Final Pharmacology

Leonila A. Estole-Casanova, MDAssociate Professor 2

Department of Pharmacology and Toxicology

May 25, 2010

t Each of you has a STUDY & REVIEW METHOD that has worked best for you

t 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

propranololprototype 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 hypotensionaminoglycoside antibiotics ototoxicityhydralazine 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, MDAssociate Professor 2

Department of Pharmacology and Toxicology

May 25, 2010

t processes of absorption, distribution, metabolism and elimination

t what the Body does to the drug

t mechanisms of action what the Drug Does to the body

Molecular / Cellular level

Organism Population

ReceptorsAffinityDissociation constant (Kd)

Agonist, antagonist

Efficacy (Emax)Potency

Graded-dose response curve

Therapeutic WindowED50TD50Therapeutic 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.10mgb.10ugc.250 mgd.250 ug

t 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


Vd = D / C

D = C (Vd) = 5ug/ml (50,000ml) = 250,000ug or

250mg

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-lifeb. volume of distributionc. elimination clearanced. creatinineclearance

t 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 distributionCsteadystate - 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-lifeb. volume of distributionc. elimination clearanced. creatinineclearance

2.The process by which the amount of orally-administered drug is reduced before it reaches the systemic circulation a. First-order kineticsb. First-pass effectc. Pharmacokineticsd. Excretione. Metabolism

FIRST-ORDERt 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-ORDERt 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 asa. Distributionb. Excretionc. First-pass effectd. First-order eliminatione. 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 concentrationb. 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 concentrationb. 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 It 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 It P450-dependent

oxidations P450

independent oxidations (alcohol or aldehyde dehydrogenation deamination, decarboxylation)

Hydrolysis Reductions

PHASE II glucuronidationacetylationglycine 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. Deaminationb. Acetylationc. Glucuronidationd. Methylatione. Sulfate conjugation

84.The rate of acetylation is important with respect to the duration of action of:a. atropineb. cocainec. isoniazidd. acetaminophen

drugs induce P450

Increased rate of metabolism

drugs inhibit P450

potentiate the actions of other drugs

Phenytoincarbamazepine barbituratesrifampicinritonavirgriseofulvin chronic ethanol

toxicity

omeprazole DISULFIRAM erythromycinvalproic acidisoniazidcimetidine 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 enzymesb.Displacement from serum albuminc.Inhibition of metabolizing enzymed.Inhibition of uptake into adrenergic

neuron

86.The expected effect of toxic hepatitis on the rate of drug metabolism by the liver:a. Increasedb. Decreasedc.Unchangedd.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.Increasedb.Decreasedc.Unchangedd.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 3b. 4 to 5c. 6 to 7d. 8 to 9e. 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 3b. 4 to 5c. 6 to 7d. 8 to 9e. 10 or more

5.The dose or concentration required to bring about 50% of a drugs maximal effecta. Potencyb. ED50c. Efficacyd. Kde. Therapeutic index


Organism Population


Agonist, antagonist





t KdA measure of a drugs affinity for a

given receptorThe concentration of drug required in

solution to achieve 50% occupancy of its receptors


Organism Population


Agonist, antagonist





t 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


Organism Population


Agonist, antagonist





t 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

t Single number that quantifies the relative margin of safety of a drug in a population of people

Ratio of the TD50 to the ED50Median 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 effecta. Potencyb. ED50c. Efficacyd. Kde. 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 agonistb. Partial agonistc. Spare receptorsd. Inert binding sitee. Effector

t 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

albumin, alpha1-acid glycoproteinbinds drugs without initiating events leading

to drug effect)

t 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)

t Drugs that interact with and activate receptors

Drugs that possess BOTH affinity and efficacy

Full an agonist with maximal efficacyPartial 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 agonistb. Partial agonistc. Spare receptorsd. Inert binding sitee. 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 antagonistd. Chemical antagonist

t Antagonists interact with the receptor but do NOT change the receptor

they have affinity but NOefficacy

receptor vs non-receptor antagonistsreceptor antagonists:

competitive vs non-competitivenon-receptor antagonists:

chemical vs physiologic

t 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 receptorex. Phenoxybenzamine

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

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 antagonistd. 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. Physiologicb. Competitive c. Irreversible antagonistd. 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 concentrationb. Time to peak blood concentrationc. Product of the volume of distribution and

the first-order rate constantd. Volume of distributione. 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 concentrationc. Product of the volume of distribution and

the first-order rate constantd. Volume of distributione. 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 dosesa. Supersensitivityb. Tachyphylaxisc. Toleranced. Anaphylaxise. 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 dosesa. Supersensitivityb. Tachyphylaxisc. Toleranced. Anaphylaxise. Synergism

100.The interaction between an acetylcholinesterase inhibitor and acetylcholine at the neuromuscular junction would be an example of:a.Additionb.Potentiationc.Competitive antagonismd.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

t Aspirin is a weak acid with a pKaof 3.5stomach pH of 2.5?

