Pharmacodynamics Flashcards
1
Q
the study of substances that interact with living systems through chemical processes
A
pharmacology
2
Q
name the 3 pillars of pharmacology
A
pharmacodynamics
pharmacokinetics
pharmacognetics
3
Q
how medications affect the body
how a drug interacts with its molecular targets
A
pharmacodynamics
4
Q
how the body affects medications
how a drug moves thorugh the body (absorption, distribution, metabolism, excretion)
A
pharmacokinetics
5
Q
how genetics impact the medication
how responses differ in a population
A
pharmacogenomics
6
Q
any substance that brings a change in biologic function through its chemical actions.
A
drug
7
Q
substances that are made within the body; growing or originating from within an organism.
A
endogenous
8
Q
substances created externally; growing or originating from outside the organism.
A
exogenous
9
Q
: a molecule that binds to another (usually larger) molecule or target. May be endogenous or exogenous..
A
ligand
10
Q
any substance not synthesized within the body and that is foreign to the body.
A
xenobioitic
11
Q
drugs that have almost exclusively harmful effects
A
poison
12
Q
poison of biologic origin (venoms)
A
toxin
13
Q
name examples of inorganic poisons
A
nonbiologic
lead and arsenic
14
Q
what are the five physical nature of drugs
A
size
shape
atomic composition
configuration
electrical charge
15
Q
how is drug size measured?
A
molecular weight (G) or molecular mass (G/mol)
16
Q
most drugs are between ____ to ____ MW
A
100 to 1000
17
Q
what is the molecular mass of water?
A
18 g/mol
18
Q
The ___ the molecule, the more off-target effects (not very specific)
A
smaller
19
Q
The ____ the molecule, the more difficulty with crossing biological barriers (GI tract, BBB, cell membrane, etc.)
A
larger
20
Q
most drugs form electrostatic bonds because they are weak bonds and are _____
A
REVERSIBLE
21
Q
what kind of bonds involve shared electron pairs between atoms
A
covalent
22
Q
name an example of a hydrophobic interaction
A
water, a polar substance, cant interact with molecules with no charge
23
Q
what are Areas that drugs may bind to, especially more lipid-soluble or non-polar drugs.
A
hydrophobic pockets
24
Q
proteins may contain amino acids that have __ charge
A
No charge or NON polar
25
what result from the attraction between oppositely charged ions or portions of a molecule.
ionic bonds
26
pairs of compounds with exactly the same connectivity but opposite three-dimensional shapes
enantimoers
27
a mix of 2 enantiomers
racemic mixture
28
each of two or more compounds with the same formula but a different arrangement of atoms in the molecule and different properties
isomer
29
4 separate moieties bound to the carbon. A mirror image, but not superimposable (is NOT the same molecule
chiral
30
not all moieties are unique. Mirror images are superimposable (the are the same molecules)
achiral
31
true or false: Enantiomers share the same chemical properties.
FALSE they do not
| One may cause intended effect, while the other causes off-target S/E
32
the ___ system identifies chiral centers and assigns priority to each group attached to that center
R/S System configuration
33
name the other terms for S and R in the R/S system
S= sinister, counterclockwise, left
R= rectus, clockwise, right
34
what is another name for enantiomers?
optical isomers
35
what is the other name for clockwise and counterclockwise directions?
dextroratory (+)
levortatory (-)
36
This naming system uses a beam of plane-polarized light to identify and categorize isomers, depending on the direction it spins in light.
d/l (+/-) system: optical activity
37
Most racemic mixtures have one major bioactive molecule called ___
eutomer.
38
the other enantiomer called ____ is either inactive, less active or potentially toxic.
distomer,
39
who created the receptor theory of drug action
paul ehrlich (1854-1915)
| a drug will not work unless bound
40
what are the 3 current day theories of drug/receptor complexes
lock and key
induced fit
conformational selection
41
ligands or drugs do not cause the receptor to change shape is known as:
conformational selection
42
Alteration in the shape of a protein as a result of an external factor, such as the binding of a ligand (to a receptor) or binding of substrate (to an enzyme) is known as:
conformational change
43
the greater the proportion of receptors in ACTIVE state at any given time in the absence of agonist, the greater teh ____ level of receptor activity
basal
44
what is this known as
drug affinity (Kd)
45
the affinity of a drug is a reflection of _____ it is bound to the receptor
how tightly
46
the ___ is the concentration of drug that occupies 50% of the receptors at equilibirium
Kd
47
the lower the Kd.... the ____ the binding affinity
higher
| inverse relationship
48
true or false: Drugs are continually binding and dissociating from the receptor population
true
49
why would we use a semilogarithmic plot?
it allows for a much wider range of concentrations to be shown on a single plot
50
a measure of the quantity of drug needed to produce maximal effect
potency
51
EC50 relates to what
concentration
| concentration of drug that generates half (50%) maximal response
52
what is used to compare the potency of 2 agonists against each other?
