Pharm Sci E 5

What are the units for steady-state concentration (Css), or infusion rate over clearance? a) mg/min b) ml/min c) mg/ml d) ml/mg e) min/mg

c) mg/ml

For a generic drug to be bioequivalent to an innovator drug (per FDA), it must be measured in ____ of subjects to fall within ____ of the mean of the test population bioavailability. A) 50; 50 B) 80; 20 C) 20; 80 D) 95; 5 E) 5; 95

B) 80; 20

The intensity of the pharmacologic action of a drug is most dependent on the (A) concentration of the drug at the receptor site. (B) elimination half-life (t½) of the drug. (C) onset time of the drug after oral administration. (D) minimum toxic concentration (MTC) of the drug in plasma. (E) minimum effective concentration (MEC) of the drug in the body.

(A) concentration of the drug at the receptor site.

Drugs that show nonlinear pharmacokinetics have which property? (A) A constant ratio of drug metabolites is formed as the administered dose increases. (B) The elimination half-life (t½) increases as the administered dose increases. (C) The area under the plasma drug concentration versus time curve (AUC) increases in direct proportion to an increase in the administered dose. (D) Both low and high doses follow first-order elimination kinetics. (E) The steady-state drug concentration increases in direct proportion to the dosing rate.

(B) The elimination half-life (t½) increases as the administered dose increases.

The earliest evidence that a drug is stored in tissue is (A) an increase in plasma protein binding. (B) a large apparent volume of distribution (VD). (C) a decrease in the rate of formation of metabolites by the liver. (D) an increase in the number of side effects produced by the drug. (E) a decrease in the amount of free drug excreted in the urine.

(B) a large apparent volume of distribution (VD).

Creatinine clearance is used as a measurement of (A) renal excretion rate. (B) glomerular filtration rate (GFR). (C) active renal secretion. (D) passive renal absorption. (E) drug metabolism rate.

(B) glomerular filtration rate (GFR).

Which of the following describes minimal effective concentration (MEC)? A. The minimal drug plasma concentration that can be detected B. The minimal drug plasma concentration to enter tissues C. The minimal drug plasma concentration to interact with receptors D. The minimal drug plasma concentration to produce effect

D. The minimal drug plasma concentration to produce effect

The half-life is A. dependent on the value of volume of distribution. B. dependent on the value of clearance. C. a function of the blood flow to clearing organs and the efficiency of the organ in extracting the drug. D. a function of the physiologic volume of blood and tissues and how the drug binds in blood and tissues. E. a and b.

E. a and b.

Half-life determines A. the time to reach steady state. B. the loading dose required to achieve the desired steady-state concentration. C. the maintenance dose required to achieve the desired steady-state concentration. D. the dosage interval. E. a and d.

E. a and d.

Pharmacokinetic models are useful to A. describe concentration-time data sets. B. predict drug serum concentrations after several doses or after different routes of administration. C. calculate pharmacokinetic constants (clearance, volume of distribution, half-life). D. a and c E. a, b, and c

E. a, b, and c

Characteristics of nonlinear pharmacokinetics include the following: A. The AUC is NOT proportional to the dose. B. The amount of drug excreted in the urine is not proportional to the dose. C. The elimination half-life may increase at high doses. D. The ratio of metabolites formed changes with increased dose. E. All of above do not relate to nonlinear pharmacokinetics F. All of the above are characteristics of nonlinear pharmacokinetics

F. All of the above are characteristics of nonlinear pharmacokinetics

An injection of two units of a drug once-daily (qd) will yield the same steady-state concentration as an injection of one unit of a drug twice-daily (bid). a) True b) False

a) True

Zero order elimination: a. Clearance is constant over the concentration range in clinical settings b. Elimination is linear and directly proportional to concentration c. Drug elimination is independent of the drug's concentration d. None of the above

c. Drug elimination is independent of the drug's concentration

Intermediate intravenous infusions are used to: a. Accumulate drug in the body b. Prevent MEC from being reached c. Prevent accumulation and toxicity d. Provide constant plasma drug concentration

c. Prevent accumulation and toxicity

The loading dose (DL) of a drug is usually based on the (A) total body clearance (ClT) of the drug. (B) percentage of drug bound to plasma proteins. (C) fraction of drug excreted unchanged in the urine. (D) apparent volume of distribution (VD) and desired drug concentration in plasma. (E) area under the plasma drug concentration versus time curve (AUC).

(D) apparent volume of distribution (VD) and desired drug concentration in plasma.

