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MedST IB: Mechanisms of Drug Action (MoDA) > 10.0 Drug List > Flashcards

10.0 Drug List Flashcards

1
Q

Vesamicol

A

Non-competative and reversible blocker of VAChT

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2
Q

Varenicline

A

High affinity partial agonist for the α4β2nAChRs<div>High affinity full agonst for the α7nAChRs</div>

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3
Q

Trimetaphan

A

Competative antagonist of the (α3)2(β2)3isoform of the nAChR

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4
Q

Hexamethonium

A

Competative antagonist of the (α3)2(β2)3isoform of the nAChR

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5
Q

Tetramethylammonium (TMA)

A

Neuronal (Nn) nAChR agonist

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6
Q

Dimethylphenylpiperazinium (DMPP)

A

Neuronal (Nn) nAChR agonist

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7
Q

Suxamethonium

A

Depolarising nAChR antagonist that initially activates the receptor but isnt hydrolysed by AChE so causes a secondary antagonism

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8
Q

Curare (d-tubocurarine)

A

Non-depolarising nAChR antagonist

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9
Q

Pancuronium

A

Synthetic non-depolarising aminosteriod nAChR antagonist

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10
Q

Rocuronium

A

Synthetic non-depolarising aminosteriod nAChR antagonist

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11
Q

Atracurium

A

Synthetic non-depolarising nAChR antagonist (benzylisoquinolinium)

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12
Q

Mivacurium

A

Synthetic non-depolarising nAChR antagonist (benzylisoquinolinium)

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13
Q

Botulinum toxin (BTx)

A

Peptidase that cleaves SNARE proteins to prevent release of ACh, hence blocking cholinergic neurotransmission

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14
Q

α-bungarotoxin

A

Irreversibly binds to the ACh binding site on the adult nAChR hence blocking cholinergic neurotransmission

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15
Q

β-bungarotoxin

A

Inhibits ACh release through a mechanism thought to involve phospholipase A2, which leads to blockage of cholinergic neurotransmission

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16
Q

α-lacrotoxin

A

Causes massive release and subsequent depletion of ACh at the NMJ thought to be due to its ability to form a Ca2+channel

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17
Q

Tetanus neurotoxin

A

Cleaves synaptobrevin to prevent glycine release by inhibitory interneurones upsteam of those innervating skeletal muscle

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18
Q

Bethanechol

A

Choline ester that acts as a non-selective agonist of mAChRs

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19
Q

Pilocarpine

A

mAChR agonist that is stable to hydrolysis by AChE

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20
Q

Atropine

A

Non-selective mAChR antagonist

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21
Q

Scopoloamine

A

Non-selective mAChR antagonist

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22
Q

Homatropine

A

Non-selective mAChR antagonist

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23
Q

Methscopolamine

A

Non-selective mAChR antagonist

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24
Q

Ipratropium

A

Short-acting non-selective mAChR antagonist (SAMA) with some selectivity for M3receptors in the airways

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25
Q

Tiotropium

A

Long-acting non-selective mAChR antagonist (LAMA) with some selectivity for M3receptors in the airways

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26
Q

Glycopyrronium

A

Long-acting non-selective mAChR antagonist (LAMA) with some selectivity for M3receptors in the airways

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27
Q

Tropicamide

A

Non-selective mAChR antagonist

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28
Q

Cyclopentolate

A

Non-selective mAChR antagonist

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29
Q

Pirenzepine

A

M1selective mAChR antagonist

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30
Q

Darifenacin

A

M3selective mAChR antagonist

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31
Q

Solifenacin

A

M3selective mAChR antagonist

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32
Q

Endrophonium

A

Non-covalent, reversible, short-acting AChE inhibitor

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33
Q

Neostigmine

A

Covalent, reversible, medium-acting AChE inhibitor

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34
Q

Physostigmine

A

Covalent, reversible, medium-acting AChE inhibitor

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35
Q

Ecothiophate

A

Long-acting, irreversible AChE inhibitor

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36
Q

Nerve gases (tabun, sarin, novichok etc.)

