Professional Documents
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Pharma 2
Pharma 2
Pharma 2
When added to an intestinal smooth muscle in a tissue bath, two different drugs both
cause relaxation of the muscle but with different EC50's values. Based on this
information, which of the following statements is true?
b) the two drugs have different potencies in causing relaxation
A
Long or continuous exposure of a receptor to an agent that is an antagonist can:
a) result in a phenomenon called supersensitivity
b) desensitize the receptor
c) produce tachyphylaxis
d) cause down regulation of the receptor
e) b and c are correct
D
The term that describes what a drug does to the body and, particularly its mechanism of action,
is called:
a) efficacy
b) pharmacodynamics
c) pharmacokinetics
d) pharmacogenetics
e) pharmacogenomics
E
Which of the following autonomic receptors results in the activation of adenylate cyclase as the
major component of the signaling transduction process?
a) nicotinic
b) muscarinic
c) α1 adrenoceptor
d) α2 adrenoceptor
e) β1 adrenoceptor
B
Bethanechol is administered subcutaneously (sc) to a patient with postoperative abdominal
distention and gastric atony. The sc route is chosen over the oral route because gastric
retention is complete and there is no passage of gastric contents into the duodenum. Which of
the following effects might be observed after the sc administration of bethanechol:
a) skeletal muscle twitching
b) decrease in heart rate
c) brochodilation of the airway in the lung
d) relaxation of the detrusor muscle in the bladder
e) inhibition of the release of nitric oxide from vascular endothelial cells
B
The most toxic substance known that affects the parasympathetic nervous system is an
exotoxin secreted by the anaerobe Clostridium botulinum. There are several forms of botulinum
toxin, all of which are highly toxic after they are ingested in contaminated food. The toxin
produces respiratory paralysis by:
a) blocking nicotinic acetylcholine receptors
b) blocking the release of acetylcholine from nerve endings
c) blocking peristalsis
d) causing circulatory collapse
e) stimulating the vagal nerve
C
The cardiovascular effects of epinephrine in a person treated with phentolamine will most likely
resemble the response after the administration of:
a) phenylephrine
b) terbutaline
c) isoproterenol
d) norepinephrine
e) dobutamine
A 70-year-old male patient comes into your office complaining of difficulty in urinating. He says
he has a poor urine stream, strains to pass urine, has prolonged micturition and a feeling of
incomplete bladder emptying. You diagnose this patient as having benign prostatic hyperplasia.
Which of the following would be the best choice of treatment.
a) bethanechol
b) phentolamine
c) dopamine
d) tamsulosin
e) phenoxybenzamine
In Professor PharmPhy's demonstration, a drug which would block the fast EPSP would be:
a) atropine
b) trimethaphan
c) prazosin
d) propranolol
e) succinylcholine
B. Trimetaphan is a nicotinic blocker.
Atropine is a M antagonist, Prazosin is a alpha-1 antagonist, Propanolol is a nonselective beta
blocker, Succinylcholine is a nicotinic Ach receptor binder that causes prolonged depolarization.
E. Alpha-1 receptors trigger PLC activation and rises in IP3 and DAG (also, M1,3,5 do the
same). Phentolamine is a nonselective alpha blocker, Carvedilol is a nonselective beta-blocker,
Metoprolol is a somewhat selective beta-1 blocker, and Atropine is a muscarinic blocker.
The above figure depicts a signaling pathway for some type of drugs or hormones. If the drug
activating this receptor was norepinephrine, which of the following would be the most selective
antagonist to block the receptor:
a) phentolamine
b) carvedilol
c) metoprolol
d) atropine
e) prazosin
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E. Phenylephrine is an alpha-1 agonist that would increase SVR and through baroreflex,
decrease HR and thus CO.
NE would increase SVR but also HR and CO through Beta-1, E would also increase HR and
CO, but not change as much SVR and BP as NE. Clonidine (alpha-2 agonist) would decrease
pressure and SVR. Isoproterenol (beta agonist) would increase HR and CO, while decreasing
diastolic and MAP by a little.
A new drug was given i.v. to 25 normal subjects in a Phase I clinical trial. The cardiovascular
effects are summarized in the table above. Which of the following drugs does the new
experimental drug most resemble?
(Hint: Human Simulation Demonstration)
a) norepinephrine
b) epinephrine
c) clonidine
d) isoproterenol
e) phenylephrine
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D. Most insecticides are organophosphate irreversible (suicide) cholinesterase blockers.
A farmer is brought into the Emergency Department after an accident with crop spraying
equipment, during which he was copiously sprayed with insecticide. He is salivating profusely
and has difficulty in breathing; his pulse rate is 40 beats/min. It is likely that the insecticide
bound to which of the following receptors or effectors?
a) anionic site of acetylcholinesterase
b) nicotinic cholinergic receptor
c) muscarinic cholinergic receptor
d) esteratic site of acetylcholinesterase
e) alpha 1 adrenoceptor
Tachycardia would beta agonists, bronchodilation would be beta2, vasodilation would be beta2.
Salivation is stimulated by alpha-1 receptors, but would be profuse only if stimulated by
muscarinic parasympathetic receptors.
A child has swallowed the contents of two bottles of a nasal decongestant whose primary
ingredient is a potent alpha adrenoceptor agonist drug. The signs of alpha activation that may
occur in this patient include:
a) bronchodilation
b) tachycardia
c) pupillary dilation
d) vasodilation
e) profuse salivation
C. At eccrine sweat gland, there are cholinergic muscarinic receptors, although it is controlled
by sympathetic innervation. Scopolamine, a muscarinic antagonist, would block this
transmission.
a) gastric secretion
b) neuromuscular junction (skeletal muscle)
c) salivary glands
d) sweat glands
e) detrusor muscle of the bladder
D.
Atropine and scopolamine are well absorbed from GI tract, but not so much from eye or intact
skin.
Ipratropium (muscarinic antag) has poor systemic absorption, and is usually inhaled for COPD
and asthma.
Physostigmine readily crosses BBB, while neostigmine/pyridostigmine do not cross very well.
Isoproterenol (beta agonist) which is used for heart block and some asthma, is poorly absorbed
after oral administration.
B. Carvedilol is nonselective beta blocker, but it also has alpha-1 adrenoceptor antagonist
activity. This would block the BP rise associated with alpha-1 receptor stimulation by epi.
Propanolol, Pindolol, Timolol are all nonselective beta blockers. Metoprolol is a somewhat
selective blocker for beta-1, but will also have activity against beta-2, and is thus not a good
option.
A new drug was administered to an anesthetized animal with the results shown. A large dose of
epinephrine was administered before and after the new agent for comparison. Which of the
following agents does the new drug most closely resemble?
a) propranolol
b) carvedilol
c) pindolol
d) metoprolol
e) timolol
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E. ???
The following systems are predominantly under symp tone: ventricles, blood vessels, arterioles,
veins.
A 30 year old man has been treated with several autonomic drugs for 4 weeks. He is now
admitted to the Emergency Department showing signs of drug toxicity. Which of the following
signs would distinguish between an overdose of a ganglion blocker and a muscarinic blocker:
a) mydriasis
b) tachycardia
c) postural hypotension
d) blurred vision
e) dry mouth, constipation
D. Isoproterenol is a non-selective beta AGONIST that usually increases HR, contractility, CO,
while also causing vasodilation. Systolic BP usually remains unchanged, but diastolic falls
somewhat.
Which of the following drugs most resembles drug X?
a) acetylcholine
b) atropine
c) epinephrine
d) isoproterenol
e) norepinephrine
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E. Norepinephrine.
Which of the following most resembles drug Y?
a) acetylcholine
b) atropine
c) epinephrine
d) isoproterenol
e) norepinephrine
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B. Neonates have low levels of glucuronyl transferase, leading to inability to do phase II
biotransformation of drugs such as antibacterial chloramphenicol. This leads to Gray Baby
syndrome.
A neonate has been diagnosed with bacterial meningitis and is being treated with drug X.
During the first 24 hrs the patient suffers from vomiting, irregular and rapid respirations. During
the second day he presents with flaccidity, an ashen-green color, a decrease in body
temperature and is very ill. You correctly surmise that drug X was not being adequately
metabolized by:
a) acetylation
b) glucuronidation
c) CYP450 hydroxylation
d) methylation
e) sulfate conjugation
Which of the following combinations of phase 1 and phase 2 biotransformations account for the
majority of drug biotransformations:
This is a type of nonreceptor antagonism, along with chemical antagonism, in which the
antagonist sequesters agonist and prevents its activity.
a) an interaction which results from one drug antagonizing the effect of another by competing for
the same receptor
b) an interaction which results from a drug binding to a receptor and providing a response
c) an interaction which results from one drug antagonizing the response of another drug
following stimulation of a different receptor
d) an interaction which results when one drug changes the absorption, distribution
biotransformation or excretion of another drug
e) a beneficial interaction when two drugs are simultaneously administered
D. Partial agonist.
Timolol (nonselective beta blocker), Labetalol (nonselective beta blocker), and celiprolol (beta-1
blocker) all have partial agonist activity.
In the absence of other drugs or an endogenous agonist, pindolol produces some increase in
heart rate by activating β-adrenoceptors. However, when the heart rate has been increased by
epinephrine, pindolol causes a dose-dependent reversible decrease in heart rate. From this
information you deduce that pindolol is:
a) a non-competitive antagonist
b) a physiological antagonist
c) a chemical antagonist
d) a partial agonist
e) an inverse agonist
Which of the following drugs is correctly matched with a receptor with which it can activate or
bind?
a) physostigmine : nicotinic acetylcholine receptor
b) tolterodine : muscarinic acetylcholine receptor
c) clonidine : α1 adrenoceptor
d) cocaine : monoamine oxidase
e) prazosin : α2 adrenoceptor
E. Pindolol. Beta-blockers and calcium channel blockers act to decrease the heart's workload,
and thus its requirement for oxygen. Only agent that would decrease HR and contractility.
Phentolamine is a alpha blocker that would produce hypotention, but also reflex tachycardia
and arrhythmias that would aggravate angina.
Isoproterenol, a beta agonist, would increase HR and contractility and oxygen demand, and
thus angina.
a) scopolamine: the muscarinic agonistic effects would reduce heart rate and therefore reduce
oxygen demand
b) phentolamine: hypotension associated with phentolamine would reduce myocardial work and
prevent ischemic symptoms
c) isoproterenol: increased β1-receptor stimulation would increase cardiac output and therefore
increase coronary perfusion resulting in decreased angina symptoms
d) phenoxybenzamine: because of its long action, phenoxybenzamine is the preferred treatment
for angina. The decrease in blood pressure from α-receptor blockade is long term and
myocardial work is decreased because of reduced afterload
e) pindolol: reduced effects of adrenergic nerve activity and circulating catecholamines on the
heart result in reduced rate and inotropy. Both factors reduce myocardial oxygen demand and
therefore may increase exercise tolerance and reduce anginal events.
D
Administration of a drug such as phenobarbital, which induces the liver microsomal system may
lead to:
a) an increase in CYP450
b) an increase in glucuronide conjugation
c) an increase in amine oxidase
d) both a and b
e) a, b and c
D. Atropine is well absorbed and crosses the BBB. Physostigmine is one of the few
pharmaceutical AChEIs that cross the BBB. It is the drug of choice for atropine poisoning.
Neostigmine and Edrophonium are AChEIs, but they don't cross the BBB. Tolterodine is a
muscarinic antagonist like atropine. Ipratropium is also an antimuscarinic (but is more poorly
absobred, and is used for COPD and asthma)
During the Iraq crisis several people, believing they had been or were about to be exposed to a
nerve gas, mistakenly injected themselves with syrettes containing a total of 10 mg of atropine.