Aspirin is a weak acid and is protonated when ph

Henderson-Hasselbalch equationpKaspirin = pHstomach + log HAA-

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 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 intestineb. pulmonary alveolic. the stomachd. arterial blood

85.A weak organic acid (pK=3) would be least ionized in:a.the small intestineb.pulmonary alveolic.the stomachd.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 approximatelya. 0.02 hb. 40 hc. 58 hd. 80 he. 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 Lclearance of 1.386 L/h?? the half-life

t1/2 = 0.693 xV dclearance

= 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 approximatelya. 0.02 hb. 40 hc. 58 hd. 80 he. 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 arteriesb. Decrease in the amount of

catecholaminesc. Decrease in requirement of the

myocardium for oxygend. 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 catecholaminesc. 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 arteriesb. Decrease in the amount of

catecholaminesc. Decrease in requirement of the

myocardium for oxygend. 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. Hydralazineb. Guanethidinec. 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. Hydralazineb. Guanethidinec. 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 secretionb. insulin secretionc. tissue sensitivity to insulind. tissue sensitivity to glycogen

17.Which of the following is reduced by the action of sulfonylurea hypoglycemic agents?a. glycogen secretionb. 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.Clozapineb.Amitriptylinec.Nortriptylined.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)d.Trazodone (MAO inhibitor)

Antichol Sedatingb.Amitriptyline (TCA) +3

+3

c.Nortriptyline (TCA) +1 +1

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.Clozapineb.Amitriptylinec.Nortriptylined.Trazodone

19.Which of the following has the lowest incidence of extrapyramidal reactions, but has the highest incidence of agranulocytosis among antipsychotic agents?a.Fluphenazineb.Pimozidec.Clozapined.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. Aspirinb. Ibuprofenc. Prednisoned. Indomethacine. 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 irreversiblya. Aspirinb. Ibuprofenc. Prednisoned. Indomethacine. Zileuton

21. Corticosteroids are usually indicated in the following conditions EXCEPT:a. Herpes simplex of the eyeb. Status asthmaticusc. Severe allergic rhinitisd. Nephrotic syndromee. Adrenal insufficiency

21. Corticosteroids are usually indicated in the following conditions EXCEPT:a. Herpes simplex of the eye

(infection)b. Status asthmaticusc. Severe allergic rhinitisd. Nephrotic syndromee. Adrenal insufficiency

22.Which of the following characterizes local anesthetics ?a.They generally block myelinated before

unmyelinated fibersb.They are generally administered along

with epinephrine to prolong its actionc.The primary action is on calcium

permeabilityd.Do not readily cross the blood-brain

barrier

t 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

t Block conduction in the following order: small myelinated axons, non-myelinated 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 anestheticsa.They generally block myelinated before

unmyelinatedfibers b.They are generally administered along

with epinephrine to prolong its actionc.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. Phenytoinb. Valproatec. Carbamazepined. Clonazepame. 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 CNSb. Blocks dopamine receptor sites in the CNSc. Makes acetylcholine more available in the CNSd. Facilitates the use of norepinephrine in the

CNSe. Makes dopamine more available in the CNS

Typical antipsychotics dopamine 2 receptor antagonists ex. Haloperidol

Chlorpromazine

Atypical antipsychotics Dopamine 2 receptor antagonistsserotonin 5-HT receptor antagonistsex. Clozapine

24.Which of the following is the mechanism of action of effective anti-psychotic agentsa. Decreases acetylcholine in the CNSb. Blocks dopamine receptor sites in the

CNSc. Makes acetylcholine more available in the CNSd. Facilitates the use of norepinephrine in the