A

Long-acting, irreversible AChE inhibitors

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37
Q

Isoprenaline

A

β-selective AR agonist

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38
Q

Noradrenaline

A

αAR-selective agonist

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39
Q

Adrenaline

A

Non-selective AR agonist

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40
Q

α-Methyldopa

A

Competative inhibitor of tyrosine hydroxylase

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41
Q

L-DOPA

A

Product of tyrosine hydroxylase that can boos dopamine synthesis

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42
Q

Carbidopa

A

Inhibitor of peripheral DOPA decarboxylase

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43
Q

Disulfiram

A

Inhibitor of dopamine β hydroxylase

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44
Q

α-Μethyldopa

A

False transmitter released with DA and NA that acts as an α2-selective AR agonist

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45
Q

Reserpine

A

Irreversible blocker of VMAT2-mediated monoamine uptake into vesicles

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46
Q

Guanethidine

A

Low doses block impulse conduction at adrenergic synapses<div>High doses leads to a depletion of NA</div>

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47
Q

Dexamfetamine

A

Indirectly-acting sympatheticomimetic that causes adrenergic neurotransmitter release via a Ca2+-independant mechansim

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48
Q

Ephedrine

A

Mixed acting sympatheticomimetic that causes both release of NA and acts directly as an agonist at adrenoceptors

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49
Q

Imipramine

A

TCA that inhibits NET/Uptake 1

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50
Q

6-Hydropamine

A

Synthetic neurotoxin used to destroy dopaminergic neurones and induce PD in animal models

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51
Q

Phenoxybenzamine

A

Irreversible αAR antagonist that also blocks ENT/Uptake 2 at high concentrations

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52
Q

Normetanephrine

A

Metabolite of NA that blocks ENT/Uptake 2

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53
Q

Entacapone

A

COMT inhibitor

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54
Q

Xylometazoline

A

αAR-selective agonist

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55
Q

Phenylephrine

A

α1AR-selective agonist

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56
Q

Clonidine

A

α2AR-selective agonist

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57
Q

Dobutamine

A

β1AR-selective agonist

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58
Q

Salbutamol

A

Short-acting β2AR-selective agonist

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59
Q

Terbutaline

A

Short-acting β2AR-selective agonist

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60
Q

Salmeterol

A

Long-acting β2AR-selective agonist

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61
Q

Formerol

A

Long-acting β2AR-selective agonist

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62
Q

Indacaterol

A

Long-acting β2AR-selective agonist

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63
Q

Mirabegron

A

β3AR-selective agonist

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64
Q

Phentolamine

A

αAR-selective antagonist

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65
Q

Phenoxybenzamine

A

αAR-selective antagonist

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66
Q

Prazosin

A

α1AR-selective and competative antagonist

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67
Q

Idazoxan

A

α2AR-selective antagonist

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68
Q

Tamsulosin

A

α1AAR-selective antagonist

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69
Q

Yohimbine

A

α2AR-selective antagonist

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70
Q

Propranolol

A

Non-selective βAR antagonist

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71
Q

Atenolol

A

β1AR-selective antagonist

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72
Q

Bisoprolol

A

β1AR-selective antagonist

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73
Q

Carvedilol

A

Mixed α1/βAR-selective antagonist that exhibits G-protein signalling bias

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74
Q

Nebivolol

A

3rd generation β1AR-selective antagonist that also stimulates NO(g) release

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75
Q

Caffeine

A

Competative antagonist of the A1 adenosine receptors

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76
Q

Regadenoson

A

A2A-selective adenosine receptor agonist

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77
Q

Tetracaine

A

Use-dependant neuronal-selective Na+channel blocker

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78
Q

Benzocaine

A

Use-dependant neuronal-selective Na+channel blocker

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79
Q

RAC-421

A

Synthetic neuronal-selective Na+channel blocker

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80
Q

QX-314

A

Synthetic use-dependant Na+channel blocker

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81
Q

Nifedapine

A

Dihydropyridine smooth muscle-selective Ca2+channel blocker

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82
Q

Amlodipine

A

Dihydropyridine smooth muscle-selective Ca2+channel blocker

83
Q

Felodipine

A

Dihydropyridine smooth muscle-selective Ca2+channel blocker

84
Q

Verapamil

A

Phenylalkylamine cardiac muscle-selective Ca2+channel blocker

85
Q

Diltiazem

A

Benzothiazepine type Ca2+channel blocker

86
Q

Tetrodotoxin

A

Highly-selective, reversible blocker to neuronal Na+ channels

87
Q

Saxitoxin

A

Highly-selective, reversible blocker to neuronal Na+channels

88
Q

Batrachotoxin

A

Neurotoxin that lowers the threshold for opening and inhibits inactivation of Na+channels

