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MODA List 1 > 1-2 Hiley > Flashcards

1-2 Hiley Flashcards

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
Q

Dyflos

A

Long acting, irreversible strong covalent bond with AChE

Glaucoma

26
Q

Malathion

A

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
Q

Pralidoxime

A

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
Q

Carbidopa

A

Inhibit peripheral dopadecarboxylase

Reduce peripheral side effects of increased NA and DA

29
Q

Methyldopa (a-methyldopa)

A 
Converted by DDC to alphamethyldopamine 
Then by DBH to alphamethylnoradrenaline 
Stored and released with NA 
False transmitter 
Anti hypertensive agent in CNS
30
Q

Reserpine

A

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
Q

Tyramine

A

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
Q

Dexamfetamine (D-amphetamine)

A

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
Q

Guanethidine

A

Taken up into nerve by uptake 1 (substrate)
Low doses - block release of NA
High doses - act as indirectly acting sympathomimetic amines

34
Q

Cocaine

A

Blocks NET (norepinephrine transport protein), blocks uptake 1

35
Q

Imipramine

A

Tricyclic antidepressant
Blocks NET (norepinephrine transporter protein), blocks uptake 1
Block NA and 5HT transport

36
Q

Amitryptyline

A

Tricyclic antidepressant
Blocks NET (norepinephrine transporter protein), blocks uptake 1
Block NA and 5HT transport

37
Q

Clorgiline

A

Selectively inhibits MAO-A

Used in depression

38
Q

Selegiline

A

Selectively inhibits MAO-B

Treats Parkinson’s (MAO-B metabolises DA)

39
Q

Tranylcypromine

A

Non selective irreversible inhibitor MAO

Treatment of refractory depression

40
Q

Entacapone

A

Inhibitor of COMT (catechol-I-methyltransferase)

Treat parkinsons

41
Q

Noradrenaline

A

Adrenoreceptor agonist

a1a2 B1B2

42
Q

Adrenaline

A

Adrenoreceptor agonist

a2a1B

43
Q

Isoprenaline

A 
Adrenoreceptor agonist 
B 
Asthma - relax bronchi 
But increase in heart rate 
Replaced by salbutamol
44
Q

Phenylephrine

A

Adrenoreceptor agonist
a1B1
Raise blood pressure in acute hypotension

45
Q

Methyl INA

A

Adrenoreceptor agonist

a2a1

46
Q

Clonidine

A

Adrenoceptor agonist
a2a1
Anti hypertensive agent

47
Q

Xylazine

A

Adrenoreceptor agonist
a2a1
Veterinary sedative

48
Q

Salbutamol

A

Adrenoreceptor agonist

B2B1

49
Q

Dobutamine

A

Adrenoreceptor agonist
B1B2
Acute cardiogenic shock

50
Q

Phentolamine

A

Adrenoreceptor antagonist
a1 a2
Anti hypertensive - but bring about large heart rate increase

51
Q

Prazosin

A

Adrenoreceptor antagonist
a1a2
Used in hypertension

52
Q

Idazoxan

A

Adrenoreceptor antagonist

a2a1

53
Q

Propranolol

A

Adrenoreceptor antagonist
B1 B2
Used to treat hypertension - but risk of bronch constriction
Replaced by atenolol

54
Q

Atenolol

A

Adrenoreceptor antagonist
B1B2
Hypertension, cardiac dysrhythmia, angina
With phenoxybenzamine, prevent effects of large releases of catecholamines after tumour displacement

55
Q

Butaxamine

A

Adrenoreceptor antagonist

B2B1

56
Q

Labetalol

A 
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
Q

Caffeine

A

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
Q

Dipyridamole

A

Blocks transport of adenosine back into cells

Potentiation responses mediated by adenosine

59
Q

Glyceryl trinitrate(Nitroglycerin)

A

Nitric oxide donor
Nitrovasodilator(Produce NO2)
Treat angina

60
Q

L-NMMA

A

NOS inhibitor
Analogue of L-arginine
Not very selective
D-isomers are inactive

61
Q

ATP

A

Released from sympathetic neurons

Rapid responses

62
Q

***Mecamylamine(Inversine)

A

Non selective,non competitive antagonist of nicotinic acetylcholine receptors
Orally active
Anti hypertensive drug

MODA List 1 (8 decks)

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