In the absence of a cholinergic agonist, 10 mg is a toxic dose for adults. The most appropriate
drug for treating atropine toxicity in these people is:
a) neostigmine
b) edrophonium
c) tolterodine
d) physostigmine
e) ipratropium
D
The use of the word "cholinergic" to describe the action of agonists at certain sites is intended to
make it clear that these agonists all:
a) work on nicotinic acetylcholine receptors
b) involve the second messenger cyclicAMP in the production of their effects
c) prevent the action of acetylcholine at the effectors of the parasympathetic nervous system
d) have actions like acetylcholine at those sites
e) are esters, as is acetylcholine
D. Prazosin is an alpha-1 antagonist. Epi's pressor effectors mostly come from stimulation of
alpha-1's in vasculature that lead to contraction of smooth muscle and thus increase in vascular
resistance.
a) essential hypertension
b) angina pectoris
c) congestive heart failure
d) chronic obstructive pulmonary disease
e) idiopathic hypertrophic subaortic stenosis
E. Muscarinic agonist used in the treatment of glaucoma.
A patient comes into your office with pain in the eye. You determine that the patient's
intraoccular pressure is 80-90 mmHg (normal is 10 mmHg). You decide the patient is suffering
from acute, narrow angle glaucoma and immediately treat with pilocarpine. You later tell your
assistant that pilocarpine:
a) is inactivated by cholinesterase
b) is a cholinesterase inhibitor
c) blocks muscarinic receptors
d) is a beta adrenoceptor antagonist
e) is a directly acting parasympathomimetic
C. Methamphetamine enhances release of vesicles containting NE, which is pointless if
reserpine (an irreversible VMAT antagonist) depleted those vesicles.
Phenylephrine is a alpha-1 agonist, isoproterenol is a beta antagonist, and epi and NE can act
directly as well
An elderly patient was treated for a long period of time with reserpine to control high blood
pressure. The subsequent administration of which of the following would be expected to
produce the least change in blood pressure:
a) phenylephrine
b) isoproterenol
c) methamphetamine
d) epinephrine
e) norepinephrine
B. Underlying disease may compromises biotransformation and excretion.
Adverse drug reactions are more frequently reported in the elderly because:
a) they always require a lower does than do younger adults
b) underlying disease may compromise biotransformation and excretion
c) they have more office visits
d) most elderly patients are depressed
e) decreased intestinal transient time increases drug absorption
D. alpha1- adrenoceptor antagonist would block this compound, which is most likely an alpha-1
agonist.
Alpha-1 agonist alone would increase SVR, while decreasing HR through baroreflexive means,
and would also produce mydriasis because alpha-1 receptors on the radial muscle produce this
response. Scopolamine, a muscarinic blocker, would dampen the parasympathetic
baroresponse and tone, producing an INCREASE in HR, while also dampening muscarinic
receptors on the iris sphincter, thus producing a more aggravated mydriasis.
After medical school you decide to take a job in the pharmaceutical industry. You are assigned
to the Pharmacology Department and are quite happy because you remember all those
wonderful times in the Principles of Pharmacology class in medical school. Your lab has been
given a new compound for screening. Following IV administration, it produced an increase in
mean arterial blood pressure, a decrease in heart rate, and mydriasis. In the presence of
scopolamine the unknown drug increased both blood pressure and heart rate and produced
even greater mydriasis you believe you have correctly categorized this compound and tell your
assistant that is could be blocked by:
a) muscarinic cholinergic antagonist
b) β1-adrenoceptor antagonist
c) α2-adrenoceptor antagonist
d) α1-adrenoceptor antagonist
e) cholinesterase inhibitor
46. C
47. B
48. A
Dose response curves are depicted in the above Figure for a number of drugs A through E in
relationship to drug X (--- x ---). All drugs act by the same mechanism. Select the letter of the
curve that best fits the description. C is one from far right, A is first curve from left.
Cl = (0.7/(half-life))*Vd
5.6 = (0.7/halflife)*8L
half life = (0.7*8)/5.6 = 1 hour
A normal volunteer will receive a new drug in a phase I clinical trial. The clearance and volume
of distribution of the drug in this subject are 5.6 L/hr and 8 L, respectively. The half-life of the
drug in this subject will be approximately
a) 8 hours
b) 1 hour
c) 40 hours
d) 2 hours
e) 0.02 hours
D. Verapamil is an example of a drug that undergoes substantial first-pass elimination, and the
fact that its clearance = liver blood flow is testament to that. Verapamil, ASA, glyceryl trinitrate,
isosorbide dinitrate, levodopa, lidocaine, metoprolol, morphine, propranolol, salbutamol are
other drugs that undergo substantial first pass metabolism.
Verapamil and phenytoin are both eliminated from the body by metabolism in the liver.
Verapamil has a clearance of 1.5 L/min, approximately equal to liver blood flow, whereas
phenytoin has a clearance of 0.1 L/min. When these compounds are administered under
conditions that increase liver blood flow, which of the following is most likely?
a) the clearance of both verapamil and phenytoin will be increased
b) the clearance of both verapamil and phenytoin will be decreased
c) the clearance of verapamil will be unchanged, whereas the clearance of phenytoin will be
increased
d) the clearance of phenytoin will be unchanged, whereas the clearance of verapamil will be
increased
e) the clearance of both verapamil and phenytoin will be unchanged
E. The time it takes for a drug to reach 97% of Css is equal to 5 half lives of that drug. 94% = 4
half lives, 90% = 3.3 half lives, 80% = 3 half lives, 75% = 2 half lives, 50% = 1 half life.
A nineteen-year-old woman is brought to the hospital with severe asthmatic wheezing. You
decide to use IV theophylline for treatment. The pharmacokinetics of theophylline include the
following average parameters: Vd is 35 L; cl is 48 mL/min; half-life 8 is hours. If an IV infusion of
theophylline is started at a rate of 0.48 mg/min, how long will it take to reach 97% of the final
steady state?
a) approximately 48 minutes
b) approximately 5.8 hours
c) approximately 6 hours
d) approximately 8 hours
e) approximately 40 hours
C
The figure above depicts the drug concentration curves vs time for three drugs labeled A, B and
C. Drug A and B were given at identical doses while C was given at 1/100 the dose of A and B.
Vd = dose/Cp(0)
39000 mL = (0.3dose) / (0.1ug/100mL)
39 ug /0.3 = dose
Dose = 130 ug
A 70 kg lean male is taking drug A orally. The drug is 30% absorbed within minutes after oral
administration. The drug distributes evenly in all body water compartments without being
sequestered in any compartments and without binding to plasma proteins. The Vd of the drug is
39 liters. What loading dose of the drug should be administered to achieve a plasma
concentration of 0.1 μg/100 ml?
a) 700 μg
b) 390 μg
c) 130 μg
d) 39 μg
e) 13 μg
D. Greater surface area in small intestine than other areas of gut.
Most weak acids as well as weak bases are absorbed primarily from the small intestine after
oral administration because:
a) both types of drug are more ionized in the small intestine
b) both types of drug are less ionized in the small intestine
c) the blood flow is greater in the small intestine than in the other parts of the gut
d) the surface area of the small intestine is greater than most other parts of the gut
e) the small intestine has nonspecific carriers for most drugs
B
Twenty (20) mg of a non-polar drug whose molecular weight is 250 is administered
intravenously as a single bolus dose to a 50 kg woman. The extracellular volume is 9.5 liters,
interstitial volume is 7.5 liters and intracellular volume is 22 liters. Taking into account the
properties of the molecule, the most likely explanation for the results presented in the figure is:
a) the drug is unable to pass across capillaries and is entirely contained within the plasma
volume.
b) the drug is highly bound to plasma proteins and is sequestered in the plasma volume
c) the drug is rapidly distributed throughout the total body water
d) the drug is contained within the extracellular water
e) the drug is sequester in fat deposits.
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B. 0.4 mg /min
Dm = (Css Cl 1 hr)/F
F=1
Cp(0) = 100 ng/mL
t(1/2) = 7 hours
dose = 1.0 mg
Css = 1ug/mL
First, you need to find Cl
Cl = k(e) * Vd
k(e) = 0.7/t(1/2) = 0.1
Vd = dose/Cp(0)
Cp(0) from the graph is 100 ng/ml = 100e-6 mg/ml
Vd = 1 mg / (100e-6 mg/ml) = 10000 mL = 10 L
Back to Cl = (0.1 * 10 L) = 1 L/hr
a) 10 μg/hr
b) 100 μg/hr
c) 1 mg/hr
d) 10 mg/hr
e) 100 mg/hr
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A. Concentration of plasma = concentration interstitial space
A patient is administered a drug that does not cross membranes, and does not bind to serum
proteins. The patient's hematocrit is 0.4, blood volume is 5 liters, and interstitial volume is 12
liters. The amount of drug in the interstitial volume is 12 mg. What is the plasma concentration
of the drug?
a) 1mg/liter
b) 1.2 mg/liter
c) 4 mg/liter
d) 2.2 mg/liter
e) 8 mg/liter
C. 3mg. Plasma volume = blood volume * (1-hematocrit) = 3 L. Drug concentration of plasma =
drug concentration of interstitial space = 1mg/L, so 3 mg
A patient is administered a drug that does not cross membranes, and does not bind to serum
proteins. The patient's hematocrit is 0.4, blood volume is 5 liters, and interstitial volume is 12
liters. The amount of drug in the interstitial volume is 12 mg. What is the mass amount of drug in
the plasma?
a) 1 mg
b) 1.2 mg
c) 3 mg
d) 4 mg
e) 6 mg
C
Drug A is 60% bound to albumin and the plasma concentration of drug A that is not bound to
albumin is 12 mg/liter. The patient is treated with a second drug that competes for albumin
binding. After addition of the second drug only 20 % of the drug A is bound. What is the new
free concentration of drug A immediately after addition of the second drug (i.e. before any of
drug A is eliminated)?
a) 1.4 mg/liter
b) 14 mg/liter
c) 24 mg/liter
d) 1.2 mg/liter
e) 12 mg/liter
C
Your patient is being administered a drug orally and you find that there are large fluctuations
between administrations. You do not want to change the therapeutic concentration. You should:
Dm = (Css Cl Tm )/F
F=1
Css = 1mg/L
Cl = 4.8 L/hr
Tm = 6 hours
Dm = 28.8 mg
Mr. Jones is admitted to General Hospital with pneumonia due to gram-negative bacteria. The
antibiotic tobramycin is ordered. The clearance (cl) and Vd of tobramycin for Mr. Jones are 4.8
liters/hr and 40 liters, respectively. What approximate maintenance dose should be
administered intravenously every 6 hours to eventually obtain average steady- state plasma
concentrations of 1mg/L?
a) 19 mg
b) 29 mg
c) 115 mg
d) 160 mg
e) 230 mg
C. chronic beta-blocker treatment caused supersensitivity of cardiac beta receptors
A patient you have been treating for hypertension with propranolol, suddenly stops taking his
medication and develops heart palpitations and rhythm irregularities. What receptor mechanism
might explain his current problem?
a. chronic beta-blockers cause down regulation of cardiac beta-receptors
b. beta-blockers are still in his bloodstream exerting an effect one day after stopping
c. chronic beta-blocker treatment caused supersensitivity of cardiac beta receptors
d. he should have been on another type of antihypertensive medication
e. over time, beta-blocker treatment caused desensitivity of beta-receptors
...
Which of the following statements best describes drugs classified as partial agonists?
a. partial agonists are prodrugs that split into full agonists in the body
b. full agonists are more potent that partial agonists
c. partial agonists have less efficacy than full agonists
d. partial agonists are also called negative antagonists
e. competitive antagonists used at a low concentration act like partial
agonists
...
Which of the following statements is correct concerning the therapeutic index (TI)?
a. TI is a measure of unit cost of drug per administration
b. penicillin has a smaller TI than warfarin
c. TI is the ratio of LD50 toxic effect/ED50 beneficial effect
d. the smaller the value of the TI, the safer the drug
e. LD50 values an equal to the TI for most drugs
...
