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First Aid for the USMLE Step 1 2011 EXPRESS workbook

page 77

Pharmacology
Questions
PHARMACODYNAMICS
1.

Competitive inhibitors ________ (do/do not) resemble the substrate, while noncompetitive
inhibitors ________ (do/do not) resemble the substrate. (p. 232)

2.

The value of Km reflects the _______________ of the enzyme for its substrate. (p. 232)

3.

True or False: In enzyme kinetics, the lower the Km, the higher the affinity. (p. 232) _____________

4.

Vmax is directly proportional to the _______________ _______________. (p. 232)

5.

A graph of substrate concentration on the x-axis and velocity of the reaction on the y-axis has
_______________ (increasing/decreasing) velocity as substrate is increased, although it will
plateau when the enzyme is saturated. (p. 232)

6.

When velocity is equal to one half of its maximum (V max), the corresponding concentration of
substrate is equal to what value? (p. 232) _____________________________________________

7.

Use the graph below to answer the following questions. (p. 232)

8.

A.

What pharmacodynamic term describes the x-intercept of the line? _____________________

B.

What pharmacodynamic term describes the y-intercept? ____________________________

C.

If the y-intercept increases, how is the maximum reaction rate affected? _________________

D.

If the x-intercept moves to the right (increases), how is the Km affected? _________________

In enzyme kinetics, a competitive inhibitor ________ (can/cannot) be overcome by increasing the


concentration of substrate; a noncompetitive inhibitor ________ (can/cannot) be overcome by
increasing the concentration of substrate. (p. 232)

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First Aid for the USMLE Step 1 2011 EXPRESS workbook

9.

Competitive inhibitors _______________ (increase/decrease/do not change) the Vmax of the


reaction, whereas noncompetitive inhibitors _______________ (increase/decrease/do not change)
the Vmax of the reaction. (p. 232)

10.

Competitive inhibitors _______________ (increase/decrease/do not change) the Km of the


reaction, whereas noncompetitive inhibitors _______________ (increase/decrease/do not change)
the Km of the reaction. (p. 232)

11.

What is the formula for calculating a drugs volume of distribution? (p. 232) ___________________

12.

Drugs with a low volume of distribution are found in the _______________


(blood/tissue/extracellular space). Drugs with a high volume of distribution are most likely found in
the _______________ (blood/tissue/extracellular space). (p. 232)

13.

What is the formula for calculating a drugs clearance? (p. 232) ____________________________

14.

What is the definition of the half-life of a drug? (p. 232) ___________________________________

15.

For a drug that is infused at a constant rate, how many half-lives must pass before the drug
reaches approximately 94% of steady-state concentration? (p. 232) ________________________

16.

Given the volume of distribution and clearance of a drug, how is the drugs half-life calculated? (p.
232) __________________________________________________________________________

17.

After one half-life, given constant intravenous infusion of a drug, how close to steady state is the
drugs concentration? How close is it after three half-lives? (p. 232) _________________________

18.

What is the formula for calculating a drugs loading dose? (p. 233) __________________________

19.

What is the formula for calculating the maintenance dose of a drug administered intravenously? (p.
233) __________________________________________________________________________

20.

How do the loading and maintenance doses of drugs differ for patients with renal or liver disease?
(p. 233) ________________________________________________________________________

21.

What is the bioavailability (%) of a drug if it is administered intravenously? (p. 233) _____________

22.

In zero-order elimination of drugs from the body, what is the relationship between the rate of
elimination and the drug concentration? (p. 233) ________________________________________

23.

Name three drugs that exhibit zero-order elimination. (p. 233) _____________________________

24.

In first-order drug elimination, what is the relationship between the rate of elimination and the drug
concentration? (p. 233) ___________________________________________________________

25.

A 24-year-old man attempts suicide by consuming the contents of a small bottle of aspirin. Three
hours later he is brought to the emergency room, where he is administered intravenous saline with
bicarbonate. By what mechanism does this help him? (p. 233) _____________________________
______________________________________________________________________________

26.

A drug that requires a very low dose to achieve its desired effect is _______________
(effective/potent). (p. 233)

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First Aid for the USMLE Step 1 2011 EXPRESS workbook

page 79

27.

The graph below shows the effects of two types of antagonists on an agonist. What type of
antagonist is represented by curve A? By curve B? (p. 234) _______________________________

28.

