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Pharmacology Flashcards

1
Q

Pharmacodynamics is..

A

What a drug does to the body

D for drug

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2
Q

Pharmacokinetics is…

A

What a body does to the drug (absorption, distribution, eliminations (metabolism + excretion) etc.)
K for Kerry (body)

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3
Q

Efficacy is…

A

They ability of an agonist to evoke a response

Higher efficacy = larger response

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4
Q

Affinity is…

A

The strength of association between agonist and its receptor
Greater affinity = greater duration of binding

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5
Q

EC50 is…

A

The concn of agonist that results in a half maximal response (i.e. 50% of receptors are occupied)

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6
Q

Agonist A requires 0.01 concn to elicit a response. Agonist B requires 0.05 concn to elicit a response. Agonist A is more ____ than agonist B.

A

Potent

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7
Q

In the presence of a competitive antagonist, EC50 is unchanged. True/False?

A

False EC50 increases (need to increase concn of agonist to get response)

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8
Q

What is competitive antagonism?

A

Binding of agonist and antagonist at same orthosteric site

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9
Q

What is non-competitive antagonism?

A

Agonist binds to orthosteric site and antagonist binds to seperate allosteric site - activation cannot occur when antagonist is bound

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10
Q

Both the ionised and unionised form of a drug readily diffuse across the lipid bilayer. True/False?

A

False

Only the unionised form does

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11
Q

pKa is…

A

The pH at which 50% of a drug is ionised and 50% is unionised

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12
Q

Henderson Hasselbach Equation

A

pH = pKa + log[A-]/[HA] pKa - pH = log[HA]/[A-]

FOR WEAK ACIDS ONLY

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13
Q

Increasing the pH of an acidic drug causes it to become less ionised. True/False?

A

False It becomes more ionised (acid drugs are less ionised in an acid environment)

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14
Q

Administration routes that by-pass first pass metabolism are…

A

Sublingual, rectal

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15
Q

List the major fluid compartments in the body…(5)

A 
Plasma water
Fat
Interstitial water
Transcellular water
Intracellular water
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16
Q

Vd = volume of distribution = ?

A

Volume in which a drug is dissolved

Dose given/Plasma Concn

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17
Q

Vd less than 5L suggests…

A

Drug is contained in vascular compartment

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18
Q

Vd less than 15L suggests…

A

Drug is restricted to extracellular water

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19
Q

Vd greater than 15L suggests…

A

Drug is in total body water

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20
Q

The concn a drug must reach in the plasma to achieve an effect is termed the…

A

Minimum effective concn

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21
Q

The maximum tolerated concn is defined as…

A

The drug concn in the plasma which must not be exceeded to prevent toxic effects

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22
Q

Therapeutic ratio/index is given by…

A

MTC/MEC (Higher = safer)

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23
Q

Co (initial concn) is given by…

A

D/Vd

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24
Q

Rule of first order kinetics is…

A

Rate of elimination (Kel) is proportional to drug concn

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25
Q

t1/2 (half life) =

A

0.69/Kel

Time taken for concentration to fall by 50%

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26
Q

For drugs exhibiting 1st order kinetics, the dose administered changes __ directly, but has no effect upon __ or __

A

Cp, t1/2, Kel

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27
Q

Plasma clearance, Clp, is given by…

A

Vd x Kel

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28
Q

Rate of 1st order kinetic drug elimination is given by…

A

Cp x Clp

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29
Q

Css = steady state concn and is normally achieved after _ half lives

A

5

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30
Q

The time to reach Css is determined by the infusion rate but not the half life. True/False?

A

False

Css is determined by the half life, not infusion rate

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31
Q

What is the loading dose?

A

Initial higher dosage given at start of treatment which is stepped down to a lower maintenance dose

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32
Q

What is zero order elimination?

A

Drugs are initially eliminated at constant rate rather than rate proportional to Cp

33
Q

The main organ of drug metabolism is…

34
Q

Give the phases of drug metabolism…

A

1: Catabolic - breaks down molecules into smaller units, increases polarity, adds reactive group (primes drug for modification)
2: Anabolic - Adds endogenous compound to increase polarity - functionalization

35
Q

CYP450 Monoxygenases are…

A

Haem proteins that contribute to oxidation of many lipid soluble drugs

36
Q

Depolarisation is when the membrane potential becomes more negative. True/False?

A

False Less negative

Hyperpolarisation = more negative

37
Q

Resting membrane potential, Vm, is normally approx…

38
Q

Activation of Na+ channels and subsequent Na+ channels is an example of ____ feedback

A

Positive (DEPOLARISING)

Flows inwardly: -70mV to +60mV

39
Q

Activation of K+ channels and subsequent K+ channels is an example of ____ feedback

A

Negative (HYPERPOLARISING)

Flows outwardly: -70mV to -90mV

40
Q

Stages of an action potential

A

Brief electrical signals in which nerve polarity is momentarily reversed - opening of K+ channels and inactivation of Na+ channels
Undershoot, Threshold, Upstroke, Overshoot, Downstroke

41
Q

Refractory period of the AP describes…

A

The inactivated state of sodium channels, ultimately causing repolarisation to closed state

42
Q

In the relative refractory period, a strong enough stimulus can elicit the generation of a new AP. True/False?

