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Leonila A.

Estole-Casanova, MD

Associate Professor 2
Department of Pharmacology and Toxicology
May 25, 2010

Each of you has a STUDY & REVIEW


METHOD that has worked best for you

GO with WHAT WORKS BEST!

Prepare yourself
Review from your notes and favorite
text

It is unnecessary to memorize many of


these facts if one learns to predict the
behavior of each drug based on a few
facts and an understanding of the
PRINCIPLES OF
PHARMACOLOGY
If you can predict the actions, clinical uses,
side effects and drug interactions of each
drug based solely on its mechanism of
action, you will only have to memorize
those facts that do not make sense

Be able to IDENTIFY main drug classes


and cite a prototype for each or be able
to work backward
ex. non-selective cyclooxygenase inhibitors
prototype drug: aspirin
for fever, inflammation and pain
propranolol
prototype non-selective - adrenergic
blocker*
for hypertension, tachycardia, etc

Be able to RECOGNIZE the most common,


most important (e.g., serious or life
threatening) or unique side effects or
adverse responses for the main drugs or
drug classes
ex. most anti-HPN drugs hypotension
aminoglycoside antibiotics ototoxicity
hydralazine lupus-like syndrome

Be able to LEARN & RECOGNIZE the intended


effects that will give you a good idea re:
precautions or contraindications
ex.- adrenergic blocker

heart rate or contractility


contraindicated: bradycardia
heart block

PRAY .
PRAY .
PRAY .

Leonila A. Estole-Casanova, MD

Associate Professor 2
Department of Pharmacology and Toxicology
May 25, 2010

processes of absorption, distribution,


metabolism and elimination
what the Body does to the drug

mechanisms of action

what the

Drug Does to the body

Molecular
/ Cellular
level

Organism

Receptors
Affinity
Dissociation
constant (Kd)

Efficacy (Emax) Therapeutic


Window
Potency
ED50
TD50
Graded-dose Therapeutic
response
Index
curve
Quantal
concentration
-effect curve

Agonist,
antagonist

Population

1.If you want to achieve a


concentration of 5 ug/ml, how much
drug must be given via intravenous
bolus? The volume of distribution is
50 liters:
a.10mg
b.10ug
c.250 mg
d.250 ug

A quantitative estimate of the tissue


localization of the drug
Can be determined by measuring the
plasma level of the drug
total amount of drug in body (D)

Vd = concentration of drug in plasma (C)


Vd = D/ C

1.If you want to achieve a


concentration of 5 ug/ml, how much
drug must be given via intravenous
bolus? The volume of distribution is
50 liters:
a.10mg
b.10ug
c.250 mg
d.250 ug

Vd = D / C
D = C (Vd)

= 5ug/ml (50,000ml)
= 250,000ug or
250mg

1.If you want to achieve a


concentration of 5 ug/ml, how much
drug must be given via intravenous
bolus? The volume of distribution is
50 liters:
a.10mg
b.10ug
c.250 mg
d.250 ug

87.A patient presents to the emergency


room with acute bronchial asthma. The
treating physician decides to administer
a loading dose of Theophylline.
Knowledge of which of the following
parameters is needed for proper
dosing?
a. elimination half-life
b. volume of distribution
c. elimination clearance
d. creatinineclearance

Initial dose of drug administered in


order to compensate for drug
distribution into the tissues.
may be much higher than would be
required if the drug were retained in the
intravascular compartment.
may be used to achieve therapeutic
levels of drug (i.e. levels at the desired
steady state concentration) with only
one or two doses of drug

Loading dose = VdxCsteady state


Vd volume of distribution
Csteadystate - the desired steady state plasma
concentration of the drug

87.A patient presents to the emergency


room with acute bronchial asthma. The
treating physician decides to administer
a loading dose of Theophylline.
Knowledge of which of the following
parameters is needed for proper
dosing?
a. elimination half-life
b. volume of distribution
c. elimination clearance
d. creatinineclearance

2.The process by which the amount of


orally-administered drug is reduced
before it reaches the systemic
circulation
a. First-order kinetics
b. First-pass effect
c. Pharmacokinetics
d. Excretion
e. Metabolism

2.The process by which the amount of


orally-administered drug is reduced
before it reaches the systemic
circulation
a. First-order kinetics
b. First-pass effect
c. Pharmacokinetics
d. Excretion
e. Metabolism

FIRST-ORDER
rate is directly
proportional to the
concentration of
free drug
constant
FRACTION of drug
is metabolized per
unit time
linear kinetics
half-life is
constant

ZERO-ORDER
rate remains
constant over
time, e.g. ASA ,
Ethanol,
Phenytoin
constant
AMOUNT of drug
is metabolized per
unit time
non-linear
kinetics
half-life increases
with dose

12. The kinetics characteristic of


elimination of ethanol and high doses
of phenytoin and aspirin is known as
a. Distribution
b. Excretion
c. First-pass effect
d. First-order elimination
e. Zero-order elimination

12. The kinetics characteristic of


elimination of ethanol and high doses
of phenytoin and aspirin is known as
a. Distribution
b. Excretion
c. First-pass effect
d. First-order elimination
e. Zero-order elimination

13. If the plasma concentration of a


drug declines with first order
kinetics, this means that:
a. The half-life is the same regardless of
plasma concentration
b. The drug is largely metabolized in the
liver after oral administration and has low
bioavailability
c. The rate of elimination is proportionate to
the rate of administration at all times
d. The drug is not distributed outside the
vascular system

13. If the plasma concentration of a


drug declines with first order
kinetics, this means that:
a. The half-life is the same regardless
of plasma concentration
b. The drug is largely metabolized in the
liver after oral administration and has low
bioavailability
c. The rate of elimination is proportionate to
the rate of administration at all times
d. The drug is not distributed outside the
vascular system

PHASE I
t functions to
convert lipophilic
materials into
more polar
molecules

PHASE II
t
consists of
conjugation
reactions that
result in polar,
usually water
soluble
compounds that
are
therapeutically
inactive

PHASE I
P450-dependent
oxidations
P450
independent
oxidations (alcohol
or aldehyde
dehydrogenation
deamination,
decarboxylation)

Hydrolysis
Reductions

PHASE II
glucuronidation
acetylation
glycine conj.
sulfate conj.
glutathione conj
N- or Omethylation

Not

all drugs undergo Phase I and


Phase II reactions in that order.

For

example, isoniazid is first


acetylated (a phase II reaction) and
then hydrolyzed to isonicotinicacid (a
phase II reaction)

11. Which of the following is NOT a


Phase II reaction of drug metabolism
a. Deamination
b. Acetylation
c. Glucuronidation
d. Methylation
e. Sulfate conjugation

11. Which of the following is NOT a


Phase II reaction of drug metabolism
a. Deamination
b. Acetylation
c. Glucuronidation
d. Methylation
e. Sulfate conjugation

84.The rate of acetylation is important


with respect to the duration of action
of:
a. atropine
b. cocaine
c. isoniazid
d. acetaminophen

84.The rate of acetylation is important


with respect to the duration of action
of:
a. atropine
b. cocaine
c. isoniazid
d. acetaminophen

drugs induce
P450

Increased rate of
metabolism

drugs inhibit P450

potentiate the
actions of other
drugs

Phenytoin

omeprazole

carbamazepine

barbiturates
rifampicin
ritonavir
griseofulvin
chronic ethanol
toxicity

DISULFIRAM
erythromycin
valproic acid
isoniazid
cimetidine
ciprofloxacin
acute ethanol
toxicity

14.The drug interaction of alcohol and


disulfiram would be an example of
which of the following?
a.Induction of metabolizing enzymes
b.Displacement from serum albumin
c.Inhibition of metabolizing enzyme
d.Inhibition of uptake into adrenergic
neuron

14.The drug interaction of alcohol and


disulfiram would be an example of
which of the following?
a.Induction of metabolizing enzymes
b.Displacement from serum albumin
c.Inhibition of metabolizing enzyme
d.Inhibition of uptake into adrenergic
neuron

86.The expected effect of toxic


hepatitis on the rate of drug
metabolism by the liver:
a. Increased
b. Decreased
c.Unchanged
d.Changed from a Type I to Type II process

86.The expected effect of toxic


hepatitis on the rate of drug
metabolism by the liver:
a.Increased
b.Decreased
c.Unchanged
d.Changed from a Type I to Type II process

3. If a drug is repeatedly administered at


dosing intervals equal to its elimination
half-life, the number of doses required
for the plasma concentration of the
drug to reach the steady state is:
a. 2 to 3
b. 4 to 5
c. 6 to 7
d. 8 to 9
e. 10 or more

input (rate of infusion) = output (rate of


elimination)