89
Q

α-scorpiotoxin

A

Neurotoxin that binds with voltage-dependance and inhibits activation of Na+channels

90
Q

Quinidine

A

Class IA antidysrhythmic that acts as a<b> </b>use-dependant sodium channel blocker

91
Q

Procainamide

A

Class IA antidysrhythmic that acts as a<b></b>use-dependant sodium channel blocker

92
Q

Disopyramide

A

Class IA antidysrhythmic that acts as a<b></b>use-dependant sodium channel blocker

93
Q

Lidocaine

A

Class IB antidysrhythmic that acts as a<b></b>use-dependant sodium channel blocker

94
Q

Mexilitine

A

Class IB antidysrhythmic that acts as a<b></b>use-dependant sodium channel blocker

95
Q

Flecainide

A

Class IC antidysrhythmic that acts as a<b></b>use-dependant sodium channel blocker

96
Q

Propafenone

A

Class IC antidysrhythmic that acts as a<b></b>use-dependant sodium channel blocker

97
Q

Amiodarone

A

Class III antidysrhythmic that acts as an action potential prolonging agent

98
Q

Sotalol

A

Class III antidysrhythmic that acts as an action potential prolonging agent

99
Q

Digoxin

A
  • Cardiac glycoside that inhibits the Na+/K+ATPase<div>- Also increases vagal activity through actions in the CNS</div>
100
Q

Ouabain

A

Cardiac glycoside that inhibits the Na+/K+ATPase

101
Q

Phenothiazine

A

PDE1 inhibitor

102
Q

Milrinone

A

PDE3 inhibitor

103
Q

Rolipram

A

PDE4 inhibitor

104
Q

Sildenafil

A

PDE5 inhibitor

105
Q

Dipyridamole

A

PDE5 inhibitor

106
Q

Caffiene

A

<div>Methylxanthine drug that acts as a non-selective PDE inhibitor and an A1/A2 adenosine receptor antagonist</div>

107
Q

Theophylline

A

Methylxanthine drug that acts as a non-selective PDE inhibitor and an A1/A2adenosine receptor antagonist

108
Q

Prednisolone

A

Glucocorticoid receptor agonist

109
Q

Mifepristone

A

Glucocorticoid receptor antagonist

110
Q

Spironolactone

A

Mineralocorticoid receptor antagonist

111
Q

Fludrocortisone

A

Mineralocorticoid receptor agonist

112
Q

Ethinylestradiol

A

Oestrogen receptor agonist

113
Q

Tamoxifen

A

Oestrogen receptor antagonist

114
Q

Norethisterone

A

Progestagen receptor agonist

115
Q

Danazol

A

Progestagen receptor antagonist

116
Q

Streptokinase

A

Tissue plasminogen activator that promotes the generation of plasmin

117
Q

Alteplase

A

Recombinant human tissue plasminogen activator that leads to activation of plasmin

118
Q

Aspirin

A

COX1 inhibitor that prevents the formation of thromboxane A2and hence inhibits platelet aggregation

119
Q

Clopidogrel

A

Irreversible, competative P2Y12receptor antagonist (pro-drug)

120
Q

Prasugrel

A

Irreversible, competative P2Y12receptor antagonist (pro-drug)

121
Q

Ticagrelor

A

Irreversible, competative P2Y12receptor antagonist

122
Q

Eptifibatide

A

Cyclic heptapeptide antagonist of gpIIb/IIIa

123
Q

Tirofiban

A

Non-peptide antagonist of gpIIb/IIIa receptor

124
Q

Abciximab

A

Monoclonal antibody against gpIIb/IIIa that also binds to the vitronectin receptor to prevent platelet aggregation

125
Q

Heparin

A

Indirect thrombin inhibitor that binds to and activates anti-thrombin

126
Q

Dalteparin

A

Low molecular weight heparin that acts as an indirect thrombin inhibitor by binding to and activating anti-thrombin