A

True

Absolute period you cant elicit a new Ap

43
Q

What is the function of Schwann cells?

A

Wrap around axons in a “myelin sheath” to provide insulation and speed up chemical conduction

44
Q

Saltatory conduction describes…

A

APs jumping between gaps (Node of Ranvier) between adjacent Schwann cells

45
Q

What voltage channels cluster at the Nodes of Ranvier?

46
Q

Type of axons that involve the passive spread of current are…

A

Unmyelinated

47
Q

Efferent signals travel ___ from the CNS

48
Q

Sympathetic preganglionic NT is?

A

Acetylcholine (cholinergic)

49
Q

Sympathetic postganglionic NT is?

A

Noradrenline (adrenergic)

50
Q

Parasympathetic pre and post ganglionic NT is acetylcholine. True/False?

51
Q

Sympathetic outflow is craniosacral. True/False?

A 
False Thoracolumbar (T1-L2)
Craniosacral is parasympathetic
52
Q

Preganglionic neurone of sympathetic chain is long. True/False?

A

False Short (GET UP QUICKLY) - preganglionic neurone of parasympathetic chain (LAZY) is long as ganglions are usually embedded in the target organ

53
Q

Location of cranial parasympathetic ganglia in the head and neck

A

C3, C7, C9, C10

54
Q

Parasympathetic stimulation decreases force of heart contraction. True/False?

A

False

Has no effect on force of contraction, but does decrease heart rate

55
Q

Components of a G-protein

A

α (contains guanine nucleotide binding site), β + γ complex

56
Q

GP couples with receptor to increase affinity for GDP. True/False?

A

False
Affinity for GDP decreases and it eventually dissociates from alpha component, increasing affinity for GTP to bind on α subunit

57
Q

When an agonist dissociates from its receptor signalling terminates. True/False?

A

False

Signalling can persist - to turn off a signal the alpha subunit acts as GTPase to hydrolyse GTP into GDP and Pi

58
Q

Ganglionic nicotinic ACh receptors, a type of ligand-gated ion channels, consist of which α and B subunits?

A

3 x B4 2 x α3

59
Q

ACh and NA can be broken down in the synaptic cleft if not taken up by the effector cell. True/False?

A

False

NA is not broken down in the cleft - U1 and U2 are involved

60
Q

Uptake 1 is located on the?

A

Post-ganglionic neurone

61
Q

Uptake 2 is located on the?

A

Effector cell

62
Q

NA can be taken up by U1 and broken down by which enzyme?

A

MAO, a target of anti-depressant drugs

63
Q

NA can be taken up by U2 and broken down by which enzyme?

64
Q

ACh binding to post-ganglionic M2 receptor causes ____ Ca2+ entry, which results in ___ NT release

A

Reduced, less

65
Q

NA binding to post-ganglionic α2 receptor causes increased Ca2+ entry, resulting in more NT release. True/False?

A

False

Decreased Ca2+ entry, resulting in less NT release

66
Q

M1 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___ and increased/decreased ____

A

q, stimulation, phospholipase C, increased, acid secretion in the stomach

67
Q

M2 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___ and increased/decreased ____

A

i, inhibition, adenyl cyclase, decreased heart rate

68
Q

M3 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___ and increased/decreased ____, airway ______ and vasculature _____

A

q, stimulation, phospholipase C, increased, gland secretion, contraction, relaxation

69
Q

B1 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___ and increased/decreased ____

A

s, stimulation, adenyl cyclase, increased heart rate and force

70
Q

B2 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___, airway _____ and vasculature ____

A

s, stimulation, adenyl cyclase, relaxation, relaxation

71
Q

a1 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___ and vasculature ____

A

q, stimulation, phospholipase C, contraction

72
Q

a2 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___ and increased/decreased ____

A

i, inhibition, adenyl cyclase, decreased, NA release from the CNS

73
Q

Cocaine blocks U_, causing an ___ in NA concn in the synaptic cleft α1 and B1 stimulation causes ____ and ____

A

Cocaine blocks U1, causing an increase in NA concn in the synaptic cleft α1 and B1 stimulation causes vasoconstriction and increased heart rate

74
Q

Amphetamine inhibits the enzyme ___, resulting in ___ in NA in the cytoplasm

A

Amphetamine inhibits the enzyme MAO, resulting in increase in NA in the cytoplasm (actions same as cocaine)

75
Q

Salbutamol is an agonist at ___ only and acts as a broncho_____ in ______

A

B2, dilator, asthma

76
Q

Atropine is a competitive agonist of ______ ___ receptors and blocks sympathetic/parasympathetic activity for example ______

A

muscarinic ACh, parasympathetic, reverses bradycardia following an MI

77
Q

Prozosin is a competitive agonist/antagonist of ___ only and is used as a vasodilator/vasoconstrictor in ____

A

a1, vasodilator, hypertension

78
Q

Atenolol is a competitive agonist/antagonist of ____ only and is used in the treatment of ____ and ____

A

B2, angina, hypertension

Y1 PRINCIPLES (10 decks)

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