Referring to the figure, which statement is correct?
a. A could be a full agonist, B a partial agonist and C an antagonist
b. A has more efficacy than B or C
c. C is the most potent drug
d. Curves B and C could be drug A plus increasing doses of competitive antagonist
e. maximal efficacy and the ED50 values of A, B, and C are the same
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...
Referring to the figure, which statement is correct?
a. A could be full agonist, B a partial agonist and C an antagonist
b. A has more efficacy than B or C
c. the rank order of potency is A>B>C
d. curves B and C could be drug A plus increasing doses of a noncompetitive
antagonist
e. maximal effect and the ED50 values of A,B and C are different
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...
An advertisement in a local newspaper seeks to enroll 200 patients with arthritis in a
medical study that would be the first time this new medicine would be tested in persons
with this disease. The study would therefore be classified as which type of trial?
a. phase 1 clinical study
b. phase II clinical study
c. phase III clinical study
d. phase IV clinical study
e. phase o preclinical study
...
A 25 year-old woman presents with muscle weakness, drooping eyelids and double
vision that she states worsened over the past 3-4 months. These symptoms are rapidly
reversed when she is given i.v. edrophonium for diagnostic purposes. Which of the
following agents might best treat her disease.
a. bethanechol
b. physostigmine
c. pilocarpine
d. pyridostigmine
e. tacrine
...
A 48 year old man is diagnosed with Sjogren's Syndrome, which is characterized by
chronic dry mouth due to undersecretion of saliva (xerostomia). Which of the following
agents might best treat this condition?
a. atropine
b. physostigmine
c. pilocarpine
d. pyridostigmine
e. donepezil
...
A 55 year old man suffers a myocardial infarction (MI or heart attack) and is stabilized in
the hospital. The next day his heart rate is less than 35 beats per min. Which of the
following agents might be administered to treat him?
a. atropine
b. sucinylcholine
c. tubocurarine
d. pilocarpine
e. pyridostigmine
...
A 24 year old medical student is taking his first spring break cruise and is worried about
getting sea sick on the ship. He asks his physician what medicine he can take so he does
not spend the entire cruise hanging over the railing. What agent that conveniently comes
in a skin patch formulation would his doctor recommend?
a. atropine
b. tolterodine
c. tubocurarine
d. ipratropium
e. scopolamine
...
A 9-year old boy is rushed to the Emergency Department wheezing, with labored
breathing and falling blood pressure. His mother tells the physician that he was stung by a
bee about 30 minutes ago. Which agent is given immediately to counteract the boy's
condition?
a. dobutamine
b. epinephrine
c. clonidine
d. ephedrine
e. amphetamine
...
A 16-year old athlete suffers from asthma after running for a touchdown. He is promptly
treated by using an inhaler and recovers in 10 minutes. Which one of the following agents
is most likely to be the active ingredient in the inhaler?
a. albuterol
b. epinephrine
c. clonidine
d. dobutamine
e. ephedrine
...
A 60 year old man is admitted to the hospital with an acute myocardial infarction (MI)
which leads to congestive heart failure. Which of the following agents known to
increase survival in patients, is most likely administered to the patient?
a. phenoxybenzamine
b. pindolol
c. carvedilol
d. dobutamine
e. dopamine
...
Which of the following drugs will decrease heart rate, cardiac contractility, and renin
secretion?
a. physotigmine
b. phentolamine
c. dobutamine
d. atropine
e. metoprolol
...
An elderly woman is found to exhibit elevated intraocular pressure, and open angle
glaucoma is diagnosed. Her physician prescribes pilocarpine every 6 hours. The
anticipated effect of pilocarpine eye drops would be to
a. relax the ciliary muscle
b. improve accommodation
c. relax the sphincter muscle of the iris
d. inhibit the production of aqueous humor by the ciliary epithelium
e. contract the longitudinal ciliary muscle and pull on the trabecular network to
relieve pressure
...
In a log dose-response plot, drug efficacy is determined by the maximal height of the
measured response on the effect axis, whereas drug potency is determined by:
a. number of animals exhibiting an all or none response
b. signal transduction pathway
c. formula, including the affinity of the drug and the number of drug receptors
d. position of the curve on the log-dose axis
e. steepness of the dose response curve
...
Which of the following drug interaction mechanisms is most likely to lead to sustained
elevations of plasma drug concentrations and drug toxicity?
a. induction of cytochrome CYP2C19
b. inhibition of cytochrome CYP3A4
c. displacement of a drug from plasma albumin binding sites
d. inhibition of the P-glycoprotein carrier protein
e. acceleration of gastric emptying by a "prokinetic" drug
...
Elderly persons have altered drug disposition because of
a. marked reduced absorption of many drugs
b. higher volumes of distribution of water soluble drugs
c. accelerated excretion of ionized drugs
d. increased permeability of the blood brain barrier
e. reduced capacity to oxidize drugs
...
If a test dose of edrophonium causes increased muscle weakness in a woman treated for
myasthenia gravis with pyridostigmine, it indicates that
a. the dose of edrophonium was too large
b. the dose of edrophonium was too small
c. the patient does not have myasthenia gravis
d. the dose of pyridostigmine should be increased
e. the dose of pyridostigmine should be reduced
...
Pyralidoxime improves muscle strength in persons exposed to toxic levels of an
organophosphate compound by
a. an action that leads to increased degradation of acetylcholine
b. binding to and activating nicotinic receptors
c. increasing the elimination of organophosphate compounds
d. increasing acetylcholine levels at cholinergic synapses
e. selectively blocking muscarinic receptors
...
Which effect is produced in the ciliary body after topical ocular administration of
clonidine or a derivative, apraclonidine?
a. increased inositol triphosphate (IP3)
b. increased cyclic AMP
c. decreased cyclic AMP
d. increased cyclic GMP
e. decreased cyclic GMP
...
Which drug is lease likely to slow recovery from hypoglycemia in a diabetic patient who
has taken an excessive dose of insulin?
a. metoprolol
b. propranolol
c. pindolol
d. labetalol
e. nadolol
...
For each patient described, select the most appropriate drug from the lettered sources
a. labetalol
b. phenoxybenzamine
c. propranolol
d. tamsulosin
e. phentolamine
23. A woman experiences pain and ischemia in her finger after accidentally injecting it with
an epinephrine auto injector that she carries for emergency treatment of allergic reactions
24. A man complains of urinary urgency, frequency and nocturia and is found to have benign
enlargement of the prostate gland
25. A woman with essential hypertension requires a drug that reduces both cardiac output
and peripheral resistance
26. A patient with episodic hypertension is found to have markedly elevated levels of
epinephrine and norepinephrine metabolites in his urine, and requires a long acting drug
to lower blood pressure before surgery
...
A patient suffering from depression and allergic to SSRI (selective serotonin reuptake
inhibitors) and tricyclic antidepressants was administered a monoamine oxidase inhibitor
(MAOI). You inform this patient that certain foods containing tyramine could now be
absorbed and could cause a hypertensive crisis. The primary site of action of tyramine is
a. ganglionic receptors
b. gut and liver catechol-o-methyltransferase
c. postganglionic sympathetic nerve terminals
d. vascular smooth muscle cell receptors
e. preganglionic sympathetic nerve terminals
...
Although it does not act at any histamine receptors, epinephrine reverses many effects of
histamine. Epinephrine is a
a. competitive inhibitor of histamine
b. noncompetitive antagonist of histamine
c. physiological antagonist of histamine
d. chemical antagonist of histamine
e. metabolic inhibitor of histamine
...
The heart rate response to the infusion of a moderate dose of phenylephrine in a
conscious patient is not blocked by
a. atropine
b. trimethaphan
c. phenoxybenzamine
d. reserpine
e. scopolamine
...
A new drug was administered to a group of normal volunteers. Intravenous bolus doses
produced the changes in blood pressure and heart rate shown in the graph below. The
most probable receptor affinities of this new drug are:
a. increase in arterial pressure, relaxation of the smooth muscle of the GI tract, and
contraction of the radial muscle of the iris
b. increase in arterial blood pressure, increase in heart rate and relaxation of the
radial muscle of the iris
c. decrease in blood pressure and relaxation of the smooth muscle of the GI tract
d. no change in heart rate, no change in blood pressure and no change in the tone of
the radial muscle of the iris
e. decrease in arterial blood pressure and no change in heart rate
...
Susceptibility to cholinesterases: -
Pharmacological Actions
Cardiovascular: +/-
GastroIntestinal: +++
Urinary
Bladder +++
Eye (topical) ++
Antagonism by Atropine +++
Nicotinic -
The above table depicts the pharmacological profile of a drug (DRUG A) that acts on the
cholinergic system. From the profile you would suppose the drug is most likely:
(+ = degree of activity)
a. pilocarpine
b. acetylcholine
c. methacholine
d. bethanechol
e. neostigmine
...
A drug (Drug 1) was given as an IV bolus to a subject while blood pressure and
heart rate were recorded as shown on the left side of the graph below. After recovery from the
effects of Drug 1, a long-acting dose of Drug 2 was given. After the recorder was turned back
on,
Drug 1 was repeated with the results shown on the right side of the graph.
In Professor PharmPhys's demonstration, a mediator of the late slow EPSP could be:
a. dopamine
b. acetylcholine
c. neuropeptide Y
d. an autacoid (eg. angiotensin)
e. nicotine
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...
During a laboratory demonstration to depict the complexity of neurotransmission in
autonomic ganglia, Professor PharmPhys sets up an anesthetized mammalian preparation in
which he is recording postsynaptic events following the electrical stimulation of preganglionic
sympathetic nerves. This demonstrates a complex action potential consisting of a fast EPSP
followed by a slow IPSP, followed by a slow EPSP and finally by a very late and slow EPSP
(see
figure below).
Drug X could be
a. cocaine
b. acetylcholine
c. propranolol
d. guanethidine
e. dobutamine
Drug Y could be
a. prazosin
b. phenoxybenzamine
c. clonidine
d. terbutaline
e. phenylephrine
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...
A patient suffering from cardiogenic shock is treated with drug X that increases blood
flow through the mesenteric and renal vascular beds, activates alpha1 adrenergic receptors in
several other vascular beds and directly and indirectly stimulates beta1 adrenergic receptors
in the heart. The effect of drug X on the mesenteric and renal vascular beds can be
blocked by a drug that antagonizes:
a. beta2-adrenergic receptors
b. muscarinic-cholinergic receptors
c. dopamine receptors
d. the release of epinephrine from the adrenal medulla
e. alpha-adrenergic receptors
...
A patient suffering from nasal congestion is being treated with drug X. Drug X produces
its pharmacological effect by activating a receptor linked via a G-protein to the opening
of membrane Ca2+ channels and to activation of phospholipase C with a resultant increase
in two second messengers. A second messenger formed following treatment with drug X
is:
a. cyclic AMP
b. cyclic GMP
c. nitric oxide
d. inositol triphosphate
e. arachidonic acid
...
During the catalytic cycle of the cytochrome P450-dependent monooxygenase system the
ferric (Fe+3) hemocytochrome P-450 substrate complex is reduced by a single electron to
the ferrous (Fe+2) hemocytochrome complex. The electron is provided by:
a. NADPH
b. NADP+
c. aldehyde dehydrogenase
d. molecular oxygen
e. GSH-S-transferase
...
Intravenous administration of Drug X to an anesthetized or unanesthetized mammal or
human produces a pressor response (increase in blood pressure). After administration of
Drug Y, Drug X produces no change in blood pressure. Which of the following pairs of
drugs would NOT produce the above sequence of events? (Drug X to Drug Y)
a. phenlyephrine phentolamine
b. ephedrine prazosin
c. isoproterenol atropine
d. norepinephrine phenoxybenzamine
e. amphetamine terazosin
...
