Pharmacology of Peripheral Neural Transmission Flashcards

1
Q

Atropine

A

Non-selective mAChR antagonist - blocks PNS actions

Dilate eyes, decrease glandular secretions, bronchodilation, decreased GI motility, increased HR

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2
Q

Atracurium, Pancuronium

A

Non-depolarising N.M.J. blockers used as muscle relaxants in surgery (greater effect on fast muscle fibres)

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3
Q

Riociguat

A

Allosteric activator of soluble guanylyl cyclase used in some forms of pulmonary hypertension

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4
Q

Carbidopa

A

Peripheral DDC inhibitor used to reduce the side-effects of L-DOPA

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5
Q

Atenolol

A

Beta-1-receptor antagonist used as an antihypertensive

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6
Q

Tetanus toxin

A

Cleaves synaptobrevin in inhibitory neurons (to motor neurons) increasing excitability

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7
Q

L-DOPA

A

Dopamine precursor used to increase production in brain in Parkinson’s

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8
Q

Entacapone

A

COMT inhibitor used in Parkinson’s

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9
Q

Reserpine

A

Binds VMAT-2 preventing uptake of NA (& 5-HT) into vesicles was used as antihypertensive but discontinued due to profound depression

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10
Q

Hexamethonium

A

Ganglionic nAChR channel pore blocker

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11
Q

Isoprenaline

A

Beta-receptor agonist was used in asthma but the increase in HR was problematic

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12
Q

Mecamylamine

A

Non-competitive ganglionic blocker

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13
Q

Pirenzepine

A

M1 antagonist used to decrease acid secretion

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14
Q

Darifenacin

A

M3 antagonist used to decrease bladder activity

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15
Q

Dipyridamole

A

Blocks uptake of adenosine - potentiates response

& inhibits PDE-V

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16
Q

Tyramine

A

Displaces NA from vesicles causing vasoconstriction (especially in people taking MAO inhibitors)

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17
Q

Clonidine

A

Slightly selective alpha-2-receptor agonist used as an anti-hypertensive (acts in hindbrain - maybe on imidazoline I-1-receptor)

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18
Q

Edrophonium

A

Short-acting anti-AChE used to diagnose myasthenia gravis

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19
Q

Alpha-bungarotoxin

A

N.M.J. blocker

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20
Q

Clorgiline

A

Selective inhibitor of MAO-A used in depression

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21
Q

Xylazine

A

Alpha-2-receptor agonist veterinary sedative (good because doesn’t cause respiratory depression)

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22
Q

Phenoxybenzamine

A

Blocks uptake 2 (& 1 at 10x high concentrations) irreversible alpha-receptor blocker

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23
Q

Dobutamine

A

Beta-1-receptor agonist used in acute cardiogenic shock

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24
Q

Benzilylcholine mustard

A

Irreversible mAChR antagonist (alkylates the receptor)

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25
Q

Triethylcholine

A

Competitive substrate for choline acetyltransferase: forms false transmitter acetyl-TECh

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26
Q

Butaxamine

A

Beta-2-receptor antagonist

27
Q

Beta-bungarotoxin

A

Binds potassium channel and has PLA2 activity - destroys the nerve ending

28
Q

Neostigmine

A

Medium-acting anti-AChE used as oral treatment for myasthenia gravis

29
Q

Sildenafil

A

PDE5 inhibitor used to treat impotence and pulmonary arterial hypertension

30
Q

Phaeochromocytoma

A

Catecholamine-secreting chromaffin tumour causing hypertension
Prazosin used to reduce BP and atenolol/phenoxybenzamine used to prevent the effects of large catecholamine release when tumour removed surgically

31
Q

Guanethidine

A

Block NA release

32
Q

Pilocarpine, Bethanechol

A

Non-selective mAChR agonist (& muscarine)
P: used topically to treat glaucoma
B: used in urinary retention

33
Q

Alpha-latrotoxin

A

Binds neurexins forming a calcium permeable pore causing mass ACh release

34
Q

Amitryptiline, Imipramine

A

Tricyclic antidepressants block uptake 1

35
Q

Trimetaphan

A

Autonomic ganglion blocker - competitive antagonist of nAChR

36
Q

Phenylephrine

A

Alpha-1-receptor agonist used to increase BP in acute hypotension

37
Q

Caffeine

A

A1-adenosine receptor antagonist it’s waking effect most prominent after prolonged wakefulness
Also inhibits PDE causing an increase in heart rate/force of contraction

38
Q

Nitroglycerin

A

Nitrovasodilators (NO donor) used to treat angina

39
Q

Cevimeline

A

M3 agonist (only selective mAChR agonist) used to treat dry mouth in Sjögren’s syndrome

40
Q

d-tubocurarine

A

Relatively non-selective nAChR antagonist

41
Q

Tranylcypromine

A

Non-selective irreversible MAO inhibitor used in refractory depression

42
Q

Tripitramine

A

M2 antagonist

43
Q

Pralidoxime

A

Reverses phosphorylation caused by Dyflos/Malathion but only in first few hours

44
Q

Vesamicol

A

Non-competitive & reversible blocker of the vesicular ACh transporter

45
Q

Dyflos, Malathion

A

Long-acting (irreversible) anti-AChE - organophosphorus compounds
Malathion used as insecticide (lice)

46
Q

Sugammadex

A

Restores transmission blocked by steroid N.M.J. blockers by forming an inactive complex in plasma, excreted in urine

47
Q

Botulinum toxins

A

Blocks transmission, preferentially affects cholinergic nerves:
B, D, F, G: cleave synaptobrevin
A, E: cleave SNAP-25
C1: cleaves syntaxin & SNAP-25

48
Q

Salbutamol

A

Beta-2-receptor agonist used to relieve bronchoconstriction in asthma
Salmeterol is a long-acting agonist

49
Q

ADMA

A

Endogenous NOS inhibitor

50
Q

Alpha-methyltyrosine

A

Competitive inhibitor of TOH used experimentally to decrease NA production

51
Q

Labetalol

A

Combined alpha/beta-receptor antagonists used to treat hypertension in pregnancy

52
Q

Dexamfetamine

A

Taken up into vesicle, reduces pH gradient and therefore amine storage
Ritalin & MDMA similar

53
Q

Propranolol

A

Beta-receptor antagonist was used as an antihypertensive but there is a risk of bronchoconstriction, also causes fatigue & claudication

54
Q

Tamsulosin

A

Alpha-1A-receptor antagonist used to allow bladder emptying in benign prostatic hyperplasia
Dutasteride used a co-therapy to inhibit testosterone production

55
Q

Phentolamine

A

Alpha-receptor antagonist used in hypertension until superseded by selective drugs (non-selective give reflex tachycardia)

56
Q

Idazoxan

A

Alpha-2-receptor antagonist

57
Q

Hemicholinium

A

Binds to the choline transporter inhibiting uptake

58
Q

Cocaine

A

Blocks uptake 1

59
Q

Selegiline

A

Selective inhibitor of MAO-B used in Parkinson’s

60
Q

Alpha-methyldopa

A

Converted to alpha-methylNA which causes vasodilation

61
Q

Decamethonium, Suxamethonium

A

N.M.J. depolarising blocker

62
Q

Prazosin

A

Alpha-1-receptor antagonist used to treat hypertension and Raynaud’s syndrome (peripheral vascular disease)

63
Q

Mirabegron

A

Beta-3-receptor agonist used to treat overactive bladder