Unit 1: Introduction Flashcards
1
Q
release of drug from dosage form
A
drug product performance
2
Q
substances intended for the use in diagnosis, cure, mitigation, treatment or prevention of disease
A
drug
3
Q
refers to the active pharmaceutical ingredient (API)
A
drug
4
Q
given in a variety of dosage forms or drug products for systematic or local therapeutic activity
A
drug
5
Q
final dosage form
A
drug product
6
Q
drug delivery systems that release and deliver drug to the site of action to produce the desired therapeutic effect and minimize adverse toxicity
A
drug product
7
Q
should be designed to meet the patient’s INDIVIDUAL requirements (safety, efficacy, cost/convenience, compliance; if orally: palatability)
A
drug product
8
Q
interrelationship of the physicochemical properties of the drug, the dosage form (drug product) in which the drug is given, and the route of administration on the rate and extent of systemic drug absorption
A
biopharmaceutics
9
Q
physical and chemical properties of a drug relate to: (4 answers)
A
bioavailability, pharmacokinetics, pharmacodynamics and toxicologic effects/toxicokinetics
10
Q
represented by F
A
bioavailability
11
Q
rate (time) & extent (amount) of systemic absorption of the therapeutically active drug
A
bioavailability
12
Q
in which organ does absorption primarily occurs
A
small intestine
13
Q
formulation parameter to predict the proportion [and frequency] of the dose that will be systemically absorbed in the patient when changing dosage forms of the same drug
A
bioavailability
14
Q
a measure of systemic availability of a drug
A
bioavailability
15
Q
biopharmaceutic classification system or BCS categorizes drugs based on: (2 answers)
A
absorption and permeability
16
Q
route of delivery:
percentage of drug bioavailability when delivered thru IV
A
100%
17
Q
route of delivery:
percentage of drug bioavailability when delivered orally
A
not 100%
18
Q
are added to enhance the performance/efficacy of drug/AI
A
excipients
19
Q
3 factors affecting bioavailability
A
nature of drug molecule, route of delivery, formulation of dosage form
20
Q
bioavailability allows us to determine if the drug is: (3 answers)
A
therapeutically active, toxic, has no apparent effect
21
Q
the time course of drug movement in the body during absorption, distribution, metabolism, & excretion (ADME)
A
pharmacokinetics
22
Q
what the body does to the drug
A
pharmacokinetics
23
Q
words of origin of pharmacokinetics
A
pharmakon + kinesis
24
Q
pharmakon meaning
A
drug
25
kinesis meaning
movement
26
drug elimination involves which processes in the body
metabolism and excretion (ME in ADME)
27
drug disposition involves which processes/stages in the body
distribution, metabolism and excretion (DME)
28
goal of application of pharmacokinetics
assure patient safety:
“Assure maintenance of therapeutic drug concentration in the body while preventing danger of toxicity.”
29
relation of the drug concentration or amount at the site of action (receptor) & its pharmacologic response
pharmacodynamics
30
what the drug is doing to the body
pharmacodynamics
31
harmful or undesirable effects of the drug
toxicologic effects
32
result of a drug activating or inactivating receptors
pharmacologic response
33
includes biochemical and physiologic effects that influence the interaction of drug with the receptor
pharmacodynamics
34
is it possible for adverse effects to appear in therapeutic concentrations
yes; are unpredictable
35
component [in or at the surface] of a cell or organism that interacts with a drug and initiates the chain of events leading to the drug’s observed effects
receptor
36
agonist that elicits 100% effect upon receptor occupancy; maximum response upon drug administration
full agonists
37
agonist with subtherapeutic effect
partial agonist
38
agonist with opposite effect
opposite agonist
39
antagonist that competes for a receptor since they have affinity to the same receptor as the agonist
competitive antagonist
40
agonist that binds to an allosteric (non-agonist) site on the receptor to prevent activation of the receptor
non-competitive antagonist
41
antagonist that prevents receptor effect thru other means (ex. interacts directly with the drug being antagonized to remove it or to prevent it from binding to its target)
chemical antagonist
42
antagonist that occupies
another receptor that when activated, counteracts the effect of the other receptor
physiological antagonist
43
drugs that occupy receptors and activate them
agonist
44
drugs that occupy receptors but do not activate them; blocks the receptors
antagonist
45
refers to dose and various measures of acute or integrated drug concentrations in plasma and other biological fluid
drug exposure
46
refers to direct measure of the pharmacologic effect of the drug
drug response
47
includes endpoints or biomarkers from: remote, presumed mechanistic effect to a potential or accepted surrogate and to a full range short/long term clinical effect
drug response
48
which particles have better dissolution: smaller or bigger
smaller; they have greater surface area
49
is there great or limited absorption is the stomach
limited
50
biopharmaceutics involves factors that influence: (6 answers)
1) design of drug product
2) stability of drug within drug product
3) manufacture of drug product
4) release of drug from drug product
5) rate of dissolution/release of drug from absorption site
6) delivery of drug to site of action
51
drug which is altered by the presence of a precipitant drug
object drug
52
any component that may affect the drug (may be food, drug etc.)