3. If a drug is repeatedly administered at


dosing intervals equal to its elimination
half-life, the number of doses required
for the plasma concentration of the
drug to reach the steady state is:
a. 2 to 3
b. 4 to 5
c. 6 to 7
d. 8 to 9
e. 10 or more

5.The dose or concentration required


to bring about 50% of a drugs
maximal effect
a. Potency
b. ED50
c. Efficacy
d. Kd
e. Therapeutic index

Molecular
/ Cellular
level

Organism

Receptors
Affinity
Dissociation
constant (Kd)

Efficacy (Emax) Therapeutic


Window
Potency
ED50
TD50
Graded-dose Therapeutic
response
Index
curve
Quantal
concentration
-effect curve

Agonist,
antagonist

Population

Kd
A

measure of a drugs affinity for a


given receptor
The concentration of drug required in
solution to achieve 50% occupancy of
its receptors

Molecular
/ Cellular
level

Organism

Receptors
Affinity
Dissociation
constant (Kd)

Efficacy (Emax) Therapeutic


Window
Potency
ED50
TD50
Graded-dose Therapeutic
response
Index
curve
Quantal
concentration
-effect curve

Agonist,
antagonist

Population

Emax

maximal
response
produced by the
drug

Refers

to the
concentration
(EC50) or dose
(ED50) of a drug
required to
produce 50% of
the drugs
maximal effect

Molecular
/ Cellular
level

Organism

Receptors
Affinity
Dissociation
constant (Kd)

Efficacy (Emax) Therapeutic


Window
Potency
ED50
TD50
Graded-dose Therapeutic
response
Index
curve
Quantal
concentration
-effect curve

Agonist,
antagonist

Population

the range of doses of a drug


that elicits a therapeutic
response, WITHOUT
unacceptable side effects
(toxicity), in a population of
patients
quantified by the

THERAPEUTIC INDEX (TI) or


THERAPEUTIC RATIO

Single number that quantifies the relative


margin of safety of a drug in a population of
people
Ratio of the TD50 to the ED50
Median toxic /lethal dose TD50 (LD50)- the
dose of a drug required to produce a toxic/lethal
effect in 50% of the population
Median effective dose (ED50) the dose of a
drug that is therapeutically effective in 50% of
the population

5.The dose or concentration required


to bring about 50% of a drugs
maximal effect
a. Potency
b. ED50
c. Efficacy
d. Kd
e. Therapeutic index

6. The maximum effect of the drug


may be produced even if not all
receptors are bound in the presence
of which of the following:
a. Full agonist
b. Partial agonist
c. Spare receptors
d. Inert binding site

e. Effector

The receptor theory assumes that all


receptors should be occupied to produce
a maximal response. In that case at half
maximal effect EC50= Kd.

Sometimes,

maximal response is seen at


a fractional receptor occupation
allow maximal response without total
receptor occupancy increase sensitivity
of the system
EC50<Kd

albumin, alpha1-acid glycoprotein


binds drugs without initiating events leading
to drug effect)

translate drug-receptor interaction to


change in cellular activity, e.g.
adenylylcyclase; may be part of the
receptor itself. e.g. Na-K channel part of
the nicotinic Ach receptor)

Drugs that interact with and activate


receptors
Drugs that possess BOTH affinity and
efficacy
Full an agonist with maximal efficacy
Partial an agonist with less then
maximal efficacy even when all the
receptors are occupied by the partial
agonist

6. The maximum effect of the drug


may be produced even if not all
receptors are bound in the presence
of which of the following:
a. Full agonist
b. Partial agonist
c. Spare receptors
d. Inert binding site

e. Effector

4.Two drugs act on the same tissue or


organ via activation of different
receptors in effects that are
qualitatively the opposite of one
another. This represents which of the
following types of antagonism?
a. Physiologic
b. Competitive
c. Irreversible antagonist
d. Chemical antagonist

Antagonists interact with the receptor


but do NOT change the receptor
they have affinity but NOefficacy

receptor vs non-receptor antagonists


receptor antagonists:
competitive vs non-competitive
non-receptor antagonists:
chemical vs physiologic

Competes with
agonist for receptor
Surmountable with
increasing agonist
concentration
Agonist affinity is
lower because a
higher dose of
agonist is required,
in the presence of
antagonist, to
achieve receptor
occupancy
Ex: Propranolol

drug binds to
receptor and
stays bound
irreversible does
not let go of
receptor
ex.
Phenoxybenzamin
e
t

inactivate an agonist
before it has the
opportunity to act
Ex Protamine (+)
charged is used to
counteract the effects
of HEPARIN, (-)
charged
acts by IONIC binding
to make heparin
unavailable for
interactions with
proteins involved in
blood clotting

Cause a
physiologic effect
opposite to that
induced by the
agonist
t

Ex. glucocorticoid
increases blood
sugar
insulin decreases
blood sugar

4.Two drugs act on the same tissue or


organ via activation of different
receptors in effects that are
qualitatively the opposite of one
another. This represents which of the
following types of antagonism?
a. Physiologic
b. Competitive
c. Irreversible antagonist
d. Chemical antagonist

4.Two drugs act on the same tissue or


organ via activation of different
receptors in effects that are
qualitatively the opposite of one
another. This represents which of the
following types of antagonism?
a. Physiologic
b. Competitive
c. Irreversible antagonist
d. Chemical antagonist

7.The pharmacokinetic value that most


reliably reflects the amount of drug
reaching the target tissue after oral
administration is the
a. Peak blood concentration
b. Time to peak blood concentration
c. Product of the volume of distribution and
the first-order rate constant
d. Volume of distribution
e. Area under the blood concentration-time
curve

a. Peak blood concentration (Cmax) rate of


absorption
b. Time to peak blood concentration (Tmax)
rate of absorption
c. Product of the volume of distribution and
the first-order rate constant
d. Volume of distribution (Vd) = (dose/plasma
concentration)

e. Area under the blood concentration-time


curve (AUC) - extent of absorption

7.The pharmacokinetic value that most


reliably reflects the amount of drug
reaching the target tissue after oral
administration is the
a. Peak blood concentration
b. Time to peak blood concentration
c. Product of the volume of distribution and
the first-order rate constant
d. Volume of distribution
e. Area under the blood concentrationtime curve

8.Which of the following terms is best


described as a rapid reduction in the
effect of a given dose of a drug after
only one or two doses
a. Supersensitivity
b. Tachyphylaxis
c. Tolerance
d. Anaphylaxis
e. Synergism

a. Supersensitivity frequently follows chronic


reduction of receptor stimulation

b. Tachyphylaxis repeated administration of the


same dose of a drug results in a reduced effect of
the drug over time

c. Tolerance drug loses its effectiveness and an


increased dose is necessary to produce same
response

d. Anaphylaxis - immediate hypersensitivity which


is antibody mediated

e. Synergism 1+1 > 2


additive 1 +1 = 2 ; potentiation 0 +1 >1

8.Which of the following terms is best


described as a rapid reduction in the
effect of a given dose of a drug after
only one or two doses
a. Supersensitivity
b. Tachyphylaxis
c. Tolerance
d. Anaphylaxis
e. Synergism

100.The interaction between an


acetylcholinesterase inhibitor and
acetylcholine at the neuromuscular
junction would be an example of:
a.Addition
b.Potentiation
c.Competitive antagonism
d.Non-competitive antagonism

100.The interaction between an


acetylcholinesterase inhibitor and
acetylcholine at the neuromuscular
junction would be an example of:
a.Addition
b.Potentiation
c.Competitive antagonism
d.Non-competitive antagonism

9. Aspirin is a weak organic acid with a


pKaof 3.5. What percentage of a
given dose will be in the lipid soluble
form at a stomach pH of 2.5?
a. About 1%
b. About 10%
c. About 50%
d. About 90%
e. About 99%

About

90%- a weak acid is


protonated when ph<pKa;
protonated weak acid is in its
non-ionized form and lipid
soluble.
Henderson-Hasselbalch equation=
log(protonated/unprotonated)=pKapH
= 1; antilog 1= 10/1; protonated
10/11

Aspirin is a weak acid with a pKaof 3.5


stomach pH of 2.5?
Aspirin is a weak acid and is protonated
when ph<pKa (2.5 < 3.5)
protonatedweak acid is in its non-ionized
form and lipid soluble

Henderson-Hasselbalch equation
pKaspirin = pHstomach + log HA (protonated)
A(deprotonated)

Henderson-Hasselbalch equation
pKaspirin = pHstomach + log HA
A3.5 2.5 = log HA / A1 = log HA / Aantilog of 1 = HA / A10 = HA /AProtonated = 10 / 11 = 90%

9. Aspirin is a weak organic acid with a


pKaof 3.5. What percentage of a
given dose will be in the lipid soluble
form at a stomach pH of 2.5?
a. About 1%
b. About 10%
c. About 50%
d. About 90%
e. About 99%

