Final Pharmacology

Leonila A. Estole-Casanova, MD

Associate Professor 2

Department of Pharmacology and Toxicology

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}

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 β- adrenergic blocker*

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.

β- adrenergic blocker –

heart rate or contractility

contraindicated: bradycardia

heart block

PRAY ….

PRAY ….

Leonila A. Estole-Casanova, MD

Associate Professor 2

Department of Pharmacology and Toxicology

processes of absorption, distribution, metabolism and elimination

mechanisms of action

Molecular

/ Cellular

level

Organism

Population

Receptors Affinity Dissociation constant (K_d) Agonist, antagonist Efficacy (E_max) Potency Graded-dose response curve Therapeutic Window ED₅₀ TD₅₀ Therapeutic Index Quantal concentration -effect curve

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)

V

d

= concentration of drug in plasma (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

V

d

= D / C

D = C (

V

d

)

= 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

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 = V

_d

xC

_{steady state}

V

_d

– volume of distribution

C

_steadystate

- 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

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 O-}

methylation



_{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

11. Which of the following is NOT a

Phase II reaction of drug metabolism

a. Deamination

b. Acetylation

c. Glucuronidation d. Methylation

84.The rate of acetylation is important

with respect to the duration of action

of:

a. atropine b. cocaine c. isoniazid

84.The rate of acetylation is important

with respect to the duration of action

of:

a. atropine b. cocaine

c. isoniazid

drugs induce

P450





Increased rate of

metabolism

drugs inhibit P450





potentiate the

actions of other

drugs



_Phenytoin



_{carbamazepine}



_barbiturates



_rifampicin



_ritonavir



_griseofulvin



_{chronic ethanol}

toxicity



_omeprazole



_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

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

86.The expected effect of toxic

hepatitis on the rate of drug

metabolism by the liver:

a.Increased

b.Decreased

c.Unchanged

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

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

5.The dose or concentration required

to bring about 50% of a drug’s

maximal effect

a. Potency b. ED₅₀ c. Efficacy d. K_d e. Therapeutic index

Molecular

/ Cellular

level

Organism

Population

Receptors Affinity Dissociation constant (K_d) Agonist, antagonist Efficacy (E_max) Potency Graded-dose response curve Therapeutic Window ED₅₀ TD₅₀ Therapeutic Index Quantal concentration -effect curve

K

_d



_{A measure of a drug’s affinity for a}

given receptor



_{The concentration of drug required in}

solution to achieve 50% occupancy of

its receptors

Molecular

/ Cellular

level

Organism

Population

Receptors Affinity Dissociation constant (K_d) Agonist, antagonist Efficacy (E_max) Potency Graded-dose response curve Therapeutic Window ED₅₀ TD₅₀ Therapeutic Index Quantal concentration -effect curve

E

_max 

_maximal

response

produced by the

drug



_{Refers to the}

concentration

(EC

₅₀

) or dose

(ED

₅₀

) of a drug

required to

produce 50% of

the drug’s

maximal effect

Molecular

/ Cellular

level

Organism

Population

Receptors Affinity Dissociation constant (K_d) Agonist, antagonist Efficacy (E_max) Potency Graded-dose response curve Therapeutic Window ED₅₀ TD₅₀ Therapeutic Index Quantal concentration -effect curve

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 drug’s

maximal effect

a. Potency b. ED₅₀ c. Efficacy d. K_d 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 EC

₅₀

= K

_d

.



_{Sometimes, maximal response is seen at}

a fractional receptor occupation



_{allow maximal response without total}

receptor occupancy – increase sensitivity

of the system



EC

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:

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 t

drug binds to

receptor and

stays bound



_{irreversible – does}

not let go of

receptor

ex.

