Chapter 2 Part II

Question 1

what are the types of penetration

Answer 1

transcellular
intercellular
transappendageal

Question 2

the major route of permeation is around the

Answer 2

corneocytes

Question 3

the larger the corneocytes the ___ the route for permeation

Answer 3

longer

Question 4

transcellular penetration is

Answer 4

across the cells

Question 5

intercellular penetration is

Answer 5

between the cells

Question 6

transappendageal penetration is

Answer 6

via hair follicles, sweat, and sebumglands, and pilsebaceous apparatus

Question 7

what is the ideal log P for transdermal applications

Answer 7

1-3

Question 8

SC/IM injections are more ___ and ___ thank oral and rectal administration

Answer 8

fast and predictable

Question 9

which is slow absorption, SC or IM??

Answer 9

SC is slower

Question 10

unionized drugs have better or worse absorption through the cornea than ionized drugs

Answer 10

better

Question 11

what is an example of an unionized drug

Answer 11

physostigmine

Question 12

what is an example of ionized drug

Answer 12

neostigmine

Question 13

what are the three major types of factors that affect a drug from reaching its delivery site to target site

Answer 13

physiochemical property of drugs
physiological factors
formulation factors

Question 14

why are drugs most frequently taken by oral administration

Answer 14

most natural
uncomplicated
pain free
safe
economical
no sterilization needed

Question 15

many drugs are not administered orally primarily due to

Answer 15

instability of the drug in the GI tract or drug degradation by the digestive enzymes in the intestine

Question 16

give two examples of drugs that are not administered orally due to instability

Answer 16

erythropoietin/ human growth hormone - IM
insulin - subQ or IM

Question 17

absorption takes place across the ___ layer

Answer 17

epithelial

Question 18

how many ml of gastric fluid is in an empty stomach

Answer 18

100

Question 19

what is the pH range of the stomach

Answer 19

1-3

Question 20

What is the primary function of the stomach

Answer 20

to grind the solid dosage form and facilitate release and dissolution

Question 21

what are some reasons for minimal drug absorption from the stomach

Answer 21

thick mucus
limited surface area for absorption

Question 22

what is the most important region for oral drug absorption

Answer 22

small intestine

Question 23

why is the small intestine the most suitable for drug absorption

Answer 23

extremely large surface area and long residence time

Question 24

what is the residence time in the small intestine

Answer 24

4 hours

Question 25

most drugs are absorbed into the blood stream via capillaries by the

Answer 25

portal vein

Question 26

what is found on the epithelial cell surface that has contact with food

Answer 26

microvilli

Question 27

what is the function of microvilli

Answer 27

to increase the surface area by 20 fold

Question 28

the microvilli in the epithelium is known as the

Answer 28

brush border epithelium

Question 29

T or F microvilli are present in the large intestine

Answer 29

F, none in the large intestine/colon

Question 30

what is absorbed in the large intestine

Answer 30

water electrolyes

Question 31

part of the drug that is unabsorbed and reaches the colon is

Answer 31

excreted in the feces

Question 32

in which portions of the small intestine are villi most abundant

Answer 32

jejunum ileum

Question 33

ionization of the drug depends on its ____ and the ___ of the medium

Answer 33

pka pH

Question 34

a weak acid will be ____ ionized when the pH is above its pKa

Answer 34

more

Question 35

a weak base will be ____ ionized when the pH is below its pKa

Answer 35

more

Question 36

what are the two environments that orally administered drugs pass through

Answer 36

gastric and small intestinal

Question 37

gastric pH is highly acidic in the

Answer 37

fasting state

Question 38

after a meal, gastric pH becomes more _____

Answer 38

alkaline

Question 39

why does the gastric pH become more alkaline

Answer 39

because of the buffering effect of food

Question 40

T or F alkaline environment of the small intestine remains essentially consistent

Answer 40

T

Question 41

T or F weakly basic and acidic drugs remain ionized form in the stomach and intestine

Answer 41

T

Question 42

gastric emptying is the process in which

Answer 42

a swallowed drug quickly reaches the stomach which empties its content into the itnestine

Question 43

the time required for gastric emptying is called

Answer 43

gastric emptying time

Question 44

any delay in gastric emtpying time for the drug to reach the duodenum means that

Answer 44

the rate of absorption will slow, and the extent of absorption

Question 45

what is MMC

Answer 45

migrating motor complex

Question 46

what does MMC mean

Answer 46

pattern of peristaltic movement that occurs int eh GI tract during fasting

Question 47

how does peristaltic movement affect drug absorption

Answer 47

mixes the contents of the duodenum and brings the drug particles in contact with the duodenum

Question 48

when a drug is in the intestine, what is needed for optimum absorption

Answer 48

sufficient time

Question 49

what happens to absorption to a drug in case of diarrhea and why>

Answer 49

reduced absorption due to shorter and brief residence time

Question 50

What factors effect gastric emptying and intestinal motility

Answer 50

amount of food caloric content temperature viscosity

Question 51

an increase in the amount of food, _____ the emptying rate

Answer 51

decreases

Question 52

which has the smallest to highest caloric content

Answer 52

carb < protein < fat

Question 53

the higher the caloric content of the meal the _____ the delay to GE and delay to drug absorption

Answer 53

longer

Question 54

for which drugs is gastric emptying rate limiting?

