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342 > drug-receptor interactions 1 > Flashcards

drug-receptor interactions 1 Flashcards

1
Q

the majority of drugs ____/____ normal physiological/ biochemical processes or ____ pathological processes

A

mimic/inhibit
inhibit

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2
Q

the magnitude of a pharmacological response depends on (3)

A

nature of drug molecule
number/ avaliability of drug targets
amount of drug interacting with target

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3
Q

pharmacodynamics is the interaction of a ____ and the interaction with its ____ to form a ____ ____

A

drug (L)
receptor (R)
ligand receptor complex (LR)

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4
Q

what is psilobycin

A

hallucinogenic component in magic mushrooms
prodrug (psilocin is active metabolite)

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5
Q

what is psilocin structurally similar to

A

serotonin - difference in placement of hydroxyl group

(therefore psilocin mimicks serotonin’s endogenous function)

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6
Q

example of drug interfering with body’s pathogenic process

A

beta lactams e.g. penicillin inhibits peptidoglycan inactivating enzymes called penicillin-binding proteins (PBPs) - formation of bacterial cell wall and osmotic pressure, causing to burst

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7
Q

k-1

A

dissociation of drug-receptor complex

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8
Q

what are full agonists

A

produce max. response which system is capable of if given enough of full agonist

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9
Q

drugs that end in mab

A

monoclonal antibody

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10
Q

example where avaliability of targets impacts pharmacodynamics

A

monoclonal antibodies can only be given to patients with an overexpression of HER2 receptor (overexpressed in breast cancer)

overexpression allows antibodies to interact with cancer and not healthy cells containing HER2

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11
Q

drugs have ___ affinity and ___ efficacy to full agonists

A

variable
high

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12
Q

what is an example of a full agonist

A

morphine

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13
Q

what receptor does the full agonist morphine act on

A

mu opioid receptor (MOR)

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14
Q

in sufficient doses, what endogenous function would morphine produce the same effect as?

A

enkephalins - endogenous opioid receptor ligands

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15
Q

neurotransmitters like dopamine and serotonin are ____ while GABA is ____

A

excitatory
inhibitory

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16
Q

what is an example of an endogenous agonist

A

serotonin

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17
Q

what is an example of an exogenous agonist

A

psilobycin (psilocin technically)

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18
Q

what is the mu opioid receptor (MOR)

A

GCPR
for pain relief

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19
Q

what drug is more potent than morphine that also is a full agonist of mu-opioid receptor (MOR)

A

heroin (diamorphine/ diacetylmorphine)

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20
Q

how are potencies typically measured

A

by comparing EC50

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21
Q

compare the EC50s of morphine and heroin (diamorphine/ diacetylmorphine)

A

heroin has a smaller EC50 - less drug is needed to elicit the same response

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22
Q

if codeine has a potency of 0.1, how big of a dose is needed to be equivalent to 10mg of morphine?

A

100mg

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22
Q

if heroin has a potency of 3, how big of a dose is needed to be equivalent to 10mg of morphine?

A

3.33mg

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22
Q

if morphine has a potency of 1, how big of a dose is needed to be equivalent to 10mg of morphine?

A

10mg

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23
Q

if fentanyl has a potency of 100, how big of a dose is needed to be equivalent to 10mg of morphine?

A

0.1mg

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23
Q

if oxycodone has a potency of 1.5, how big of a dose is needed to be equivalent to 10mg of morphine?

