The Following Pharmacokinetic Properties of Drug X Should Be Used to Answer the Following Two

The following pharmacokinetic properties of drug X should be used to answer the following two

questions.

Oral Bioavailability = 81 %,

Clearance = 16.2 liters/hour,

Volume of Distribution = 20 liters

1. What i.v. loading dose of drug X (in mg) should be administered to reach an initial plasma

concentration of 0.05 mg/liter?

A. 0.1

B. 1

C. 10

D. 100

2. If oral tablets of drug X contain 12 mg of the drug, how often (in hours) will you administer a

tablet to maintain an average steady-state plasma concentration of 0.05 mg/liter?

A. 4

B. 8

C. 12

D. 24

3. Which class of drugs is currently approved for use in the management of both asthma and

allergic rhinitis?

A. α-adrenergic receptor agonists (e.g. phenylephrine)

B. β-adrenergic receptor agonists (e.g. terbutaline)

C. first-generation H1 receptor antagonists (e.g. diphenhydramine)

D. mucolytics (e.g. acetylcysteine)

E. cromones (e.g. cromolyn)

4. A patient is being maintained on corticosteroids by inhalation for long-term control of her

asthma. This has worked well until recently when she started undergoing short periods of minor

difficulties in breathing that were not associated with increased physical activity. Which of the

following drugs would be preferred to abort these intermittent attacks?

A. Monteleukast

B. Nedocromil

C. Ipratropium

D. Terbutaline

E. Theophylline

5. Spironolactone acts as a specific antagonist of

A. Na+ channels at site IV

B. K+ channels at site IV

C. the glucocorticoid receptor

D. K+ channels at site III

E. the aldosterone receptor

6. Drug X obeys a one-compartment model of distribution and its elimination is first order.Following i.v. administration of a loading dose of X, an initial plasma concentration of 18pg/liter is obtained. If the rate constant of elimination of the X is 0.248 hours", how long (inhours) will it take for the plasma concentration to fall from 18 to 6.7 µg/liter.

A. 2

B. 4

C. 6

D. 8

E. 10

7. Cholinergic receptor subtypes

A. utilize the same signal transduction mechanism.

B. elicit the same cellular response, although the signaling pathway may differ.

C. have a similar three dimensional structure.

D. recognize the same natural neurotransmitter, but can often be distinguished by

more selective drugs.

8. Codeine and dextromethorphane are effective antitussives because they both

A. induce analgesia

B. suppress activity of the "cough center" in the CNS

C. directly reduce sputum viscosity

D. act as local anesthetics on respiratory tract sensory receptors

E. stimulate secretion of low viscosity fluid

9. By definition, an inverse (negative) agonist

A. activates a compensatory reflex

B. interacts with an agonist and neutralizes it

C. inactivates a receptor, which has some activity in the unbound state

D. promotes desensitization of the receptor

E. inhibits recycling of the receptor

10. Which of the following antihypertensive agents would be the drug of choice to reduce blood

pressure in an elderly patient with bone loss because of low plasma Ca2+ levels?

A. Furosemide

B. Hydrochlorothiazide

C. Enalapril

D. Captopril

E. Prasozin

11. Which of the following drugs would be most likely to cause postural hypotension?

A. β1- receptor antagonist

B. β1- receptor agonist

C. α1-receptor agonist

D. α1 - receptor antagonist

E. α2 - receptor antagonist

CHOOSE THE SINGLE BEST ANSWER

Matching. Matching each of the following drugs with its site of action.

A. Distal Convoluted tubule

B. Proximal Tubule

C. Ascending loop of Henle

D. Proximal Tubule

E. Collecting Duct

12. _____ Metolazone

13. _____Triamterene

14. Probenecid is effective in treating gout because at high doses it decreases urate

A. biosynthesis

B. reabsorption

C. secretion

D. solubility

E. clearance by granulocytes

15. The alpha-latrotoxin produced by a black widow spider

A. Blocks effector cell interactions with acetylcholine

B. Facilitates effector cell interactions with acetylcholine

C. Blocks release of acetylcholine from synaptic vesicles

D. Facilitates release of acetylcholine from synaptic vesicles

E. Blocks termination of acetylcholine actions

16. Drug A is a weak acid and drug B is a weak base, and both drugs have a pK of 6.5. If a mixture

of the drugs is placed in two solutions of different pH separated by a semi-permeable membrane,

how will the total amount of A and B distribute between the two solutions at equilibrium?

