ADMET

Question 1

Disposition

Answer 1

-Distribution and elimination (Metabolism and Excretion)

Question 1

ADMET

Answer 1

-Absorption
-disposition (Distribution and elimination (Metabolism and Excretion)
-Toxicity

Question 2

elimination

Answer 2

-removal of drug via metabolism and excretion

Question 3

Toxicity

Answer 3

result of exposure

Question 4

Plasma vs Time curves

Answer 4

can determine each phase of ADMET

Question 5

Pharmacokinetic view

Answer 5

dresser (person) vs drawers (organs)

Question 6

Sampling sites (exposure)

Answer 6

-blood, plasma, serum
-urine

Question 7

Sites of delivery

Answer 7

-arterial
-venous
-SC,IM
-pulmonary
-oral

Question 8

Elimination site

Answer 8

-gut metabolism
-exhalation
-hepatic metabolism
-fecal excretion
-renal excretion

Question 9

Drug distribution

Answer 9

-dependent on physiochemical properties
-lipophillic vs hydrophillic

Question 10

Lipophilic drugs

Answer 10

-partition into fatty tissues

Question 11

Hydrophillic drugs

Answer 11

-partition into tissues where endothelium is permissive

Question 12

Pharmacokinetic Process

Answer 12

-defined by concentration vs time profiles
-compartments represent kinetically similar tissues
-reversible or irreversible
-linear or nonlinear
-fast and slow processes tend to disappear

Question 13

Differences in blood perfusion rates after drug distribution

Answer 13

-dictate organ distribution levels

Question 14

Distribution Limitations

Answer 14

-perfusion rate
-permeability rate
-convection
-diffusion

Question 15

Perfusion rate

Answer 15

-blood flow to tissues

Question 16

Permeability rate

Answer 16

-membrane permeability

Question 17

convection

Answer 17

-mechanism of transvascular transport
-pressure gradient

Question 18

Diffusion

Answer 18

concentration gradient

Question 19

Typical Plasma vs time curve

Answer 19

-increase to peak during absorption (Cmax, Tmax)
-decrease through the rest of the phases

Question 20

AUC

Answer 20

area under curve

Question 21

Tmax

Answer 21

time to reach maximum blood concentration

Question 22

Cmax

Answer 22

maximum blood concentration of dosage form

Question 23

Bioavailability

Answer 23

rate and extent of drug absorption

Question 24

Absolute bioavailability

Answer 24

AUC of given dosge form compared to AUC of same dose injected intravenously

Question 25

Relative bioavailability

Answer 25

AUC of given dosage form compared to arbitrary reference standard

Question 26

Bioequivalence

Answer 26

does NOT mean the therapeutic effect of the two dosage froms are equivalent

Question 27

Paracelsus

Answer 27

"everything is poison actually it's just the dose"

Question 28

Paraclesian theory

Answer 28

chemical may have no effect, beneficial effect or toxic effect

Question 29

dose-response relationship

Answer 29

-most important factor in pharmacology and toxicology

Question 30

Dose

Answer 30

-amount of chemical -local concentration of chemical at response site

Question 31

dose-receptor concentration

Answer 31

function of ADME

Question 32

Absorption rate (Kabs) defined by

Answer 32

-drug properties -excipient/drug composition -physiological barriers between GI tract and systemic circulation

Question 33

Absorption rate controlled by

Answer 33

-formulation parameters that are optimized to provide a Cmax and Tmax associated with safe and efficacious response = therapy is realized

Question 34

Influences of efficacy and safety

Answer 34

-duration of drug plasma concentration in the therapeutic window (Cmax and T max) -duration of chronic therapy

Question 35

Potential Worsening of disease

Answer 35

Prolonged exposure to subtherapeutic doses or ineffective drugs

Question 36

Therapeutic window

Answer 36

-concentration of drug between the minimum effective level and the minimum toxic level

Question 37

MTC

Answer 37

minimum toxic level

Question 38

MEC

Answer 38

minimum effective level

Question 39

True (A) or False (B): BIOAVAILABILITY is the fraction of an administered dose that reaches the systemic circulation intact.

Answer 39

True

Question 40

True (A) or False (B): Dosage forms are designed to convey performance by balancing the composition of the excipients, the drug’s physicochemical properties and to overcome the physiological barriers required for a safe and efficacious response.

Answer 40

True

Question 41

True (A) or False (B): When blinding clinical trials, it is often important to mask the ORGANOLEPTIC properties of the comparator and the drug being tested. These senses include sight, smell, taste, touch, and sound.

Answer 41

True

Question 42

True (A) or False (B): The STOMACH has a significantly increased surface area due to villi, folds of Keckring, and microvilli.

Answer 42

FALSE, intestine

Question 43

Which is NOT included in the acronym of ADMET?

Answer 43

Dissolution

Question 44

True (a) or False (f): The microenvironmental pH at the membrane surface may be different than the lumen based on the fact that the mucus and the glycocalyx have buffering effects.

Answer 44

True

Question 45

True (a) or False (b): Drug levels observed in the therapeutic window can be governed in part by transporters and metabolism, based on the compound being studied. Therefore, transporters and enzymes do not play an important role in drug product performance.

Answer 45

FALSE

Question 46

All of the following can reduce the bioavailability of an orally administered drug EXCEPT: a) Poor dissolution in the GI tract b) Poor penetration of the blood-brain barrier Ans c) Chemical degradation in the GI tract d) Poor solubility in the GI fluids e) Poor absorption across the GI mucosa