Beta adrenergic blocking agents are very useful drugs and can be used to treat numerous
clinical conditions. Because of this there are many beta blockers on the market. In which
way does metoprolol differ from propranolol?
a) vecuronium
b) succinylcholine
c) atracurium
d) miracurium
e) d-tubocurarine
D
A 51-year-old male has been treated over the last 3 months for hypertension with a
medication that works by inhibiting the transport of norepinephrine from the neuronal cytoplasm
into synaptic vesicles. On a check-up visit to his primary care physician, the patient notes that
he has been feeling "depressed and sluggish" over the last week. The
patient was most likely receiving:
a) guanadrel
b) clonidine
c) methyldopa
d) reserpine
e) propranolol
E. Cimetidine is an important inhibitor of CYP1A2, as is grapefruit juice
A 46-year-old female with asthma has been stabilized on theophylline, a drug
metabolized by CYP1A2. She has been treated for 6 months without any complaints of adverse
effects. One week after the patient went to the pharmacy to purchase an over-the-counter
(OTC) medication to help relieve her "heartburn" symptoms she began experiencing
palpitations, tremors and nausea (side effects of theophylline). What was the most likely OTC
medication?
a) chlorpheniramine
b) atropine
c) ethanol
d) aspirin
e) cimetidine
C. Beta blockers are used to prevent cardiovascular effects seen in thyrotoxicosis
A 43-year-old female with thyroid dysfunction is currently thought to be in thyroid storm
(thyrotoxicosis). She is given a drug to prevent cardiovascular effects seen in thyrotoxicosis.
This drug was most likely:
a) clonidine
b) prazosin
c) propranolol
d) methyldopa
e) atropine
C. Histamine, because nothing else makes sense.
In experimental studies, when anesthetized subjects are treated intravenously with drug X, they
exhibit a marked decrease in blood pressure and a large reflex increase in heart
rate. Pretreatment of the subjects with either atropine or propranolol fails to block the decrease
in blood pressure. Drug X is most likely to be which of the following agents?
a) acetylcholine
b) epinephrine
c) histamine
d) isoproterenol
e) succinylcholine
B. Clonidine
The accompanying table shows cardiovascular changes induced by drug treatment in
experimental subjects. Which of the following drugs is most likely to cause changes shown in
Profile 4?
a) amphetamine
b) clonidine
c) epinephrine
d) isoproterenol
e) tyramine
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C. Epinephrine
Which of the following drugs would most likely cause the effects observed in Profile 2:
a) amphetamine
b) clonidine
c) epinephrine
d) isoproterenol
e) tyramine
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D. Isoproterenol
Which of the following drugs would most likely cause the effects observed in Profile 3:
a) amphetamine
b) clonidine
c) epinephrine
d) isoproterenol
e) tyramine
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D. Pilocarpine
A 71-year-old man with acute angle-closure (narrow angle) glaucoma is brought into the
emergency department because he is experiencing extreme pain in his left eye, is seeing halos
around lights and has an intensely red left eye and a steamy-appearing cornea. Which of the
following drugs would be considered appropriate medical treatment for this disorder?
a) atropine
b) edrophonium
c) timolol
d) pilocarpine
e) carvedilol
D. Succinylcholine is a depolarizing agent, initial stage of overactivation.
A 42-year-old man requires emergency tracheal intubation and is given succinylcholine. Which
of the following best described the molecular action of succinylcholine as a neuromuscular
blocker in this patient?
a) acetylcholinesterase inhibitor
b) muscarinic receptor agonist
c) muscarinic receptor antagonist
d) nicotinic receptor agonist
e) nicotinic receptor antagonist
E. Propanolol
In experimental studies when anesthetized subjects are treated intravenously with an agonist
(drug X), they have an increase in their blood glucose level and in the force of ventricular
contraction and a slight decrease in peripheral resistance. Pretreatment of the subjects with an
antagonist (drug Y) almost completely blocks all of these effects. Drug Y is most likely to be
which of the following agents?
a) metoprolol
b) atropine
c) guanethidine
d) phentolamine
e) propranolol
E
In experimental studies when anesthetized subjects are treated intravenously with drug X, they
show a marked increase in both systolic and diastolic blood pressure and a
decrease in heart rate. However, if they are pretreated with prazosin they show a modest to
slight increase in the systolic blood pressure and a marked increase in heart rate.
a) acetylcholine
b) epinephrine
c) histamine
d) isoproterenol
e) norepinephrine
...
The accompanying figure depicts nerves in the autonomic and somatic nervous system. Five
sites are labeled with the numbers 1 through 5. Muscarinic receptors are commonly associated
with which site?
a) Site 1
b) Site 2
c) Site 3
d) Site 4
e) Site 5
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D
Norepinephrine is the neurotransmitter commonly associated with which site?
a) Site 1
b) Site 2
c) Site 3
d) Site 4
e) Site 5
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B
The neurotransmitter associated with Site 5 is:
a) norepinephrine
b) acetylcholine
c) serotonin
d) neuropeptide Y
e) epinephrine
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B.
Mydriasis is controlled by alpha-1 receptors, and hypotension that results from blocking alpha-1
receptors would produce reflex tachycardia.
A patient comes into your office and upon examination and careful history you observe the
following effects. Orthostatic hypotension, miosis and tachycardia. The patient had been taking
medication but couldn't remember the name. You surmise this was a drug that acted on which
of the following receptors:
a) M2 receptors
b) alpha1 receptors
c) nicotinic cholinergic receptors
d) beta1 adrenergic receptors
e) alpha2 adrenergic receptors
D
The above diagram represents concentration effect curves to norepinephrine showing
increases in mean arterial blood pressure in an anesthetized individual. Curve X and Y
represent the effect of norepinephrine in the presence of Drug X or Drug Y. Drug X is
most likely acting at which of the following:
a) vesicular amine transporter
b) uptake 2
c) monoamine oxidase
d) uptake 1
e) catechol-o-methyltransferase
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E
The above diagram represents concentration effect curves to norepinephrine showing increases
in mean arterial blood pressure in an anesthetized individual. Curve X and Y represent the
effect of norepinephrine in the presence of Drug X or Drug Y.
a) alpha2 adrenergic
b) nicotinic cholinergic
c) beta1 adrenergic
d) muscarinic cholinergic
e) alpha1 adrenergic
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B
As a busy third year student you are working in an outpatient clinic and find yourself treating an
interesting patient. This young woman is a violinist for the famous St. Louis
symphony. She tells you she gets frightfully nervous before each performance. Her symptoms
include muscle tremor, diarrhea, nervousness and palpitations. She asks for some medication
to help. The drug you choose most likely works on which of the
following receptors:
a) alpha1 adrenergic
b) beta1 and beta2 adrenergic
3) muscarinic cholinergic
d) nicotinic cholinergic
e) alpha2 adrenergic
22. C
23. B, atracurium is a nondepolarizing neuromuscular relaxant
24. E
25. C, Tamsulosin is an alpha-1 blocker used in the treatment of BPH
The above diagram depicts targets for drug actions (A-->E) located in nerves or innervated
organs. Match the following drugs with their primary site of action. (Letter can be used more
than once).
22. carvedilol
23. atracurium
24. tacrine
25. tamsulosin
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C. Terazosin, which is an alpha-1 blocker, used in the treatment of BPH. It leads to symptoms of
urinary hesitancy, frequent urination, dysuria (painful urination), increased risk of urinary tract
infections, and urinary retention.
A 70-year-old male patient comes into your office complaining of urinary tract symptoms. He
states that he has hesitancy in voiding, needs to void with great frequency and has a poor
stream when voiding. A drug that would be useful in helping these symptoms would be which of
the following:
a) tolterodine
b) propranolol
c) terazosin
d) phenylephrine
e) terbutaline
B. Phenylephrine, which activates alpha-1 receptors, which are linked to PLC and IP3, DAG and
Ca2+
A patient suffering from nasal congestion is being treated with drug Y. Drug Y produces its
pharmacological effect by activating a receptor that is linked via a Gprotein to the opening of
membrane Ca2+ channels and to the activation of phospholipase C with a resultant increase in
two additional second messengers. Drug Y is most likely:
a) edrophonium
b) phenylephrine
c) phentolamine
d) pindolol
e) pancuronium
D
The above graph depicts the hydrolysis and % inhibition of succinylcholine in two
patients (patients X and Y). Patient Y is one that has which of the following:
a) normal pseudocholinesterase
b) polymorphism of CYP3A4
c) polymorphism of N-acetylation
d) atypical pseudocholinesterase
e) polymorphism of glucuronal transferase
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C
According to the above table, C refers to a:
a) toxic response
b) idiosyncratic response
c) allergic response
d) placebo response
e) supersensitivity response
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E. CYP450 reactions include dehalogenation among other oxidation reactions. Phase II are
conjugation, and cyp-independent include the others
Cytochrome P450's (CYP 450) are an important family of enzymes involved in the
biotransformation of xenobiotics or drugs. Which of the following is a CYP450 reaction:
a) amine oxidation
b) alcohol dehydrogenation
c) acetylation
d) methylation
e) dehalogenation
C. Muscarinic, probably ipratropium
When applied to the airway of an asthmatic individual, drug X causes bronchodilation. The
effect is not blocked by labetalol. Drug X does not normally have any central nervous system
effect and if given by mouth has a bioavailability of less than 30%.
a) atropine alone
b) atropine plus neostigmine
c) atropine plus pralidoxime
d) atropine plus ipratropium
e) atropine plus physostigmine
D
Unfortunately you have a wisdom tooth that has to be removed. You go to your favorite dentist
and he gives you a local anesthetic prior to proceeding to extract the tooth. The
local anesthetic he gives you is procaine. He explains that epinephrine is also present in
the solution containing procaine. Epinephrine is present in the procaine solution in order
to:
What changes (if any) in firing rates of the nerves would be expected to occur following the
administration of the last drug in each series of drugs listed below? Presume that sufficient time
for the actions of the premedicating agents has been allowed and then the last agent is given
intravenously.
Give one answer for each set of nerves (in order I-IV) from the choices below.
= increase of nerve activity; = decrease nerve activity; ↔ = no change in neural firing
What changes (if any) in firing rates of the nerves would be expected to occur following
the administration of the last drug in each series of drugs listed below? Presume that sufficient
time for the actions of the premedicating agents has been allowed and then the last agent is
given intravenously.
Give one answer for each set of nerves (in order I-IV) from the choices below.
= increase of nerve activity; = decrease nerve activity; ↔ = no change in neural firing
What changes (if any) in firing rates of the nerves would be expected to occur following
the administration of the last drug in each series of drugs listed below? Presume that sufficient
time for the actions of the premedicating agents has been allowed and then the last agent is
given intravenously.
Give one answer for each set of nerves (in order I-IV) from the choices below.
= increase of nerve activity; = decrease nerve activity; ↔ = no change in neural firing
a) schedule V drug
b) schedule II drug
c) schedule I drug
d) schedule III drug
e) unscheduled drug
E
The drug act that established guidelines for the truthful labeling of drugs and set
guidelines for the safety of drugs and established the Food and Drug Administration
(FDA) was:
a) Kefauver-Harris Amendments of 1962
b) Orphan Drug Amendments of 1983
c) Expediated Drug Approval Act of 1992
d) Pure Food and Drug Act of 1906
e) Food, Drug and Cosmetic Act of 1938
C
You have a patient that suffers from angina pectoris, hypertension and chronic obstructive
pulmonary disease (COPD).You are concerned about the use of beta blockers in this patient.