127
Q

Tinzaparin

A

Low molecular weight heparin that acts as an indirect thrombin inhibitor by binding to and activating anti-thrombin

128
Q

Warafin

A

Vitamin K antagonist that inhibits VKORC1 and the formation of factors II, VII, IX and X

129
Q

Dabigatran

A

Direct thrombin inhibitor

130
Q

Rivaroxaban

A

Direct oral anticoagulant that acts as a factor Xa inhibitor

131
Q

Apixaban

A

Direct oral anticoagulant that acts as a factor Xa inhibitor

132
Q

Edoxaban

A

Direct oral anticoagulant that acts as a factor Xa inhibitor

133
Q

Fondaparinux

A

Indirect inhibitor of factor Xa

134
Q

Argatroban

A

Synthetic direct thrombin inhibitor

135
Q

Bivalirudin

A

Hirudin analogue that acts as a thrombin inhibitor

136
Q

Danaparoid

A

Indirect inactivator of factor Xa<div>Direct inhibitor of factor IX activation</div>

137
Q

Tranexamic acid

A

Competative inhibitor of tissue plasminogen activator

138
Q

Furosemide

A

Loop diuretic that blocks NKCC2 in the apical membrane of cells in the TAL

139
Q

Bumetanide

A

Loop diuretic that blocks NKCC2 in the apical membrane of cells in the TAL

140
Q

Probenecid

A

Competative ligand for the uric acid transporter that inhibits its reabsorption

141
Q

Hydrochlorothiazide

A

Thiazide diuretic that blocks NCC on the apical membrane of the cells of the TAL/DCT

142
Q

Bendroflumethiazide

A

Thiazide diuretic that blocks NCC on the apical membrane of the cells of the TAL/DCT

143
Q

Amiloride

A

K+sparring diuretic that blocks the ENaC channel on the apical membrane of cells in the late DCT

144
Q

Triamterene

A

K+sparring diuretic that blocks the ENaC channel on the apical membrane of cells in the late DCT

145
Q

Spironolactone

A

K+sparring diuretic that acts as an antagonists of the mineralocorticoid receptor in the cells of the late DCT

146
Q

Acetozolamide

A

Carbonic anhydrase inhibitor that acts as a weak diuretic

147
Q

Mannitol

A

Osmotic diuretic

148
Q

Ramipril

A

ACE-Inhibitor

149
Q

Captopril

A

ACE-Inhibitor

150
Q

Enalapril

A

ACE-Inhibitor

151
Q

Lisinopril

A

ACE-Inhibitor

152
Q

Perindopril

A

ACE-Inhibitor

153
Q

Saralasin

A

Partial agonist of the angiotensin receptor

154
Q

Losartan

A

Angiotensin receptor blocker

155
Q

Valsartan

A

Angiotensin receptor blocker

156
Q

Candesartan

A

Angiotensin receptor blocker

157
Q

Desmopressin

A

AVP/ADH analogue and agonst of the AVPR2 receptor

158
Q

Aliskiren

A

Direct renin inhibitor

159
Q

Doxazocin

A

α1AR antagonist

160
Q

Labetalol

A

<div>α1, β1 and β2 antagonist that is β-selective</div>

161
Q

Minoxidil

A

KATP channel activator that causes relaxation of vascular smooth muscle

162
Q

Nicorandil

A

KATPchannel activator that also acts as an NO(g)donor to trigger relaxation of vascular smooth muscle

163
Q

Diazoxide

A

KATPchannel activator

164
Q

Simvastatin

A

Short-acting HMG-CoA Inhibitor

165
Q

Lovastatin

A

Short-acting HMG-CoA Inhibitor

166
Q

Pravastatin

A

Short-acting HMG-CoA Inhibitor

167
Q

Atorvostatin

A

Long-acting HMG-CoA Inhibitor

168
Q

Rosuvastatin

A

Long-acting HMG-CoA Inhibitor

169
Q

Alirocumab

A

PCSK9 Inhibitor

170
Q

Evolocumab

A

PCSK9 Inhibitor

171
Q

Bezafibrate

A

PPARα activator that increases transcription of genes involved in lipid metabolism

