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Neuroscience > Drugs > Flashcards

Drugs Flashcards

1
Q

Types of drugs acting via GPCR

A 
Antidepressants
Antipsychotics
Antiasthma
Blood Pressure
Glaucoma
Abuse
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2
Q

The G protein Gq is coupled to

A

phospholipase

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3
Q

Structure of a ligand gated ion channel subunit

e.g. nicotinic acetylcholine receptor

A

4 transmembrane domains
N terminus extracellular
Large loop between TM3 and TM4
TM2 forms lining of channel

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4
Q

The most diverse receptor class

A

G protein coupled receptors

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5
Q

G protein

A

Protein that links GPCRs to intracellular signalling pathways.
They are trimeric and come in different forms.
Have GTPase enzyme activity.

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6
Q

3 most common forms of G protein

A

Gs
Gi
Gq

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7
Q

G proteins are trimeric

A

They contain alpha, beta and gamma subunits

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8
Q

IP3

A

Inositol tris-phosphate

A second messenger produced in the PLC pathway. (coupled to Gq)

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9
Q

Phospholipase C

A

PLC - hydrolyses PIP2 into Diacyl glycerol and IP3

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10
Q

Orphan receptor

A

Receptor for which the endogenous ligand is not known

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11
Q

Adenylate cyclase is linked to which G proteins

A

Gs and Gi

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12
Q

Structure of a voltage gated sodium or calcium channel

A

24 TM domains, arranged into 4 pseudosubunits.
TM4 is the voltage sensor.
There is a membrane dipping loop between TM5 and TM6.
N terminus intracellular

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13
Q

G protein Gi is coupled to

A

adenylate cyclase (negatively)

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14
Q

The receptor class that is most frequently targetted by drugs

A

G protein coupled receptors

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15
Q

Before entering the nucleus, transactivation nuclear hormone receptors must…

A

Bind ligand, dissociate from heat shock proteins and dimerize

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16
Q

G protein coupled receptor

A

Receptor for a neurotransmitter, hormone or other signalling molecule that is coupled to intracellular signalling pathways via G proteins

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17
Q

G proteins

A

guanine nucleotide binding proteins

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18
Q

Structure of a GPCR subunit

A

7 transmembrane domains
N terminus extracellular
Large loop between TM5 and TM6

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19
Q

The G protein Gs is coupled to

A

adenylate cyclase (positively)

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20
Q

What is gating

A

process by which ion channel opening and closing is controlled.

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21
Q

Transrepression

A

Process by which nuclear hormone receptors decrease expression of a protein

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22
Q

Ligand gated ion channel

A

Ion channel with a binding site for a ligand built into it.

The ion channel is opened by actions of the neurotransmitter.

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23
Q

Nuclear hormone receptors are usually present in the

A

cytoplasm

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24
Q

Phospholipase C is linked to

A

Gq

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25
Q

Transactivation

A

The process by which nuclear hormone receptors increase expression of a protein

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26
Q

The time to onset of a functional effect following binding of an agonist to its binding site in a ligand-gated ion channel is

A

less than a second

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27
Q

What is the major inhibitory neurotransmitter in the CNS

A

GABA

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28
Q

How many subunits do nicotonic receptors contain

A

five

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29
Q

Structure of nicotonic receptors in foetal tissue

A

2 alpha
1 beta
1 delta
1 gamma

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30
Q

Structure of nicotonic receptors in a adult tissue

A

2 alpha
1 beta
1 delta
1 epsilon

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31
Q

Where are GABA receptors found in the cell?

A

Cell surface

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32
Q

Where are glucocorticoid receptors found in the cell?

A

Intracellular

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33
Q

Where are muscarinic acetylcholine receptors found in the cell?

A

Cell surface

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34
Q

Where are nicotinic acetylcholine receptors found in the cell?

A

Cell surface

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35
Q

Where does adrenaline act in the cell

A

G protein coupled receptors

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36
Q

Agonist

A

Activating substances.

Bind to receptors and activate by mimicking the effects of a transmitter at receptors, due to structural similarities

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37
Q

Drug binding domain

A

a. Point on receptor protein where drug interaction is most favourable

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38
Q

Antagonist

A

bind the receptor but does not transduce a response

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39
Q

Amiodarone

A

Class III antidysrhythmic drug which targets K+ channels

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40
Q

Verapamil

A

Class IV antidysrhytmic drug which targets Ca2+ channels

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41
Q

Unclassified antidysrhythmic drugs

A

adenosine
atropine
digoxine

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42
Q

Lidocaine

A

Class Ib antidysrhythmic drug which targets Na+ channels

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43
Q

Atenolol

A

Class II antidysrhythmic drug which targets Beta 1 adrenoreceptors

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44
Q

Drug X has a Kd of 5nm
Drug Y has a Kd of 50nm
Which has a higher affintiy

A

Drug X has 10x higher affinity than drug Y.