The addition of a noncompetitive agonist _______________ (increases/decreases/does not


change) the efficacy of the agonist. (p. 234)

29.

How does the efficacy of a partial agonist relate to the efficacy of a full agonist of the same
receptor? (p. 234) ________________________________________________________________

30.

How does the potency of a partial agonist relate to the potency of a full agonist of the same
receptor? (p. 234) ________________________________________________________________

AUTONOMIC DRUGS
31.

How does botulinum toxin work? (p. 235) _____________________________________________

32.

Identify the G-protein class for each receptor. (Numbers may be used more than once.) (p. 236)
_____ A. 1
_____ B. 2
_____ C. 1
_____ D. 2
_____ E. D1
_____ F. D2
_____ G. H1
_____ H. H2
_____ I. M1
_____ J. M2
_____ K. M3
_____ L. V1
_____ M. V2

33.

1. Gi
2. Gq
3. Gs

What are the major effects of 1-receptor activation? (p. 236) ______________________________
______________________________________________________________________________

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34.

First Aid for the USMLE Step 1 2011 EXPRESS workbook

What are the major functions of 2-receptor activation? (p. 236) ___________________________
______________________________________________________________________________

35.

What are the major functions of 1-receptor activation? (p. 236) ____________________________
______________________________________________________________________________

36.

What is the major effect of 2-receptor activation on the body's vasculature? What is the effect on
the respiratory system? (p. 236) _____________________________________________________

37.

How does 2-receptor activation affect glucagon release? (p. 236) __________________________

38.

In the images below, identify which autonomic drugs work at which site of action. (p. 237)

(Adapted, with permission, from Katzung BG, Trevor AJ. Pharmacology: Examination &
Board Review, 5th ed. Stamford, CT: Appleton & Lange, 1998: 42.)

39.

Name five indirect cholinergic agonists. (p. 238) ________________________________________


______________________________________________________________________________

40.

What symptoms are likely in patients taking cholinomimetic agents? (p. 238) __________________
______________________________________________________________________________

41.

Which pharmacologic agent is used to treat atropine overdose? (p. 238) _____________________

42.

What is a methacholine challenge test? (p. 238) ________________________________________


______________________________________________________________________________

43.

A farmer presents with diarrhea, abdominal pain, wheezing, pinpoint pupils, copious tears, and
salivation. What medications should be prescribed? (p. 238) ______________________________

44.

Why is pyridostigmine used to treat myasthenia gravis? (p. 238) ___________________________


______________________________________________________________________________

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45.

A patient recently began taking haloperidol to treat schizophrenia, but visits his physician because
of new-onset Parkinson's-like motor symptoms. What drug could be used to treat these symptoms?
(p. 239) ________________________________________________________________________

46.

What are the two effects of atropine on the eye? (p. 239) _________________________________

47.

True or False: Diarrhea is a sign of atropine toxicity. (p. 239) ______________________________

48.

Low doses of epinephrine are selective for _______ (1, 2, 1, 2) adrenergic receptors. (p. 240)

49.

Isoproterenol is an agonist for which receptors? (p. 240) _________________________________

50.

Dopamine __________ (is/is not) ionotropic and __________ (is/is not) chronotropic, whereas
dobutamine __________ (is/is not) ionotropic and __________ (is/is not) chronotropic. (p. 240)

51.

What are the clinical applications of epinephrine? (p. 240) ________________________________


______________________________________________________________________________

52.

What role does dopamine have in treating shock? (p. 240) ________________________________
______________________________________________________________________________

53.

What are the clinical applications of phenylephrine? (p. 240) ______________________________


______________________________________________________________________________

54.

What is the clinical application for albuterol? (p. 240) ____________________________________


______________________________________________________________________________

55.

Which sympathomimetics can reduce premature uterine contractions? (p. 240) _______________

56.

What effect does isoproterenol have on pulse pressure and heart rate? (p. 240) _______________
______________________________________________________________________________

57.

What is the effect of clonidine on central adrenergic outflow? On which receptor does it act? (p.
241) __________________________________________________________________________

58.

What is the clinical application and mechanism of action of phentolamine? (p. 241) _____________
______________________________________________________________________________

59.

What is the net effect of epinephrine on blood pressure before and after nonselective -blockade?
Why? (p. 241) ___________________________________________________________________
______________________________________________________________________________

60.