85.A weak organic acid (pK=3) would


be least ionized in:
a. the small intestine
b. pulmonary alveoli
c. the stomach
d. arterial blood

85.A weak organic acid (pK=3) would


be least ionized in:
a.the small intestine
b.pulmonary alveoli
c.the stomach
d.arterial blood

10. Given a drug with a volume of


distribution of 80 L and clearance of
1.386 L/h, the half-life is
approximately
a. 0.02 h
b. 40 h
c. 58 h
d. 80 h
e. 111 h

defined as
the amount of
time required
for the drug
concentration
to decrease
by 50%

the pharmacokinetic parameter that


most significantly limits the time
course of action of the drug

the volume of plasma from which all


drug appears to be removed in a
given time

a decrease in clerance tends to


prolong the half-life and enhance the
effect of the drug on the target organ

volume of distribution of 80 L
clearance of 1.386 L/h
?? the half-life

t1/2 = 0.693 xVd


clearance
= 0.693 (80L)
1.386 L / h
= 40 h

10. Given a drug with a volume of


distribution of 80 L and clearance of
1.386 L/h, the half-life is
approximately
a. 0.02 h
b. 40 h
c. 58 h
d. 80 h
e. 111 h

15.Which of the following is


therapeutic action of beta adrenergic
receptor blockers in the treatment of
angina pectoris?
a. Dilatation of coronary arteries
b. Decrease in the amount of
catecholamines
c. Decrease in requirement of the
myocardium for oxygen
d. Increase in the sensitivity to
catecholamines

15.Which of the following is therapeutic


action of beta adrenergic receptor
blockers in the treatment of angina
pectoris?
a. Dilatation of coronary arteries
(nitroglycerin)
b. Decrease in the amount of catecholamines
c. Decrease in requirement of the myocardium
for oxygen
d. Increase in the sensitivity to
catecholamines

15.Which of the following is


therapeutic action of beta adrenergic
receptor blockers in the treatment of
angina pectoris?
a. Dilatation of coronary arteries
b. Decrease in the amount of
catecholamines
c. Decrease in requirement of the
myocardium for oxygen
d. Increase in the sensitivity to
catecholamines

16.Which of the following drugs should


be used with extra caution in the
treatment of hypertension in a
diabetic patient?
a. Hydralazine
b. Guanethidine
c. Propranolol -d. Methyldopa

16.Which of the following drugs should


be used with extra caution in the
treatment of hypertension in a
diabetic patient?
a. Hydralazine
b. Guanethidine
c. Propranolol non-selective B
Blocker decreased secretion of
insulin -- diabetes
d. Methyldopa

17.Which of the following is reduced by


the action of sulfonylurea
hypoglycemic agents?
a. glycogen secretion
b. insulin secretion
c. tissue sensitivity to insulin
d. tissue sensitivity to glycogen

17.Which of the following is reduced by


the action of sulfonylurea
hypoglycemic agents?
a. glycogen secretion
b. insulin secretion
c. tissue sensitivity to insulin
d. tissue sensitivity to glycogen

18.Which of the following is a tricyclic


antidepressant that has a high
anticholinergic activity, is sedating
and is biotransformed to a longacting active product?
a.Clozapine
b.Amitriptyline
c.Nortriptyline
d.Trazodone

18.Which of the following is a tricyclic


antidepressant that has a high anticholinergic activity, is sedating and is
biotransformed to a long-acting
active product?
a.Clozapine (antipsychotics)
b.Amitriptyline (TCA)
c.Nortriptyline (TCA)
d.Trazodone (MAO inhibitor)

Antichol
Sedating
b.Amitriptyline (TCA)
+3
c.Nortriptyline (TCA)

+3

+1

+1

18.Which of the following is a tricyclic


antidepressant that has a high
anticholinergic activity, is sedating
and is biotransformed to a longacting active product?
a.Clozapine
b.Amitriptyline
c.Nortriptyline
d.Trazodone

19.Which of the following has the


lowest incidence of extrapyramidal
reactions, but has the highest
incidence of agranulocytosis among
antipsychotic agents?
a.Fluphenazine
b.Pimozide
c.Clozapine
d.Molindone

19.Which of the following has the


lowest incidence of extrapyramidal
reactions, but has the highest
incidence of agranulocytosis among
antipsychotic agents?
a.Fluphenazine (more EPS)
b.Pimozide (more EPS)
c.Clozapine(very few EPS, agranulocytosis
in 2%)
d.Molindone (few EPS)

20. Which of the following drugs


inhibits cyclooxygenaseirreversibly?
a. Aspirin
b. Ibuprofen
c. Prednisone
d. Indomethacin
e. Zileuton

Aspirin ONLY irreversible inhibitor of COX 1 and COX 2


Ibuprofen reversible inhibitor of COX 1 and COX 2
Prednisone- inhibits PhospholipaseA2
Indomethacin - reversible inhibitor of COX 1 and COX 2
Zileuton- inhibits lipoxygenase (LOX inhibitor)
Zafrilukast-/montelukast- inhibitors of LTD4; leukotriene
antagonist
celecoxib/rofecoxib - COX-2 selective inhibitors

20. Which of the following drugs


inhibits cyclooxygenase irreversibly
a. Aspirin
b. Ibuprofen
c. Prednisone
d. Indomethacin
e. Zileuton

21. Corticosteroids are usually


indicated in the following conditions
EXCEPT:
a. Herpes simplex of the eye
b. Status asthmaticus
c. Severe allergic rhinitis
d. Nephrotic syndrome
e. Adrenal insufficiency

21. Corticosteroids are usually


indicated in the following conditions
EXCEPT:
a. Herpes simplex of the eye
(infection)
b. Status asthmaticus
c. Severe allergic rhinitis
d. Nephrotic syndrome
e. Adrenal insufficiency

22.Which of the following characterizes


local anesthetics ?
a.They generally block myelinated before
unmyelinated fibers
b.They are generally administered along
with epinephrine to prolong its action
c.The primary action is on calcium
permeability
d.Do not readily cross the blood-brain
barrier

Primary mechanism of action:


BLOCKADE OF VOLTAGE-GATED
SODIUM CHANNELS
Vasoconstrictor

substances such as
epinephrine reduce systemic absorption
of LA from the injection site by
decreasing the blood flow in these areas

Block conduction in the following order:


small myelinated axons, nonmyelinated axons, large myelinated
axons
Unwanted

effects result mainly from


ESCAPE of LAs INTO the systemic
circulation Main unwanted effects:
CNS & CVS

22.Which of the following characterizes


local anesthetics
a.They generally block myelinated before
unmyelinatedfibers
b.They are generally administered along
with epinephrine to prolong its action
c.The primary action is on calcium permeability

d.Do not readily cross the blood-brain barrier

23. Which of the following is commonly


used to treat both absence and
generalized tonic-clonic seizures?
a. Phenytoin
b. Valproate
c. Carbamazepine
d. Clonazepam
e. Phenobarbital

23. Which of the following is commonly


used to treat both absence and
generalized tonic-clonic seizures?
a. Phenytoin (partial, tonic-clonic)
b. Valproate (partial, tonic clonic,
ABSENCE)
c. Carbamazepine (partial, tonic-clonic)
d. Clonazepam (partial, absence)
e. Phenobarbital (partial, tonic-clonic)

24.Which of the following is the mechanism


of action of effective anti-psychotic
agents?
a. Decreases acetylcholine in the CNS
b. Blocks dopamine receptor sites in the CNS
c. Makes acetylcholine more available in the CNS
d. Facilitates the use of norepinephrine in the
CNS
e. Makes dopamine more available in the CNS

Typical antipsychotics
dopamine 2 receptor antagonists
ex. Haloperidol
Chlorpromazine
Atypical antipsychotics
Dopamine 2 receptor antagonists
serotonin 5-HT receptor antagonists
ex. Clozapine

24.Which of the following is the mechanism


of action of effective anti-psychotic
agents
a. Decreases acetylcholine in the CNS
b. Blocks dopamine receptor sites in the
CNS
c. Makes acetylcholine more available in the CNS
d. Facilitates the use of norepinephrine in the
CNS
e. Makes dopamine more available in the CNS

25.Which of the following drugs can


cause Stevens-Johnson syndrome,
megaloblasticanemia, ataxia, and
gingival hyperplasia?
a. Phenobarbital
b. Disulfiram
c. Phenytoin
d. Valproic acid
e. Carbamazepine

25.Which of the following drugs can cause


Stevens-Johnson syndrome, megaloblastic
anemia, ataxia, and gingival hyperplasia?
a.Phenobarbital sedation, enzyme induction,
tolerance, dependence
b. Disulfiram- inhibits alcohol dehydrogenase;
flushing from acetaldehyde with ethanol intake
c.Phenytoin- teratogenic
d.Valproic acid- GI distress, hepatotoxicity (rare but
possible fatal), enzyme inhibition, teratogenic
e.Carbamazepine- diplopia, ataxia, enzyme
induction, blood dyscrasia

