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PDA I Test 1
Part 1 (Introduction to Drugs)
109
Other
Professional
02/11/2012

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Term
Define a drug
Definition
substance that alters an EXISTING physiological or biochemical process

used in diagnostics, treatment, or prevention of a disease
Term
What does gene therapy do?
Definition
impart new function in cells/tissues
Term
What are two types of non traditional therapies?
Definition
gene therapy
vaccines
Term
What is pharmacodynamics?
Definition
the discription of interactions that occur between a drug and its receptor

eventually lead to the actions of the drug
Term
What does binding to more than one intended receptor cause?
Definition
toxicity
Term
What are lead compounds?
Definition
compounds with known structures that are used as bases for building drugs
Term
What is molecular modeling?
Definition
designing structures that fit with receptors

ex-"plug" drugs that are more affinitive toward virus than body recptors
Term
How many years and how much does it cost to get a drug to the market?
Definition
10-15 years

500mil-1bil
Term
What is the chemical name of a drug?
Definition
depicts chemical structure

useful to only trained individuals
Term
What is the generic name? (non proprietary)
Definition
no linked to any manufacturer

USAN and WHO approved

not capitalized
Term
What is the brand name? (proprietary)
Definition
aka trade name

selected by manufacturing company and copyrighted

can have many brand names per generic
Term
Who assigns the international non proprietary name?
Definition
WHO :P

-world health organization
Term
Which groups make up the USAN? U.S adopted name council
Definition
AMA, USP, APhA, FDA, and one member at large
Term
What does the FDA have authority over concerning drug labeling?
Definition
every written piece of information
Term
What is a -barb stem name?
Definition
barbituate
Term
What is a -cillin stem name?
Definition
penicillin
Term
What is a -cycline stem name?
Definition
tetracycline derivative antibiotic
Term
What is a -oxacin stem name?
Definition
quinolone derivative antibiotic
Term
What is a -vastatin stem name?
Definition
cholesterol(lipid) lowering
Term
How many syllables can a drug name have?
Definition
4
Term
How do most drugs work?
Definition
by binding to a receptor and then boosting or blocking activity
Term
What are the four physio chemical properties?
Definition
crystal form
solubility
partition coefficient(lipophilicity)
ionization (pKa)
Term
What two things must a drug do to be effective?
Definition
reach site of action

interact with target long enough
Term
What are anatomical barriers?
Definition
membranes
Term
What are chemical barriers?
Definition
body fluid pH
Term
What are biochemical barriers?
Definition
enzymes
Term
What are excipients?
Definition
substances added to provide desired characteristics
Term
What are the three characteristics of a good drug?
Definition
1) effective release (good absorption & strong activity)

2) stable over a long period of time and shelf life

3) appealing (little side effects, frequency of dosing)
Term
What is dissolution?
Definition
a process by which a compound goes from the solid state to a solution in a solvent

this is the first step of absorption for drugs
Term
What happens simultaneously during dissolution?
Definition
solute particles separate
solvent particles separate
formation of solute-solvent interactions
Term
What are the two forms of solid compounds?
Definition
crystalline and amorphous
Term
Differentiate crystalline and amorphous solids.
Definition
Crystalline-regular, repetitive arrangement, symmetrical crystal lattice, strong intramolecular bonds

Amorphous- irregular, no crystal lattice, no symmetry, weak intramolecular bonds
Term
Which form of Insulin is good for intermediate acting injection?
Definition
amorphous form
Term
Which form of Insulin is good for long acting injection?
Definition
crystalline form
Term
What are polymorphs?
Definition
substance that can have more than one amorphous form
Term
What is characteristic of stable polymorphs?
Definition
insoluble
Term
What is characteristic of high energy polymorphs?
Definition
soluble
Term
How likely is it for an unstable polymorph to revert back to stable insoluble polymorph?
Definition
high possibility
Term
Was form 1 or form 2 of ritonavir insoluble?
Definition
form 2
Term
What are the four molecular interactions discussed?
Definition
Van der Waals
Dipole-Dipole
Ionic attractions
Ion-Dipole
Term
Describe Van der Waals attractions
Definition
weakest
electrostatic
between NONpolar portions of molecules
Term
Describe Dipole-Dipole interactions
Definition
results from unequal sharing of electrons in a covalent bond within each molecule in the interaction

