MODA List 1 > 1-2 Hiley > Flashcards

1-2 Hiley Flashcards

(62 cards)

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1
Q

Tetanus toxin

A

Retrogradely transported to motor cell body
Transfers to inhibitory inter neuron, blocking it
Motor neuron more excitable
Targets SNARE synaptobrevin

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2
Q

Botulinum toxins

A

Preferentially effects cholinergic neurons
C terminus of heavy chain binds ganglioside receptor
N terminus translocates light chain into the cell through a channel
Light chain has peptidase activity, and inside, cleaves the snare
Blocks ACh release

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3
Q

Botulinum toxin C1Target

A

Syntaxin and SNAP25

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4
Q

Botulinum toxins A&ETarget

A

SNAP25

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5
Q

Botulinum toxins B,D,F,GTarget

A

Synaptobrevin

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6
Q

Hemicholinium

A

Blocks transporter that takes up choline into nerve cell

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7
Q

Vesamicol

A

Blocks transporter that carries ACh into storage vesicles

Non-Competitive and reversible inhibition

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8
Q

B-bungarotoxin

A

Blocks ACh release

Acts through phospholipase A2

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9
Q

a-latrotoxin

A

Binds neurexins

Cause massive release if ACh

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10
Q

a-bungarotoxin

A

Irreversible antagonist at nmj, at nicotinic ACh receptor

Doesn’t affect ganglionic receptors

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11
Q

Nicotine

A

Nicotinic ACh agonist
Stimulates post synaptic cell
Long-lasting
Phase I block - VGNa channels inactivated
Phase II block - nicotinic receptors become desensitised -can be directly stimulated by electrical means

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12
Q

Hexamethonium

A

Use dependent blockade of ganglionic transmission nACh receptor
Double positive charge - had to be administered frequently by injection
Causes loss of sympathetic and parasympathetic control

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13
Q

D-tubocurarine

A

Nicotinic receptor antagonist
Non selective between ganglion and nmj
Quaternary ammonium compounds so not orally active

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14
Q

Atracurium

A

Competitive antagonist at the nicotinic receptor of the nmj
Quaternary ammonium compound
Not orally active
Tetanic fade (tetanus is not maintained) due to block of nicotinic receptors on nerve endings auto receptors , positive feedback to maintain transmitter release
Ester - spontaneous hydrolysis and plasma esterases

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15
Q

Pancuronium

A

Competitive antagonist at the nicotinic receptor of the nmj
Quaternary ammonium compound
Not orally active
Tetanic fade (tetanus is not maintained) due to block of nicotinic receptors on nerve endings auto receptors , positive feedback to maintain transmitter release
Long action, not hydrolysed

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16
Q

Suxamethonium

A

Block nicotinic receptor at nmj by causing prolonged depolarisation
Depolarisation of phase I- anticholinesterases deepen the blockade
Effects can be opposed by non-depolarising blockers
Phase II - repolarisation, anticholinesterases reverse the blockade
Only depolarising blocker in clinical use
Short duration - ester broken down by plasma BuCHE

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17
Q

Muscarine

A

Muscarinic receptor (agonist)

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18
Q

Acetylcholine

A

Non selective agonist at muscarinic acetyl choline receptors

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19
Q

Bethanechol

A

Non selective agonist at muscarinic acetyl choline receptors
Poorly absorbed in GI tract
Systemic use in bladder dysfunction

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20
Q

Pilocarpine

A

Non selective agonist at muscarinic acetyl choline receptors
Poorly absorbed from GI tract
Treatment of glaucoma, contracts ciliary muscle, traction on trabecular meshwork, facilitates aqueous humour drainage

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21
Q

Atropine

A 
Non selective antagonist of muscarinic acetylcholine receptor 
Dilate pupils (mydriasis) 
Long duration
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22
Q

Darifenacin

A

Antagonist m3 muscarinic acetylcholine receptor

Mediate bladder constriction

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23
Q

Edrophonium

A

Short acting, reversible ionic interaction with AChE

Used for diagnosis of myasthenia gravis

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24
Q

Neostigmine

A

Medium acting, reversible weak covalent bond with AChE
Orally treats myasthenia gravis
Bind esteratic site and carbomylate enzyme
Intravenously to reverse neuromuscular blockade

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25
Dyflos
Long acting, irreversible strong covalent bond with AChE | Glaucoma
26
Malathion
Long acting, irreversible strong covalent bond with AChE Insecticide to kill lice Activated by replacement of S with O More efficient in insect cytochrome P450
27
Pralidoxime
Reverse inhibition of AchE by organophosphorous agents Brings oxime (nucleophile) close to phosphorylated serine Only occur a few hours after inhibition - before ageing occurs
28
Carbidopa
Inhibit peripheral dopadecarboxylase | Reduce peripheral side effects of increased NA and DA
29
Methyldopa (a-methyldopa)
``` Converted by DDC to alphamethyldopamine Then by DBH to alphamethylnoradrenaline Stored and released with NA False transmitter Anti hypertensive agent in CNS ```
30
Reserpine
Binds amine binding site Irreversibly blocks VMAT (vesicular monoamine transporter) Prevents transport of NA and DA from cytoplasm into vesicles Blocks uptake Long lasting depletion of stored NA Anti hypertensive Side effects of psychological depression from serotonin depletion
31
Tyramine
In cheese, red wine and marmite Transported into nerve endings and storage vesicles Displaces NA from vesicle, NA reaches extra cellular space and activates local adrenoceptors= indirectly acting sympathomimetic amine Uptake 1 substrate
32
Dexamfetamine (D-amphetamine)
Alpha methyl group so not metabolised by MAO Weak inhibitor of MAO Taken up into vesicles, reduces pH gradient and packing of amines Displaced NA leaves nerve and stimulates receptors Uptake 1 substrate
33
Guanethidine
Taken up into nerve by uptake 1 (substrate) Low doses - block release of NA High doses - act as indirectly acting sympathomimetic amines
34
Cocaine
Blocks NET (norepinephrine transport protein), blocks uptake 1
35
Imipramine
Tricyclic antidepressant Blocks NET (norepinephrine transporter protein), blocks uptake 1 Block NA and 5HT transport
36
Amitryptyline
Tricyclic antidepressant Blocks NET (norepinephrine transporter protein), blocks uptake 1 Block NA and 5HT transport
37
Clorgiline
Selectively inhibits MAO-A | Used in depression
38
Selegiline
Selectively inhibits MAO-B | Treats Parkinson's (MAO-B metabolises DA)
39
Tranylcypromine
Non selective irreversible inhibitor MAO | Treatment of refractory depression
40
Entacapone
Inhibitor of COMT (catechol-I-methyltransferase) | Treat parkinsons
41
Noradrenaline
Adrenoreceptor agonist | a1a2 B1B2
42
Adrenaline
Adrenoreceptor agonist | a2a1B
43
Isoprenaline
``` Adrenoreceptor agonist B Asthma - relax bronchi But increase in heart rate Replaced by salbutamol ```
44
Phenylephrine
Adrenoreceptor agonist a1B1 Raise blood pressure in acute hypotension
45
Methyl INA
Adrenoreceptor agonist | a2a1
46
Clonidine
Adrenoceptor agonist a2a1 Anti hypertensive agent
47
Xylazine
Adrenoreceptor agonist a2a1 Veterinary sedative
48
Salbutamol
Adrenoreceptor agonist | B2B1
49
Dobutamine
Adrenoreceptor agonist B1B2 Acute cardiogenic shock
50
Phentolamine
Adrenoreceptor antagonist a1 a2 Anti hypertensive - but bring about large heart rate increase
51
Prazosin
Adrenoreceptor antagonist a1a2 Used in hypertension
52
Idazoxan
Adrenoreceptor antagonist | a2a1
53
Propranolol
Adrenoreceptor antagonist B1 B2 Used to treat hypertension - but risk of bronch constriction Replaced by atenolol
54
Atenolol
Adrenoreceptor antagonist B1B2 Hypertension, cardiac dysrhythmia, angina With phenoxybenzamine, prevent effects of large releases of catecholamines after tumour displacement
55
Butaxamine
Adrenoreceptor antagonist | B2B1
56
Labetalol
``` Adrenoreceptor antagonist a1 B1 B2 3rd generation B blocker Treat hypertension in pregnancy 4 isomers -RR B blocker, weak a blocker -RS a blocker, weak B blocker -SR no activity -SS a1 blocker ```
57
Caffeine
A1 receptor antagonist Non-selective, also inhibits phosphodiesterase (breaks down cyclic nucleotides) increase rate and force of cardiac contraction Potentiation of cAMP mediated signalling
58
Dipyridamole
Blocks transport of adenosine back into cells | Potentiation responses mediated by adenosine
59
Glyceryl trinitrate(Nitroglycerin)
Nitric oxide donor Nitrovasodilator(Produce NO2) Treat angina
60
L-NMMA
NOS inhibitor Analogue of L-arginine Not very selective D-isomers are inactive
61
ATP
Released from sympathetic neurons | Rapid responses
62
***Mecamylamine(Inversine)
Non selective,non competitive antagonist of nicotinic acetylcholine receptors Orally active Anti hypertensive drug
MODA List 1
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