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Neuro 2 Exam 1 > Intro to Pharmacodynamics > Flashcards

Intro to Pharmacodynamics Flashcards

1
Q

Receptor:

what role does it play?

initiates what events?

A

regulatory role

interacts with a drug and initiates the biochemical events leading to drug effect

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2
Q

Drug-Receptor Interaction–> Covalent

  • can it be reversed?
  • reactivation requires?
A

Irreversible and reactivation requires resynthesis of the receptor or enzymatic removal of the drug

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3
Q

Drug Receptor Interaction–> Noncovalent

  • is it reversible?
  • how common
A

reversible, most drugs bind to receptors via non-covalent bonds

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4
Q

Strongest to weakest drug receptor interactions

(four)

A

Ionic>hydrogen>hydrophobic>Van der waals

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5
Q

Hyperbolic curve

x axis?

y axis?

A

drug dose on the x axis

drug effect on the y axis

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6
Q

how do you get a sigmoidal dose response curve?

-x, vs y axis

A

log of drug dose on x

response on y

more common than hyperbolic curve

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7
Q

Emax

-define

A

The maximal effect that can be produced by the drug

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8
Q

ED50

A

The dose of the drug that produces 50% of its maximal effect

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9
Q

Graded Response curve:

  • what question does it answer?
  • What varies continuously?
  • represents mean value of what?
A

Answers the question how much

magnitude of a response varies continously

typically represents the mean value within a population or a single subject

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10
Q

Quantal Response:

  • question it answers
  • type of response
  • requires what
  • used for what?
A

all or none; yes-no binary response

  • does the response occur or not?
  • in how many?
  • requires a pre-defined response (death, falling asleep, 10% reduction in bp)
  • used to examine the frequency of the number of individuals showing a response within a large population
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11
Q

non-cumulative quantal dose-response curve

-define

A

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

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12
Q

Cumulative quantal dose response curve

-define

A

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

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13
Q

Therapeutic index:

  • what ratio?
  • meaning of the value?
A

TD50/ED50

higher the TI the safer the drug

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14
Q

Therapeutic window:

-define

A

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

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15
Q

KD:

  • meaning of this value
  • unit
  • low vs high
A

KD is the equilibirum dissociation constant, which is the drug concentration at which 50% of the drug receptor binding sites are occupied by the drug

  • unit is molar concentration
  • lower the value, higher the affinity of a drug for a receptor

Where [L], [R] and [LR] represent molar concentrations of ligand, receptor, and their complex

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16
Q

What is the EC50

-how is it different than KD

A
  • It is simply the concentration of agonist required to provoke a response halfway between the baseline and maximum responses. Because the EC50 defines the location of the dose-response curve for a particular drug, it is the most commonly used measure of an agonist’s potency.
  • However, the EC50 is usually not the same as the Kd for the binding of agonist to its receptor – it is not a direct measure of drug affinity.
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17
Q

-Magnitude of a drug’s effects will be proportional to what?

A

proportional to the degreee of its interaction with a receptor

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18
Q

Drug selectivity:

  • define
  • measured how?
A
  • property of a drug determined by its affinities at various binding sites
  • measured by comparing affinities of a drug to different receprots
  • a more selective drug would affect fewer targets over a specific concentration range (therapeutic range)
19
Q

Intrinsic activity:

-define

A

ability of a drug to change a receprot function and produce a physiological response upon its binding to a receptor

20
Q

Agonist

-definition, does it have intrinsiv activity?