A. A will accumulate at the higher pH and B at the lower pH

B. A will accumulate at the lower pH and B at the higher pH

C. both will accumulate at the lower pH

D. both will accumulate at the higher pH

17. An agent that is effective for the long-term control of asthma, but that has a narrow therapeutic

index and multiple drug-drug interactions is

A. theophylline

B. loratadine

C. salmeterol

D. diphenhydramine

E. dextromethorphane

18. Survival in congestive heart failure can be increased with ACE inhibitors and diuretics in

combination with the following drug

A. ephedrine

B. prazosin

C. carvedilol

D. dopamine

E. metaproterenol

19. Which of these side effects would NOT be expected with muscarine poisoning?

A. nausea and vomiting

B. paralysis of the diaphragm

C. bronchoconstriction

D. sweating

E. visual disturbances

20. Corticosteroids such as beclomethasone enhance the bronchodilator activity of β2-adrenergic

agonists by

A. slowing the metabolism of the β2-adrenergic agonists.

B. enhancing the absorption of the β2-adrenergic agonists.

C. being a bronchodilator itself.

D. increasing the number of β2-adrenergic receptors.

E. increasing the activity of phosphodiesterase.

21. The fastest relaxation of bronchial smooth muscle would be achieved with

A. epinephrine

B. salmeterol

C. dobutamine

D. amphetamine

E. yohimbine

22. Thiazide diuretics cause loss of Na+ because they inhibit a specific

A. Na+C1- co-transporter in the descending loop of Henle

B. Na+K+2C1- co-transporter in the distal convoluted tubule

C. Na+K+ co-transporter in the collecting duct

D. Na+ Cl- co-transporter in the distal convoluted tubule

E. Na+HCO3 transporter in the proximal tubule

23. Quantal dose response curves may be used to determine which of the following?

A. therapeutic index of a drug

B. slope of the dose response curve for a patient

C. variability in drug responses of individual patients

D. competitive vs. non-competitive antagonism

E. bioavailability of a drug

24. All of the following are mechanisms of action for drugs useful in the treatment of asthma

EXCEPT:

A. Inhibit release of inflammatory mediators

B. Induce smooth muscle relaxation

C. Bind circulating IgE antibodies

D. Inhibit release of neurotransmitters from adrenergic nerves

E. Block the action of ACh at muscarinic cholinergic receptors

25. Nicotinic cholinergic and muscarinic cholinergic receptors can be distinguished from each other

by the relative effects of

A. Bethanechol and pilocarpine

B. Epinephrine and propranolol

C. Epinephrine and norepinephrine

D. Atropine and curare

E. Acetylcholine and epinephrine

26. If the renal clearance of a drug is 550 ml/min., it must be

A. eliminated in its first Pass through the kidney

B. cleared by both renal and hepatic mechanisms

C. extensively bound to plasma proteins

D. filtered and secreted in the kidney

E. well distributed throughout the kidney

27. Norepinepbrine most directly inhibits adenyly cyclase by binding to which of the following

adrenergic receptors?

A. α1

B. α2

C. β1

D. β2

28. A commonly used herbal remedy to "boost" the immune system during the common cold is

A. Kava

B. Majuang

C. Aloe vera

D. Black cohosh

E. Echinacea

29. The efficacy of a drug is most dependent upon which of the following?

A. bioavailability of the drug

B. affinity of the receptor for the drug

C. fraction of drug bound to plasma proteins

D. ability of the drug to activate the receptor

E. clearance of the drug

30. Which of the following is a consequence of the activity of losartan?

A. Increased bradykinin degradation

B. Decreased bradykinin degradation

C. Increased activity at angiotensin type 2 (AT-2) receptors

D. Increased activity at angiotensin type 1 (AT-1) receptors

E. Decreased production of angiotensinogen

31. Which of the following should NOT be used to treat hypertension in a patient with asthma?

A. Propranolol

B. Hydrochlorothiazide

C. Losartan

D. Enalapril

E. Prazosin

32. Which of the following drugs can be coadministered with neostigmine in treatment of patients

with myasthenia gravis to reduce cholinergic side effects without blocking the effect of

neostigmine on skeletal muscle?

A. d-Tubocurarine

B. Succinylcholine

C. Atropine

D. Edrophonium

E. Pilocarpine

33. The proximal tubule anion secretion system is important for the action of hydochlorothiazide

because the drug

A. requires an acidic environment

B. acts on the tubular side of the nephron

C. is inhibited by uric acid

D. is highly charged

E. acts in that region of the nephron

Matching. Each may be used once, more than once, or not at all.

A. Trimethaphan

B. Ipratropium

C. Succinylcholine

D. d-Tubocurarine

E. Pralidoxime

34. _____ Rapidly hydrolyzed by plasma cholinesterases

35. _____ Produces a nondepolarizing neuromuscular blockade

36. The topical corticosteroid budesonide is useful in the treatment of allergic rhinitis because it

causes all of the following EXCEPT:

A. Decreased numbers of inflammatory cells in the nasal epithelium

B. Decreased nasal epithelial permeability

C. Decreased response to stimulation of cholinergic nerves to nasal epithelium

D. Inhibition of nasal leukotriene production

E. Relaxation of vasculature in the nasal epithelium

37. ADH (anti-diuretic hormone) acts to increase

A. the pressure in the collecting duct

B. insertion of aquaporin 2 into the apical membranes at site IV

C. urate filtration in the glomerulus

D. free water clearance in the glomerulus

E. breakdown of the basement membrane at site IV

38. Intravenous infusion of drug X at a dose rate of 1 µg/hour produces a steady-state plasma drug

concentration of 0.05 µg/liter. What is the total body clearance (in liters/hour) of the drug?