All of the following statements about plasma protein binding of a drug are true except which one? (A) Displacement of a drug from plasma protein binding sites results in a transient increased volume of distribution (VD). (B) Displacement of a drug from plasma protein binding sites makes more free drug available for glomerular filtration. (C) Displacement of a potent drug that is normally > 95% bound may cause toxicity. (D) Albumin is the major protein involved in protein binding of drugs. (E) Drugs that are highly bound to plasma proteins generally have a greater VD compared with drugs that are highly bound to tissue proteins.

(E) Drugs that are highly bound to plasma proteins generally have a greater VD compared with drugs that are highly bound to tissue proteins.

Creatinine clearance is used as a measurement of A. renal excretion rate. B. glomerular filtration rate (GFR). C. active renal secretion. D. passive renal absorption. E. drug metabolism rate.

B. glomerular filtration rate (GFR).

Volume of distribution determines A. the time to reach steady state. B. the loading dose required to achieve the desired steady-state concentration. C. the maintenance dose required to achieve the desired steady-state concentration. the dosage interval. D. a and d.

B. the loading dose required to achieve the desired steady-state concentration.

Clearance is A. dependent on the value of volume of distribution. B. dependent on the value of half-life. C. a function of the blood flow to clearing organs and the efficiency of the organ in extracting the drug. D. a function of the physiologic volume of blood and tissues and how the drug binds in blood and tissues. E. a and b.

C. a function of the blood flow to clearing organs and the efficiency of the organ in extracting the drug.

1. Which Clearance determines A. the time to reach steady state. B. the loading dose required to achieve the desired steady-state concentration. C. the maintenance dose required to achieve the desired steady-state concentration. the dosage interval. D. a and d.

C. the maintenance dose required to achieve the desired steady-state concentration. the dosage interval.

The volume of distribution is A. dependent on the value of clearance. B. dependent on the value of half-life. C. a function of the blood flow to clearing organs and the efficiency of the organ in extracting the drug. D. a function of the physiologic volume of blood and tissues and how the drug binds in blood and tissues. E. a and b.

D. a function of the physiologic volume of blood and tissues and how the drug binds in blood and tissues.

The following is a generalized plot showing plasma drug concentration levels after administration of multiple doses of the same drug, and levels of accumulation when equal doses are given at equal time intervals. The region indicated with a question mark can be described as the: a. steady state b. first-pass effect c. phase I conjugation d. first-order effect e. none of the above

a. steady state

For first-order drug elimination, half-life t(1/2) is ____ at two places on the curve and a constant ____ is lost per unit time. a) Equal; Amount b) Equal; Percentage c) Not equal; Amount d) Not equal; Percentage

b) Equal; Percentage

Increasing the rate of infusion changes the time necessary to reach the steady-state concentration. a) True b) False

b) False

1. The distribution of a drug agent may exhibit all the following schematic flows except: a. Drugs distribute rapidly to tissues with high blood flow (e.g., liver) and more slowly to tissues with low blood flow (e.g., adipose) b. Drugs rapidly cross capillary membranes into tissues because of active transport and hydrostatic pressure c.Drugs may accumulate in tissues as a result of their physicochemical characteristics or special affinity for the tissue (ex: lipophilic drugs accumulate in adipose tissue). d. Plasma protein binding of drugs affects drug distribution. e. None of the above

b. Drugs rapidly cross capillary membranes into tissues because of active transport and hydrostatic pressure

Intravenous infusion systemic absorption follows which order (if any): a. First order kinetics b. Zero order kinetics c. Second order kinetics d. None of the above

b. Zero order kinetics

To maintain a drug concentration at steady state, the dosing rate should equal the elimination rate. Which of the following is true? (CL = Drug Clearance) a) Dosing rate = CL + target concentration b) Dosing rate = CL - target concentration c) Dosing rate = CL * target concentration d) Dosing rate = CL / target concentration

c) Dosing rate = CL * target concentration

Which of the following is most useful in determining the rate of elimination of a drug, in general? a) Drug concentration in urine (renal elimination) b) Drug concentration in stool (bilary elimination) c) Drug concentration in blood d) Drug concentration in brain

c) Drug concentration in blood

For zero-order drug elimination, half-life t(1/2) is ____ at two places on the curve and a constant ____ is lost per unit time. a) Equal; Amount b) Equal; Percentage c) Not equal; Amount d) Not equal; Percentage

c) Not equal; Amount

Which of the following is/are plasma protein(s) that affect drug distribution? a. Albumin b. alpha 1 - glycoprotein c. Glycophorin d. A & B

d. A & B

Which of the following is NOT needed for drug bioequivalence? a) Same active ingredients b) Same strength or concentration c) Same dosage form d) Same route of administration e) Same side effects

e) Same side effects