A 63-year-old man is referred long-term care after his first myocardial infarction. Is a -blocker
suggested or contraindicated for this patient? Why? (p. 242) ______________________________
______________________________________________________________________________

61.

How do -blockers work in the setting of angina pectoris? (p. 242) __________________________
______________________________________________________________________________

62.

Which -blockers have partial agonist activity? (p. 242) __________________________________

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63.

First Aid for the USMLE Step 1 2011 EXPRESS workbook

Name two nonselective - and -antagonists. (p. 242) ___________________________________

TOXICITIES AND SIDE EFFECTS


64.

Match the specific antidote(s) with each of the toxicities. (p. 243)
_____ A. Acetaminophen
_____ B. Amphetamines
_____ C. Antimuscarinics and
anticholinergics
_____ D. Benzodiazepines
_____ E. -Blockers
_____ F. Carbon monoxide
_____ G. Copper, arsenic, gold
_____ H. Cyanide
_____ I. Digitalis
_____ J. Heparin
_____ K. Iron
_____ L. Lead
_____ M. Mercury, arsenic, gold
_____ N. Methanol, antifreeze
_____ O. Methemoglobin
_____ P. Opioids
_____ Q. Organophosphates, anticholinesterase inhibitors
_____ R. Salicylates
_____ S. TCAs
_____ T. Theophylline
_____ U. tPA, streptokinase
_____ V. Warfarin

65.

1.
2.
3.
4.
5.
6.
7.
8.
9.
10.
11.
12.
13.
14.
15.
16.
17.
18.
19.
20.
21.

100% oxygen, hyperbaric oxygen


Aminocaproic acid
Atropine, pralidoxime
-Blocker
CaEDTA, dimercaprol, succimer, penicillamine
Deferoxamine
Dimercaprol, succimer
Ethanol, dialysis, fomepizole
Flumazenil
Glucagon
Methylene blue, vitamin C
N-Acetylcysteine
NaHCO3
NaCHO3, dialysis
NH4Cl
Nalaxone/naltrexone
Nitrite, hydroxocobalamin, thiosulfate
Phosphostigmine salicylate
Penicillamine
Protamine
+
Stop the drug, normalize K , lidocaine, anti-dig
2+
Fab fragments, Mg
22. Vitamin K, fresh frozen plasma

Which medications can cause agranulocytosis? (pp. 244-245) _____________________________


______________________________________________________________________________

66.

OCPs can cause what kind of complications? (pp. 244-245) _______________________________

67.

Which medications can cause hemolysis in patients with G6PD deficiency? (pp. 244-245) _______
______________________________________________________________________________

68.

Which medications can cause gynecomastia? (pp. 244-245) ______________________________


______________________________________________________________________________

60.

Which medications can cause pulmonary fibrosis? (pp. 244-245) ___________________________


______________________________________________________________________________

70.

Which medications can cause photosensitivity? (pp. 244-245) _____________________________


______________________________________________________________________________

71.

Which medications can cause megaloblastic anemia? (pp. 244-245) ________________________


______________________________________________________________________________
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72.

page 83

Which medications can induce seizures? (pp. 244-245) __________________________________


______________________________________________________________________________

73.

Which medications can cause a Parkinson-like syndrome? (pp. 244-245) ____________________


______________________________________________________________________________

74.

Which medications can cause a disulfiram-like reaction? (pp. 244-245) ______________________


______________________________________________________________________________

75.

Which medications can cause nephrotoxicity and ototoxicity? (pp. 244-245) __________________
______________________________________________________________________________

76.

In the chart below, checkmark which of the substances are P-450 inducers vs. inhibitors. (p. 245)
Substance

P-450 inducer

P-450 Inhibitor

Alcohol use, acute


Alcohol use, chronic
Barbiturates
Carbamazepine
Cimetidine
Erythromycin
Grapefruit juice
Griseofulvin
HIV protease inhibitors
Isoniazid
Ketoconazole
Phenytoin
Quinidine
Rifampin
St. Johns wort
Sulfonamides
77.

How does disulfiram work to treat alcoholism? (p. 246) __________________________________


______________________________________________________________________________

78.

Which drugs must be avoided in patients with sulfa allergy? (p. 246) ________________________
______________________________________________________________________________

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First Aid for the USMLE Step 1 2011 EXPRESS workbook

MISCELLANEOUS
79.

