drug changes the response of target tissues to another drug D. All of the above
Answer: D
What are important molecules that actively transports drugs and compounds back out of the cells and into the intestinal lumen? A. Organic anion transporting polypeptide (OATP) B. P-glycoprotein C. HMG-CoA D. Multidrug resistance protein 1 (MDR1) E. More than one of the above
Answer: E
What are the factors that can affect drug metabolism? A. Race and ethnicity B. Diet and environment C. Age and gender D. Medical backgrounds and family history E. All the above
Answer: E
What does an Adverse effect include? A. Side effects B. Allergic effects C. Idiosyncratic effect D. Toxic effects E. All of them
Answer: E
What is the general method(s) for entry of drugs? A. Endocytosis B. Facilitated diffusion C. Active diffusion D. Human Solute Carriers E. All-of-the above
Answer: E
T/F When potency increases, efficacy will always also increase.
Answer: F
T/F. ABCA & ABCD transporters transport more than just endogenous substrate
Answer: F
T/F. All receptors have to be bound to give maximal effect.
Answer: F
T/F. Competitive antagonist stabilizes the conformation required for receptor activation.
Answer: F
T/F. In the presence of spare receptors, potency (EC50) is greater than Kd because not all receptors are needed for maximal effect.
Answer: F
T/F. In the presence of spare receptors, the agonist response curve will always experience a decrease in efficacy when a noncompetitive antagonist is introduced.
Answer: F
T/F. TD50 is the dose at which 50 percent of the population manifests a given therapeutic effect
Answer: F
T/F. Transport via Organic Cation Transporter (OCT) travels against the electrochemical gradient?
Answer: F
True/False 1.) The higher the Kd, the more potent the drug. 2.) 1/Kd is potency and Kd is affinity. 3.) Some drugs have affinity but no efficacy. 4.) In the following figure, M has the lowest Emax.
Answer: F, F, T, T
T/F Receptors for drugs exist in a reversible equilibrium.
Answer: T
T/F. Grapefruit juice was initially identified as an inhibitor of the drug metabolizing enzyme CYP34A?
Answer: T
T/F. In the presence of spare receptors, if a low concentration of noncompetitive antagonist is present, the efficacy of the agonist would most likely not be decreased.
Answer: T
T/F. P-glycoproteins (P-gp) are typically expressed on the apical membrane of small intestine, in addition to liver, kidney, endothelial cells of the blood brain barrier, and placenta
Answer: T
Antisense therapeutics, such as mipomersen, are responsible for binding mRNAs in order to block ______________ of specific proteins.
Answer: Translation
Which systems does the body primarily use to achieve volume distribution? A. Lymphatic System B. Renal System C. Circulatory System D. Two of the above
Answer:D
A new drug, "Spiderman" is under trial. Although the drug may have therapeutic effects for diabetes, Spiderman is a 30 dB macromolecule that inhibits OATPs and effectively leads to muscle pain. Spiderman inhibits OATPs by binding at the active site of a receptor on hepatocytes. The addition of Spiderman leads to some activated drug-receptor and some inactive drug receptor forms. Spiderman most likely acts as what type of molecule? A. Partial Agonist B. Inverse Agonist C. Receptor Antagonist D. Non-competitive Antagonist
Answer: A
A patient is prescribed the antiviral drug, Cidovir, which is transported by the OAT transporters and demonstrates nephrotoxicity. Why would this patient's physician also prescribe Probenecid? A. Probenecid chemically neutralizes Cidovir's activity B. Probenecid inhibits OAT1 & OAT3, preventing renal uptake thereby protecting the patient's kidneys C. Probenecid's molecular properties make Cidovir a more active antiviral medication D. Probenecid is a blood-thinner and makes it easier for nephrons to filter the patient's blood
Answer: B
All of the following statements are true about spare receptors, EXCEPT: A. There is a discrepancy in Kd-values when comparing the binding curve and dose-response curve. B. The potency (EC50) value is equivalent to Kd. C. Cell-signaling amplification may produce maximal response when only few receptors are bound. D. Spare receptors may alter the effect of a noncompetitive antagonist.
