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Foundations in Medicine 1 > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

What is an agonist?

A

a drug or molecule that binds to its receptor AND causes a downstream biological effect

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2
Q

What is an antagonist?

A

a drug or molecule that binds to its receptor physically preventing another substance bind therefore preventing downstream effects indirectly

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3
Q

What are ligand-gated ion channels?

A

transport that requires a ligand to bind thus allowing the transfer of ions through the membrane

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4
Q

Give an example of g-protein coupled receptors?

A

adrenoreceptors

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5
Q

what hormone binds to adrenoreceptors?

A

adrenaline

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6
Q

adrenoreceptors are involved in the parasympathetic response, true or false

A

false, they are involved in the sympathetic response as they respond to adrenaline

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7
Q

Give an example of a drug that uses kinase linked receptors?

A

insulin

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8
Q

What is the role of alpha 1 and 2 adrenoreceptors upon stimulus by adrenaline?

A

1 - g protein couples with phospholipase C causing vasoconstriction

2 g protein blocks the activity of adenyl cyclase preventing ATP-generated cAMP and increasing potassium channels thereby relaxing the GI tract

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9
Q

adrenoreceptor beta 1 causes dilation of the bronchi, true or false?

A

false, this is the role of adrenoreceptor 2

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10
Q

How do beta adrenoreceptors illicit downstream effects?

A

upon binding of adrenaline to the receptor the g protein is activated and then binds to adenyl cyclase, this allows ATP to produce cAMP

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11
Q

What are the physiological effects of beta 1 2 and 3 adrenoreceptor stimulation?

A

1 - increased heart rate and cardaic muscle contraction
2 - bronchial-dilation
3 - thermogenesis of skeltal muscle

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12
Q

what is an example of a drug that is a beta 2 adrenoreceptor agonist?

A

salbutamol

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13
Q

What partial agonists reduce heart rate and bind to beta-adrenoreceptors?

A

propanolol and pindolol

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14
Q

What is a partial agonist?

A

a drug or molecule that exerts sub-maximal responses

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15
Q

What is the EC50

A

the minimum plasma concentration required for the drug to be effective

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16
Q

What is efficacy?

A

tendency of the drug to activate the receptor and result in a biological response

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17
Q

What is affinity?

A

tendency of the drug to bind to its receptor successfully

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18
Q

What drug compensates for the adrenoreceptor downregulation?

A

theophylline
also inhibits phosphodiesterase

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19
Q

What are nuclear receptors?

A

protein monomers located in the nucleus of target cells and contain DNA binding domains

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20
Q

What is Ka

A

dissociation equilibrium constant

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21
Q

what is the dissociation equilibrium constant (Ka)?

A

the concentration at which the ligand occupies 50% of the receptors

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22
Q

Give an example of an antidepressant that is a antagonist?

A

amitryptiline

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23
Q

What drug is a calcium channel blocker and important for hypertension?

A

amlodipine

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24
Q

What enzymes does ibuprofen block

A

Cox1 and Cox2

25
Q

What is the mechanism of amlodipine?

A

calcium channel blockers used for hypertension

26
Q

Which beta receptor does propranolol primarily target and which is the secondary target?

A

primary - beta 1 adrenoreceptor
secondary - beta 2 adrenoreceptor

27
Q

propranolol is an agonist, true or false?

A

false it is an antagonist

28
Q

Are SSRIs antagonists or agonists?

A

they are antagonists that bind to SERT which usually reuptakes excess serotonin leaving more freely available in the synapse

29
Q

If EC50 of Drug A is 0.5 and Drug B is 1.4, which has the higher potency?

A

Drug A

30
Q

ionised molecules readily diffuse over membranes, true or false

A

false, unionised diffuse more readily because they are non-polar

31
Q

What is Pka?

A

the pH at which 50% of the drug is ionised and 50% is unionised

32
Q

Which two types of transport can be involved in saturation kinetics

A

facilitated diffusion and active transport

33
Q

active transport requires ATP and occurs along the concentration gradient, true or false?

A

false, it does require ATP but occurs against the concentration gradient

34
Q

What does the Henderson hasslebach equation tell us?

A

how drugs ionise each other at different pH levels

35
Q

Why will a weak base be absorbed in the gut more readily?

A

because it has a higher pH - more basic conditions which is favourable to a weak base

36
Q

weak acids are ore readily absorbed by the stomach, true or false?

A

true because it has a lower pH

37
Q

how much body water does the intracellular fluid/water comprise?

A

2/3

38
Q

what is the equation for the apparent volume of distribution (Vd)?

A

dose/drug plasma concentration

39
Q

what does a low Vd suggest about the drug distribution in the body?

A

it is retained in the vascular compartment

40
Q

what does a high Vd suggest about the drug distribution in the body?

A

the drug can be found in non-vascular compartments such as the muscle and adipose tissue

can also find plasma protein binding

41
Q

What is the most abundant plasma-binding protein

A

albumin

42
Q

What is the bioavailability?

A

The amount of drug that reaches circulation

43
Q

lipophilic drugs tend to have a high Vd, true or false

A

true, as they are uptaken by fatty tissue

44
Q

What is the equation for bioavailability (f)?

A

F = quantity of drug that reached circulation/dose

45
Q

What is the responsibility of cytochrome P450 (CYP450)

A

It is an enzyme family that can modify the drug making it more excretable and activating drugs in some cases influencing drug interactions

46
Q

What happens during phase II reactions

A

the drugs are modified to become more polar (different molecular groups added on) and more readily excreted from the kidneys

47
Q

CYP450 is used in which phase reaction?

A

Phase 1

48
Q

What is clearance

A

the volume of blood that is completely cleared of drug per unit of time (usually L/hr)

49
Q

What does clearance aid in?

A

helps determine dosage rate needed to maintain a desired plasma concentration

50
Q

What is the equation for clearance?

A

CL = rate of drug elimination/drug plasma concentration

51
Q

What is first-order kinetics?

A

where the rate of elimination increases and the plasma concentration of the drug increases also

52
Q

What is zero-order kinetics?

A

where elimination reaches a maximum as the elimination mechanisms have become saturated

53
Q

What is the elimination half-life

A

determines how much time is required for the drug to be eliminated from the body

54
Q

What is the equation for the elimination half-life

A

0.693 x Vd/CL

55
Q

What do Cox 1 and Cox 2 enzymes produce?

A

prostaglandins

56
Q

Name a few factors that affect the Vd?

A

ageing and obesity

57
Q

How do ageing and obesity influence the elimination half-life?

A

ageing causes a decrease in muscle mass thereby recreated the half-life and obesity causes an increase in adipose disse thereby increasing the half-life

58
Q
A

Foundations in Medicine 1 (11 decks)

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