Match the drug name suffix with its category or usage. (Numbers may be used more than once) (p.
247)
_____ A.
_____ B.
_____ C.
_____ D.
_____ E.
_____ F.
_____ G.
_____ H.
_____ I.
_____ J.
_____ K.
_____ L.
_____ M.
_____ N.
_____ O.
_____ P.
_____ Q.
_____ R.
_____ S.
_____ T.
_____ U.
_____ V.
_____ W.
_____ X.

-afil
-ane
-azepam
-azine
-azole
-barbital
-caine
-cillin
-cycline
-etine
-ipramine
-navir
-olol
-operidol
-oxin
-phylline
-pril
-terol
-tidine
-triptan
-triptyline
-tropin
-zolam
-zosin

1.
2.
3.
4.
5.
6.
7.
8.
9.
10.
11.
12.
13.
14.
15.
16.
17.
18.
19.
20.
21.
22.

5-HT1B/1D agonist
1 Antagonist
ACE inhibitor
Antibiotic, protein synthesis inhibitor
Antifungal
antagonist
2 agonist
Barbiturate
Benzodiazepine
Butyrophenone (neuroleptic)
Cardiac glycoside (inotropic)
Erectile dysfunction
H2 antagonist
Inhalational general anesthetic
Local anesthetic
Methylxanthine
Penicillin
Phenothiazine
Pituitary hormone
Protease inhibitor
SSRI
TCA

Answers
PHARMACODYNAMICS
1.

Do; do not.

2.

Affinity.

3.

True.

4.

Enzyme concentration.

5.

Increasing.

6.

Km.

7.

A = 1/-Km; B = 1/Vmax; C = it decreases; D = it increases.

8.

Can; cannot. This is because competitive inhibitors bind the active site of the enzyme, competing
with the substrate, whereas noncompetitive inhibitors bind elsewhere on the enzyme and so are
not affected by substrate concentration.
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9.

Do not change; decrease.

10.

Increase; do not change.

11.

Volume of distribution = amount of drug in the body / plasma drug concentration.

12.

Blood alone (these drugs do not distribute outside the plasma); tissue (these drugs distribute
throughout the body).

13.

Clearance (L/min) = rate of elimination of drug (g/min) / plasma drug concentration (g/L).

14.

The time required to reduce the amount of drug in the body by one half.

15.

Four.

16.

Half-life = (0.7 volume of distribution) / clearance.

17.

50% of steady-state concentration; 87.5% of steady-state concentration.

18.

Loading dose = (target plasma concentration volume of distribution) / bioavailability.

19.

Maintenance dose = target plasma concentration (clearance / bioavailability).

20.

For both diseases, the loading dose does not change, but the maintenance dose decreases.

21.

100%.

22.

The rate of elimination is constant, regardless of the drug concentration.

23.

Phenytoin, ethanol, and aspirin (at high or toxic concentrations).

24.

The rate of elimination is directly proportional to the drug concentration. A constant fraction (rather
than a constant amount) is eliminated.

25.

Bicarbonate alkalinizes the lumen of the nephrons, which traps acetylsalicylic acid within the lumen
because it is a weak acid and is ionized in a basic environment.

26.

Potent.

27.

A = noncompetitive antagonist; B = competitive antagonist.

28.

Decreases.

29.

A partial agonist has lower maximal efficacy than a full agonist.

30.

A partial agonist may be more potent than, less potent than, or equally as potent as a full agonist.

AUTONOMIC DRUGS
31.

Botulinum toxin prevents the release of neurotransmitter at all cholinergic terminals.

32.

A-2, B-1, C-3, D-3, E-3, F-1, G-2, H-3, I-2, J-1, K-2, L-2, M-3.

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33.

1-Receptor activation increases vascular smooth muscle contraction, as well as pupillary dilator
muscle contraction (mydriasis).

34.

2-Receptor activation decreases sympathetic outflow and insulin release.

35.

1-Receptor activation increases the following: heart rate and contractility; release from the
kidneys; and lipolysis of adipose tissue.

36.

Vasodilation; bronchodilation.

37.

2-Receptor activation increases glucagon release.

38.

(Adapted, with permission, from Katzung BG, Trevor AJ. Pharmacology: Examination &
Board Review, 5th ed. Stamford, CT: Appleton & Lange, 1998: 42.)