CNSe. Makes dopamine more available in the CNS

25.Which of the following drugs can cause Stevens-Johnson syndrome, megaloblasticanemia, ataxia, and gingival hyperplasia?a. Phenobarbitalb. Disulfiramc. Phenytoind. Valproic acide. Carbamazepine

25.Which of the following drugs can cause Stevens-Johnson syndrome, megaloblastic anemia, ataxia, and gingival hyperplasia?a.Phenobarbital sedation, enzyme induction,

tolerance, dependenceb. Disulfiram- inhibits alcohol dehydrogenase;

flushing from acetaldehyde with ethanol intakec.Phenytoin- teratogenicd.Valproic acid- GI distress, hepatotoxicity (rare but

possible fatal), enzyme inhibition, teratogenice.Carbamazepine- diplopia, ataxia, enzyme

induction, blood dyscrasia

25.Which of the following drugs can cause Stevens-Johnson syndrome, megaloblasticanemia, ataxia, and gingival hyperplasia?a. Phenobarbitalb. Disulfiramc. Phenytoind. Valproic acide. Carbamazepine

26.A pure opioid antagonist with a greater affinity for receptors and used for acute opioid overdosea. Morphineb. Naloxonec. Codeined. Dextromethorpane. Diphenoxylate

26.A pure opioid antagonist with a greater affinity for receptors and used for acute opioid overdosea. Morphine strong opiod agonistb. Naloxone (antagonist)c. Codeine moderate opioid agonistd. Dextromethorpan NMDA receptor

blockere. Diphenoxylate u receptor agonist

(lomotil)

27. A patient with overdose toxicity of MDMA or ecstasy is UNLIKELY to manifest which of the following symptomsa. Agitationb. Hyperthermiac. Hyperreflexiad. Bradycardiae. Seizures

t 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 symptomsa. Agitationb. Hyperthermiac. Hyperreflexiad. 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 mechanismsa. Irreversible inhibition of ADP receptorb. Inhibition of thromboxane synthesisc. Reversible blockade of glycoprotein IIb/IIIad. Conversion of plasminogen to plasmine. 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, eptifabitideConversion of plasminogen to plasmin-

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

Posttranslational modification of vitamin K-dependent clotting factors- warfarin

t Inhibitors of phosphodiesterase 3 dipyridamole, cilostazol (increased CAMP inhibits platelet aggregation)

Irreversible inhibition of ADP receptor also ticlopidine

Inhibition of thromboxane synthesis- NSAIDsReversible blockade of glycoprotein IIb/IIIa

abciximab, tirofiban, eptifabitideConversion 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 mechanismsa. Irreversible inhibition of ADP receptorb. Inhibition of thromboxane synthesisc. Reversible blockade of glycoprotein IIb/IIIad. Conversion of plasminogen to plasmine. 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 Kb. Ascorbic acidc. EDTAd. Protaminee. 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 - warfarinb. Ascorbic acidc. EDTA lead poisoningd. Protamine - heparine. 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 marrowa. Erythropoietinb. Hemosiderinc. Transferrind. Folic acide. 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 marrowa. 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 B12e. 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 difficilea. Aztreonamb. Clavulanic acid c. Imipinemd. Cefepimee. 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 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 difficilea. Aztreonamb. Clavulanic acid c. Imipinemd. Cefepimee. Vancomycin

32.Which of the following cephalosporins is highly effective against pseudomonas?a. Cefazolinb. Cefuroximec. Ceftazidimed. Cefaclore. 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 +, HENPEcKe. 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 subunita. Clindamycinb. Erythromycinc. Chloramphenicold. Tetracyclinee. Linezolid

Drugs targeting the 30S ribosomal unit (SAT)

Drugs targeting the 50S ribosomal unit

Spectinomycin Chloramphenicol

Aminoglycosidegentamicinamikacin streptomycin

Macrolides erythromycinazithromycinclarithromycin

Tetracyclines LincosamidesclindamycinStreptograminsdalfopristin

Oxazolidones (linezolid)

33.Which of the following antibiotics inhibit microbial protein synthesis by binding to the 30S ribosomal subunit?a. Clindamycin 50sb. Erythromycin 50Sc. Chloramphenicol 50sd. Tetracycline -30Se. Linezolid 50S

34.Aminoglycoside toxicity includes the following EXCEPT:a. Auditory or vestibular damageb. Acute tubular necrosisc. Respiratory paralysis in high dosesd. Contact dermatitise. Encephalopathy