Phenoxybenzamin

e

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 t

_{Cause a}

physiologic effect

opposite to that

induced by the

agonist

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 (C_max) – rate of absorption

b. Time to peak blood concentration (T_max) – rate of absorption

c. Product of the volume of distribution and the first-order rate constant

d. Volume of distribution (V_d) = (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 concentration-time 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 it’s effectiveness and an increased dose is necessary to produce same

response

d. Anaphylaxis - immediate hypersensitivity which is antibody mediated

e. Synergism 1+1 > 2

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

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

9. Aspirin is a weak organic acid with a

pK

_a

of 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)=pKa-pH



_{= 1; antilog 1= 10/1; protonated}

10/11

Aspirin is a weak acid with a pK_aof 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

pK

_aspirin

= pH

_stomach

+ log HA (protonated)

A

-

Henderson-Hasselbalch equation

pK

_aspirin

= pH

_stomach

+ log HA

A

-

3.5 – 2.5 = log HA / A

-

1 = log HA / A

-

antilog of 1 = HA / A

-

10 = HA /A

-

Protonated = 10 / 11 = 90%

9. Aspirin is a weak organic acid with a

pK

_a

of 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

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

be least ionized in:

a.the small intestine b.pulmonary alveoli

c.the stomach

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

t

_1/2

= 0.693 xV

_d

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

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

long-acting active product?

a.Clozapine

b.Amitriptyline c.Nortriptyline d.Trazodone

18.Which of the following is a tricyclic

antidepressant that has a high

anti-cholinergic activity, is sedating and is

biotransformed to a long-acting

active product?

a.Clozapine (antipsychotics) ✖ b.Amitriptyline (TCA)

c.Nortriptyline (TCA)

Antichol Sedating

b.Amitriptyline (TCA) +3 +3

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

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%)

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

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

Block conduction in the following order: small myelinated axons,

non-myelinated axons, large non-myelinated axons

_{Unwanted effects result mainly from}

ESCAPE of LAs INTO the systemic circulation – Main unwanted effects:

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 ✖

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

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)

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

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

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 μ 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 μ 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 K-dependent 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 plasmin-

thrombolytic agents (t-PA- alteptelase, reteplase;urokinase, streptokinase)

Posttranslational modification of vitamin

K-dependent 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 plasmin- thrombolytic agents (t-PA- alteptelase, reteplase;urokinase, streptokinase)

Posttranslational modification of vitamin K-dependent 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 K-dependent 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

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

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 (first’s

gram positive plus third’s gram negative, penicillin-resistant strep and pseudomonas

Vancomycin – for infections caused by B-lactam 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

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

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

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

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

35.The following are drugs used in the

treatment of Tuberculosis, EXCEPT:

a.Ethambutol b.Rifampicin

c.Streptomycine

d.Dapsone

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

38.The use of chloroquine in

Plasmodium vivax

infection 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

Artemisinin & its derivatives Lumefantrine Chloroquine Quinine Mefloquine Tissue schizonticide - _Primaquine

Radical cure of acute vivax and ovale malaria

Chloroquine – eradicates erythrocytic forms

Primaquine - eradicates liver hypnozoites and

38.The use of chloroquine in

Plasmodium vivax

infection 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

40. Drug of choice for the relief of

acute exacerbations of asthma

a. Terbutaline

b. Ipatropium bromide c. Cromolyn sodium d. Montelukast

40. Drug of choice for the relief of

acute exacerbations of asthma

a. Terbutaline

b. Ipatropiumbromide – for COPD c. Cromolynsodium - controller d. Montelukast - 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 NSAIDs

Colchicine

Glucocorticoids

Inhibitor of uric acid synthesis by

inhibiting

xanthineoxidase Allopurinol

Agents that increase excretion of uric acid Sulfinpyrazone

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

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

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

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

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

Major effect is inhibition of

acetylcholinesterase



_{Acute toxic effects are those of}

muscarinic excess followed rapidly by

CNS involvement; respiration in

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

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

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

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)

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(β₁ selective blocker)

b.Clonidine(centrally acting α₂ agonist)

c.Prazosin(α₁ selective antagonist, decrease tone

in the smooth muscle of the bladder neck and improves urine flow)

d.Ephedrine(inhibitor of catecholamine storage)

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 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 (α₂ selective antagonist) b.Methyldopa(centrally acting α₂ agonist)

c.Terazosin(α₁ selective antagonist)

d.Phenoxybenzamine (non-selective α antagonist)

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(β,α2 adrenoceptors)

c.Increased IP3 and DAG (α1

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 - 

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)

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

wrist-drop, 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

59.A patient manifesting with

wrist-drop, 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

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

62.Which of the following will confer

passive immunity?

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

62.Which of the following will confer

passive immunity

a.Diphtheriatoxoid b.Measles vaccine

c.Tetanus antitoxin

d.Oral polio vaccine