Unit 1: Nature of Drug Flashcards
(135 cards)
1
Q
the science of drug preparation & the
medical uses of drugs
A
Materia medica
2
Q
Receptors for which no ligand has been discovered & function can only be guessed
A
orphan receptors
3
Q
short nucleotide chains that can interfere with the readout of genes & the transcription of RNA
A
Antisense Oligonucleotides (ANOs)
4
Q
Body of knowledge concerned with the action of chemicals on biologic systems, especially by binding to regulatory molecules (receptors) and activating or inhibiting normal body processes
A
pharmacology
5
Q
Area of pharmacology concerned with the use of chemicals in the prevention, diagnosis, and treatment of disease, especially in humans
A
medical pharmacology
6
Q
Area of pharmacology concerned with the undesirable effects of chemicals on biologic systems
A
toxicology
7
Q
Relation of the individual’s genetic makeup to his or her response to specific drugs (brought about by the exploration of the human gene)
A
pharmacogenomics
8
Q
Any substance that brings about a change in biologic function through chemical actions
A
drug
9
Q
Specific molecule in the biologic system that plays a regulatory role
A
receptor
10
Q
Explains what the body will do with the drug (how the drug is handled by the patient)
A
pharmacokinetics
11
Q
4 basic concepts of pharmacokinetics
A
absorption
distribution
metabolism
elimination
12
Q
Explains what the drug does to the body
A
pharmacodynamics
13
Q
Involves the follwing concepts: receptor, receptor sites, and inert binding sites
A
pharmacodynamics
14
Q
T/F:
Drugs can produce effects in the body with or without binding sites.
A
false
Receptors (binding sites) are always required; no binding site = no effect in the body
15
Q
T/F:
Drugs are made of chemical components similar to the human body: inorganic ions, nonpeptide organic molecules, small peptides and proteins, nucleic acids, lipids, and carbohydrates.
A
true
16
Q
molecules or substances found in plants or animals, where many are partially or completely synthetic
A
hormones
xenobiotics (foreign substances that enter the body)
17
Q
3 physical natures of drugs
A
solid (tablets, granules)
liquid (syrup, suspension)
gas (aerosolized anesthetics)
18
Q
Drugs are given:
a. directly at the intended site of action
b. at a site distant from the intended site of action
A
b. at a site distant from the intended site of action
(ex. For headache, you consume an analgesic (pain reliever) instead of patching it to your head.)
19
Q
Most drugs have MW between _____ and _____.
A
100
1000
20
Q
MW for selective binding
A
100 MW
(Small drugs require small receptors therefore it could only accept or adapt certain size of molecules)
21
Q
MW for traversing to different barriers of the body
A
1000 MW
22
Q
MW where drugs cannot move within the body and are given at the site of action
A
> 1000 MW
23
Q
T/F:
The shape of the drug affects the duration of the action as well as the potency of a drug.
A
true
24
Q
chemical forces or bonds through which the drug interacts with the receptors
A
drug receptor bonds
25
__________ bonds are more selective bonds
a. stronger
b. weaker
b. weaker
26
Arrange the types of bonds from strongest to weakest:
electrostatic
hydrophobic
covalent
covalent > electrostatic > hydrophobic
27
strongest bond that is irreversible
covalent bond
28
type of bond that is more common but is weaker (e.g. bond between cation and an anion)
electrostatic
29
weakest bond seen in highly soluble drugs
hydrophobic bonds
30
Give the pharmacodynamic sequence where the receptor makes the effects (no effector molecule)
Drug (D) + receptor-effector (R) → drug-receptor-effector complex → effect
31
Give the pharmacodynamic sequence where the drug receptor complex produces an intracellular effector, and it is this intracellular effector that mediates an action of the drug
D + R → drug-receptor complex → effector molecule → effect
32
Give the pharmacodynamic sequence where the drug receptor complex activates a coupling molecule or enzyme inside
D + R → D-R complex → activation of coupling molecule → effector molecule → effect
33
Inhibition of metabolism of endogenous activator → _________ (increased, decreased) activator action on an effector molecule → increased effect
increased
34
T/F:
Some of the receptor pool must exist in Ra (active) form, and this can occur in the absence of the agonist.
true
(constitutive activity; may produce same physiologic effect as agonist-induced activity)
35
Antagonist action can be overcome by increasing the dosage of ________.