However, because of drug allergies to other drugs, you decide
to use a beta blocker anyway. The best choice in such a patient would be:
a) propranolol
b) labetalol
c) metoprolol
d) pindolol
e) carvedilol
C. A beta blocker with an alpha blocker
The effects depicted on the graph above on blood pressure were recorded in a subject before (I)
and after (II) pretreatment with a drug or combination of drugs. Which pretreatment regimen was
used (select a single drug in preference to a combination if
possible).
a) trimethaphan
b) phentolamine + propranolol
c) carvedilol + phenoxybenzamine
d) metoprolol
e) atropine
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B
Concerning clinical trials, which phase involves numerous physicians and is designed to provide
information on adverse drug reactions following use in large numbers of patients:
a) phase 1
b) phase 4
c) phase 3
d) phase 2
e) phase 5
C
Patient X is asked to climb a set of stairs. After a few minutes he is unable to continue.
Treatment with pyridostigmine allows him to continue to climb the stairs without difficulty. A side
effect that may occur in patient X is:
a) mydriasis
b) tachycardia
c) bronchoconstriction
d) dry mouth
e) hypertension
A
You are testing drug combinations containing two drugs. Both drugs bind to serum proteins.
Given alone drug A binds with a Kd of 10-7 while given alone drug B binds with a Kd of 10-3.
You give a bolus dose of drug that contains 1mg of each drug. Assume that there is no
difference in the distribution of the drugs. Which of the following statements is true concerning
the amounts of drug A and B?
a) 6ug/liter
b) 8ug/liter
c) 12ug/liter
d) 20ug/liter
e) 40ug/liter
D
A pharmaceutical company is testing the clearance (Cl) of two drugs, drug A and drug B. The
drugs are cleared by the liver. Drug A is cleared at the rate of liver perfusion, drug B at much
lower rate. Both drugs are 50% bound to albumin. If liver perfusion rate is increased, which of
the following is likely true concerning the clearance of drugs
A and B?
a) 5mg
b) 10mg
c) 70mg
d) 100mg
e) 700mg
C
In the absence of other drugs, pindolol causes an increase in heart rate by activating beta
receptors. However, in the presence of potent beta stimulants, administration of pindolol results
in a dose-dependant, reversible decrease in heart rate. Therefore, pindolol is:
a) noncompetitive antagonist
b) irreversible antagonist
c) partial agonist
d) spare receptor agonist
e) none of the above
D
Aspirin is a weak organic acid with a pKa of 3.5. What percentage of a given dose will be in the
lipid-soluble form at a stomach pH of 2.5?
a) 1%
b) 10%
c) 50%
d) 90%
e) 99%
E
Drug X is a weak acid, pKa = 6.0. It is eliminated almost entirely by glomerular filtration. Under
which of the following conditions would drug x likely be eliminated
most rapidly?
a) urinary pH = 4.5
b) urinary pH = 5.0
c) urinary pH = 6.0
d) urinary pH = 7.0
e) urinary pH = 8.0
D
A drug when administered at 3mg i.v. The following data has been collected for the plasma
concentration as a function of time. Which of the following answers best
describes these kinetics?
Five half lives needed to reach steady state concentration after a dosing regimen
Drug A has a drug half-life 80% of Drug B. Both drugs are eliminated by first order kinetics and
are administered with identical dosing regimens. The volume of distributions of Drugs A and B
are identical. Which of the following statements is true?
a) 4mg
b) 12mg
c) 40mg
d) 56mg
e) 60mg
E
The following Figure represents the concentration of drug in plasma with time.
Which of the following statements best describes the drug characteristics during the times
shown?
a) the drug is eliminated by only first order elimination
b) the drug is eliminated by only zero order kinetics
c) the drug is eliminated by passive diffusion
d) the drug is eliminated by passive diffusion then facilitated transport
e) the drug is eliminated by facilitated transport
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C
a) 0.5
b) 1.0
c) 1.5
d) 15
e) 50
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B
The figure above shows the elimination of drug x following administration of a 200 mg dose to a
50 kg woman. Calculate the elimination rate for the drug.
a) (0.1mg/liter)/hr
b) (1mg/liter)/hr
c) (10mg/liter)/hr
d) (100ug/liter)/hr
e) can not be calculated
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D
A drug is used to treat a patient suffering from nasal congestion. The drug produces its effect by
activating a G-protein coupled receptor that activates the G-protein Gq. The most likely
signaling pathway that this drug activates is:
a) 4 liters
b) 20 liters
c) 40 liters
d) 200 liters
e) 400 liters
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A
A drug is 50% absorbed and 80% of the drug is biotransformed in the liver. The transformed
form of the drug is not active. You administer 5mg of the drug orally 3 times a day. Calculate the
bioavailability of the drug.
a) 0.1
b) 0.2
c) 0.4
d) 0.5
e) 0.8
D
Drug A is to be administered I.V. to a healthy 60kg individual. The clearance of the drug is
20liters/hr, and the half-life is 10hrs. The therapeutic concentration is 0.2mg/liter. After steady
state has been achieved, what maintenance dose should be
administered?
a) age
b) social situation
c) his several medical problems
d) his number of medications
e) his compliance problem (the fact that he doesn't take the medications as prescribed)
A
Which pharmacokinetic parameter is least likely to change as a person ages?
a) absorption
b) distribution
c) biotransformation
d) excretion
D
A 39-year-old female is given a muscle relaxant prior to endotracheal intubation. Minutes later
the patient is noted to have a sudden onset of hyperthermia, tachycardia, sweating, cyanosis,
tachypnea and muscle rigidity. The muscle relaxant causing these
symptoms has the following mechanism of action:
a) competitive antagonist
b) cholinesterase inhibitor
c) antimuscarinic antagonist
d) depolarizing agent
e) muscarinic agonist
A
A pharmaceutical company has a promising drug that they think would be an advance in the
treatment of a disease. They have received permission to test their drug in normal volunteers.
This study would be classified as which type of trial?
a) alpha2-adrenergic
b) muscarinic-cholinergic
c) nicotinic-cholinergic
d) beta1-adrenergic
e) beta2-adrenergic
C. Metaproterenol is a Beta-2 agonist used in the treatment of asthma and COPD.
Dobutamine is a beta-1 agonist, Clonidine is an alpha-2 agonist, Ephedrine is like longer acting
epi, dopamine would not be suitable
A 16-year-old athlete suffers an asthmatic attack after running for a touchdown. He is promptly
treated by using an inhaler and recovers in 10 minutes. Which of the following agents is most
likely to be the active ingredient in the inhaler?
a) clonidine
b) dobutamine
c) metaproterenol
d) ephedrine
e) dopamine
C
An elderly woman living in Kansas City suffers from primary open-angle (chronic simple)
glaucoma. She has been taking a medication once per day but upon visiting her sister in St.
Louis, she discovers she has forgotten her medication. You prescribe timolol and explain it most
likely works primarily by:
a) contraction of the detrusor muscle of the bladder, relaxation of the trigone muscle and
sphincter, relaxation of the external sphincter
b) contraction of both the detrusor and trigone muscle as well as the external sphincter
c) relaxation of the detrusor muscles and contraction of the trigone muscle and sphincter and
contraction of the external sphincter
d) contraction of the detrusor muscle only
e) relaxation of the detrusor and trigone muscle and relaxation of the external
sphincter
D. Oxybutynin, an m1,2,3 antagonist.
Ipratroprium is also a muscarinic ant, but it is poorly absorbed, and mostly used to treat COPD.
Atropine is a muscarinic antagonist that is pretty nonselective, and has lots of side effects. So
would scopolamine.
Physostigmine would produce the opposite effect.
A problem that approaches nearly 10% of elderly women is incontinence. This can be
embarrassing and affect one's life style. A drug that is commonly used to help with this problem
is which of the following:
a) ipratroprium
b) atropine
c) physostigmine
d) oxybutynin
e) scopolamine
E. Ipratroprium is a muscarinic antagonist used for first line treatment against COPD attacks.
Scopolamine is a muscarinic antagonist and so is atropine.
Tolterodine (Detrol) is a muscarinic antagonist usually used for urinary issues.
Physostigmine is a AChEI that would do the opposite.
Patients who smoke cigarettes often have a higher incident of chronic obstructive pulmonary
disease (COPD) which includes emphysema and bronchitis. Several types of drugs are
available to treat COPD. Which of the following would be preferred to treat acute bronchospasm
that can accompany COPD?
a) scopolamine
b) physostigmine
c) atropine
d) tolterodine
e) ipratropium
B. Trimethaphan, which is a nicotinic antagonist that would block fast EPSP.
Drug X has been given to a patient who developed a hypertensive crisis with a precipitous
severe elevation of blood pressure. Drug X produced the following effects: tachycardia,
cycloplegia, urinary retention, dry mouth, relaxation of arterial and venous smooth muscle and
pooling of blood. Drug X is most likely:
a) atropine
b) trimethaphan
c) datroline
d) pilocarpine
e) neostigmine
B
Drug X is most likely:
a) phentolamine
b) metoprolol
c) reserpine
d) clonidine
e) methyldopa
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E, an alpha-1 blocker
Drug Y is most likely:
a) reserpine
b) methyldopa
c) propranolol
d) clonidine
e) prazosin
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A
When norepinephrine is administered by a bolus iv injection of a therapeutic dose, which is the
most likely effect illustrated in the above table.
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A???
A drug which would cause the appearance of the direct effect of norepinephrine on heart rate
could be:
a) phentolamine
b) propranolol
c) isoproterenol
d) atropine
e) albuterol
C
Botulinium toxin (BoTox) has been found useful in treating several ocular conditions such as
strabismus (cross-eyes), hemifacial spasms), muscle spasms such as cervical dystonia;
achalasia) as well as dermatological conditions such as hyperhidrosis. This drug works by which
of the following mechanisms?
a) atropine
b) pralidoxime
c) atropine + pralidoxime
d) epinephrine + atropine
e) ipratroprium + atropine
B
In comparing methyldopa and guanethidine which of the following is correct?
a) guanethidine - but not methyldopa - results in salt and water retention when used alone
b) guanethidine causes fewer CNS side effects (such as sedation) than methyldopa
c) guanethidine causes more immunologic adverse effects (e.g. hemolytic anemia)
than methyldopa
d) guanethidine is less efficacious than methyldopa in severe hypertension
e) methyldopa causes more orthostatic hypotension; than guanethidine
A. Phenylephrine is an alpha-1 agonist, leads to increases in SVR and reflex bradycardia.
Phentolamine is an alpha blocker that would reduce this effect.
When given to a patient, phentolamine blocks which of the following?
a) acetylcholinesterase
b) tyrosine hydroxylase
c) choline acetyltransferase
d) choline hydroxylase
e) monoamine oxidase
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C. Ambenonium is a cholinesterase inhibitor
A drug that acts on Enzyme Z to break down neurotransmitter 2 could be:
a) atropine
b) bethanechol
c) ambenonium
d) succinylcholine
e) vecuronium
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D
In comparing metoprolol and propranolol which of the following is a correct statement?
a) administration of bethanechol
b) administration of histamine
c) administration of isoproterenol
d) stimulation of sympathetic nerves
e) stimulation of the vagus nerve
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D. Carvedilol is, along with labetalol, a non selective beta blocker with also alpha-1 blocker
activities.
A new drug was administered to an anesthetized animal with the results shown. A large
dose of epinephrine was administered before and after the new agent for comparison.
Which of the following agents does the new drug most closely resemble?
a) nadolol
b) scopolamine
c) prazosin
d) carvedilol
e) metoprolol
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C
Of the following pairs of drugs and the CYP450 enzyme that carries out
biotransformation which pair is not correctly matched?
Phase I are mostly nitro reductions, oxidations, deaminations, dealkylations, and hydroxylations.
