Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

NS2 Pharm > Introduction to pharmacodynamics > Flashcards

Introduction to pharmacodynamics Flashcards

1
Q

Difference between pharmacokinetics and pharmacodynamics

A

kinetics–effects of body on drugs

dynamics effects of drugs on body

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

covalent bonds

A

irreversible

drug removal/receptor re-activation requires resynthesis of the receptor or enzymatic removal of the drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

non-covalent bonds

A

reversible

most drugs bind to receptors via non-covalent bonds

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

non covalent bonds strongest to weakest

A 
ionic bonds (bw positive and negative charged ions)
hydrogen bonds (electrostatic bond bw net positive charge of H and net negative charge of electronegative atom
hydrophobic interactions (bw hydrophobic regions of the drug and receptor)
van der waals forces (weak electrostatic interactions involving dipole moments within functional groups)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

dose-response curve presented 2 ways. What are the two ways and what are the differences between the two?

A
  1. Arithmetically–drug dose vs. drug effect=hyperbolic curve
  2. Logarithm of drug dose vs. effect=sigmoidal curve
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is the drug response curve?

A

relationship bw drug dose and its effects
drug dose on x axis
drug effect on y axis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

dose response cruve 2 phases

A

linear phase
plateau phase
hyperbolic curve or sigmoidal curve

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

dose-response curve is more commonly presented how?

A

logarithm of drug dose vs. response
sigmoidal curve
still have linear phase and plateau phase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is EMax?

A

maximal effect that can be produced by the drug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

wHAT IS ED50?

A

Effective Dose 50

dose of drug that produces 50% of maximal effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

3 parameters describing the interaction of a drug with a receptor

A

affinity
selectivity
intrinsic activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

what is affinity?

A

how readily/tightly a drug binds to its rec
high affinity=good drug-rec interaction; LESS drug needed to produce a response
Low affinity=poor drug-receptor interaction; MORE drug needed to produce a response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What describes the affinity?

A

Kd (equilibrium dissociation constant)–molar concentration is the unit
drug conc at which 50% of the drug rec binding sites are occupied by the drug
lower Kd=higher affinity of drug for rec
higher Kd=lower affinity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is selectivity?

A
  • property of a drug determined by its affinities at various binding sites
  • measured by comparing affinities of a drug to different receptors
  • MORE selective drug affects FEWER targets
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What is intrinsic activity?

A

ability of a drug to change a receptor function and produce a physiologic response upon its binding to the rec

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What do agonists do?

A

bind to rec and stabalize it in a particular conformation (usually the active conformation), producing a physiologc response
-have intrinsic activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What do antagonists do?

A

bind to rec but dont change its function
prevent action of the receptor in presence of agonist
do NOT have intrinsic activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What do full agonists do?

A

fully activate receptors
produce a maximal pharmacological effect when all receptors are occupied
MAXIMAL intrinsic activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What do partial agonists do?

A

partially activate receptors
produce a sub-maximal pharmacological effect when all receptors are occupied
intrinsic efficacy varies depending on drug but is ALWAYS SUBMAXIMAL

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What do inverse agonists do?

A

decrease receptor signaling
decrease response at receptors with a level of constitutive receptor activity
intrinsic activity is present–inhibits receptor function

21
Q

What do antagonists do?

A

do not change function of receptor upon binding
no pharmacological effect in absence of agonists
no intrinsic efficacy

22
Q

Difference in Emax between full agonists and partial agonists

A

Emax is lower in partial agonists than in full agonists

23
Q

Pharmacologic (R) antagonism

A

action at the same Rec as endogenous ligands or agonist drugs

24
Q

What is chemical antagonism?

A

When chemical antagonist make the other drug unavailable

25
Q

What is physiologic antagonism?

A

Occurs bw endogenous pathways regulated by different receptors

26
Q

Types of pharmacologic antagonism

A

competitive and non competitive

27
Q

what do competitive antagonists do?

A

compete with endogenous chemicals or agonist drugs for binding of receptors
can be displaced from the receptor by other drugs

28
Q

What do non-competitive antagonists do and what are the two types?

A

Receptor inactivation not possible

two types: irreversible and allosteric

29
Q

How do irreversible antagonists work?

A

irreversibly bind to and occlude the agonist site on the rec by forming covalent bonds

30
Q

How do allosteric antagonists work?

A

bind to a site other than the agonist site to prevent or reduce agonist binding or activation of receptor

31
Q

competitive antagonism graph

A

agonist EC50 increases

Emax does not change

32
Q

Non-competive antagonism graph

A

agonist Emax decreases and EC50 does not change

33
Q

Beneficial effects of a drug–full agonists

A

mimic the actions of endogenous chemicals at receptors

Example: action of mu opiod receptors by opiod analgesics–pain killers)

34
Q

Beneficial effects of a drug–antagonists, partial and inverse agonists

A

blocks the endogenous ligands at receptors

example–blocking alpha adrenoceptors by antihypertensive drugs

35
Q

beneficial and adverse effects are mediated by the same receptors/signal transduction pathway on the same cell types…how to manage?

A

a tight dowse control–can become toxic with too much drug

example: insulin

36
Q

beneficial and adverse effects are mediated by the same receptors/signal transduction pathway on different cell types–how to manage?

A

avoid systemic administration

example: B2 agonist relaxes bronchial smooth muscle; increases breakdown of glycogen in liver

37
Q

beneficial and adverse effects are mediated by different types of receptors

A

highly selective drugs–have less side effects

lower selectivity leads to increased incidence of side effects

38
Q

What is potency?

A

amount of drug required to produce a specific phamacological effect
drugs with higher affinities for a recepter (lower Kd)=more potent

39
Q

What is efficacy?

A

maximal pharmacological effect that a drug can produce
related to total number of receptors available to bind a drug (Bmax)
higher Bmax=higher efficacy

40
Q

what is potency represented by?

A

amount of drug required to produce a specific effect
ED50
lower ED50=more potent drug

41
Q

What is efficacy represented by?

A

maximal effect that a drug can produce
represented by Emax
greater Emax=more efficacious

42
Q

What is a graded response and what does it answer?

A

answers “how much?”
response varies
mean value within a population or single subject

43
Q

what does quantal response answer?

A

does the response occur or not?
in how many?
pre-defined response
frequency of a response within large population

44
Q

graded-dose response curve

A

relates dose to the magnitude of a drug’s effect on a continuous scale (how much)

45
Q

What does a quantal dose response curve do?

A

relates dose to frequency of a response within general population (in how many)

46
Q

what is a non-cumulative quantal dose response curve?

A

number or % of individuals responding at a dose of a drug and only at that dose

47
Q

cumulative quantal dose response curve

A

number or % of individuals responding at a dose of a drug AND at all doses lower than that dose

48
Q

TI (therapeutic index)

A

TI=TD50/ED50
higher the TI=safer the drug
ED50=median effective dose
TD50=median toxic dose

49
Q

therapeutic window

A

range of doses of a drug or of its concentration in a bodily system that provides safe and effective therapy

NS2 Pharm (6 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions