MODA Drugs (2)

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Author:
yl456
ID:
180174
Filename:
MODA Drugs (2)
Updated:
2013-03-26 12:27:19
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Peripheral Neural Transmission
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Mechanism and Effect
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  1. Botulinum Toxin
    • Bind to SNAREs on cholinergic neurons
    • Blocks ACh release
    • Loss of cholinergic activity
    • Muscle weakness
  2. Tetanus Toxin
    • Binds to SNAREs
    • Retrogradely transported to cell body and transfers to an inhibitory interneuron
    • Motor neuron becomes more excitable
  3. Hemicholinium
    Blocks uptake of choline by nerve cell
  4. Vesamicol
    Blocks transporter that carries newly synthesised ACh into storage vesicles
  5. β-bungarotoxin
    • Blocks ACh release
    • Acts through a phospholipase A2
    • Localises to the membrane by a K+ channel-binding moiety
    • May lead to respiratory failure
  6. α-latrotoxin
    • Venom from black widow spider
    • Binds to neurexins and causes massive release of ACh
    • May lead to respiratory failure
  7. Hexamethonium
    • Ganglionic blocker
    • Causes use dependent blockade of ganglionic transmission
    • Loss of sympathetic control and parasympathetic responses
    • Used for hypertension
  8. d-tubocurarine
    • Nicotinic receptor agonist
    • Non-selective between n.m.j and ganglion
  9. Pancuronium
    • Competitive antagonists of nicotinic receptor at n.m.j
    • Quarternary ammonium compounds- not orally active
    • Block end-plate potential in response to stimulation
    • Antagonise effects of ACh
  10. Atracurium
    • Competitive antagonists of nicotinic receptor at n.m.j
    • Quarternary ammonium compounds- not orally active
    • Block end-plate potential in response to stimulation
    • Antagonise effects of ACh
  11. Suxamethonium
    • Block nicotonic receptor at n.m.j
    • Block transmission by causing prolonged depolarisation(only suxa in clinical use-short duration of action)
  12. Muscarine
    Muscarinic receptor agonist
  13. Metacholine
    • Non-selective muscarinic receptor agonist
    • Has two isomers
    • (+) is 200x more potent and is a substrate for AChE
  14. Bethanechol
    • Non-selective muscarinic receptor agonist
    • Poorly absorbed in GI tract
    • Use in bladder dysfunction
  15. Pilocarpine
    • Non-selective muscarinic receptor agonist
    • Poorly absorbed in GI tract
    • Used in treatment of glaucoma as eye drops
  16. Atropine
    Non-selective muscarinic receptor antagonist
  17. Benzilylcholine Mustard
    Non-selective muscarinic receptor antagonist
  18. Darifenacin
    • Selective muscarinic receptor antagonist
    • Acts on M3, Gq/11
    • Mediates bladder constriction
  19. Edrophonium
    Reversible, short ionic interaction with AChE
  20. Neostigmine
    • Forms weak covalent bond with AChE
    • Medium length, reversible
    • Carbamic acid ester of choline
    • Used intravenously to reverse neuromuscular blockade
    • Used orally to treat myasthenia gravis
  21. Dyflos
    • Forms irreversible strong covalent bond with AChE
    • Long
  22. Malathion
    • Form irreversible strong covalent bond with AChE
    • Long
  23. Pralidoxime
    • Reverses inhibition by organophosphorous agents
    • Transfers phophate group to reactivator
  24. Carbidopa
    • Inhibits DOPA decarboxylase (only peripherally)
    • Used in treatment of Parkinson's
  25. Disulfiram
    • Used in treatment of alcohol abuse
    • Used experimentally to inhibit DBH
    • Chelates Cu2+ ion essential for function of DBH
  26. Methyldopa
    • α2-adrenergic agonist
    • Used to treat hypertension
    • Taken into noradrenergic nerve endings and converted into α-methyldopamine then α-methylnoradrenaline
  27. Reserpine
    • Discontinued antihypertensive
    • Binds to amine binding site of VMAT-2 transporter, blocking uptake of NA and DA
    • Acts in periphery and brain
  28. Tyramine
    • Indirectly acting sympathomimetic amine
    • Transported into nerve endings and storage vesicles to displace NA
    • Found in foodstuffs eg. cheese
  29. Dexamfetamine
    • Indirectly acting sympathomimetic amine
    • Weak inhibitor of MAO
    • Reduces packaging of amines
    • Weake base taken up by vesicle
  30. Guanethidine
    • Blocks release of NA
    • Taken up by uptake 1
    • Potentiates exogenously applied NA
    • Acts as indirectly acting sympathomimetic amine in large doses
  31. Cocaine
    • Re-uptake inhibitor for serotonin, norepinephrine and dopamine
    • Blocks NET
  32. Imipramine
    • Tricyclic antidepressant
    • Blocks NET
    • Block NA and 5-HT transport
  33. Amitryptyline
    • Tricyclic antidepressant
    • Blocks NET
    • Block NA and 5-HT transport
  34. Clorgiline
    Selectively inhibits MAO-A
  35. Selegiline
    • Selectively inhibits MAO-B
    • Used in treatment of Parkinson's
  36. Tranylcypromine
    • Non-selective irreversible inhibitor of MAO
    • Used in treatment of refractory depression
  37. Entacapone
    • Inhibitor of COMT
    • Used in Parkinson's
  38. Phenylephrine
    • Selective α1-receptor agonist
    • Used to raise blood pressure in acute hypotension
  39. Clonidine
    • Selective α2-receptor agonist
    • Anti-hypertensive agent
  40. Xylazine
    • More selective α2-receptor agonist
    • Veterinary medicine for sedative effects in CNS
  41. Isoprenaline
    • β-receptor agonist
    • Used in asthma to relax bronchioles via β2
    • Side effect of increasing heart rate via β1
  42. Salbutamol
    • Selective β2-receptor agonist
    • Used in asthma to relax bronchioles
  43. Dobutamine
    • Selective β1-receptor agonist
    • Used in acute cardiogenic shock
  44. Prazosin
    • Selective α1-receptor antagonist
    • Used in hypertension
  45. Phentolamine
    • Non-selective α-receptor antagonist
    • Brings about large increase in heart rate
  46. Atenolol
    • β1-blocker
    • Used in combination with phenoxybenzamine to prevent effects of catecholamine release when tumour is displaced in surgery
  47. Labetalol
    • Combined α- and β-adrenoceptor blocker
    • Four isomers with different actions:
    • R,R= β-blocker, weak α1-blocker
    • S,R= α1-blocker, very weak β-blocker
    • R,S= No effect
    • S,S= α1-blocker
  48. Propranolol
    • Non-selective β-blocker
    • Treatment of hypertension
  49. Ergotamine
    • Partial α-receptor agonist
    • Used for migraines (involves 5-HT receptors)
  50. Caffeine
    • A1 receptor antagonist
    • Waking action after prolonged wakefulness
    • Inhibits phosphodiesterase, increasing rate and force of cardiac contraction
  51. Dipyridamole
    • Potentiates response mediated by adenosine
    • Blocks inactivation of adenosine transport
  52. Glyceryl Trinitrate
    • Nitrovasodilator
    • Used to treat angina
  53. Sildenafil
    • Selective inhibitor phosphodiesterase type 5
    • Used to treat impotence
  54. L-NMMA
    • NOS inhibitor
    • Not very selective
  55. 7-NI
    Selective NOS inhibitor in neurons
  56. Butoxamine
    • β2-selective beta blocker
    • Experimental situations
  57. Idazoxan
    • Selective α2-receptor antagonist
    • Experimental
  58. Mecamylamine
    • Nicotinic Ach receptor antagonist
    • Non-selective
  59. Nicotine
    Nicotinic Ach receptor agonist

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