39.

Neostigmine, pyridostigmine, edrophonium, physostigmine, and echothiophate.

40.

Exacerbation of COPD, asthma, and peptic ulcers.

41.

Physostigmine. It crosses the blood-brain barrier and is able to reverse effects on the CNS and the
peripheral nervous system.

42.

A test in which methacholine is inhaled to stimulate muscarinic receptors and induce bronchoconstriction. The test is used to diagnose asthma.

43.

This patient has the classic signs of organophosphate poisoning, which is treated with atropine and
pralidoxime.

44.

Pyridostigmine increases the amount of acetylcholine in the neuromuscular synapse, thereby


increasing muscle strength.

45.

Benztropine.

46.

Pupil dilation and cycloplegia.


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47.

False. (Constipation is a sign of atropine toxicity.)

48.

1.

49.

1 and 2 (equally).

50.

Dopamine is ionotropic and chronotropic; dobutamine is ionotropic but is not chronotropic.

51.

Anaphylaxis, open-angle glaucoma, asthma, and hypotension.

52.

Dopamine increases blood pressure while maintaining renal perfusion.

53.

Phenylephrine treats nasal decongestion, causes vasoconstriction, and dilates pupils.

54.

Acute asthma.

55.

Terbutaline and salmeterol.

56.

Isoproterenol increases pulse pressure and heart rate.

57.

Clonidine is an 2-agonist that decreases central adrenergic outflow. (Remember: the 2-receptor is
responsible for negative feedback).

58.

Phentolamine is a nonselective -blocker used to treat pheochromocytoma.

59.

Before -blockade, epinephrine increases blood pressure. After -blockade, it decreases blood
pressure. This is because epinephrine also activates 2, which lowers blood pressure and is not
blocked.

60.

Suggested. After myocardial infarction, patients should receive -blockers to decrease risk of
mortality.

61.

They decrease heart rate and contractility as well as myocardial oxygen consumption.

62.

Pindolol and acebutolol. (Remember: PA = Partial Agonist)

63.

Carvedilol and labetalol.

TOXICITIES AND SIDE EFFECTS


64.

A-12, B-15, C-18, D-9, E-10, F-1, G-19, H-17, I-21, J-20, K-6, L-5, M-7, N-8, O-11, P-16, Q-3, R-14,
S-13, T-4, U-2, V-22.

65.

Carbamazepine, colchicine, clozapine, dapsone, methimazole, and propylthiouracil.

66.

Thrombotic complications.

67.

Isoniazid, sulfonamides, primaquine, aspirin, ibuprofen, and nitrofurantoin.

68.

Spironolactone, digitalis, cimetidine, chronic alcohol use, estrogens, and ketoconazole.

69.

Bleomycin, amiodarone, and busulfan.

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70.

Sulfonamides, amiodarone, and tetracycline.

71.

Phenytoin, methotrexate, and sulfa drugs.

72.

Bupropion, imipenem/cilastatin, and isoniazid.

73.

Chlorpromazine, haloperidol, metoclopramide, and reserpine.

74.

Certain cephalosporins, first-generation sulfonylureas, metronidazole, and procarbazine.

75.

Aminoglycosides, cisplatin, loop diuretics, and vancomycin.

76.
Substance

P-450 inducer

P-450 Inhibitor

Alcohol use, acute


Alcohol use, chronic

Barbiturates

Carbamazepine

Cimetidine

Erythromycin

Grapefruit juice

Griseofulvin

HIV protease inhibitors

Isoniazid

Ketoconazole

Phenytoin

Quinidine

Rifampin

St. Johns wort

Sulfonamides

77.

Disulfiram inhibits acetylaldehyde dehydrogenase, which breaks down acetaldehyde. Thus alcohol
consumption while taking disulfiram results in nausea, vomiting, headache, and hypotension.

78.

Acetazolamide, celecoxib, furosemide, probenicid, thiazides, TMP-SMX, sulfasalazine, sulfonamide


antibiotics, and sulfonylureas.

MISCELLANEOUS
79.

A-12, B-14, C-9, D-18, E-5, F-8, G-15, H-17, I-4, J-21, K-22, L-20, M-6, N-10, O-11, P-16, Q-3, R-7,
S-13, T-1, U-22, V-19, W-9, X-2.

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