A

6.67mg

23
Q

what is a partial agonist

A

produces a response but not fully activates to full response, regardless of dose

23
Q

partial agonists have ____ affinity and ____ efficacy

A

variable
variable

23
Q

what is an example of a partial agonist

A

buprenorphine

24
Q

what does buprenophrine bind to

A

mu opioid receptor (MOR) - high affinity, partially activated

partial agonist

25
Q

what is buprenophrine used for

A

decrease doses to wean patients off methadone - opioid replacement therapy

if not weaned off, sudden withdrawal causes shock and potential death

26
Q

what are antagonists

A

bind with no effect - also called neutral antagonists

27
Q

antagonists have ____ affinity and ____ efficacy

A

variable
no

28
Q

what are the two types of antagonism

A

competitive and non competitive

29
Q

what is competitive antagonism

A

surmountable
prevents activation of receptor

30
Q

what is non-competitive antagonism

A

insurmountable
as binds to separate allosteric binding site - no competition

31
Q

what is an example of a competitive antagonist

A

naloxone
can be used to reverse opioid effects during overdose

32
Q

what does naloxone bind to

A

opioid receptors
prevents activation of mu opioid receptors MOR

33
Q

what is an example of a non competitive antagonist (2)

A

ketamine
cyanide

34
Q

what does ketamine bind to

A

NMDA-glutamate receptors

35
Q

how does naloxone work to reverse opioid overdose

A

naloxone outcompetes opioids (morphine) for binding to the opioid receptors at the same orthosteric site as they are structurally similar, and outcompetes already bound opioids

reverses overdose symptoms e.g. respiratory depression

36
Q

agonists and competitive antagonists bind to the ____

A

orthosteric site

37
Q

what is meant by a competitive antagonist being surmountable

A

the competitive antagonist’s effects can be overcome by increasing dose of agonist

38
Q

compare the dose response sigmoid curve of a agonist vs a competitive antagonist + agonist

A

antagonist shifts curves to right - more agonist needed to overcome antagonist

39
Q

the orthosteric binding site is also called the ____

A

ligand binding site

40
Q

what binds to the allosteric site

A

non competitive antagonists

41
Q

what do non competitive antagonists look like on a dose response sigmoid curve

A

shifts to right but does not reach maximal response

42
Q

how does cyanide work as a non competitive antagonist

A

C triple bond N
non competitive antagonist/ inhibitor of cytochrome c oxidase in ETC, inhibiting ATP production
insurmountable

43
Q

what are allosteric modulators

A

bind to receptor to change receptor’s responses to drug/ stimulus

cannot cause a response alone, only act on response from stimulus

44
Q

what are the two types of allosteric modulators

A

negative allosteric modulator NAM - inhibit
positive allosteric modulator PAM - enhance

45
Q

what is a type of NAM

A

non competitive antagonism

46
Q

how do NAM/PAMs affect dose response curve

A

curve moves to the left as less agonist needed for same response (PAM)
right if NAM

47
Q

what is an example of a negative allosteric modulator (NAM)

A

GABA neurotransmitter

48
Q

what does GABA bind to

A

GABA a or GABA b

49
Q

what is GABA a

A

ionotropic receptor - activation causes receptor to open and allow ions to flow through receptor

50
Q

what occurs when GABAa is activated

A

Cl- ions flow into cell causing hyperpolarisation - inhibits action potential firing, signalling in brain

51
Q

GABAa is activated by ____ (2)

A

GABA binding at orthosteric site
allosteric modulation at BZD allosteric site (PAM)

52
Q

examples of GABAa PAMs

A

benziodiazepines, zolpidem, barbituates

53
Q

what impact do PAMs have on GABAa

A

increase affinity for GABAa of GABA so channel remains open for longer, more Cl- enters neuron, inc hyperpolarisation - the neuron action potential activity is further inhibited

54
Q

what is an inverse agonist

A

inhibit agonist independent low-level signalling
dec response

55
Q

example of an inverse agonist

A

histamine (histamine receptors work without histamine being bound)

were considered prev as antagonists

56
Q

how do anti histamine drugs function

A

prevent histamine activating receptor and constitutive/ independent activity - less effect result

57
Q

what are superagonists

A

capable of producing maximal response beyond than capable max response - unknown how

58
Q

example of superagonist

A

gaboxadol of GABAa receptors

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