Week 1

Question 1

Pharmacokinetics (PK)

Answer 1

What the body does to the drug - physiological processes that affect drug concentration in the body.

Question 2

Pharmacodynamics (PD)

Answer 2

What the drug does to the body - pharmacological response and subsequent clinical outcome resulting from the drug concentration.

Question 3

Absorption

Answer 3

Transportation of unmetabolized drug from the administration site to body circulation.

Question 4

Distribution

Answer 4

Dispersment of unmetabolized drug as it moves through the body’s blood and tissues.

Question 5

Excretion

Answer 5

Irreversible loss of a drug.

Question 6

Routes of excretion

Answer 6

Kidneys (Urine), Feces, Bile, Breast Milk, Saliva, Sweat.

Question 7

Phase 1 Metabolism

Answer 7

Oxidation, epoxidation, dealkylation, and hydroxylation reactions catalyzed by the cytochrome P450 enzyme system.

Question 8

Phase 2 Metabolism

Answer 8

Glucoronidation and sulfation processes.

Question 9

Elimination

Answer 9

Sum of drug excretion and metabolism.

Question 10

Disposition

Answer 10

Kinetic time-course of drug distribution, excretion, and metabolism

Question 11

Passive diffusion

Answer 11

Movement of drug using a concentration gradient from higher drug concentration to lower drug concentration until an equilibrium is reached.

Question 12

Plasma protein factors influencing drug binding

Answer 12

Total concentration of available plasma protein

Question 13

Comorbid conditions influencing drug binding

Answer 13

Diseases may alter plasma protein levels or binding affinity

Question 14

Drug interactions influencing drug binding

Answer 14

Competitive binding by two drugs for the same plasma protein. Alterations in binding affinity by one drug affecting another drug.

Question 15

Inducers

Answer 15

Increase activity of specific cytochrome P450 isoenzymes, leading to increased metabolism of drugs that are substrates of that particular isoenzyme.

Question 16

Inducers effects on plasma concentration

Answer 16

Decreased therapeutic effects

Question 17

Inhibitors

Answer 17

Decrease metabolism of drugs that are substrates, increasing substrate plasma concentration.

Question 18

Inhibitors effects on plasma concentration

Answer 18

Enhanced pharmacological effects and enhanced toxicological effects.

Question 19

Glomerular filtration rate

Answer 19

Measurement that indicates how much of plasma volume has been filtered by the glomerulus per unit of time

Question 20

Active Secretion

Answer 20

Active transport process requiring energy. Occurs following glomerular filtration.

Question 21

Reabsorption

Answer 21

Active or passive process that places drugs back into the plasma

Question 22

pH influence on reabosprtion

Answer 22

pH of renal tubules influences amount of drug reabsorbed

Question 23

Negative consequence of active secretion

Answer 23

Drugs competing for the same transport process can result in drug interactions.

Question 24

Bioavailability

Answer 24

Rate and extent of drug absorption; percentage or fraction of the parent compound that reaches systemic (plasma) circulation. Typicall denoted as “F”

Question 25

Factors influencing bioavailability

Answer 25

food and drug interactions; gastrointestinal motility; first pass metabolism; route of administration.

Question 26

Rate of absorption

Answer 26

Influences onset of action for drugs

Question 27

Absolute bioavailability

Answer 27

Determined by comparing bioavailability of an extravascular route of administration against bioavailability of the same drug administered intravenously.

Question 28

Area Under the Curve

Answer 28

Extent of absorption, but not the rate.

Question 29

Clearance

Answer 29

Volume of blood that is completely cleared of the drug per unit of time.

Question 30

Components of drug clearence

Answer 30

Metabolism and elimination

Question 31

Liver

Answer 31

Organ primarily responsible for drug metabolism.

Question 32

Kidneys

Answer 32

Organ primarily responsible for parent drug and metabolite excretion (filtration and secretion).

Question 33

Volume of Distribution

Answer 33

Extent of drug distribution into the tissue from the blood.

Question 34

Factors influencing Vd

Answer 34

Physicochemical properties of a drug, plasma protein binding, tissue binding.

Question 35

Low Vd

Answer 35

Large fraction of drug stays in blood plasma and little amount of drug has permeated into the extravascular tissue.

Question 36

High Vd

Answer 36

Substantial drug permeation into the tissue(s) and extensive tissue distribution.

Question 37

Loading Dose

Answer 37

Larger than maintenance doses used to reach a steady state of drug concentration more rapidly.

Question 38

Loading dose requirement for drugs with high Vd

Answer 38

Larger dose required

Question 39

Loading dose requirement for drugs with low Vd

Answer 39

Smaller dose required

Question 40

Creatinine Clearance

Answer 40

Measure of how well the kidneys filter creatinine from the blood and excrete it in the urine.

Question 41

Elimination Constant (K)

Answer 41

Percentage or fraction of the amount of drug that is cleared from the body per unit time

Question 42

Effects on clearance of a large Elimination Constant (K)

Answer 42

Rapid elimination of the drug

Question 43

Effects on clearance of a small Elimination Constant (K)

Answer 43

Decreased elimination of the drug.

Question 44

Half-life

Answer 44

Amount of time it takes for a drug in the body to be reduced by 50%

Question 45

What does the half-life predict?

Answer 45

Amount of time it takes for a patient to achieve steady-state drug concentrations.

Question 46

Number of half-lifves to reach steady state

Answer 46

Four to Five

Question 47

First pass effect

Answer 47

Decreases active drug's concentration upon reaching systemic circulation or its site of action after being metabolized.

Question 48

Carrier-mediated membrane transporters

Answer 48

Specialized carrier-metiated membrane transport systems move ion and nutrients in the body.

Question 49

Active diffusion

Answer 49

Enables movement of drugs from regions with low drug concentrations to regions with higher drug concentrations.

Question 50

Lipophilic Compounds

Answer 50

Fat solubule; easily diffuse across lipid bilayers of cell membranes; bioransformed in the liver; excreted through the bile duct.

Question 51

Hydrophilic Compounds

Answer 51

Water soluble; cross lipid layer via facilitated transport; eliminated by kidneys.

Question 52

Zero-order kinetics

Answer 52

The rate of metabolism/elimination remains constant and is independent of the concentration of a drug. 

Question 53

First-order kinetics

Answer 53

The rate of metabolism/elimination is directly proportional to the plasma concentration of the drug.

Question 54

Clinical Significance of Antagonism

Answer 54

Effects of noncompetitive inhibitors cannot be overcome by increasing the dose, whereas increasing dose can overcome competitive inhibition.

Question 55

Implications of Drug Tolerance

Answer 55

Clinician must decide whether to increase the dose to achieve similar outcomes previously achieved at a lower dose.