precipitant drug
53
scope of biopharmaceutics:
all possible effects observed following the administration of the drug in its various dosage forms, including (3 answers)
therapeutic effect, adverse effect, drug-drug interaction
54
reflects the minimum concentration of drug needed at the receptors to produce the desired pharmacologic effect
minimum effective concentration (MEC)
55
represents the lowest drug concentration needed to just barely produce a toxic effect
minimum toxic concentration (MTC)
56
the concentration between MTC and MEC
therapeutic window
57
is it safer to have a wide or narrow therapeutic window
wide - safer
58
ratio between toxic and therapeutic dose; measurement of drug safety
therapeutic index
59
corresponds to the time required for the drug to reach the MEC
onset time
60
proportional to the number of drug receptors occupied, which is reflected in the observation that higher plasma drug concentrations produce a greater pharmacologic response, up to a maximum
intensity of pharmacologic effect
61
difference between the onset time and the time for the drug to decline back to the MEC
duration of drug
62
onset of minimal observable effect to normal physiologic respone
duration of drug
63
time of maximum drug concentration in the plasma and is a rough marker of average rate of drug absorption
time of peak plasma level/peak time
64
related to the dose, the rate constant for absorption, and the elimination constant of the drug
peak plasma level or maximum drug concentration
65
related to the amount of drug absorbed systemically in the body
AUC or area under the curve
66
scope of biopharmaceutics:
all possible effects of various dosage forms on biological response including:
onset of action and duration of action [and intensity]
66
scope of biopharmaceutics:
all possible effects of various dosage forms on biological response including:
onset of action and duration of action [and intensity]
67
scope of biopharmaceutics:
all possible physiological factors which may affect the drug contained in the dosage form, including (2 examples from ppt)
pH of the stomach & intestine, surface area of skin
68
4 scopes of biopharmaceutics
1) all possible effects observed following the administration of the drug in its various dosage forms
2) all possible effects of various dosage forms on biological response
3) all possible physiological factors which may affect the drug contained in the dosage form
4) dosage form of the drug
69
a drug that is bioavailable is [more or less] likely to cause an effect in the body
more
70
breaking down into smaller particles
disintergation
71
conversion from solid to liquid
dissolution
72
most absorbable oral dosage form
solution
73
a process of how the body deals with the drug
pharmacokinetics
74
a process of how your drug deals with the body
pharmacodynamics
75
individualized treatment/therapy; considers patient factors
clinical pharmacy
76
application of pharmacokinetic models to drug therapy
clinical pharmacokinetics
77
serves as basis of dosing regimens
drug disposition
78
disease, age, gender and genetic and ethnic differences are factors that affect _______
drug disposition
78
observation of drug manifestations on patient
therapeutic drug monitoring (TDM)
79
used for very potent drugs ex. w/ narrow therapeutic range; optimize efficacy and prevent adverse toxicity
therapeutic drug monitoring (TDM)
80
drug examples that require plasma drug concentration monitoring (4 answers from ppt)
theophylline, chemotherapeutic drugs, anticonvulsants, aminoglycosides
81
monitor specific pharmacodynamic endpoint (1 example from ppt)
prothrombim clotting time - warfarin
82
Goal in drug making – design a drug product that will deliver active drug in the most ________ form
bioavailable
83
pharmaceutic factors affecting drug bioavailability (3 answers)
1) type of drug
2) nature of excipients in the drug
3) physicochemical properties of the drug molecule
84
measurable characteristics
physicochemical characteristics
85
determined by the number, kind, arrangement of atoms
physicochemical characteristics
86
preferred expression of the properties that relate to biological action vs physical or chemical
physicochemical characteristics
87
pH, solubility, H-bonding, partition coefficient, hydrophilicity, lipophilicity, BBB, placental barrier are examples of
physicochemical characteristics
88
physicochemical factors that may alter bioavailability (6 answers)
1) particle size of drug in solid dosage form
2) particle size of dispersed phase in an emulsion
3) tablet disintegration
4) tablet and capsule adjuncts
5) tablet coating
6) crystalline drug properties
89
solution to Griseofulvin being not very soluble
micronized Griseofulvin
90
mixture of oil and liquid phase with each other
emulsion
91
Griseofulvin has high affinity to ___
fats
92
excipients that help with the equal distribution of both phases in an emulsion