Answer: B
Membrane transporters which allows substrates to pass through the phospholipid bilayer without spending energy are an important part of which form of drug transportation? A. Simple diffusion B. Passive transport C. Active transport
Answer: B
Of the following, which administration technique immediately overcomes barriers? A. Enteral B. Parenteral C. Mucous D. Transdermal
Answer: B
SGLT2 is responsible for more than 90% of glucose reuptake from what organs filtrate? A. Liver B. Kidney C. Pancreas D. Testicles
Answer: B
The OAT4 protein is designed to mediate reabsorption of uric acid from urine. What type of protein is OAT4? A. Storage Protein B. Uptake Transporter C. Efflux Transporter D. Contractile Protein
Answer: B
The combination of St. John's Wort and selective serotonin reuptake inhibitors may result in: A. Dubin-Johnson Syndrome B. Serotonin Syndrome C. Gray Baby Syndrome D. Down Syndrome
Answer: B
The term used to describe the effects of a drug on the body is: A. Toxicity B. Pharmacodynamics C. Physical response D. Potency
Answer: B
Type I hypersensitivity responses may include the following: A.Tachyphylaxis and Immediate Hypersensitivity B. Anaphylaxis and Immediate Hypersensitivity C. Tachyphylaxis and Antibody-Dependent Cytotoxic Hypersensitivity D. Anaphylaxis and Antibody-Dependent Cytotoxic Hypersensitivity
Answer: B
What do co-administered drugs impair and increase within uptake transporters? A. Impair drug clearance and increase efficacy B. Impair statin uptake by the liver and increase statin plasma concentration C. Impair drug disposition and increase bioavailability D. Impair renal uptake and increase statin uptake
Answer: B
What is Idiosyncratic toxicity? A. Adverse effects due to drug-herb interactions B. Rare adverse effects of drugs that appear unpredictably with no apparent mechanism C. Adverse effects resulting from immune hypersensitization to drugs D. Hepatotoxicity due to drugs metabolism
Answer: B
What will inhibit P450 3A4? A. Carbamazepine B. Grapefruit Juice C. Guava Juice D. Saquinavir E. More than one of the above
Answer: B
Which is a way that efflux transporters affect oral bioavailability? A. By sorting drugs into their respective targets B. By limiting the amount of drug that is absorbed across enterocytes C. By metabolizing drugs and thereby inactivating them D. They don't-only uptake transporters affect bioavailability
Answer: B
Which method of administration does First pass metabolism happen? A. Intravenous B. Oral C. Subcutaneous D. Intrathecal
Answer: B
Which of the following does not describe a difference between inverse agonists and competitive antagonists? A. They both reduce receptor activity. B. Inverse agonists do not inhibit full agonist activity. C. Competitive antagonist has no effect in the absence of an agonist. D. An inverse agonist deactivates receptors that are constitutively active in the absence of an agonist.
Answer: B
Which one of these receptor types' function results in extracellular activity (as opposed to that in the cytoplasm or nucleus)? A. Transmembrane ion channel B. Adhesion C. Transmembrane linked to intracellular G protein D. Intracellular E. Transmembrane linked with enzymatic domain
Answer: B
__________ reduces the transport of drugs into nonvascular compartments? A. Increased filtration rate B. Plasma protein binding C. Hydrophilicity D. Enzyme inhibition
Answer: B
All of the following are true regarding competitive antagonist except: A. Acts to reduce the activity of the receptor. B. Competitive antagonist stabilizes R form. C. Competitive antagonist decreases agonist down. D. Competitive antagonist has no effect in the absence of an agonist.
Answer: C
Approximately, how many elimination half-lives are required for the tissue distribution and plasma concentration of a drug to reach steady state in the absence of a loading dose? A. 2 half-lives B. 3 half-lives C. 4 half-lives D. 5 half-lives
Answer: C
Co-transport is a form of which kind of drug transportation A. Simple diffusion B. Passive transport C. Active transport D. None of the Above
Answer: C
Competitive antagonists will ____ agonist activity, while inverse agonist will _____ it. A. Inhibit, increase B. Promote, decrease C. inhibit, decrease D. Decrease, promote
Answer: C
Concomitant use of ginkgo and nonsteroidal anti-inflammatory drugs (NSAIDs) may increase the risk of: A. Heart attack B. Renal Failure C. Bleeding D. Hypertension
Answer: C
Considering the agonist dose-response curve in the presence of spare receptors. At high concentrations, which of the following values decrease? A. Efficacy only B. Potency only C. Efficacy and potency D. None of the above.
Answer: C
Drug B has a Vd of 40L and a clearance of 2 L/hour. Which of the following is the half life of Drug B? A. 2 hours B. 6 hours C. 14 hours D. 21 hours E. 40 hours
Answer: C
Drug Y has a half life of 4 hours. A continuous IV fusion of Drug Y is started on the patient. How long will it take for the plasma levels of Drug Y to reach 75% of steady state? A. 2 hours B. 4 hours C. 8 hours D. 12 hours E. 16 hours
Answer: C
Jacob is suffering from pulmonary arterial hypertension and has been prescribed bosentan, a dual endothelin receptor antagonist. After four weeks, he visits his doctor complaining about a pain in his abdomen. The doctor recognizes the ailment as cholestasis, which had been caused due to the bosentan's inhibition of a protein which leads to intracellular accumulation of cytotoxic bile salts. The protein that had been inhibited was which type of protein? A. Hormone B. Uptake Transporter C. Efflux Transporter D. Structural
Answer: C
Ketoconazole, antifungal drug, is a competitive molecule that binds to P450 enzymes. What happens to the co-administered prodrug? A. Concentration of prodrug in plasma will decrease B. More prodrug is needed to reach therapeutic index C. Concentration of drug in plasma will decreases D. Concentration of drug in plasma remains unaffected E. None of the above
Answer: C
Match the appropriate term with the appropriate description/definition. A. Potency is the maximal response produced by a drug; Efficacy is the concentration at which the drug elicits 50% of its maximal response B. Potency is Emax; Efficacy is Kd C. Potency is related to drug binding and affinity and Efficacy is drug impact on receptor to cause an effect. D. Potency and Efficacy change with increasing drug concentration
Answer: C
Patient A was diagnosed with HIV and, as a result, was prescribed Ritonavir, an HIV protease inhibitor. Patient A is otherwise moderately healthy but mentioned that they cannot resist excessive sugary meals. Why might Patient A's physician be concerned about Patient A's glucose levels? A. Excessive sugar intake disables Ritonavir's functionality B. HIV infection is exacerbated by unabsorbed plasma glucose C. Ritonavir blocks GLUT4, leading to hyperglycemia in prediabetic patients D. Ritonavir disables pancreatic beta cell secretion of insulin, ultimately leading to type I diabetes.