Phase II are conjugation rxns: glucuronidations, acetylations, mercapturic acid formation, sulfate
conjugation, N O and S methylation, trans-sulfuration
Biotransformation reactions have been conveniently placed in two types; namely phase 1 and
phase 2. Which of the following is a phase 2 reaction?
a) nitro reduction
b) deamination of epinephrine
c) o-dealkylation
d) aliphatic hydroxylation
e) acetylation
A. Phenoxybenzamine is an alpha blocker
The following diagram depicts the effects of various drugs on blood pressure on an anesthetized
mammal before and after pretreatment with Drug X.
Drug X is:
a) phenoxybenzomine
b) propranolol
c) atropine
d) neostigmine
e) reserpine
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B. Atropine
The following diagram depicts the effects of various drugs on blood pressure on an anesthetized
mammal before and after pretreatment with Drug Y.
a) absorption
b) distribution
c) hepatic metabolism
d) renal excretion
A. Isoniazid is transformated mainly by n-acetyation.
Isoniazid is an important anti-tubercular drug that can result in drug interactions. It is
biotransformed primarily by which of the following
a) N-acetylation
b) ester hydrolysis
c) oxidation
d) glycine conjugation
e) dehydrogeneration
D
A patient is admitted to the emergency room 4 hours after taking an overdose of barbiturate.
The plasma concentration of the drug at the time of admission is 100mg/liter, and the volume of
distribution and the half-life of the drug are 30liters and 2 hours, respectively. The ingested dose
was?
a) 25mg/liter
b) 50mg/liter
c) 200mg/liter
d) 400mg/liter
e) 800mg/liter
C
A patient suffering from depression and is allergic to SSRI drugs (selective serotonin reuptake
inhibitors) and tricyclic antidepressants was administered a monoamine oxidase inhibitor
(MAOI). You inform this patient that certain foods containing tyramine could now be absorbed
and could cause dangerously elevated blood pressure. The primary mechanism of action of
tyramine is a:
a) alpha1-adrenergic
b) muscarinic cholinergic
c) beta adrenergic
d) nicotinic cholinergic
e) alpha2-adrenergic
C
Dm = (Css Cl Tm)/F
Dm = (1 L/Hr 10 mg/LTm)/(0.40)
Dm/Tm = 25 mg/Hr
A patient (55kg) is taking a drug orally to reduce blood pressure. The clearance of the drug is
1.0liters/hour. The volume of distribution is 10ug/ml and the drug is 40% absorbed and does not
undergo biotransformation. What dosing regimen should be
administered to attain a therapeutic concentration of 10mg/liter?
a) 2 hours
b) 3 hours
c) 5 hours
d) 8 hours
e) 10 hours
B
A patient is on "Drug A" for pain. Drug A is a substrate of the CYP450 enzyme 2D6, and it is
metabolized to an inactive metabolite. Drug A is working well and the patient's pain is under
good control. The patient decides to take a second drug, "Drug B" for sinus congestion. Drug B
is an inducer of 2D6. What will be the potential clinical consequence of this patient taking Drug
B?
a) 10
b) 50
c) 100
d) 200
e) 400
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D. Involves trapping the drug in ionized form in urine.
You are treating a patient with a drug that is a weak base. The pK of the drug is 8.6 and its
molecular weight is 205. The drug is eliminated exclusively in the kidney by passive diffusion.
The extent of urinary excretion of the weak base will increase when:
a) her age
b) her number of medications
c) the type of medications she is prescribed
d) the pharmacodynamics of the drugs she is prescribed
e) the pharmacokinetics of the drugs she is prescribed
D
A new drug (drug X) is an antagonist against a beta1 adrenergic receptor. Additions of
increasing concentrations of norepinephrine overcome the effect of the drug so that values of
Emax are reached that equal those found in the absence of the drug. Drug X can be classified
as:
a) a chemical antagonist
b) a physiological antagonist
c) an irreversible non-competitive antagonist
d) a reversible competitive antagonist
e) an irreversible competitive antagonist
D
Disulfiram has been used to treat patient suffering from severe alcoholism. In the presence of
disulfiram, ethanol consumption results in patients being very sick. They experience nausea,
vomiting, dyspnea and occasional hypotension. The nausea, vomiting
and dyspnea is due to inhibition of:
a) CYP 2D6
b) alcohol dehydrogenase
c) monoamine oxidase
d) aldehyde dehydroxygenase
e) glutathione dehydrogenase
B
The pharmacological effect of drugs acting on different membrane receptors occur at quite
different time scales. Which of the following membrane receptors has the fastest time scale in
mediating its pharmacological effect?
a) nuclear receptors
b) ion channels
c) G-protein coupled receptors
d) tyrosine kinase receptors
e) serine/thereonine receptors
D. 280 mg
a) 4mg
b) 40mg
c) 28mg
d) 280mg
e) 320mg
B
You have administered 20mg of a drug i.v. and collected the data shown below. Calculate the
volume of distribution using the graph below.
a) 4 ml
b) 3.3liters
c) 4liters
d) 13.3liters
e) 400ml
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D
Phenylephrine is an alpha-1 agonist. It would trigger a change in heart rate through baroreflex
mechanisms.
Drug X causes an increase in blood pressure and a decrease in heart rate when administered
intravenously. If an antagonist at ganglionic nicotinic receptors is administered first, drug X
causes an increase in blood pressure and no change in heart rate. Drug X is most likely:
a) epinephrine
b) dopamine
c) norepinephrine
d) phenlyephrine
e) dobutamine
D
A drug company has just concluded drug tests with two drugs (drug 1 and 2) that lower blood
pressure. The figure above represents the quantal dose-effect curves.
a) 3mg
b) 12mg
c) 30mg
d) 120mg
e) 300mg
C. Tacrine is a AChEI used to treat Alzheimer's disease
Acetylcholinesterase inhibitors have been used to improve the symptoms of Alzeheimer's
Disease, a devastating disease of the elderly. This includes which of the following?
a) neostigmine
b) pralidoxime
c) tacrine
d) pyridostigmine
e) parathion
B
The company you work for has developed a new drug. You have determined that 90% of the
drug binds to serum proteins. The plasma concentration of the drug is 100mg/liter. The
extracellular and plasma volumes are 11 and 3 liters, respectively.
The amount of drug in the interstitial volume is:
a) 30mg
b) 80mg
c) 110mg
d) 200mg
e) 300mg
D. Resting state has GDP bound. Binding makes GDP release, allowing binding of GTP, then G
proteins dissociate. GTP hydrolysis to GDP makes G protein couple with the receptor again.
A new G-protein coupled receptor that regulates heart rate has just been isolated. Your
technician characterizes the receptor. Which of the characteristic concerning your receptor is
true?
a) less than 1%
b) 1%
c) more than 1%, less than 10%
d) 10%
e) 90%
E
A 50kg patient is given a hypnotic i.v. If the hypnotic drug is infused continuously at the rate of
1mg/kg/hr, and the steady state concentration is attained in 10 hours the half-life of the drug is:
a) 20 minutes
b) 30 minutes
c) 1 hour
d) 1 hour 30 minutes
e) 2 hours
C, Carvedilol along with Labetalol (two 3rd gen beta blockers) also have alpha-1 antagonist
activity.
a) timolol
b) carvedilol
c) propranolol
d) pinodol
e) prazosin
C
Two drugs A and B that are competitive inhibitors of acetylcholine are being compared. Drug A
is 75% absorbed in the gut and is not metabolized in the liver. Drug B is 90% absorbed in the
gut and 80% metabolized in the liver. Only the unmetabolized drug B is
active. Which of the following statements concerning drugs A and B is true?
a) 2mg/liter
b) 4.2mg/liter
c) 8.8mg/liter
d) 10mg/liter
e) 12.8mg/liter
D
The graph above is the plasma concentration versus time plot of drug A. Using the graph which
of the following statements is true?
a) beta 1-adrenergic
b) muscarinic-cholinergic
c) alpha 2-adrenergic
d) beta 2-adrenergic
e) alpha 1-adrenergic
D. The higher the partition coefficient, the better it can pass over membranes, the more the drug
is absorbed.
Drug X is a weak acid and can be taken orally. The drug is absorbed in the small intestine by
passive diffusion. To increase the rate of uptake the company should modify the drug to:
a) fentanyl
b) meperidine
c) morphine
d) oxycodone
D. Activation of alpha-1 receptors leads to activation through Gq/11 and PLC --> Dag and IP3
--> increasein Ca2+
A 69 year old man receives an infusion of norepinephrine to increase blood pressure following a
traumatic spinal cord injury. The signal transduction mechanisms leading to this effect include:
a) activation of a tyrosine kinase receptor
b) inhibition of adenylyl cyclase
c) activation of guanylyl cyclase
d) activation of phospholipase C
e) activation of protein kinase A
E. phosphorylation of receptors
A 72 year old woman is treated for acute heart failure with an infusion of
dobutamine. The duration of dobutamine infusion should be limited to several hours per day
because prolonged infusion may lead to drug tolerance as a result of:
a) cycloplegia
b) miosis
c) mydriasis
d) miosis and cycloplegia
e) mydriasis and cycloplegia
C
A 29 year old woman with myasthenia gravis is being treated with a steroid (prednisone) and
pyridostigmine. She complains to her physician of increasing diplopia and facial weakness. If an
intravenous dose of edrophonium causes increased muscle weakness in this patient, it indicates
that:
a) glucose-6-phosphate dehydrogenase
b) cytochrome P450
c) UDP-glucuronyl transferase
d) N-acetyl transferase
e) plasma cholinesterase
C. Disulfiram inhibits aldehyde deH and thus leads to build up of acetaldehyde.
Chronic alcoholics are sometimes treated with a drug that results in a series of
violent unpleasant effects including flushing, dyspnea, nausea, vomiting and
hypotension. The mechanism of action of this drug is to inhibit:
a) CYP3A4
b) monoamine oxidase
c) aldehyde dehydrogenase
d) CYP1A2
e) alcohol dehydrogenase
D.
A patient is taking drug A orally that gives a plasma drug concentration of
10ug/ml. Drug A is 90% bound to serum albumin. The patient now is put on a
new drug such that: The total amount of drug A in plasma is unchanged but a
fraction of drug A is displaced from albumin. In the presence of the two drugs
only 80% of drug A is bound to albumin. After administration of the second drug:
a) excessive sweating
b) dilation of the pupils
c) involuntary muscle contractions
d) flushing of the skin
e) sedation
C. Alpha-1 adrenergic agonist would
A man with diabetic autonomic neuropathy complains of dizziness and fainting when arising
from bed in the morning. A drug activating which receptors would be most beneficial to this
patient?
a) a β1 adrenergic agonist
b) a β2 adrenergic agonist
c) an α1 adrenergic agonist
d) α2 adrenergic agonist
e) a non-selective β adrenergic agonist
A. Increased cyclic AMP levels
After being stung by a yellow jacket, a woman experiences urticaria, laryngeal
edema, difficult breathing and hypertension. She receives oxygen and administration of an
adrenergic agonist. Which action would lead to bronchodilation?
a) amphetamine
b) clonidine
c) epinephrine
d) isoproterenol
e) tyramine
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A. administration of bethanechol, which is a muscarinic agonist.
In the accompanying figure, changes in bronchomotor tone in experimental subjects are
depicted in terms of constriction (+) or relaxation (-). The first panel of the figure (control) shows
changes that were elicited by five different procedures (numbered 1 through 5), each of which
was performed alone. The remaining panels show changes that were elicited by the same five
procedures, each of which was performed after pretreatment with a different drug. Based on the
results, procedure 1 is most likely:
a) administration of bethanechol
b) administration of histamine
c) administration of isoproterenol
d) stimulation of sympathetic nerves
e) stimulation of or the vagus nerve
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C. Prazosin, which is an alpha-1 blocker, along with Tamsulosin and Doxasozin (Cardura)
The above schema shows the effect of norepinephrine (NE), Drug X and Drug Y at the
sympathetic neuroeffector junction. Based on the sequence of events that NE, Drug X and Drug
Y produce, Drug Y is most likely which of the following:
a) phentolamine
b) phenoxybenzamine
c) prazosin
d) propranolol
e) metoprolol
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B. New Drug Application (NDA)
Following phase 3 clinical trial, if a drug meets expectations, a drug company will make an
application to the FDA for permission to market the new drug. Such an application is called:
a) propranolol
b) phentolamine
c) atropine
d) neostigmine
e) bethanechol
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D
Drug A has an EC50 of 10 nM and a maximum effect of 95%. Drug B has an EC50 of 75 nM
and a maximum effect of 100%. Drug C has an EC50 of 190 nM and a maximum effect of 34%.