34.Aminoglycoside toxicity includes the following EXCEPT:a. Auditory or vestibular damageb. Acute tubular necrosisc. Respiratory paralysis in high dosesd. Contact dermatitis - neomycine. Encephalopathy does not cross

blood brain barrier

35.The following are drugs used in the treatment of Tuberculosis, EXCEPT:a.Ethambutolb.Rifampicinc.Streptomycined.Dapsonee.Ciprofloxacin

36.Urinary tract infection due to Chlamydia trachomatis will NOT respond to which of the following drug?a.Tetracyclineb.Erythromycinc.Nitrofurantoind.Ciprofloxacin

37.Which of the following drugs is a reverse transcriptase inhibitor that is useful in the treatment of Hepatitis B infectiona. Amantadineb. Ganciclovirc. amivudined. Interferon-alphae. Acyclovir

37.Which of the following drugs is a reverse transcriptase inhibitor that is useful in the treatment of Hepatitis B infectiona. Amantadine inhibitor of viral uncoating- influenza Ab. Ganciclovir antiherpesvirus nucleoside analoguec. Lamivudine antiHIV / anti HepaB virus

nucleoside analogued. Interferon-alpha immunoregulatorfor hepa C infe. 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 parasitea. Secondary tissue schizontsb. Exoerythrocyticschizontsc. Erythrocytic staged. Asexual formse. Liver stages

Blood schizonticidesArtemisinin & its derivativesLumefantrineChloroquineQuinineMefloquine

Tissue schizonticide - Primaquine

Radical cure of acute vivax and ovale malariaChloroquine eradicates erythrocytic formsPrimaquine - 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 parasitea. Secondary tissue schizontsb. Exoerythrocyticschizontsc. Erythrocytic staged. Asexual formse. Liver stages

39.Which of the following is the drug of choice for Schistosomahaematobium?a. Praziquantelb. Mebendazolec. Metronidazoled. Diethlcarbamazinee. Albendazole

39.Which of the following is the drug of choice for Schistosomahaematobium?a. Praziquantel tapeworm infectionsb. Mebendazole nematode infectionsc. Metronidazole amebiasis, giardiasis,

trichomoniasisd. Diethlcarbamazine - filariasise. Albendazole nematode infections

40. Drug of choice for the relief of acute exacerbations of asthmaa. Terbutalineb. Ipatropium bromidec. Cromolyn sodiumd. Montelukaste. Prednisone

40. Drug of choice for the relief of acute exacerbations of asthmaa. Terbutalineb. Ipatropiumbromide for COPDc. Cromolynsodium - controllerd. Montelukast - controllere. Prednisone - controller

41.Which of the following drugs is used to decrease uric acid production in gout?a.Allopurinolb.Aspirinc.Colchicined.Probenecide.Hydroxychloroquine

ACUTE GOUT CHRONIC GOUT

Leukocyte inhibitors

NSAIDsColchicineGlucocorticoids

Inhibitor of uric acid synthesis by inhibiting xanthineoxidase

Allopurinol

Agents that increase excretion of uric acid

SulfinpyrazoneProbenecid

41.Which of the following drugs is used to decrease uric acid production in gouta.Allopurinolb.Aspirinc.Colchicined.Probenecide.Hydroxychloroquine

42.Treatment for thyrotoxicosis does not include which of the following drugsa. Radioactive iodineb. Thyroglobulinc. Propylthiouracild. Potassium iodidee. Methimazole

42.Treatment for thyrotoxicosis does not include which of the following drugsa. Radioactive iodine b. Thyroglobulin protein synthesized

by thyroid follicular cells and secreted at the apical surface into the colloid space

c. Propylthiouracild. Potassium iodidee. Methimazole

43. Action of Sulfonylurea hypoglycemic agents does NOT includea. Stimulate release of endogenous insulinb. Reduce glucagon releasec. Increase functional insulin receptors in

peripheral tissuesd. 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 includea. Stimulate release of endogenous insulinb. Reduce glucagon releasec. Increase functional insulin receptors in

peripheral tissuesd. 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. Acarboseb. Glimepiridec. Metformind. Rosiglitazonee. Miglitol

44.Which of the following is most likely to cause hypoglycemia when used as a monotherapy for Type II diabetes?a. Acarbose GI distressb. Glimepiridec. Metformin GI distress, sl. Weight lossd. Rosiglitazone weight gaine. Miglitol GI distress