A. 5

B. 10

C. 15

D. 20

E. 25

39. Which of the following would be effective in treating a patient with hypercalcemia?

A. Metolazone

B. ethacrinic acid

C. Spironolactone

D. Triamterene

E. Prazosin

40. A change in which of the following parameters may reduce the maximum response (i.e.

efficacy) to a drug as seen on a graded dose response curve?

A. absorption

B. distribution

C. elimination

D. receptor affinity

E. receptor number

41. Muscarinic antagonists are useful in treating all of the following conditions EXCEPT?

A. postoperative urinary retention

B. anticholinesterase poisoning

C. chronic obstructive pulmonary disease,

D. Parkinson's Disease

E. motion sickness

42. Polymorphisms in which of the following genes are responsible for the greatest number of

pharmacogenetic variations in drug metabolism?

A. N-acetyltransferase

B. plasma cholinesterase

C. glucose-6-phosphate dehydrogenase

D. the CYP2 family of P450s

43. All of the following enhance adrenergic neurotransmission EXCEPT

A. tyramine

B. cocaine

C. pargyline

D. clonidine

E. phenylephrine

44. A drug is metabolized exclusively by hepatic glucuronyl transferase (GT). With chronic

administration of the drug, a patient's graded dose response curve shifts to the right. This change

in the dose response curve results from which of the following?

A. a decrease in the Km of GT

B. an increase in the Vmax of GT

C. increased synthesis of GT

D. decreased degradation of GT

E. activation of GT by reactive metabolites

45. Of the following, which would be the best choice for treating an acute attack of gout?

A. aspirin

B. allopurinol

C. Probenecid

D. colchicine

E. hypoxanthine

46. The direct effect of G proteins coupled to α1-adrenergic receptors is to

A. inhibit adenylyl cyclase

B. activate phospholipase C

C. inhibit synthesis of nitric oxide

D. activate guanylyl cyclase

47. Which of the following reverses the muscle relaxant effects of d-tubocurarine?

A. Neostigmine

B. Atropine

C. Scopolamine

D. Succinylcholine

E. Ether

48. Which of the following is the correct ranking, from lowest to highest, of the maximum amount of

sodium excretion that could be accomplished with these diuretics?

A. spironolactone < furosemide < hydrochlorothiazide < acetazolamide

B. acetazolamide < spironolactone < hydrochlorothiazide < furosemide

C. hydrochlorothiazide < furosemide < spironolactone < acetazolamide

D. furosemide = hydrochlorothiazide, acetazolamide, spironolactone

E. acetazolamide < furosemide < hydrochlorothiazide < spironolactone

49. How will the addition of a chemical substituent that increases the pK of a weak acid with a

molecular weight of 250 affect its rate of absorption from the stomach and its rate of elimination

in the urine?

A. increase absorption and increase elimination

B. increase absorption and decrease elimination

C. decrease absorption and increase elimination

D. decrease absorption and decrease elimination

50. Manufacturers of nutriceuticals are able to "advertise" their effectiveness for certain diseases

without regulation from FDA by

A. Doing limited clinical trials

B. Not making specific drug claims

C. Showing appropriate animal studies

D. Comparing themselves with an FDA approved agent

E. Getting congressional pressure for right to market

51. Thiazide diurectics cause potassium loss because they

A. stimulate Na+ reabsorption and K+ excretion at site IV

B. inhibit K+ reabsorption at site I

C. inhibit HCO3- reabsorption at site I

D. stimulate K+ secretion at site III

E. inhibit anion-K+ exchange at site I

52. Massive activation of the sympathetic nervous system directly causes

A. release of NE from fibers innervating eccrine sweat glands on the back

B. bradycardia

C. terror-induced defecation

D. contraction of circular (constrictor) muscle in iris

E. increased tonic release of NE in arterioles of small intestine

53. Tricyclic antidepressants

A. block re-uptake of NE into sympathetic nerve terminals

B. block monoamine oxidase

C. block α2-adrenergic receptors

D. act indirectly to cause non-exocytotic release of NE

54. A commonly used herbal remedy for depression is

A. Ginko baloba

B. Evening Primrose

C. Garlic

D. St. John's wort

E. Saw palmetto

55. Allopurinol

A. decreases urate production

B. increases hypoxanthine biosynthesis

C. increases hypoxanthine secretion

D. increases urate secretion

E. decreases prostaglandin biosynthesis

56. A patient initially receiving drug X alone, begins receiving cimetidine which inhibits the P450

catalyzed metabolism of X to an inactive metabolite. What is the effect of cimetidine on the

patient's dose response curve to X7

A. increase the efficacy

B. decrease the efficacy

C. increase the potency

D. decrease the potency

ANSWERS: