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MODA drugs list > PHARMACOLOGY OF PERIPHERAL NEURAL TRANSMISSION > Flashcards

PHARMACOLOGY OF PERIPHERAL NEURAL TRANSMISSION Flashcards

1
Q

α-latrotoxin

A

1 - binds neurexins (TM proteins on nerve membrane) and causes massive ACh release via pore formation.
2 - black widow spider venom
3 - can cause respiratory failure.

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2
Q

7-nitroindazole (7-NI)

A

1 - selectively inhibits neuron nNOS. specific to cell type not isoenzyme.
2 - doesnt effect eNOS or iNOS.

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3
Q

α-methyl tyrosine

A

1 - Experimentally used to competitively inhibt TOH which converts tyrsoine to DOPA and is the rate limiting step in NA synthesis.

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4
Q

α-methyldopa

A

1 - subs for NA and acts as a false transitter.
2 - converted to α-methyldopamine and α-methylNA
3 - α-methylNA has lower activity at α1 but higher at α2R.
4 - an antihypertensive due to lower α1 vasoconstriction and high negative feedback on NA release (α2?)

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5
Q

Amitriptyline

A

1 - used as a tricyclic antidepressant, blocks NET (norepinephrine transport protein), blocking NA and 5HT transport.
2 - NET responsible for uptake 1

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6
Q

Atenolol

A 
1 - selective β1 adrenoceptor antagonist. 
2 - its selectivity reduces the risk of bronchoconstriction. 
3 - a class 2 antidysrhthmic.
4 - can be used with phenoxybenzamine to block the effects of a large release of catecholamines when a phaeochromocytoma is removed.
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7
Q

ATP

A

1 - a purine
2 - natural agonist of P2XR and P2YR
3 - co-released with ACh from motor neurones
4 - P2X is ligand gated ion channel, P2Y is GPCR. many subtypes of both

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8
Q

Atracurium

A

1 - competitive NACHR antagonist. NMJ block.
2 - quaternary ammonium
3 - causes tetanic fade due to autoreceptor block
4 - an ester so rapidly hydrolysed and hence short action.
5 - used in anaesthesia as a muscle relaxant. white muscle>red muscle so reduced risk of respiratory depression.
6 - reversed by anti-AChE

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9
Q

Atropine

A 
1 - MACHR anatagonist nonselective
2 - sympathomimetic effects as it inhibits parasympathetics
3 - tertiary ammonium
4 - from deadly nightshade
5 - mydriasis (dilates pupils)
6 - prolonged action (1 hr ish)
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10
Q

Benzilylcholine mustard

A

1 - irreversible alkylates the MACHR. sympathomimetic.

2 - an ethylamine

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11
Q

Bethanechol

A

1 - an analogue of ACh.
2 - non selective MACHR agonist
3 - poorly absorbed from the GI
4 - occasionally used as a laxative or to stimulate bladder emptying.

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12
Q

Botulinium toxins

A

1 - irreversible antagonist.
2 - preferential to cholinergic neurons.
3 - The light chain has pepsidase activity to cleave the target SNARE.
4 - antitoxin only works within 30 mins of toxin absorption.
5 - Toxin A and E taget SNAP-25. B,D,F and G target synaptobrevin. C1 targets syntaxin and SNAP-25.
6 - somatic muscle weakness and autonomic loss - constipation, blurred vision, dry skin.

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13
Q

β-Bungarotoxin

A

1 - blocks ACh release via phospholipase A2 activity.
2 - localises to the membrane via K channel binding moiety.
3 - common in Krait venoms.