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45
Q

Kd / dissociation constant

A

Concentration that gives 50% of maximal occupancy

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46
Q

EC50

A

Concentration giving 50% maximum effect

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47
Q

Potency

A

The concentration of drug required to give a specified response. Often enough is given to achieve the EC50.

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48
Q

Ligand

A

A molecule that binds to something

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49
Q

Receptor

A

Binds a ligand and transduces information

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50
Q

Is a enzyme a receptor?

A

NO

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51
Q

Orthosteric antagonism

A

Reversible binding of antagonist to the same site on the receptor as the agonist. Not activating receptor.

52
Q

IC50

A

Concentration of antagonist giving 50% of control response

53
Q

Issue with IC50

A

Changes with agonist concentration. Doesn’t only measure antagonist.

54
Q

Selectivity

A

The relative potency or affinity at one receptor compared with another

55
Q

efficacy

A

Ability of a drug to produce desired result

56
Q

What kind of response does a partial agonist give?

A

A submaximal response

57
Q

Constitutive activity

A

Model explaining an agonist has a higher affinity for its receptor when in its active state

58
Q

Tone or Basal activity

A

Occurs due to ongoing underlying neurotransmitter release

59
Q

Non-competitive inhibitor

A

Binds at site other than agonist site (allosteric)
Reduces maximum effect
Not affected by agonist concentration

60
Q

Un-competitive inhibitor

A

Use-dependent - more effective at higher agonist concentrations.

61
Q

Heart failure

A

Failure of the heart to meet the body’s oxygen demands. Often due to failures of contractile mechanisms.

62
Q

A small EC50 tells you what about a drugs potency/affinity?

A

It is high

63
Q

Role of calcium in cholinergic transmission

A

Stimulates vesicle fusion with the presynaptic membrane - thus exocytosis of ACh.

64
Q

Device used to measure polarised light

A

polarimeter

65
Q

d- / (+) enantiomer

A

Rotates polarised light clockwise

66
Q

If an enantiomer rotates polarised light anticlockwise, it is…

A

i- / (-)

67
Q

What’s a method of classifying the stereochemistry of a molecule, that can determine structure of amino acids?

A

D/L

68
Q

(+)/(-) is a method of identification in stereochemistry which classifies based on…

A

direction a molecule rotates polarised light when in solution

69
Q

Give a type of isomer that can be readily interconverted

A

Chair/boat

70
Q

Why are doses expressed in mg/kg?

A

Patients may differ in body weight and size. Using this type of dose means the plasma conc. of the drug should be about the same no matter how big or small the subject.

71
Q

Rectangular hyperbola

A

Curve that rises and then smoothly reaches a plateau. Characteristic of conc.-response/binding relationships. Predicted by Hill-Langmuir

72
Q

Competitive antagonist

A

Drug that binds to the same site as an agonist, but doesnt activate the receptor. Presence of competitive antagonist will reduce occupancy by agonist. In a functional assay, it will cause a parallel rightward shift in the agonist conc. response curve.

73
Q

Ki

A

Term used to define the affinity of a competitive antagonist, or to define the affinity of a ligand derived from a competitive binding assay.

74
Q

Sigmoid curve

A

S shaped curve

Seen with conc.response relationships

75
Q

A large EC50 tells you what about a drugs potency/affinity?

A

it is low

76
Q

A low kd for a drug

A

high potency/affinity

77
Q

A high pkd for a drug means

A

high potency/affinity

78
Q

A high EC50 means

A

high potency/affinity

79
Q

A low pA2 means

A

A low drug potency

80
Q

How does adrenaline differ from how NA interacts

A

Acts as hormone, released by adrenal medulla into bloodstream

81
Q

Monoamine oxidase

A

Enzyme responsible for metabolism of various neurotransmitters - adrenaline and serotonin

82
Q

Paravertebral ganglia

A

sympathetic ganglia lying close to the spinal cord

83
Q

Amlodipine

A

Calcium antagonist used to treat hypertension

84
Q

Perindorpil

A

ACE inhibitor used to treat hypertension, alongside calcium blockers.

