Pharmaceutics I Test 1

Front 1

What % change is allowed among generic and brand name drugs in order to be considered AB rated?

Back 1

25%

Front 2

Name the six different drug travels

Back 2

-Administration
-Release into dosage form
-Absorption
-Distribution
-Metabolism
-Elimination

Front 3

What are the three reasons we prepare dosage forms?

Back 3

-safety
-efficacy
-identification

Front 4

Describe drug behavior in the stomach and in the small intestine

Back 4

stomach - dissolution/disintegration
small intestine - absorption

Front 5

What is the main route of drug distribution in the human body?

Back 5

-circulatory system

Front 6

What four ways can a drug be excreted in the human body?

Back 6

kidney - urine
bile - feces
lungs - expired air
metabolism - makes drug water soluble

Front 7

The initial reaction of drugs is often _______.

Back 7

oxidation

Front 8

A steady state is usually obtained after about _____ half lives.

Back 8

five

Front 9

Describe intravenous route of administration

Back 9

-immediate effect
IV push or bolus
-sometimes to get a drug into solution we use alchohol

Front 10

Describe intramuscular route of administration

Back 10

-often in buttocks
-sustained drug effect because drug is often in oil for longer duration
-preferably isotonic or slightly hypertonic

Front 11

Describe the subcutaneous route of administration

Back 11

-easiest route of administration
-onset 1-4 hrs for suspension
-aqueous solutions onset is 15 to 60 minutes

Front 12

Describe the enteral route of administration

Back 12

-enters the GI tract
-must be palatable
-sublingual (eg nitroglycerin)

Front 13

Describe the boucal route of administration

Back 13

-a bit more sustained then sublingual
-tablet (200mg - 500mg)
-lozenges and troches (500mg 1g)
-chewing gum (500mg - 1g)

Front 14

Describe the rectal route of administration

Back 14

-safe but inconvenient
-morphine faster in this route than oral, but other medications are often slower

Front 15

Describe the topical route of administration

Back 15

-local treatment
-very slow onset for systemic drugs

Front 16

Describe drug administration to the eye

Back 16

-It is important drug is isotonic
-cannot reach posterior part of eye by this route of administration
-gel is very promising but not popular in this form

Front 17

What two characteristics of organic drugs make up the vast majority?

Back 17

-weak bases (75%)
-small molecules (MW<1000)

Front 18

What are some of the inorganic drugs?

Back 18

-Li+ (smallest drug)
-Electrolytes
-Mineral replacement
-Antacids
-Elements (activated charcoal)

Front 19

Few drugs are intrinsically active, which four are actually intrinsically active?

Back 19

-O2, penicillins, nitrates, nitrogen mustards

Front 20

Medicinal actions are generally mediated by ________ interactions with cellular proteins.

Back 20

-noncovalent

Front 21

With noncovalent interactions, ________ becomes an important factor.

Back 21

-concentration

Front 22

Enantiomers are ______ or mirror images of each other

Back 22

-chiral
(behave identically except in asymetric media)

Front 23

Rate at which something dissolves

Back 23

-kinetic

Front 24

Extent at which something dissolves

Back 24

-thermodynamics

Front 25

What is the difference between nexium and prilosec?

Back 25

Nexium - the more active (more expensive) stereoisomer of prilosec
Prilosec - 1:1 racemic mixture, not as active

Front 26

Name two examples of biological membranes drugs must cross

Back 26

-GI tract
-blood brain barrier

Front 27

Substances are generally soluble when the delta G is > or < 0?

Back 27

Favorable net reaction
delta G <0

Front 28

If delta G < 0, then ln P > 1, therefore _______

Back 28

C (organic) > C (aqueous)

Front 29

If delta G > 0, then ln P < 1, therefore _______

Back 29

C (organic) < C (aqueous)

Front 30

The USP arbitrary distinction for solubility is _____

Back 30

>3.3% in water or >3.3mg/100ml

Front 31

What does Lipinski's rule of five refer to?

Back 31

Drug must have reasonable aqueous and organic solubility

Front 32

Rapid cooling has what effect on liquid to solid phase

Back 32

More disorder

Front 33

True / False
Infinite time would allow constituents to fall into place and form crystalline structure

Back 33

True

Front 34

Describe the difference in melting points between ionic crystals and molecular crystals

Back 34

Ionic - 100 to 1000 C
Molecular - 10 to 100 C

Front 35

What are three examples of differences polymorphs might have

Back 35

-Melting points
-Solubility and dissolution rate
-Amorphous forms

Front 36

Explain an example of a stable metastable state

Back 36

-Diamond at atmospheric conditions is not most stable state diamonds are found in but diamonds do not go straight to graphite because it is kinetically trapped

Front 37

When might it be challenging to determine the ground state for a crystalline structure?

Back 37

If the metastable state is very long it may be difficult to determine the ground state for a crystalline structure

Front 38

Briefly describe ground state and metastable state

Back 38

ground state - thermodynamically stable form
metastable state - kinetically trapped

Front 39

Amoxicillin trihydrate is an example of:

Back 39

pseudopolymorph

Front 40

What is different about the melting point of pseudopolymorphs?

Back 40

-"melting point behavior of psuedopolymorphs is much crazier because solvent molecules driven off first followed by solute melting; larger MP range"

Front 41

In what order would solubility and dissolution rate occur given a substance?

Back 41

amorphous > metastable > ground state polymorph

anhydrous >solvates

Front 42

When might it be challenging to determine the ground state for a crystalline structure?

Back 42

If the metastable state is very long it may be difficult to determine the ground state for a crystalline structure

Front 43

Briefly describe ground state and metastable state

Back 43

ground state - thermodynamically stable form
metastable state - kinetically trapped

Front 44

Amoxicillin trihydrate is an example of:

Back 44

pseudopolymorph

Front 45

What is different about the melting point of pseudopolymorphs?

Back 45

-melting point behavior of psuedopolymorphs is much crazier because solvent molecules driven off first followed by solute melting; larger MP range

Front 46

In what order would solubility and dissolution rate occur given a substance?

Back 46

amorphous > metastable > ground state polymorph

anhydrous >solvates

Front 47

Ritonavir is an extraordinary example of confomational polymorphism, explain

Back 47

The form I solid was not actually in the ground state. Form II was the actual ground state and when the drug went from form I to form II on the shelf, a much different solubility was the outcome. Bioavailability dropped significantly, thereby not getting into the blood stream

Front 48

McCrone's dictum states

Back 48

"The number of polymorphs found is directly proportional to the time spent searching for them
-kind like murphy's law

Front 49

Describe four important factors in pharmaceutics in micromeritics

Back 49

-Density
-Angle of repose
-Flowability
-Surface phenomena

Front 50

List three different kinds of stability that the formulator has to consider

Back 50

-Chemical
-Physical
-Microbiological

Front 51

What does LADME stand for?

Back 51

-Admininstration
-Liberation from the dosage form
-Absorption
-Distribution
-Metabolism
-Elimination