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14
Q

Butaxamine

A

1 - β2 blocker (some β1)

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15
Q

Caffeine

A

1 - A1 (acts via Gi/o) antagonist (hence diuresis via decreased renin?) (also an A2 antagonist)
2 - nonselectively inhibits PDEs so potentiates cAMP signalling and hence rate and force of cardiac contraction along with more disposed to dysrhythmias.
3 - adenosine acts via A1 Rs in the brain to presynaptically inhibits glutamate releasing neurons causing decreased motor activity, respiration, anxiety and to induce sleep. Caffeine inhibits this.
a methylxanthine.
CNS effects due to adenosine antagonism

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16
Q

Carbachol

A

1 - cholinergic agonist, nonselective

2 - quaternary ammonium

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17
Q

Carbidopa

A

1 - inhibits DDC (DOPA decarboxylase)
2 - cant cross BBB so only acts peripherally.
3 - given with DOPA to raise brain DA but reduce peripheral effects
4 - benserazide is similar.

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18
Q

Clonidine

A

1 - α2 (and α1) agonist

2 - antihypertensive but can cause rebound hypertension if a dose is missed. acts via hindbrain receptors

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19
Q

Clorgiline

A

1 - selective MAO-A inhibitor. an antidepressant

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20
Q

Cocaine

A

1 - a NET inhibitor, blocks uptake 1 of catecholamines.

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21
Q

D-amphetamine

A

1 - sympathomimetic amine
2 - weakly inhibits MAO. acts as a weak base so increases pH in vesicles and decreases the pH gradient for neurot uptake.
3 - also inhibits reuptake and is long lasting as it cant be metabolised by MAO. end result is increased NA and DA activity.
4 - ritalin similar effects.
5 - response dependent upon presence of NA in vesicles therefore repeated use causes tolerance.
6 - taken up by uptake 1 NET.

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22
Q

Darifenacin

A

1 - M3 specific MACHR antagonist
2 - inhibits micturition
3 - side effects dry mouth and constipation

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23
Q

Decamethonium

A

1 - NMJ NACHR selective partial agonist, causes depolarisation block.

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24
Q

Dipyridamole

A

1 - inhibits adenosine transporter, thus prevents inactivation.
2 - causes vasodilation and inhibits thrombus formation.

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25
Q

Disulfiram

A

1 - inhibits alcohol dehydrogenase, possibly chelates the catalytic Cu2+.
2 - used to treat alcohol addiction, causes acetaldehyde build up when alcohol is consumed.

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26
Q

Dobutamine

A

1 - analogue of dopamine
2 - β1 agonist. greater ionotroph than chronotroph.
3 - used in acute cardiogenic shock to raise HR and CO
4 - increases HR and O2 demand so arrhythmogenic
5 - can be used to treat heart failure in the absence of hypertension, and improve CO after open heart surgery.

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27
Q

D-tubocurarine

A

1 - NACHR antagonist

2 - quaternary ammonium compound so not orally active

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28
Q

Dyflos (diisopropyl fluorophosphate/DFP)

A

1 - irreversible AChE inhibitor. phosphorylates the serine at the esteratic site.
2 - long lasting and of little use except in glaucoma.
3 - side effect of convulsions, respiratory distress and demyelination.
4 - an organophosphorus compound

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29
Q

Edrophonium

A

1 - quaternary amine
2 - reversible inhibitor of AChE via electrostatic interaction with its ionic site
3 - short acting. cant enter CNS as charged
4 - used to diagnose myesthenia gravis by causing a temporary increase in muscle tension.

30
Q

Entacapone

A

1 - COMP inhibitor
2 - prevents methylation of ring hydroxyls in the liver, neuronal and non-neuronal tissues.
3 - blocks uptake 2 activity
4 - used in parkinsonism.

31
Q

Ergotamine

A

1 - α adrenoceptor and 5HT R partial agonist
2 - used for migranes probs due to 5HT activity.
3 - St Anthony’s fire is the intense peripheral α1 vasoconstriction caused when ergot infected cereals are eaten and can cause gangrene.

32
Q

Guanethidine

A

1 - large doses act as sympathomimetics.
2 - competes with NA for uptake 1 and replaces in vesicles and blocks NA release in response to APs.
3 - an antihypertensive drug that reduces the release of catecholamines, such as NA.
4 - still licensed in the UK for the rapid control of blood pressure in a hypertensive emergency.

33
Q

Hemicholinium

A

1 - blocks reuptake of choline by high affinity choline transporter at the presynaptic membrane. the rate limiting step of ACh production.

34
Q

Hexamethonium

A

1 - 1st ganglion blocker to treat hypertension
2 - use dependent block of NACHR
3 - use discontinued due to loss of symp and para - hexamethonium man.
4 - mecamylamine similar

35
Q

Idazoxan

A

1 - a synthetic yohimbine
2 - both a selective α2 adrenergic receptor antagonist, and an antagonist for the imidazoline receptor.
3 - used experimentally.

36
Q

Imipramine

A

1 - blocks NET

2 - used as tricyclic antidepressant blocking NA and 5HT reuptake.

37
Q

Isoprenaline

A

1 - similar to adrenaline but only β not α.

2 - was used in asthma to relax bronchi but had side effects such as increased HR from β1.

38
Q

Isosorbide dinitrate

A

1 - an NO donor, metabolised in liver to mononitrate and used as a nitrovasodilator to treat angina..

39
Q

Labetalol

A

1 - four isomers have different actions.
2 - all 4 isomers together act as antagonists for α1, β1 and β2.
3 - used to treat hypertension in pregnancy

40
Q

L-NIO (N-iminoethyl-L-ornithine)

A

1 - potent irreversible inhibitor of iNOS in phagosytic cells

41
Q

L-NMMA

A

1 - an analogue of L-arginine
2 - non-selective inhibitor of all NOS isoforms
3 - D-isomer is inactive

42
Q

Malathion

A

1 - an organophosphate
2 - irreversible inhibitor of AChE. phosphorylates serine at the esteratic site.
3 - long lasting, little clinical use except as insecticide to kill lice.

43
Q

Mecamylamine

A

1 - Ganglionic NAChR antagonist. similar to hexamethonium.

44
Q

Methacholine

A

1 - an ACh analogue
2 - nonselective MAChR agonist
3 - +ve isomer hydrolysed by AChE, neither by BuChE.
4 - +ve isomer around 200 times more potent than -ve at muscarinic Rs.

45
Q

Muscarine

A

1 - MAChR agonist from fly agaric muschroom

46
Q

Neostigmine

A

1 - A carbamic acid ester of choline
2 - reversible inhibitor of AChE, carbamoylates the esteratic site.
3 - to treat myasthenia gravis
4 - used IV to reverse NMJ block by raising ACh conc.
5 - given orally to treat myasthenia gravis
6 - the carbamoylated serine hydrolyses much slower than the acetylated serine and thus is inactivated for several minutes.

47
Q

Nicotine

A

1 - NACHR agonist primarily at ganglion.
2 - prolonged exposure causes phase 1 depolarising block
3 - a tertiary amine

48
Q

Nitroglycerine (glyceryl trinitrate)

A

1 - Nitrovasodilator. used to treat angina. NO donor

49
Q

Octopamine

A

?

50
Q

Pancuronium

A

1 - competitive antagonist of NMJ NAChR
2 - quaternary ammonium
3 - causes tetanic fade due to autoreceptor block
4 - unlike atracurium it isnt hydrolysed and hence acts for longer.
5 - muscle relaxant in anaesthesia.
6 - effect reversed by AChE inhibitor
7 - reduced risk of severe respiratory depression.

51
Q

Phenoxybenzamine

A

1 - irreversible α blocker.
2 - blocks ENT transporter of uptake 2. also blocks uptake 1 when at 10 times higher concs.
3 - its a 2-chloroethylamine like BCM.

52
Q

Phentolamine

A

1 - non selective α anatagonist

2 - largely obsolete as antihypertensive due to reflex tachycardia and postural hypotension.

