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Y1 PRINCIPLES > Pharmacology > Flashcards

Pharmacology Flashcards

(78 cards)

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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
t1/2 (half life) =
0.69/Kel | Time taken for concentration to fall by 50%
26
For drugs exhibiting 1st order kinetics, the dose administered changes __ directly, but has no effect upon __ or __
Cp, t1/2, Kel
27
Plasma clearance, Clp, is given by...
Vd x Kel
28
Rate of 1st order kinetic drug elimination is given by...
Cp x Clp
29
Css = steady state concn and is normally achieved after _ half lives
5
30
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
31
What is the loading dose?
Initial higher dosage given at start of treatment which is stepped down to a lower maintenance dose
32
What is zero order elimination?
Drugs are initially eliminated at constant rate rather than rate proportional to Cp
33
The main organ of drug metabolism is...
The Liver
34
Give the phases of drug metabolism...
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
CYP450 Monoxygenases are...
Haem proteins that contribute to oxidation of many lipid soluble drugs
36
Depolarisation is when the membrane potential becomes more negative. True/False?
False Less negative | Hyperpolarisation = more negative
37
Resting membrane potential, Vm, is normally approx...
-70mV
38
Activation of Na+ channels and subsequent Na+ channels is an example of ____ feedback
Positive (DEPOLARISING) | Flows inwardly: -70mV to +60mV
39
Activation of K+ channels and subsequent K+ channels is an example of ____ feedback
Negative (HYPERPOLARISING) | Flows outwardly: -70mV to -90mV
40
Stages of an action potential
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
Refractory period of the AP describes...
The inactivated state of sodium channels, ultimately causing repolarisation to closed state
42
In the relative refractory period, a strong enough stimulus can elicit the generation of a new AP. True/False?
True | Absolute period you cant elicit a new Ap
43
What is the function of Schwann cells?
Wrap around axons in a "myelin sheath" to provide insulation and speed up chemical conduction
44
Saltatory conduction describes...
APs jumping between gaps (Node of Ranvier) between adjacent Schwann cells
45
What voltage channels cluster at the Nodes of Ranvier?
Na+
46
Type of axons that involve the passive spread of current are...
Unmyelinated
47
Efferent signals travel ___ from the CNS
Away
48
Sympathetic preganglionic NT is?
Acetylcholine (cholinergic)
49
Sympathetic postganglionic NT is?
Noradrenline (adrenergic)
50
Parasympathetic pre and post ganglionic NT is acetylcholine. True/False?
True
51
Sympathetic outflow is craniosacral. True/False?
``` False Thoracolumbar (T1-L2) Craniosacral is parasympathetic ```
52
Preganglionic neurone of sympathetic chain is long. True/False?
False Short (GET UP QUICKLY) - preganglionic neurone of parasympathetic chain (LAZY) is long as ganglions are usually embedded in the target organ
53
Location of cranial parasympathetic ganglia in the head and neck
C3, C7, C9, C10
54
Parasympathetic stimulation decreases force of heart contraction. True/False?
False | Has no effect on force of contraction, but does decrease heart rate
55
Components of a G-protein
α (contains guanine nucleotide binding site), β + γ complex
56
GP couples with receptor to increase affinity for GDP. True/False?
False Affinity for GDP decreases and it eventually dissociates from alpha component, increasing affinity for GTP to bind on α subunit
57
When an agonist dissociates from its receptor signalling terminates. True/False?
False | Signalling can persist - to turn off a signal the alpha subunit acts as GTPase to hydrolyse GTP into GDP and Pi
58
Ganglionic nicotinic ACh receptors, a type of ligand-gated ion channels, consist of which α and B subunits?
3 x B4 2 x α3
59
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
60
Uptake 1 is located on the?
Post-ganglionic neurone
61
Uptake 2 is located on the?
Effector cell
62
NA can be taken up by U1 and broken down by which enzyme?
MAO, a target of anti-depressant drugs
63
NA can be taken up by U2 and broken down by which enzyme?
COMT
64
ACh binding to post-ganglionic M2 receptor causes ____ Ca2+ entry, which results in ___ NT release
Reduced, less
65
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
66
M1 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___ and increased/decreased ____
q, stimulation, phospholipase C, increased, acid secretion in the stomach
67
M2 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___ and increased/decreased ____
i, inhibition, adenyl cyclase, decreased heart rate
68
M3 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___ and increased/decreased ____, airway ______ and vasculature _____
q, stimulation, phospholipase C, increased, gland secretion, contraction, relaxation
69
B1 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___ and increased/decreased ____
s, stimulation, adenyl cyclase, increased heart rate and force
70
B2 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___, airway _____ and vasculature ____
s, stimulation, adenyl cyclase, relaxation, relaxation
71
a1 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___ and vasculature ____
q, stimulation, phospholipase C, contraction
72
a2 G-protein coupled receptor is G_ Causes inhibition/ stimulation of ___ and increased/decreased ____
i, inhibition, adenyl cyclase, decreased, NA release from the CNS
73
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
74
Amphetamine inhibits the enzyme ___, resulting in ___ in NA in the cytoplasm
Amphetamine inhibits the enzyme MAO, resulting in increase in NA in the cytoplasm (actions same as cocaine)
75
Salbutamol is an agonist at ___ only and acts as a broncho_____ in ______
B2, dilator, asthma
76
Atropine is a competitive agonist of ______ ___ receptors and blocks sympathetic/parasympathetic activity for example ______
muscarinic ACh, parasympathetic, reverses bradycardia following an MI
77
Prozosin is a competitive agonist/antagonist of ___ only and is used as a vasodilator/vasoconstrictor in ____
a1, vasodilator, hypertension
78
Atenolol is a competitive agonist/antagonist of ____ only and is used in the treatment of ____ and ____
B2, angina, hypertension

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