agonist
36
binds to and activate the receptor
agonist
37
Activates receptor-effector system to the maximum extent (Ra-D pool) {activated form}
full agonist
38
Binds to the same receptors and activate them in the same way but do not evoke as great a response
partial agonist
39
Binds to a site on the receptor molecule separate from the agonist binding site
allosteric modulators
40
T/F:
Allosteric modulators modifies receptor activity by blocking agonist activity
false
(does not block agonist activity, binds to another site)
41
T/F:
Allosteric modulators are noncompetitive and may increase or decrease response to agonist
true
42
Drug has a stronger affinity for the Ri pool (nonfunctional form)
inverse agonist
43
Inverse agonist ___________ constitutive activity
a. increases
b. decreases
decreases
44
T/F:
Inverse agonist results in effects that are almost the same with the effects
produced by conventional agonists
false
opposite effects
45
Several other binding sites in the
receptors and for other chemicals that bind to the receptors
allosteric site
46
binds to a receptor, competes with and prevent binding by other molecules
antagonist (competitive inhibitor)
47
inactive precursor that must be administered and converted to the active drug by biologic process inside the body
prodrug
48
Movement of drug molecules into and within the biologic environment
permeation
49
type of permeation:
for water-soluble drugs
Aqueous Diffusion
50
type of permeation for membranes of capillaries with small water-filled pores
Aqueous Diffusion
51
Aqueous Diffusion
a. active process, governed by Fick's law
b. active process, not governed by Fick's law
c. passive process, governed by Fick's law
d. passive process, not governed by Fick's law
c. passive process, governed by Fick's law
52
equation for Fick's Law of Diffusion
Flux (moles/ unit time) = C1 - C2 * (Permeability coefficient / thickness) * area
53
type of permeation:
movement of molecules through membranes and other lipid structures
lipid diffusion
54
type of permeation:
Most important factor for drug permeation
lipid diffusion
55
Lipid Diffusion
a. active process, governed by Fick's law
b. active process, not governed by Fick's law
c. passive process, governed by Fick's law
d. passive process, not governed by Fick's law
c. passive process, governed by Fick's law
56
type of permeation:
Drugs transported across barriers by mechanisms that carry similar endogenous substances
Transport by Special Carriers
57
T/F:
Transport by Special Carriers is capacity-limited and is governed by Fick's law.
false
capacity-limited but not governed by Fick's law
58
2 types of Transport by Special Carriers
active transport
facilitated diffusion
59
needs energy, against a concentration gradient
a. active transport
b. facilitated diffusion
a. active transport
60
no energy required, downhill
a. active transport
b. facilitated diffusion
b. facilitated diffusion
61
type of permeation:
Binding to specialized components (receptors) on cell membranes
endocytosis
62
type of permeation:
Internalization by infolding of the area of the membrane and contents of the vesicle are subsequently released into the cytoplasm
endocytosis
63
type of permeation:
Permits very large or very lipid-insoluble chemicals to enter the cell
endocytosis
64
type of permeation:
for B12 with intrinsic factor and Iron with transferrin (large chemicals)
endocytosis
65
type of permeation:
Expulsion of membrane-encapsulated material from the cell (intracellular content)
exocytosis
66
type of permeation:
for neurotransmitters
exocytosis
67
Predicts the movement of molecules across a barrier
Fick's Law of Diffusion
68
According to Fick's Law of Diffusion, drug absorption is:
_________ (faster, slower) in organs with LARGER surface areas
_________ (faster, slower) in organs with SMALLER surface areas
FASTER in organs with LARGER surface areas
SLOWER in organs with SMALLER surface areas
69
According to Fick's Law of Diffusion, drug absorption is:
_________ (faster, slower) from organs with THICK membrane barriers
_________ (faster, slower) from organs with THIN membrane barriers
SLOWER from organs with THICK membrane barriers
FASTER from organs with THIN membrane barriers
70
Rate of absorption:
stomach ___ small intestine
(< or >)
<
(small intestine: larger surface area)
71
Rate of absorption:
lungs ___ skin
(< or >)
>
(lungs: thinner membrane barrier)
72
In Fick's law, this refers to the measure of the mobility of the drug in medium of the diffusion path
permeability coefficient
73
↑ Rate of diffusion: ____ concentration gradient
↑
74
↑ Rate of diffusion: ____ surface area
↑
75
↑ Rate of diffusion: ____ permeability coefficient
↑
76
↑ Rate of diffusion: ____ thickness
↓
77
↑ Lipid solubility: _____ charge
↓
78
_________ solubility of a drug is a function of the electrostatic charge (degree of ionization, polarity) of the molecule
a. aqeous
b. lipid
aqeous
79
__________ molecules are attracted to charged drug molecules forming an aqueous shell around them
a. water
b. lipid
water
80
T/F:
Many drugs are strong bases or strong acids
false
weak acids/ bases
81
_____ of the medium determines the fraction of molecules charged (ionized) versus uncharged (nonionized)
pH
82
T/F:
Weak bases/acids can be charged or
uncharged, ionized or non-ionized depending on the pH where they are located
true
83
In lipid diffusion, fraction of molecules in the ionized state can be predicted by means of?