45.The hypoglycemic agent of choice in pregnant womena.Biguanidesb.Sulfonylureac.Insulind.Rosiglitazonee.Acarbose

46.Which of the following is NOT an effect of muscarinic blocking drugs?a.Miosisb.Constipationc.Reduced salivation and gastric secretiond.Urinary retentione.Bronchodilation

47.Which of the following is NOT a direct-acting cholinergic agonist?a. Bethanecholb. Carbacholc. Pilocarpined. Neostigminee. Nicotine

47.Which of the following is NOT a direct-acting cholinergic agonist?a.Bethanecholb.Carbacholc.Pilocarpined.Neostigmine cholinesterase

inhibitore.Nicotine

48.Cause of death from exposure to a high concentration of organophosphate insecticide will most likely be:a. Cardiac arrhythmiab. Respiratory failurec. Hypertensiond. Renal failuree. Gastrointestinal hemorrhage

t 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 bea. Cardiac arrhythmiab. Respiratory failurec. Hypertension d. Renal failuree. 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-1b.Alpha-1c.Alpha-2d.D1e.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 druga. Bronchodilationb. Vasodilationc. Decreased cardiac contractilityd. Pupillary constrictione. 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 druga. Bronchodilationb. 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. Metoprololb. Clonidinec. Prazosind. Ephedrinee. 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 alpha-antagonist, an example of which isa.Yohimbineb.Methyldopac.Terazosind.Phenoxybenzaminee.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 isa.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 hypertensionb.Glaucomac.Hypothyroidismd.Chronic heart failuree.Angina

53.The following is NOT a clinical use of beta-adrenoceptor antagonists:a.Portal hypertensionb.Glaucomac.Hypothyroidism (hyperthyroidism,

increases peripheral conversion of T4 to T3

d.Chronic heart failuree.Angina

54.Postsynaptic activation of Alpha-1 receptors will lead to the following cellular effectsa.Decreased intracellular calciumb.IncreasedcAMPc.Increased IP3 and DAGd.Inhibition of phospholipase activitye.Inhibition of Phosphodiesterase III

54.Postsynaptic activation of Alpha-1 receptors will lead to the following cellular effectsa.Decreased intracellular calciumb.IncreasedcAMP(,2 adrenoceptors)c.Increased IP3 and DAG (1

adrenoceptors, cholinergic muscarinicreceptors)d.Inhibition of phospholipase activitye.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.Phenylephrineb.Isoproterenolc.Dobutamined.Epinephrinee.Prazosin

55.Which of the following drugs will decrease heart rate in a normal heart but has little or no effect in a denervated hearta.Phenylephrine causes intense

vasoconstriction leading to reflex HRb.Isoproterenol - c.Dobutamine - d.Epinephrine - e.Prazosin - no effect

56.Which among the following is the most potent diuretic? a.Furosemideb.Hydrochlorothiazidec.Spironolactoned.Acetazolamidee.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.Methyldopab.Guanethedinec.Reserpined.Propranolole.Prazosin

58.A major air pollutant which can cause headache, tachycardia, and syncopea.Carbon monoxideb.Nicotinec.Nitrogen dioxided.Ozonee.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 followinga.Acute mercury poisoningb.Chronic mercury poisoningc.Iron poisoningd.Chronic lead poisoninge.Chronic arsenic poisoning

60.A child with diagnosed to have acute lead poisoning with signs and symptoms of encephalopathy should be givena.Acetylcysteineb.Deferoxaminec.EDTAd.Penicillaminee.Succimer

60.A child with diagnosed to have acute lead poisoning with signs and symptoms of encephalopathy should be givena.Acetylcysteine paracetamol poisoningb.Deferoxamine - Ironc.EDTAd.Penicillamine - Coppere.Succimer - Cadmium

61.A patient who suddenly deteriorated due to respiratory depression after being given diazepam may benefit from this antidote a.Flumazenilb.Acetylcysteinec.Atropined.Oxygene.Pralidoxime

61.A patient who suddenly deteriorated due to respiratory depression after being given diazepam may benefit from this antidote a.Flumazenilb.Acetylcysteinec.Atropine organophosphate poisoningd.Oxygene.Pralidoxime organophosphate poisoning

