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 _________ the CNS

A

Away from

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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
Components of a G-protein
α (contains guanine nucleotide binding site) | β + γ complex
26
GP couples with receptor to increase affinity for GDP. True/False?
False | Affinity for GDP decreases and it eventually dissociates, increasing affinity for GTP to bind on α subunit
27
M1 G-protein coupled receptor is G_ | Causes ___ acid secretion in stomach
q | Increased
28
M2 G-protein coupled receptor is G_ | Causes ___ heart rate
i | Decreased
29
M3 G-protein coupled receptor is G_ | Causes ___ of airways; ___ of vasculature
q | Contraction, relaxation
30
ACh and NA can be broken down in the synaptic cleft if not taken up by the effector cell. True/False?
False | NA is not broken down in the cleft - U1 and U2 are involved
31
Uptake 1 is located on the?
Post-ganglionic neurone
32
Uptake 2 is located on the?
Effector cell
33
NA can be taken up by U1 and broken down by which enzyme?
MAO, a target of anti-depressant drugs
34
NA can be taken up by U2 and broken down by which enzyme?
COMT
35
B1 G-protein coupled receptor is G_ | Causes ____ heart rate and force
s | Increased
36
B2 G-protein coupled receptor is G_ | Causes ___ of airways and vasculature
s | Relaxation
37
α1 G-protein coupled receptor is G_ | Causes ____ of vasculature
q | Contraction
38
α2 G-protein coupled receptor is G_ | Causes ____ NA release
i | Decreased
39
ACh binding to post-ganglionic M2 receptor causes ____ Ca2+ entry, which results in ___ NT release
Reduced, less
40
NA binding to post-ganglionic α2 receptor causes increased Ca2+ entry, resulting in more NT release. True/False?
False | Decreased Ca2+ entry, resulting in less NT release
41
Cocaine blocks U_, causing an ___ in NA concn in the synaptic cleft α1 and B1 stimulation causes ____ and ____
Cocaine blocks U1, causing an increase in NA concn in the synaptic cleft α1 and B1 stimulation causes vasoconstriction and increased heart rate
42
Amphetamine inhibits the enzyme ___, resulting in ___ in NA in the cytoplasm
Amphetamine inhibits the enzyme MAO, resulting in increase in NA in the cytoplasm
43
Ganglionic nicotinic ACh receptors, a type of ligand-gated ion channels, consist of which α and B subunits?
3 x B4 | 2 x α3
44
The concn a drug must reach in the plasma to achieve an effect is termed the...
Minimum effective concn
45
The maximum tolerated concn is defined as...
The drug concn in the plasma which must not be exceeded to prevent toxic effects
46
Therapeutic ratio/index is given by...
MTC/MEC
47
Co (initial concn) is given by...
D/Vd
48
Rule of first order kinetics is...
Rate of elimination (Kel) is proportional to drug concn
49
t1/2 (half life) =
0.69/Kel
50
For drugs exhibiting 1st order kinetics, the dose administered changes __ directly, but has no effect upon __ or __
Cp, t1/2, Kel
51
Plasma clearance, Clp, is given by...
Vd x Kel
52
Rate of 1st order kinetic drug elimination is given by...
Cp x Clp
53
Css = steady state concn and is normally achieved after _ half lives
5
54
The time to reach Css is determined by the infusion rate but not the half life. True/False?
False | Css is determined by the half life, not infusion rate
55
Depolarisation is when the membrane potential becomes more negative. True/False?
False | Less negative
56
Resting membrane potential, Vm, is normally approx...
-70mV
57
Activation of Na+ channels and subsequent Na+ channels is an example of ____ feedback
Positive
58
Refractory period of the AP describes...
The inactivated state of sodium channels, ultimately causing repolarisation to closed state
59
In the relative refractory period, a strong enough stimulus can elicit the generation of a new AP. True/False?
True
60
What is the function of Schwann cells?
Wrap around axons in a "myelin sheath" to provide insulation and speed up chemical conduction
61
Saltatory conduction describes...
APs jumping between gaps between adjacent Schwann cells