COLLEGE OF PHARMACY

3/F St. Therese Bldg.

900 San Marcelino St.
1000 Ermita, Manila
Tel. No.: (02) 521-2621
(02) 524-2011 local 390

Biopharmaceutics and Pharmacokinetics

MIDTERM EXAMINATION

General Instructions: Use blue or black ink only. STRICTLY NO ERASURES of any sort. You may use you test
questionnaire as your scratch. CHEATING OF ANY FORMS is strictly PROHIBITED. If you have concerns, do
not talk to your classmates. Ask the instructor/proctor. Anyone caught cheating will automatically get a
score of zero (0) in the exam.

1. The rate of drug transport across a cell b. 1:10

membrane by lipid diffusion depends on c. 10:1
all of the following EXCEPT: d. 100:1
a. Drug size (diffusion constant) 9. A characteristic of drugs eliminated by
b. Surface area of absorption zero order kinetics processes is that half-
c. Density of transporters life is not constant.
d. Concentration gradient a. True
2. A characteristic of absorption by lipid b. False
diffusion is its saturability at high drug 10. The plasma drug concentration versus
concentrations. time curve for a drug eliminated by zero
a. True order kinetics is linear.
b. False a. True
3. Drugs with low oil: water partition b. False
coefficients undergo lipid diffusion more 11. Drug metabolism is the process that
rapidly than drugs with high oil:water converts chemicals into less polar
partition coefficients. metabolites so that they are more
a. True difficult to excrete.
b. False a. True
4. The following IV administration, drugs b. False
are distributed fastest to: 12. All of the following are examples of
a. The skin, kidney, and brain Phase I drug metabolizing reactions
b. The liver, kidney, and brain EXCEPT:
c. The liver, adipose, and brain a. N-dealkylation of theophylline
d. The liver, kidney, and adipose b. Aliphatic oxidation of
e. The adipose, skin, and brain pentobarbital
5. A fundamental characteristic of all first c. Hydrolysis of succinylcholine
order pharmacokinetic process is that d. Glucuronidation of
the rate of the process is proportional to acetaminophen
drug concentration: e. Reductive dehalogenation of
a. True halothane
b. False 13. The termination of action of the
6. Competition between two drugs for preanesthetic muscle relaxant,
binding to plasma protein(s) can result in succinylcholine is markedly affected by:
the change in the concentration of free a. Redistribution from the brain to
drug and potential drug toxicity. the adipose tissue
a. True b. Enzyme induction
b. False c. Enzyme inhibition
7. At pH 9.0, morphine (a weak base d. Pharmacogenetic factors
containing an ionizable amine group, 14. For a drug that is eliminated primarily by
pKa of 7.0) would exist predominantly in renal glomerular filtration, the
the charged form. theoretical maximum clearance is
a. True approximately:
b. False a. 1-2 mL/min
8. At pH 5.0, the ratio of the protonated to b. 12 mL/min
unprotonated forms of morphine (a c. 120 mL/min
weak base containing an ionizable amine d. 1250 mL/min
group, pKa=7.0) would be: 15. The volume of distribution of
a. 1:100 gentamicin, a highly polar water-soluble

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drug, is 14L per 70 kg. This reflects the
distribution of gentamicin into:
a. Plasma
b. Plasma and blood
c. Plasma, blood, and interstitial
fluid (extracellular water)
d. Total body water
16. First order kinetics, EXCEPT
a. Means rate of reaction is
proportional to concentration
b. Are more common than zero
order kinetics
c. Apply to exponential processes
d. Generally apply to high plasma
concentrations (>20mg/100ml)
of ethanol
e. Result in steady state
concentrations after multiple
dosing
17. . Pharmacokinetics is:
a. The study of biological and
therapeutic effects of drugs
b. The study of absorption,
distribution, metabolism and
excretion of drugs
c. The study of mechanisms of
drug action
d. The study of methods of new
drug development
18. What kind of substances cant permeate
membranes by passive diffusion?
a. Lipid-soluble
b. Non-ionized substances
c. Hydrophobic substances
d. Hydrophilic substances
19. What does the term bioavailability
mean?
a. Plasma protein binding degree
of substance
b. Permeability through the brain-
blood barrier
c. Fraction of an uncharged drug
reaching the systemic
circulation following any route
administration
d. Amount of a substance in urine
relative to the initial doze
20. Which route of drug administration is
most likely to lead to the first-pass
effect?
a. Sublingual
b. Oral
c. Intravenous
d. Intramuscular
21. Parenteral administration:
COLLEGE OF PHARMACY
3/F St. Therese Bldg.
900 San Marcelino St.
1000 Ermita, Manila
Tel. No.: (02) 521-2621
(02) 524-2011 local 390
a. Cannot be used with
unconsciousness patients
b. Generally results in a less
accurate dosage than oral
administration
c. Usually produces a more rapid
response than oral
administration
d. Is too slow for emergency use
22. The volume of distribution (Vd) relates:
a. Single to a daily dose of an
administrated drug
b. An administrated dose to a body
weight
c. An uncharged drug reaching the
systemic circulation
d. The amount of a drug in the
body to the concentration of a
drug in plasma
23. Biotransformation of the drugs is to
render them:
a. Less ionized
b. More pharmacologically active
c. More lipid soluble
d. Less lipid soluble
24. Metabolic transformation (phase 1) is:
a. Acetylation and methylation of
substances
b. Transformation of substances
due to oxidation, reduction or
hydrolysis
c. Glucuronide formation
d. Binding to plasma proteins
25. Biotransformation of a medicinal
substance results in:
a. Faster urinary excretion
b. Slower urinary excretion
c. Easier distribution in organism
d. Higher binding to membranes
26. An example of a situation that would not
support therapeutic drug monitoring
with plasma drug concentration would
be one in which:
a. A wide variation in plasma drug
concentration is achieved in
different patients given a
standard drug dose
b. The toxic plasma concentration
is many times the therapeutic
concentration range
c. Correlation between a drugs
plasma concentration and
therapeutic response is positive.
27. For a drug with a narrow therapeutic
index the plasma concentration required
for their therapeutic effects is near the
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 COLLEGE OF PHARMACY
3/F St. Therese Bldg.
900 San Marcelino St.
1000 Ermita, Manila
Tel. No.: (02) 521-2621
(02) 524-2011 local 390