62.Which of the following will confer passive immunity?a.Diphtheriatoxoidb.Measles vaccinec.Tetanus antitoxind.Oral polio vaccinee.Purified protein derivative

62.Which of the following will confer passive immunitya.Diphtheriatoxoidb.Measles vaccinec.Tetanus antitoxind.Oral polio vaccinee.Purified protein derivative

63.Drug that blocks estrogen receptors in the pituitary gland increasing FSH and LH outputa. Clomipheneb. Diethylstilbesterolc. Danazold. Tamoxifene. Raloxifene

63.Drug that blocks estrogen receptors in the pituitary gland increasing FSH and LH outputa. Clomiphene - SERMb. Diethylstilbestrol non-steroidal

estrogen c. Danazol - antiandrogend. Tamoxifen - SERMe. Raloxifene SERM

64.Estrogen used in most combined hormonal contraceptivesa.Clomipheneb.Ethinylestradiolc.Estroned.DESe.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 phaseb.G0 phasec.G1 phased.G2 phase

Cell cycle Antineoplastic Drugs

M (mitosis) Cell division into two identical daughter cells

Inhibitors of microtubule function

G1 (gap 1) Active metabolism in the absence of DNA sythesis)

glucocorticoids

S (synthesis) Cell replication AntimetabolitesFolate pathway inhibitorsTopoisomerase inhibitors

G2 (gap 2) Cell preparation for mitosis

Antitumor antibioticsTopoisomerase inhibitors

t 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 phaseb.G0 phasec.G1 phased.G2 phase

66.By which of the following mechanisms do vinca alkaloids work in cancer chemotherapy?a.Inhibition of function of microtubulesb.Damage and prevention of repair of DNA c.Inhibition of purine synthesisd.Inhibition of DNA gyrasee.Inhibition of protein synthesis

66.By which of the following mechanisms do vinca alkaloids work in cancer chemotherapya.Inhibition of function of microtubulesb.Damage and prevention of repair of DNA

topoisomerase inhibitorsc.Inhibition of purinesynthesis

-mercaptopurined.Inhibition of DNA gyrasee.Inhibition of protein synthesis

67.Doxorubicin, a drug used in the treatment of Hodgkins disease belongs to which group of antineoplastic drugsa.Alkylating agentsb.Antimetabolitesc.Plant alkaloidsd.Antibioticse.Hormones

67.Doxorubicin, a drug used in the treatment of Hodgkins disease belongs to which group of antineoplastic drugsa.Alkylatingagents (cyclophosphamide)b.Antimetabolites (methotrexate) c.Plantalkaloids (vincristine)d.Antibioticse.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 likelya.Spironolactoneb.Hydrochlorothiazidec.Amilorided.Furosemidee.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 acidosisb.Hyperuricemiac.Hypoglycemiad.Hypocalcemiae.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.Hyperuricemiac.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.Enalaprilb.Furosemidec.Metoprolold.Clonidinee.Losartan

71.An anti-hypertensive agent which acts through nitric oxide, dilates arterioles but not veins, and causes a lupus-erythematosus-like syndromea.Minoxidilb.Nitroprussidec.Fenoldapamd.Hydralazinee.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.Diureticsb.Beta- adrenoceptor agonistsc.Calcium channel blockersd.ACE inhibitorse.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 drugsa.Lovastatinb.Ezetimibec.Niacind.Cholestyramine

74.Most potent H2 blocker with negligible binding with CYP450 enzymea.Cimetidineb.Famotidinec.Ranitidined.Nizatidine

75.A laxative usually given as suppository and promotes peristaltic action and defecation in 15-30 minutesa.Methylcelluloseb.Bisacodylc.Magnesium sulfated.Lactulose

Bulk-formers Hold water and expand in stool, promoting peristalsise.g Methylcellulose

Stool softeners Soften fecal material via detergent action that allows water to penetrate stoole.g. Docusate sodium

Stimulant laxative Direct irritation of intestinal mucosa leading to peristalsisBisacodyl (Dulcolax,Senokot)