25.Which of the following drugs can


cause Stevens-Johnson syndrome,
megaloblasticanemia, ataxia, and
gingival hyperplasia?
a. Phenobarbital
b. Disulfiram
c. Phenytoin
d. Valproic acid
e. Carbamazepine

26.A pure opioid antagonist with a


greater affinity for receptors and
used for acute opioid overdose
a. Morphine
b. Naloxone
c. Codeine
d. Dextromethorpan
e. Diphenoxylate

26.A pure opioid antagonist with a


greater affinity for receptors and
used for acute opioid overdose
a. Morphine strong opiod agonist
b. Naloxone (antagonist)
c. Codeine moderate opioid agonist
d. Dextromethorpan NMDA receptor
blocker
e. Diphenoxylate u receptor agonist
(lomotil)

27. A patient with overdose toxicity of


MDMA or ecstasy is UNLIKELY to
manifest which of the following
symptoms
a. Agitation
b. Hyperthermia
c. Hyperreflexia
d. Bradycardia
e. Seizures

mehylenedioxymetamphetamine- facilitate
interpersonal communication and act as
sexual enhancer)
Congener of amphetamine: Promotes the
release of NE from nerve endings; blocks the
reuptake of norepinephrine
acute effects: feelings of high energy,
altered sense of time and pleasant sensory
experiences
side (negative) effects: tachycardia, dry
mouth
higher doses: visual hallucinations, agitation,
hyperthermia, panic attacks

27. A patient with overdose toxicity of


MDMA or ecstasy is UNLIKELY to
manifest which of the following
symptoms
a. Agitation
b. Hyperthermia
c. Hyperreflexia
d. Bradycardia (tachycardia)
e. Seizures

28. A patient who underwent percutaneous


coronary angioplasty with placement of a
stent in a coronary vessel was started on
clopidogrel. This drug exerts its
antithrombotic effect through which of
the following mechanisms
a. Irreversible inhibition of ADP receptor
b. Inhibition of thromboxane synthesis
c. Reversible blockade of glycoprotein IIb/IIIa
d. Conversion of plasminogen to plasmin
e. Posttranslational modification of vitamin Kdependent clotting factors

Irreversible inhibition of ADP receptor also


ticlopidine
Inhibition of thromboxane synthesis Reversible blockade of glycoprotein IIb/IIIa
abciximab, tirofiban, eptifabitide
Conversion of plasminogen to plasminthrombolytic agents (t-PA- alteptelase,
reteplase;urokinase, streptokinase)
Posttranslational modification of vitamin Kdependent clotting factors- warfarin
Inhibitors of phosphodiesterase 3
dipyridamole, cilostazol (increased CAMP
inhibits platelet aggregation)

Irreversible inhibition of ADP receptor also


ticlopidine
Inhibition of thromboxane synthesis- NSAIDs
Reversible blockade of glycoprotein IIb/IIIa
abciximab, tirofiban, eptifabitide
Conversion of plasminogen to plasminthrombolytic agents (t-PA- alteptelase,
reteplase;urokinase, streptokinase)
Posttranslational modification of vitamin Kdependent clotting factors- warfarin
inhibitors of phosphodiesterase 3
dipyridamole, cilostazol (increased CAMP
inhibits platelet aggregation)

28. A patient who underwent percutaneous


coronary angioplasty with placement of a stent
in a coronary vessel was started on clopidogrel.
This drug exerts its antithrombotic effect
through which of the following mechanisms
a. Irreversible inhibition of ADP receptor
b. Inhibition of thromboxane synthesis
c. Reversible blockade of glycoprotein IIb/IIIa
d. Conversion of plasminogen to plasmin
e. Posttranslational modification of vitamin Kdependent clotting factors

29.The effect of heparin in a patient


who suddenly presented with
gastrointestinal hemorrhage may be
promptly reversed with which of the
following:
a. Vitamin K
b. Ascorbic acid
c. EDTA
d. Protamine
e. Folic Acid

29.The effect of heparin in a patient


who suddenly presented with
gastrointestinal hemorrhage may be
promptly reversed with which of the
following:
a. Vitamin K - warfarin
b. Ascorbic acid
c. EDTA lead poisoning
d. Protamine - heparin
e. Folic Acid

30.Which of the following is most


useful for patients with red cell
deficiency caused by renal disease or
depression of the bone marrow
a. Erythropoietin
b. Hemosiderin
c. Transferrin
d. Folic acid
e. Vitamin B 12

30.Which of the following is most useful for


patients with red cell deficiency caused by
renal disease or depression of the bone marrow
a. Erythropoietin (kidney cant produce EPO)
b. Hemosiderin - iron-storage complex within cells
c. Transferrin - iron transport protein (Ferritin-storage
protein)
d. Folic acid for megaloblastic anemia + Vit B12
e. Vitamin B 12 for pernicious anemia

31.A bactericidal glycoprotein with a narrow


spectrum of activity and is used for serious
infections caused by methicillin-resistant
staphylococci (MRSA), penicillin-resistant
pneumococci, and Clostridium difficile
a. Aztreonam
b. Clavulanic acid
c. Imipinem
d. Cefepime
e. Vancomycin

Aztreonam- monobactam; no activity


against gram positive bacteria or
anaerobes, primarily directed against
enterobacter and aerobic gram negative
rods
Clavulanic acid beta-lactamase inhibitor
used in fixed combination with penicillins
- almost devoid of antibacterial activity

Imipinem- carbapenem (meropenem,


ertapenem); wide activity gram positive,
negative anaerobes; carbapenems- drug of
choice for enterobacter.
Cefepime- 4th generation cephalosporin (firsts
gram positive plus thirds gram negative,
penicillin-resistant strep and pseudomonas
Vancomycin for infections caused by Blactam resistant organisms, for
patients w/ gram + infections who have
serious allergy to B lactam; for
potentially life-threatening colitis due
to Clostridium difficile

31.A bactericidal glycoprotein with a narrow


spectrum of activity and is used for serious
infections caused by methicillin resistant
staphylococci (MRSA), penicillin-resistant
pneumococci, and Clostridium difficile
a. Aztreonam
b. Clavulanic acid
c. Imipinem
d. Cefepime
e. Vancomycin

32.Which of the following


cephalosporins is highly effective
against pseudomonas?
a. Cefazolin
b. Cefuroxime
c. Ceftazidime
d. Cefaclor
e. Ceftriaxone

32.Which of the following cephalosporins is


highly effective against pseudomonas?
a. Cefazolin (1st, gram +, PEcK)
b. Cefuroxime (2nd weaker gram +, HENPEcK)
c. Ceftazidime (3rd , enhanced gram -, for
Pseudomonas)
d. Cefaclor (2nd, weaker gram +, HENPEcK
e. Ceftriaxone (3rd, enhanced gram negative act.,
(-) anti-pseudomonas)
4thCefepime

33.Which of the following antibiotics


inhibit microbial protein synthesis by
binding to the 30s ribosomal subunit
a. Clindamycin
b. Erythromycin
c. Chloramphenicol
d. Tetracycline
e. Linezolid

Drugs targeting the


30S ribosomal unit
(SAT)

Drugs targeting the


50S ribosomal unit

Spectinomycin

Chloramphenicol

Aminoglycoside
gentamicin
amikacin
streptomycin

Macrolides
erythromycin
azithromycin
clarithromycin

Tetracyclines

Lincosamides
clindamycin
Streptogramins
dalfopristin
Oxazolidones (linezolid)

33.Which of the following antibiotics


inhibit microbial protein synthesis by
binding to the 30S ribosomal subunit?
a. Clindamycin 50s
b. Erythromycin 50S
c. Chloramphenicol 50s
d. Tetracycline -30S
e. Linezolid 50S

34.Aminoglycoside toxicity includes


the following EXCEPT:
a. Auditory or vestibular damage
b. Acute tubular necrosis
c. Respiratory paralysis in high doses
d. Contact dermatitis
e. Encephalopathy

34.Aminoglycoside toxicity includes


the following EXCEPT:
a. Auditory or vestibular damage
b. Acute tubular necrosis
c. Respiratory paralysis in high doses
d. Contact dermatitis - neomycin
e. Encephalopathy does not cross
blood brain barrier

35.The following are drugs used in the


treatment of Tuberculosis, EXCEPT:
a.Ethambutol
b.Rifampicin
c.Streptomycine
d.Dapsone
e.Ciprofloxacin

35.The following are drugs used in the


treatment of Tuberculosis, EXCEPT:
a.Ethambutol
b.Rifampicin
c.Streptomycine
d.Dapsone
e.Ciprofloxacin