concentration that produces toxic b. False

effects. 29. The volume of distribution equals
a. True ______ divided by the initial drug
b. False concentration.
28. Highly perfused organs and blood a. Clearance
comprise what is usually known as b. Initial drug concentration
peripheral compartment. c. Half-life
a. True d. Dose

Match the drugs with their corresponding indications

30. Chloramphenicol A. Anticoagulant
31. Colchicine B. bronchial asthma
32. Digoxin C. HIV infection
33. Zidovudine D. CHF with atrial fibrillation
34. Minoxidil E. Non-Hodgkins lymphoma
35. Methotrexate AB. Typhoid infection
36. Theophylline AC. Multiple sclerosis
37. Phenytoin AD. Acute gout
38. Corticosteroid AE. Status epilepticus
39. Vancomycin BC. Baldness
40. Warfarin BD. MRSA infection

Match the drug with their corresponding adverse effects.

41. Chloramphenicol A. fetal hydantoin syndrome
42. Phenytoin B. Oral thrush
43. Corticosteroids C. hirsutism
44. Minoxidil D. Gray Baby syndrome
45. Warfarin E. Purple toe syndrome

Match the pharmacokinetic studies undertaken with each stage of pharmaceutical product
development.
46. Preclinical studies A. Biochemical studies
47. Phase I Clinical studies B. Fundamental pharmacokinetics
48. Phase II Clinical studies C. Pharmacokinetic parameters in patients
49. Phase III Clinical Studies D. Population pharmacokinetics
50. Phase IV Clinical studies E. Post-marketing surveillance

Part II. Problem Solving. Write all the necessary computations. Round-off your answers to 4 decimal
places. BOX YOUR FINAL ANSWER. (5 points each)
1. Drug Y is given by an intravenous injection and plasma concentration are then determined as
follows:
Time after injection Concentration
(hours) (mg/L)
0 12
1 9.8
2 7.9
3 6.4
4 5.2
5 4.2
6 3.4
7 2.8
8 2.2
Compute for the following:
a. Does the decrease in the amount of drug A appear to be a zero-order or first-order
reaction? Provide evidence for your answer.

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 COLLEGE OF PHARMACY
3/F St. Therese Bldg.
900 San Marcelino St.
1000 Ermita, Manila
Tel. No.: (02) 521-2621
(02) 524-2011 local 390

b. What is the rate constant k?

c. What is the half-life t1/2?
2. Theophylline is effective in the treatment of bronchitis at a blood level of 10-20mcg/ml. at
therapeutic range, theophylline follows first-order kinetics. The average t1/2 is 3.4 hours, and the
range is 1.8 to 6.8 hours. The average volume of distribution is 30 L.
a. The renal clearance of theophylline is 0.36 L/hr. what are the km and ke assuming all
nonrenal clearance is due to metabolism?
3. The initial plasma concentration of a drug given IV at 9:00am is 250 mg/ml. If the half-life of the
drug is 6 hours, perform a calculation to predict the plasma concentration will be at 9:00pm same
day.
4. The data in represent the average findings in antibiotic plasma samples taken from 10 humans
(average weight 70 kg), tabulated in a four-way crossover design.

Plasma Concentration (g/ml)

Time after Dose IV Solution Oral Solution Oral Tablet Oral Capsule
(hr) (2 mg/kg) (10 mg/kg) (10 mg/kg) (10 mg/kg)
0.5 5.94 23.4 13.2 18.7
1.0 5.30 26.6 18.0 21.3
1.5 4.72 25.2 19.0 20.1
2.0 4.21 22.8 18.3 18.2
3.0 3.34 18.2 15.4 14.6
4.0 2.66 14.5 12.5 11.6
6.0 1.68 9.14 7.92 7.31
8.0 1.06 5.77 5.00 4.61
10.0 0.67 3.64 3.16 2.91
12.0 0.42 2.30 1.99 1.83

( ) 29.0 145.0 116.0 116.0

a. From which oral drug product is the drug absorbed more rapidly?
b. What is the absolute bioavailability of the drug from the oral solution?
c. What is the relative bioavailability of the drug from the oral tablet compared to the
reference standard?
d. What is the total body clearance?

Formula:
= 0 + 0

ln = + 0

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 COLLEGE OF PHARMACY
3/F St. Therese Bldg.
900 San Marcelino St.
1000 Ermita, Manila
Tel. No.: (02) 521-2621
(02) 524-2011 local 390

EXAMINATION ANSWER SHEET

Part II. Problem Solving.

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