75.A laxative usually given as suppository and promotes peristaltic action and defecation in 15-30 minutesa.Methylcellulose (bulk-former)b.Bisacodylc.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

daysb.Bismuth, PPI, Amoxicillin, Clarithromycin

for 4-6 weeksc.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 antibioticsProton 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

daysb.Bismuth, PPI, Amoxicillin, Clarithromycin for

4-6 weeksc.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 sitesb.Bromocriptine stimulates dopamine receptors c.Levodopa enhances the synthesis of

dopamined.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 sitesb. Bromocriptinestimulates dopamine

receptorsc. Levodopaenhances the synthesis of

dopamined. Selegelineis an inhibitor of monoamine

oxidase

t 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.Isoniazidb.Phenomymethyl penicillinc.Erythromycind.Tetracycline

t 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.Isoniazidb.Phenomymethyl penicillinc.Erythromycind.Tetracycline

79.Which of the following mechanisms is associated with bacterial resistance to B-lactampenicillins?a.bacterial production of lysozymesb.alteration of penicillin-binding proteins

(PBPs)c.increased metabolism of the penicillind.ability of the bacteria to produce an acid

media

80.Which of the following drugs exhibit linear kinetics?a.phenytoinb.penicillinc.digoxind.procainamide

80.Which of the following drugs exhibit linear kinetics?a.phenytoin, aspirin, ethanolb.penicillinc.digoxind.procainamide

81.The following drugs are metabolized in the liver, EXCEPT;a.Cefoperazoneb.Chloramphenicolc.Clindamycind.Amikacin

81.The following drugs are metabolized in the liver, EXCEPT;a.Cefoperazoneb.Chloramphenicolc.Clindamycind.Amikacin (kidney)

82.The following are time dependent antibiotics, EXCEPT:a.Ceftriaxoneb.Meropenemc.Erythromycind.Gentamicin

Rate of killing increases with drug concentration

a SINGLE very large dose can have a profound therapeutic effect and may be sufficient to eliminate the infection

Ex: AminoglycosidesQuinolonesBacitracin

t 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)

t Beta-lactamsvancomycinPolmyxinsPyrazinamide IsoniazidRifampinMetronidazole

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.Phenytoinb.Phenobarbitalc.Carbamazepined.Ethosuximide

83.Which of the following anti-epileptic drugs have active metabolites that are clinically significant?a.Phenytoinb.Phenobarbitalc.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 diureticb.sodiumnitroprussidec.reserpined.hydralazine

89.Drug with a low therapeutic index that induces delayed after-depolarization in cardiac tissue:a.quinidineb.isoproterenolc.adenosined.digoxin

90.An anti-arrhythmic drug known to produce a potentially fatal form of pulmonary fibrosisa.Lidocaineb.Amiodaronec.Sotalold.Procainamide

91.Which of the following anticancer drugs does not produce covalent modification of DNA or breakage of DNA strands?a.bleomycinb.cyclophosphamdiec.melphaland.vinblastine

t Alkylating agents ex cyclophosphamidemelphalan

t platinum compoundsex cisplatin

carboplatin

bleomycin

91.Which of the following anti-cancer drugs does not produce covalent modification of DNA or breakage of DNA strands?a.bleomycinb.Cyclophosphamidec.melphaland.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 cellsc.Do not damage the bone marrow cellsd.Are not cell cycle specific

t 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 depressionb.hallucinationsc.bradycardiad.decreased GI motility

93.All of the following pharmacological actions of morphine are mu opioid receptor responses, EXCEPT: a.respiratory depressionb.Hallucinations (behavioral

restlessness, hyperactivity)c.Bradycardia ? Postural hypotensiond.decreased GI motility

94.Which of the following provides information about the variation in sensitivity to a drug within the population studied?a.maximal efficacyb.therapeutic indexc.graded-dose response curved.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

t 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 efficacyb.therapeutic indexc.graded-dose response curved.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.fentanylb.ketaminec.propofold.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, hallucinationsc.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 doseb.the patients agec.the route of exposured.the duration of exposure

97.Three symptoms of atropine intoxication are:a.dry mouth, cutaneous vasodilatationb.dry mouth, spasm of accommodation,

miosisc.fever, dry mouth, CNS excitationd.fever, bed wetting, dry mouth

97.Three symptoms of atropine intoxication are:a.dry mouth, cutaneousvasodilatation b.dry mouth, spasm of accommodation,

miosisc.fever, dry mouth, CNS excitationd.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 receptorb.the B-1 adrenergic receptorc.a K+ channeld.adenylcyclase