Which of the following is correct?
a) cyclic AMP
b) stat translocation to the nucleus
c) cyclic GMP
d) inositol triphosphate
e) nitric oxide
D. Partial agonist, either Pindolol, Labetalol, or Celiprolol
When drug A is administered alone it results in an increase in heart rate by activating beta
adrenoreceptors. However, when you administer a highly effective beta stimulant, drug A
causes a dose dependent, reversible decrease in heart rate. Drug A is most likely?
a) a physiologic antagonist
b) a chemical antagonist
c) an irreversible antagonist
d) a partial agonist
e) a reversible antagonist
C
A drug company is testing two new high blood pressure drugs, drug A and drug B. Drug A and
drug B have half-lives of 4 hours and 8 hours, respectively. Both drugs exhibit the same Vd. You
administer 20mg/kg of each drug. Which of the following statements is most correct?
a) 2.5mg
b) 4mg
c) 4μg
d) 250μg
e) 1000μg
B
The patient's hematocrit is 0.4. The concentration of the drug in the plasma is 10μg/liter and the
concentration in the pelleted cells is 1μg/liter. Calculate the concentration of the drug in blood.
Choose the answer that is closest to the
calculated value.
a) 4.2μg/liter
b) 6.3μg/liter
c) 8.4μg/liter
d) 10μg/liter
e) 9.4μg/liter
D. Reserpine would deplete catecholamines, and thus prevent the effects of amphetamines,
which help with catecholamine release.
Amphetamine like drugs (dextro-amphetamine, methamphetamine) are known to have marked
CNS activity including wakefulness, alertness, decreased feeling of fatigue, self confidence,
elevation of mood as well as peripheral effects such as an increase in blood pressure and
myocardial stimulation. Pretreatment of which of the following drugs would prevent these effects
of dextro-amphetamine.
a) nadolol
b) atropine
c) clonidine
d) reserpine
e) terbutaline
B.
Use:
D(L) = (Vd * Css)/F
With Css = 10 ug/L, which is total blood concentration:
Plasma concentration = 9ug/L
Bound to serum proteins = 1ug/L
A 70kg male is taking drug A, a vitamin K inhibitor. The drug is 50% absorbed within minutes of
oral administration. None of the drug undergoes biotransformation. The volume of distribution =
10 liters. Ten percent of the drug binds to serum proteins. What dose of drug should be given to
attain an interstitial concentration of 9ug/liter of drug, if the drug is administered once a
day?
a) 0.1mg
b) 0.2mg
c) 0.3mg
d) 0.4mg
e) 0.8mg
C
Why should the use of amitriptyline be avoided in older persons?
Physiological antagonism refers to an interaction which results from one drug antagonizing the
response of another drug following stimulation of a different receptor.
This is a type of nonreceptor antagonism, along with chemical antagonism, in which the
antagonist sequesters agonist and prevents its activity.
a) chemical antagonism
b) non-competitive antagonism
c) physiologic antagonism
d) pseudo-irreversible antagonism
e) competitive antagonism
E
The figure shows the plasma concentration of an antibiotic as a function of time obtained after
an i.v. injection of 7mg.
If this drug is given as a constant i.v. drip it will attain its therapeutic concentration at what time
after the start of the administration.
a) ½ hr
b) 1 hr
c) 2 hrs
d) 3 hrs
e) 5 hrs
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E
Vd = dose/Cp(0)
The figure shows the plasma concentration of an antibiotic as a function of time obtained after
an i.v. injection of 7mg.
a) 0.2 liters
b) 0.3 liters
c) 0.35 liters
d) 3 liters
e) 3.5 liters
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B
Margin of safety = TD1/ED99
Therapeutic index = TD50/ED50
Drug A was studied in a large group of patients and the percentages of the group
showing a specific therapeutic effect was determined and toxic effect was
determined (see the table below). Calculate the Margin of Safety (Certain Safety
Factor) of drug A.
a) 0.33
b) 1
c) 10
d) 3.3
e) 33
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E. Internalization of receptor proteins
During the first 2 weeks of therapy with a beta 2 adrenoceptor agonist, a 50 year old man with
asthma complains that his inhaler is gradually losing effectiveness. Which
mechanism is most likely responsible for this effect?
a) autoinduction of drug metabolizing enzymes
b) formation of antibodies to the drug
c) exacerbation of his disease
d) depletion of adenosine triphosphate
e) internalization of receptor proteins
C
For drug X, the volume of distribution is normally 35L, and 80% of the drug is bound to plasma
proteins. In patients with hypoalbuminemia, plasma protein binding is reduced to
60%. You now measure the amount of drug in the plasma volume and find:
a) reserpine
b) guanethidine
c) metatyrosine (alpha methylparatyrosine)
d) alpha-methyldopa
e) clonidine
C. Phospholipase C
Eccrine sweat glands have mostly M3 receptors. Muscarinic receptors 1,3,5 are excitatory, and
activate PLC through Gq/11, leading to increases in DAG and IP3, and sometimes PLA2 and
arachidonic acid release. Muscarinic receptors 2 and 4 have Gi/0 subunits that lead to inhibition
of adenylate cyclase and decrease in cAMP.
A one week old infant with failure to thrive was evaluated for aptic fibrosis by collecting sweat
via dermal iontophoresis of a drug that evokes eccrine sweat gland secretion. Which enzyme is
activated during the signaling cascade responsible for stimulating
sweat gland secretion?
a) cholinesterase
b) adenylyl cyclase
c) phospholipase C
d) phosphodiesterase
e) choline acetyl transferase
E. Release of calcium from sarcoplasmic reticulum.
A good way to treat orthostatic hypotension is to increase blood pressure, and a good way to
increase blood pressure is to activate alpha-1 receptors in vasculature in order to raise SVR.
Alpha-1 receptors activate through a Gq/11 subunit to activate PLC, increasing IP3 and DAG,
and increasing intracellular Ca2+.
A 55-year-old woman with diabetic autonomic neuropathy complains of feeling lightheaded and
dizzy whenever she gets out of bed. Examination reveals that has blood
pressure falls abruptly upon arising from the supine position and she is placed on drug therapy
for the condition. Which action is most likely responsible for the therapeutic
effect of the patients drug therapy:
a) clonidine
b) epinephrine
c) isoproterenol
d) phenylephrine
e) dobutamine
B. Timolol. Used to decrease humor flow.
Pilocarpine is a muscarinic agonist which helps with drainage in wide angle glaucoma.
A man is found to have an intraocular pressure of 24 mmHg (normal 10-20) but no evidence of
optic nerve damage. He is placed on an antagonist of G-protein coupled receptor in order to
lower his intraocular pressure. Which drug was most likely used:
a) pilocarpine
b) timolol
c) clonidine
d) isofluorphate (DFP)
e) epinephrine
B.
Most likely he was put on an alpha-1 antagonist such as Tamsulosin. Alpha-1 antagonist can
also decrease vascular tone and thus increase risk for postural hypotension.
A man complains of needing to urinate frequently in the daytime and at night and of difficulty of
maintaining urine outflow during micturation. Examination reveals prostatic enlargement. His
prostate specific antigen (PSA) is normal and he is placed on a drug to relax prostate and
trigone smooth muscle. Which side effects may be likely to result from taking this medication?
a) bradycardia
b) postural hypotension
c) insomnia
d) priapism
e) constipation
C. Tamulosin is a alpha-1 antagonist used in the treatment of BPH, and it also blocks the
receptor responsible for trigone and sphincter contraction.
A man complains of needing to urinate frequently in the daytime and at night and of difficulty of
maintaining urine outflow during micturition. Examination reveals prostatic enlargement. His
prostate specific antigen (PSA) is normal and he is placed on a drug to
relax prostate and trigone smooth muscle. The drug administered to this patient is most likely:
a) tolterodine
b) ipratropium
c) tamulosin
d) atropine
e) propranolol
B. Stomach
Which organ is least important when considering changing pharmacokinetics and normal aging
(that is, not due to disease)?
a) Brain
b) Stomach
c) Liver
d) Kidneys
e) Heart
D. Clonidine, which is an alpha-2 agonist that dampens sympathetic response.
Phentolamine is a alpha blocker that doesn't affect the heart directly, Metoprolol is a
beta1>beta2 blocker, Propanolol is a beta blocker, Phenoxybenzamine is an alpha antagonist.
A woman presents to an afterhours medical clinic with a blood pressure of 178/98 (normal range
120-129/80-89). She has been taking antihypertensive medication but ran out of medicine
several days ago. The physician orders a single dose of a drug that
reduces sympathetic tone to the heart and circulation in order to lower her blood
pressure. The drug prescribed is most likely:
a) phentolamine
b) metoprolol
c) propranolol
d) clonidine
e) phenoxybenzamine
C. Dobutamine is a beta-1 agonist that leads to Gs activation, rise in cAMP. Increases inotropy
and HR, with net effect raise in cardiac contractility and CO. Tends to mildly decreas SVR due
to counterbalancing beta-2 and alpha 1 effects.
DESPITE raise in HR, dobutamine can actually decrease myocardial oxygen demand by raising
inotropy and lowering SVR.
Used in the acute management of decompensated CHF. Arrhythmias and possible
Hypotension?
A 72 year old woman is treated for acute heart failure with an infusion of dobutamine. The
duration of dobutamine infusion should be limited to several hours each day
because prolonged infusion may lead to drug tolerance. The principal receptor being activated
by dobutamine is:
a) α1
b) α2
c) ß1
d) ß2
e) ß3
B
A 29 year old woman with myasthenia gravis is being treated with prednisone and
pyridostigmine. She complains to her physician of increasing diplopia and facial weakness. If an
intravenous dose of edrophonium improves her muscle weakness in this patient indicates:
a) propranolol
b) clonidine
c) prazosin
d) dobutamine
e) phenoxybenzamine
C. Atropine, which is a muscarinic antagonist. Patient's symptoms are due to muscarinic
overactivity, and this would bring it back in line.
a) pyridostigmine
b) propranolol
c) atropine
d) prazosin
e) metoprolol
C. Pindolol.
Pindolol, along with Labetalol, and Celiprolol have what is called partial agonist activity.
A drug is administered to a patient that increases heart rate in the absence of norepinephrine
but blocks norepinephrine induced positive inotropic and chronotropic
effects when the two are present together. It is most likely:
a) nadolol
b) metoprolol
c) pindolol
d) timolol
e) labetalol
C. Prazosin, which is an alpha-1 blocker
Administration of a high dose of epinephrine to a patient produced a paradoxically decrease in
mean arterial pressure. Which of the following drugs may the patient have previously taken to
account for this unexpected effect?
a) cocaine
b) atropine
c) prazosin
d) reserpine
e) propranolol
C. Phase III
Phase I and II are generally smaller. Phase I is to assess safety, bio effects, metabolism,
kinetics, drug itneractions, usually done by clinical pharmacologists (Is it safe?).
Phase II is through selected patients to assess therapeutic efficacy, dose range, kinetics,
metabolism (Does it work?).
Phase III is a large sample used to assess safety, efficcacy, esp. compared to other drugs,
placebos.
Phase IV is post drug approval, postmarket surveillance.
Phase V, doesn't exist.
