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Pharmaceutics Spring 2016 > Bioavailability > Flashcards

Flashcards in Bioavailability Deck (48)
1

Generic drugs are ____ and ____ alternatives to brand name prescriptions

safe and effective

2

T/F One of the primary ways physicians can practice cost effective prescribing is by offering patients a generic medicine when one is available

TRUE

3

When can a generic be created?

once the patent expires on the innovator

4

What are the applications of bioavailability and bioequivalence studies? (5)

-determine the effect of various formulations
-determine food effects
-evaluate the effect of age, disease, etc
-assess route of administration effect or first pass effect
-ANDA

5

ANDA

abbreviated new drug application--> used for the approval of generic drugs

6

The goal of bioavailability studies is to....

control all the variables except for the one you are testing

7

bioequivalent= similar

bioavailability

8

Steps for bioavailability study? (5)

1. recruit healthy volunteers
2. administer the drugs to volunteers
3. Collect samples of biological fluids (typically blood)
4. Analyze
5. Draw graph

9

availability

-measure of relative amount absorbed (looking at ratios of AUC)
-range from 0 to 1

10

______ compares AUC to an IV DOSE

absolute availability

11

_______ compares AUC to a reference

relative availability

12

Which availability is used for ANDA?

relative

13

How can you calculate the total amount absorbed?

absolute availability

14

A test oral formulation has the same area under the plasma concentration-time curve as the reference formulation. This means that the two formulations...
A) are bioequivalent by definition- related to AUC
B) deliver the same total amount of drug to the body but are not necessarily bioequivalent
C) are bioequivalent if they both meet USP dissolution standards
D) deliver the same total amount of drug to the body and are, therefore, bioequivalent
E) have the same rate of absorption

B) deliver the same total amount of drug to the body but are not necessarily bioequivalent because the rate may be different (if the rate is dif. Then they may not be considered bioequivalent)

15

excretion vs. metabolism

excretion: drug is unchanged
metabolism: drug is converted to some other form

16

urinary excretion studies

graph the cumulative excretion

17

T/F Urinary Excretion studies increase and then decrease.

FALSE: starts at zero--> increases until it plates--> It NEVER decreases because it is cumulative

18

When a cumulative excretion graph plateaus, what does this mean?

all the drug is out of the body; time to plateau is related to the rate of absorption

19

Potassium Penicillin G was given IV to volunteers, 80% of a 500mg dose was recovered unchanged in the urine. 280 mg was recovered in urine when the same dose was given IM to the same subjects. Calculate the availability of the IM injection. What type of availability is this?

F = 280/400 = 0.70; absolute

20

urinary excretion studies are used for.. (2)

-drugs extensively eliminated in the urine
-drug where UT is site of action

21

For valid estimates in the urinary excretion studies... (3)

-excretion to extent of greater than 25%
-analysis must be specific for unchanged drug
-complete urine collection

22

_____ the study design usually used for bioavailability/ bioequivalence testing

crossover design (typically single dose study)

23

Crossover designs have a period known as wash out period...what does this mean?

allows time for all the drug from the first round to be completely out of the system before administering the next

24

______ proof of bioequivalence is required for generic products

reference product

25

the reference is the _____ product. What does the reference product have to have?

innovator: NDA (new dug application) have to show efficacy and safety

26

Bioequivalence criteria?

you want EVERYTHING to be the same--> to show that the PRODUCT is the reason for any differences in the outcome

27

______ or ____ are used for bioequivalence testing

90% confidence interval or two, one sided t-test

28

90% confidence interval or two, one sided t test:
-Bioequivalent if entire range is between _____ and _____
- testing the ____
- Need to be ____ close to each other

-0.80 and 1.25
-AUC
-20%

29

Cmax and Tmax are used for the bioequivalence, but....

they are not as strict

30

Who completes the bioequivalent studies?

the company trying to get it on the market

31

Approved Drug Products with Therapeutic Equivalence Evaluations=

Orange Book

32

____ code are therapeutically equivalent

A

33

Therapeutically equivalent =

bioequivalent (similar rate and extent of absorption)

34

T/F Therapeutic effect is tested in the Orange Book

FALSE: NOT

35

RLD abbreviation?

reference listed drug

36

B codes

NOT therapeutically equivalent

37

______ is the rate and extent to which the active ingredient or active moiety is absorbed from a drug product and becomes available at the site of action

bioavailability

38

For drug products that ARE not intended to be absorbed in to the blood stream bioavailability.....

may be assessed by measurements intended to reflect rate and extent

39

____ is the absence of a significant difference in the rate at which or extent to which the active ingredient is pharmaceutical equivalent or alternative becomes

bioequivalence

40

T/F A product may also be considered bioequivalent to an innovator product if the difference in rate of absorption of the drug between the two products is intentional

TRUE

41

_____ a finished dosage form that contains an active ingredient

drug product

42

narrow therapeutic index.: there is less than ____ difference in median lethal dose and median effective dose values for a drug product

2-fold

43

To safely and effectively use drug products with narrow therapeutic index require (2)

-careful dosage titration
-patient monitoring

44

______ drug products that contain the SAME active ingredient, are of the same dosage form, route of administration and are identical in strength

pharmaceutical equivalents

45

T/F pharmaceutical equivalents are NOT allowed to differ in shape, scoring configuration, excipients, release mechanism

FALSE: are (they can not differ in strength, quality, purity and identity)

46

________ drug products contain the same THERAPEUTIC MOIETY, but different SALTS, ESTERS, or complexes of that moiety

pharmaceutical alternatives

47

T/F Different dosage forms and strengths within a product line by a single manufacturer are thus pharmaceutical alternatives

TRUE

48

Therapeutic equivalents are expected to have the same ____ and ______ when administered to patients under the conditions specified in the labeling

clinical effect and safety profile