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MODA drugs > 2 - Pharmacology Of Peripheral Neurotransmission > Flashcards

2 - Pharmacology Of Peripheral Neurotransmission Flashcards

1
Q

Tetanus toxin

A

Retrogradely transported to motor cell body
Transfers to inhibitory inter neutron, 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 translocation light chain into the cell through a channel
Light chain has peptidase activity, and once inside, cleaves the snare
Blocks ACh release

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3
Q

Botulinum toxin C1

Target

A

Syntaxin and SNAP25

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4
Q

Botulinum toxins A&E

Target

A

SNAP25

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5
Q

Botulinum toxins B,D,F,G

Target

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

Trimetaphan

A

Blocks ganglionic nicotinic receptors

Competitive antagonist

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11
Q

a-bungarotoxin

A

Irreversible antagonist at nmj

Doesn’t affect ganglionic receptors

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12
Q

Nicotine

A

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

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13
Q

Hexamethonium

A

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

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14
Q

D-tubocurarine

A

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

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15
Q

Atracurium

A

Competitive antagonist at the nicotinic receptor of the nmj
Quaternary ammonium compound
Not orally active
Block end plate potential in response to nerve stimulation
Antagonise affects directly applied by ACh etc
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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16
Q

Pancuronium

A

Competitive antagonist at the nicotinic receptor of the nmj
Quaternary ammonium compound
Not orally active
Block end plate potential in response to nerve stimulation
Antagonise affects directly applied by ACh etc
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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17
Q

Decemethonium

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

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18
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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19
Q

Carbachol

A

Non selective agonist at muscarinic acetyl choline receptors
Not selective between nicotinic and muscarinic receptors

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20
Q

Muscarine

A

Muscarinic receptor (agonist)

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21
Q

Methacholine

A

Agonist for muscarinic receptors
2 isomers
Neither hydrolysed by BuCHE
(+) is a substrate for AChE. More potent than at muscarinic receptors (-)

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22
Q

Acetylcholine

A

Non selective agonist at muscarinic acetyl choline receptors

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23
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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24
Q

Pilocarpine

A

Non selective agonist at muscarinic acetyl choline receptors
Poorly absorbed from GI tract
Treatment of glaucoma, contracts ciliary muscle

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25
Q

Atropine

A 
Non selective antagonist of muscarinic acetylcholine receptor
Dilate pupils (mydriasis)
Long duration
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26
Q

Benzilylcholine mustard

A

Non selective antagonist of muscarinic acetylcholine receptor

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27
Q

Pirenzepine

A

Antagonist of m1 muscarinic acetylcholine receptor

Anti secretory agent, gastro duodenal ulcers

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28
Q

Darifenacin

A

Antagonist m3 muscarinic acetylcholine receptor

Mediate bladder constriction

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29
Q

Edrophonium

A

Short acting, reversible ionic interaction with AChE

Used for diagnosis of myasthenia gravis

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30
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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31
Q

Dyflos

A

Long acting, irreversible strong covalent bond with AChE

Glaucoma

32
Q

Malathion

A

Long acting, irreversible string covalent bond with AChE

Insecticide to kill lice

33
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

34
Q

a-methyltyrosine

A

Competitive inhibitor of TOH (Tyrosine Hydroxylase)

Reduces NA production

35
Q

Carbidopa

A

Inhibit peripheral dopadecarboxylase

Reduce peripheral side effects of increased NA and DA

36
Q

Disulfiram

A

Inhibits DBH (dopa-B-Hydroxylase)

37
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
38
Q

Reserpine

A 
Binds amine binding site
Blocks uptake
Long lasting depletion of stored NA
Anti hypertensive
Side effects of psychological depression from serotonin depletion
39
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

40
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

41
Q

Guanethidine

A 
Blocks release of NA
Taken up into nerve by uptake 1
Low doses - block release of NA
High doses - act as indirectly acting sympathomimetic amines
Uptake 1 substrate
42
Q

Cocaine

A

Blocks NET (norepinephrine transport protein), blocks uptake 1

43
Q

Imipramine

A

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

44
Q

Amitryptyline

A

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

45
Q

Clorgiline

A

Selectively inhibits MAO-A

Used in depression

46
Q

Selegiline

A

Selectively inhibits MAO-B
Treats Parkinson’s
(MAO-B metabolises DA)

47
Q

Tranylcypromine

A

Non selective irreversible inhibitor MAO

Treatment of refractory depression

48
Q

Entacapone

A

Inhibitor of COMT (catechol-I-methyltransferase)

Treat parkinsons

49
Q

Noradrenaline

A

Adrenoreceptor agonist
a1
a2 B1
B2

50
Q

Adrenaline

A

Adrenoreceptor agonist
a2
a1
B

51
Q

Isoprenaline

A 
Adrenoreceptor agonist
B
Asthma - relax bronchi
But increase in heart rate
Replaced by salbutamol
52
Q

Phenylephrine

A

Adrenoreceptor agonist
a1
B1
Raise blood pressure in acute hypotension

53
Q

Methyl INA

A

Adrenoreceptor agonist
a2
a1

54
Q

Clonidine

A

Adrenoceptor agonist
a2
a1
Anti hypertensive agent

55
Q

Xylazine

A

Adrenoreceptor agonist
a2
a1
Veterinary sedative

56
Q

Salbutamol

A

Adrenoreceptor agonist
B2
B1

57
Q

Dobutamine

A

Adrenoreceptor agonist
B1
B2
Acute cardiogenic shock

58
Q

Phentolamine

A

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

59
Q

Phenoxybenzamine

A

Adrenoreceptor antagonist (irreversible)
a2
a1
With atenolol prevent effects of large releases of catecholamines after tumour displacement

60
Q

Prazosin

A

Adrenoreceptor antagonist
a1
a2
Used in hypertension

61
Q

Yohimbine

A

Adrenoreceptor antagonist
a2
a1

62
Q

Idazoxan

A

Adrenoreceptor antagonist
a2
a1

63
Q

Propranolol

A

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

64
Q

Atenolol

A

Adrenoreceptor antagonist
B1
B2
Hypertension, cardiac dysrhythmia, angina
With phenoxybenzamine, prevent effects of large releases of catecholamines after tumour displacement

65
Q

Butaxamine

A

Adrenoreceptor antagonist
B2
B1

66
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
67
Q

Ergotamine

A

Partial agonist at a adrenoreceptors
-used in migraine, but acts on 5HT receptors
Ingested - st Anthony’s fire, peripheral vasoconstriction, (a1) gangrene

68
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

69
Q

Dipyramidole

A

Blocks transport of adenosine back into cells

Potentiation responses mediated by adenosine

70
Q

Glyceryl trinitrate

Nitroglycerin

A

Nitric oxide donor
Nitrovasodilator
(Produce NO2)
Treat angina

71
Q

Isosorbide dinitrate

A

Nitric oxide donor
Nitrovasodilator
(Produce NO2)
Treat angina

72
Q

L-NMMA

A

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

73
Q

7-NI

7-nitroindazole

A

Selectively inhibits neuronal NOS

74
Q

L-NIO

A

Potent and irreversible inhibitor of iNOS (inducible NOS in macrophages)

75
Q

ATP

A

Released from sympathetic neurons

Rapid responses

76
Q

***Mecamylamine

Inversine

A

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

77
Q

***Octopamine

A

Similar to norepinephrine
Acts on adrenergic and dopaminergic receptors
Sympathomimetic agent

MODA drugs (5 decks)

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