intro to pharmacology Flashcards

1
Q

what is pharmacology?

A

the study of substances that interact with living systems through chemical processes

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2
Q

define drug

A

any substance that interacts with a molecule or protein that plays a regulatory role in living systems

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3
Q

define endogenous drugs

A

drugs originating inside the body, including hormones

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4
Q

define poisons

A

drugs that almost exclusively have harmful effects

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5
Q

why are all drugs poisons?

A

because all drugs have adverse effects

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6
Q

what are toxins?

A

poisons of biological origin, usually synthesised by plants or animals

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7
Q

define receptor

A

a specific molecule (usually a protein) that interacts with a specific chemical, causing a change in the receptor that produces a regulated function

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8
Q

name the types of receptors

A

ion channels
g-protein coupled receptor
RTKs
intracellular hormone receptors (nuclear receptor)

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9
Q

what is the largest category of receptor?

A

GCPRs

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10
Q

what is an agonist

A

any drug that binds to a receptor and activates it

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11
Q

name the types of ion channels

A

ligand gated
voltage gated
2nd messenger regulated

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12
Q

how does an agonist work?

A

mimics the natural ligand of the receptor. when the agonist leaves the receptor is usually deactivated and the effect stop

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13
Q

give some examples of agonists that cause a covalent change in the receptor

A

aspirin - makes a covalent change in the receptor that keeps anti-platelet action on for the life of the platelet

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14
Q

what is a partial agonist?

A

an agonist that binds to a receptor at the active site but is unable to cause maximal response even if all the receptors are occupied

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15
Q

why are partial agonists useful?

A

its hard to give an overdose with them

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16
Q

why do partial agonists have a smaller effect than full agonists?

A

they bind with a lower affinity for the receptor so they dont bind as strongly

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17
Q

why does a partial agonist block the full agonist?

A

because they both bind to the same active site

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18
Q

what is an inverse agonist?

A

an agonist that produces a response below the baseline response. it has an opposite effect to an agonist

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19
Q

give an example of an inverse agonist and how it works

A

antihistamine - binds to a histamine receptor and stabilises it so it stops mast cells and basophils from releasing histamine granules and causing an immune response

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20
Q

what is an antagonist?

A

any drug that binds to the receptor and prevents activation of the receptor

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21
Q

define competitive antagonist

A

a drug that competes with the endogenous ligand for the the binding site. fits into active site and prevents activation of the receptor

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22
Q

define non-competitive antagonist

A

a drug that binds to the receptor at a point that isn’t the binding site

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23
Q

what is a chemical antagonist?

A

a chemical that binds directly to an agonist and prevents it from binding to a receptor

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24
Q

what is a physiological antagonist?

A

when 2 substances have exactly opposite actions via different pathways

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25
Q

what does ADME stand for?

A

absorption
delivery
metabolism
elimination

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26
Q

what is a strong acid?

A

an acid that dissociates completely into a negative ion and a proton

27
Q

what is a weak acid?

A

an acid that only partially dissociates

28
Q

which form of a drug is lipid soluble?

A

undissociated form

uncharged and protonated

29
Q

which form a drug is water soluble?

A

dissociated form

30
Q

what is the advantage of a drug being a weak acid/base?

A

it can switch between the dissociated and undissociated form so it can travel through different parts of the body

31
Q

in acidic solution, what form is a weak acid drug going to be in and why?

A

in the uncharged and undissociated form because the H+ ions in solution push the equilibrium to the left

32
Q

in alkali solution, what form is a weak acid drug going to be in and why?

A

charged and dissociated form because fewer H+ ions so equilibrium moves to the right

33
Q

when does pKa = pH?

A

when there is complete balance between the uncharged and charged form of the drug

34
Q

what is the range of pH of the body?

A

7.35-7.45

35
Q

what form is a weak acid drug generally going to be in the body and why?

A

charged and dissociated form because body pH is slightly alkaline so equilibrium shifts to the right to make more H+

36
Q

where is most of the protonated form of a drug found?

A

in the stomach

37
Q

what are drugs filtered by?

A

the glomerulus of the kidney

38
Q

what form of a drug will be reabsorbed back into the blood in a kidney?

A

a protonated, undissociated drug

39
Q

in what pH blood is a weak acid drug excreted fastest and why?

A

alkaline urine because more will be in the unprotonated form

40
Q

in what form will a drug be excreted?

A

dissociated form

41
Q

in what pH blood is a weak alkali drug excreted fastest?

A

acidic

42
Q

what is specificity?

A

which organ(s) a drug works on

43
Q

what is selectivity?

A

what receptor a drug binds to to produce an effect?

44
Q

define affinity

A

how tightly the drug binds to the receptor

45
Q

what bonds can a drug bind to a receptor with?

A
covalent
ionic
electrostatic
lipophilic
van der waals
46
Q

define pharmacokinetics

A

actions of the body on the drug

47
Q

define pharmacodynamics

A

actions of the drug on the body

48
Q

why is a logarithmic scale used?

A

easier to get dose reading on a logarithmic scale

49
Q

what is the maximal response?

A

the point where there is no further increase in response

50
Q

what does EC mean?

A

concentration

51
Q

what does ED mean?

A

dose

52
Q

what does EC50 mean?

A

the drug concentration at half the maximal response

53
Q

how can you tell a drug is a competitive antagonist from a graph of response against concentration?

A

need to add more of the drug to get a response. with enough of the agonist added, a maximal response can be achieved

54
Q

how can you tell a drug is a non-competitive antagonist from a graph of response against concentration?

A

maximal effect is reduced
no matter how much agonist you bind, it cannot activate receptor at the same level bc the receptors its binded to cannot be used anymore.

55
Q

do all receptors have to be occupied to produce a response?

A

no

56
Q

how do spare receptors impact a tissue’s response to a ligand?

A

increase sensitivity and speed of the response

57
Q

define efficacy

A

the maximal effect that a drug can produce regardless of dose

58
Q

define potency

A

the amount of drug that is needed to produce a given effect

59
Q

what determines potency?

A

affinity of a drug for a receptor and the number of receptors available

60
Q

which axis does the curve move in to show potency

A

horizontally

61
Q

which axis does the curve move to show efficacy?

A

vertical

62
Q

if a drug is more potent, which direction does the curve move in?

A

the right

63
Q

if a drug has a lower efficacy, which way does the curve move in?

A

down

64
Q

define intrinsic activity

A

the ability of a ligand to bind to receptors and activate them