D&D Unit 1

Question 1

Bioavailability

Answer 1

F; %; amount of drug absorbed; extent of absorption

Question 2

Vd

Answer 2

L/kg; an abstract volume; inverse to drug in plasma (High Vd means drug is elsewhere)

Question 3

CL

Answer 3

ml/min/kg; clearance; Rin=Rout;

CL=[DOSE/tau]/Cpss

Question 4

Ke

Answer 4

1/hrs; change in Cp with time; from slope of lnCp vs time

Question 5

t1/2

Answer 5

hrs; =.693/Ke

Question 6

first order elimination

Answer 6

fraction eliminated; half life; 4-5 half lives to reach steady state

Question 7

zero order elimination

Answer 7

elimination of a constant amount per time

Question 8

pharmacology

Answer 8

interactions of drugs with biological systems

Question 9

pharmacotherapy

Answer 9

right drug, right does, interact with right drug target to produce desired therapeutic effects;
prevention, diagnosis, treatment or cure of disease

Question 10

pharmacokinetic

Answer 10

what the body does to the drug;

absorption, distribution, metabolism, excretion

Question 11

pharmacodynamic

Answer 11

receptor binding, signal transduction, physiological effect

Question 12

Cp

Answer 12

plasma concentration

Question 13

Cp vs time graph determines ***

Answer 13

pharmacokinetics

Question 14

MEC

Answer 14

minimum effective concentration

Question 15

time to steady state

Answer 15

4-5 half lives

Question 16

Rate of absorption ***

Answer 16

estimated as peak Cp or time to attain peak Cp; Tmax or Cmax

Question 17

physiology

Answer 17

identify potential targets

Question 18

pathophysiology

Answer 18

how the target should be manipulated

Question 19

pharmacology

Answer 19

select appropriate drug for disease

Question 20

absorption

Answer 20

passage of drug from site of durg administration into blood

Question 21

distribution

Answer 21

movement of the drug from bloodstream to tissues

Question 22

side effects

Answer 22

drug target at non-target system (therapeutic doses)

Question 23

extension effects

Answer 23

drug target at target system (higher than therapeutic doses)

Question 24

idiosyncratic reactions

Answer 24

immunologic and metabolic; less predictable and less common

Question 25

factors influencing absorption

Answer 25

molecular size, lipid solubility, degree of ionization, concentration gradient

Question 26

aqueous diffusion

Answer 26

water soluble; mw

Question 27

lipid diffusion

Answer 27

unionized moiety crosses membrane down concentration gradient; mw 500-800

Question 28

carrier-mediated diffusion

Answer 28

drugs mimic physiologic molecules

Question 29

increase rate of absorption

Answer 29

liquid preparation or rapidly disintegrating tablets

Question 30

decrease rate of absorption

Answer 30

enteric coated products or sustained release preparations

Question 31

rate of absorption from different routes

Answer 31

intravenous = inhalation > intramuscular > subcutaneous > oral

Question 32

bioequivalent

Answer 32

``` if rate (Cmax) and extent (bioavailability) that the active ingredient drug is absorbed and becomes available at the site of action is similar; 90% confidence interval of mean AUC and mean Cmax of T-test within 80%-125% of brand product ```

Question 33

enteral administration

Answer 33

in GI tract (oral and rectal)

Question 34

parenteral administration

Answer 34

outside GI tract

Question 35

oral

Answer 35

slow onset; varied bioavailability (0-100%)

Question 36

increased GI motility

Answer 36

increase rapidity of absorption

Question 37

rectal

Answer 37

slow onset; greater bioavailability than oral; 50% bypass liver; absprotion is irregular and incomplete

Question 38

sublingual - buccal

Answer 38

onset within minutes; high bioavailability; directly into vena cava;

Question 39

intravenous

Answer 39

rapid onset; bioavailability 100% by defn; most direct but most hazardous

Question 40

intramuscular

Answer 40

rapid; bioavailability approaches 100% (aqueous); deposit forms slower

Question 41

subcutaneous

Answer 41

slower; bioavailability approaches 100%; volume of dose limited

Question 42

inhalation

Answer 42

rapid onset; bioavailability 100%; large SA and high blood flow

Question 43

transermal

Answer 43

systemic conditions; first pass avoided; drugs must be potent (

Question 44

inhalation local

Answer 44

aerosolized particles | 10 um deposited in oropharynx (side effects)

Question 45

topical

Answer 45

local conditions; minimal systemic absorption (greater in children); skin or mucous membranes (vaginal-conjunctival-nasal-throat)

Question 46

Metabolism of active drug to more active compound

Answer 46

codeine to morphine; hydrocodone to hydromorphone

Question 47

Metabolism of inactive prodrug to active drug

Answer 47

omeprazole to a sulfenamide; enalapril to enalaprilat; valacyclovir to acyclovir

Question 48

Metabolism to toxic metabolite

Answer 48

acetaminophen to n-acetly-benzoquinoneimine (hepatotoxic)

Question 49

Oxidation reactions

Answer 49

Phase 1; hydrolysis, oxidation and reduction

Question 50

Phase 1 enzymes

Answer 50

CYP450, esterases-amidases, reductases

Question 51

Conjugation reactions

Answer 51

Phase 2

Question 52

Phase 2 enzymes

Answer 52

transferases; Glucuronidation, acetylation, glutathione / glycine / sulfate conjugation

Question 53

Induce-inhibit effects phase

Answer 53

Phase 1

Question 54

Which phase can be effected by age

Answer 54

Phase 1; decrease in 1/3

Question 55

Which phase can get saturated

Answer 55

Phase 2