1.

A 50-kg woman was given a single IV bolus dose of an antibacterial drug at a dose level
of 6 mg/kg. Blood samples were taken at various time intervals. The concentration of the
drug (C p) was determined in the plasma fraction of each blood sample and the following
data were obtained. Assume the drug follows one compartment model.

t(hr) C p ( µg/mL)
0.25 8.21
0.50 7.87
1.00 7.23
3.00 5.15
6.00 3.09
12.0 1.11
18.0 0.40

When these data plotted on semilog graph paper, the graph showed an intercept of 8.4
and slope of -0.0751. Answer the following questions accordingly .
a) Calculate V D, k, and t 1/2 for this drug?
b) This antibacterial agent is not effective at a plasma concentration of less than
2µg/mL. What is the duration of activity for this drug?
c) How long would it take for 99.9% of this drug to be eliminated?
d) If the dose of the antibiotic were doubled exactly, what would be the increase in
duration of activity?
2. An antibiotic drug is to be given to an adult male patient (75 kg, 58 years old) by IV
infusion. The drug is supplied in sterile vials containing 30 mL of the antibiotic solution
at a concentration of 125 mg/mL. What rate in milliliters per hour would you infuse this
patient to obtain a steady-state concentration of 20µ g/mL? What loading dose would you
suggest? Assume the drug follows the pharmacokinetics of a one-compartment open
model. The apparent volume of distribution of this drug is 0.5 L/kg, and the elimination
half-life is 3 hours .
3. Explain why plasma protein binding will prolong the renal clearance of a drug that is
excreted only by glomerular filtration but does not affect the renal clearance of a drug
excreted by both glomerular filtration and active tubular secretion.
4. A drug has an elimination half-life of 2 hours and a volume of distribution of 40 L. The
drug is given at a dose of 200 mg every 4 hours by multiple IV bolus injections. Predict
the plasma drug concentration at 1 hour after the third dose.4.64
5. How would induction or inhibition of the hepatic enzymes involved in drug
biotransformation theoretically affect the pharmacokinetics of a drug that demonstrates
nonlinear pharmacokinetics due to saturation of its hepatic elimination pathway? Mention
the causes of nonlinear pharmacokinetics.
6. Discuss the common ways of increasing steady state concentrations of a drug

7.What affects average steady-state concentration?

8. Steady-state concentration can fluctuate depending on many factors.
Let’s talk about three of the main ones:
1. Dosing interval
 The dosing interval affects steady-state concentration in a
proportional way. The more frequently the drug is given, the
higher the steady-state concentration values.
2. Dose
 In the same way, higher doses will increase the Css values, and
lower doses will decrease them. The dose required to reach and
maintain steady state depends on the drug clearance rate, which
in turn can be affected by the patient’s demographic.
3. Drug clearance
 Drug clearance (CL) dictates the rate at which a drug is eliminated
from the body. The slower the clearance, the more of the drug will
remain in the system and the higher the Css (and vice versa).