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Pharmacodynamics Flashcards

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1
Q

What is delineated under pharmacodynamics?

A

Drug receptors Dose-response curves MOA

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2
Q

What is the difference between a hyperbolic and sigmoidal dose-response curve?

A

Hyperbolic when drug dose vs response Sigmoidal when log of drug dose vs response

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3
Q

What is ED50

A

dose of drug that produces 50% maximal effect

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4
Q

What is Emax

A

maximal drug effect

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5
Q

What is a graded response?

A

Magnitude of response of population mean or single person –> “how much”

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6
Q

What is a quantal response?

A

frequency of individuals responding to a pre-defined variable

–> does a response occur, in how many yes or no, binary responses

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7
Q

Describe cumulative vs noncumulative quantal dose-response graphs

A

Cumulative: resposne of individuals to the dose and all doses lower than it

Noncumulative: response of individuals to only one dose

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8
Q

What are ED50, TD50 and LD50 in a cumulative quantal dose-response graph?

A

ED50: median effective dose

TD50: median toxic dose

LD50: median lethal dose

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9
Q

What is the equation for a therapuetic index?

A

TD50/ ED50

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10
Q

The higher the TI, the …

A

safer the drug

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11
Q

What is the therapeutic window?

A

range of doses that provides safe and effective therapy

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12
Q

Is it better for a drug to have a narrow or high therapeutic window?

A

High–> more space between therapeutic effect and adverse reaction

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13
Q

What is potency?

A

amount of drug required to produce specific pharm effect

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14
Q

What represents potency?

A

ED50

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15
Q

The lower the ED50, the…

A

more potent the drug

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16
Q

What is efficacy?

A

maximal pharm effect that a drug can produce

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17
Q

What represents efficacy?

A

Emax

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18
Q

The greater the Emax, …..

A

the more efficacious the drug

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19
Q

What relates the total number of receptors available to bind a drug?

A

efficacy

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20
Q

What kind of bonds do most drugs bind?

A

non-covalent

Reversible (ionic, hydrogen, hydrophobic)

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21
Q

Why aren’t covalent bonds used with most drugs?

A

since irreversible bonds, must resynthesize receptor or remove drug via enzyme

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22
Q

Describe relationship of Kd to affinity

A

inverse

low Kd, high affinity

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23
Q

Describe affinity in terms of drug dose

A

inverse

high affinity, low drug dose required

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24
Q

What affinity requires more drug due to poor receptor-drug interaction?

A

low affinity

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25
What is the relationship of Bmax to Emax?
Bmax is maximal binding on a drug-receptor curve Emax is maximal effect of drug on dose-response curve BOTH look the same on graph--\> Kd=EC50 on x axis
26
What is the difference between Kd and EC50?
same thing--\> Kd used on drug-receptor graph, EC50 used on dose-response graph
27
What is the relationship of Kd to selectivity?
higher Kd, lower affinity, more selective, affects fewer targets, fewer adverse effects
28
Do agonists or antagonists have intrinsic activity?
Agonists ONLY
29
What is intrinsic activity?
ability of drug to change receptor function and produce physiological response on binding
30
Do antagonists change receptor function?
NO, no intrinsic activity to prevent agonist from binding instead
31
What types of agonists exist?
Full Partial Inverse
32
Describe full agonists
fully activate receptors produce maximal effect when all receptors occupied maximal intrinsic activity
33
What is a main difference between full and partial agonists?
intrinsic activity
34
Describe partial agonists
partially activate receptor on binding produce sub-maximal effect when all receptors occupied intrinsic efficacy varied (always sub-maximal)
35
Describe inverse agonists
decrease receptor signaling decrease response at receptors intrinsic activity present and related to inhibition of receptor function opposite of full and partial agonist
36
What types of antagonists exist?
pharmacologic chemical physiologic
37
Describe pharmacologic (receptor) antagonism
act as same receptor as endogenous ligand or agonists
38
Describe chemical antagonism
makes another drug unavailable DOESN'T interact with receptor
39
Describe physiologic antagonism
1 pathway antagonizes another pathway with different receptors
40
What types of pharmacologic antagonists exist?
Competitive and Non-competitive
41
Can competitive antgonist be displaced?
yes if enough drug is there
42
What are the types of non-competitive antagonists
Irreversible Allosteric
43
Why are irreversible antagonists irreversible
they form covalent bonds over binding site
44
Action of allosteric antagonist
bind to site other than agonist binding site--\> prevent or reduce binding OR prevent activation of receptor
45
EC50 increases Emax does not change
competitive antagonist
46
Emax decreases EC50 does not change
noncompetitive antagonist
47
Which antagonist is this
competitive antagonist
48
Which antagonist is this
Noncompetitive
49
What is the function of a full agonist
mimiks action of endogenous chemicals at receptors
50
What drugs can block actions of endogenous ligands at receptors?
antagonists partial agonist inverse agonist
51
What are drugs designed to target
important regulatory proteins in signaling pathways
52
What part of the G-protein receptor has GTPase activity
alpha subunit
53
What does Gs activate
adenylyl cyclase--\> AC activation
54
What does Gi activate
adenylyl cyclases--\> AC INHIBITION
55
What does Gq activate
phospholipase C--\> PLC activation
56
What does G 12/13 activate
Rho GTPases--\> cytoskeletal rearrangements
57
What downregulates G-protein receptors
beta-arrestin G-protein coupled receptor kinase protein phosphatase
58
What trigger JAK receptors
growth hormone erythropoietin leptin INF-2, 10, 15
59
Why are receptor tyrosine kinases target for cancer drugs?
oncogenes in growth factor pathways point mutation sites in cancer anticancer drugs inhibit upregulated GF signaling
60
Point mutations in Ras cause what cancer
pancreatic adenocarcinoma
61
Point mutations in Raf cause what cancer
melanoma
62
Where are nuclear receptors
cytoplasm
63
What activate nuclear receptors
lipophilic so can cross into cytoplasm and activate receptor steroid and thyroid hormones vitamins D and A lipid mediators
64
Why is L-type calcium channel a drug target?
everywhere, can cause arrhythmias, angina, HTN, constipation

Pharmacology (6 decks)

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