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Drugs acting on ion channel

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pharmacology Mind Map on Drugs acting on ion channel, created by Ha Mi Vu on 05/12/2016.
Ha Mi Vu
Mind Map by Ha Mi Vu, updated more than 1 year ago
Ha Mi Vu
Created by Ha Mi Vu about 8 years ago
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Drugs acting on ion channel
  1. Importance of ion channels
    1. Neuronal excitability - action potential neurotransmitters
      1. coupling contraction- muscle (NMJ)
        1. control the volume - prevent from swelling
          1. Mutation in channels can lead to channelopathies - LQ syndrome
            1. animal venom - blocking neurotoxin
              1. dendrotoxin
                1. W-agatoxin IV and W-agatoxin IIIA
                  1. apamin
                    1. Puffer fish has TTX in the intestines
                  2. Mechanisms of ion channel modulation - TTX
                    1. sy,mbiotic organism
                      1. Block Na Channel
                        1. Na channel mechanism
                          2. Guanidium moiety
                            1. Puffer fish has Glutamate on 387 - does not get affected
                              1. cardiac Na channel
                                1. 385, (cys) 387(glutamine), 388 (Arg)
                              2. Local Anesthetics
                                1. Two groups - aromatic ring + ester(procaine)/amide (lidocaine)
                                  1. Hydrophilic pathway
                                    1. LA block when Na channel is open
                                    2. Hydrophobic pathway
                                      1. LA enters when channel inactivated
                                        1. pore portals
                                        2. Unwanted effects
                                          1. CNS
                                            1. cardiovascular
                                            2. Binds to F1759 ub Nav1.5
                                              1. physical block
                                                1. electrostatic repulsion
                                              2. Other drugs acting on channel
                                                1. Anticonvulsants - carbazepine
                                                  1. Class I antidyshythmic drugs
                                                    1. Dihydropyrifine - Ca antagonist
                                                      1. Tolbutamine - BK channel
                                                        1. isoflurane - two K pore domain

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