36.Urinary tract infection due to


Chlamydia trachomatis will NOT
respond to which of the following
drug?
a.Tetracycline
b.Erythromycin
c.Nitrofurantoin
d.Ciprofloxacin

36.Urinary tract infection due to


Chlamydia trachomatis will NOT
respond to which of the following
drug?
a.Tetracycline
b.Erythromycin
c.Nitrofurantoin
d.Ciprofloxacin

37.Which of the following drugs is a


reverse transcriptase inhibitor that is
useful in the treatment of Hepatitis B
infection
a. Amantadine
b. Ganciclovir
c. amivudine
d. Interferon-alpha
e. Acyclovir

37.Which of the following drugs is a reverse


transcriptase inhibitor that is useful in the
treatment of Hepatitis B infection
a. Amantadine inhibitor of viral uncoating- influenza A
b. Ganciclovir antiherpesvirus nucleoside analogue
c. Lamivudine antiHIV / anti HepaB virus
nucleoside analogue
d. Interferon-alpha immunoregulatorfor hepa C inf
e. Acyclovir - antiherpesvirus nucleoside analogue

38.The use of chloroquine in


Plasmodium vivaxinfection is
primarily targeted on the elimination
of which of the following forms of the
parasite
a. Secondary tissue schizonts
b. Exoerythrocyticschizonts
c. Erythrocytic stage
d. Asexual forms
e. Liver stages

Blood schizonticides Tissue schizonticide


- Primaquine
Artemisinin & its
derivatives
Lumefantrine
Chloroquine
Quinine
Mefloquine

Radical cure of acute vivax and ovale malaria


Chloroquine eradicates erythrocytic forms
Primaquine - eradicates liver hypnozoites and
prevent subsequent relapse

38.The use of chloroquine in


Plasmodium vivaxinfection is
primarily targeted on the elimination
of which of the following forms of the
parasite
a. Secondary tissue schizonts
b. Exoerythrocyticschizonts
c. Erythrocytic stage
d. Asexual forms
e. Liver stages

39.Which of the following is the drug of


choice for Schistosomahaematobium?
a. Praziquantel
b. Mebendazole
c. Metronidazole
d. Diethlcarbamazine
e. Albendazole

39.Which of the following is the drug of


choice for Schistosomahaematobium?
a. Praziquantel tapeworm infections
b. Mebendazole nematode infections
c. Metronidazole amebiasis, giardiasis,
trichomoniasis
d. Diethlcarbamazine - filariasis
e. Albendazole nematode infections

40. Drug of choice for the relief of


acute exacerbations of asthma
a. Terbutaline
b. Ipatropium bromide
c. Cromolyn sodium
d. Montelukast
e. Prednisone

40. Drug of choice for the relief of


acute exacerbations of asthma
a. Terbutaline
b. Ipatropiumbromide for COPD
c. Cromolynsodium - controller
d. Montelukast - controller
e. Prednisone - controller

41.Which of the following drugs is used


to decrease uric acid production in
gout?
a.Allopurinol
b.Aspirin
c.Colchicine
d.Probenecid
e.Hydroxychloroquine

ACUTE GOUT

CHRONIC GOUT

Leukocyte inhibitors

Inhibitor of uric acid


synthesis by
inhibiting
xanthineoxidase

NSAIDs
Colchicine
Glucocorticoids

Allopurinol

Agents that increase


excretion of uric acid
Sulfinpyrazone
Probenecid

41.Which of the following drugs is used


to decrease uric acid production in
gout
a.Allopurinol
b.Aspirin
c.Colchicine
d.Probenecid
e.Hydroxychloroquine

42.Treatment for thyrotoxicosis does


not include which of the following
drugs
a. Radioactive iodine
b. Thyroglobulin
c. Propylthiouracil
d. Potassium iodide
e. Methimazole

42.Treatment for thyrotoxicosis does


not include which of the following
drugs
a. Radioactive iodine
b. Thyroglobulin protein synthesized
by thyroid follicular cells and secreted
at the apical surface into the colloid
space
c. Propylthiouracil
d. Potassium iodide
e. Methimazole

43. Action of Sulfonylurea hypoglycemic


agents does NOT include
a. Stimulate release of endogenous insulin
b. Reduce glucagon release
c. Increase functional insulin receptors in
peripheral tissues
d. Increase target tissue sensitivity to insulin
e. Closing of potassium channels in the
pancreatic B cell membrane

43. Action of Sulfonylurea hypoglycemic


agents does NOT include
a. Stimulate release of endogenous insulin
b. Reduce glucagon release
c. Increase functional insulin receptors in
peripheral tissues
d. Increase target tissue sensitivity to
insulin (biguanides -metformin; TZDs
rosiglitazone)
e. Closing of potassium channels in the
pancreatic B cell membrane

44.Which of the following is most likely


to cause hypoglycemia when used as
a monotherapy for Type II diabetes?
a. Acarbose
b. Glimepiride
c. Metformin
d. Rosiglitazone
e. Miglitol

44.Which of the following is most likely


to cause hypoglycemia when used as
a monotherapy for Type II diabetes?
a. Acarbose GI distress
b. Glimepiride
c. Metformin GI distress, sl. Weight loss
d. Rosiglitazone weight gain
e. Miglitol GI distress

45.The hypoglycemic agent of choice


in pregnant women
a.Biguanides
b.Sulfonylurea
c.Insulin
d.Rosiglitazone
e.Acarbose

45.The hypoglycemic agent of choice


in pregnant women
a.Biguanides
b.Sulfonylurea
c.Insulin
d.Rosiglitazone
e.Acarbose

46.Which of the following is NOT an


effect of muscarinic blocking drugs?
a.Miosis
b.Constipation
c.Reduced salivation and gastric secretion
d.Urinary retention
e.Bronchodilation

46.Which of the following is NOT an


effect of muscarinic blocking drugs?
a.Miosis
b.Constipation
c.Reduced salivation and gastric secretion
d.Urinary retention
e.Bronchodilation

47.Which of the following is NOT a


direct-acting cholinergic agonist?
a. Bethanechol
b. Carbachol
c. Pilocarpine
d. Neostigmine
e. Nicotine

47.Which of the following is NOT a


direct-acting cholinergic agonist?
a.Bethanechol
b.Carbachol
c.Pilocarpine
d.Neostigmine cholinesterase
inhibitor
e.Nicotine

48.Cause of death from exposure to a


high concentration of
organophosphate insecticide will
most likely be:
a. Cardiac arrhythmia
b. Respiratory failure
c. Hypertension
d. Renal failure
e. Gastrointestinal hemorrhage

Major effect is inhibition of


acetylcholinesterase

Acute toxic effects are those of


muscarinic excess followed rapidly by
CNS involvement; respiration in
particular may be impaired

48.Cause of death from exposure to a


high concentration of
organophosphate insecticide will
most likely be
a. Cardiac arrhythmia
b. Respiratory failure
c. Hypertension
d. Renal failure
e. Gastrointestinal hemorrhage

49.A patient with warm septic shock


presents with hypotension and
generalized vasodilation. High dose
Dopamine intravenous infusion was
started. Which adrenoceptor does
dopamine act to constrict the vessels?
a.Beta-1
b.Alpha-1
c.Alpha-2
d.D1
e.D2

49.A patient with warm septic shock


presents with hypotension and
generalized vasodilation. High dose
Dopamine intravenous infusion was
started. Which adrenoceptor does
dopamine act to constrict the vessels?
a.Beta-1
b.Alpha-1
c.Alpha-2
d.D1
e.D2

50.A patient rushed to the emergency


room for anaphylactic shock was
given intramuscular epinephrine.
Which of the following are expected
effects of the drug
a. Bronchodilation
b. Vasodilation
c. Decreased cardiac contractility
d. Pupillary constriction
e. Uterine contraction

50.A patient rushed to the emergency


room for anaphylactic shock was
given intramuscular epinephrine.
Which of the following are expected
effects of the drug
a. Bronchodilation
b. Vasodilation (vasoconstriction)
c. Decreased cardiac contractility
d. Pupillaryconstriction (dilatation)
e. Uterine contraction (uterine relaxation)

51.Which of the following is the drug of


choice for a hypertensive patient with
benign prostatic hypertrophy and
urinary obstruction?
a. Metoprolol
b. Clonidine
c. Prazosin
d. Ephedrine
e. Methlydopa

51.Which of the following is the drug of


choice for a hypertensive patient with
benign prostatic hypertrophy and
urinary obstruction?
a.Metoprolol(1 selective blocker)
b.Clonidine(centrally acting 2 agonist)
c.Prazosin(1 selective antagonist, decrease tone
in the smooth muscle of the bladder neck and
improves urine flow)

d.Ephedrine(inhibitor of catecholamine storage)


e.Methlydopa(centrally acting 2 agonist)