98.Both acetylcholine and norepinephrine affect cardiac force of contraction. They do this by influencing:a.the M-2 muscarinic receptorb.the B-1 adrenergic receptorc.a K+ channeld.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

norepinephrineb.interfering with the storage of

norepinephrinec.interfering with the release of

norepinephrined.interfering with the metabolism of

norepinephrine

t 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

UPCM 2010 BOARDS ORIENTATION AND REVIEW COURSE IN PHARMACOLOGYSTUDY TIPS !!!STUDY TIPS!!!Try to organize things to accomplish the ff:Slide 5Slide 6Slide 7Slide 8PHARMACOKINETICSPHARMACOKINETICS (ADME)Slide 11Slide 12Slide 13Apparent volume of distribution (Vd) Slide 15Slide 16Slide 17LOADING DOSESlide 19Slide 20Slide 21Slide 22FIRST-PASS EFFECTSlide 24Slide 25Slide 26Slide 27Slide 28Pathways of drug metabolismSlide 30Slide 31Metabolism of isoniazidSlide 33Slide 34Slide 35Slide 36p450 INDUCersSlide 38Slide 39Slide 40Slide 41Slide 42Slide 43Slide 44AT STEADY STATE,Slide 46Slide 47`Dissociation Constant Slide 50EFFICACY vs potencySlide 52Therapeutic WINDOWTherapeutic INDEXSlide 55Slide 56Receptor drug theoryInert binding siteagonistSlide 60Slide 61antagonistCOMPETITIVE VS NON-COMPETITIVESlide 64CHEMICAL VS PHYSIOLOGICSlide 66Slide 67Slide 68Slide 69Slide 70Slide 71Slide 72Slide 73Slide 74Slide 75Slide 76Slide 77Slide 78Slide 79Slide 80Slide 81Slide 82Slide 83Half-life ClearanceSlide 86Slide 87Slide 88Slide 89Slide 90Slide 91Slide 92Slide 93Slide 94Slide 95Slide 96Slide 97Slide 98Slide 99Slide 100Slide 101Slide 102Slide 103Slide 104Slide 105Slide 106Local AnestheticsLocal anestheticsSlide 109Slide 110Slide 111Slide 112AntipsychoticsSlide 114Slide 115Slide 116Slide 117Slide 118Slide 119Slide 120Mdma or EcstacySlide 122Slide 123Slide 124Slide 125Slide 126Slide 127Slide 128Slide 129Slide 130Slide 131Slide 132Slide 133Slide 134Slide 135Slide 136Slide 137Slide 138Slide 139Slide 140Slide 141Slide 142Slide 143Slide 144Slide 145Slide 146Slide 147Slide 148Slide 149Slide 150Slide 151Slide 152Slide 153Slide 154Slide 155Slide 156Slide 157Slide 158Slide 159Slide 160Slide 161Slide 162Slide 163Slide 164Slide 165Slide 166Slide 167Slide 168Slide 169Slide 170Organophosphate poisoningSlide 172Slide 173Slide 174Slide 175Slide 176Slide 177Slide 178Slide 179Slide 180Slide 181Slide 182Slide 183Slide 184Slide 185Slide 186Slide 187Slide 188Slide 189Slide 190Slide 191Slide 192Slide 193Slide 194Slide 195Slide 196Slide 197Slide 198Slide 199Slide 200Slide 201Slide 202Slide 203Slide 204Slide 205Slide 206Slide 207Slide 208Slide 209Slide 210Slide 211Slide 212Slide 213Slide 214Slide 215Slide 216Slide 217Slide 218Slide 219Slide 220Slide 221Slide 222Slide 223Slide 224Slide 225Slide 226Slide 227laxativesSlide 229Slide 230Slide 231Slide 232Slide 233Slide 234Slide 235amantadineSlide 237TetracyclineSlide 239Slide 240Slide 241Slide 242Slide 243Slide 244Slide 245Slide 246Bactericidal agents Concentration vs time Slide 248time - dependentSlide 250Slide 251Slide 252Slide 253Slide 254Slide 255Slide 256Slide 257Slide 258Slide 259Agents that directly modify dna structureSlide 261Slide 262Slide 263Slide 264Slide 265Slide 266Slide 267Slide 268Graded vs quantalSlide 270Slide 271Slide 272Slide 273Slide 274Slide 275Slide 276Slide 277Slide 278Slide 279Slide 280Slide 281Slide 282Slide 283Slide 284

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Final Pharmacology