emulsifying agent/surfactant
93
break up of intact dosage form to its
component aggregates
tablet disintegration
94
excipients that help break down tablets
disnintegrants
95
“That state in which any residue of the tablet, except fragments of insoluble coating remaining on the screen of the test apparatus in the soft mass have no palpably firm core”
complete disintegration (USP)
96
reference for quality control pharmacopoeial test
USP
97
solid products exempted from disintegration test (2 answers)
troches and chewable tabs
98
separate specs for (5 answers)
uncoated, buccal, enteric, plain coated, SL (sublingual) tabs
99
added to form the dosage form; inert, inactive
excipients
100
has no pharmacologic effect but has effect on physical and chemical characteristics of drug
excipients
101
roles of tablet and capsule adjuncts
1) affect drug absorption
2) increase solubility
3) increase retention time of drug in GIT
4) act as carrier to increase drug diffusion across the intestinal wall
102
increase viscosity of drug vehicle, resulting to changes in drug dissolution
suspending agents
103
promote suspension throughout the formulation
suspending agent
104
prevent the sticking of fill material to the punches and dies to produce tablets having a sheen
lubricant
105
enhance the flow of the tableting material in the tablet dies, minimize wear of punches and dies
glidant
106
prevent adhesion; aka non sticking agent; enhance adhesion properties
anti-adherents
107
magnesium stearate
hydrophobic lubricant
108
talc
glidant
109
Talc, hydrogenated vegetable oil, magnesium stearate
lubricants, glidants, anti-adherents
110
excessive use of lubricants, glidants and anti-adherents will result to
repel water and reduce dissolution
111
increase bulk or mass of the dosage form
diluent/filler
112
excess use will retard dissolution
diluent/filler
113
lactose
diluent/filler
114
dibasic calcium phosphate
diluent/filler
115
starch
tablet disintegrant, diluent/filler
116
explotab
tablet disintegrant
117
avicel
tablet disintegrants
118
sodium starch glycolate
tablet disintegrant
119
microcrystalline cellulose
tablet disintegrant, diluent/filler
120
makes diluent adhere to the tablet to form a compact mass
binder
121
excessive use will retard disintegration and dissolution
binder
122
acacia
binder
123
amount of force required to break the tablet
tablet hardness/breaking force
124
can tablet hardness/breaking force be found in pharmacopoeia
non pharmacopoeial
125
added when drug is easily degraded
tablet coating
126
thickness will affect drug release
tablet coating
127
uneven release or not released at all
tablet coating
128
protection against gastric acid
enteric coated
129
cellulose acetate phthalate
enteric coated
130
aspirin EC is an example of what type of coating
enteric coated
131
protection against light, moisture & air during storage
film coated
132
hydroxypropylmethyl cellulose
film coated
133
to conceal or mask bitter taste
sugar coated
134
sucrose
sugar coated
135
glucose
sugar coated
136
use of aspirin EC
anti-inflammatory, antipyretic
137
adverse effect of aspirin EC
reye's syndrome
138
adverse effects of paracetamol
hepatoxicity and jaundice
139
which has slower dissolution time/rate
amorphous or crystalline
crystalline
140
which is less thermodynamically stable
amorphous or crystalline
amorphous
141
which is more rigid
amorphous or crystalline
crystalline
142
drug + water
hydrates (crystal)
143
T/F
hydrates and anhydrous have same solubility
false
144
which has faster dissolution
erythromycin dihydrate or monohydrate/anhydrous in phosphate buffer
dihydrate
145
which has faster dissolution
anhydrous ampicillin or ampicillin trihydrate
anhydrous ampicillin
146
different crystal forms, same chemical structure, different physical properties
polymorphs
147
are the following physical or chemical properties:
solubility, density, hardness, compression characteristics
physical
148
arrangement of drug in various crystal forms
polymorphism
149
has several polymorphs, ß polymorph is used for suspension
chloramphenicol
150
how soluble and absorbable is a ß polymorph when used for suspension
more soluble and better absorbed
151
rank chloramphenicol A, B and C based on stability, the first being the most stable
A > B > C
152
chloramphenicol used for suspension and is metastable
B
153
erythromycin coating
enteric coated
154
stability of erythromycin in acidic, neutral and alkaline medium
acid = unstable
neutral and alkaline = stable
155
enalapril is an example of
prodrug
156
therapeutic form of enalapril
enalaprilate
157
L DOPA
prodrug
158
diazepam
active drug with active metabolite
159
active metabolite of diazepam
temazepam
160
acetaminophen/paracetamol
active drug with toxic metabolite
161
acetaminophen/paracetamol toxic metabolite
n-acetyl-p-benzoquinone imine (NAPQI)
162
needed for very potent drugs like digoxin
therapeutic drug monitoring