52.A patient diagnosed to have


pheochromocytoma, a tumor of the adrenal
medulla causing excessive release of
epinephrine and norepinephrine, was
started on a non-selective alphaantagonist, an example of which is
a.Yohimbine
b.Methyldopa
c.Terazosin
d.Phenoxybenzamine
e.Clonidine

52.A patient diagnosed to have pheochromocytoma,


a tumor of the adrenal medulla causing excessive
release of epinephrine and norepinephrine, was
started on a non-selective alpha-antagonist, an
example of which is
a.Yohimbine (2 selective antagonist)
b.Methyldopa(centrally acting 2 agonist)
c.Terazosin(1 selective antagonist)
d.Phenoxybenzamine (non-selective antagonist)
e.Clonidine(centrally acting 2 agonist)

53.The following is NOT a clinical use


of beta-adrenoceptor antagonists:
a.Portal hypertension
b.Glaucoma
c.Hypothyroidism
d.Chronic heart failure
e.Angina

53.The following is NOT a clinical use


of beta-adrenoceptor antagonists:
a.Portal hypertension
b.Glaucoma
c.Hypothyroidism (hyperthyroidism,
increases peripheral conversion of T4
to T3
d.Chronic heart failure
e.Angina

54.Postsynaptic activation of Alpha-1


receptors will lead to the following
cellular effects
a.Decreased intracellular calcium
b.IncreasedcAMP
c.Increased IP3 and DAG
d.Inhibition of phospholipase activity
e.Inhibition of Phosphodiesterase III

54.Postsynaptic activation of Alpha-1


receptors will lead to the following
cellular effects
a.Decreased intracellular calcium
b.IncreasedcAMP(,2 adrenoceptors)
c.Increased IP3 and DAG (1
adrenoceptors, cholinergic muscarinicreceptors)

d.Inhibition of phospholipase activity


e.Inhibition of Phosphodiesterase III

55.Which of the following drugs will


decrease heart rate in a normal heart
but has little or no effect in a
denervatedheart?
a.Phenylephrine
b.Isoproterenol
c.Dobutamine
d.Epinephrine
e.Prazosin

55.Which of the following drugs will


decrease heart rate in a normal heart
but has little or no effect in a
denervated heart
a.Phenylephrine causes intense
vasoconstriction leading to reflex HR
b.Isoproterenol -
c.Dobutamine -
d.Epinephrine -
e.Prazosin - no effect

56.Which among the following is the


most potent diuretic?
a.Furosemide
b.Hydrochlorothiazide
c.Spironolactone
d.Acetazolamide
e.Eplerenone

56.Which among the following is the


most potent diuretic
a.Furosemide (loop diuretic)
b.Hydrochlorothiazide (thiazide diuretics)
c.Spironolactone (Postassium sparing
diuretics)
d.Acetazolamide (carbonic anhydrase
inhibitor)
e.Eplerenone (potassium sparing diuretics)

57.Which of the following is a direct


centrally-acting sympatholytic agent?
a.Methyldopa
b.Guanethedine
c.Reserpine
d.Propranolol
e.Prazosin

57.Which of the following is a direct


centrally-acting sympatholytic agent?
a.Methyldopa
b.Guanethedine
c.Reserpine
d.Propranolol
e.Prazosin

58.A major air pollutant which can


cause headache, tachycardia, and
syncope
a.Carbon monoxide
b.Nicotine
c.Nitrogen dioxide
d.Ozone
e.Sulfur dioxide

58.A major air pollutant which can


cause headache, tachycardia, and
syncope
a.Carbon monoxide
b.Nicotine
c.Nitrogen dioxide
d.Ozone
e.Sulfur dioxide

59.A patient manifesting with wristdrop, anorexia, anemia, tremor,


weight loss and gastrointestinal
symptoms is most likely suffering
from which of the following
a.Acute mercury poisoning
b.Chronic mercury poisoning
c.Iron poisoning
d.Chronic lead poisoning
e.Chronic arsenic poisoning

59.A patient manifesting with wristdrop, anorexia, anemia, tremor,


weight loss and gastrointestinal
symptoms is most likely suffering
from which of the following
a.Acute mercury poisoning
b.Chronic mercury poisoning
c.Iron poisoning
d.Chronic lead poisoning
e.Chronic arsenic poisoning

60.A child with diagnosed to have


acute lead poisoning with signs and
symptoms of encephalopathy should
be given
a.Acetylcysteine
b.Deferoxamine
c.EDTA
d.Penicillamine
e.Succimer

60.A child with diagnosed to have


acute lead poisoning with signs and
symptoms of encephalopathy should
be given
a.Acetylcysteine paracetamol poisoning
b.Deferoxamine - Iron
c.EDTA
d.Penicillamine - Copper
e.Succimer - Cadmium

61.A patient who suddenly


deteriorated due to respiratory
depression after being given
diazepam may benefit from this
antidote
a.Flumazenil
b.Acetylcysteine
c.Atropine
d.Oxygen
e.Pralidoxime

61.A patient who suddenly


deteriorated due to respiratory
depression after being given
diazepam may benefit from this
antidote
a.Flumazenil
b.Acetylcysteine
c.Atropine organophosphate poisoning
d.Oxygen
e.Pralidoxime organophosphate poisoning

62.Which of the following will confer


passive immunity?
a.Diphtheriatoxoid
b.Measles vaccine
c.Tetanus antitoxin
d.Oral polio vaccine
e.Purified protein derivative

62.Which of the following will confer


passive immunity
a.Diphtheriatoxoid
b.Measles vaccine
c.Tetanus antitoxin
d.Oral polio vaccine

e.Purified protein derivative

63.Drug that blocks estrogen receptors


in the pituitary gland increasing FSH
and LH output
a. Clomiphene
b. Diethylstilbesterol
c. Danazol
d. Tamoxifen
e. Raloxifene

63.Drug that blocks estrogen receptors


in the pituitary gland increasing FSH
and LH output
a. Clomiphene - SERM
b. Diethylstilbestrol non-steroidal
estrogen
c. Danazol - antiandrogen
d. Tamoxifen - SERM
e. Raloxifene SERM

64.Estrogen used in most combined


hormonal contraceptives
a.Clomiphene
b.Ethinylestradiol
c.Estrone
d.DES

e.Norgestrel

64.Estrogen used in most combined


hormonal contraceptives
a.Clomiphene
b.Ethinylestradiol
c.Estrone
d.DES

e.Norgestrel

65.Which of the phases of the cell


cycle is most resistant to most
chemotherapeutic agents and
requires increased drug dose to
obtain response?
a.S phase
b.G0 phase
c.G1 phase
d.G2 phase

Cell cycle

Antineoplastic
Drugs

M (mitosis)

Cell division into


two identical
daughter cells

Inhibitors of
microtubule
function

G1 (gap 1)

Active
glucocorticoids
metabolism in the
absence of DNA
sythesis)

S (synthesis)

Cell replication

Antimetabolites
Folate pathway
inhibitors
Topoisomerase
inhibitors

G2 (gap 2)

Cell preparation
for mitosis

Antitumor
antibiotics
Topoisomerase
inhibitors

Alkylating agents and platinum


complexes affect cell function in ALL
phases and are therefore, NON-CYCLE
SPECIFIC
The differential cell-cycle specificity of
the various drug classes allows them to
be used in combination
Cell-cycle specific drugs target
actively replicating neoplastic cells
Cell-cycle non-specific agents taget
quiescent (non-replicating) cells

65.Which of the phases of the cell


cycle is most resistant to most
chemotherapeutic agents and
requires increased drug dose to
obtain response?
a. S phase
b.G0 phase
c.G1 phase
d.G2 phase

66.By which of the following


mechanisms do vinca alkaloids work
in cancer chemotherapy?
a.Inhibition of function of microtubules
b.Damage and prevention of repair of DNA
c.Inhibition of purine synthesis
d.Inhibition of DNA gyrase
e.Inhibition of protein synthesis

66.By which of the following


mechanisms do vinca alkaloids work
in cancer chemotherapy
a.Inhibition of function of microtubules
b.Damage and prevention of repair of DNA
topoisomerase inhibitors
c.Inhibition of purinesynthesis
-mercaptopurine
d.Inhibition of DNA gyrase
e.Inhibition of protein synthesis

67.Doxorubicin, a drug used in the


treatment of Hodgkins disease
belongs to which group of
antineoplastic drugs
a.Alkylating agents
b.Antimetabolites
c.Plant alkaloids
d.Antibiotics
e.Hormones

67.Doxorubicin, a drug used in the


treatment of Hodgkins disease
belongs to which group of
antineoplastic drugs
a.Alkylatingagents (cyclophosphamide)
b.Antimetabolites (methotrexate)
c.Plantalkaloids (vincristine)
d.Antibiotics
e.Hormones

