how do drugs work Flashcards

1
Q

what is the plasma mebrane

A

a selectively permeable barrier between the extracellular environment and the cytosol

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

what are the components of the plasma membrane

A

Na+, K+, Ca2+, Cl-, Glucose

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

is there a similar amount of calcium inside and outside the cell

A

no

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

is there more calcium inside or outside the cell

A

outside

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

how do drugs work

A

once they arrive at the proper site of action, they bind to receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

where are receptors usually located

A

on the outer membrane of cells

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

what does the binding of drugs to receptor do

A

it can sometimes trigger activation of enzymes located within the cell

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

what type of proteins are receptors usually

A

integral membrane proteins at the plasma membrane, can also be found inside the cell

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

what do receptors do

A

recognise and bind to specific chemicals which invokes response

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

can receptor numbers change

A

yes they can be increased (up-regulation) or decreased (down-regulation)

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

why would up regulation or down-regulation occur

A

in response to a chronically low or high concentration of the agonist to optimise sensitivity

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

what two properties do agonists have

A
  1. affinity - strength of binding to receptor
  2. efficacy - intrinsic activity
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

what does efficacy do

A

induces a conformational change in the receptor and activation of a response

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

what property does an antagonist have

A

has affinity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

what does an antagonist do

A

blocks the receptor

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

why can’t antagonists activate a response

A

they don’t have efficacy

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

examples of antagonists

A

anti-histamines, beta-blockers

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

when does down-regulation occur

A

in response to chronically high concentration of ligand.

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

what does down-regulation do

A

decreases the sensitivity of the cell response to frequent or intense stimulation

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

when does up regulation happen

A

in response to very low levels of a ligand

21
Q

what does up regulation do

A

increase sensitivity

22
Q

what underlies disease processes

A

aberrant cellular signalling

23
Q

does the intercellular signal chemical (first messenger) enter the cell

A

no

24
Q

what does binding of the signal chemical to the receptor do

A

initiate a series of chemical changes (activation of intracellular second messenger) in the cell

25
Q

what does signal transduction enable

A

amplification

26
Q

steps of signal transduction

A
  1. direct opening of ion channels
  2. direct activation of an enzyme
  3. indirect activation/inactivation of enzyme, indirect opening/closing of ion channel
    involves a g-protein
  4. intracellular second messengers involved include: Cyclic nucleotides (eg cAMP)
    Inositol triphosphate and diacylglycerol and Ca2+
27
Q

what are 3 G-protein component

A
  1. seven transmembrane receptor where the ligand binds
  2. G-protein (‘switch’ coupling receptor to effector enzyme)
  3. effector enzyme
28
Q

what does GTP bound mean

A

the G protein is on

29
Q

What does GDP bound mean

A

the G protein is off

30
Q

how does a G protein switch itself on and off

A

the protein itself is an enzyme which converts GTP to GDP and thereby switches itself on and off

31
Q

what is the first signal following fertilisation

A

calcium signalling

32
Q

is Ca2+ ever produced or destroyed

A

no it is moved between compartments

33
Q

what does the effects of Ca2+ depend on

A

concentration

34
Q

what are the actions of calcium

A
  • activation of specific protein kinases, ion channels
  • regulation of activity of many enzymes
35
Q

what can Ca2+ channel blockers be used to do

A

modulate muscle contractions

36
Q

what do Ca2+ release channels do

A

release Ca2+ into the cytosol in response to an increase in intracellular IP3 or Ca2+

37
Q

what is the functional effect of Ca2+ release channels

A

contraction, proliferation

38
Q

what are targets for histamine receptors

A

parietal cells - decreased gastric acid secretion

39
Q

what happens when opioid receptors are targeted

A

decreased peristalsis, increases tone of anal sphincter (partly via Ca2+ channel blockade)

40
Q

example of drug that targets histamine receptors

A

ranitidine

41
Q

examples of drugs that targets opioid receptors

A

loperamide

42
Q

what can cause drug side effects (receptor based)

A

when enzymes bind to receptors found in more than one place in the body

43
Q

why is there low levels of calcium intracellularly

A

because calcium is a trigger for many functions

44
Q

what do you need to consider when designing drugs

A

absorption, distribution, metabolism, excretion (ADME)

45
Q

how do receptors work as second messengers

A

chemicals enter cells and bind to the receptors which changes the confirmation of that receptor

46
Q

what is the GI tract predominantly made up

A

smooth muscle

47
Q

how are calcium ions kept low

A

by storing them in many different areas

48
Q

what is a key factor in triggering relaxation in smooth muscle contraction

A

nitric oxide