A

bind to the receptor and stabilize it in a particular conformation (usually active), producing a physicological response

*have an intrinsic activity*

21
Q

Antagonist

  • define, does it have intrinsic activity?
  • effect in absence of an agonist?
A
  • receptor antagonists bind to the receprot but do not change its function. however, they prevent activation of the receport in the presence of an agonist
  • don’t have intrinsic activity
  • don’t change function of receptor upon binding
  • no pharmacological effect in the absence of an agonist
22
Q

Full agonist:

  • when do they produce maximal pharm. effect?
  • intrinsic activity levels?
A

fully activate receptors producing a max pharm effect when all receptors are occupied

-maximal intrinsic activity

23
Q

partial agonist:

  • describe activation of receptor
  • pharm effect
  • intrinsic efficacy
A

partially activate the receptor upon binding

  • produce a sub-maximal pharm effect when all receptors are occupied
  • intrinsic efficacy varies depending on drug, but ALWAYS submaximal
24
Q

Inverse Agonists:

  • effect on receptor signaling
  • constitutive receptor activity?
  • intrinsic activity, why?
A
  • decrease receptor signaling
  • decrease response at receprotrs with a significant level of constitutive receptor activity
  • intrinsic activity is present and related to the inhibition of receptor function
25
Q

Pharmacologic antagonism

Chemical antagonism

Physiologic antagonism

A

Pharm: (receptor) antagonism action at the same receptor as endogenous ligands or agonist drugs

Chemical: when chemical antagonist makes the other drug not available

Physiologic: occurs between endogenous pathways regulated by different receptors

26
Q

Competitive antagonist:

  • compete with what?
  • can be displaced by what
A
  • compete with endogenous chemicals or agonist drugs for binding to the receptor
  • can be displaced from the receptor by other drugs (effects are surmountable)
27
Q

Non-competitive antagonists:

types, define (x2)

A

-receptor inactivation is not surmountable

Irreversible antagonists: irreversibly bind to and occlude the agonist site on the receptor by forming covalent bonds

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

28
Q

Competitive antagonism:

  • EC50 effect
  • Emax effect
A

-EC50 increases, Emax does not change

29
Q

Noncompetitive antagonism:

  • effect on EC50
  • effect on Emax
A

EC50 does not change, but Emax decreases

30
Q

Drug Potency:

  • define
  • what drugs tend to be more potent
  • what value represents drug potency? (lower vs higher)
A
  • Potency describes the amount of drug required to produce a specific pharmacological effect
  • drugs with higher affinities for a receptor–> lower KD tend to be more potent
  • potency describes the amount of drug required to produce a specific effect and is represented by the ED50–> the lower the value, the more potent

*determines the drug dose that will be used clinically*

31
Q

Drug Efficacy:

  • define
  • represented by what value?
  • efficacy is related to total number of?
  • determines clinical what?
A
  • describes the maximal pharmacological effect the drug can produce
  • represented by the Emax, the greater the Emax the more efficacious the drug
  • efficacy is related to the total number of receptors available to bind a drug, and it determines the clinical effectiveness of a drug
32
Q

Describe increasing potency vs increasing efficacy graphs

A
33
Q

microgram

-define

A

1/1000th of a milligram, which is 1/1000th of a gram

34
Q

1 kg = how many pounds?

A

2.2

35
Q

Volume:

-tsp, tbsp, ounce, cup

A
36
Q

Volume:

  • ml/cc
  • quart=how many ml? how many pints in quart?
  • pint=ml? how many oz in one pint?
  • gallon=how many L? quarts in a gallon? pints in gallon?
A
37
Q

Dosing Frequency abbreviations:

  • qd
  • bid
  • tid
  • qid
  • qod
  • q”x”h
A
38
Q

Dosing frequency:

  • qam
  • qpm
  • qhs
  • prn
  • ac
  • pc
A
39
Q

Routes of administration:

  • od
  • os
  • ou
  • ad
  • as
  • au
  • gtt
A
40
Q

Routes of administration:

  • po
  • sl
  • iv
  • im
  • sq
  • pr
  • NGT
  • OGT
A
41
Q

abbreviations:

  • ut.dict.
  • tra
  • kvo
A
  • as directed
  • to run at
  • keep vein open
42
Q

of gms in 100ml

A

W/V%

43
Q
A

Neuro 2 Exam 1 (7 decks)

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