hydrogen bonding is a type of dipoledipole
Term
Describe ionic attractions
Definition
attraction of oppositely charged atoms

inorganic molecules and salts of organic molecules
Term
Describe Ion-Dipole interactions
Definition
Cation/anion will bind to oppositely charged part of organic molecule

most important bonding for dissolving organic salts(drugs)
Term
What forms when a base and acid are mixed?
Definition
an ionic salt
Term
Give the dissolution rate equation.
Identify components D,A,S,C,S-C,H
Definition
Rate=DxA(S-C)/H

D=diffusion Coefficient
A=surface area
S=drug solubility
C=concentration
S-C= concentration gradient
H=diffusion layer thickness
Term
How do you calculate intrinsic solubility?
Definition
K=conc in soln/conc in solid
Term
If a compound has a lot of polar groups(polar solvent) what is its K value like?
Definition
High K value
Term
What three things does intrinsic solubility depend on?
Definition
chemical structure, solid-state structure, and solution temperature
Term
What kind of solvents cant solvate(& break apart covalent bonds) molecules?
Definition
non-polar
Term
What three things happen when dissolving in water?
Definition
break intermolecular bonds
break intramolecular bonds
hydrogen bonding occurs
Term
Which kind of bonding is important for monofunctional(one functional group) groups?
Definition
INTERmolecular bonding
Term
Which kind of bonding is important for poly functional groups?
Definition
INTRAmolecular and INTERmolecular bonding

*the multiple functional groups on the same compound interact with each other while the compound interacts with another compound
Term
How do you use the Empiric method to predict solubility?

**do we need to know chart saying how much each type of functional group can solvate?**
Definition
by using certain functional groups to estimate how many carbons it can make soluble.
*polyfunctional groups are added together to give total amount of carbons
Term
How do you use the Analytical method for predicting solubility?
Definition
based on partioning of drug between octanol and water
-more accurate the empirical

logP= conc in octanol/ conc in water

sum TT values=logp
Term
What are the steps of the Analytical method?
Definition
1)identify fragments
2)add pi values
3)plug in for log p
Term
What is the solubility if...
- logP>.5

-logP<.5
Definition
-logP>.5= water insoluble
-logP<.5=water soluble
Term
What range do you want the logP of drugs to be in?
Definition
0-3.5
Term
The higher the logP the more _________ it is.
Definition
lipophilic
Term
What are the two forms of amphiphillic compounds?
Definition
miscelles(tails in heads out) and bi-layers
Term
Do ion-dipole interactions increase or decrease water solubility?
Definition
increase
Term
Define a bronsted lowry acid.
Definition
a substance that donates a proton
Term
Define a bronsted lowry base.
Definition
a substance that accepts a proton
Term
Is water amphoteric?
Definition
yes
H3O+
OH-
Term
What does the ionization constant K represent?
Definition
Concentration of each ionized form
Term
How do you calculate Ka? Kw?
Definition
Ka=(A-)(H+)/(HA) ionized over unionized

Kw=[H+][OH-]
Term
What is the pH and H+ conversion

**same for pka and Ka
Definition
pH=-log[H+]

H+=10^pH
Term
Define pH
Definition
the measure of the concentration of protons [H+]
Term
What kind of acid/base is always in its ionized form?
Definition
A STRONG acid and base
Term
Which kind of acid/base form a conjugate base/acid and has ionization dependent on the pH of the solution?
Definition
A WEAK acid and base
Term
Which kind of acids/bases have ionization equations that are reversible?
Definition
WEAK acids and bases
Term
What does a higher Ka and lower pKa mean?
Definition
more acidic
Term
What does a lower Ka and higher pKa mean?
Definition
more basic
Term
What is the difference in conjugate bases for strong and weak acids?
Definition
Stong acids=weak conj bases(do not accept protons)

Weak acids=strong conj bases that readily accept protons to convert back to the acid form
Term
What is aspirin a stong/weak acid/base?
Definition
weak acid
Term
What is benzocaine a strong/weak acid/base?
Definition
weak base
Term
What are the four advantages of forming a salt?
Definition
easier to crystallize
more stable
dissolve faster
easier to handle
Term
What is the most common acidic functional group?
Definition
carboxilic acid
Term
What is the most common basic functional group?
Definition
amine
Term
What are acidic monovalent salts? acidic Multivalent salts?
Definition
Monovalent have a +1 charge (Na, K)

Multivalent have more then +1 (Mg, Al)
Term
What are common salts of basic drugs?
Definition
Inorganic salts (hydrochlorides, sulfates)

Sugar salts (gluconates)
Term
Are salts with complex amines like procaine and benzathine water soluble?
Definition
no they are insoluble in water
Term
Are salts with fatty acids like stearate water soluble?
Definition
no they are insoluble in water
Term
What are the requirements for calcium carbonate?
Definition
acidic pH for absorption
must be taken with meal
Term
What are the requirements for Calcium Citrate?
Definition
no specific pH
full or empty stomach
Term
What are the requirements for Calcium gluconate, lactate, and phosphate?
Definition
must take a large amount due to the little calcium content
Term
Give the henderson hasselback equation.
Definition
pH=pKa+log [base]/[acid]
Term
What is an electrolyte?
Definition
a substance that ionizes in solution

-conducts electricity
Term
What kind of electrolytes are strong acids?
Definition
strong
Term
What kind of electrolytes are weak acids?
Definition
weak
Term
Are most drugs strong or weak acids and bases?
Definition
weak
Term
What are the general normal conditions of pH in the body?
Definition
pH is very stable in the blood and tissue but can vary between organs
Term
What is the total physiological pH range?
Definition
1-8
Term
What is the pH range in the stomach?
Definition
1-3.5
Term
What is the pH range in the small intestine?
Definition
5.5-7.5
Term
What is the pH in the lungs and blood?
Definition
7.4
Term
Weak acids have higher solubility at ______ pH in the ______ while weak bases have higher solubility at ______ pH in the ______.
Definition
1)high... small intestine

2)low... stomach
Term
What are the advantages of a drug ionizing?
Definition
-dissolve faster
-higher s(solubility) values
-better dissolution
-more drug available
Term
What are the components of an acidic buffer?
Definition
weak acid and its salt
ex- acetic acid and sodium acetate
Term
What are the components of a basic buffer?
Definition
weak base and its salt
ex-ammonia and ammonium chloride
Term
What is the purpose of biological buffers?
Definition
to prevent drugs from changing the pH of the physiological environment

the pH does not change but the concentrations of the ionized and unionized do
Term
What are two examples of biological buffers?
Definition
phosphate buffer
proteins
Term
If pH=pKa then what is the ratio of ionized to unionized?
Definition
50:50
Term
If pH>pKa then what is the ratio of ionized to unionized?
Definition
ionized>unionized
Term
If pH
Definition
ionized
Term
Do changes in pH close to the drugs pKa value affect ionization?
Definition
if <2 units away yes

variations of pH far from the pKa dont affect it
Term
If the pH value is less than or equal to the value of the pKa minus 4 of a weak acid what is the ionization?
Definition
completely non ionized
Term
If the pH value is greater than or equal to the value of the pKa plus 4 of a weak base what is the ionization?
Definition
completely non ionized
Term
Look at the activity question at the end of physiochemical properties IV
Definition
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