68.A patient in heart failure was given a


diuretic which inhibits Na reabsorption
and potassium secretion by acting as a
competitive antagonist of a receptor
located at the blood side of the tubule.
The drug is most likely
a.Spironolactone
b.Hydrochlorothiazide
c.Amiloride
d.Furosemide
e.Mannitol

68.A patient in heart failure was given a


diuretic which inhibits Na reabsorption
and potassium secretion by acting as a
competitive antagonist of a receptor
located at the blood side of the tubule.
The drug is most likely
a.Spironolactone
b.Hydrochlorothiazide
c.Amiloride
d.Furosemide
e.Mannitol

69.Hydrochlorothiazide was prescribed


when lifestyle modification failed to
lower the blood pressure of a patient
with Stage I hypertension. Adverse
effects of this drug include which of the
following:
a.Hypokalemic metabolic acidosis
b.Hyperuricemia
c.Hypoglycemia
d.Hypocalcemia
e.Decrease in serum cholesterol and LDL

69.Hydrochlorothiazide was prescribed when


lifestyle modification failed to lower the
blood pressure of a patient with Stage I
hypertension. Adverse effects of this drug
include which of the following:
a.Hypokalemic metabolic acidosis (alkalosis)
b.Hyperuricemia
c.Hypoglycemia (hyperglycemia)
d.Hypocalcemia (hypercalcemia)
e.Decrease in serum cholesterol and LDL

70.A patient diagnosed to have essential


hypertension was receiving enalapril,
furosemide, metoprolol and clonidine.
Good control of hypertension made the
doctor decide to discontinue one drug.
Gradual withdrawal of which drug will
prevent rebound hypertension:
a.Enalapril
b.Furosemide
c.Metoprolol
d.Clonidine

e.Losartan

70.A patient diagnosed to have essential


hypertension was receiving enalapril,
furosemide, metoprolol and clonidine.
Good control of hypertension made the
doctor decide to discontinue one drug.
Gradual withdrawal of which drug will
prevent rebound hypertension:
a.Enalapril
b.Furosemide
c.Metoprolol
d.Clonidine

e.Losartan

71.An anti-hypertensive agent which


acts through nitric oxide, dilates
arterioles but not veins, and causes a
lupus-erythematosus-like syndrome
a.Minoxidil
b.Nitroprusside
c.Fenoldapam
d.Hydralazine
e.Verapamil

71.An anti-hypertensive agent which


acts through nitric oxide, dilates
arterioles but not veins, and causes a
lupus-erythematosus-like syndrome
a.Minoxidil
b.Nitroprusside
c.Fenoldapam
d.Hydralazine
e.Verapamil

72.A 20-year old male was admitted in


moderate cardiorespiratory distress due
to heart failure secondary to
Rheumatic Heart Disease. Drugs which
were found useful in heart failure
include the following EXCEPT:
a.Diuretics
b.Beta- adrenoceptor agonists
c.Calcium channel blockers
d.ACE inhibitors
e.Digoxin

72.A 20-year old male was admitted in


moderate cardiorespiratory distress due
to heart failure secondary to
Rheumatic Heart Disease. Drugs which
were found useful in heart failure
include the following EXCEPT:
a.Diuretics
b.Beta- adrenoceptor agonists
c.Calcium channel blockers
d.ACE inhibitors
e.Digoxin

73.A 37-year old male presenting with


pancreatitis, eruptive xanthoma and
centripetal obesity had a triglyceride
level of 900 mg/dL. The rest of the lipid
profile was normal. This patient will
most likely benefit from which of the
following drugs
a.Lovastatin
b.Ezetimibe
c.Niacin
d.Cholestyramine

73.A 37-year old male presenting with


pancreatitis, eruptive xanthoma and
centripetal obesity had a triglyceride
level of 900 mg/dL. The rest of the lipid
profile was normal. This patient will
most likely benefit from which of the
following drugs
a.Lovastatin
b.Ezetimibe
c.Niacin
d.Cholestyramine

74.Most potent H2 blocker with


negligible binding with CYP450
enzyme
a.Cimetidine
b.Famotidine
c.Ranitidine
d.Nizatidine

74.Most potent H2 blocker with


negligible binding with CYP450
enzyme
a.Cimetidine
b.Famotidine
c.Ranitidine
d.Nizatidine

75.A laxative usually given as


suppository and promotes peristaltic
action and defecation in 15-30
minutes
a.Methylcellulose
b.Bisacodyl
c.Magnesium sulfate
d.Lactulose

Bulk-formers

Hold water and expand in


stool, promoting peristalsis
e.g Methylcellulose

Stool softeners

Soften fecal material via


detergent action that allows
water to penetrate stool
e.g. Docusate sodium

Stimulant laxative

Direct irritation of intestinal


mucosa leading to peristalsis
Bisacodyl (Dulcolax,Senokot)

75.A laxative usually given as


suppository and promotes peristaltic
action and defecation in 15-30
minutes
a.Methylcellulose (bulk-former)
b.Bisacodyl
c.Magnesiumsulfate
d.Lactulose (non-absorbable sugar)

76.H. pylori associated peptic ulcer can


be treated with the following
regimen:
a.PPI, Amoxicillin, Metronidazole for 10-14
days
b.Bismuth, PPI, Amoxicillin, Clarithromycin
for 4-6 weeks
c.PPI for 10-14 days; Clarithromycin and
Amoxicillin for 4-6 weeks

d.PPI for 4-6 weeks; Clarithromycin


and Amoxicillin for 10-14 days

2 therapeutic goals:
Heal the ulcer Eradicate the organisms
Combination of 2 antibiotics
Proton pump inhibitor raise
intragastric pH lowering the MIC
against H pylori
10-14 day regimen

76.H. pylori associated peptic ulcer can


be treated with the following regimen:
a.PPI, Amoxicillin, Metronidazole for 10-14
days
b.Bismuth, PPI, Amoxicillin, Clarithromycin for
4-6 weeks
c.PPI for 10-14 days; Clarithromycin and
Amoxicillin for 4-6 weeks

d.PPI for 4-6 weeks;


Clarithromycin and Amoxicillin for
10-14 days

77.Which of the following is NOT a drug


mechanism used in the treatment of
parkinsonism?
a.Amantadine stimulates release of dopamine
from storage sites
b.Bromocriptine stimulates dopamine receptors
c.Levodopa enhances the synthesis of
dopamine
d.Selegeline is an inhibitor of monoamine
oxidase

77.Which of the following is NOT a drug


mechanism used in the treatment of
parkinsonism?
a.Amantadine stimulates release of dopamine
from storage sites
b.Bromocriptine stimulates dopamine receptors

c.Levodopa enhances the synthesis of


dopamine
d.Selegeline is an inhibitor of monoamine
oxidase

77.Which of the following is NOT a drug


mechanism used in the treatment of
parkinsonism?
a. Amantadinestimulates release of
dopamine from storage sites
b. Bromocriptinestimulates dopamine
receptors
c. Levodopaenhances the synthesis of
dopamine
d. Selegelineis an inhibitor of monoamine
oxidase

Do not affect the dopaminergic


pathways directly
Used to treat levodopa-induced
dykinesias
by global blockade of excitatory
NMDA receptors

78.Aluminum and calcium salts inhibit


the intestinal absorption of which of
the following agents?
a.Isoniazid
b.Phenomymethyl penicillin
c.Erythromycin
d.Tetracycline

An important pharmacokinetic feature of


Tetracyclines is the interaction with foods
high in CALCIUM such as dairy products
and with such medicines as ANTACIDS
that contain divalent and trivalent cations
bec of impaired absorption, it is best
taken on an empty stomach
Once tetracyclines are in the circulation, it
can cause sequestration of the drug in
bone and teeth

78.Aluminum and calcium salts inhibit


the intestinal absorption of which of
the following agents?
a.Isoniazid
b.Phenomymethyl penicillin
c.Erythromycin

d.Tetracycline

79.Which of the following mechanisms


is associated with bacterial resistance
to B-lactampenicillins?
a.bacterial production of lysozymes
b.alteration of penicillin-binding proteins
(PBPs)
c.increased metabolism of the penicillin
d.ability of the bacteria to produce an acid
media

79.Which of the following mechanisms


is associated with bacterial resistance
to B-lactampenicillins?
a.bacterial production of lysozymes
b.alteration of penicillin-binding proteins
(PBPs)
c.increased metabolism of the penicillin
d.ability of the bacteria to produce an acid
media

80.Which of the following drugs exhibit


linear kinetics?
a.phenytoin
b.penicillin
c.digoxin
d.procainamide

80.Which of the following drugs exhibit


linear kinetics?
a.phenytoin, aspirin, ethanol
b.penicillin
c.digoxin
d.procainamide