53
Q

Phenylephrine

A

1 - selective α1 agonist. used to raise ABP in acute hypotension

54
Q

Pilocarpine

A

1 - non selective MAChR agonist
2 - poorly absorbed from GI
3 - used to treat glaucome as eyedrops, readily absorbed across conjunctival membrane
4 - contracts ciliary membrane - traction on trabecular meshwork - facilitates aqueous humour drainage - lowers intraocular pressure.

55
Q

Pirenzepine

A

1 - selective M1 antagonist
2 - M1 coupled to Gq/11, found in peripheral and central neurons.
3 - antisecretory agent for gastroduodenal ulcers, thought to act on intramural nerves serving oxyntic cells.

56
Q

Pralidoxime

A

1 - can reverse organophosphate inhibition of AChE.
2 - its oxime group is a strong nucleophile, if in close proximity to the phosphorylated serine it’ll take the phosphate group.
3 - can only work within the first few hours before the complex undergoes ‘ageing’ and is no longer susceptible to nucleophilic attack.

57
Q

Prazosin

A

1 - selective α1 antagonist to treat hypertension
2 - causes postural hypotension
3 - α antagonists used to treat reynaud’s phenomenon and reduce the hypertension caused by a phaeochromocytoma.

58
Q

Propranolol

A 
1 - non selective β antagonist. replaced by atenolol.
2 - class 2 antidysrhythmic
3 - non-selective so can cause bronchoconstriction
4 - β1 is linked to Gs causing a rise of cAMP, increases likelihood of opening of L types and T types hence ionotrophic and chronotrophic.
59
Q

Reserpine

A

1 - blocks NA and DA transport into vesicle by tightly binding amine binding site of VMAT-2 (vesicular monoamine transporter). also causes long term NA (and 5HT in brain) depletion as they leak out of vesicles and are metabolised by MAO.
2 - acts in periphery and brain.
3 - used as antihypertensive but discontinued due to profound psychological depression
4 - recovery requires synthesis of new vesicles

60
Q

salbutamol

A

1 - short acting β2 agonist used to bronchodilate in asthma.
2 - replaced the non selective isoprenaline
3 - Salmeterol is a long-acting β2 agonist prescribed for the treatment of asthma and COPD

61
Q

Selegiline

A

1 - MAO-B inhibitor. MAO-B metabolises DA so inhibitor used in Parkinson’s.

62
Q

Sildenafil

A

1 - selective inhibitor of PDE5 which selectively breaks down cGMP. PKG activated by cGMP and causes S.M. relaxation inc in vessels.
2 - used to treat impotence.

63
Q

Suxamethonium

A

1 - NMJ NAChR agonist, causes depolarising block. the only one in clinical use.
2 - v.short duration of action so used for short procedures ie intubation
3 - an ester so rapidly metabolised by plasma BuChE.
4 - 0.1-0.2% of pop has BuChE deficiency causing prolonged action

64
Q

Tetanus toxin

A

Degrades Synaptobrevin. Retrograde transport up the motor neuron, trasferred to an inhibitory interneuron where it acts, hence causing motoneuron hyperexcitability.
prevents NeuroT release.

65
Q

Tranylcypromine

A

1 - non selective reversible inhibitor of MAO,used to treat refractory depression

66
Q

Trimetaphan

A

1 - Blocks ganglionic NACHR.

2 - Competitive antagonist

67
Q

Tyramine

A

1 - found in many foodstuffs
2 - indirectly acting sympathomimetic amine
3 - displaces NA from vesicles, some metabolised but some reaches adrenoceptors
4 - taken up via NET uptake 1
5 - large ingestion causes NA out, widespread vasoconstriction and ABP rise which can be fatal. the cheese effect. those taking MAOI are vulnerable

68
Q

Vesamicol

A

1 - inhibits the transport of acetylcholine into synaptic vesicles in cholinergic nerve terminals. non competitive and reversible.

69
Q

Xylazine

A

1 - more selective version of clonidine

2 - vet med for sedation via CNS α2

70
Q

Yohimbine

A

1 - α antagonist. α2 > α1

MODA drugs list (5 decks)

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