172
Q

Ezetimibe

A

<div>NPC1L1 transport proteinblocker that inhibitsintestinal absorptionofcholesterolinbrush border of enterocytes</div>

173
Q

Colestyramine

A

Anion exchange resin that inhibits bile acid uptake by the liver that leads to an upregulation of LDL-R surface expression

174
Q

Niacin/nicotinic acid

A

Pro-drug that is converted to nicotinamide which inhibits hepatic VLDL secretion causing a secrease in LDL

175
Q

Glyceryl Trinitrate/Nitroglycerine/GTN

A

Short-acting nitrate derivative that activates guanylyl cyclase

176
Q

Isosorbide mononitrate

A

Long-acting nitrate derivative that activates guanylyl cyclase

177
Q

Ivabradine

A

HCN (If current) blocker

178
Q

Ranolazine

A

Inhibitor of the late phase Na+currents

179
Q

Adenosine

A

Agonist of the A1receptors which trigger hyperpolarisation of pacemaker and conductive cells

180
Q

Benserazide

A

Peripheral DOPA-decarboxylase inhibitor

181
Q

Ether

A
  • Inhalational general anaesthetic<div>- Prevents cellular depolarisation<br></br></div>
182
Q

Etomidate

A
  • Intravenous general anaesthetic<div>- Acts on β3 (or β2) subunit of the GABAA receptor resulting in Cl-influx andhyperpolarisation ofthe postsynaptic membrane</div>
183
Q

Halothane

A
  • Inhalational general anaesthetic<div>- Activates the TASK3 member of the two-pore domain potassium channel (K2P) family leading to hyperpolarisation and reduced neuronal activity<br></br></div><div>-Also acts on theα and β subunits of the GABAAreceptor to cause Cl-influx and hyperpolarisation</div>
184
Q

Nitrous Oxide, NO(g)

A
  • Inhalational general anaesthetic that activates the TASK3 member of the two-pore domain potassium channel (K2P) family leading to hyperpolarisation and reduced neuronal activity<div>- May also inhibit the excitatory NMDA receptors</div>
185
Q

Propofol

A
  • Intravenous general anaesthetic<br></br>- Acts on β3(or β2) subunit of the GABAAreceptor resulting in Cl-influx andhyperpolarisation ofthe postsynaptic membrane<br></br>
186
Q

Thiopental (thiopentone)

A
  • Intravenous general anaesthetic<div>- Short acting barbiturate (positive allosteric modulator)</div><div>- Acts on β3(or β2) subunit of the GABAAreceptor resulting in Cl-influx andhyperpolarisation ofthe postsynaptic membrane<br></br></div>
187
Q

Isoflurane

A
  • Inhalational general anaesthetic<div>- Activates the TASK3 member of the two-pore domain potassium channel (K2P) family leading to hyperpolarisation and reduced neuronal activity<br></br></div><div>-Also acts on theα and β subunits of the GABAAreceptor to cause Cl-influx and hyperpolarisation</div>
188
Q

Xenon

A
  • Inhalational anaesthetic<div>- Mayinhibit the excitatory NMDA receptors, which are activated by glutamate</div>
189
Q

Fosfomycin

A
  • Bacterial cell wall synthesis inhibitor<div>- StructuralanalogueofPEPthat competitivelyinhibits pyruvyl transferasetoprevent synthesisofNAM</div>
190
Q

Cycloserine

A

<div>- Bacterial cell wall synthesis inhibitor</div>

<div>- Structural analogue of D-Alanine that competitively inhibits the enzymes responsible for D-Alanine biosynthesis and addition to the peptide crossbridge</div>

191
Q

Bacitracin

A

<div>- Bacterial cell wall synthesis inhibitor</div>

<div>- Binds to bactoprenol-pyrophosphate in the extracellular leaflet and prevents its hydrolysis and return to the cytosolic leaflet</div>

192
Q

Penicillin

A
  • Bacterial cell wall synthesis inhibitor<div>- β-lactam mimicsthe peptide bond in the D-Ala-D-Ala terminus</div><div>- Binds to transpeptidase and prevents it from acting on its target in peptidoglycan synthesis</div>
193
Q

