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1MB Principles - Rafi Ahmed > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Pharmacodynamics is…

A

What a drug does to the body

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2
Q

Pharmacokinectics is…

A

What a body does to the drug (absorption, distribution, eliminations etc.)

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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

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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9
Q

pKa is…

A

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

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10
Q

Henderson Hasselbach Equation

A

pH = pKa + log[A-]/[HA]
pKa - pH = log[HA]/[A-]
FOR WEAK ACIDS ONLY

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11
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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12
Q

Administration routes that by-pass first pass metabolism are…

A

Sublingual, rectal

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13
Q

Vd = volume of distribution = ?

A

Volume in which a drug is dissolved

Dose given/Plasma Concn

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14
Q

Vd less than 5L suggests…

A

Drug is contained in vascular compartment

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15
Q

Vd less than 15L suggests…

A

Drug is restricted to extracellular water

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16
Q

Vd greater than 15L suggests…

A

Drug is in total body water

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17
Q

Efferent signals travel ___ from the CNS

A

Away

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18
Q

Sympathetic preganglionic NT is?

A

Acetylcholine (cholinergic)

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19
Q

Sympathetic postganglionic NT is?

A

Noradrenline (adrenergic)

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20
Q

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

A

True

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21
Q

Sympathetic outflow is craniosacral. True/False?

A

False

Thoracolumbar (T1-L2)

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22
Q

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

A

False

Short - preganglionic neurone of parasympathetic chain is long as ganglions are usually embedded in the target organ

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23
Q

Location of cranial parasympathetic ganglia in the head and neck

A

C3, C7, C9, C10

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24
Q

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

A

False

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

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25
Q

Components of a G-protein

A

α (contains guanine nucleotide binding site)

β + γ complex

26
Q

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

A

False

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

27
Q

M1 G-protein coupled receptor is G_

Causes ___ acid secretion in stomach

A

q

Increased

28
Q

M2 G-protein coupled receptor is G_

Causes ___ heart rate

A

i

Decreased

29
Q

M3 G-protein coupled receptor is G_

Causes ___ of airways; ___ of vasculature

A

q

Contraction, relaxation

30
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

31
Q

Uptake 1 is located on the?

A

Post-ganglionic neurone

32
Q

Uptake 2 is located on the?

A

Effector cell

33
Q

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

A

MAO, a target of anti-depressant drugs

34
Q

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

A

COMT

35
Q

B1 G-protein coupled receptor is G_

Causes ____ heart rate and force

A

s

Increased

36
Q

B2 G-protein coupled receptor is G_

Causes ___ of airways and vasculature

A

s

Relaxation

37
Q

α1 G-protein coupled receptor is G_

Causes ____ of vasculature

A

q

Contraction

38
Q

α2 G-protein coupled receptor is G_

Causes ____ NA release

A

i

Decreased

39
Q

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

A

Reduced, less

40
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

41
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

42
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

43
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

44
Q

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

A

Minimum effective concn

45
Q

The maximum tolerated concn is defined as…

A

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

46
Q

Therapeutic ratio/index is given by…

A

MTC/MEC

47
Q

Co (initial concn) is given by…

A

D/Vd

48
Q

Rule of first order kinetics is…

A

Rate of elimination (Kel) is proportional to drug concn

49
Q

t1/2 (half life) =

A

0.69/Kel

50
Q

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

A

Cp, t1/2, Kel

51
Q

Plasma clearance, Clp, is given by…

A

Vd x Kel

52
Q

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

A

Cp x Clp

53
Q

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

A

5

54
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

55
Q

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

A

False

Less negative

56
Q

Resting membrane potential, Vm, is normally approx…

A

-70mV

57
Q

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

A

Positive

58
Q

Refractory period of the AP describes…

A

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

59
Q

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

A

True

60
Q

What is the function of Schwann cells?

A

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

61
Q

Saltatory conduction describes…

A

APs jumping between gaps between adjacent Schwann cells

1MB Principles - Rafi Ahmed (9 decks)

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