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foundations of medicine > Pharmacology > Flashcards

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

A

YES

25
Q

Can maximal response be achieved with irreversible competitive antagonism

A

NO

26
Q

Where does the antagonist bind in non-competitive antagonism

A

Allosteric site

27
Q

Chemical antagonism

A

The antagonist combines in solution directly with the chemical being antagonised

28
Q

Physiological antagonism

A

2 antagonists produce opposing physiological actions and cancel each other out

29
Q

Pharmacokinetic antagonism

A

Antagonist reduces the concentration of the active drug at its site of action

30
Q

State the 4 main types of receptors

A

Ligand gated ion channels
G protein coupled receptors
Kinase linked receptors
Nuclear receptors

31
Q

Give an example of a ligand gated ion channel

A

Nicotinic ACh receptor

32
Q

Give an example of a G coupled receptor

A

Muscarinic ACh receptor

33
Q

Give an example of a kinase linked receptor

A

Cytokines receptor

34
Q

Give an exam pls of a nuclear receptor

A

Oestrogen receptor

35
Q

Where are ligand gated ion channels found

A

Plasma membrane

36
Q

Sequence of action of a ligand gated ion channel (3)

A

Agonist binds to receptor and causes a conformational change
Ion channel opens
Ions flow through channel down electrochemical gradient

37
Q

Name 3 drugs that act as agonists at nicotinic ACh receptors

A

Acetylcholine
Nicotine
Varenicline

38
Q

a1 adrencoeptors role

A

Activation of phospholipase C

39
Q

a1 adrenoceptors effect

A

Vasoconstriction of the blood vessels

40
Q

a2 adrenoceptors role

A

Inhibition of adenylyl cyclase

41
Q

a2 adrenoceptors effect (2)

A

Presynaptic inhibition of noradrenaline in the CNS
relaxation of the GI tract

42
Q

b1,2 and 3 adrenoceptors role

A

Stimulation of adenylyl cyclase

43
Q

b1 adrenoceptor effect (2)

A

Increased heart rate and cardiac contraction

44
Q

b2 adrenoceptors role (3)

A

Dilation of the bronchi
Increased heart rate and cardiac muscle contraction

45
Q

b3 adrenoceptors effect (2)

A

Thermogenesis in skeletal muscle
Lipolysis

46
Q

Where are G protein coupled receptors found

A

Plasma membrane

47
Q

How is a G coupled receptor activated (4)

A

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
Q

How do you turn off G coupled protein receptors (2)

A

a subunit acts as an enzyme and hydrolyses GTP to GDP
Recombines with its subunit

49
Q

What are kinase linked receptors associated with

A

An enzyme

50
Q

Where are kinase linked receptors found

A

Plasma membrane

51
Q

What is the ligand for a mineralocorticoid receptor

A

Aldosterone

52
Q

What is the ligand for a glucocorticoid receptor

A

Cortisol

53
Q

Where are nuclear receptors found

A

Nucleus or cytoplasm

foundations of medicine (12 decks)

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