H-H equation
84
Protonated weak base:
a. water-soluble
b. lipid-soluble
a. water-soluble
85
Protonated weak acid:
a. water-soluble
b. lipid-soluble
b. lipid-soluble
86
Deprotonated weak acid:
a. water-soluble
b. lipid-soluble
a. water-soluble
87
Clinically important when it is necessary to estimate or alter the partition of drugs between compartments of different pH
Henderson-Hasselbach Equation
88
Amount drug of absorbed into the systemic circulation to that amount of drug administered
bioavailability
89
Route of administration:
Maximum convenience
oral (swallowed)
90
Oral route:
Absorption may be _______ (faster, slower) and ________ (more, less) complete
slower
less
91
Some drugs have ______ bioavailability when given orally
a. high
b. low
low
92
Route of administration:
Subject to first-pass effect
oral (swallowed)
(significant amount of the agent is metabolized in the gut wall, portal circulation, and liver before it reaches the systemic circulation)
93
Route of administration:
Bioavailability by definition is 100% (gold standard)
Intravenously (IV)/ parenteral
94
Intravenously (IV)/ parenteral:
Instantaneous and ________ (complete, incomplete) absorption
complete
95
T/F:
Drugs taken intravenously are potentially more dangerous.
true
(high blood levels reached if administration is too rapid)
96
Intramuscular (IM):
Because of the large amount of blood vessels in the muscles, absorption is often ______ (faster, slower) and ______ (more, less) complete than oral.
faster
more
97
T/F:
Drugs administered intramuscularly should be limited to less than 5mL into each buttock.
false
(Can be administered through large volumes (>5ml into each buttock) if the drug is not irritating)
98
Enumerate the routes of administration where first-pass effect is avoided
intramuscular
subcutaneous
transdermal
rectal/ suppository (partial avoidance)
99
Heparin can be given by this route as it does not cause hematoma in the muscle
a. intramuscular
b. subcutaneous
subcutaneous
100
Heparin cannot be given by this route as it causes bleeding in the muscle
a. intramuscular
b. subcutaneous
intramuscular
101
Rate of absorption:
intramuscular ____ subcutaneous
>
102
Route of administration:
in the pouch between gums and
cheeks
buccal route
103
Route of administration:
under the tongue; offers the same features as the buccal route
sublingual route
104
T/F:
Suppositories tend to migrate upward in the rectum where absorption is partially into the portal circulation.
true
105
Ideal route of administration for larger amounts of unpleasant drugs
rectal (suppository)
(may cause significant irritation)
106
Route of administration:
For respiratory diseases; delivery closest to the target tissue
inhalation
107
Inhalation results into ______ (faster, slower) absorption because of the thin alveolar surface area
faster
108
Route of administration:
Application to the skin or mucous membrane of the eye (eyedrops), nose, throat, airway, or vagina (vaginal suppositories) for local effect
topical
109
T/F:
For topical administration, rate of absorption varies with the area of
application and drug’s formulation.
true
110
For topical administration, absorption is ______ (faster, slower) compared to other routes
slower
(because it still would have to traverse the tissues)
111
Route of administration:
Application to the skin for systemic effect
transdermal
112
For topical administration, absorption is very ______ (fast, slow)
slow
113
Influences absorption from intramuscular, subcutaneous, and in shock
blood flow
114
High blood flow maintains a _____ (high, low) drug depot-to-blood concentration gradient.
high
115
Major determinant of the rate of absorption (Fick’s law)
concentration
116
determines the concentration gradient
between blood and the organ
size of the organ
117
Important determinant of the rate of uptake
blood flow
118
Enumerate well-perfused organs, where blood flow is good
1. Brain
2. Heart, Kidneys
3. Splanchnic organs - responsible for indigestion during times of stress
119
If the drug is very soluble in cells, concentration in the perivascular space will be _______ (higher, lower)
lower
(diffusion from the vessel into the extravascular tissue will be facilitated)
120
Binding of drugs to macromolecules in the blood or tissue compartment will tend to ________ (increase, decrease) the drug’s concentration in that compartment.
increase
121
A parameter in pharmacokinetics
Apparent volume of distribution (Vd)
122
3 types of drug metabolism
1. Action of many drugs is terminated before they are excreted (converted to metabolite before excreted)
2. Prodrugs (inactive, metabolized to be active)
3. Drugs not modified by the body (eliminated as metabolite)
123
For most drugs, excretion is by way of the ____________
kidneys (except anesthetic gases-lungs)
124
T/F:
For drugs with active metabolites (ex: diazepam), elimination of the parent molecule by metabolism is not synonymous with termination of action.
true
125
For drugs that are not metabolized (not metabolized = not water soluble), __________ is the mode of elimination.
excretion
(through the bile)
126
most common process of elimination followed by most drugs
first order elimination
127
In first order, rate of elimination is ____________ to drug concentration.
a. proportionate
b. inversely proportionate
a. proportionate
(The higher the concentration, the greater the amount eliminated per unit time.)
128
In first order elimination, concentration of such drug in the blood will decrease by ____% for every half-life until amount of drug is negligible.
50
129
Rate of elimination is constant regardless of drug concentration
zero order elimination
130
type of elimination that occurs with drugs that saturate their elimination of mechanism at concentrations of clinical interest
zero order elimination
131
Identify the transporter:
norepinephrine reuptake from synapse
NET (Norepinephrine Transporter)
132
Identify the transporter:
serotonin reuptake from synapse
SERT (Serotonin Transporter)
133
Identify the transporter:
transport of dopamine and norepinephrine into adrenergic vesicles in nerve endings
VMAT (Vesicular Monoamine Transporter)
134
Identify the transporter:
transport of many xenobiotics out of cells
MDR1 (Multidrug Resistance Protein 1)
135
Identify the transporter:
leukotriene secretion
MRP1 (Multidrug Resistance-Associated Protein 1)