dose ratios
53
whats the formula for dose ratio
EC50 lower potency drug/EC50 of higher potency drug
54
a measure of the magnitude of the effect once the drug is bound
efficacy
55
concentration of drug that occupies 50% receptors
Kd
| binding affinity
56
concentration of drug that creates 50% maximal response
EC50
| potency
57
the dose for 50% of population to obtain 50% therapeutic efect
ED50
| effective dose
58
dose tht produces death in 50% of the population
LD50
59
a quantitative measure of the safety of a drug
therapeutic index
| LD50/ED50
60
what describes the dosage range between a minimum effective therapeutic concentration and the minimum toxic concentration
therapeutic window
61
what helps assess a drugs safety and effectiveness
the amount of drug that is lethal 1% to test animals divided by the amount that produces a therapeutic effect in 99% of animals
margin of safety
62
label this picture
63
name the differences between an ionotropic receptor and a metabotropic receptor
| 5
* ionotropic has a binding site and channel combined while meta is not associated witha. channel
* iono is second-messenger dependent while meta needs G protein or 2nd messenger involvement
* iono is short latency while meta is longer
* iono has rapid responses, meta slow
* iono is postsynaptic while meta is pre and post
64
name the 5 steps of the G protein-coupled receptor (GCPR) pathway
Epinephrine (first messenger) stimulates GPCR (receptor) bound to Gšs (G protein); GDP (inactive) ļ GTP (active)
Gšs dissociates from Ī²š and GPCR, and binds to and activates adenylyl cyclase (effector)
AC catalyzes the conversion of ATP to cAMP (second messenger)
cAMP activates Protein Kinase A (PKA)
Activated PKA regulates numbers signaling mechanisms that control transcriptional regulation and activity of other enzymes (phosphorylation)
65
identify the G protein subunit and their effector:
Gas:
Ga:
Gšq:
GĪ²š:
Gas: adenyl cyclase (stimulation)
Ga: adenyl cyclase (inhibition)
Gšq: phospholipase (activation)
GĪ²š:
66
what is cyclic adenosine monophosphate derived from and degraded by?
derived: adenosine triphosphate (ATP) thru adenylyl cyclase (AC)
degraded: phosphodiesterases (PDE)
67
what are the two adrenergic receptors
alpha and beta
68
what are the muscarinic receptors
m1,m2,m3,m4,m5
69
true or false: acetylcholine is an endogenous ligand?
true
70
name a few drugs that are antimuscarinics
atropine, glycopyrrolate, scopalamine, ipratropium bromide
71
true or false: GABA is an exogenous ligand
false- it is endogenous
72
sodium depolarizes the cell which them causes ____
Chloride ions hyperpolarizes the cell which then causes ____
stimulation
inhibition
73
which of these are endogenous ligands?
glutamine
glycine
or serotonin
trick questions- they ALL are!
74
ARE 5-HT3 ligan gated ion channels or GCPRs?
ligands
other 5-HT subtypes are GCPRs tho
75
what drug class Binds to region in pore of voltage gated calcium channels that are present in heart and vascular smooth muscle
calcium channel blockers
76
receptor tyrosine kinases particpate in _____
autophosphorylation
77
# name these two terms from the definition:
making RNA from DNA
making protein from RNA
transcription
translation
78
what class of drug Prevents inactivation of second messengers (cAMP, cGMP) ļ ā activation of PKA
phosphodiesterase inhibitors (PDE)
79
COX inhibitors such as NSAIDs and Aspirin are known as _____ while ketoralac and ibuprofen are known as ____
irreversible
reversible
80
what bind to molecules & encapsulate or inactivate it
chelating agents
| such as sugammadex
81
binds to an directly activates a receptor
agonist
82
binds to and blocks the activation of receptor normally activated by the endogenous agonist
antagonist
## Footnote
zero efficacy
83
Agonist that is capable of reaching 100% stimulation at saturating concentrations
full agonist
84
agonists whose maximal simulation <100%
partial agonists
85
can partial agonists block the effect of a full agonist?
YES
86
can agonists also have antagonist activity?
yes
ex: methadone/suboxone
87
which way does the curve shift in the presense of an antagonist?
rightward
88
in the prescence of a fixed amount of antagonist, ____ agonist is required to achieve the same level of response as was seen in the absence of the antagonist
MORE
89
an antagonist binds to the same site on the receptor as the endogenous ligand or agonist (see orthosteric) and competes with it for the binding site
competitive
90
an antagonist binds to a different site on the receptor as the endogenous ligand (see allosteric); or covalently (nonreversible)
noncompetitive
91
which type of binding only allows one molecule to be bound at any given moment?
orthosteric
92
which type of binding allows both molecules to be bound at any given time
allosteric
93
Increase affinity of agonist for receptor
Decrease the off-rate (Koff) of agonist from receptor
positive allosteric modulators (PAMs)
94
Decrease affinity of agonist for receptor
Increase the off-rate (Koff) of agonist from receptor
negative allosteric modulators (NAMs)
95
# name the agonist by the line
96
which two things play a role in the degree of toxicity
EC50 and Emax
97
# label the chart
98
two drugs acting together is the sum of the effects that they would have if acting alone
additive effect
99
two drugs produce effect that is greater than their sum
synergistic effect
100
normla dose of drug produces an increased clinical effect
hyperactive
101
allergic or sensitivity to drug
hypersensitive
102
Decreased response to agonist; requires increasing doses; receptor still on membrane
desensitization
103
Short-term treatment (or one-time dose) causes decreased response (seconds to minutes) e.g. ephedrine
tachyphylaxis
104
: prolonged treatment causes decreased response to same dose (hours to weeks)
tolerance
105
physiologic response to cessation of drug treatment eg. Abrupt cessation of Ī² blockers ļ HTN crisis
withdrawal
106
develop among drugs of same or different class that produce similar effects. Eg. Alcohol and inhalational agents
cross-tolerance
