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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


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 a. 1:100

membrane by lipid diffusion depends on b. 1:10
all of the following EXCEPT: c. 10:1
a. Drug size (diffusion constant) d. 100:1
b. Surface area of absorption 9. A characteristic of drugs eliminated by
c. Lipid partition coefficient zero order kinetics processes is that half-
d. Density of transporters life is not constant.
e. 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:

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

15. The volume of distribution of 20. Which route of drug administration is

gentamicin, a highly polar water-soluble most likely to lead to the first-pass
drug, is 14L per 70 kg. This reflects the effect?
distribution of gentamicin into: a. Sublingual
a. Plasma b. Oral
b. Plasma and blood c. Intravenous
c. Plasma, blood, and interstitial d. Intramuscular
fluid (extracellular water) 21. Parenteral administration:
d. Total body water a. Cannot be used with
e. Adipose tissue unconsciousness patients
16. First order kinetics b. Generally results in a less
a. Means rate of reaction is accurate dosage than oral
proportional to concentration administration
b. Are more common than zero c. Usually produces a more rapid
order kinetics response than oral
c. Apply to exponential processes administration
d. Generally apply to high plasma d. Is too slow for emergency use
concentrations (>20mg/100ml) 22. The volume of distribution (Vd) relates:
of ethanol a. Single to a daily dose of an
e. Result in steady state administrated drug
concentrations after multiple b. An administrated dose to a body
dosing weight
17. . Pharmacokinetics is: c. An uncharged drug reaching the
a. The study of biological and systemic circulation
therapeutic effects of drugs d. The amount of a drug in the
b. The study of absorption, body to the concentration of a
distribution, metabolism and drug in plasma
excretion of drugs 23. Biotransformation of the drugs is to
c. The study of mechanisms of render them:
drug action a. Less ionized
d. The study of methods of new b. More pharmacologically active
drug development c. More lipid soluble
18. What kind of substances cant permeate d. Less lipid soluble
membranes by passive diffusion? 24. Metabolic transformation (phase 1) is:
a. Lipid-soluble a. Acetylation and methylation of
b. Non-ionized substances substances
c. Hydrophobic substances b. Transformation of substances
d. Hydrophilic substances due to oxidation, reduction or
19. What does the term bioavailability hydrolysis
mean? c. Glucuronide formation
a. Plasma protein binding degree d. Binding to plasma proteins
of substance 25. Biotransformation of a medicinal
b. Permeability through the brain- substance results in:
blood barrier a. Faster urinary excretion
c. Fraction of an uncharged drug b. Slower urinary excretion
reaching the systemic c. Easier distribution in organism
circulation following any route d. Higher binding to membranes
d. Amount of a substance in urine
relative to the initial doze

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

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. If the half-life for decomposition of a drug is 12 hours, how long will it take for 125 mg of the drug
to decompose by 30%? Assume first-order kinetics and constant temperature.
2. A solution of a drug was freshly prepared at a concentration of 300 mg/ml. after 30 days at 25C,
the drug concentration in the solution was 75mg/ml.
a. Assuming first-order kinetics, when will the drug decline to one-half of the original
b. Assuming zero-order kinetics, when will the drug decline to one-half of the original
3. How many half-lives (t1/2) would it take for 99.9% of any initial concentration of a drug to
decompose? Assume first-order kinetics.
4. Exactly 300 mg of a drug are dissolve into an unknown volume of distilled water. After complete
dissolution of the drug, 1.0-ml samples were removed and assayed for the drug. The following
results were obtained:
Time (hr) Concentration (mg/ml)
0.5 0.45
2.0 0.3
Assuming zero-order decomposition of the drug, what was the original volume in which the drug
was dissolved?
5. The following data were obtained after assay of a drug:
Time (min) Drug A(mg)
10 96.0
20 89.0
40 73.0
60 57.0
90 34.0
120 10.0
130 2.5
Compute for the following:
a. Does the decrease in the amount of drug A appear to be a zero-order or first-order
b. What is the rate constant k?
c. What is the half-life t1/2?
d. What will be the concentration of Drug A after 50mins?
e. How much time will it take for Drug A to eliminate 99.9% of its concentration?

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


Part II. Problem Solving.

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