Pharmacology Flashcards

1
Q

Pharmacology

A

The study of the manner in which the function of living tissues and organs is modified by chemical substances

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2
Q

Pharmacokinetics

A

What the body does to a drug

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3
Q

Receptor

A

A class of macromolecules that are concerned specifically and directly with chemical signalling

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4
Q

Ligand

A

A substance that is bound to a protein

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5
Q

Affinity

A

The tendency of a ligand to bind to its receptor

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6
Q

Agonist

A

A ligand that binds to a receptor and alters the state resulting in a biological response

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7
Q

Antagonists

A

A drug that reduces or blocks the actions of an agonist by binding to the receptor

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8
Q

Selectivity

A

The ability of a drug to distinguish between different molecular targets within the body

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9
Q

Potency

A

The amount of drug required to produce the desired effect

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10
Q

Efficacy

A

The tendency for an agonist to activate the receptor

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11
Q

Partial agonist

A

Response is sub-maximal even when 100% of the receptors are occupied

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12
Q

Equilibrium

A

The point at which the rate of the forward reaction and backward reaction are equal

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13
Q

When is the disassociation equilibrium constant used

A

To compare the affinity of one drug to another

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14
Q

What kind of curve does the hill-Langmuir equation form on a logarithmic scale

A

Sigmoidal

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15
Q

What does the hill-Langmuir equation model

A

The relationship between ligand concentration and receptor occupancy

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16
Q

Fractional occupancy

A

The proportion of the receptors that have been occupied

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17
Q

State 1 of the 2 state model

A

The agonist binds the the receptor

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18
Q

State 1 of the 2 state model

A

The agonist activates the receptor

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19
Q

What governs the formation of a ligand receptor complex

A

Affinity

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20
Q

What governs a receptor being activated

A

Efficacy

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21
Q

What is EC50

A

The concentration of agonist that elicits half maximal effect

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22
Q

When is EC50 useful

A

Determining drug potency

23
Q

Reversible competitive antagonism

A

Antagonist competes for the same binding site, can be overcome

24
Q

Can maximal response still be achieved with reversible competitive antagonism

25
Can maximal response be achieved with irreversible competitive antagonism
NO
26
Where does the antagonist bind in non-competitive antagonism
Allosteric site
27
Chemical antagonism
The antagonist combines in solution directly with the chemical being antagonised
28
Physiological antagonism
2 antagonists produce opposing physiological actions and cancel each other out
29
Pharmacokinetic antagonism
Antagonist reduces the concentration of the active drug at its site of action
30
State the 4 main types of receptors
Ligand gated ion channels G protein coupled receptors Kinase linked receptors Nuclear receptors
31
Give an example of a ligand gated ion channel
Nicotinic ACh receptor
32
Give an example of a G coupled receptor
Muscarinic ACh receptor
33
Give an example of a kinase linked receptor
Cytokines receptor
34
Give an exam pls of a nuclear receptor
Oestrogen receptor
35
Where are ligand gated ion channels found
Plasma membrane
36
Sequence of action of a ligand gated ion channel (3)
Agonist binds to receptor and causes a conformational change Ion channel opens Ions flow through channel down electrochemical gradient
37
Name 3 drugs that act as agonists at nicotinic ACh receptors
Acetylcholine Nicotine Varenicline
38
a1 adrencoeptors role
Activation of phospholipase C
39
a1 adrenoceptors effect
Vasoconstriction of the blood vessels
40
a2 adrenoceptors role
Inhibition of adenylyl cyclase
41
a2 adrenoceptors effect (2)
Presynaptic inhibition of noradrenaline in the CNS relaxation of the GI tract
42
b1,2 and 3 adrenoceptors role
Stimulation of adenylyl cyclase
43
b1 adrenoceptor effect (2)
Increased heart rate and cardiac contraction
44
b2 adrenoceptors role (3)
Dilation of the bronchi Increased heart rate and cardiac muscle contraction
45
b3 adrenoceptors effect (2)
Thermogenesis in skeletal muscle Lipolysis
46
Where are G protein coupled receptors found
Plasma membrane
47
How is a G coupled receptor activated (4)
Agonist binds causing conformational change G protein binds with receptor a subunit releases GDP and GTP binds in its place a subunit dissociates from receptor and combines with effector to modify its activity
48
How do you turn off G coupled protein receptors (2)
a subunit acts as an enzyme and hydrolyses GTP to GDP Recombines with its subunit
49
What are kinase linked receptors associated with
An enzyme
50
Where are kinase linked receptors found
Plasma membrane
51
What is the ligand for a mineralocorticoid receptor
Aldosterone
52
What is the ligand for a glucocorticoid receptor
Cortisol
53
Where are nuclear receptors found
Nucleus or cytoplasm