Answer 54

paracetamol busulfan ampicillin riboflavin levetiracetam

Question 55

T or F hot solid meals significantly accelerate gastric emptying compared to room temperature meals

Answer 55

T

Question 56

a hgih viscosity within the intestinal lumen can ___ the diffusion rate of a drug and reduce its absorption

Answer 56

reduce

Question 57

T or F the physical form of food alters absorption

Answer 57

T

Question 58

an increase in the solid content of food ______ the emptying rate

Answer 58

decreases

Question 59

an increase in acidic content ___ the emptying rate

Answer 59

decreases

Question 60

why does an increase in acidic content decrease the emptying rate

Answer 60

acid has to be neutralized by pancreatic juices, intestional juices, and secretions after is is emptied

Question 61

T or F young people have a faster emptying rate than elderly

Answer 61

T

Question 62

what hormone increases GI transit time

Answer 62

progesterone

Question 63

progesterone increases GI transit time but decreses

Answer 63

esophageal sphinction tone

Question 64

stomach contents are emptied faster when ____ than ___

Answer 64

standing up lying down

Question 65

drugs absorbed after oral administration are transported via the _____ to the hepatic portal vein

Answer 65

mesenteric vessels

Question 66

first pass metabolism is when drugs that are highly metabolized by the liver or the intestinal mucosal cells have

Answer 66

poor systemic availability when given orally

Question 67

what two effects can food have

Answer 67

positive - enhanced cmax, higher F negative - reduced cmax, low F

Question 68

a drug can exhibit negative food effects if when coadministered the AUC

Answer 68

decreases

Question 69

which drugs does absorption decrease when given with food

Answer 69

penicillins erythromycin tetracyclines

Question 70

which drugs when given with food have delayed absorption

Answer 70

aspirin paracetamol diclofenac

Question 71

which drugs when given with food increase drug absorption

Answer 71

griseofluvins diazapam

Question 72

which drugs are unaffected in their absoprtion with food

Answer 72

methyl dopa propylthio uracil

Question 73

which drugs have no food effects

Answer 73

prednisolone hydrochlorothiazide ibuprofen

Question 74

which drugs have negative food effects

Answer 74

furosemide nadolol tacrine atenolol

Question 75

lipid soluble drugs are better absorbed with foods with

Answer 75

high fat content

Question 76

should lovastatin be taken with food

Answer 76

yes to increase F

Question 77

should rosuvastatin be administered with food

Answer 77

no taken on an empty stomach

Question 78

T or F high fiber diets may lower the efficacy of simvastatin, ezetimibe, pravastatin, and fluvastatin

Answer 78

T

Question 79

which drugs may or may not be taken without food

Answer 79

simvastatin ezetimibe pravastatin fluvastatin

Question 80

the binding of drugs also known as _____ to components in teh GI lumen can reduce their absorption

Answer 80

chelation

Question 81

ciprofloxacine F is reduced as a result of the presence of _______

Answer 81

enteral nutrition formula

Question 82

chelation to ____ is a food interaction reported with fluroquinolones, tetracyclines, and oral cephalosporins which limits absorption

Answer 82

metal ions

Question 83

_____ in the gut also affects absorption and metabolism of various drugs

Answer 83

microbiodata

Question 84

________ diet may decrease the absorption of TCA

Answer 84

high fiber

Question 85

T or F absorption may be influenced by circadian rhythyms

Answer 85

T

Question 86

lipophilic or water soluble drugs have better absorption rate when taken in the morning compared to evening

Answer 86

lipophillic

Question 87

the absorption of ketoconazole was ___ in the presence of omeprazole induced achlorhydria

Answer 87

reduced

Question 88

what two enzymes work synergistically to reduce bioavailability fo drugs

Answer 88

p glyco protein P450

Question 89

P glycoprotein is a

Answer 89

efflux transporter

Question 90

what drugs are affected by the synergy of p gp and CYP450

Answer 90

felodipine midazolam cyclosporine ritonavir digoxin intraconazole

Question 91

____ may inhibit the activity of CUP2C9

Answer 91

cranberry juice

Question 92

the primary enzyme involved in the metabolism of warfarin is

Answer 92

cyp2c9

Question 93

celiprolol is inhibited when taken with

Answer 93

orange juice

Question 94

what does the interaction between amiodarone and grapefruit lead to

Answer 94

increase in QT prolongation and vtach

Question 95

what are the three major disease state classes that influence the rate and extent of drug absorption

Answer 95

GI diseases cardiovascular disease hepatic disease

Question 96

what GI conditions alter drug absorption

Answer 96

crohns celiac GI surgery

Question 97

how does crohsn affect drug absorption

Answer 97

altered gut transit time, decreased gut SA and intestinal transit rate

Question 98

how does celiac disease affect drug absorption

Answer 98

destruction of villi and microvilli, increase gastric emptying time and altered intestinal drug metabolism

Question 99

how does GI surgery affect drug absorption

Answer 99

may cause drug dumping in the intestine

Question 100

patients with CHF have

Answer 100

reduced intestinal motility which decrease drug absorption

Question 101

patients with hepatic disease have altered drug absorption due to

Answer 101

liver cirrhosis affecting F

Question 102

which neurologic disease affects drug absorption due to diminished GI motility

Answer 102

parkisons disease