Answer: C
Receptors for drugs can be modeled as having _____ conformational states, in reverse equilibrium. A. 4 B. 6 C. 2 D. 3
Answer: C
Teratogenesis is not induced by: A. Drugs that have few adverse effects on the mother B. Developmental stage C. Anuria D. ACE inhibitors E. All of the above are correct
Answer: C
The presence of ATP and a NA+/K+ pump causes a higher concentration of NA+, which SGLT proteins are able to utilize to transport glucose into the cell following its gradient. What form of transport is this? A. Passive Transport B. Primary Active Transport C. Secondary Active Transport D. Tertiary Active Transport
Answer: C
This type of hypersensitivity most commonly presents as contact dermatitis when a substance acts as a hapten and binds to host protein: A. Type II hypersensitivity B. Type I hypersensitivity C. Type IV hypersensitivity D. Type III hypersensitivity
Answer: C
Use the image/equation to answer the question. A student is working in the lab to determine drug-receptor interactions. Student X finds that molecule binding results in increased DR state. Which of the following is a correct statement about the molecule? A. The molecule has maximal efficacy B. The molecule possesses both affinity and efficacy C. The molecule only has an effect in the presence of an agonist D. The molecule can only bind to the active site
Answer: C
What are the two principal immune mechanisms by which drugs can produce damage? A. Hypersensitivity and antibody-dependent cytotoxic response B. Inflammation and Mast Cell activation C. Hypersensitivity responses and autoimmune reactions D. Cell-mediated response and humoral immunity
Answer: C
What endogenous compound causes GLUT4 translocation? A. Glucagon B. Glutathione C. Insulin D. Lipids
Answer: C
What is the only uptake transporter that is not a member of the SLC family? A. CNT B. OAT C. OST D. PEPT
Answer: C
What is true of the two following figures? A. Drug B is safer than Drug A; Drug B has a lower therapeutic index B. Drug A is safer than Drug B; Drug A has a lower therapeutic index C. Drug B is safer than Drug A; Drug B has a higher therapeutic index D. Drug A is safer than Drug B; Drug A has a higher therapeutic index
Answer: C
What types of transporters have been cloned and expressed in cell lines? A. ABC transporters B. Lipid soluble molecules C. Human D. Secondary messengers
Answer: C
When the drug binds to the receptor which of the following state is caused by inverse agonist : A. DR* B. R C. DR D. DR*+R
Answer: C
Which of the following denotes an active ligand-receptor complex? A. L + R B. LR C. LR* D. L + R*
Answer: C
Which of the following is true regarding acetaminophen overdose? A. It is responsible for some 40% of the cases of acute liver failure in the United States B. excess acetaminophen can be broken down by NAPQI C. Overdosing with acetaminophen depletes glutathione reserves D. acetaminophen is predominantly metabolized by the N-acetylcysteine E. A and C
Answer: C
Which of the following receptors has a linked enzymatic domain? A. Voltage-gated channels. B. G-protein coupled receptors (GPCRs). C. Receptor tyrosine kinases. D. Ca2+ channels.
Answer: C
Which of the following statements are false? A. Potency and efficacy are parameters that can be deduced from a graded dose-response curve B. Efficacy is the maximal response produced by a drug C. Quantal dose-response relationships describe the effect of various doses of a drug on an individual D. ED50 is a parameter found on a quantal dose-response curve
Answer: C
Which true about the Free or unbound form of a drug? A. High level of binding to plasma protein B. Low level of pharmacological action C. Low level of binding to plasma protein D. Low rate or elimination
Answer: C
A patient is prescribed amikacin. The parameters for amikacin are: CL = 5.5 L/h; Vd = 19 L What maintenance dose should be given IV every 8 hours to obtain an average steady state plasma concentration of 15 mg/L of amikacin? A. 18 mg B. 33 mg C. 82.5 mg D. 660 mg E. 1300 mg
Answer: D
All of the following are true regarding inverse agonist except: A. Acts to reduce the activity of the receptor . B. Inverse agonist stabilizes DR . C. Inverse agonist deactivates receptors that are constitutively active . D. Inverse agonist has no effect in the absence of an agonist
Answer: D