A drug is being developed that will selectively bind and reverse the effects of skeletal muscle
relaxants. This new medication will not possess the unwanted muscarinic effects of neostigmine
which is currently used for that purpose. The drug appears to be effective. However, in a large
study group/trial prior to the release of the drug on the
market, it was discovered that the medication might produce allergic reactions at an
unacceptable high rate. Release of the drug was held back by the FDA. At what phase
of drug development was this possible allergic side effect discovered?
a) Phase I
b) Phase II
c) Phase III
d) Phase IV
e) Phase V
D
You are administering a drug orally and it has a narrow therapeutic window. You want to
decrease the plasma concentration fluctuations. Which of the following actions would
decrease the fluctuations without altering the average steady state drug level for a person on an
intermittent dose regimen?
a) double the size of the dose and keep dose interval the same
b) double the dose interval and keep the size of the dose the same
c) double the dose interval and the decrease the size of the dose by 1/2
d) decrease the dose interval by 1/2 and decrease the size of the dose by 1/2
e) decrease the dose interval by one half and increase the dose by factor of 2
E. Brain. Highly ionized and quarternary molecular structure is associated with low penetrance
of BBB.
A 14 year old boy is brought by his mother to his primary care physician after development of
fever, nausea, headache and diffuse muscle pain. He has a macular rash that started on his
hands and feet and has spread toward his chest and thighs. His physician prescribes an
antibiotic that has a highly ionized, quaternary molecular structure. Which organ is likely to
exhibit the lowest concentration of this drug:
a) kidney
b ) liver
c) spleen
d) heart
e) brain
B. Oxidation.
Oxidation is rarely a part of phase II reactions. Phase I reactions usually include oxidation,
reduction, and hydrolysis.
a) sulfation
b) oxidation
c) methylation
d) glucuronidation
e) acetylation
E
A 42 year old man with chronic low back pain attributed to a compressed nerve is scheduled to
undergo a lumbar laminectomy in the prone position. Prior to the procedure an anesthesiologist
administers a muscarinic antagonist to reduce the patient's salivation. Which of the following
additional side effects of the medication would be most likely to occur?
a) bradycardia
b) miosis
c) hyperhidrosis
d) diarrhea
e) urinary retention
A. Acetylcholine.
Vasodilation due to muscarinic receptors on peripheral sympathetic nerve terminals that block
the release of NE thus reducing sympathetic vascular tone.
a) acetylcholine
b) epinephrine
c) histamine
d) isoproterenol
e) norepinephrine
E
After ingestion of a massive dose of cocaine an 18 year old man participates in a game of
soccer and suffers a fatal myocardial infarction. What autonomic mechanism was blocked by
cocaine to contribute to cardiac death in this individual?
a) β-adrenergic receptors
b) incorporation of norepinephrine into storage vesicles
c) release of norepinephrine from sympathetic nerve terminals
d) synthesis of norepinephrine in sympathetic nerves
e) uptake of catecholamines into sympathetic nerve terminals
E. Propranolol
In experiments when anesthetized subjects are treated intravenously with an agonist (drug X)
they have an increase in their blood glucose and in the force ventricular contraction, and a
decrease in peripheral resistance. Pretreatment of the subjects with
an antagonist (drug Y) almost completely blocks all of these effects.
a) terbutaline
b) atropine
c) guanethidine
d) phentolamine
e) propranolol
C. Isoproterenol, which is a beta agonist
In experiments when anesthetized subjects are treated intravenously with an agonist (drug X)
they have an increase in their blood glucose and in the force ventricular contraction, and a
decrease in peripheral resistance. Pretreatment of the subjects with an antagonist (drug Y)
almost completely blocks all of these effects.
Drug X is:
a) terbutaline
b) epinephrine
c) isoproterenol
d) bethanechol
e) phenylephrine
B. Bethanechol is a muscarinic agonist, muscarinic receptors --> bronchoconstriction. Timolol
will also cause bronchoconstriction but through inhibition of beta-2 receptors that cause
bronchodilation.
Atropine is a muscarinic antagonist, isoproterenol is a beta-1,2 agonist, and phentolaine is an
alpha blocker. These would either shift to bronchodilation or have little effect.
A 35-year old woman has severe bronchial asthma. What agent would most likely cause a
severe bronchospasm reaction in this patient?
a) atropine
b) bethanechol
c) timolol
d) isoproterenol
e) phentolamine
E. Norepinephrine
In experimental studies when anesthetized subjects are treated intravenously with drug X, they
show a marked increase in both diastolic and systolic blood pressure and a
slowing of the heart rate. However, if they are pretreated with prazosin, they show a modest
increase in the systolic blood pressure and heart rate. What agent is drug X?
a) acetylcholine
b) epinephrine
c) histamine
d) isoproterenol
e) norepinephrine
A. Albuterol, which is a beta-2 agonist.
A 13 year-old girl has severe, frequently recurring asthmatic attacks. During the attacks, she
becomes cyanotic, dyspneic and agitated. What drug is expected to provide immediate relief
with the fewest adverse effects in controlling asthmatic attacks in this patient?
a) albuterol
b) atropine
c) ephedrine
d) epinephrine
e) phenylephrine
C. Phenylephrine is an alpha-1 agonist. Mydriasis is controlled by alpha-1 receptors in iris.
There would be cardiac deceleration because alpha-1 receptors would increase BP.
a) sedation
b) rapid heart rate
c) muscle weakness
d) high blood pressure
e) blurred vision
A
After being stung by a bee, a woman experiences urticaria, laryngeal edema, difficulty breathing
and hypotension. She receives oxygen and the administration of an adrenergic agonist. Which
action would lead to bronchodilation?
a) ipratropium
b) succinylcholine
c) vecuronium
d) scopolamine
e) d-tubocurarine
A (because it is metabolized to an active metabolite)
A patient is on "Drug A" which is a type of blood thinner used to "keep his stents in his coronary
arteries open." Drug A is a substrate of the CYP450 enzyme 2C19, and it is metabolized to an
active metabolite. The patient decides to take a second drug, "Drug B" for acid reflux. Drug B is
an inhibitor of 2C19. What will be the potential clinical consequence of this patient taking Drug
B?
a) a non-competitive antagonist
b) a irreversible partial agonist
c) a partial agonist
d) a chemical antagonist
e) a physiologic antagonist
a) prolonged occupation of nicotinic receptors by acetylcholine
A 27-year old woman being treated with pyridostigmine complains of blurred double vision and
facial drooping 2 weeks after her last appointment with her doctor. After injection of a diagnostic
agent intravenously, her grip strength declines rapidly. Which
mechanism is most likely responsible for this loss of muscle tone?
a) elimination of the drug does not change as the plasma concentration increases
b) elimination of the drug increases as plasma concentration increases
c) the half-life of the drug increases as the plasma concentration increases
d) the drug will reach steady state faster than 5 half-lives
e) clearance of the drug increases as the plasma concentration increases
E
You, the physician, are taking care of a 74 year old woman. She is taking 3 medicines for her
high blood pressure, 2 medicines for her arthritis, 1 medicine for her insomnia, 2 medicines for
her diabetes, 2 laxatives, and 1 bladder medicine. What is the best thing
you can do to decrease her risk of adverse drug events (ADEs)?
Ipratropium is also a muscarinic antagonist, but it is poorly absorbed, and usually just inhaled to
treat COPD and asthma.
a) atropine
b) tolterodine
c) ipratropium
d) neostigmine
e) bethanechol
C
The diagram above shows concentration response curves of drug A, in the presence of
increasing concentrations of an interacting drug X. Curve A is drug A alone, curves B - E are in
the presence of increasing concentrations of drug X. From the data it can be deduced that:
Cl = k(e) * Vd
with k(e) = 0.7/t(1/2).
Dm = (Css Cl Tm)/F
Cl = Vd*Ke = 4.6 L/hr
Vd = 2 L/kg * 80 kg = 160 L
Ke = 0.7 / t(1/2)
Dm = (10004.6/0.7)Tm
And the way it comes out is 80mg/12hours
Your patient has been diagnosed with a urinary tract infection and needs to be given a dosing
regimen of an antibiotic. Calculate a suitable dosage regimen for an 80 kg patient
who is to be given an oral fluoroquinolone. The therapeutic plasma concentration of the drug is
1.0μg/ml. The volume of distribution for this drug is 2 liters/kg and the half-life is 24 hours. The
oral bioavailability is 70%.
Dl = (Vd * Css)/F
Dl = (20 L * 30mg/L)
Dl = 600 mg
The therapeutic range of a drug is 20-40mg/liter. The half-life of the drug is 2days,
clearance is 7liters/day and the volume of distribution is equal to 20liters. Calculate the
loading dose that is required to attain the therapeutic concentration.
a) 20mg
b) 200mg
c) 600mg
d) 800mg
e) 1600mg
D
You have just developed a new agonist, drug X, for a nicotinic ion channel. You plot the effects
of several drugs including drug X. In the graph below, curve X represents a concentration-
response of drug X, which is a full agonist (Emax= 100%). In comparison
to curve X, which curve represents the concentration-response of drug X in the presence
of a competitive reversible antagonist?
a) Curve A
b) Curve B
c) Curve C
d) Curve D
e) Curve X
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D
A pharmaceutical company has developed a new antagonist against beta 1 adrenergic
receptors. You administer the antagonist and observe a decreased in the activation of Gs. You
would expect to observe:
a) increase in calcium
b) increase in inositol triphosphate
c) increase in DAG
d) decrease in cAMP
e) decrease in inositol triphosphate
A) less than 1%
Drug A is a base with a pK of 9.0. The drug is eliminated by the kidneys exclusively via passive
diffusion. The pH of the plasma is 7. Calculate the % of drug in the plasma that is unionized.
a) less than 1%
b) less than 5% but greater than 1%
c) less than 10% but greater than 5%
d) less than 20% but greater than 10%
e) exactly 1%
E. Cocaine.
Cocaine is a NE uptake inhibitor, that will potentiate NE response because that is how it is
inactivated. Tyramine, however, is a catecholamine releasing agent. Cocaine would deplete
intracellular NE stores, thus reducing the effect of Tyramine.
a) metoprolol
b) nadolol
c) carvedilol
d) methyldopa
e) cocaine
E
Dm = (Cl Css Tm)/F
Your patient has been given a loading dose to achieve a therapeutic concentration of 10mg/liter.
Clearance of the drug is 1liter/8hours and the bioavailability of the drug is 0.5.
You have prescribed an oral preparation of the drug. Calculate the maintenance dose
that the patient will take to maintain the therapeutic concentration.
a) 20mg twice a day
b) 20mg three times a day
c) 40mg once a day
d) 40mg twice a day
e) 40mg three times a day
D
70% is absorbed, but 40% of the absorbed is metabolized, leaving 60% of what is absorbed to
be bioavailable. F = .7*.6 = .42
The drug you are administering to your patient is taken orally. The drug is 70% absorbed in the
gut, and 40% is metabolized in the liver. The bioavailability of the drug is:
a) 0.12
b) 0.18
c) 0.28
d) 0.42
e) 0.7
69. E
70. A
71. B
72.
69. A woman experiences pain and ischemia in her finger after accidently injecting it with an
auto-injector that she carries for emergency treatment of allergic reactions
70. A man complains of urinary urgency, frequency and nocturia and is found to have
enlargement of the prostate gland
71. A woman with essential hypertension requires a drug that reduces both cardiac output
and peripheral resistance.
72. A man with episodic severe hypertension is found to have markedly elevated
epinephrine and norepinephrine metabolites in his urine and requires a long-acting drug
to lower blood pressure before surgery.
C. 50 liters
Vd = dose/Cp(0)
As the leader of the project testing a new drug, drug A you have carried out several test for the
new drug. You administer i.v.10 mg of drug A and get the graph shown below for the plasma
concentration vs time after drug administration.