pharmacodynamics Flashcards

1
Q

what is pharmacodynamics

A

the study of the effects of drugs and their mechanism of action

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2
Q

what are the 4 categories where drugs exert effect

A
  • receptors
  • ion channels
  • transporters
  • enzyme
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3
Q

what is an acellular interaction

A

no cells to interact with

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4
Q

how do receptors work

A

macromolecules on a cells surface that have an effect when a drug binds to it

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5
Q

what are agonists

A

a drug that interacts with a receptor and initiates a cellular reaction similar to its endogenous neurotransmitter

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6
Q

what are antagonists

A

a drug that interacts with a receptor that is unable to induce a cellular rection

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7
Q

what factors affect a drugs affinity to its receptor

A
  • size
  • electrical charge
  • shape
  • atomic composition
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8
Q

what is efficacy

A
  • intrinsic activity of a drug that determines its ability to produce an effect - Emax
  • the maximum response achievable
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9
Q

what is potency

A
  • a measure of necessary amount of the drug to produce an effect of a given magnitude - ED50
  • the strength of the drug for the needed effect
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10
Q

how does ED50 work

A

the lower the ED50 the more potent as less of a drug is needed to produce the same effect

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11
Q

what is a partial agonist

A

produces maximal effect but is less than the amount produced by a full agonist

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12
Q

what is a full agonist

A
  • has a high affinity for a receptors
  • produces maximal response by occupying a fraction of receptors
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13
Q

what is the purpose of an antagonist

A
  • prevent agonist from binding
  • no effect on biological function
  • decreases effect of agonist
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14
Q

what are the different types of antagonism

A
  • reversible antagonism
  • irreversible antagonism
  • non-competitive
  • functional
  • chemical
  • physical
  • pharmacokinetic
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15
Q

what is reversible antagonism

A
  • able to bind to the receptor but can be released
  • higher agonist will displace antagonist
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16
Q

what is irreversible antagonism

A

antagonist binding can’t be displaced = covalently bonded

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17
Q

what is non-competitive antagonism

A

the antagonist binding site is not the active site

18
Q

what is functional antagonism

A

antagonist that works on a different receptor but results in reducing the effect of the other drug

19
Q

what is chemical antagonism

A

the chemical combination of an antagonist with the substance it is antagonising

20
Q

what is physical antagonism

A

based on the physical properties of the drug

21
Q

what is pharmacokinetic anatgonism

A

when one drug accelerates the metabolism or elimination of another

22
Q

what are the pharmacological actions targeting enzyme

A
  • enzyme inhibitors
  • false substrates
  • prodrugs
23
Q

what are the different types of competitive inhibition

A
  • reversible - change back to original state
  • irreversible - can’t change back
24
Q

what are false substrates

A

drug molecules which chemically change to form abnormal products that overthrow the normal metabolic pathway

25
Q

what are prodrugs

A

drugs needing enzyme degradation to convert from inactive to active to have a therapeutic effect

26
Q

what is the function of carrier proteins

A

to selectively uptake and efflux compounds either unidirectionally or bidrecetionaly

27
Q

how do replacement molecules affect carrier proteins

A

replacements resemble indigenous molecules so they can travel through carrier proteins as they look the same

28
Q

how do inhibitors affect carrier proteins

A

prevent transport of molecules

29
Q

how do selective serotonin reuptake inhibitors work

A
  • block uptake of 5-HT by nerve terminals in brain
  • increasing 5-HT levels depresses symptoms
30
Q

how do false substrates affect carrier proteins

A
  • out-compete natural ligand for the carrier protein
  • transporter takes them up as they resemble the substance in our body
31
Q

example of false substrate on carrier proteins

A

methyldopa taken up by noradrenaline transporter -> false transmitter a-methylNA -> accumulates and displaces methylNA -> released -> less active than NA on a receptors -> less effective vasoconstriction

32
Q

how do ion channels work

A

selectively allow passage of ions that can’t go through the lipid bilayer

33
Q

how can drugs affect ion channel function

A
  • activator
  • inhibitor
34
Q

what indirect actions can drugs have on ion channels

A
  • intracellular signalling molecule
  • produce effects on channel
35
Q

what are acellular substances cause pharmacodynamic effects

A
  • antacids
  • heavy metal chelators
  • absorbing agents
36
Q

what is the therapeutic index

A

ratio of dose producing toxicity in half the population to a dose producing a desired response in half the population

37
Q

what is the calculation for therapeutic index

A

TI = TD50/ED50

38
Q

what does a large therapeutic index show

A

a wide margin between doses that are effective and doses that are toxic

39
Q

what is the therapeutic window

A

the concentration range over which a drug produces its therapeutic effect

40
Q

what does a low therapeutic index mean

A

giving a higher dose that what is minimally required to get the desired effect can cause adverse effects

41
Q
A