drug-target pharmacodynamics part 1 Flashcards

1
Q

what is a drug

A

molecules that interact with a biological system to produce a biological response

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2
Q

what is the MW of drugs

A

under 600

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3
Q

are drugs endogenous

A

no

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4
Q

examples of biologics

A

antibodies and proteins

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5
Q

what is drug safety dependent on

A

therapeutic index

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6
Q

how do you make drugs safe

A

keep it between the therapeutic window from efficacy vs toxicity

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7
Q

why are drugs administered

A

to achieve a biological response that alleviates the symptoms or cause of an illness

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8
Q

what is a biological process responsible for

A

producing the symptoms or causing the illness

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9
Q

at the molecular level what is a drug target

A

usually a biomacromolecule (enzyme, receptor, ion channel) that’s involved in the biological process

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10
Q

what are they intermolecular interactions that cause the drug to bind to the receptor

A

hydrogen bonding, VDW or LDF, ionic/electrostatic, pi-pi bonding and dipole interactions

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11
Q

what determines the types of interactions available for drug molecules

A

the functional groups it contains

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12
Q

what determines physiochemical properties such as water solubility and membrane permeability

A

the functional groups present

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13
Q

how do drugs with non polar, aliphatic side groups bind to targets

A

short range vdw forces

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14
Q

how do drugs with aromatic side groups bind to targets

A

short range vdw forces

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15
Q

how do drugs with polar uncharged side groups bind to targets

A

midrange H-bonds

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16
Q

how do drugs with positive and negatively charged side groups bind to targets

A

long range ionic

17
Q

what does the tertiary structure allow the enzyme to do

A

perform its function and maintain the integrity of the active site where catalysis is performed

18
Q

what do the amino acids that border the active site do

A

produce a particular 3D shape that maximises interactions between the enzyme and the substrate which ensure that the substrate is in the correct position

19
Q

how does the movement of the active site lower the activation energy

A

by forcing the substrate into a transition-state confirmation which is why it is catalytic

20
Q

what are the types of interactions between the amino acids that border the active site and the substrate

A

a mixture of H-bonds which are directional and specific for H-bonding groups on the substrate

and short range vdW interactions

21
Q

what is a competitive inhibitor of cox

A

flurbiprofen

22
Q

how does flurbiprofen work

A

it binds in preference to arachidonic acid and blocks prostaglandin synthesis which reduces the inflammatory response

23
Q

how do competitive inhibitors compete with substrates

A
  • must have some structural resemblance so that it can match the 3D shape of the active site
  • must form stronger interactions with the active site so that it binds in preference to the substrate
  • need to stay in longer than the substrate as usually the binding process is dynamic and molecules will associate and dissociate
24
Q

what type of interactions happen between the enzymes that border the active site and an inhibtor/drug

A

the same as the interactions between the substrate and the active site

25
what does endogenous mean
it was produced in the body
26
do biologics follow basic rules of drugs
no
27
what do efflux pumps do
pump molecules that weren't absorbed back out of the intestine
28
what is the primary site of metabolism in the body
the liver
29
what balance of solubility must have
a balance of water and lipid solubility
30
what does low logP/logD mean
low absorption
31
what does high logP/logD mean
high absorption