85
Q

ACE inhibitor

A

Reduce activity of ACE in blood, preventing formation of AGII, reducing high BP

86
Q

Three main classes of diuretics…

A

Thiazide
Loop
K+ sparing

87
Q

Spirinolactone

A

Potassium sparing diuretic works by blocking aldosterone receptors

88
Q

Amiloride

A

Potassium sparing diuretic works by inhibiting Na+ channels in luminal membrane

89
Q

How does aldosterone increase Na+ absorption in principal cells?

A
  • Increases Na+/K+ ATPases
  • Increase Na+ channels
  • Stimulate Na+ channels via protein mediator
90
Q

Examples of ACE inhibitors

A

Captopril

Lisinopril

91
Q

AGII receptor types

A

type 1 - vascular effects and aldosterone release

type 2 - growth and development

92
Q

Propranolol

A

Non-selective competitive antagonist at β-adrenoreceptors

lipid soluble, penetrates CNS causing vivid dreams

93
Q

Atenolol and Bisopropol

A

Competitive β1-adrenoreceptor antagonists.

Water soluble.

94
Q

What pain mediators might cardiac muscle cells release when they become ischaemic?

A

adenosine
bradykinin
K+

95
Q

Features of LDL and VLDL making them bad?

A
  • fatty streak formation
  • inhibit fibrinolysis
  • activate platelets
96
Q

Dietary changes to treat hyperlipidaemia

A
  • Reduce saturated fat
  • Increase unsaturated fat
  • Increase fibre
  • Avoid trans-fats
  • Avoid hydrogenated fats
97
Q

Lipid lowering drugs to treat hyperlipidaemia’s

A

Statins

ezetimibe

98
Q

Statins

A

Inhibit HMG-CoA reductase.
Interfere body’s ability to produce cholesterol.
Causes more LDL receptors.

99
Q

salbutamol interacts with what receptor

A

Agonist at beta 2 adrenoreceptors

100
Q

Atropine

A

mAChR antagonist

101
Q

beta1 adrenoreceptors

A

control heart rate and force of contraction

102
Q

chronotropic drugs

A

Affect heart rate

103
Q

Ionotropic drugs

A

affect strength of heart contractions

104
Q

Thrombin

A

Enzyme which converts soluble fibrinogen to insoluble fibrin. produced from prothrombin.

105
Q

according to VW system, class I drugs are:

A

sodium channel blockers

106
Q

According to VW system, class II drugs are:

A

beta-adrenoceptor antagonists

107
Q

According to VW system, class III drugs are:

A

amiodarone

sotalol

108
Q

According to VW system, class IV drugs are:

A

Calcium channel blockers

109
Q

Statins

A

Lipid lowering drugs

Cause muscle inflammation and damage.

110
Q

Plasmin

A

Enzyme which breaks down fibrin into soluble products. Precursor is plasminogen.

111
Q

ECG showing ST elevation suggests…

A

STEMI

112
Q

Blood markes in ACS suggests

A

NSTEMI

113
Q

No blood markers in ACS suggests

A

Unstable angina

114
Q

Drugs to prevent thrombosis

A

Aspirin
Ticagrelor/clopidogrel
Heparins
Atorvastatin

115
Q

What type of drugs would be prescribed to someone with arterial thrombosis?

A

Drugs which modify platelet aggregation

116
Q

What drugs would be prescribed to some with venous thrombosis?

A

Ones which modify coagulation

e.g. heparins

117
Q

What does antithrombin act on?

A

Factor X

and thrombin

118
Q

PLATO trial

A

Showed ticagrelor more effective than clopidogrel

119
Q

Re-entry dysrhythmia

A

A disorder of impulse generation, e.g. atrial fibrillation

120
Q

Disorders of impulse conduction

A

WPW syndrome

Atrio-ventricular block.

121
Q

Ectopic focus

A

Abnormal impulse generation

122
Q

Ventricular fibrillation

A

Abnormal impulse generation in ventricles

123
Q

Class IV drugs

A

Block L-type VSCC
Slow SA & AV node conduction
Suppress ectopic pacemaker

124
Q

forward symptoms of congestive heart failure

A

inability of heart to pump blood efficiently.

Low output symptoms

125
Q

backward symptoms of congestive heart failure

A

inability of heart to fill with blood efficiently.

Congestive symptoms

126
Q

glucocorticoid receptor

A

GPCR involved in gene regulation.

Neuroscience (22 decks)

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