81.The following drugs are metabolized


in the liver, EXCEPT;
a.Cefoperazone
b.Chloramphenicol
c.Clindamycin
d.Amikacin

81.The following drugs are metabolized


in the liver, EXCEPT;
a.Cefoperazone
b.Chloramphenicol
c.Clindamycin
d.Amikacin (kidney)

82.The following are time dependent


antibiotics, EXCEPT:
a.Ceftriaxone
b.Meropenem
c.Erythromycin
d.Gentamicin

Rate

of killing increases with drug


concentration

SINGLE very large dose can have a


profound therapeutic effect and may
be sufficient to eliminate the infection

Ex: Aminoglycosides
Quinolones
Bacitracin

exhibit a constant rate of killing that is


INDEPENDENT of drug concentration,
provided that the drug concentration
is greater than the MBC (minimum
bactericidal concentration)

overriding consideration is not the


absolute drug concentration that is
achieved, but FOR HOW LONG the
drug concentration remains in the
therapeutic range ( drug conc> MBC)

Beta-lactams
vancomycin
Polmyxins
Pyrazinamide
Isoniazid
Rifampin
Metronidazole

82.The following are time dependent


antibiotics, EXCEPT:
a.Ceftriaxone (beta lactam cidal time)
b.Meropenem (beta-lactam cidal-time)
c.Erythromycin (macrolide bacteriostatic)
d.Gentamicin (aminoglycoside cidal-conc.)

83.Which of the following anti-epileptic


drugs have active metabolites that
are clinically significant?
a.Phenytoin
b.Phenobarbital
c.Carbamazepine
d.Ethosuximide

83.Which of the following anti-epileptic


drugs have active metabolites that
are clinically significant?
a.Phenytoin
b.Phenobarbital
c.Carbamazepine 10-11
epoxycarbamazepinew/c slows Na+
channel recovery
d.Ethosuximide

88.In the treatment of hypertensive


emergency (crisis), the drug of choice
is:
a.thiazide diuretic
b.sodiumnitroprusside
c.reserpine
d.hydralazine

88.In the treatment of hypertensive


emergency (crisis), the drug of choice
is:
a.thiazide diuretic
b.sodiumnitroprusside
c.reserpine
d.hydralazine

89.Drug with a low therapeutic index


that induces delayed afterdepolarization in cardiac tissue:
a.quinidine
b.isoproterenol
c.adenosine
d.digoxin

89.Drug with a low therapeutic index


that induces delayed afterdepolarization in cardiac tissue:
a.quinidine
b.isoproterenol
c.adenosine
d.digoxin

90.An anti-arrhythmic drug known to


produce a potentially fatal form of
pulmonary fibrosis
a.Lidocaine
b.Amiodarone
c.Sotalol
d.Procainamide

90.An anti-arrhythmic drug known to


produce a potentially fatal form of
pulmonary fibrosis
a.Lidocaine
b.Amiodarone
c.Sotalol
d.Procainamide

91.Which of the following anticancer


drugs does not produce covalent
modification of DNA or breakage of
DNA strands?
a.bleomycin
b.cyclophosphamdie
c.melphalan
d.vinblastine

Alkylating agents
ex cyclophosphamide
melphalan
platinum compounds
ex cisplatin
carboplatin
t

bleomycin

91.Which of the following anti-cancer


drugs does not produce covalent
modification of DNA or breakage of
DNA strands?
a.bleomycin
b.Cyclophosphamide
c.melphalan
d.Vinblastine (agent that inhibits
microtubule polymerization)

92.In cancer chemotherapy, alkylating


agents are used in combination
regimens with anti-metabolites to
treat patients with certain cancers
because they:
a.Do not cause hair root toxicity
b.Are selectively toxic to cancer cells
c.Do not damage the bone marrow cells
d.Are not cell cycle specific

Page 1320, GG, fig 51.2

92.In cancer chemotherapy, alkylating


agents are used in combination
regimens with anti-metabolites to
treat patients with certain cancers
because they:
a.Do not cause hair root toxicity
b.Are selectively toxic to cancer cells
c.Do not damage the bone marrow cells
d.Are not cell cycle specific

93. All of the following pharmacological


actions of morphine are mu opioid
receptor responses, EXCEPT:
a.respiratory depression
b.hallucinations
c.bradycardia
d.decreased GI motility

93.All of the following pharmacological


actions of morphine are mu opioid
receptor responses, EXCEPT:
a.respiratory depression
b.Hallucinations (behavioral
restlessness, hyperactivity)
c.Bradycardia ? Postural hypotension
d.decreased GI motility

94.Which of the following provides


information about the variation in
sensitivity to a drug within the
population studied?
a.maximal efficacy
b.therapeutic index
c.graded-dose response curve
d.quantal-dose response curve

94.Which of the following provides


information about the variation in
sensitivity to a drug within the
population studied?
a.maximalefficacy
b.therapeuticindex
c.graded-dose response curve
d.quantal-dose response curve

A concentration
effect curve applies
only to a single
individual at one
time or to an
average individual
The curve
represents the
effects and dose of
a drug within an
individual animal or
tissue rather in a
population

Pharmacodynamic
variability in a
population may
be analyzed by
constructing a
QUANTAL
CONCENTRATION
EFFECT CURVE

94.Which of the following provides


information about the variation in
sensitivity to a drug within the
population studied?
a.maximal efficacy
b.therapeutic index
c.graded-dose response curve
d.quantal-dose response curve

95.A patient is to undergo day surgery


for a short procedure, and intravenous
anesthesia will be used. A short-acting
drug that appears to affect GABAergic
neurotransmission and is often used for
day surgery because patients are not
hampered by post-operative nausea
and malaise:
a.fentanyl
b.ketamine
c.propofol
d.thiopental

95.A patient is to undergo day surgery for a short


procedure, and intravenous anesthesia will be
used. A short-acting drug that appears to affect
GABAergic neurotransmission and is often used for
day surgery because patients are not hampered by
post-operative nausea and malaise:
a.Fentanyl (analgesic)
b.Ketamine (IV, dissociative anesthesia, hallucinations
c.Propofol (IV)
d.Thiopental (IV, drowsiness)

96.When treating a patient who has


been exposed to a chemical agent
with known toxicity, the primary
determinant of whether or not a toxic
effect will be seen is:
a.the agents dose
b.the patients age
c.the route of exposure
d.the duration of exposure

96.When treating a patient who has


been exposed to a chemical agent
with known toxicity, the primary
determinant of whether or not a toxic
effect will be seen is:
a.the agents dose
b.the patients age
c.the route of exposure
d.the duration of exposure

97.Three symptoms of atropine


intoxication are:
a.dry mouth, cutaneous vasodilatation
b.dry mouth, spasm of accommodation,
miosis
c.fever, dry mouth, CNS excitation
d.fever, bed wetting, dry mouth

97.Three symptoms of atropine


intoxication are:
a.dry mouth, cutaneousvasodilatation
b.dry mouth, spasm of accommodation,
miosis
c.fever, dry mouth, CNS excitation
d.fever, bed wetting , dry mouth

98.Both acetylcholine and


norepinephrine affect cardiac force of
contraction. They do this by
influencing:
a.the M-2 muscarinic receptor
b.the B-1 adrenergic receptor
c.a K+ channel
d.adenylcyclase

98.Both acetylcholine and norepinephrine


affect cardiac force of contraction. They do
this by influencing:
a.the M-2 muscarinic receptor
b.the B-1 adrenergic receptor
c.a K+ channel
d.adenylcyclase (ACETYLCHOLINE - binding to
M2 or M4 muscarinic receptors leads to
inhibition of adenylcyclase;
NOREPINEPHRINE - binding to B1 receptors
leads to stimulation of adenylcyclase

99.Reserpine decreases arterial


pressure by:
a.interfering with the synthesis of
norepinephrine
b.interfering with the storage of
norepinephrine
c.interfering with the release of
norepinephrine
d.interfering with the metabolism of
norepinephrine

99.Reserpine decreases arterial


pressure by:
a.interfering with the synthesis of
norepinephrine
b.interfering with the storage of
norepinephrine
c.interfering with the release of
norepinephrine
d.interfering with the metabolism of
norepinephrine

UNDERSTAND the basic principles of


pharmacology: PK (ADME) & PD (MOA)
memorize the autonomic nervous
system
be familiar with the different drug
classifications and the prototype drugs
(drug summary tables)
associate the drugs to those persons
whom you know are using them
again, REVIEW using the method that
best suits you

PRAY .
PRAY .
PRAY .

Basic and Clinical Pharmacology


10thedition,Katzung BG

Principles

of Pharmacology: The
Pathophysiologic Basis of Drug
Therapy
Golan et al

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