Vancomycin

A

<div>- Bacterial cells wall synthesis inhibitor</div>

<div>- Forms hydrogen bonds with the D-Ala-D-Ala terminus<br></br></div>

<div>-This causes steric hindrance of transglycosylation <b></b></div>

<div>- Inhibits bacterial protein synthesis<br></br></div>

194
Q

Tetracycline

A
  • Broad spectrum tetracycline-class of bacteriostatic antibiotic<div><div>- Reversibly binds to the 30S ribosomal subunit<br></br></div> <div>-Inhibits the entry of aminoacyl-tRNA into the acceptor site (A-site) on the 70S ribosome</div></div><div>- Inhibits bacterial protein synthesis<br></br></div>
195
Q

Doxycycline

A
  • Broad spectrum tetracycline-class of bacteriostatic antibiotic<div><div>- Reversibly bindsto the30S ribosomalsubunit<br></br></div><div>-Inhibitstheentryofaminoacyl-tRNAinto theacceptor site(A-site) on the 70S ribosome</div></div><div>- Inhibits bacterial protein synthesis</div>
196
Q

Streptomycin

A

<div>- Narrow spectrum aminoglycoside bactericidal antibiotic</div>

<div>-Binds to the 30S ribosomal subunit and freeze the 30S pre-initiation complex so that no further initiation can occur</div>

<div>-Also slows down protein synthesis that has already been initiated and induce misreading of the mRNA</div>

<div>- Inhibits bacterial protein synthesis<br></br></div>

197
Q

Gentamycin

A

<div>- Narrow spectrum aminoglycosidebactericidalantibiotic</div>

<div>-Binds to the30S ribosomalsubunit andfreezethe 30Spre-initiation complexso that no further initiation can occur.</div>

<div>-Also slows down protein synthesisthat hasalready been initiatedandinduce misreadingof themRNA</div>

<div>- Inhibits bacterial protein synthesis<br></br></div>

198
Q

Neomycin

A

<div>- Narrow spectrum aminoglycosidebactericidalantibiotic</div>

<div>-Binds to the30S ribosomalsubunit andfreezethe 30Spre-initiation complexso that no further initiation can occur</div>

<div>-Also slows down protein synthesisthat hasalready been initiatedandinduce misreadingof themRNA</div>

<div>- Inhibits bacterial protein synthesis<br></br></div>

199
Q

Erythromycin

A

<div>- Narrow spectrum bacteriostatic macrolide antibiotic</div>

<div>-Binds to the entrance of the polypeptide exit tunnelin 50S subunit</div>

<div>-Specifically,binds to the 23S rRNA component via hydrogen bonds with nitrogenous bases</div>

<div>- Inhibits bacterial protein synthesis</div>

200
Q

Clarithromycin

A

<div>- Extended spectrum bacteriostatic macrolide antibiotic</div>

<div>-Binds to the entrance of thepolypeptide exit tunnelin 50S subunit</div>

<div>-Specifically,bindsto the23S rRNAcomponent via hydrogen bonds with nitrogenous bases</div>

<div>- Inhibits bacterial protein synthesis</div>

201
Q

Azithromycin

A

<div>- Extended spectrum bacteriostatic macrolideantibiotic</div>

<div>-Binds to the entrance of thepolypeptide exit tunnelin 50S subunit</div>

<div>-Specifically,bindsto the23S rRNAcomponent via hydrogen bonds with nitrogenous bases</div>

<div>- Inhibits bacterial protein synthesis</div>

202
Q

Chloramphenicol

A

<div>- Broad-spectrumbacteriostaticantibiotic</div>

<div>- Binds to the 50S ribosomal subunit and binds near aminoacyl-tRNA binding site (A site)</div>

<div>-Prevents peptidyl transferase activity</div>

<div>- Inhibits bacterial protein synthesis</div>

203
Q

Fusidic Acid

A

<div>- Narrow spectrum bacteriostatic antibiotic</div>

<div>-Binds to elongation factor G (EF-G) and inhibits its GTPase activity,preventing peptide translocation </div>

<div>- Inhibits bacterial protein synthesis</div>

MedST IB: Mechanisms of Drug Action (MoDA) (10 decks)

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