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MODA drugs > 2 - Pharmacology Of Peripheral Neurotransmission > Flashcards

2 - Pharmacology Of Peripheral Neurotransmission Flashcards

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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
Atropine
``` Non selective antagonist of muscarinic acetylcholine receptor Dilate pupils (mydriasis) Long duration ```
26
Benzilylcholine mustard
Non selective antagonist of muscarinic acetylcholine receptor
27
Pirenzepine
Antagonist of m1 muscarinic acetylcholine receptor | Anti secretory agent, gastro duodenal ulcers
28
Darifenacin
Antagonist m3 muscarinic acetylcholine receptor | Mediate bladder constriction
29
Edrophonium
Short acting, reversible ionic interaction with AChE | Used for diagnosis of myasthenia gravis
30
Neostigmine
Medium acting reversible weak covalent bond with AChE Orally treats myasthenia gravis Bind esteratic site and carbomylate enzyme Intravenously to reverse neuromuscular blockade
31
Dyflos
Long acting, irreversible strong covalent bond with AChE | Glaucoma
32
Malathion
Long acting, irreversible string covalent bond with AChE | Insecticide to kill lice
33
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
34
a-methyltyrosine
Competitive inhibitor of TOH (Tyrosine Hydroxylase) | Reduces NA production
35
Carbidopa
Inhibit peripheral dopadecarboxylase | Reduce peripheral side effects of increased NA and DA
36
Disulfiram
Inhibits DBH (dopa-B-Hydroxylase)
37
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 ```
38
Reserpine
``` Binds amine binding site Blocks uptake Long lasting depletion of stored NA Anti hypertensive Side effects of psychological depression from serotonin depletion ```
39
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
40
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
41
Guanethidine
``` 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
Cocaine
Blocks NET (norepinephrine transport protein), blocks uptake 1
43
Imipramine
Tricyclic antidepressant Blocks NET (norepinephrine transporter protein), blocks uptake 1 Block NA and 5HT transport
44
Amitryptyline
Tricyclic antidepressant Blocks NET (norepinephrine transporter protein), blocks uptake 1 Block NA and 5HT transport
45
Clorgiline
Selectively inhibits MAO-A | Used in depression
46
Selegiline
Selectively inhibits MAO-B Treats Parkinson's (MAO-B metabolises DA)
47
Tranylcypromine
Non selective irreversible inhibitor MAO | Treatment of refractory depression
48
Entacapone
Inhibitor of COMT (catechol-I-methyltransferase) | Treat parkinsons
49
Noradrenaline
Adrenoreceptor agonist a1 a2 B1 B2
50
Adrenaline
Adrenoreceptor agonist a2 a1 B
51
Isoprenaline
``` Adrenoreceptor agonist B Asthma - relax bronchi But increase in heart rate Replaced by salbutamol ```
52
Phenylephrine
Adrenoreceptor agonist a1 B1 Raise blood pressure in acute hypotension
53
Methyl INA
Adrenoreceptor agonist a2 a1
54
Clonidine
Adrenoceptor agonist a2 a1 Anti hypertensive agent
55
Xylazine
Adrenoreceptor agonist a2 a1 Veterinary sedative
56
Salbutamol
Adrenoreceptor agonist B2 B1
57
Dobutamine
Adrenoreceptor agonist B1 B2 Acute cardiogenic shock
58
Phentolamine
Adrenoreceptor antagonist a1 a2 Anti hypertensive - but bring about large heart rate increase
59
Phenoxybenzamine
Adrenoreceptor antagonist (irreversible) a2 a1 With atenolol prevent effects of large releases of catecholamines after tumour displacement
60
Prazosin
Adrenoreceptor antagonist a1 a2 Used in hypertension
61
Yohimbine
Adrenoreceptor antagonist a2 a1
62
Idazoxan
Adrenoreceptor antagonist a2 a1
63
Propranolol
Adrenoreceptor antagonist B1 B2 Used to treat hypertension - but risk of brunch constriction Replaced by atenolol
64
Atenolol
Adrenoreceptor antagonist B1 B2 Hypertension, cardiac dysrhythmia, angina With phenoxybenzamine, prevent effects of large releases of catecholamines after tumour displacement
65
Butaxamine
Adrenoreceptor antagonist B2 B1
66
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 ```
67
Ergotamine
Partial agonist at a adrenoreceptors -used in migraine, but acts on 5HT receptors Ingested - st Anthony's fire, peripheral vasoconstriction, (a1) gangrene
68
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
69
Dipyramidole
Blocks transport of adenosine back into cells | Potentiation responses mediated by adenosine
70
Glyceryl trinitrate | Nitroglycerin
Nitric oxide donor Nitrovasodilator (Produce NO2) Treat angina
71
Isosorbide dinitrate
Nitric oxide donor Nitrovasodilator (Produce NO2) Treat angina
72
L-NMMA
NOS inhibitor Analogue of L-arginine Not very selective D-isomers are inactive
73
7-NI | 7-nitroindazole
Selectively inhibits neuronal NOS
74
L-NIO
Potent and irreversible inhibitor of iNOS (inducible NOS in macrophages)
75
ATP
Released from sympathetic neurons | Rapid responses
76
***Mecamylamine | Inversine
Non selective,non competitive antagonist of nicotinic acetylcholine receptors Orally active Anti hypertensive drug
77
***Octopamine
Similar to norepinephrine Acts on adrenergic and dopaminergic receptors Sympathomimetic agent

MODA drugs (5 decks)

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